Title of Invention

NOVEL DIAZABICYCLONONENE DERIVATIVES

Abstract The invention relates to novel 3,9-diazabicyclo[3.3.1]nonene derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors or renin.
Full Text

The invention relates to novel Diazabicyclononene Derivates. The invention ako consfflBE related adjects iocludmg processes foi the prepazation of the compounds, pharmaceutical conqjositioiis containing one or more compounds of fiinnula I and especially their use as renin inhibitors in cardiovascular events and renal insufSciency. Fuithamore, these compounds can be regarded as inhibitors of other aspart^ proteases and might thcrefoie be useful as iohibitois of plasmepsins to treat malaria and as inhibitors of Candida albicans secreted aspartyl proteases to treat Amgal tnfsctioQS.
bi the tenia-angiotensin syst^u (ElAS) the biologically active angiotersin 11 (Aug D) is generated by a two-stfip mechanism. The highly specific enzyme renin cleaves angiotensinogen to aDgioteasin I (Aug I), which is then further processed to Ang H by the less specific angiotensia-converting enzyme (ACE). Ang n is known to woA on at least two receptor subtypes called ATi and ATl- Wherras ATi seems to transmit most of the Icnowii fimctions of Ang H, ihe role of AT2 is still onknown.
Modulaition of the BAS le^trraents a n^oi advaiu^ in the tieatment of cardiovascular diseases. ACE inhibitors and ATi blockers have been accepted to treat hypertmsion (Waeber B. et al., "The renin-angiotensin system: role in expoimfflital and human hyperteosion", in Bedcenhager W. H., Rdd J. t. (eds): Ifypertension, Amsterdam, Elsevier Science Publishing Co, 1996, 489-519; Weber M. A,» Am. J. Hypertens., 1992, i, 247S). hi addition, ACE inhibitors are used for renal protection (Rosenberg M. E. et al. Kidney International, 1994, 45, 403; Breyer J. A. et al., Kidney International, 1994, 45, S156), in the prcvration of congestive heart feilure (VaughanD. E. et al, Cardiovasc. Res., 1994, 28,159;

Fouad-Tarazi F. et ai. Am. J. Med., 1988, 84 (Suppl. 3A), 83) and myocardial infarction (Pfeffer M. A. et al, N. Engl J. Med., 1992, 327, 669).
The rationale to develop renin inhibitors is the specificity of renin (Kleinert H. D., Cardiovasc. Drugs, 1995, 9, 645). The only substrate known for renin is angiotensinogen, which can only be processed (under physiological conditions) by renin. In contrast, ACE can also cleave bradykinin besides Ang I and can be by¬passed by chymase, a serine protease (Husain A., J. Hypertens., 1993, U, 1155). In patients inhibition of ACE thus leads to bradykinin accumulation causing cough (5-20%) and potentially life-threatening angioneurotic edema (0.1-0.2%) (IsraiU Z. H. et ai. Annals of Internal Medicine, 1992, II7, 234). Chymase is not inhibited by ACE inhibitors. Therefore, the formation of Ang II is still possible in patients treated with ACE inhibitors. Blockade of the ATi receptor (e.g. by losartan) on the other hand overexposes other AT-receptor subtypes to Ang II, whose concentration is dramatically increased by the blockade of AT] receptors. This may raise serious questions regarding the safety and efficacy profile of ATi receptor antagonists. In summary, renin inhibitors are not only expected to be different from ACE inhibhora and ATi blockers with regard to safety, but more importantly also with regard to their efficacy to block the RAS.
Only limited clinical experience (Azizi M. et al, J. Hypertens., 1994, 12, 419; Neutel J. M. et al. Am. Heart, 1991, 122, 1094) has been created with renin inhibitors because of their insufEcient oral activity due to their peptidomimetic character (Kleinert H. D., Cardiovasc, Drugs, 1995, 9, 645). The clinical development of several compounds has been stopped because of this problem together with the high cost of goods. Only one compound containing four chiral centers has entered clinical trials (Rahuel J. et ai, Chem. Biol, 2000, 7, 493; Mealy N. E., Drugs of the Future, 2001, 26, 1139). Thus, metabolically stable, orally bioavailable and sufficiently soluble renin inhibitors that can be prepared on a large scale are missing and sought. Recently, the first non-peptide renin inhibitors were described which show high in vitro activity (Oefiier C. et ah, Chem. Biol, 1999, 6, 127; Patent Application "WO97/09311; Marki H. P. et al, H

Farmaco, 2001,56^ 21). However, the development status of these compounds is not known.
The present invention relates to the identification of renin inhibitors of a non-peptidic nature and of low molecular weight. Orally active renin inhibitors of long duration of action which are active in indications beyond blood pressure regulation where the tissulai renin-chymase system may be activated leading to pathophysiologically altered local functions such as renal, cardiac and vascular remodeling, atherosclerosis, and possibly restenosis are described.
The present invention describes non-peptidic renin inhibitors.
In particular, the present invention relates to novel compounds of the general formula I,


A and B independently represent -0-; -S-; -SO-; -SO2-;
U represents aryl; heteroaryl;
T represents -COlSfR^-; -{CH2)pOC0-; -(CH2)pN(R^)C0-; -(CH3)pN(R')S02-; or -C00-;
Q represents lower alkylene; lower alkenylene;
M represents hydrogen; cycloalkyi; aryl; heterocyclyl; heteroaryl;
L represents -R^ -COR^ -COOR^; -CONR^R^; -S02R^ -S02NR^R^ -C0CH(Aryl)2;
R' represents hydrogen; lower alkyl; tower alkenyl; lower alkinyl; cycloalkyi; aryl; cycloalkyi - lower alkyl;
R^ and R^' independently represent hydrogen; lower alkyl; lower alkenyl;
cycloalkyi; cycloalkyi - lower alkyl;
R"' represents hydrogen; lower alkyl; lower alkenyl; cycloalkyi; aryl; heteroaryl; heterocyclyl; cycloalkyi - lower alkyl; aryl - lower alkyl; heteroaryl - lower alkyl; heterocyclyl - lower allo'I; aryloxy - lower alkyl; heteroaryloxy - lower alkyl, whereby these groups may be unsubstituted or mono-, di- or trisubstituted with hydroxy, -OCOR^ -COOR^ lower alkoxy, cyano, -CONR^R^', CO-mDrphoUii-4-yl, CO-((4-loweralkyl)piperazin-l-yl), -NH(NH)NH^ -NRV' or lower alkyl, with the proviso that a carbon atom is attached at the most to one heteroatom in case this carbon atom is sp3-hybridized;
R^ and R"*' independently represent hydrogen; lower alkyl; cycloalkyi; cycloalkyi -lower alkyl; hydroxy - lower alkyl; -COOR^; -CONH2;

m and n represent the integer 0 or 1, with the proviso that in case m represents the integer 1, n is the integer 0, and in case n represents the integer 1, m is the integer 0;
p is the integer 1, 2, 3 or 4; ris the integer 3,4, 5, or 6; s is the integer 2, 3, 4, or 5; t is the integer 1, 2, 3, or 4; u is the integer 1, 2, or 3; V is the integer 2, 3, or 4;
and optically pure enantiomers, mixtures of enantiomers such as racemates, diastereomers, mixtures of diastereomers, diastereomeric racemates, mixtures of diastereomenc racemates, and the meso-form; as well as pharmaceutically acceptable salts, solvent complexes and morphological forms.
In the definitions of general formula I - if not otherwise stated - the term lower alkyl, alone or in combination with other groups, means saturated, straight and branched cham groups with one to seven carbon atoms, preferably one to four carbon atoms that can be optionally substituted by halogens. Examples of lower alkyl groups are methyl, ethyl, n-propyi, iso-propyl, n-butyl, iso-butyl, sec-butyl, tert-butyl, pentyl, liexyl and heptyl. The methyl, ethyl nad isopropyl groups are preferred.
The term lower alkoxy refers to a R-0 group, wherein R is a lower alkyl. Examples of lower alkoxy groups are methoxy, ethoxy, propoxy, iso-propoxy, iso-butoxy, sec-butoxy and tert-butoxy.
The term \ower alkenyl, alone or in combination with other groups, means straight and branched chain groups comprismg an olefinic bond and consisting of two to seven carbon atoms, preferably two to four carbon atoms, that can be

optionally substituted by halogens. Examples of lower alkenyl are vinyl, propenyl or butenyl.
The term lower alkinyl, alone or in combination with other groups, means straight and branched chain groups comprising a triple bond and consisting of two to seven carbon atoms, preferably two to four carbon atoms, that can be optionally substituted by halogens. Examples of lower alkinyl are ethinyl, propinyl or butinyl.
The term lower alkylene, alone or in combination with other groups, means straight and branched divalent chain groups with one to seven carbon atoms, preferably one to four carbon atoms, that can be optionally substituted by halogens. Examples of lower alkylene are ethylene, propylene orbutylene.
The term lower alkenylene, alone or in combination with other groups, means straight and branched divalent chain groups comprising an olefinic bond and consisting of two to seven carbon atoms, preferably two to four carbon atoms, that can be optionally substituted by halogens. Examples of lower alkenylene are vinylene, propenylene and butenylene.
The term lower alkylenedioxy, refers to a lower alkylene substituted at each end by an oxygen atom. Examples of lower alkylenedioxy groups are preferably methylenedioxy and ethylenedioxy.
The term lower alhylenoxy refers to a lower alkylene substituted at one end by an oxygen atom. Examples of lower alkylenoxy groups are preferably methylenoxy, ethyienoxy and propylenoxy.
The term halogen means fluorine, chlorine, bromine or iodine, preferably fluorine, chlorine and bromine.

The term cycloalkyl alone or in combination, means a saturated cyclic hydrocarbon ring system with 3 to 7 carbon atoms, e.g. cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, which can be optionally mono- or multisubstituted by lower alkyl, lower allcenyl, lower alkenylene, lower alkoxy, lower allcylenoxy, lower alkyleaedioxy, hydroxy, halogen, 'CF3, -NR'R', -NR^C(0)R', -NR'S(02)R1', -C(0)NR'R', lower alkylcarbonyl, -COOR', -SR\ -SOR', -S02R\ 'SO^NR'R^' whereby R' represents hydrogen; lower alkyl; lower alkenyl; lower alkinyl; cycloalkyl; aryl; cycloalkyl - lower alkyl. The cyclopropyl group is a preferred group.
The term aryl, alone or in combination, relates to the phenyl, the naphthyl or the indanyi group, preferably the phenyl group, which can be optionally mono- or multisubstituted by lower alkyl, lower aikenyl, lower alkinyl, lower alkenylene or lower alkylene forming with the aryl ring a five- or six-membered ring, lower alkoxy, lower alkylenedioxy, lower alkylenoxy, hydroxy, hydroxy-Iower alkyl, halogen, cyano, -CF3, -OCF3, -NR'R', -NR'R^' - lower alkyl, -NR'C(0)R', -NRIS(02)R', -C(0)NR'R', -NO2, lower alkylcarbonyl, -COOR', -SR', -SOR', -SO2R', -S03NR'R', benzyloxy, whereby R' has the meaning given above. Prefen"ed substituents are halogen, lower alkoxy, lower alkyl, CF3, OCF3.
The tenn aryloxy refers to an Ar-0 group, wherein Ar is an aryl. An example of 1 lower aryloxy group is phenoxy.
rhe term heterocyclyl, alone or in combination, means saturated or unsaturated but not aromatic) five-, six- or seven-membered rings containing one or two litrogeu, oxygen or sulfiir atoms which may be the same or different and which ings can be optionally substituted with lower alkyl, hydroxy, lower alkoxy and lalogen. The nitrogen atoms, if present, can be substituted by a -COOR^ group, '.samples of such rings are piperidinyl, morpholinyl, thiomorpholinyl, iperazinyl, tetrahydropyranyl, dihydropyranyl, 1,4-dioxanyl, pyrrolidinyl, itrahydro&ranyl, dihydropyrrolyl, iraidazolidinyl, dihydropyrazolyl, yrazolidinyl, dihydroquinolinyl, tetrahydioquinolinyl, tetrahydroisoquinolinyl.

The term heteroaryl, alone or in combination, means six-membered aromatic rings containing one to four nitrogen atoms; benzofused six-membered aromatic rings containing one to three nitrogen atoms; five-membered aromatic rings containing one oxygen, one nitrogen oi one snifiiT atom; benzoftised five-membered aromatic rings containing one oxygen, one nitrogen or one sulfur atom; five-membered aromatic rings containing one oxygen and one nitrogen atom and benzoftised derivatives thereof; five-membered aromatic rings containing a sulfiir and a nitrogen or an oxygen atom and benzofiised derivatives thereof; five-membered aromatic rings containing two nitrogen atoms and benzofiised derivatives thereof; five-membered aromatic rings containing three nitrogen atoms and benzofused derivatives thereof, or a tetrazolyl ring. Examples of such ring systems are furanyl, thiophenyl, pyrrolyl, pyridinyl, pyrimidinyl, indolyl, quinolinyl, isoquinolinyl, iniidazolyl, triazmyl, thiazinyl, thiazolyl, isothiazolyl, pyridazinyl, pyrazolyl, oxazolyl, isoxazolyl, coumarinyl, benzothiophenyl, quinazolinyi, quinoxalinyl. Such rings may be adequatly substituted with lower aikyi, lower alkenyl, lower alkinyl, lower alkylene, lower alkenylene, lower alkylenedioxy, lower alkyleaeoxy, hydroxy-lower alkyl, lower alkoxy, hydroxy, halogen, cyaao, -CFj, -OCF3, -NR^R*', -NR^R*' - lower alkyl, -N(R')C0R\ -N(R')S02R', -CONR'R', -NO2, lower alkylcarbonyl, -COOR', -SR', -SOR', -SChR", -SOINR'R', another aryl, another heteroaryl or another heterocyclyl and the like, whereby R' ' has the meaning given above.
The term heteroaryloxy refers to a Het-O group, wherein Het is a heteroaryl.
The term sp3-hybridi2ed refers to a carbom atom and means that this carbon atom forms four bonds to four substituents placed in a tetragonal fashion around this carbon atom.
The expression pharmaceutically acceptable salts encompasses either salts with inorganic acids or organic acids hke hydrochloric or hydrobromic acid, sulfuric acid, phosphoric acid, citric acid, formic acid, acetic acid, maleic acid, tartaric

acid, benzoic acid, metlianesulfonic acid, p-toluenesulfooic acid, and the like that are non toxic to living organisms or in case the compound of formula I is acidic in nature with an ioiorganic base like an alkali or earth alkali base, e.g. sodium hydroxide, potassium hydroxide, calcium hydroxide and the like.
The compounds of the genera! formula I can contain two or more asymmetric carbon atoms and may be prepared in form of optically pure enantiomers, mixtures of enantiomers such as racemates, diastereomers, mixtures of diastereomers, diastereomeric racemates, mixtures of diastereomeric racemates, and the meso-form and pharraaceutically acceptable salts fherof The present invention encompasses all these forms. Mixtures may be separated in a manner known per se, i.e. by column chromatography, thin layer chromatography, HPLC or crystaihzation.
A group of preferred compounds are compounds of general formula I wherein X, W, V, U, T, Q, L, and M are as defined in general formula I above and wherein
n is 0 and
m is 1.
Another group of preferred compounds of general formula I are those wherein X, W, V, U, T, Q, M, m, and n are as defined in general formula \ above and
L represents H; -COR^"; -COOR^"; -CONR^"R^";
whereby R^" and R " represent independently lower alkyl, lower cycloalkyl -lower alkyl, winch lower alkyl and lower cycloalkyl - lower alkyl groups are unsubstituted or monosubstituted with halogen, cyano, hydroxy, -OCOCH3, -CONH2, -COOH, -NH2, with the proviso that a carbon atom is attached at the most to one heteroatom in case this carbon atom is sp3-hybridized.

Another group of preferred compounds of general fonnula I above are those wherem X, W, V, U, L, m, and n are as defined in general formula I and
Tis-CO^fR';
Q is methylene;
M is hydrogen; aryl; or heteroaryl.
Another group of even more preferred compounds of general formula I are those wherein X, W, U, L, T, Q, M, m, and n are as defined in general formula I above and
V is -CH2CH2O-; -CH2CH2CH2O-; -OCH2CH2O-; - -.
Another group of also more preferred compounds of general formula I are those wherein V, V, T, Q, M, L, m, and n are as defined in general formula I above and
X and W represent -CH-.
Another group of also more preferred compounds of general formula I are those wherein X, W, V, Q, T, M, L, m, and n are as defined in general formula I above and
U is a mono-, di-, or trisubstituted phenyl wherein the substituents are halogen; lower alkyl or lower alkoxy.
Especially preferred compounds of general formula I are those selected from the group consisting of:
(rac.yOR* 5^*)-3-acetyl-7-{4-[2-{2,3-dichlorophenoxy)ethyl]phenyI}-3,9-di' azabicyclo[3,3.1]non-6-ene-6-carboxybc acid methylphenethylamide;

(rac.)-(JR*, ^"iS*)-3-acetyl-7-{4-[3-{2-chloro-5-methylphenoxy)propyI]phenyI}-3,9-diazabicyclo[3.3.]]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.)-(2-methoxyphenyI)acetic acid (/i?* 5^*)-3-acetyl-7--(4-[3-(2-chloro-5 phenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-yIniethyl ester;
(r 3 (rac. )-(2-methoxyptienyl)acetic acid {IR*, 5S*)-3-acetyl-7-{4-[3-(2-chlorO' phenoxy)propoxy]phenyl}-3,9-diazabicyclo[3.3,l]non-6-en-6-yIniethyl ester;
(rac.)-(IR*, 55'*)-3-acetyI-7-{4-[3-(2,4-dimethylphenQxy)propyl]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
{rac.)'(JR*. 56'*)-3-acetyl-7-{4-[3-(4-bromo-3-methylphenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3. l]non-6-ene-6-carboxyhc acid methylphenethylamide;
{rac.y(JR*. Ji'*)-3'acetyl-7-{4-[2-(2-acetylphenoxy)ethyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
{racHiR*, 55*)-3-acetyl-7-{4-[2-(2-ethylphenoxy)ethyl]pheayl}-3,9-dia2abi-cycIo[3.3.l]noii-6-ene-6-carboxylic acid methylphenethylamide;
(rac.)-(lR*, 55'*)-3-acetyI-7-{4'[2-(3,5-diclilorophenoxy)ethyl]phenyl)-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxyIic acid methylphenethylamide;
{rac.)'(]R*, 55*)-3-acetyl-7-{4-[3-(3,4-dich]orophenoxy)propyl]phenyl}-3,9-di-azabicycIo[3.3.1]non-6-ene-6-carboxyIic acid methylphenethylamide;
(rac.y{JR*. J5*)-3-acetyl-7-{4-[2-(2,4-dimethyIphenoxy)ethyl]phenyl}-3,9'di-azabJcyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;

(rac.)-(JR*, 5i?*)-3-acetyl-7-[4-(3-o-toiy3oxypropyl)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(rflc.)-(2-methoxypbenyl)acetic acid (ii?*, 55*)-3-acetyl-7-{6-[3-(2-methoxy-
benzyloxy)propoxy]pyridiii-3-yl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl
ester;
{rac.)-(IR*, 55'*)-3-acetyl-7-{4-[2-{2-chlorophenoxy)ethoxy]pbenyl}-3,9-dia2abi-cyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
{rac.)'{JR*. 55*)-3-AcetyI-7-[4-(2-/H-tolyloxyethyl)phenyO-3,9-diazabicyc]o-[3.3.1]non-6-ene-6-carfaoxylic acid methylphenethylamide;
{rac.)-{}R*. 5i5*)-3'acetyl-7-{4-[2-{3-methoxyphenoxy)ethyl]phenyl}-3,9-diaza-bicyclop.3.1]non-6-ene-6-carboxylic acid methylpbenethylamide;
{rac.y{lR*. 55*)-3-acetyl-7-{4-{;2-(2-chloro-3-trifluoromethyiphenoxy)ethyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carbQxylic acid methylphenethylainide;
irac.y(JR*. 5S*)-3-acetyl-7-{4-[2-(4-rert-butyl-2-methylphenoxy)ethyl]plienyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid methylphenethylamide;
(rac.)-(2-methoxyphenyl)acetic acid (IR*, 55*>3-acetyl-7-{4-[3-(2-bromophen-oxy)propyl]phenyI}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl ester;
(rac.y(lR*. J5*)-3-acetyl-7-{4-[3-(3-chlorophenoxy)propyl]phenyl}-3,9-dia2abi-
cyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
[rac.yUR*, J5*)-3-acetyl-7-{4-[3-(2-isopropylphenoxy)propyl]phenyI}-3,9-di-izabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;

(rac.y(]R*. J6'*)-3-acetyl--7-{4-[2'(3-bromophenoxy)ethyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.yilK*, J5*)-3-acetyl-7-{4-[3-(2-bromophenoxy)propyi]phenyl}-3,9-diazabi-cyclo[3.3.1]non--6-ene-6-carboKylic acid methylphenethylamide;
(rac. )-(2-methoxyphenyl)acetic acid (IR*, 55*)-3-acetyl-7-[4-(3'0-tolyIoxy-propyl)phenyI]-3,9-dia2abicyclo[3.3.1]noii-6-en-6-ylmethyl ester;
{rac.y(lR*, J5'*>3-acetyl-7-{4-[2-(3,4-dichlorophenoxy)ethyl]phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxyIic acid methylphenethylamide;
(rac.y(]R*, 55'*)-3-Acetyl-7-{4-[3-(2-ter?-butylphenoxy)propyl]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxyUc acid methylphenethylamide;
{rac.y{lR*. 5S*)-3-acetyl-7-(4-[2-(3-chloropheiioxy)ethyl]phenyI}-3,9-dia2abi-cyclo[3.3.l^iion-6-ene-6-Garboxylic acid methylphenethylamide;
{rac.y{lR*. 55*)-3-acetyl-7-{4-[3-(2-ethylphenoxy)propyl]phenyi}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.y(lR*, 5iy*)-3-acetyl-7-{4-[3-(2,3-dimethylphenoxy)propyl]phenyl}-3,9-di-azabicyclo[3.3.l]non-6-ene-6-carboxyUc acid methylphenethylamide;
(rflc.)-(ifi*. 55*)-3-acetyl-7-{4-[2-(3-trifluoromethoxypheDoxy)ethyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxyhc acid methylphenethylamide;
(raayilR*, 55*)-3-acetyl-7-{4-[3-(3,4-dimethylphenoxy)propyl]phenyl}-3,9-di-a2abicycIo[3.3.1]non-6-eoe-6-carboxyhc acid methylphenethylamide;
(rac.yiJR*. 55*)-3-acetyl-7-{4-[3-(2-chIoro-4,5-dimethylphenoxy)propyI]phe-nyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyiic acid methylphenethylamide;

{rac.)-{lR*. 5iS'*)-3-acetyl-7-{4'[2-(2-cMorophenyI}ethoxy]phenyl}-3,9-dia2abi-cyclo[3.3.1]non-6'ene-6-carboxylic acid methyiphenethylamide;
(rac.)-(2-methoxyphenyl)acetic acid (IR*. 55*;-3-[2-(4-chlorophenyl)ethyl]-7-{4-[3-(2-methoxybeiizyloxy)propoxy]phenyl}-3,9-diazabicycio[3.3.1]iion-6-en-6-yl methyl ester;
{rac.)-{IR*. JiS'*)-3-acetyl-7-{4-[3-(2-chloro-3-triiluoromethyIphenoxy)propyI]-phenyl}-3,9-diazabicycIop.3.I]non-6-ene-6-carboxylic acid methyiphenethyl¬amide;
(rac.)-(2-m6thoxyphenyl)acetic acid (IR*, 56'*>3-acetyl-7-{4-[2-(3-ch]oro-phenoxy)ethyl]phenyl}-3,9-dia2abicyclo[3,3.1]nQn-6-en-6-yhnethylester;
{rac.)-{}R*. 5S *)-3-acetyl-7-[4-{2-7«-tolyloxyethoxy)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxyhc acid methyiphenethylamide;
{rac.)-{lR*, 55*)-3-acetyl-7-{4-[3'(2,4-dichlorophenoxy}propyl]-phenyl}-3,9-di-azabicycIo[3.3.1]non-6-ene-6-carboxyhc acid methyiphenethylamide;
(rac.yilR*. 55'*)-3-acetyl-7-{4-[3-(2,5-dunethylphenoxy)propyl]phenyl}-3,9-di-azabicycIo[3.3.1]non-6-ene-6-carboxyiic acid methyiphenethylamide;
irac.y{lR*. 5S*)-3-acetyl-7-{4-[2-(3,5-dimethylpheiioxy)ethyl]phenyl)-3,9-di-azabicyclo[3.3.1]noD-6-ene-6-caiboxylic acid methyiphenethylamide;
(rac.yQR'*, 55*)-3-acetyl-7-{4-[2-(2-6thoxyplienoxy)ethyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxyHc acid methyiphenethylamide;
(rac.H2-methoxyph6nyl)acetic acid (IR*. 55*;-3-acetyl-7-{4-[3-(3-chlorophen-oxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en-6-ylmethyIester;

(rac.)-(7i?* 55*)-3-acetyl-7-{4-[3-(3,5-dimethyIphenoxy)propyl]pbenyl}-3,9-di-azabicyclo[3.3.1}non-6-ene-6-carboxylic acid methylphenethylamide;
{rac.)-{lR*. 5i'*)-3-acetyI-7-{4-[3-(2-fluQrophenoxy)propyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-cai"boxylic acid methylphenethylamide;
(rac.>(2--niethoxypheDyl)acetic acid {IR*, 5S*)-3-acetyl-7-{4-[2-(2-chlorophen-oxy}ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl ester;
{rac.)-{lR*. 55*)-3-acetyl-7-{4-[2-(2,5-dichiorophenoxy)ethyl]phenyl}-3,9-diaEa-bic.yGlo[3.3.1]noii-6-ene-6-carboxylic acid metbylphenethylamide;
{rac.)-(}R*. 55*)-3-acetyl-7-{4-[3-(2,3,5-trimethylphenoxy)propy]]-ph6nyI}-3,9-diazabicyclo[3,3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.yUR*. 55*)-3-acetyl-7-{4-[2-(3-chlorophenyl)ethoxy]phenyl}'3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
{rac.yOR*, J5*)-3-acetyl-7-{4-(:2-(2,3-diauQrophenoxy)ethyl]pheayl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
{rac:)-{lR*. 55*)-3-acetyI-7-{4-[2-{2-chloroph6noxy)ethyl]phenyl}-3,9-diazabi-cyclo[3.3.1]aon-6-ene-6-carboxyUc acid methylphenethylamide;
{rac.)-{lR*, J5*)-3-acetyl-7-{4-[2-(2,4-dichlorophenoxy)ethyl]phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(i-ac.)-(lR*. J^*)-3-acetyl-7-{4-[2-(2,3,6-trifIuorophenoxy)ethyl]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;

(?-ac.)-(2-methoxyphenyl)acetic acid (IR*, 5iS'*)-3-acetyl-7-{4-[3-(2-trifluoro-methylphenoxy)propyl]phenyI}-3,9-diazabicyclo[3.3,l]non-6-en-6-ylinethy] ester;
{rac.)-(IR*, 5.5*)-3-acetyl-7'{4-[2-(3-trifluoromethylphenoxy)ethyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide,
[rac.)-{}R*, 5S*)-3-acetyl-7-{443-(3,5-dichlorophenoxy)propyi]phenyl}-3,9-di-a2abicycio[3.3.1]non-6-ene-6-carboxyHc acid methylphenethylamide;
{rac.)-(IR*, J^*)-3-acetyl-7-(4-[3-(m-tolyloxy)propyl]phenyl}-3,9-diazabicyclo-[3.3. l]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.)-{lR*. 55*)-3-acetyl-7'{4-[2-(2-methoxyphenyl)ethoxy]phenyl}-3,9-diaza-bicyclo[3.3.1]n,on-6-ene-6-carboxylic acid methylphenethylamide;
(rac.yOR*, 55*)-3-acetyl-7-{4-[3-(4-fluorophenoxy)propyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxyhc acid methylphenethylamide;
{rac.y(JR*. J5*>3-acetyl-7-{4-[2-(3,4-dimethylphenoxy)ethyl]phenyl}-3,9-di-a2abicyclo[3.3.T,]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.)-(2-methoxyphenyl)acetic acid (JR*. 55*)-3-acetyl-7-{4-[3-(3-fluorophen-oxy)propyi]phenyl}-3,9-diazabicyclo[3.3.1]iion-6-en-6-ylmethyl ester;
{racy^lR*, JiS'*^-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid phenethylamide;
(rac.)-(2-mettioxyphenyl)acetic acid {IR*, 5S*)-3-acetyl-7-[4-(3-phenoxypropyl)-phenyl]-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl ester;
{rac,y{lR*, J5*)-3-acetyl-7-{4-[3-(2-acetyl-5-fluoropheaoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyhc acid methylphenethylamide;

5

(rac.yiJR*. J5*)-7-{4-[3-(2-methoxyben2yloxy)propoxy]phenyl}-6-[2-(2-me-thoxyphenyl)acetoxymethyl]-3,9-dia2abicyclo[3.3.I]non-6-ene-9-carboxy]ic acid 2,2,2-trichloro-l,l-dmietbylethyl ester;
(i-ac.)-(]R*, 55'*)-3'acetyI-7-{4-[3-(2-ch]oropheiioxy)propyl]piienyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;

(?-ac.y(JR*, 55*)-3-acetyl-7-{4-[3-(2,3-difluorophenoxy)propylJphenyi}-3,9-di-: azabicycIo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
{rac.y{lR*, 5S*)-3-acetyl-7-(4-[2-(2-ie)-i-butylpiienoxy)ethyl]phenyl>-3,9-[li^ a2ab!cyclo[3.3.1]non-6-ene-6-carboxyIic acid methylphenethylamide;
■ (rac.y(JR*, 55*)-3-acetyI-7'{4-[2-(2-propioQylphenoxy)ethyl]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
1:1 mixture of {2Ry and (2S)'N-({IR*, 55*)-3-acetyl-7-{4-[3-(2-methoxybenzyl-
oxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-yhnethyl)-A'-methyl-2-
phenylpropionamide;
(rac.)-(lR* 55*)-3-acetyl-7-{4-[3-(2-rerf-butyi-4-methylphenoxy)propyl]phe-nyl}-3,9- (rac.)-(]R*, 55*)'3-acetyl-7-{4-[3-(2-i'er^butyl-6-methylphenoxy)propyl]phe-nyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.)-(iR*, 5S*)-3-acetyl-7-(4-[3-(4-chloio-2-methoxyphe!ioxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.I]non-6-ene-6-carboxylic acid methylphenethylamide;
{rac.y(lR^ J5*)-3-acetyl-7-{4-[2-(2-raethoxy-5'methylphenoxy)ethyl]phenyl)-3,9-dia2abicyclo[3,3.1]non-6-ene-6-carboxyiic acid methylphenethylamide;

(rac.)-(IR*, J5*)-3-acetyl-7-(4-[3-(3-methoxyphenoxy)propyl]pheny]}-3,9-diaza-bicycIo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
{rac.)-{lR*, 5S*)-3-acetyl-7-(4-[3-(4-rert-butyl-2-methylphenoxy)propyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.)-(JR*, 55*)-3-acetyI-7-{4-[2-(3,5-dimethoxyphenoxy)6thyI]phenyI}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxyhc acid methylphenethylamide;
{rac.yiJR*, 5^*)-3-acetyl-7-{4-[2-(2-i5o-propyIphenoxy)ethyi]phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.)-(Jft*, 5S*)-3-acetyl-7-{4-[3-(2-metlioxybenzyloxy)pTopoxy]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid [2-(2-methoxyphenyI)ethyl]amide;
{rac.yilR*, J5*)-3-acetyl-7-{4-[3-(3-bromophenoxy)propyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.)-(2-methoxyphenyl)acetic acid (/iJ*, 5iS*)-3-acetyl-7-[4-(3-p-tolyloxypro-pyi)phenyl]-3,9-dia2abicyclo[3.3.1]non-6-en-6-ylmethylester;
(rac.)-acetic acid 2-((JR*, 5i5*)-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]methylcarbamoyI}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-2-oxoethyi ester;
(rac.yilR*. J5*)-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3-(2-cyanoacetyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid [2-(2-chlorophenyl)ethyl]-methylamide;

{}-ac.y{}R*. 55'*)-3~(2-acetylammoacetyl)-7-{4-[3-{2-chloropIienoxy)propyl]ptie-ttyl}-3,9-diazabicyclo[3.3.l]non-6-eiie-6-carboxylic acid [2-(2-chlorophenyl)-ethyljmethylamide;
1:1 mixture of (JR, 55)'3-((^ie)-2-acetylamino-4-methyIpeatanoyl)-7-{4"[3-(2-chlorophenoxy)propyl]phenyl)-3,9-diazabicycio[3.3.1]non-6-ene-6-carboxylic acid [2-(2-chloTophenyl)ettiyl]methylamide and (IS, 5i?)-3-((^i?)-2-acetyiamiiio-4-mediylpentanoyl)-7-{4-[3-(2-chlorophenoxy)propyI]phenyl}-3,9-diazabicyclo-[3.3. l]non-6-ene-6-carboxylic acid [2-(2-chloropheiiyl)ethyl]methy]amide;
(rac.y(lR*, 5iS'*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyI]phenyi}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxylicacid[2-(2-chlorophenyl)ethyl]meth.ylamide;
{rac.y(]R*. 55*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyi]phenyl}'3,9-diazabi-cyclo[3.3.1]non-6-ene'6-carboxylic acid (2-hydroxybenzyl)methylamide;
1:1 mixture of {rac.yiJR", 5,S'*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]-pheayl)-3,9'diazabicyclo[3.3.1]non-6-ene-6-caTboxylic acid [(3i?*)-3-(2-chloro-phenyl)butyl]methylamide and (racyilR*, ^5*)-3-acetyl-7-{4-[3-(2-chlorophen-oxy)propyIjphenyI}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxyUc acid [(5iS'*)-3-(2-chloropli6nyi)butyl]methylamide;
[rac.y{lR*, 5S*)-3-acetyl-7-{4-[3-(2-chloiophenoxy)pTopyl]phenyl}-3,9-diazabi-cycIo[3.3.l]non-6-ene-6-carboxylie acid methyI-(4-phenylbutyl)airude;
(rflc.)-(;i?* J^*)'3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carbosylic acidmethyl-(3-phenoxypropyI)anude;
{rac.y(lR*. i5'*)-3-acetyl-7-(4-[3-(2-chloropheiioxy)pcopyl]pbenyl}-3.9-diazabi-cycIo[3.3. l]non-6-ene-6-carboxylic acid methyI-(4-phenylpeiityI)ainide;

{rac.)'{lR*. J5*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxyiic acid (3-benzo[l,3]dioxol-5-ylpropyl)methyl-amide;
{rac.)-{lR*. J>y*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxylic acid [2-(4-meth,oxypiienoxy)ethyl]methyI-amide;
(rac.)-{JR*, 5>S'*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-dia2abi-cycIo[3.3.]]noii-6-ene-6-carboxyIic acid [2-(4-chloropheBOXy)ethyl]methylamide;
{rac.)-{]R*. 55*)-3-acetyI-7-{4-[3-(2-chloTophenoxy)propyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxylic acidmethyl-(2-/)-tolyloxyet±iyI)ainide;
(rac.yiJR*, 55*)-3-acetyI-7-{4-[3-(2-chlorophenoxy)propyl]phenyi}-3,9-dia2abi-cyclo[3.3.1]non-6-ene-6-carboxylic acid diethylamide;
(rac.)-(lR*, 5iy*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxylic acidmethyl-(2-pyridin-2-ylethyl)amide;
{rac. )-(IR *. J5*)-3-acetyI-7- {4-[3-(2-bromo-5-fluorophenoxy)ethyl]phenyl} -3,9-diazabicyclo[3.3.1Jnon-6-ene-6-carboxylic acid (2-chlorobenzyl)cycIopropyl-amide;
{rac.yQR*. 55*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyI]phenyI}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)cycIopropylainide;
{rac.)-{lR', 55*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diaza-bicyclo[3.3. l]non-6-ene-6-carboxylic acid [2-(4-methoxyphenoxy)ethyI]methyl-amide;

(mc.)-{]R*. J.S'*>3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diaza-bicyclo[3.3.1]non'6-ene-6-carboxylic acid methyl-(3-trif]uoromethylben2yl)' amide;
(rac.)-(i-R*, 55*)-3-acetyl-7-{4-[3-(2-chiorophenoxy)propyl]phenyl}-3,9-dia2a-bicyclo[3.3. l]non-6-ene-6-carboxy!ic acid [2-(3,4-dimethylphenoxy)ethyl]methyl-amide;
{raa)-{IR*, J5*)-3-acetyl-7-(4-[3-(2-ctLlQrophe!iQxy)propyl]plienyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid (3,5-dimethoxybenzyI)methyIaimde;
(rac.y(]R*, J5*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-dia2a-bicyclo[3.3.1]non-6-ene-6-carboxylic acid(2-chIorobenzyl)methylamide;
(rac.)-(lJi *, J5*)-3-acetyI-7- {4-[2-(2-chloro-4,5-dimeIhylphenoxy)ethoxy]-
ph6nyl)-3,9-diazabicyclo[3.3.1]non-6-6ne-6-carboxylic acid methylphenethyl-amide;
(rac.)-{lR*, 5.S*)-3-acetyl~7-{4-[2-(3,4-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxyIic acid methylpbenethylamide;
(rac.)-(JR*, J5*)-3-acetyl-7-{4-[3-(2-chIorophenoxy)propyl]phenyl}-3,9'diaza-bicyclo[3.3.1]noii-6-ene-6-carboxyiic acid (2-chloroben2yl)ethylamide;
{racHJR*, 55'*)-3-acetyi-7'{4-[3-(2,3,6-trichIorophenoxy)ethyljphenyl}-3,9-diazabicyclo[3.3.1]noii-6-ene-6-carboxylicacidine1hylphenethyiaimde;
{rac.y{lR*, J5'*)-3-acetyl-7-{4-[3-(3-fluorophenoxy)propyl]phenyl}-3,9-diaza-bicyclo[3.3.1 ]non-6-ene-6-carboxylic acid (2-chlorobenzyl)cyclopropyI-ainide;
{rac.y{lR*, 5S*)-3-acstyI-7-{4-[3-(2-cMorophenoKy)propyl]phenyI}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)isopropylamide;

{rac.)-{lli*, 55*)-5-[7-{4-[2-(2-bromo-5-fluorophenoxy)etliyl]phenyU-6-(inethyl-phenethylcarbanioyl)-3,9-diazabicycio[3.3.1]non-6-en-3-yi]-2,2-dtmethyl-5-oxo-pentanoic acid;
{JS. 5S)-3-acetyl-7-{4-[2-{2,3,6-trifluorophenoxy)ethyl]phenyl}-3,9-diaza-
bicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
l:l-mixture of (rac.)-UR*, 5iS'*)-3-acetyl-7-(4-[3-(2-bromo-5-fluoropheaoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3J]non-6-ene-6-carboxylic acid cyclopropyl-[2-((2^*)-2,3-dihydroxypropyl)benzyl]amide and (rac.)-(JR*. 5iS'*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acidcyclopropyl-[2-((2iS*)-2,3-dihydroxypropyl)benzyl]ainide;
{rac.)-(JR*, 55*>3-acetyl-7-{4-[3-{2-bromo-5-fluorophenoxy)propyl]phenyI}-3,9-dia2abicyclo[3.3.1]non-6-eiie-6-caTboxylic acid cyciopropyl-[2-(2-hydroxy-ethyl)benzyl]ainide;
{rac.)'(lR*, 55*)-3-acetyl-7-(4-[3-(2-broino-5-fluorophenoxy)propyl]phenyI}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid benzylcyclopropylamide;
(rac.)-(lR*, JiS'*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-clilorobenzyl)ethylamide;
(rac.)-(lR*, 5iS*)-3-acety!-7-{4-[3-(2-bromo-5-fluoropheiioxy)propyl]ph6nyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-cariioxylic acid cyclopropyl-(2-fluoro-beazyl)amide;
(rac.)-(IR*. J5*)-3-acetyI-7-{4-[3-(2-bromo-5'fluorophenoxy)propyl]phenyl}-3,9-diazabicyc!o[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2-methyl-beiizyl)ainide;

(rac.)-(JR*, 55'*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3,3.1]non-6-ene-6-carboxyIic acid cyclopropyI-[2-(4-methoxy-phenoxy)etbyl] amide;
{rac.)-(JR*, 5i.S'*)-3-acetyI-7-{4-[3-(2-brorao-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3,3.1]non-6-ene-6-carboxy]ic acid cyclopropyl-(2-/?i-toiyloxy-ethyl)amidc;
(rac.yiJR*, i5*)-3-acetyl-7--{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyI}-3,9-diazabicycIo[3.3. l]non-6-ene-6-carboxylic acid cyclopropyl-[2-(3,4-diraethyl-pheiiQxy)etby[] amide;
(mc.)'(JR*. 5iS'*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propy!]pbenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropylphenethylamide;
{rac.)-{JR*, 5iS'*)-3-acetyI-7-{4-[3-(2-brorno-5-fluoTophenoxy)propyl]phenyI}-3,9-diazabicyclo[3.3. ] ]noa-6-ene-6-carboxyiic acid [2-(2-chlorophenyl)efliyl]-cyclopropylamide;
(rac.)-{]R*, 5iS*)-3-acetyl-7-{4'[3-(2-bromo-5-fluorophenoxy)propy]]phenyl}-3,9-dia2abicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-[2-(2,3-difluoro-pheayl)ethyl]amide;
(rac.y(IR*, J5*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}~ 3,9-diazabicyclo[3.3.1]noii-6-ene-6-carboxylic acid cyclopropyl-[2-(4-fluoro-phenyl)ethyl]amide;
(rac.y{JR*, J5*)-3-acetyl-7-{4-[3-(2-bromo-5-fluoropbenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]noa-6-ene-6-carboxylic acid cyclopropyl-(2-o-tolylethyl)-amide;

l;l-mixture of irac.)'{lR*, 55*)-3-acetyy-7-(4-[3-(2-bTomo-5-fluorophenoxy)-propyI]piienyl} -3,9-diazabicyclo [3.3.1 ]noii-6-ene-6-carboxylic acid ((2R *}-2-hydroxy-2-plienylethyl)methylamide and (rac.)-(JR*, J^*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid ((i5*)-2-hydroxy-2-phenylethyl)niethyIamide;
(rac.)-(]R'*, 5.V*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyc]o[3.3.I]non-6-ene-6-carboxylic acid cyclopropyH3-trifluoro-rnethylbeiizy])amide;
{rac.y{IR*, 5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxyUc acid cyclopropyi-(2-o-tolyletbyl)-amide;
{rac)-(]R*, J5*)-6-[(2-clilorobenzyl)ethylcari7amoylJ-7-{4-[3-(2,3,6-trifluoro-
p!ienoxy)propyl]phenyI} -3,9-diazabicyclo[3.3,1 ]non-6-eTie-9-carboxylic acid
2,2,2-trichloro-1,1 -dimethylethyl ester;
{rac.)-ilR*, 5i5*)-6-[{2-fluorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-
trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-diaiethylethyl ester;
(rac.)-(JR*, 5,y*)-6-[(2-methylbeiizyI)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-
trifluoro-pheiioxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-dimetiiylethyl ester;
{rac.)-{lR*, J5'*)-6-[cyclopropyl-(2-o-toIylethyl)carbamoyl]-7-{4-[3-{2,3,6-
trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid 2,2,2-trichIoro-l,l-dimethylethyl ester;

(rac.)-(JJi*. 55*)^6-[cyc!apropyl-(2-p-tolylethyI)Gai-ba!noyl]-7-{4-[3-(2,3,6-
trifluorophenoxy)piopyl]phenyl}-3,9-diazabicycio[3.3-l]noii-6-ene-9-caTboxyUc acid 2,2,2-trichloro-] ,1-dimethylethyl ester;
(rac.y{lR*, 5iS*)-6-[cyclopropyl-(3,5-diinethoxyben7yl)carbamoyl]-7-{4-[3-
{2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid 2,2,2-lTichloro-l,l-diinethylethyi ester;
(rac.y{JR*, 55*)-3-(4-carbamoylbulyryl)-7-{4-[3-(2,3,6-trifluorophenoxy}-
propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxyiic acid cyclopropyl-[ 2 -(4-methoxyphenoxy)etbyl]amide;
{rac.)-{}R*, J^*)-3-(4-carbamoyIbutyryI)-7-{4-[3'(2,3,6-trifluorophenoxy)-
propyI]phenyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxy[ic acid cyclopropyl-[2-(3 -methoxypheiioxy)ethyl]airade;
{rac.)-{lR*, 55*)-3-(4-carbainoylbutyry!)-7-{4-[3-(2,3,6-trifluoroph6noxy)-
propyl]pbeny]}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2-m-tolyloxyethyl)amide;
{rac.)-{lR*, 55'*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-
propyI]phenyl)-3,9-diazabicyclo[3.3.1]non-6-eiie-6-carboxyIic acid cyclopropyl-
[2-(3,4-dimet±LyIph6noxy)ethyl] amide;
{rac.)-{lR*, 55'*)-3-(4-carbamoylbutyryI)-7-{4-[3-(2,3,6-trifluorophenoxy)-
propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-[2-(2,3-difluorophenyl)ethyl] amide;
(rac.)-{lR*, 55*)-3-(4-carbamoyIbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-
propyI]ph.enyl}-3^9-diazabicycIo[3.3.llnon-6-ene-6-caTboxylic acid cyclopropyl-[2-(4-fluorophenyl)ethyl]amide;

(rac.)-{lR*, J5*)-3-(4-carbamoylbutyryl)-7-{4-[3-(23,6-trifluoTOplvenoxy)-
propyI]phenyl}-3,9-diazabicycIo[3.3.1]non-6-6ne-6-carboxylic acid cyclopropyl-(2-o-tolylethyl)araide;
{rac.)-{}R*, 55*)o-(4-carbainoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-
propyi]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid cyclopropyi-(2';?-tolyIethyl)amide;
l:l-mixture of (JR, 5S)-3-((}S, •/i;)-4-hydroxypynoIidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyi]phenyl}-3,9-diaz;abicyclo[3.3.1]iion-6-ene-6-carboxylic acid benzylcyclopropylamide and (JS, 5R)-3-{(JS, ■/fi)-4-hydroxypyrrolidiiie-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)pTopyI]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid benzylcyclopropylamide;
I:l-mixture of (IR, 5S)-3-i(JS, •/i?)-4-hydroxypyiToIidiiie-2-carbonyl>7-{4-[;3-{2,3,6-trifluorophenoxy)propylplienyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)ethylamide and (JS. 5Ry3-((JS, •?ie)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propylphenyl}-3,9-diazabicyclo[3.3,l]non-6-eiie-6-carboxylic acid (2-chlorobenzyl)ethylaniide;
l:l-mixture of (JR. 5S)-3-(i}S. '^ii)-4-iiydJ'oxypyrrolidine-2-carboayl)-7-{4-[3-
(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.I]non-6-ene-6-
carboxylic acid cyclopropyH2-fluoTobenzyl)aniide and (IS, JJ?)-3-((/S, 4R)A-
hydroxypyiTolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]pheayl}-
3,9-diazabicyclo-[3.3. l]non-6-ene-6-carboxylic acid cyclopropyl-(2'
fluorobenzyl)amide;
l:Uniixture of (IR, 5S)-3-({IS. '/i?)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3' (2,3,6-trifluorophenoxy)propyl]pbenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyI-(3-trifluoromethylben2yl)amide and (IS, JR)-3-((JS, '^i?)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-lrifluorophenoxy)propyl]-

phenyl}-3,9-diazabicyclo[3.3.l]non-6-ene-6-carboxyiic acid cyclopTopyl-(3-trifluoromethylbenzyl) ami de;
l:l-mixture of (JR. 5S)'3'{(]S. ^ie)-4-hydroxypyn-olidme-2-carbony!)-7-{4-[3-(2,3,6-trif!uorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2-metIiylbenzyl)amide and (IS, 5R)-3-((JS, '?S)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trif]uorophenoxy)propyl]phenyl}-3,9'diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2-methyl-enzyl)ainide;
l:l-mixture of (IR, 55)-3-((75, '/^)-4-hydroxypyrrolidine-2-carbonyI)-7-{443-{2,3,6-trifluorophenoxy)propyl]plienyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2-m-tolyloKyethyi)amide and (IS, 5R)-3'{(IR 4S-4-hydroxypyrro!idine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2-;«-tolyloxy-ethyl)amide;
l:l-mixture of (iR, 5S)'3-((JS. ■#fi)-4-hydroxypyrTolidine-2-carbonyI)-7-(4-[3-(2,3,6-trifluorophenoxy)pTopyI]phenyI}-3,9-diazabicyclo[3.3.1]noa-6-ene-6-carboxylic acid cyclQpropyl-(3,5-dimethoxybenzyI)amide and (IS, 5R)-3-{(lS, '^J?)-4-hydroxypyTrolidiiie-2-carbonyl)-7-{4-[3-(2,3,6-trifliiorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyHc acid cyclopropyl-(3,5-dimethoxybenzyl)amide;
l:l-mixture of (JR, 5S)-3-((]S. •#ii)-hydroxypyiToHdine-2-carbonyl>7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2-p-toIyletliyl)amide and (IS, 5R)-3'{(1S, 4R)' hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluoropIienoxy)propyljphenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyHc acid cydopropyl-(2-p-tolylethyl)-amide;

1:1-mixture of {rac.y{3R *)-S-{(lR *, 55*)-6- {cyclopropyl-[2-(3-methoxy-phenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trii]uorophenoxy}propyl]pheayl}-3,9-diazabicyclo[3.3.1]non--6-eii-3-yl)-3'hydroxy-5-oxopentanoic acid and (rac.)-(3S*)-5-(OR*, 5iS'*>6-{cyclopropyI-[2-(3-methoxyphenoxy)ethyl]c3rbamoyl}-7-(4-[3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of (rac.y(3R*)-5-{(JR*. J5*)-6-{cyclopropyl-[2-(3,4-dimethyi-phenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propy]]phenyl}-3,9-diazabicyGlo[3.3.1]nou-6-en-3-y!)-3-bydroxy-5-oxopentanoic acid and (rac.)-i3S*)-5-((IR*. 55*)-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyI]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yI)-3-hydroxy-5-oxopeDtanoic acid;
l:I-mixture of (rac.)-(3R*)-5-((]R*, 55*}-(6-(cycIopropylphenethyl-carbamoyl)-7-{4-[3-(2,3,6-trifluoropheiioxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.y(3S*)'5-((JR*, 55*)-5-(6-(cyclopropylpheneaiylcarbamoyl)-7-{4-[3-(2,3,6-trifluoroplienoxy)propyl]-phenyl}-3,9-diazabicyclo-[3.3.1]non-6-eu-3-yl)-3-h.ydroxy-5-oxopentanoic acid;
1:1-mixture of (rac. y(3R*y5-({}R * 5S*y6- {cyclopropyl-[2-(2,3-difluoro-phenyl)ethyl]carbamoyI}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-6n-3-yl)-3-iiydroxy-5-oxopefltanoic acid and (rac.y (3S*y5-((JR* J5*)-6-{cycloprQpyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifIuoropbeiioxy)propyI]phenyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
l;I-mixture of (racy(3R*y5-{(lR*, JS*)-6-{cyclopropyl-[2-(4-fluorophenyl)-ethyl]carbamoyl}-7-{4-[3-(2,3,6-rtiifluorophenoxy)propyl]phenyl}-3,9-dia2a-bicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.y(3S*y5-{{IR* 55*)-6-{cyclopropyH2-(4-fluorophenyl)ethyi]carbamoyl)-7-{4-[3-(2,3,6-

triflnorophcnoxy)propyl]phenyl}-3,9-diazabicyclo[3.3,l]non-6-en-3-yl)-3-hydroxy-5-QXopen.tanoic acid;
l:]-mixture of (rac.)-(3-ff*)-5-((//e* 55*)-6-[cyc!opropyl-(2-D-tolyl ethyl)-
carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicycIo-
[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.)-{3S*y5-((]R*,
.5S*)-6-[cyclopropyl-(2-o-tolyiethyi)carbamoyl]-7-{4-[3"(2,3,6-trifluorophenoxy)-
propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yI)-3-hydroxy-5-oxopentanoic
acid;
1:1 -mixture of (rac. y(3R *)-5-{{]R * 55'*)-6-[cyclopropyl'(2-/?-tolylethyl)-carbamoyl]-7-{4-[3-(2,3,6-trifliiorophenoxy)propyl]phenyl}-3,9-dia2abicyclo-[3.3.i]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.)-(3i?*)-5-((iiJ*, 55*)-6-[cyclopropyI-(2-;)-toIylethyl)carbamoyl]-7-{4-[3-{2,3,6-trifluoro-phenoxy)propyi]pheTiy!}-3,9-diazabicyclo-[3.3.1]non-6-eii-3-yl)-3-hydroxy-5-oxopentanoic acid;
(rac.)-{lR*. 55*)-3-acetyI-7-{4-[3-(2,3,6-trifluoropheiioxy)propyl]phenyl}-3,9--diazabicyclo[3.3.1]non-6-ene-6-carboxylicacidben2ylcyclopropyIamide;
{rac.y{IR*, 5^*)-3-acetyl-7-{4-[3-(2,3,6-trifluoropbenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]noii-6-ene-6-carboxyIic acid cyclopropyl-(2-fluorobenzyl)-amide;
(rac.y(lR*, 5iS'*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-diazabicyclo[3.3.1]non-6-en6-5-carboxylic acid cyclopropyl-(2-methylbenzyl)-amide;
{rac.y(IR*. 5iS*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl)-3,9-diazabicyclo[3.3.1]non-6-en6-6-carboxylic acid cyclopropyl-[2-(4-metlioxy-phenoxy)ethyl]amide;

{rac.yUR*. 55*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propy[]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-[2-(3-raethoxy-pbenoxy)ethyl]ainide;
{rac.y{lR*. 55'*)-3-acetyl-7-{4-[3-(2,3,6-trifluoropIienoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1]iion-6-ene-6-carboxyIic acid cyclopropy!-[2-(3-methyl-phenoxy)ethyl] amide;
{rac.yilR*. 55*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-dLazabicyclo[3.3.1]n.on-6-ene-6-carboxylic acidcyclopropylpheaethylamide;
[rac.yUR*, 5S*)-3-acetyl-7-{4-[3-(2,3,6-trifliioTopiienoxy)propy\]plienyl>-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acidcycIopropyl(2-/'-tolylethyl)aniide;
(racy5-({JR*. 5xS'*)-6-{cyclopropyl-[2-(4-inethoxyphenoxy)ethy]]carbamoyl}-7-{4-[3~(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid;
(rac.)-5-((ii!* i5*)-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifIuorophenoxy)propyl]phenyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopeQtanoic acid;
(rac.y5-i{lR*, 5S*)-6- (cyclopropyl[2-(3-methylph6noxy)ethyl]carbamoyl} -7- {4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid;
(rac.yS-iOR*, 55*)'6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-
7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yi)-5-oxopentanoic acid;

{rac.)-5-((lR*. 56'*)-6-(cyclopropyIphenethylcarbamoyI)-7-(4-(3-(2,3,6-trifluoro-
phenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.1]Don-6-en-3-yl)-5-oxopentanoic
acid;
{rac.)-S-{{}R*, 55*)-6-{cyclopropyl-[2-(2,3--difluorophenyl)ethyl]carbamoyi}-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl)-3,9-diazabicyclo[3.3.1]iion-6-en-3-y!)-5-oxopentanoic acid;
(rac.)-5-((JR*. 55*)-6-{cycIopropyl-[2-(4-fluoropheRyi)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifIuorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-eii-3-yl)-5-oxopentanoic acid;
(rac.yS'iiJR*. iiS'*)-6-(cyclopropyl-[2-(2-methylphenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en'3-yl)-5-oxopentanoic acid;
(rac.}-5-((/i;*, 55*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propylJphenyl}-3,9-dia2abicycIo[3.3.1]noii-6-en-3-yl)-5-oxopentanoic acid methyl ester;
(rac.)-5'({lR*, 55*)-6-[cyclopropyl-(3-txifluoromethylbeiizyl)carbamoyl]-7-{4-[3-{2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3.1]iion-6-en-3-yl)-5-oxopeatanoic acid methyl ester;
(rac.)-5-((ii;* 55*)-6-[cyclopropyl-{2-methylmethylbenzyl)carbanioyl]-7-{4-[3-(2,3,6'trifluorophenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
(rac.)-5-((IR*, JiS'*)-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;

(rac.)-5-({lR*, J5'*)-6-(cyclopropyl-[2-(3-inethoxyphenoxy)ethyl]carbamoyi}-7-{4-[3-(2,3,6-trifluorophenoxy)propyt]phenyl}-3,9-diazabicyclo[3.3.I]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
{rac.)-5-{{]R*. 55*)-6-(cyclopropyl-[2-(3-methylphenoxy)ethyl]carbainoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9- (rac.yS'dJR*, J5'*)-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
{rac.y5-i(lR*, 55*)-6-(cyclopropylphenethylcarbamoyl}-7-{4-[3-(2,3,6-trif]uoro-phenoxy)propyl]pheny!}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
(rac.y5-((JR*. 55*)-6-{[2-(2-chlorophenyl)ethyl]cycIopropyIcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
{rac.yS-dlR*, 55*)-6-{cyclopropyl-[2-(2,3-difluorophenyI)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ett-3-yl)-5-oxopentanoic acid methyl ester;
{racyS-aiR*, 55*)-6-{cyclopropyl-[2-(4-fluoroplienyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]pheayl}-3,9-diazabicyclo[3.3.1]noii-6-en-3-yl)-S-oxopentanoic acid methyl ester;
(rac.y5-(_UR*. 55'*)-6-{cyclopropyl-[2-(2-methylpheiiyl)ethyl]carbamoyl}-7-{4-[3'(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopeiitanoic acid methyl ester;

(rac.)-5-((IR*, 5i)'*)-6-{cyc!opropyI-[2-(4-methyIphenyl)etbyl]carbanioyl}-7-{4-[3-(2,3,6-trifluoropbenoxy)propyl]phenyI}-3,9-diai^abicyclo[3.3.1]non-6-en-3-y])-5-oxopentanoic acid methyl ester;
(rac.yS'dJR*. 5iS'")-6-(benzylcycIopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-din"iethyl-5-oxopentanoic acid;
(roc.)-5'{{IR *, 5i'^^)-6-[cyclopropyl-(3-trifluoTomethylbenzyl)carbamoyI]-7- {4-[3-(2,3,6-trifluoTophcnoxy)propyl]phenyl}-3,9-dia2abicyclo[3,3,l]i"\on-6-eii-3-yl)-2,2-dimcthyl-5-oxopentanoic acid;
(rac.yS-ifJR*, 5,S'*)-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyL]carbamoyi}-7-
{4-[3-(2,3,6-trifluoropbenoxy)propyI]phenyl)-3,9-diazabicyclo[3.3.1jnon-6-en-3-
yl)-2,2-dimethyl-5-oxopentanoicacid;
(rac.y5'({]R*, 55*)-6-(cyciopropyl-[2-(3-methoxyph6noxy)ethy]]carbaraoyl}-7-{4-[3-{2,3,6-b-ifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.l3non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
(rac.)-5-((/i^*, 5S*)-6-{cyclopropyl-t2-(3-inethylphenoxy)6tbyl]cai:bamoyl}-7-
{4-[3-(2,3,6-trifluorophenoxy)propyljphenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-
yl)-2,2-dimethy]-5-oxopentanoicacid;
(mc.y5-({IR *, 5S*y6' {cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl] carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-dia2;abicycIo[3.3.1]non-6-en-3-yl)-2,2-diiiiethyl-5-oxopentanoic acid;
{rac.yS'iilR', 5S*)-6-tcyclopropylphenetfaylcarbamoyl)-7-{4'[3-(2,3,6-trifiiioTO-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1Jnon-6-eii-3-yI}-2,2-dimethyl-5-oxo-pentanoic acid;

{rac.y5-((lR*, 55*)-6^{[2-(2-chIorophenyl)ethyI]cyclopropyIcarbamoyI}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicycio[3.3.1]noii-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
(rac.)-5-((IR*, J5*)-6-{[2-(2,3-difluorophenyI)ethyI]cyclopropylcarbamoyI}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
{rac.)-5-{{]R*, 55*)-6-{[2-(4-fluoroplienyl)ethyl]cyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.I]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
(rac.)-5-((]R*, 55*)-6-{[2-(2-methyIphenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyi}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)~ 2,2-diniethyl-5-oxopentanoic acid;
(rac.)-5-(_(JR*, 55*)-6-{|;2-(4-methyIphenyl)ethyl]cycIopropylcarbamoyI}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-dia2:abicyclo[3.3.1]non-6-en-3-yI)-2,2-dimethyl-5-oxopentanoic acid;
l:l-mixtiire of (rac.)-i2R*, 3S*)-4-(UR*. 55*)-6-[(2-chlorobenzyl)ethyI-
carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo-
[3.3.1]aon-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid and {rac.y(2S*, 3R*yA-
({IR * 55*)-6-[{2-chlorobenzyl)ethylcarbamoyl]-7- {4-[3-(2,3,6-trifluoro-
phenoxy)propyI]phenyl}-3,9-diazabicycIo-[3.3.1]non-6-en-3-yl)-2,3- l:l-mixture of {rac.y{2R*, 3S*y4-{{IR*. J5*)-6-[cyclopropyl-(2-fluorobenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid and {rac.y(2S*, 5ii*)-4-((IR*, J5*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluoro-

phenoxy)propyljphenyI}-3,9-diazabicyclo-[3.3,l]non-6-en--3-yl)-2,3-dihydroxy-4-oxobut\Tic acid;
l:l-mixtm-e of (i-ac.y(2R^; 5^V*)-4^((7/^, 5,S'*)-6-[cyclopropyl'(3-lrifluoromethyl^ benzyl)carbamoyl]-7-|4-[3-(2,3,6-triflLioroplienoxy)propyL]phenyI}-3,9-diaza-bicyclo[3-3.i]non-6-en-3-yl)-2,3-dihydroxy-4-oxobuli'Tic acid and (rac,)-(25*, 3R*)-4-((JR*. 55'*)-6-[cyclopropyl-(3-trifiuoromet]iylben3yi)carbainoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]ptienyl}-3,9-diazabicyclo-[3.3.1]n.on-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid;
l:I-mixtiire or {rac.y(2R*. 3S*)-4-{{JR^ 55'*>6-{cyclopropyl-[2-(2,3-difluoro-
phenyl)etliyI]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]n.on-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid and (rac.)-
(2S*, 3R*y4-(lIR*. 55*)-6-{cyclopropy[-[2-(2,3-difluorophenyl)ethyI]-
carbamoyi}-7-{4-[3-(2,3,6-trifIuorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid;
Ill-mixture of (rac.y{2R*. 3S*y4-((lR*, 55'*)-6-{cyclopropyl-[2-(2-methy^ phenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]plienyl)-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid -and (rac.y {2S*. 3R*y4-{(]R*. 5>S*)-6-{cyclopropyl-[2-(2-mefhylphenyl)ethyl]carbamoyI}-7-{4-[3-(2,3.6-txifluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo-[3.3.1]nou-6-ea-3-yl)-2,3-dihydroxy-4-oxobutyricacid;
l:l-raixture of (rac.y(2R*, 3S*)-4-{(ii?*, 55'*)-6-[cyclopropyl-(3,5-diniethoxy-ben2yl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propylJplienyl}-3,9-diaza-bicyclo[3,3.1]non-6-en-3-yl)-2,3-dihydroxy-4~oxobutyric acid and (rac.y{2S*, 3R*y4'iiJR*. 55*)-6--[cyclopropyl-(3,5-diraethoxybenzyl)caTbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]pheny!}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-2,3-dthydroxy-4-oxobutyric acid;

l:l-mixture of {rac.y{2R*, 3S*)-4'(UR*. 55*)-6-{cyclopropyl-[2-(4-methyl-phenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluoroplienoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid and (rac.)-{2S* 3R*)A-(ilR*. 55*)-6-{cyclopropyl-[2-(4-methyIphenyl)ethyl]carbanioyi}-7-(4-[3-(2,3,6-trifluoropheQOxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-y!)-2,3-dihydroxy-4-oxobutyric acid;
1:1 -mixture of (rac. y{3R *)-5-((lR *, 55*)-6-[(2-chloroben2yl)cycIopropyl-carbamoy!]-7-{4-[3-{2,3,5-trimethylphenoxy)ethyl]phenyI}-3,9-diazabicyclo-[3.3.l]iion-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (?-ac.)-(3S*)~5-i(IR*. iiS*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-y!)-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of (rac.)-(3R*)-5-((JR*, 55*)-6-[(2-chloroben2yl)ethyicarbamoyl]-7-{4-[3-(2,3,5-trimethyIphenoxy)ethyl]phenyi}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.)-(i5*)-5-((i^ * 55*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1 ]non-6~en-3-yl)-3-hydroxy-5-oxopentaiioic acid;
irac.)-5'(ilR*. i5*)-7~{4-[3-(2-bronio-5-fluoTOphenoxy)propyl]phenyl}-6-
{cyclopropyl-[2-(2-hydroxyethyl)benzyI]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid;
irac.)-5-((lR * 55*)-7- {4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl} -6-
{cyclopropyl-[2-(2-hydroxyethyI)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid methyl ester;
(rac.yUR* 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-
carbamoylbutyryl)-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid
eye loprop yl-[2-(2-hydroxyethyI)ben2yl] amide;

(mcyiin-^, ^.S0-3-acetyl^7-{4-[3-(2,3,6-trinuorophenoxy)propy!]phenyl}"3,9-diazabicyclo[3,3,l]non-6-ene-6-ca!boxylic acid cyclopropyl-[2-(2-Iiydroxyethyi)-b en zylj amide;
{mc.)-5-{{lR*, 55"*)"6-{cyclopropyl-[2'(2"hydroxyetliyl)benzyl]carbamoyl}-7-{4-[3'(2,3/>trifluorophenoxy)propyl]ph3nyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yI)-5-oxo-pentanoic acid;
{mc.y5-((IR*, 55*)-6-{cyclopTOpyl-[2-(2-hydroxyethyl)ben2yl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3,3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
{rac.y5-((lR*; 55*)-6-{cyclopropyl-[2-(2-hydroxyethyl)benz.yl]carbamoyl}-7-{4-[3-{2,3,6-tiifluoiopiienoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
(racy(JR* 55^*)-3-(4-carbamoy!butyryl)-7-{4-[3-(2,3,6-tTifluoropheiioxy)-
propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-[2-(2-hydroxyethyl)beiizyl]amide;
(rac.y5-{{lR*. 5S'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]plieiiyl}-6-[(2-chloroben2;yl)ethylcarbamQyI]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoic acid;
(rac.y5-{(]R*. 55'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]plienyl)-6-
[cyclopropyI-(3-trifluoromethyibenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid;
irac.yS'iiJR*. 55*)-7-{4-[3-(2-broino-5-fluorophenoxy)propyl]phenyl}--6-
[cyclopropyl-(2-methy!ben2yl)carbamoyi]-3,9-diazabicycIo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid;

{racyS-iilR*, 5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propylJphenyI}-6-
{cyclopropyl-[2-(4-methoxyphenoxy)ethyI]carbamoyi}-3,9-diazabicyclo[3.3.I]-noii-6-en-3-yl)-5-oxopentaiioic acid;
{rac.)-5'{ilJi*. i^*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-
{cyclopropyl-[2-(3,4-diinethylphenoxy)ethyI]carbanioyl}-3,9-dia2abicycIo[3.3.1]-non-6-en-3-yl)-5-oxopentanoicacid;
(mc.)-5-((JR*, J5'*)-7-{4-[3-(2-bromo-5-fIuorophenoxy)propylJphenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropyIcarbamoyl}-3,9-dia2abicyc!o[3.3.1]iion-6-en-3-yl)-5-oxopentanoic acid;
(rac.)-5-{(JR*, 5i'*>7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chloroben2yI)ethyicarbamoyl]-3,9-diazabicyc]o[3.3.1]noa-6-en-3-yl}-5-oxo-pentanoic acid methyl ester;
(rac.)-5'{(JR*, i5*>7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyi}-6-
[cycIopropyl-(2-fluorobeiizyi)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-S-oxopeotanoic acid methyl ester;
(rac.)-5-{iJR*. J>S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-
[cycloprc)pyl-(3-triiluoromethylben2yl)caibamoyl]-3,9-diazabicyclo[3.3.1]non-6-eii-3-yl}-5-oxopaitanQic acid methyl ester,
(rac.y5-i(JR*, J5*)-7-{4-[3-(2-bromo-5-fluoropfaenoxy)propyljphenyI}-6-
[cyclopropyl-(2-methylbenzyi)carbamoyl]-3,9-diazabicyclo[3.3.1]iion-6-en-3-yl}-S-oxopentanoic acid methyl ester;
(rac.)-5-i(JR*, J5'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-
{cycIopropyl-[2-(4-methoxyphenoxy}ethyl]carbamoyI}-3,9-diazabicyclo[3.3.1]-n.ott-6-en-3-yi)-5-oxopentanoic acid methyl ester;

{riiC.y5-{{!R*; 5.V^)-7-(4-[3-(2-bromo-5-l]uorophcnoxy')pi-opyllphKnyl}-6-
{cyclopropyl42-(3-inL-Lhylphenoxy)ethylJcai-brii]]oyi}-3,9-diazabicyclo[3-3.1Jiioji-6--en-3-yl)-5-oxopentanoic acid mcJiiy! ester;
{rac.)-S-((!R--\ 5vS"'^")-?-{4-[3-(2-bromo-5--auoraphcuoxy)prap>i]phcnyl}-6'
{cyc\opropyb[2-{3,4-G[methylphcnoxy)ethyi]carb2nioy])-3,9-diazabicyclo[3.3.1]-non-6-en-3-yi)-5-oxopcntaiioic acid methyl ester;
(rac.)-5'[(JR'-^, .^"6'*)-7-(4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyIt-6-
(cyciopropy!phencthylcarbanioy!)-3,9-di?-7,abicydo[3.3.1]i"ion-6-cn-3->'13-5-oxo-pcntarioic acid nietby! ester;
(rac.)-5-({JR*, 5^*)-7-{4-[3-(2-bromoo-fluorophenoxy)propyl]phenyl}-6~{[2-(2-chloropbenyl)ethyl]cyclopropylcaibamoyl}-3,9--dLazabicycIo[3,3,l]uon-6-en-3-yl)-5-oxDpentanoic acid metbyl csler;
(rac.)-5~((JR * J^*)-7- {4-[3-{2-bromo-5-fluorophenoxy)propyl]phenyl} -6- {[2-(2,3-difIuorophenyl)ethyl]cyclopropylcarbanioyI}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
(rac.)'5-(iJR*, J5*}-7-{4-[3-(2-bromo-5-fIuorophenoxy)propyI]phenyl}-6-{[2-(4-fluorophenyl)ethyI]cyclopropylcarbamoyI}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
(rac.yS-iilR*, 55*)-7-{4-[3-{2-bromo-5-fluorophenoxy)propyl]pbenyl}-6-{[2-(2-methyIphenyI)ethyl]cyclopropyicarbamoyi}-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
{rac.yS-iilR*, 55^*^)-7-{4^[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbaraoyl}-3,9-diazabicyclo[3.3.1]non-8-en-3-yl)-5-oxopentanoic acid methyl ester;

irac:)~5-{(2R*, 5i'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyI}-6-[(2-chlorobenzy]}ethylcarbamoyi]-3,9-diazabicyclo[3.3.1]non-6-en-3-yi}-2,2-dimethyl-5-oxopentanoic acid;
(rac.)-5-{(/fi*. 5.S*)-7-{4-[3-(2-bromo'5-fluorophenoxy)propyl]phenyI}-6-
[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diaz;abicycro[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxo-pentanoic acid;
{mc.)-5-((lR*, J^*)-7'{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-
{cyclopropyI-[2-{4-inethoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicycIo[3.3.1]-non-6-en-3-yl)-2,2-dimethyI-5-oxopentanoic acid;
(rac.)-5~(liJR*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-
{cyclopropyl-[2-(3-methyiphenoxy)ethyncarbamoyl}-3,9-diazabicyclo[3.3,ll-non-6-en-3-yl)-2,2-diniethyl-5-oxopen.tanoic acid;
{rac.yS-iilR*, 55'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyi]phenyl)-6-
{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbainoyl}-3,9-diazabicyclo-
[3.3.1,]non-6-en-3-y\)-2,2-diin6thyl-5-oxopentanoicacidi
(rac.)-5-((i-R*, 5S*)-1'(4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-([2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-diniethyl-5-oxopentanoic acid;
(rac.)-5-((JR * J5*)-7- {4-t3-(2-bromo-5-fluorophenoxy)propyl]pheiiyl} -6- {[2-(2,3-diiluoropheny!)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-
en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;
(rac.)-5~({IR*. 5^*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyI]phenyl}-6-{[2-(4' fiuorophenyI)ethyl]cyclopropyIcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

(rac.)-5-((JR*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyI}-6-{[2-(2-
methy)phenyl)ethyl]cyc3opropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-
yl)-2,2-dimelhyl-5-oxopeiitanoicacid;
l:i-mixture of {rac.)-{2R*, 3S*)-4-{(iJ?*, 55'*)-7-{4-I3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric acid and (rac.)-(2S*, 3R*)'4-{{IR*, 5S*yi- (4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl} -6-[(2-cMoro-benzyl)ethylcarbamoylj-3,9-diazabicyclo-[3.3,l]non'6-en-3-yI}-2,3-dihydroxy-4-oxobutyric acid;
l:l-mixture of (rac.)-(2if* 3S*)-4-{(lR^ 55*)-7-{4-[3-(2-bromo-5-fluoro-
phenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyI)carbaraoyl]-3,9-diaza-
bicyclo[3.3.1]non-6-en-3-yi'}-2,3-dihydroxy-4'OXobutyric acid and {rac.)-{2S*,
3R*y4'{{lR*, J5'*)-7-{4-[3-{2-bromo-5-fluoro-phenoxy)propyl]pheny]}-6-
[cyclopropyl-(2-fluorobenzyl)carbamoy]]-3,9-diaza-bicyc]o[3.3.I]non-6-en-3-yl}-2,3-diliydroxy-4-oxobutyric acid;
l:l-rmxture of (rac.)-(2R*. 3S*)-4'{UR*, J,S'*)-7-{4'[3-(2-bromo-5-fluoro-pheiioxy)propyl]phenyI)-6-[cyclopropyl-(3-trifluoTomethylbeiizyl)caibamoyl]-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl}-2,3-dibydroxy-4-oxobutyric acid and (rac.)-(2S*. 3R *)-4- {(IR * 5S*)-7~ {4-[3-(2-bromo-5-fluoro-phenoxy)propyl]-phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyI)caibamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yI}-2,3-diliydroxy-4-oxobutyiic acJd;
l-.l-mixture of (rac.y{2R*. 3S*yA-{{lR*, JS*)"7-{4-[3-(2-bTomo-5-fluoro-
phenoxy)propyl]phenyl}-6-[cyclopropyl'(2-methylbeiizyl)carbamoyI]-3,9-diaza-
bicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric acid and {rac.y{2S*,
3R*y4-{iIR*, J5*)-7-{4-[3-(2-bromQ-5-fluorQpheaoxy)propyl]-phenyl}-6-
[cyclopropyl-(2-methylbenzyi)carbamoyI]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric acid;

Ill-mixture of (rac.)-(2R*, 3S*y4-({lR*. 55*)-7-{4-[3-{2-bromo-5-fluoro-
phenoxy)propyl]phe]iy!}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]-
carbamoyl) -3,9-diazabicyclo[3.3.1 ]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric
acid and (rac.)-{2S*, 3R*)-4-iil R*. J5*)-7-{4-[3-(2-bromo-5-fluoro-
pheiioxy)propyl]pheiiyl}-6-(cyclopropyl-[2-(4-i:nethoxypheiioxy)ethyl]-
carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric
acid;
l;l-mixture of (rac.)-{2]i*. 3S*y4-i(]R*. 55*)-7-{4-[3-(2-brorao-5-fluoro-phenoxy)propyl]phenyl}-6-{cyc]opropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid and {rac.)-{2S*. 3R*)-4-(iiR*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propy!]-phenyl}-6-{cyclopropyl-[2-(3-methylpbenoxy)elhyl]carbainoyl}-3,9-diaza-bicyc]o[3.3.1]non-6-eD-3-yl)-2,3-dihydroxy-4-oxobutyric acid;
l:l-mixture of (rac.)-(2i?*. 3S*)-4-((/i?*, 5S*)-7-(4-[3-(2-brDmo-5-fluoro-pbenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyI]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyTic acid and (rac.)-(_2S*, 3R*)-4-i{lR*, J5*)-7-(4-[3-(2-broino-5-fluoropheiioxy)-propyI]phenyI}-6-{cyclopropyi-[2-(3,4-dimethylphenoxy)ethyl]caibamoyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yI)-2,3-dibydroxy-4-oxobutyric acid;
l:l-mixture of (racH^R*, 3S*)-4-[(JR*. 55*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]pheii>i)-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo-[3.3.1]noii-6-en-3-yl]-2,3-dihydroxy-4-oxobutyric acid and (rac.)-(2S*. 3R*)A-[(IR*. 55*>7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropyl-pheiietbyIcarbamoyl)-3,9-diazabicycIo-[3.3.1]aoii-6-eii-3-yl3-2,3-diliydioxy-4-oxobutyric acid;
l:l-niixture of {rac.y{2R*. 3S*)-A-{ilR*, J5*)-7-{4-[3-(2-broino-5-fluoro-pheooxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yI)-2,3-dihydroxy-4-oxobutyric acid and

{rac.)-i2S*, 3R*)-4-{{IR*, J5*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyc]opropyIcarbamoyl}-3,9-dia2abicycIo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid;
5 l;l-mixture of (rac.y(2R* 3S*y4-((IR*. 55*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]pfaen\-l}-6-{[2-(4-fluoTophenyl)ethyl]cycIopropylcarbamoyl}-3,9'dia2abicyclo[3.3.1]non-6-en-3-yI')-2,3-dihydroxy-4-oxobutyric acid and (rac.X3S*, 3R*)-4-{{IR*. 55*)-7-{4-[3-(2-bronio-5-fluorophettoxy}propyl]-phenyI}-6-{[2-(4-fluorophenyl)ethyl]cyciopropylcarbamoyI}-3,9-diazabicyclo-
0 [3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid;
l:l-mixture of (rac.)-(2K*, i5*)-4-((;R*, 5S*)-7-(4-[3-(2-bromo-5-fluoro-phenoxy)propyl|phenyl}-6-{[2-(2-methylphenyl)etliyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]Eon-6-en-3-yl)-2,3-dihydroxy-4-osobutyric acid and 5 (rac.y{2S*, 3R*)A-{{1R*, 5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]' pbenyl}-6-{[2-{2-methyIphenyl)ethylJcyclopropylcarbamoyl}-3,9-dia2abicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid;
l:l-mixture of {rac.)'{2R*, 3S*)-A-{{2R* 55*)-7-{4-[3-(2-bromo-5-fluoro-I phenoxy)propylJphenyl}-6-([2-(4-methy]phenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-2,3-di]iydroxy-4-oxobutyric acid and {rac.)-(2S*, 3R*y4-i(JR*, ^5*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbainoyl}-3,9-diazabicyclo-[3.3.l]non-6-en-3-yI)-2,3-dihydroxy-4-oxobutyric acid;
(rac.)-OR*. 55*)-7-{4-[3-(2-bromo-5-f!uorophenoxy)propyl]phenyl}-3-(4-
carbamoyIbutyryI)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chloro-benzyl)ethylaniide;
(rac.yilR*, J5*)-7-{4'[3-(2-bromo-5-fluorophenoxy)propyI]phenyl}-3-(4-
carbamoylbutyryl)-3,9-dia2abicycio[3.3.I]non-6-ene-6'Carboxylic acid
cycloprQpyl-(2-fluorobenzyl)amide;

(rac.)-(iK*, 5S*)-7-{4-[3-(2-bromo-5-fluoTophenoxy)propyi]phenyl}-3-(4-
carbamoyIbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid
cyclopropyl~(2-methylbenzyl)amide;
(rac.yOR*. 5.^*)-7-{4-[3-(2-brorao-5-fluorophenoxy)propyl]phenyI}-3-(4'
caTbamoylbutyryl)-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxyIic acid
eye lopropyl-[2-(4-inethQxyphenQxy)ethy I] amide;
(rac.)-(lR*, 5:5'*)-7-{4-[3-{2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-
carbamoy]butyryI)-3,9-dia2abicyclo[3.3.1]non-6~ene-6-carboxylic acid
cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl] amide;
(_rac-)-{IR*. J5*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyI]phenyl}-3-(4-
carbamoyIbutyryl)-3,9-diazabicyclo[3.3.I]non-6-ene-6-carboxylic acid [2-(2-chlorophenyl)ethyl]cyclopropylaTmde;
(rac.)-(]R*, 55*)-7-(4-[3-(2-bromo-5-fluoropheaoxy)propyl]phenyl}-3-(4-
carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]nQn-6-en.e-6-carboxylic acid [2-(2,3-difluorophenyl)ethyl]cyclopropylainide;
{rac.)-{lR*, 5i5*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyi]phenyl>-3-(4-
carbamoylbutyryl)-3,9-diazabicycIo[3.3.I]iiou-6-ene-^-carboxylic acid [2-(4-fluorophenyl)ethyl] cyclopropylamide;
irac.)-{lR*, 5.S'*)-7-{4-[3-(2'bromo-5-fluorophenoxy)propyI]phenyl}-3-(4-
cacbamoylbutyryi)-3,9-diazabicyclo[3.3.1]non-6-eiie-6-caiboxyIic acid [2-(2-methylphenyl)ethyi]cyclopropylamide;
{rac)-{lR*, 55*)-7-{4-[3-(2-brQmo-5-fluoropheiioxy)prQpyl]pheiiyl}-3-(4-
carbamoylbutyryi)-3,9-diazabicyclo[3.3.1]non-6-6ne-6-carboxyIic acid [2-(4-methylphenyI)ethyl]cyclopropylainide;

{rac.y{lR*, 55*)-7-{4-[3-(2-bromo-5-f]uorophenoxy)pTopyl]phenyl}-3-(4-
carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid
cyclopropyl-(3,5-dim ethoxyben2yl)amide;
l:l-mixture of {rac.)-(3R')-5-{{lR*, J5'*)-7-(4-[3-(2-bromo-5-fluorophenoxy)-
propyl]phenyI}-6-[{2-chloroben2yl)ethylcarbaraoyl]-3,9-dia2abicyclo[3.3.1]non-
6-en-3-yl}-3-hydTOxy-5-oxopentanoic acid and (rac.)-{3S*)-5-{(iii*, 5S*)-7-{4-
[3-(2-bromo-5-fluorophenoxy)-propyI]phenyl}-6-[(2-chlorobenzyI)ethyl-
carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic
acid;
l:l'mixture of (rac,y{3R*y5-{ilR\ 5^*)-7-{4-[3-(2'broniO'5-fluorophenoxy)-propyl]phenyl}-6-[cyclopropyI-(2-fluorobenzyl)carbamoyl]-3,9'diazabicycIo-[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid and (roc.)-(35*)-5-{(iii*, J5*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobeii2yI)carbamoyl]-3,9-diazabicycIo[3.3.1]non-6-6n-3-yl}-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of irac.)-{3R*)-5-{(lR*. i5*)-7-{4-[3 l:l-mixture of {rac.y(3R*)-5-{(JR*, J5*)-7-{4-[3-(2-bromo-5-fluoropbenoxy)-
propyl]phenyl}-6-[cyclopropyl-(2-metbylbenzyl)carbamoyl]-3,9-diaza-bicyclo[3.3.1]noii-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid and {rac.)-{3S*yS~ {(IR*, 55'*)-7-{4-[3-(2-bromo-5-fluDrophenoxy)propyI]phenyi}-6-[cyclopropyl-(2-methyIb6nzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid;

Ill-mixture of {rac.)-(3R*)-5'((lR*. 5^*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-
propyl]phenyl}-6-{cyclopropyI-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-
dia2abicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.)-
{3S*]-5-{{lR*, 5S*)-7-{4-[3-(2-bromo-5-{luoraphenoxy)propyqphenyl}-6-
{cyclopropyl-[2-(4-methoxypheiioxy)ethyI]carbamoyl}-3,9-dia2abicycio[3.3.1]-non-6-en-3-yI)-3-hydroxy-5-0xopentanoic acid;
l-.l-mixture of {rac.y{SR*)-HUR*, 55*)-7-{4-[3-(2-bromo-5-fluoropheaoxy)-
propyl]phenyI}-6-{cyclopropyl-[2-(3-methylphenoxy)ethy!]carbamoyl}-3,9-
diazabicyclo[3.3.1jnon-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.)-
{3S*)-5-({IR*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-
{cyclopropyI-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of (rac.H3R*)-5-((JR*, J5'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-
propyl]phenyl}-6-{cycloprQpyl-[2-(3,4-dimethy!phenoxy)ethyl]carbamoyl}-3,9-
diazabicycIo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.)-
(3S*)-5-{(JR*, 55*)-7-{4.[3-{2-bromo-5-fluorophenoxy)propyl]phenyl)-6-
{cycIopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-iiOQ-6-en-3-yl)-3-liydroxy-5-oxope!itanoicaGid;
l:I-mixtuxe of (rac.)-(3R*)-H0R*. i5*)'7-{4-[3-(2-bromo-5-fluorophenoxy)-
propyl]phenyl}-6-(cyclopropylphenethylcarbanioyl>-3,9-diazabicycIo[3.3.1]non-
6-en-3-yl]-3-hydroxy-5-oxopeiitaiioic acid and {rac.)-{3R*)-5-[QR*. 5S*)-l-{4-
[3-(2-bromo-5-fluoropheiioxy)propyl]phenyl}-6-(cyclopropylphenethyl-
carbamoyl)-3,9-diazabicyclo[3.3.1]non-6-eii-3-yl]-3-hydroxy-5-oxopentaiioic
acid;
l:l-mixture of (rac.)-(3R*y5~((IR*. J5'*)-7-(4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-dia2a-bicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and {rflc.)-(3fi*)-5-

i{}R*. 55*)-7-{4-[3-(2-bromo-5-nuorophenoxy)propyl]phenyl}-6-{[2-(2-chloro-plienyl)ethyl]cyclopropylcarbamoyl)-3,9-diazabicyclo[3.3,l]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of (rac.)-(3R*)-S-({JR*. 55*)-7-{4-[3-(2-bromo-5-fluoropbenoxy)-propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cycIopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxop6ntaiioic acid and {rac.)-(3R*y5-(iIR*, J5*)-7-(4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2,3-difluorophenyl)eihyl]cyclopropylcarbainoyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-3-hydroxy-5 -oxopentanoic acid;
l:l-mixture of (rac.)-(3S*)-5-((iJi* 5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-(4-fluoropheuyl)ethyl]cyclQpropylcarbanioyl}-3,9-diaza-bicyclo[3.3.1]non-6-en-3-yi)-3-hydroxy-5-oxopentanoic acid and (rac.)-(3R*)-5-((IR*, ^5*)-7-{4-[3-(2-bromo-5-fluoropbenoxy)propyl]pbenyI)-6-{[2-(4-fluoro-plienyl)ethyI]cyclopropyIcarbamoyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of (rac.y(3R*)-5-i(]R*, i5'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-{2-methylphenyl)ethyl]cyclopropyIcarbamoyl}-3,9-dia2a-bicycio[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.)-i3R*)-5-((JR*, 55*)-7-{4-[3-(2-bromo-5-fluoropheaioxy)propyI]phenyI}-6-{[2-(2-metbyl-phenyl)et}iyl]cyciopropylcaibamoyl} -3,9-di^abicyclo[3.3.1 ]non-6-en-3-yl)'3-hydroxy-5-oxopentanoic acid;
l;l-mixture of {rac.)'(3R*y5-({lR*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]pheiiyI}-6-{[2-(4-metbylphenyl)ethyl]cyclopropylcarbamoyi}-3,9-diaza-bicyclo[3.3.1]non'6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.)-(3i?*)-5-((/fi* 5S'*)-7-{4'[3-{2-bromo-5-fluorophenoxy)propyI]pheayl}-6-{[2-(4-methyl-phenyI)ethyI]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;

l:l-mixture of (rac.)-{3R*y5~{{lR*, 5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[cyciopropyl-(3,5-dimethoxyben2yl)carbanioyI]-3,9-diaza-bicyc]o[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentajioic acid and (rac.)-(3S*)'5-{(IR*, 5iS'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-diinethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3'yl}-3-hydroxy-5-oxopentanoic acid;
l;l-mixture of (rac.y{3R*)-5~((JR* 5i'*)-6'{cycIopropyl-[2'(2-hydroxyethyI)-
benzyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyi]pbenyl}-3,9-diaza-
bicyc!o[3.3.1]non-6-en-3-y!)-3-hydroxy-5-oxopentanoic acid and (mc.)-(5S*)-5-
((IR*, 55*)-6'{cyclopropyl-[2-{2-hydroxyethyi)benzyI]carbamoyl}-7-{4-[3-
(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6"en-3-yI)-3-hydroxy-S-oxopentanoic acid;
(rac.)-{}R*, J5*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethy]]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-ch]orobenzyl)oyclopropyl-amide;
{rac.)-{lR*, 55*)-3-acetyl-7-{4-[2-(2,3,5-trimethylpheaoxy)etbyi]phenyl}-3,9-diazabicyclo[3.3.I]non-6-ene-6-carboxylic acid(2-chlorobeii2yI)ethyIamide;
irac.)-(lR*, i5'*>3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyI}-3,9' diazabicyclo[3.3.1]non-6-aie-6-caiboxyUc acid (2-fluoroben2yl)cyclopropyl-amide;
(rac.y(lR*. J-y*)-3-acetyl-7-{4-[2-(2,3,5-fiimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-eiie-6~caTboxyUc acid (3-trifluorometh.ylbenzyl)-
cyclopropylamide;
(rac.)-(JR*, J5*)-3-acetyl-7-{4-[2-(2,3,5-trimethy]phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2'methylbenzyl)cyclopropyl-amide;

(rac.)-{i-R* 55*)-3-acetyl-7-{4-[2-(2,3,5-trimetliylphenoxy)ethyl]phenyi}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid cycIopropyl-[2-{4-methoxy-phenoxy)ethyl] amide;
{rac.)-5-((ii?*, 5S*)-6-(ben2ylcyclopropylcarbamoyl)-7-{4-t2-(2,3,5-triniethyl-
phenoxy)ethyl]phenyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-5-oxopentanoic
acid;
(rac.yS-{(lR*. 5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2,3,5-trimethyI-
phenoxy)etliyl]phenyI}-3,9-diazabicycIo[3.3.1]noQ-6-en-3-yl)-5-oxopentanoic
acid;
(rac.)-5-((i^* 5-S'*)-6-[(2-fluoroben2y[)cyclopropylcarbamoyll-7-(4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyi}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid;
(rac.y5'((IR*, J5'*)-6-{cycIopropyl-[2-{4-methoxyphenoxy)ethyl]carbanioyl}-7-{4-[2-(2,3,5-trimethylphenoxy)eliiyl]phenyI}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid;
(rac.y5-((JR*, J5'*)-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyI]carbamoyl}-7-{4-[2-{2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicycIo[3.3.1]nou-6-eii-3-yl)-5-oxopentanoic acid;
(rac.y5-((JR*, J5'*)-6-{cyclopropyl-[2-(3-methylphenoxy)ethyI]carbamoyl}-7-
{4-[2-(2,3,5-triinethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid;
(rac.y5-((]R* J5*)-6-[{2-clilorobenzyl)ethylcarbamoyI]-7-{4-[2-(2,3,5'trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;

(rac.y5-((lR*. 55*)-6-[cyclopropyl-{2-fluorobenzyl)carbaraoyl]-7-{4-[2-(2,3,5-trmiethylpbenoxy)ethy!]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid methyl ester;
(rac.)-5-((lR*. 55'*)-6-[cyclopropyl-{2-methyIbenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyI]phenyi}-3,9-diazabicyclo[3.3.I]non-6-en-3-yl)-5-oxo-pentanoic acid methyl ester;
(rac.y5-((lR*, J5'*)-6-[(2-chloroben2yl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trmiethylphenoxy)ethyl]phenyl}-3,9-diazabicycio[3.3.1]non-6-en'3-yl)-2,2-dimethyl-5-oxopeatanoic acid;
irac.y5~((lR*, 55*)-6-(beDzylcyclopropylcarbamoyl)-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-2,2-dimethyI-5-oxopentanoic acid;
(rac.)-5'(0R*, 55*)-6-[cycIopropyl-(2-methylbenzyI)carbamoyl]-7-{4-[2-(2,3,5-tTimethylphenoxy)ethyl]phenyI}-3,9-diazabicyclo[3.3.1]non~6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
l:l-mixture of (rac.)-(3R*)A'(lilR* 55*)-6-[cyclopropyl-(2-methylbenzyl)-carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)etfayl]phenyl}-3,9-diazabicyclo-[3.3.1]iaon-6-en-3-yl)-2,3-dihydroxy-4-oxobutyiic acid and (rac.)-(3S*)-4-(i}R*. 55'*)-6- [cyclopropyl-(2-methylbenzyl)carbainoyl] -7- {4-[2-(2,3,5-trimethyl-plieQoxy)ethyl]phen,yl}-3,9-diazabicyclo-[3.3.1]noa-6-ea-3-yl)-2,3-dihydroxy-4-oxobutyric acid;
(rac.)-(JR*, 55'*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-
ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxy!ic acid benzyl-cyclopropylamide;
(rac.y(]R*, J5*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-
ethyI]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chloro-benzyOethylamide;
5 {rac.)-{JR*, 5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-
ethyl]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyc!opropyl-(2-fluorobenzyl)aniide;
1;l-mixture of {IR, 5S)-7-{4-[3-(2-broino-5-flaorophenOxy)prQpyl]pheiiyl}-3-) ((2S, 4R)-4-hydroxypyrroIidine-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,5-dimethoxybenzy])amide and (IS, 5i?)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]pbenyl}-3-((25, 4R)-4-hydroxypyrroUdme-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyI-(3,5-dimethoxybenzyl)ainide; >
{rac.)-5-{{lR*. 55*)-7-{4-[3-(2-broino-5-fluoTophenoxy)piopyl]phenyl}-6-[(2-chlorobeiizyl)cycloprDpylcarbamoyl]-3,9-diazabicyc]o[3.3.1jnon-6-en-3-yl}-5-oxopentanoic acid methy! ester;
l:l-mixture of (rac.)-(3R*y4'{(IR* 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-dia2abicyclo-[3.3.1]non-6-eii-3-yI}-2,3-dihydroxy-4-oxobutyric acid and (rac.'y(3S*y4-{(JR*. 55'*)-7-{4-[3-(2-bromo-5-fIuoropheiioxy)propyl]pheayl}-6-[(2-cMorobenzyl)-cyclopropylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric acid;
(rac.yS-iOR*. J5'*)-6-(beDzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluoro-
phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-5-oxopen.tanoic acid;
l:l-mixture of (rac.y(2R*, 3S*y4-((}R*. 55'*)-6-(benzylcyclopropyIcarbamoyI)-7-{4-[3-(2-bTomo-5~fluoiophenoxy)propy!]phenyl)-3,9-diazabicycIo[3.3.1}non-6-

en-3-yl)-2,3-dihydroxy-4-oxobutyric acid and {rac.y{2S\ 3ii*)-4-((JJJ* 55*>6-(ben2yIcyclopropylcaibamoyl)-7-{4-[3-(2-bromo-5-fluorQphenoxy)prQpyI]-phenyl}-3,9-dia2abicyclo[3.3,l]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid;
(rac.yilR*. 5^*)-7-{4-[3-(2-bromo'5-fluorophenoxy)propyl]phenyl}-3-(4-
carbamoylbutyryl)-3,9-diazabicycio[3-3.1]non-6-ene-6-carboxylic acid benzyl-cyclopropylamide;
l:l-mixture of (rac.)-5-{{lR*, i>S*)-7-{4-[3-(2'bromo-5-fluorophenoxy)propy]]-phenyl}-6-[((2i;*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-dia2abicyclo-[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid and (rac.y5-{ilR*, J5*)-7-{4-[3-(2-bromo-3-fluoropb,enoxy)propyl]phenyi)-6-[((2S*)-2-bydrox:y-2-phenylethyi)-methylcarbamoyl3-3,9-diazabicyclQ-[3.3.1]non-6-ea-3-yl}-5-oxQpentanoic acid;
l:l-mixture of (rac.y5-{(JR*. 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyI}-6-[{(2i;*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-ea-3-yl)-5-oxopentanoic acid methyl ester and (_rac.y5-{{lR*, 55*)-7-{4-[3-(2-bromo-5-fluoropheiioxy)propyl]pbenyl}-6-[((2S*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid methyl ester;
l:l-mixture of (rac.y5-{(_lR*, 5;S*)-7-{4-[3-(2-brQmo-5-fluorophenoxy)propyl]-phenyi}--6-[((2ii*)'2-hydroxy-2-phenylethyl)inethylcart)amoyI]-3,9-dia2abicyclo-[3.3.1]non-6-en-3-yl}-2,2-diinethyl-5-oxopentanoic acid and (rac.)-5-{(/ie* 5S*y 7-(4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[((25*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo-[3.3.1]noii-6-en-3-yl}-2,2-dimethyl-5-oxopeutanoic acid;
l:l-mixtiire of (i-ac.y(lR*. J5*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyIl-phenyl}-3-{4-carbamoylbutyryl)-3,9-diazabicycIo[3.3.1]non-6-ene-6-caTboxylic acid ((27e*)-2-hydroxy-2-phenyIethyI)methylamide and (rac.y{lR*. 55'*)-7-{4-[3-(2-bromo-5-fIuorophenoxy)propyl]-phenyl}-3-(4-carbanioyIbutyryl)-3,9-

diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid ((2^*)'2-hydroxy-2-phenylethyl)-methylamide;
l:l-mixture of (rac.)-(3R*)-5-{(lR* 55'*)-7-{4-[3-(2-bromo-5-f]uorophenoxy)-propyl]plienyl}-6-[(2-chlorobenzyi)cycIopropy!carbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid and {rac.)-(3S*)-5-{(lK*, 5S*)-7-{4-[3-(2-brQmo-5-fluorophenoxy)pTOpyl]phenyl}-6-((2-chlorobenzyl)-cycIopropylcarbanioyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-y]}-3-hydroxy-5-oxopentanoic acid;
l:l-niixture of (rac.)-(3if*)-5-((ifl*, 55*)-6-(ben2ylcyclopropylcarbamoyl)-7-{4-[3-{2-bromo-5'fluorophenoxy)propyi]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.y(3S*y5-({lR*, 5S*)-6' (benzylcyclopropylcarbamoyl)-7-(4-[3-{2-bromo-5-fluorophenoxy)propyI]-plienyI}-3,9-diazabicycIo[3.3.1]non-6-en-3-yI)-3-hydroxy-5-oxopentanoic acid;
{rac.)-(}R*, 5^*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1Jnon-6-ene-6-carboxylic acid [2-(2-chloropheayl)ethyl]-cyclopropylamide;
(rac.)-(lR*. 55*)-7'{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]plienyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,5-diinethoxy-benzyl)amide;
(rac.)-(IR*. i5'*)-7-{4-[2-(2-chloro-4,5-diniethylphenoxy)ethoxy]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-eae-6-carbQxyUc acid cyclopropyl-(p-toluyl-
ethyl)amide;
(rac.)-(JR*, J5*)-3-acetyl-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3,9-diaza-bicyclo[3.3.1 ]non-6-ene-6-carboxylic acid (2-clilorobenzyl)cyclopropylaTiide;

{rac,)-UR*. 3S*)-3-acetyl-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxyiic acid cycIopropyl-(3,5-dmiethoxybenzyI)-amide;
(rac.)-5'{(lR*, 55*)-7-{4-[2-(4-bronioph6noxy)ethoxy]phenyl}-6"[(2-chloro-benzyl)cyclopropylcarbamoyl]-3,9-d!azabicycIo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoic acid;
{rac.)-5-{(lR*, 55*)-6-(ben2ylcyclopropylcarbainoy]}-7-{4-[2-(4-bromophenoxy)-ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-eii-3-yl)-5-oxopeiitanoic acid;
{rac.)-5-{{lR*. 5-S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluoroben2yl)carbamoyl]~3,9-diazabicyclo[3.3.1]noa-6-en-3-yl}-5-oxo-pentanoic acid;
(rac.)~5-{{}R*, 5S*)-7-{4-[2-{4~bromophenoxy)ethoxy]pheDyl}-6-[cyclopropyi-(3-trifluoroinethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid;
{rac.y5-{(lR*, 55*)-7-{4-[2 (rac.)-5-{(JR*, 55*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-5-oxop6ntanoic acid;
irac.}-5-{{lR*. 55*)-7-{4-[2-(4-bromopheiioxy)ethoxy]phenyl}-6-{[2-(2-chloro-phenyl)ethyl]cyclopropy]carbamoyl}-3,9-diazabicyclc[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid;

{rac.y5-{(lR*, 5S*>7-{4-[2-(4-bromoplienoxy)ethoxy]phenyl)-6'{cyclopiopyl-[2-(4-fluorophenyI)ethyl]carbanioyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid;
(mc.y5-{(lR*, 5LS'*)-7-(4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{cycIopropyl-[2-(2-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1}non-6-en-3-yl}-5-oxopentanoic acid;
(/■ac.ys- {{IR * 5S*y7' (4-[2-(4-bromophenoxy)ethoxy]phenyl}-6- {cyclopropyl-[2-(4-methylphenyl)ethyl]carbamoyl}-3,9-dia2abicycIo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid;
(rac.y5-{(JR*, J5'*}-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-diinethoxybenzyl)carbamoyi]-3,9-diazabicyclo[3.3.I]non-6-en-3-yl}-5-oxo-pentanoic acid;
{rac.y5-{(JR*, 55'*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyI]-3,9-diazabicyclo[3.3.13non-6-en-3-yl}-2,2-diinethyl-5-oxopentanoic acid;
{rac.yS-{{lR*, 55*)-7-(4-[2-(4-bromoptieiioxy)ethQxylplienyl}-6-{[2-(2-chloro-phenyl)etliyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-diinethyl-5-oxopeiitanoic acid;
(rac.y5-((IR *, 5S*yi- {4-[2-(4-bromophenoxy)ethoxy]phenyl} -6- {cyclopropyl-[2-(2,3-difluotophenyI)ethyl]carbamoyI}-3,9-diazabicyclo[3,3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
{rac.yS'iQR*. 55*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{cycIopropyl-[2-{2-methylphenyi)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopeiitanoic acid;

(rac.)-5-((lR*. J5*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{cycIopropyI-[2-(4-methylphenyl)ethyllcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyI-5-oxopentanoic acid;
(rac.)-5-{(lR*, JiS'*)-7-{4-[2-{4-bromophenoxy)ethoxy]phenyi}-6-[cyclopropyl-(3,5-dimethoxybenzyI)carbamoyl]-3,9-diazabicyclo[3.3.I]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic acid;
(rac.)-(JJi*, 55*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyc!o[3.3.1]non-6-ene-6-carboxylic acid benzylcyclopropyl-amide;
{rac.)-(JR*, 55*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3-(4-carbainoyI-butyryi)-3,9-dia2abicyclo[3.3.1]noii-6-ene-6-carboxyIic acid (2-chlorobenzyl)-ethylamide;
{mc.)-{lR*. 55*)-7-{4-[2-(4-brom.Qphenoxy)ethoKy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclof3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2-fluoroben2yl)amide;
{rac.)-{lR*, 55*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3-(4-carbainoyl-butyryl)-3,9-diazabicyclo[3.3.1 ]non-6-ene-6-carboxylic acid cyciopropyl-[2-(4-methoxyphenoxy)ethyl] amide;
{rac.)-{lR*, 55*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid [2-(2-chlorophenyl)-
ethyljcyclopropylamide;
{rac.)'{}R*. 55*)-7-{4-[2-(4-bromophenoxy)ethoxy]pbenyl}-3-(4-carbamoyi-butyryl)-3,9-diazabicyclQ[3.3-l]non.-6-ene-6-carboxylic acid cyclopropyI-(3,5-dLinedioxybenzyI)amide;

{rac. )-(JR * 5S*)-7' {4-[2-(4-broraophenoxy)ethoxy]pheny]} -3-(4-carbamoyI'
butyryl)-3,9-dia2abicycIo[3.3.]lnon-6-ene-6-carboxylic acid cyclopropyl-[2-(2-hydroxyethy])benzy]] amide;
{rac.)-{IR*. 55'*)-7-{4-[2-(2-chIoro-4,5-dimethyIphenoxy)ethoxy]phenyl}-3'
foniiyl-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chIorobenz}-i)-ethylaniide;
{rac,y{lR*. 55*)-7-{4-[2-(2-cliloro-4,5-diinethyiphenoxy)ethoxy]phenyl}-3-
formyl-3,9-diazabicycIo[3.3.1]non-6-ene-6-caiboxylic acid cyclopropyi-(2-o-tolylethyI)amide;
{rac.)-(lli*, 55*)-7-{4-[2-(2-chloro-4,5-diniethylphenoxy)ethoxy]phenyl}-3-
formyl-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyI-(3,5-diinethoxybenzyl)amide;
{rac.y{lR*, 55*}-3-acetyl-7-{4-[2-(2-chloro-4,5-diinethylpheiioxy)ethoxy]-
phenyl)-3,9-diazabicyclo[3.3.1]non-6-ene'6-carboxylic acid (2-cWorobenzyi)-ethylamide;
{rac.)-(lR*, 5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylpheiioxy)ethoxy]-
phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-{2-fluorobenzyI)amide;
{rac.)-(lR*. y5*)-3-acetyl-7-{4-[2-(2-chIoro-4,5-dimethylphenoxy)ethoxy]-
phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid cycIopropyl-{2-methylbenzyl)amide;
(rac.)-(lR*, 55*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-
phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyI-(3,5-dimethoxybeiizyl)amide;

(rac.y(IR*, 5,y*)-3-acety!-7-{4-[2-(2-chIoTO-4,5-dimethylphenoxy)6thoxy]-
phenyI)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxy]ic acid cyclopropyl-(2-;7-to]ylethyl)amide;
(rac.yS-aiR*, 55*)-6'[C2-chlorobenzyl)ethylcarbamoyI]-7-{4-[2-(2-chloro-4,5-diinethylphenoxy)ethQx.y]phenyl}-3,9-diazabicycIo[3.3.1]nQa-6-en-3-yl)~5~oxo-pentanoic acid;
{rac.)-S-{{lR*, 5S*)-7-{4-[2-(2-chloro-4,5-dimefeylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-f]uorobenzyl)carbamoyl]-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid;
(rac.y5-{{]R*, 55*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6' [cyclopropyl-(3-trifluoroinethylbenzyi)carbaraoyI]-3,9-diazabicycIo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid;
(rac.y5-{{IR*, 55'*)-7-{4-[2-(2-chIoro-4,5-diniethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]cariiainoyl}-3,9-diazabicyclo[3.3.1]-non-6-6n-3-yl)-5-oxopentanoic acid;
(rac.y5-((_lR*. J5*>7-{4-[2-(2-chloro-4,5-diniethyIpbenoxy)ethoxy]phenyl}-6-{cyclopropyI-[2-(3-methoxypheiioxy)etliyI]carbamoyl} -3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic acid;
(rac.y5-(0R*, JiS'*)-7-{4-[2-(2-chloro-4,5'dimethylphenoxy)ethoxy]phenyl}-6-
{cycIopropyl-[2-(3-methyIphenoxy)ethyl]carbainoyl}-3,9-diazabicyclo[3.3.1]-
non-6-eii-3-yl)-5-oxopentaiioicacid;
(rac.yS'KJR*. i6'*)-7-(4-[2-(2-chloro-4,5-dimethyIphenoxy)etboxy]phenyl}-6-(cyclopropylphenethyicarbamoyl)-3,9-dia2abicyclo[3.3.1]non-6-en-3-yI]-5-oxo-pentanoic acid;

(rac.y5'(iJR*, 55*)-7-{4-[2-(2-chloro-4,5-dimethy!phenoxy)ethoxy}phenyI}-6-{[2-(2-chlorophenyl)etliyl]cyclopropyl-carbamoyl}-3,9-dia2abicyclo[3.3,l]non-6-en-3-yl)-5-oxopentaiioic acid;
{rac,y5~((JR*. j5*)-7-{4-[2-(2-chIoro-4,5-diniethylphenoxy)ethoxy]pheny[}-6-
{cyclopropyI-[2-(2,3-difIuorophenyi)ethyI]carbamoyl}-3,9-diazabicyclo[3.3.1]-
non-6-en-3-yl)-5-oxopentanoicacid;
{rac.yS'iilR*, ;5'*)-7-{4-(2'(2-chlorQ-4,5-dimettiylphenQxy)ethoxy]phenyl}-6' {cyclopropyl-[2-{4-fIuorophenyl)ethyi]carbamoyI}-3,9-diazabicyclo[3.3.i]-noii-6-en-3-yI)-5-oxopentanoic acid;
{rac.y5-((lR*. 5i^*)-7'{4-|;2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyI}-6-{cyclopropyl-[2-(2-methyiphenyl)ethyl]carbamoyI}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxop6ntaiioic acid;
irac.y5-((IR*, J5*)-7-{4-[2-(2-ch]oro-4,5-dimethylphenoxy)ethoxy]pheny!}-6-{cyclcfpropyl-[2-{4-methylphenyl)ethyl]carbamoyl)-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic acid;
[rac.yS-iilR*. 55*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl>7-(4-[2-(2-
chloro-4,5-diinethylphenoxy)ethoxy]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3~ yl)-5-oxopentanoic acid methyl ester;
(rac.y5-((JR * J,y*)-6-[(2-chlorobenzyl)ethyIcarbamoyI]-7- {4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}~3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
{rac.y5'{(lR*. 55*)-7-{4-[2-(2-chloro-4,5-diinethylpheEOxy)ethoxy]phenyI}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-dia2abicycIo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid methyl ester;

(rac.)-5-{(7ii*, iS*)-7-{4-[2-(2-chloro-4,5-dLmethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylben2yl)carbamoy!]-3,9-diazabicycIo[3.3.1]non-6-en-3-y!}-5-oxopentanoic acid methyl ester;
{rac.)-5'{(IR*, 55'*)-7-{4-|;2-(2-chioro-4,5-dimethylphenoxy)ethoxy]ptLenyI}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5~oxopentanoic acid methyl ester;
(rac.)'5-[0Ji*, 55*)-7-(4-[2-(2-ch]oro-4,5-dimethylphenoxy}ethoxy]phenyI}-6-{cyclopropyIphenethyIcarbamoyt)-3,9-diazabicyclo[3,3.1]non-6-en-3-yI]-5-oxo-penlanoic acid methyl ester;
{rac)-5-iiIR*, J5*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyI}-6-{[2-(2-chlorophenyl)ethyI]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]noii-6-en-3-yl)-5-oxopentaiioic acid methyl ester;
{rac.)-5-({lR*, 55*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2,3-difluoropheDyl)ethyl]cyclopropylcarbamoyI}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
{racyS-iilR*. 5S*)-7-t4-[2-(2-chloro-4,5-dimethyipheiioxy)ethoxy]phenyI)-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbaraoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
(rac.)-5-(0R *, 55*)-7- {4-[2-(2-chIoro^,5-dimethylphenoxy)ethoxy]phenyl} -6-{[2-(2-methylphenyl)etiiyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3-3.1]non.-6-en-3-yl)-5-oxopentanoic acid methyl ester;
irac.)-5-i{lR*, 55*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(4-methyIphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-5-oxopeiitancic acid methyl ester;

(mc.y5'{(JR* 55'*>7-(4-[2-{2-chIoro-4,5-dmiethyIphenoxy)ethoxy]phenyI}-6-[cyclopropyl-(3,5-dimethoxyb6nzyI)carbamoyl]-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl}-5-oxopentaiioic acid methyl ester;
irac.y5-{(IR*, 55*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[2-(2-chloro-4.5-
dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non.-6-eii-3-yl)-2,2-diraethyl-S-oxopentanoic acid;
{rac,yS-{{lR*, 55*)-7-{4-[2-(2-chloro-4,5-dimethylphenQxy)ethoxy]pheayl}-6-[cyclopropyl-(2-methyIbenzyl)carbamoyi]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dLmethyl-5-oxopentanoic acid;
(rac.y5-((IR* J5*)-7-{4-[2-(2-chloro-4,5-dimethyIphenoxy)ethoxy]phenyI}-6-{cyclopropyi-[2-(3,4-diinethylphenoxy)ethyl]carbamoyI}-3,9-diazabicyclo[3.3.1]-non-6-eii-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
(rac.yS-iilR*, J5*)-7-{4-[2-(2-chloro-4,5-dimethy]phenoxy)ethoxy]phenyl}-6-(cyclopropylphenethykarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-2,2-dimethyl-S-oxopentanoic acid;
(rac.yS-iilR*, JS*>7-{4-[2-(2-cliloro^,5-diinethylph6noxy)ethoxy]pbenyl)-6-{[2-(2-chlorophenyI)ethyl]cyclopropylcaibanioyl} -3,9-diazabicyclo[3.3.1 ]non-6-
eii-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
(rac.yS-dJR*, J.S*)-7-{4-[2-(2-cliloro-4,5-dimethyIphenoxy)ethoxy]phenyl}-6-{[2-(2,3-difluorophenyI)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-
6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;
(rac.y5-((lR*. J5'*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-
{[2-(4-fluorophenyl)ethyl]cycIopropylcarfaamoyl}-3,9-diazabicyclo[3.3.1]noii-6-
ea-3-yl)-2,2-dimethyI-5-oxopentanoicacid;

irac.)'5-((JR*. 5S*)-7-{4-[2-(2-chloro-4,5-diinethyIphenoxy)ethoxy]phenyl}'6-{[2-(2-methylphenyl)ethyI]cycIopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
irac.)-5'((lR*. 55*)-7-(4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-{4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
(rac.yS-iilR*, J5*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy}ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybeiizyl)carbamoyl]-3,9-diazabicyc!o[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic acid;
(rac.yOR*. J5*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-
phenoxy)etboxy]plienyl}-3,9-diazabicyclo[3.3.1]nDn-6-ene-6-carboxylic acid (2-clilorobenzyl)cyclopropylamide;
(rac.y(]R*. Ji?*)-3-(4-carbamoylbutyryl)-7-{4-[2-{2-cliloro-4,5-dimethyl-
phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid
benzylcyclopropylamide;
(rac.y(lR*, J5*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-
phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyUc acid (2-chlorobenzyl)ethylamide;
(rac.y(lR* 55*)-3-(4-carbamoylbutyryI)-7-{4-[2-(2-chloro-4,5'dimetfayl-
phenoxy)ethoxy]phenyl) -3,9-diazabicyclo[3.3.1 ]non-6-ene-6-carboxylic acid
cyclopropyl-(2-fluorobenzyl)amide;
(raay{IR*. 55*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-
phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid
cyclopropyI-(3-trifluoromethylbeiizyl)amide;

{rac.)-{lR*. 55*)-3-(4-carbaraoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyI-
phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid
cyclopropyl-(2-raethylbeiizyl)amide;
5 irac.)-{lR*, ->5*)-3-(4-carbamoyIbutyryl)'7-{4-[2-(2-chloro-4,5-diraethyl-
phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid
cyclopropyl-[2-(4-methoxyphenoxy)ethyl] amide;
{rac.y{lR*. i5*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethy]-
) plienoxy)ethoxy]phenyii-3,9-diazabiGyclo[3.3.1]non-6-ene-6-carboxylic acid
cyclopropylphenethylamide;
{rac.yilR', 5S*)-3-(4-caibamoylbutyryl)-7-{4-[2-(2-cliloro-4,5-dimelhyl-
phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1 ]non-6-ene-6-carboxylic acid [2-(2-chlorophenyl)ethyl]cyclopropylamide;
(rac.)'(JR*. 5,S'*)-3-(4-carbamoyIbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-
phenoxy)ethoxy]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid
cyclopropyl-[2-(2,3-difiuorophenyl)ethyl]ainide;
{rac.)-QR*, 55*)-3-(4-carbamoylbutyryl)-7-{4^[2-(2-chloro-4,5-diinethyl-
phenoxy)ethoxy]pIienyl} -3,9-diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid
cyclopropyI-[2-(4-fluorophenyl)ethyl]amide;
(rac.)-(JR * J6'*)-3-(4-carbamoyIbutyryl)-7- {4-[2-(2-chloro-4,5-diinetbyl-
pheuoxy)ethoxy]phenyl} -3,9-diazabicycIo[3.3.1 ]iion-6-ene-6-carboxylic acid
cycloprop yI-(2 -o-tolylethyl)amide;
{rac.)-(IR *, 5.S'*)-3-(4-carbamoylbutyryi)-7- {4-[2-(2-chIoro-4,5-dimethyl-
phenoxy)ethoxy]phenyl)-3,9-diazabicyGlo[3.3.1]non-6-ene-6-carboxy!ic acid
cyclopropyl-(2-/j-tolylethyl)amide;

(rac.HIR*, 55*)-3-(4-carbamoylbutyryl)-7-{4-[2-{2-chloro-4,5-dimethyl-
phenoxy)ethoxy]phenyl}-3,9-diazabicycIo[3.3,l]non-6-ene-6-carboxylic acid
cyclopropyl-(3,5-diniethoxybenzyl)amide;
l:l-mixture of (rac.)-{3R*y5-{{lR*, 55*)-6-[(2-chlorobenzyl)cyclopropyU carbamoyl]-?-{4-[2-(2-chloro-4,5-dimethy]phenoxy)ethoxy]phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-en-3-yI)-3-hydroxy-5-oxopentanoic acid and (rac.)-(?S*)-5-((IR*, 55*)-6-[(2-chIorobenzyl)cyclopropyIcarbamoyI]-7-{4-[2-(2-chloro-4,5-diniethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yi)-3-hydroxy-5-oxopentanoic acid;
l:l-mixtuTe of {rac.)-{3R*)-5-{{lR*, 55*)-6-[(2-ch]orobeiizyI)ethylcaTbamoyl]-7-{4-[2-(2-chloro-4,5-diniethyIphenoxy)ethoxy]phenyI}-3,9-diazabicyclo[3.3.1]-non-6-eii-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.)-{3S*y5-((iR*, 55'*)-6-[(2-clilorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)' ethoxy]phenyl}-3,9-diazafaicyclo[3.3.1]-non-6-en-3-yI)-3-hydroxy-5-oxo-pentanoic acid;
l:l-mixtiire of {rac.H3R*y5-{OR* 55*)-7-{4-[2-{2-chloro-4,5-dimethyl-
phenoxy)ethoxy]phenyl}-6-[cyclopropy!-(2-fluoroben2yl)carbamoyl]-3,9-diaza-
bicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid and (rac.)-(55*>5-
{(IR*. J5*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)etfaoxy]phenyI}-6-
[cyclopropyl-(2-fIuorobenzyI)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of (rac.y(3R*y5-[(lR* 55'*)-7-{4-[2-(2-chloro-4,5-diDiethyl-phenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethyIben2yl)carbanioyI]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-liydioxy-5-oxopentanoic acid and (rac.y i3S*y5-{{lR*. 55*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-pheriyl}-6-[cyclopropyl-(3-trifluormethylobenzyl)carbamoyl]-3,9-diazabicycI-o[3.3.1]iion-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid;

1:1 -mixture of (rac. )-(3R *)-5-((iJ; * 5S*)-7- (4-[2-(2-chloro-4,5-dimetIiyl-phenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]noii-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid aiid (rac,)-(3S*)-5-((JR*. J5'*)-7-{4-[2-(2-chlorO'4,5-dimetliyIphenoxy)-ethoxylphenyl}-6-{cyclopTopyl-[2-(4-methoxyphenoxy)ettiyL]carbamoyl}-3,9-diazabicyclo[3.3.1]iion-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of (roc.V(3ii*)-5-[(iK*, 5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-(cyclopropylphenethyIcarbamoyi)-3,9-diazabicyclo-[3.3.1]non~6-en-3-yi]-3-hydroxy-5-oxopentanoic acid and (rac.)-(3S'^)-5-[(lR*, 55*)-7-{4-[2-(2-chloro-4,5-dimetliylpheaoxy)ethoxy]phenyl}-6-(cyclopropyI-phenethylcarbamoyl)-3,9-diazabicyclo-[3.3.1]non-6-en-3-yJ]-3-hydroxy-5-oxopentanoic acid;
1:1 -mixture of (rac. y(3R *)-5-((]R * 55*)-7- {4-[2-(2-chloro-4,5-dimethyI-phenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyI]cyclopropylcarbanioyI}-3,9-dia2abicyclo[3.3.1]non-6-eu-3-yI)-3-!iydroxy-5-oxopentanoic acid and (rac.y (3R*)-5-((JR*, 55*)-7-{4-[2-(2-chloro-4,5-dimetbylphenoxy)ethoxy]pheny]}-6-{[2-(2-chlorophenyI)ethy]]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5HDxopentanoic acid;
l:l-mixture of (rac.y(3R*)-5-((]R*, J5*)-7-{4-[2-(2-cIiloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-{cyc]opropyl-[2-(2,3-difluoropIienyl)efliyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]uon-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.y(3S*y5-(0R*, 5^*)-7-{4-[2-(2-chloro-4,5-diinethylphenoxy)-
ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbanioyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of (rac.y(3R*y5-{(JR*. 55*)-7-{4-[2-(2-chloro-4,5-dimethyI-phenoxy)ethoxy]pheiiyl}-6-{cyclopropyI-[2-{4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and {rac.y (3S*y5-(OR*, 55'*)-7-{4-[2-(2'Chloro-4,5-dimethyIphenoxy)ethoxy]phenyl}-6-

(cyclopropyl-[2-{4-fluorophenyl)etbyl]carbamoyl}-3,9-diazabicyclo[33.1]non-6' eii-3-yl)-3-hydToxy-5-oxopentanoic acid;
1:1 -mixture of (rac.)-(3R *)-5- {(]R * 5S*)-7- {4-[2-(2-chloro-4,5-dimethyl-
phenoxy)ethoxy]phenyl}-6-[cyclopropyl{2-o-toIylethyl)carbamoyl]-3,9-diaza-
bicycio[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid and (rac.)-(3S*y5-
{(IR*, J5*)-7-{4-[2-{2-chIoro-4,5-dimethylphenoxy)ethoxy]phenyI}-6-
[cyclopropyl(2-ci-tolylethyl)carbamoyI]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid;
1:1 -mixture of (rac. )-(3R *)'5- {(IR *, 55*)-?- {4-[2-(2-chloro-4,5-dimetliyl-
phenoxy)ethoxy]pheiiy!}-6-[cyclopropyl(2-p-tolylethyl)carbamoyl]-3,9-diaza-
bicyclo[3.3.I]non-6-en-3-yI}-3-hydroxy-5-oxopeatanoic acid and (rac.)-(3S*y5-
{(IR*. 55*)-7-{4-[2-(2-chloro-4,5'dimethylphenoxy)ethoxy]phenyl}-6-
[cyclopropyl(2-p-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid;
1:1 -mixture of (rac.y(3R *)-5- {(Jii*, 5S*)-7- {4-[2-(2-chloro-4,5-dimethyl' phenoxy)ethoxy]pheiiyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid and (rac.)-(3S*y5- {(IR * 55*)-?- {4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl} -6-[cyclopropyl-(3,5-diinethoxyben2;yl)caibamoyl]-3,9-diazabicycIo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of (IR. J5>7-{4-[2-(2-chloro-4,5-diinethyIpbenoxy)ethoxy]phenyl}-
3-((25, '/i!)-4-hydroxypyirolidine-2-caibonyl)-3,9-diazabicycIo[3.3.1]non-6-ene-
6-carboxylic acid {2-chlorobenzyi)cyclopropylamide and (JS. 5J?)-7-{4-[2-(2-
cbIoro-4,5-dimethylpbenoxy)ethoxy]phenyl}-3-((25, carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-
chloroben2yl)cycIopropylamide;

l:l-mixture of (IR, J'5)-7-{4-[2-(2-chloro-4,5-dimethyIphenoxy)ethoxy]phenyl}-3-((25', 4R)-4-liydroxypyrroUdine-2-carbonyl)-3,9-dia2abicyclo[33.l]non-6-ene-6-carboxy!ic acid cyclopropyl-(2-methylbenzyl)aniide and {IS, 5S)-7-{4-[2-{2-chloro-4,5-dimethyIphenoxy)ethoxy]phenyI}-3-{(25, ^i;)-4-hydroxypyrroIidine-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid cyclopropyl-(2-methylbenzyl) amide;
(rac.)-(lR*. 55*)-3-acelyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabioyclo[3.3.1]iion-6-ene-6-carboxylic acid [2-(2-chloTophenyi)ethyl}-cyclopropylamide;
{rac.)-{lR*. 55*)-3-acetyl-7-{4-[2-(2,3,5-triinethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyiic acid cyclopropylphenethylamide;
(rac.)-(JR*. J5'*)-3-acetyl-7-{4-[2-(2,3,5-tTimethylphenoxy)ethyI]phenyl}-3,9-diazabicyclo[3.3.1]iion-6-ene-6-carboxylic acid cyclopropyl-[2-(2,3-difluoro-phenyl)ethyl] amide;
{rac.HlR*, 55*)-3-acetyt-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-dia2abicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,5-diinethoxy-benzyl)amide;
iracyQR*, 55*)-3-acetyl-7-{4-[2-(2,3,5-triinethylphenoxy)ethyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxyIic acid cyclopropyI-(2-/>-tolylethyl)-amide;
(rac.)-(lR*, 55*)-3-acctyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyI]pheayI}-3,9-dia2abicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-[2-(2-hydroxyethyl)-benzyl] amide;

(rac)-(iS* 55*)-3-acetyl-7-{4-[2-{2-chloro-4,5-dimethylphenoxy)ethoxy]-
phenyl}-3,9-diazabicyc]o[3.3.1]non-6-ene-6-carboxyIic acid cycIopropyl-[2-{2-hydro xyethyl)benzyi] amide;
(rac.)-5-((Jfi*, JS*)-6-(cyclopropylphenethylcarbamoyl)-7-{4-[2-(2,3,5-trimethyl-
phenoxy)ethyI]phenyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic
acid;
{rac.)-5-((IR*, J5*)-6-{i;2-(2 (rac.yS-iOR*, 55*)-6-{cyclopropy]-[2-(2,3-difluoropheny!)ethyl]carbainoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yi)-5-oxopeiitanoic acid;
(rac.y5-((]R*, 5iS*)-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyi}.7-{4-[2-(2,3,5-trimethyi-phenoxy)ethyI]phenyl}-3,9-diazabicyclo[3.3.I]noii-6-en-3-yl)-5-oxopentanoic acid;
(rac.y5-i(_lR*. 55*)-6-[cyclopTopyl-(2-o-tolylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid;
1: l-mixture of (rac. y5-((lR *. i5*}-6-[cyclopropyl-((2J; *)-2-hydroxy-2-phenyleiiiyl)carbamoyI]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid and (rac.)-5-{(iif*, 5S*y 6-[cyclopropyl-((25*)-2-hydroxy-2-phenylethyl)carbamoyl]-7-{4-[2-(2,3,5-lTimethylphenoxy)ethyl]phenyl}-3,9-diazabicycIo-[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid;

(rac.)-5-((]R*, 55*)-6-{cyclopropyl-[2-(2-hydroxyetiayl)beiizyl]carbamoyl}-7-{4-[2-(2,3,5-trimethy!pbenoxy)ethyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid;
{rac.)-5-({lR*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]pheiiyl}-6-
{cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyc]o[3.3.1]-non-6-en-3-yl)-5-oxopentanoic acid;
{rac.)-5-((IR*, J5'*)-6-{[2'(2-chloropheDyl)ethyl]cycIopropylcarbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)et]iyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-S-oxopentanoic acid;
{rac.)-5-i{}R*. 5S*)-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoy]}-7-
{4-[2-{2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-
yl)-2,2-dimethyl-5-oxopentajioicacid;
(rac.yS'dlR*, 55*)-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbainoy]}-7-{4-[2-{2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]noii-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
{rac.y5-(_(lR*. 5S»)-6-[cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]aon-6-en-3-yI)-2^-dimethyl-5-oxopentanoic acid;
(rac.y5-((IR*. 55*)-6-[cyclopropyl-(2-;7-tolylethyl)carbamoyl]-7-{4-[2-(2,3,5-triinethylphenoxy)ethyl]phenyl} -3,9-diazabicyclo[3.3. l]iion-6-en-3 -yi)-2,2-dimethyl-5-oxopentanoic acid;
(rac.y5~({lR*, J5'*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-dia2abicycio[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

(rac,)-5-i(lR*, J5*>7-{4-[2-{2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)ben2yl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyI-5-oxopentanoic acid;
(rac.)-{}R*, 55*)"3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-
ethyl]phenyi}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-phenethylamide;
(rac.y(lR*. 55*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-triniethylphenoxy)ethyl]-phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid [2-(2-chloFo-pheny!)-ethyl] eye lopropylamide;
(rac.)-{lR*, J5*)-3-(4-carbamoylbutyry])-7-{4-[2-{2,3,5-trimethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-[2-(2,3-difluorophenyl)ethy!] amide;
(rac.y(lR*, 5>y*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-triniethylphenoxy)ethyl]-phenyl}-3,9-diazabicycio[3,3.1 ]non-6-ene-6-carboxylic acid cyclopropyl-[2-(4-fluorophenyt)ethyl] amide;
{rac.y{lR*, J5'*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyI-(3,5-dimethoxybenzyl)amide;
(rac.yiJR*, 55'*)-3-(4-carbamoylbutyry])-7-{4-[2-(2,3,5-trimethytphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2-p-tolylethyl)amide;
(rac.yUR*', J5*)-3-{4-carbamoyIbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)ethyI]-phenyl}-3,9-dia2abicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-[2-(2-hydroxyethyI)beiizyl] amide;

{rac.)-{lR*. 55*)-3-(4-carbainoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyI-
phenoxy)ethoxy]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxyUc acid
cycIopropyl-[2-(2-hydroxyethyl)benzyiJamide;
(rac.)-acetic acid {IR*, 55*)-2-(2-{[(3-acetyl-7-{4-[2-(2,3,5-trimetliylphenoxy-)ethyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carbonyl)cyclopropylamino]-methyl}phenyl)ethyl ester;
{rac.)-acetic acid {IR*, 55*)-2-(2-{[(3-acetyI-7-{4-[2-(2-cliloro-4,5-dimethyl-phenoxy)ethoxy]phenyi}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carbonyl)-cyclopropylamiiio]methyl}phenyi)ethyl ester;
(rac.)'{lR*, 55'*)-7-{4-[2-(2,3,5-triinethylphenoxy)etiiyl]phenyl}-3,9-diaza-
bicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-[2-(4-fluorophenyl)ethyl]-amide;
(rac.)-(IR*. i5'*)-7-{4-[2-(2,3,5-trimethylphenoxy)etbyl]phenyl}-3,9-diaza-
bicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,5-dimethoxybeazyl)-amide;
(rac.)-acetic acid {IR*. 55*)-2-(2-([(3-acetyl-7-{4-[2-(4-bromopheiioxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboayl)cyclopropylainino]methyl}-phenyl)ethyl ester;
1:1 mixture of (rac.y5-{ilR*. 5iS'*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-6-[((2i;*)-2-hydroxy-2-phenylethyl)metl)ylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,2-dimethyi~5-oxopent3noic acid and (rac.)-5-{(lR*. 55*)-7-{4-[2-(2-cliloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[((25*> 2-liydroxy-2-phenylethyI)methylcarbainoyl]-3,9-dia2:abicyclo-[3.3.1]non-6-en-3-yl}-2,2-dimetliyl-5-oxopentanoicacid;

{rac.yOR*. 5S*)-3-acetyl-7-{4-[3-(2-broino-5-fluoTophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.!]non-6-ene-6-carboxy!ic acid (2-chlorobenzyl)cyclopropyl-amide;
irac.)-{}R*, 55*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diaza-
bicycIo[3.3,l]non-6-ene-6-carboxylic acid benzylcyclopropylamide;
(rac.y{JR*, 55*)-7-{4-[3-(2,3,6~trifluoropheROxy)propyl]phenyI}-3,9-diaza.
bicyclo[3.3,l]non-6-ene-6-carboxylic acidcyclopropyl-(2-fluorobeiizyl)amide;
(rac.y(JR*. 5.S'*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diaza-
bicyclo[3.3.13non-6-ene-6-carboxylic acid cyclopropyl-(3-trifluorometliylbenzyl)-araide;
(rac.y(]R*, 55*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-diaza-
bicyclo[3.3.1]non-6-ene-6-carboxylic acidcycIopropyl-(2-methylben2yl)amide;
(rac.yUR*, 55*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyI}-3,9-diaza-
bicyclo[3.3.1 ]nQE-6-ene-6-carboxyUc acid cyclopropyl-[2-(4-methoKypheiioxy)-ethyl] amide;
(rac.y(JR*. i5*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-diaza-
bicyclo[3.3.1]non-6-eiie-6-carboxylic acid (2-(2-chlorophenyl)ethyl]cyclopropyl-amide;
{racyiJR*. J5*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diaza-
bicyclo[3.3.1]iion-6-ene-6-carboxylic acid cycIopropyl-[2-(2,3-difluorophenyl)-ethyl]ainide;
{rac.yilR*. 5S*V7-{4-[3-(2,3,6-tdfluoropbeiioxy)propyllptieiiyl5-3,9-dia2,a-
bicyclo[3.3.I]non-6-ene-6-carboxylic acid cyclopropyl-(2-o-tolylethyI)amid6;

{rac.)~(JR*, J5'*)-7-(4-[3-(2,3,6-trif]uoropbenoxy)propyl]phenyl}-3,9-diaza-
bicyclo[3.3.1]aon-6-ene-6-carboxylic ac!dcyclopropyl-(2-/j-tolyIethyl)amide;
{rac,)-(i-R*, Ji'*)-3-acetyl-7-{4-[3-(2,5-dif]uorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.l]non-6-eue-6'CarboxyUc acid (2-chlotobenzyl)cyclopropyl-amide;
{rac.)-{]R*, J5*)-3-acetyI-7-{4-[3-(2,3-dichlorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]noii-6-ene-6-carboxylic acid (2-chlorobenzyl)cyclopropyl-amide;
{rac.)-{lli*. Ji?*)-3-acetyl-7-{4-[3'(2-chloro-5-f]uorophenoxy)propyl]pheDyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid (2-chlorobenzyl)cyclQpropyl-amide;
{rac.yUR*, 5iS*)-3-acetyl-7-{4-[3-{3-cyanopyridiii-2-yloxy)propyl]phenyU-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)cyclopropyl-amide;
{rac.)-{lR*, JS*)-3-acetyl-7-{4-[2-(2,3-dimetliylphenoxy)ethyl]phenyl}-3,9-
dia2abicyclo[3.3.1 ]non-6-ene-6-carboxyUc acid (2-chlorobenzyl)cyclopropyl-amide;
(rac.yU^*. 5S*)-3-acetyl-7-{4-[2-(2,5-dimethylphenoxy)ethyl]phenyl)-3,9-
diazabicyclo[3.3.11non-6-eiie-6-carboxyIic acid (2-chloroben2yl)cyclopropyl-amide;
{rac.)-{}R*. 5S*)-3-acetyl-7-{4-[2-(2-cMoro-4,5-dime1iiylplienoxy)eliiyl]-
phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxy]ic acid {2-chloroben2yl)-cyclopropylamide;

{rac.)-{IR*, 55*)-3-ac6tyl-7-{4-[2-(2,4-dichlorophenoxy)ethyI]pheny!}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxyl!cacid(2~chlorobenzyI)cyclopropylamide;
(mc.)-(IJi*, 55*)-3-acetyI-7-{4-[2-(2,3-dichIorophenoxy)ethyl]phenyl}-3,9-diaza-bicycIo[3.3. l]non-6-ene-6-carboxylic acid (2-chlorobenzy!)cyciopropyiamide;
{rac.y{IR*, 5S'^)-3'acetyl-7-(4-[2-(2,6-difluorophenoxy)ethyl]phenyI}-3,9-diaxa-bicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)cyclopropyiajnide;
(rac.)'{JR*, 55*)-3-acetyl-7-{4-[2-{2,5-difluorophenoxy)ethyl]phenyl}-3,9-diaza-bicycIo[3.3.1]non-6-ene-6-carboxylic acid(2-chlorobenzy])cyclopropyiainide;
(rac.yilR*, 5S*)-3-acetyl-7-{4-[2-(3,5-dichlorophenDxy)eihyl]phenyl}-3,9-diaza-bicyclo[3,3.1]non-6-ene-6-carboxylic acid(2-chlorobenzyl)cyclopropylamide;
{rac.)-{m*, i5*)-3-acetyl-7-{4'[2-(2-chloro-5'methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chloroben2yl)cyciopropyl-amide;
{rac.)-{lR*, ^5*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethyl]ph6nyl}-3,9-diazabicyclo[3.3.1]noa-6-en6-6-carboxylic acid (2-chlorobenzyI)cyclopropyl-amide;
(j-ac.)-{lR*, 55*)-3-acetyl-7-{4-[2-(23,6-trichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]noii-6-ene-6-carboxyUc acid (2-chloToben2;yI)cyclDpiopyl-
amide;
{rac.)-{lR*, J5*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)pTopyl]phenyl}-3,9-dia2abicyclo[3.3. l]noD-6-ene-6-carboxy]ic acid cyclopropyl-(2-methoxyben2yl)-amide;

(rac.]-{!R*, 5S*)-3-acetyl-7-{4-[3-(23,6-trifluorophenoxy)propyi]pheiiyl}-3,9-diazabicyclo[3.3.1]noa-6-eae-6-caiboxylic acidcyclopropyl-(5-fluoro-2-methoxy-be!izyl)amide;
{rac.y{lR*. 55*)-3-acetyl-7-{4-[3-(23,6-trifluorophenoKy)propyl]phenyl}-3,9-diazabicyGlo[3.3.1]noD-6-ene-6-carboxyUc acid cyc!opropyl-(2,6-difiuoro-benzyl)ainide;
{rac.y{lR*. JS*)-3-acetyi-7-{4-[3-(2,3,6-trifluorophenoxy)propy[]phenyi}-3,9-diazabicyclo[3.3.i]non-6-ene-6-carboxylic acid cyclopropyi-(3-fluoro-2-iD.etliyl-benzyl)amide;
(rac.)-(ifi* 55*V3-acetyl-7-{4-[3-(2,3,6-trifluoropheaoxy)prQpyl]plienyl}-3,9-dia2abicycIo[3.3.l]non-6-ene-6-carboxylic acid (2-chloro-3,6-difluQrob6n2yl)-cyclopropylamide;
{rac.y(lR*. ii?*)-3-acetyl-7-(4-[3-(2,3,6-trifluoropheiioxy)propyl]pheiiyl}-3,9-diazabicyclo[3.3.1]non-6-eiie-6-carboxylic acid cyclopropyI-(2,3-difluoro-benzyl)amide;
(rac.)-(ifi* 55'*)-3-acetyl-7-{4-[3'(2.3,6-trifluorophenoxy)propyI]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropy]-(4-fluorobenzyI)-amide;
(rac.y(JR*, J^*)-7-(4-[3-(2-bromo-5-iluorophenoxy)propyl]phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-ciiiorobenzyl)ethylamide;
{rac.y(lR*, 55*)-7-{4-[3-(2-bromo-5-fluoropheDOxy)propyl]phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyi-(3,5-dimethoxybenzyl)-amide;

(rac.}-(JR*, 55'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diaza-bicyclo[3.3.1]Tion-6-ene-6-carboxyIic acid cyclopropyl-(2-methylbenzyl)arnide;
{rac)-{lR-*. Ji'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]plienyI}-3,9-diaza-bicyclo[3.3.1]non'6-ene-6-carboxylic acid cyclopropyl-[2-(4-inethoxypheiioxy)-ethyl] amide;
{rac.)'{IR*, 55'*)-3-methyl-7-{4-[3-{2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyI)cyclopropyl-araide;
{rac.)-{lR*, J5'*)-3-ethyl-7'{4-[3-(23,6'trifluorophenoxy)propyljphenyl}-3,9-dia2abicyclo[3.3.l3non-6'ene-6-carboxylic acid (2-chlorobenzyl)cyclopropyl-aiiiide;
(rac.yOR*, 55'*)-3-(2-ainiiioacetyl)-7-(4-[3-(2,3,6-trifiuorophenoxy)pTopyI]-
phenyl}-3,9-dia2abicycIo[3.3.1]non-6-ene-6-carboxyIic acid (2-chlorobenzyl)-cyclopropylamide;
{rac.)-{lR*, i.S'*)-3-(3-aiiiiiiopropionyI)-7-{4-[3-(2,3,6-trifIuorophenoxy)-propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (l-chlorobenzyl)-cyclopropylamide;
{rac.y{lR*, i,S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)-
cyclopropylamide;
(rac.)-(i-fi*, J5*)-3-acetyl-7-(4-[2-(2-bromo-5-fluoroplienoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxy5ic acid (2-chloro-3-trifluoro-methyIbenzyl)cyciopropylaniide;

irac.)-{JR*, 5S*)-3-acetyi-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]p!ienyl}-3,9-
diazabicyclo-[3.3,l]non-6-ene-6-carboxylic acid (2-bromobenzyl)-
cyclopropylamide;
{rac.)-{}R*, 5S*)-3-acetyl-7-i^4-[2-(2-bromo-5-fluorophenoxy)ethoxy]pbenyl}-3,9-diazabicycio[3.3.I]non-6-ene-6-carboxylic acid cyc]opropyl-(2,3-dimethyl-benzyi)amide;
{rac:)-{lR*, 55*)-3-acetyI'7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabiGyclo[3.3.1 ]ii,on-6-ene-6-carboKy!ic acid (2-chloro-3-trifluoroinethyl-benzyl)cyclopropylaraide;
(rac.y(lR*. ii'*)-3-acetyl-7-{4-[2-{2-chloro-4,5-diraethylphenoxy)ethoxy]-
pheny\}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid (3-chloTobenzyl)-cyclopropylamide;
{rac.)-{lR*, J5*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyI}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxyHc acid(2-chlorobenzyl)ethylaniide;
{rac.)-{lR*. i5'*)-3-acetyl-7'{4-[2-(2-chloro-5-f]uorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-bromob6nzyI)cyclo-propylamide;
{rac.)-OR*. 5i^*)-3-acetyl-7-{4-[2-(4-chloro-2-inethylphenoxy)ethoxy]-phenyl}-
3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cycIopropyl-(2,3-
dichloroben2yl)amide;
(rac.)-(i-R*, 55*)-3-acetyl-7-{4-[2-(2-cMoro-4,5-dimethylphenoxy)ethoxy]-
phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3-inethoxybenzyl)anude;

(fac.)-(IR*, 55'*)'3-acetyl-7-{4-[2-(2-bromo-5'fluorQphenoxy)ethoxy]-phenyl}-
3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid {2-bromobenzyl)-
cyclopropylamide;
(rac.)-{lR*, 55*)-3-acetyl-7-{4-[2-(4-chloro-2-fnethylphenoxy)ethoxy]-phenyl}-
3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cycIopropyI-(2,3-
diinethylben2yl)aniide;
(rac.)-(JR*, J^*)-3-acelyi-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]pheny]}-3,9~ diazabicyclo[33.1]non-6-ene-6-carboxylic acid cyclopropyl-(3-metlioxy' benzyl)amide;
{rac.yim*, 55*)-3-acetyl-7-{4-[2-(2-cbloro-4,5-dimethylphenoxy)ethoxy]-
phenyl}-3,9-diazabicycIo[3.3.1]noii-6-ene-6-carboxylic acid cyclopropy]-(2-fluoro-5-methoxybenzy! )amide;
{rac.)-{}R*, 55*)-3-acety]-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-pheny]}-
3,9-diazabicycIo[3.3,l]non-6-ene-6-carboxyIic acid (2-bromobenzyi)-
cyclopropylamide;
{rac.)-{lR\ 55*)-3-acetyl-7-(4-[2-(2-chloro-5-fl:uorophenQxy)ethoxy]pheuyl}-
3,9-dia2abicycio[3.3.1]non-6-ene-6-caiboxylic acid (2-chiorobeiizyl)-
cyclopropylamide;
{rac.)-{lR*. 55*)-3-Acetyl-7-{4-[2-(2,4,5-bichlorophenoxy)ethoxy]phenyl)-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,5-
dimethoxyben2yl)aniide;
{rac.)-{IR*. i3'*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non.-6-ene-6-carboxy[ic acid (2-broniobenzyl)cyc[oprQpy]-amide;

{rac.)-{]R*. 35*)-3-acetyl-7-{4-[2-(2-chloro-4,5-diraethylphenoxy)6thoxy]-
phenyI}-3,9-diazabicycio[3.3.1]non-6-ene-6-carboxyIic acid (6-ch.ioro-
benzo[l,3]dioxol-5-\'lmethyl)-cyclopropylamide;
{rac.yUR*, 55*)-3'acetyl-7-{4-[2-(2,3-dichIorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobeiizyl)cyclopropyl-amide;
(7-ac.)-iIR*. J5*)-3-acetyl-7-(4-[2-(4-chlorO'2-methyiphenoxy)ethoxy]-phenyI}-
3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chloro-3-
trifluoromethylben2yl)cyclopropylarmde;
(rac.)-(JR*, 5>S'*)-3-acetyl-7-{4-[2-{2-chloro-4,5-dimethylphenoxy)ethoxy]-
phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyiic acid cyclopropyl-(3-methylbenzyl)amide;
(rac.y(JR*, 55*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]pheny!}-3,9-d:azabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobeiizyI)ethylamide;
(rac.y{lR*. 5^*)-3-acetyl-7-{4-[2-(2-chloro-5-fIuoropheiioxy)etboxy]pheiiyl}-3,9-dia2abicyclo[3.3.1]noa-6-ene-6-carboxylic acid cyclopropyl-(2-fluoro-5-methoxybeiizyI)armde;
{rac.y{lR*, J5*)-3-acetyI-7-{4-[2-(4-chloro-2-methylpi2enoxy)ethoxy]-phenyl}-
3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)-
cyclopropylamide;
{rac.y(lR*, 55*)-3-acetyl-7-{4-[2-(2-bromo-5-fluoropheiioxy)ethoxy]-pheiiyl}-
3,9-diazabicycio[3.3.1]non-6-ene-6-carboxylic acid cyclopropy)-(3,5-
dimethoxybenzyI)aniide;

(rac.)-(lR*, 55*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]-phenyl}-
3,9-dia2abicycIof3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3-
methoxybenzyl)amide;
{rac.yilR*, 55*)-3-acetyl-7-{4-[2-(2,4,5-trichloTophenoxy)ethoxy]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (3-chloroben2yI)-
cyciopropyl amide;
(rac.y(lR*, 5>?*)-3-acetyl-7'{4-[2-{2,6-dichloro-4-methylphenoxy-ethoxy]-
phenyl}-3,9-diazabicyclo[3.3.I]non-6-ene-6-carboxylic acid cyclopropyI-(3,5-difluorobenzyl)amide;
(rac.)-(lR*, 55'*)-3-acetyl-7-{4-[2-{2,4,5-trichlorophenoxy)ethoxy]pheQyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-caiboxyUc acid cyclopropyl-(2-fluoro-5-methoxybea2yl)amide;
(rac.)-(lR*, 55*)-3-acetyI-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxyUc acid cyclopropyl-(3,4-
diinetboxybenzyl)aimde;
(rac.y{}R*, 55'*)-3-acetyl-7-{4-[2-{2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6'Carboxylic acid (6-chloro-benzo[l,3]-dioxol-5-ylinethyl)cyclopropylamide;
(rac.)-(JR*. J5*)-3-Acetyl-7-{4-[2-(2-bromo-5-fIuorophenoxy)ethoxy]phenyl}-
3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyiic acid (3-chlorobenzyl)-
cyclopropylamide;
{rac.)-{lR*. 55'*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]plienyl}-3,9-diazabicyclo[3.3.1 ]non-6-ene-6-carboxylic acid cycIopropyI-(3,4-diinethoxy-benzyl)amide;

{rac.yilR*. 55*>3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl)-3,9-diazabicyclo[3.3.I]non-6-ene-6-carboxylicacid(2-chioroben2yI)-ethyIamide;
{rac.)-(IR*. 55*)-3-acetyl-7-{4-[2-(4-chloio-2-methylphenoxy)ethoxy]-pheiiyl}-
3,9-diazabicycLo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,5-
dimethoxyben2yl)amide;
(rac.)-(IR*, J5'*)-3-acetyl-7-{4-[2-(2,4,5-tricMorophenoxy)ethoxy]phenyl}-3,9-
dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3-methyl-
benzyl)amide;
{rac.)-{lR*, 5S*)-3-acetyl-7-(4-[2-(2,3-dichlorophenQxy)etiioxy]plienyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid cycIopropyl-(2-fluorO'5-raethoxybenzyI)amide;
(rac.yUR*, 55*)'3-acetyl-7-{4-[2-(2-chloro-4,5-dim6thylphenoxy)ethoxy]-
phenyl}-3,9-diazabicyclo[3.3.1]non-6-eae-6-caiboxylic acid cyclopropyl-(3,5-difluorobenzyl)amide;
(rac.y(]R* i5*)-3-acetyl-7-{4-[2-(2,3-dichIorophenoxy)ethoxy]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-eiie-6-carboxylic acid cyclopropyl-(3,5-dimethoxy-beiizyl)amide;
irac.)-{lR*. i.S'*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]-phenyl}-
3,9-diazabicyclo[3.3.1]non-6-erLe-6-catbQxylic acid (2-chlorobeiizyl)-
cyclopropyiamide;
{rac.)-{lR*, 5S*)-3-acetyl-7-{4-[2-(2-bromo-5-f!uorophenoxy)ethoxy]-phenyl}-
3,9-diazabicyclo[3.3.I]noa-6-ene-6-carboxyIic acid (2-chIorobeii2yi)-
cyclopropylamide;

(rac.)-(]R*, 55*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-
phenyl}-3,9-diazabicyclo[3.3.1]noii-6-ene-6-carboxylic acid cycIopropyl-(3,4-dimethoxybetizyl)amide;
{rac.yilR*. 5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-
phenyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyHc acid cyclopropyl-(3-trifluoromethoxybenzyOami de;
{rac.)-(lR*. J5'*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyI}-
3,9-diazabicyclo[3-3.1]non-6-ene-6-carboxyIic acid cyclopropyl-(3-
inethylbenzyl)ainide;
(rac. )-(-/-«*, 55*)-3-acetyl'7-{4-[2-{2-chloro-5-f]uorophenoxy)ethoxy]phenyl}-
3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,5-
dimethoxybenzyl)amide;
{rac.)-{}R*, 55'*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)etlioxy]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyI-(3-methyl-
ben2yl)amide;
{rac.)-(lR*, 55*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2-fluoro-5-methoxybenzyI)amide;
(rac.y(JR*. J5*)-3-acetyl-7-{4-[2-(2-bromo-5-£luorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid(2-chlorobenzyl)ethylamide;
{rac.)-(]R*. 55*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)etboxy]phenyl}-3,9-dia2abicycIo[3.3.1]non-6-ene-6-carboxylic acid (6-chIorobenzo[l,3]dioxol-5-ylmetbyOcyclopropylamide;

iracyilR"*. i5*)-3-acety!-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (3-chlorobenzyl)cycIopropyl-amide;
{rac.yilR", 55*)-3-acetyI-7-{4-[2-(4-chioro-2-methylpiienoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-Garboxylic acid (6-chloro-beii2o[l,3]dioxol-5-ylmethyl)cyclopropylamide;
{rac.y{lR*, 5S*)-3-acetyl-7-{4-[2'(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-eae-6-carboxylic acid cyclopropyi-(3-methoxy-benzyl)amide;
(rac.)-(lR*, Ji?*)-3-acetyl-7-{4-[2-{4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid (2-chJorobenzyl)ethyIamide;
(racHIR*, 55*)-3-acetyi-7-{4-[2-(4-cbIoro-2-methylphenoxy)ethoxy]-pheny]}-
3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid cycIopropyl-(3-
inethylbenzyl)amide;
(rac.)-(lR*, 55*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]iion-6-eiie-6-carboxylic acid {6-chlorobenzo[l,3]dioxol-5-yIinethyl)cyclopropylamide;
{rac.y(JR*, i5*)-3-acetyl-7-{4-[3-(2,6-dichloro-4-methylphenoxy)propyI]-
phenyl}-3,9-diazabicyclo[3.3.11non-6-ene-6-carboxylic acid (2-chlorobenzyI)-
cyclopropylamide fonnate salt;
{rac.y{lR*. 55'*)-7-(4-[3-(2-bromo-5-fiuoroplienQxy)propyl]pheayl}-3,9-
dia2abicycIo[3.3.1]non-6-ene-6-carboxylic acid {2-chlorobeiizyl)cyclopropyI-amide.

Most preferred compounds of general formula I are those selected from the gcoup consisting of
(rac.)-(2-methoxyphenyl)acetic acid (JR*, JjS'*)-7-{4'[3-{2-methoxybenzyloxy)-prQpoxy]phenyl}-3-(2-thiophen-2-ylacetyl)-3,9-diazabicyclo[3.3.1]non-6-en-6'yl-methyl ester;
(rac.)-(2-methoxyphenyI)acetic acid (IR*. 56'*)-3-[2-(4~chlorophenyl)acetyl]-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl ester;
(rac.)-{2-methoxyphenyl)acetic acid (IR*. 55*)-7-{4-[3-(2-methoxybenzyloxy)-propQxy]phenyl}-3-(quinoxaUne-2-carboayl)-3,9-diazabicyclo[3.3.1]noa-6-en-6-yhnethyl ester;
(racyiJR*. 55*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-di-a2abicyclQ[3.3.1]non-6-ene-6-carbQxylic acid [2-(2-chlorophenyl)ethyl]methyl-amide;
(rac. )-(2-methoxypheriyl)acetic acid (IR*. 55*)-3-(benzo[i']thiophene-3-carbonyl)-7-{4-[3-(2-methoxybet!Zyloxy)propoxy]plienyl}-3,9-dia2Mibicyclo-[3.3.1]non-6-en-6-yl-methyI ester;
{rac.)-(2-methoxyphenyl)acetic acid {IR*, 55*>3-acetyl-7-{4-t3-(2-methoxy-benzyIoxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.l]noa-6-ea-6-ylinethyl ester;
(rac.)-{2-methoxypheny])acetic acid (IR*, J5*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3-phenylmethaiiesulfonyl-3,9-diazabicyclo[3.3.1]non-6-en-6-ylraethyl ester;

{rac.)-(JR*, J5*)-3--acetyl-7-{4-[3-(2-methoxybenzyIoxy)propoxy]phenyl}-3,9-diazabicyclo[3.3,l]non-6-ene-6-carboxylic acid [2-(4-methQxyptLenyl)ethyl]-methylamide;
(rac.)-{lR*. 55*)-3-acetyl-7-{4-[2'(2-chloro-5-methylphenoxy)ethyl]phenyl}-3,9' dia2abicycIo[3.3.1]non-6-ene-6-carboxylic acid methyiphenethylamide;
(rac.HlR*, 5iy*)-3-acetyI-7-{4-[2-(2-bromo-5-fluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.i]non-6-ene-6-carboxyIic acid methyiphenethylamide;
(7-ac.)-(2-methoxyphenyl)acetic acid (JJi*. J5*)-3-[2-(4-chlorophenyl)ac6tyI]-7-{6-[3-{2-methoxybenzyloxy)propoxy]pyridin-3-yl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylniethyl ester;
(rac-HJR* 55*)-3-acetyl-7-{4-[2-(2,5-dimethylphenoxy)ethyl]phenyl}-3,9-di-azab!cycIo[3.3. l]non-6-ene-6-carboxylic acid methyiphenethylamide;
(rac.)-{JR*, J5*)-3'acetyl-7-{4-[3-(2-methoxybenzyioxy)propoxy]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid [2-(4-chIorophenyl)6thyl]methyl-amide;
(rac.yiJR*, J5*)-3-acetyl-7-{4-[3-{2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-caiboxyIic acid t2-(3-chlorophenyl)ethyI]methyI-amide;
{rac.)-{JR*. J5*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid ethylphenethylamide;
{rac.)-{lR*, J5*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxyhc acid [2-(3-methoxyphenyl)ethyl]methyl-amide;

(rac.y(JR*, 55*)-3-acetyl-7-{4~[3-C2,3,6-trifIuorophenoxy)propyl]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac,y{!R*, JS'*)-3-acetyl-7'{4-[3-(2-methoxybenzyloxy)prQpoxy]pheayl}-3,9-di-azabicyclo[3.3.1]noii-6-ene-6-carboxyiic acid methylphenethylamide;
(rac.y(IR*, 55'*)-3-acer}'l-7-{4-[3-(2-bromo-5-fluoropbenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3. l]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.)-(2-methoxyphenyi)acetic acid (7i?*, 56'*)-7-{4-[3-(2-methoxybenzyioxy)-propoxy]phenyl}-3-methyl-3,9-dia2abicyclo[3,3.1]non-6-eii-6-ylmethyl ester;
{rac.y{lR*. J5*)-3-acetyl-7-{4-[3-(2-methoxyben2yloxy)propoxy]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid [2-(3,4-dimethoxyphenyl)ethyl]-methylamide;
{rac.yiiR*. 5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyI]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
{rac.y(lR*, 55*)-3-acetyl-7-{4-[3-(2,5-dichJoropheaoxy)propyl]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxyUc acid methylphenethylamide;
{rac.y{lR*. J5*)'3-acetyi-7-{4-[2-(2,3-dimethylphenoxy)ethyI]phenyl}-3,9-di-a2abicyclo[3.3.1]non-6-ene-6-carboxyUc acid methylphenethylamide;
(}-ac.yN-((lR*, 55*)-3-acetyI-7-{4-[2-C2-chloro-4,5-dimethylphenoxy)ethyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(r(3c.H2-methoxyphenyI)acetic acid (JR*. J5'*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl} -3,9-diazabicyclo[3.3. l]non-6-en-6-ylinethyl ester;

(rac.)-N-{(lR*, 55'*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-
3,9-diazabicycIo[3.3.1]non-6-en-6-ykiiethyI)-2-(2-methoxyphenyl)-iV-methy[-
acetamide;
(rac.)-N'{{lR*, 55*)-3-acetyl-7-{4-[2-(2-(err-butyI-4-methylphenoxy)ethy!]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.)-{JR*. 5,S*)-3-acetyl-7-{4-[2-(2,5-difluorophenoxy)ethyiJphenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
{rac.)-{IR*, 55*)-3-acetyl-7-{4-[3-(2-methoxybenzyIoxy)propoxy]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid methyl(3-phenylpropyl)aniide;
(rac.y{lR*, J5*)-3-acetyl-7-{4-[3-(2,3-dichlorophenoxy)propyl]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.)-(lR*, J5*)-3-acetyl-7-{4-[3-(2-acetyIphenoxy)propyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
{rac.y{lR*. J5*)-3-acety!-7~{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-di-azabicyclo[3.3.l]non-6-ene-6-carboxylic acid [2-(2-methoxyphenyl)et]iyl]methyl-amide;
{rac.y(lR*. J5'*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicycIo[3.3.1]iion-6-ene-6-carboxyIic acid benzylmethylamide;
{rac.y(lR*, 55*)-3-acetyl-7-{4-[3-(2,5-difluorophenoxy)propyl]phenyl>-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(rac.y{lR*, 55*)-3-acetyl-7-[4-(2"0-toly]oxyethyl)phenyl]-3,9-diazabicyclo-
[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;

(rac.)-(JJi*, 5i?*)-3-acetyl-7-{4-[2-(3-isopropylphenoxy)ethyl]plienyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethyiamide;
{rac.)-{lR*, 55*)-3-acetyl-7-{4-[3-(2-cUorophenoxy)propyl]phenyi}-3,9-diazabi-cycIo[3.3.]]non-6-ene'6-carboxyUc acid(2-chlorob6nzyl)cyclopTopylam!de;
irac.)-OR*. J5'*)-5-|;7-{4-[2-(2-bromo-5-fluorophenoxy)ethyI]phenyl}-6-(mefhyi-phenethylcarbamQyl)-3,9-diazabicyclo[3.3.1]non.-6-en-3-yl]-5-QXopentanoic acid;
(rac.)-{lR*, 5^*)-3-acet>'l-7-{4-[3-(2,3,6-trif]uorophenoxy)propyI]phenyI)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyUc acid (2-chlorobenzyl)cyclopropyl-amide;
(rac.)-{lR*, J5*)-7-(4-[3-(2,3,6-trifluorophenoxy)propyI-phenyl}-3,9-dia2a-
bicyclo[3.3.1]non-6-ene-6-carboxylicacid(2-cblorobenzyI)cyclopiopylamide;
(rac.)-5-((IR*, i5*)-6-[{2-chlorobenzyl)cycIopropyIcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyIphenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-peotanoic acid;
{rac.y(lR*, 55*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-
trifluoroplienoxy)propyl]pheDyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-diinethyletbyI ester;
(rac.)-5-((IR* 55*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-
trifluorophenoxy)propyl]phen.yl}-3,9-diazabicyclo[3.3.1]noii-6-en-3-yl)-2,2-dimethyi-5-oxopentanoic acid;
[mc.yS-iiJR*. JiS*)-6-[(2-chlorobenzyl)cycIopropylcarbamoyI]-7-{4-[3-(2,3,6-rifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-:)entanoic acid methyl ester;

l;l-mixture of (JR, 5S)-3-((JS, '/i;)-4-hydroxypyiTolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluoropbenoxy)propyl]phenyl}-3,9-diazabicyclof3.3-l]non-6-ene-6-carboxyVic acid (2-chlorobenzyl)cyclopropylamide and {IS. 5R)-2>-{{lS, ^R)-A-hydroxypyiToIidme-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6'Carboxylic acid (2-ch!oroben2yl)cyclopropyl-amide;
(rac.)-iJR* 5>?*)-3-(4-carbamoylbutyryl)-7-{4-[3-{2,3,6-trifluoropheaoxy)-
propyl]phenyI)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid {2-chloro-benzyl)cyclopropy!aimde;
(rac.yUR *, 5S*)-3-{4-carbamoylbutyryl)-7- {4-[3-{2,3,6-trifluorophenoxy)-
propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid benzyl-cyclopropylamide;
(rac.yiJR*, 55*)-3-(4-carbamoyIbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-
propyljphenyl} -3,9-diazabicyclQ[3.3. l]non-6-ene-6-carboxylic acid (2-chloro-benzyl)ethylamide;
irac.)-{lR*. 5S*)'3-(4-caTbamoylbutyryl)-7-{4-[3-(2,3.6-trifluoTophenoxy)-
propyl]pheiiyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyUc acid cyclopropyl-(2-fluoroben2yl)amide;
(rac.)-(JR * iiy*)-3-(4-carbamoyIbutyryl)-7- {4-[3-(2,3,6-tiifluorophenoxy)-
propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid cyclopropyl-(3-triiIuoromethyIbeiizyl)ainide;
{rac,)'(IR *, J5*)-3-(4-carbamoylbutyryl)-7- {4-[3-(2,3,6-trifluorophenoxy)-
propyI]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxyIic acid cyclopropyl-(2-methylbenzyl)ainide;

(_rac.)-{lR*, 55*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-
propyI]phenyl}-3,9-diazabicycIo[3.3.i]non-6-ene-6-carboxylic acid cyclopropyl-phenethylamide;
(roc. )-(/-«* 55*)-3-C4-carbaraoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-
propyl]phenyl}-3,9-diazabicyclo[3.3.1Jnon-6-ene-6-carboxyiic acid [2-(2-chloro-phenyi)ethyl]cyclopropylamide;
{rac.)-{}R*, 55*)-3-{4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-
propyljphenyl) -3,9-diazabicyclo [3.3.1 ]non-6-ene-6-carboxylic acid cyclopropyl-(3,5-dimethoxybenzyl)amide;
l:l-mixture of {rac.')-{3R*)-5-{{lR*. 5>S'*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,6-trifl,uorophenoxy)propyl]phenyl}-3,9-diazabicycIo-[3.3.l]non-6-en-3-yI)-3-hydroxy-5-oxopentanoic acid and irac.)-{3S*y5-{{lR*. 55'*)-6-[(2-chiorobenzyl)cyclopropyI-carbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyI}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
l:l-mixrure of {rac.)-{3R*)-5-{{lR*. 55*)-6-(benzylcyclopropyIcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopeiitanoic acid and irac.)-{3S*)-S-{{lR*, SS'^-O-(ben2ylcyclopropylcarbamoyI)-7- {4-[3 -(2,3,6-trifluorophenoxy)propyi]phenyl} -3,9-diazabicycIo[3.3.1]iion-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of (rac.)-(3R*)-5-({]R*, 55*)-64(2-chloroben2yI)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.)-(35*)-5-((Jfi* 55*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;

1:1-mixture of (mc.)-(3R *)-5-((JR *, Ji'*)-6-[cyclopropyl-{2-fluoroben2yl)-caTbamoyl]-7-{4-[3-(2,3,6-trifiuorophenoxy)propyl]phenyI}-3,9-diazbicyclo-[3.3.I]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (f-ac.)-(3S*)-5-((}R*, 5S*)-6-[cyc!opropy!-(2-3uorobenzyl)carbamoyl]-7-{4-[3-(2,3.6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazbicyclo-[3.3.1]non-6-en-3-yl)-3-hydrDxy-5-oxopentanoic acid;
1:1 -mixture of (rac,y(3R*)-5-i{}R* 5i'*)-6-[cyclopropyI-(3-trifluoromethyl-benzyl)carba!noyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]plienyl}-3,9-diaza-bicycIo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.)-{3S*)'5-{(1R\ J5*)-6-[cyclopropyl-(3-trifluoromethylben2yI)carbamoyI]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
1:1 -mixture of (rac. )-(3R *)-5-({IR * 55'*)-6-[cycIopropyI-(2-methylbenzyi)-carbamoyI]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yI)-3-hydroxy-5-oxopentanoic acid and (rac.)-(3S*)-5-((JR*, 5i'*)-6-[cycIoprcpyl-(2-niethylbenzyl)carbamoyi]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3,3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of (rac.)-(3R*)-H0R*. 55*)-6-{cyclopropyl-[2-(4-methoxy-phenoxy)etliyl]carbanioyI}-7-{4-[3-(2,3,6-trifluoropheiioxy)propyl]phenyI}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid and (rac.)-(3S*y5-((lR*, 55*)-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]caibanioyI}-7-
{4-[3-(2,3,6-trifluoroplienoxy)propyl]phenyl>-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoJc acid;
l:l-mixture of (rac.y(3R*y5-i(IR*, J5*)-6-[cyclopropyl-(2-m-toiyioxy6thyl)-carbamoyl]-7-(4-[3-(2,3,6-trifluorophenoxy)propyl]pheiiyl}-3,9-diazabicyclo-[3.3,l]non-6-en-3-y!)-3-hydTOxy.5-oxopentanoic acid and (rac.)-(5S'*)-5-((-/S*, J5'*)-6-[cyclopropy!-(2-m-tolyIoxyethyI)carbamoyl]-7-{4-[3-(2,3,6-trifluoro-

phenoxy)propyl]phenyl}-3,9-diazabicycio[3.3.1]noii-6-en-3-yI)-3-hydroxy-5-oxopentanoic acid;
l:l-mixture of (rac.)-(3R*)-5-(OR*, 55*)-6-{[2-{2-chlorophenyI)ethyl]-cyclopropylcarbamoyl) -7- {4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl} -3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-3-hydroxy-5-oxopeiitanoic acid and (rac)-(3S*)-5-((}R*, 55*)-6-([2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-3-hydroxy-5-oxopentanoic acid;
I; 1 -mixture of (rac. )'{3R *y5-({IR *, J5'*)-6-[cycIopropyl-(3,5-dimethoxy-beiizyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propy!]phenyl}-3,9-dia2a-bicyclo[3.3.1]non-6-en-3-y!)-3-hydroxy-5-oxopentanoic acid and (rac-)'{3S*)'5-{{]R*, JS*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)caibamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyi}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
[rac.)-{lR*, 5S*)-3-acetyl-7-{4-13-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid (2-ch]orobenzyl)ethylamide;
(rac.)-{JR*, 5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]pheiiyl}-3,9-diaMbicyclo[3.3.1]iioa-6-eiie-6-carbQxylic acid cyclopropyL(3,5-diinethoxy-beiizyl)aiiiide;
(rac.y5-((lR*. J5*)-6-(benzylcyclopropylcarbamoyi)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopeiitanoic
acid;
(rac.)-5-(ilR* 55'*)-6-[(2'Chloroben2yl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-
phenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3.1]noii-6-en-3-yl)-5-oxopentanoic
acid;

(rac.yS-iOR*, 5.?*)-6-[cycIopropyI-(2-fluorobenzyI)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]pheDyi}-3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-5-oxo-pentanoic acid;
irac.y5-({}R*, 55*)-6-[cyclopropyl-(3-trifluoTomethylbenzyl)caTbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-5-oxopentanoic acid;
(rac.yS-dlR *. 55*)-6-[cyclopropyI(2-methyIbenzyl)carbamoyl]-7- (4-[3-(2,3,6-trifluoropheiioxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non'6-en-3-yl)-5-oxo-pentanoic acid;
{rac.yS-dlR*. J5*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifIuorophenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yI)-5-oxopentanoic acid;
{rac.yS-{(lR*, 5S*)-6-[cyc!opropyl(3,5-diinethoxyben2yi)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopeatanoic acid;
(rac.y5-((lR*, 55*)-6-[cyclopropyIC2-;;-tolylethyI)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-5-oxo-pentanoic acid;
(rac.y5-((lR*, 55*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-pbenoxy)propyl]pbenyl}-3,9-dia2abicyclo[3.3.1]noii-6-en-3-yl)-5-oxopentanoic acid methyl ester;
(rac.y5-((JR*, J5'*)-6-[cyclopropyI-(2-fluorob6nzyI)carbamoylj-7-{4-[3-(2,3,6-triflaorophenoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.11non-6-en-3-yl)-5-oxo-pentanoic acid methyl ester;

(rac.)'5-{(!R*. J-S'*)-6-[cyclopropyl-(3,5-dijnethoxybenzyl)carbamoyl]-7-(4-[3-(2,3,6'trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yi)-5-Qxopentanoic acid methyl ester;
(rQc.)-5-((Jii*, 5S*)-6-[(2-chloiobenzy5)ethylcaibamoyl]-7-{4-[3-(2,3,6-trifluoto-phenoxy}propyI]phenyl}-3,9-dia2;abicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopenlanoic acid;
(rac.)-5-((IR*, 55*)-6-[cycIopropyl-(2-fluorobenzyl)carbamoyI]-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
(rac.)-5-((IR*, 55*)-6-[cyclopropyl-(2-methyIben2yl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yI)-2,2-dimethyl-S-oxopentanoic acid;
(rac.}-5-((IR*, J5*)-6-[cyclopropyI-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicycto[3.3.1]non-6-en-3-yI)-2,2-dimethyl-5-oxopentanoic acid;
l:l-raixture of (racH^i?*, 3S*)-4-{{lR*, 55'*)-6-[cyclopropyK2-inetbylbeiizyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluoropheiioxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]noii-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid and (rac.)-(2S*. 3R*)-4-{{IR* 5iS*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-i;3-(2,3,6-triauoro-phenoxy)propyl]phenyI}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-diliydroxy-4-oxobutyric acid;
{i-ac.)-5~{ilR*, 55*)-7-(4-[3-(2-bromo-5-fiuorophenoxy)propyl]phenyI}-6-
[cyc]opropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ea-3-yl}-5-oxopentanoic acid;

(rac.)-5-{iiR*, J5*)-7-{4-[3-{2-bronio-5-fluorophenoxy)propyI]ph6nyl}-6-
{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbaraoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic acid;
{rac.)-5-[{iii* 55*)-7-{4'[3-{2-bromo-5-fluorophenoxy)propyl]pbeny]}-6-
(cyclopropylphenethyIcarbamoyl)-3,9-diazabicycIo[3.3.1]non-6-en-3-yl]-5-oxo-pentanoic acid;
(rac.yS'iOR*. 5iS'*)-7-{4-[3-{2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyI)ethyl]cyclopropylcarbamoyI}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid;
(rac.)-5'(_(lR*, J5*)-7-(4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentaBoic acid;
{rac.yS'iOR*, 5S*)-7-{4-[3-(2-bromo-5-fluoropheaoxy)propyl]phenyl}-6'{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicycio[3.3.1]non-6-en-3-yI)-5-oxopentanoic acid;
{rac.)-5-(ilR*, J5*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6'{[2-C4-methylphenyl)ethyl]cyclopropylcarbanioyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-5-oxopentanoic acid;
(rac.)-5'{(lR*, J5*)-7-{4-p-(2-bromo-5-fiuoroplienoxy)propyI]phenyl}'6-
[cyclopropyl-(3,5 -diniethoxyben2yl)carbainoyl]-3,9-diazabicyclo[3.3. l]non-6-eo-3-yl}-5-oxopentanoic acid;
{rac.yS'iOR*. 5S'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]p!ienyl}-6-
[cyclopropyl-(3,5-dimethoxybenzyI)carbainoyl]-3,9-diazabicyclo[3.3.1]aon-6-eii-3-yl}-5-oxopentanoic acidmediyl ester;

(rac.yS'iilR*, 55'*>-7-{4-[3-{2-bromo-5-f]uorophenoxy)propyl]phenyl}-6-
[cyclopropyl-(2-fluorobenz^-l)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyI-5-oxopentanoic acid;
{rac.yS'iiJR* JS*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyI]phenyl}-6-
[cyclopropyl-(2-melhylbenEyl)carbaraoyl]-3,9-diazabicyclo[3,3.1]iion-6-en-3-yi)-2,2-diraethyl-5-oxopeatanoic acid;
{rac.y5-[(lR*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-
(cyclopropy]phenethylcarbanioyI)-3,9-diazabicyclo[3.3.1]non-6-en-3-yi]-2,2-dimethyl-5-oxopeatanoic acid;
{rac.yS'iilR*. 5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-methyIphenyl)ethyl]cycIopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
(rac.y5-{(]R*, J5*)'7-{4-[3-(2-bronio-5-fluorophenoxy)propyl]phenyl}-6-
[cyclopropyl-(3,5-dimethoxybeD2yl)carbamoyl]-3,9-dia2abicyclo[3.3.1]non-6-en-3-yI}'2,2-dimethyl-5-oxopentanoic acid;
l:l-inixture of (rac.y{2R*. 3S*y4-{{}R*. i5'*>7-{4-[3-(2'bromo-5-fluoro-phenoxy)propyi]phenyi}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-dia2abicyclo[3.3.1]non-6-en-3-y!}-2,3-dihydroxy-4-oxobutyric acid and (rac.y {28*. 3R*yA-{(JR*, 55'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyI]plienyI}-6-[cyclopropyl-(3,5-diinetlioxybenzyI)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric acid;
{rac.y S-(iJR*. 55*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)elliyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-5-oxo-pentanoic acid;

(rac.yS-iUR", 55*)-6-[(3-trif]uoromethyIbenzyI)cyclopropylcarbamoyi]-7-(4-[2-(2,3,5-trimethylpheQoxy)ethyl]phenyl)-3,9-diazabicyc!o[3.3.1]non-6-en-3-y!)-5-oxopentanoic acid;
5 {rac.)-5-{{lR*. i5*)^6-[(2-methylberizy!)cyclopropyIcarbanioyl]-7-{4-[2-(2,3,5-triiiiethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid;
{yac)-5-{{lR*, 55*>6-[(2-cWorobenzyl)ethylcarbamoyl]-7-{4-i:2-{2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1Jnon-6-en-3-yI)-2,2-diniethyl-5-oxopentanoic acid;
irac.y5-iilR*, i50-6-[cyclopropyl-(2-fluoroben2yl)carbamoyl]-7-{4-[2-(2,3,5-triaiethylpheaoxy)ethyI]pheny!}-3,9-diazabicyc!o[3.3.1]non-6-en-3-yl)-2,2-diraethyl-5-oxopentarioic acid;
(rac.)-5-{(7ie* J^*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chIorobenzyl)cyclopropyIcarbamoyIJ-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid;
{rac.)-5~{{lR*. 55*)-7'(4-[3-(2-bromo-5-fluoropheiioxy)propyl]phenyl>-6-[(2-ch]orobeii2yl)cyclopropylcarbamoyI]-3,9-diazabicyclo[3.3.1]non-6-eii-3-yI}-2^-dimethyI-5-oxopentanoic acid;
{rac.yS-iilR*. 55'*)-4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyI}-3-(4-
caibamQylbutyryl)-3,9-diazabicyclo[3.3. l]noa-6-ene-6-carboxyUc acid (2-chloTO-beiizyi)c>^lopropylamide;
{rac.yS-iilR*, 5A*)-6-(benzylcyclopropylcarbamoyI}-7-{4-[3-(2-bromo-5-fluoro-phenoxy}propyl]phenyl}-3^9-diazabicyclo[3.3.1]non-6-en-3-yI)-5-oxopentanoic acid methyl ester;

(rac.)-(JR*. J5'*)-3-acetyI-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-
phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)-cyclopropylamide;
{rac.)-5-({}R*, ^"S*)-6-[{2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2-
chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicycio[3.3.1]non-6-en-3-yl)-5'0xopentanoic acid;
{rac.)-5-{ilR*, 55'*)-7-{4-[2-(2-chloro-4,5-dimethyIphenoxy)ethoxy]pheiayl}-6-[cyclopropyl-(2-methylbenzyi)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-S-oxopentanoic acid;
irac.)-5-{(}R*'. J5*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]pheiiyl}-6-[cyclopropyI-(3,5-dimethoxybenzyl)carbainoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopeiitanoic acid;
(rac.)-5-((JR*, J5*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl3-7-{4'[2-(2-
chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-diinethyl-5-oxopentanoic acid;
(rac.)-5-((i-R*, 55*)'6-[(2-chloroben2yl)ethyicarbamoyl]-7-{4-[2-(2-chloro^,5-dimethylphenoxy)ethoxy]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en~3-yl)-2,2-dimethyl-S-oxopentanoic acid;
irac.y5'{(IR*, J5*)'7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]pheDyl}-6-[cycIopropyl-(2-fluorobenzyl)carbamoyI]-3,9-diazabicyclo[3.3.1]non-6-ea-3-yl}-
2,2-dimethyl-5-oxopentanoic acid;
(rac.)-5-((lR*, 55*)'6-[cycIopropyI-{3,5-dimethoxyben2yl)carbamoyI]-7-{4-[2-(2,3,5-trimetbylphenoxy)ethyi]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-
oxopentanoic acid;

(rac.yS'dlR*. JS*)-6-[cyclopropyl-(2-/?-tolylethy!)carbamoyl]-7'{4-[2-(2,3,5-trinietIiy[pheiioxy)ethyI]pheQyl)-3,9-d!azabicyclo[3.3.1]non-6-en-3-yI)-5-oxo-pentanoic acid;
(rac.)-5-((JR*. 55*)-7-{4-[2-(2-ch!oro-4,5-dimethy!phenoxy)ethoxy]phenyl}-6-{cyc]opropyI-[2-(2-hydroxyethyI}b6nzyI]carbamoyI}-3,9-diazabicyclo[3.3.IJnon-6-en-3-yl)-5-oxopentanoic acid;
imc.y5-{iIR*. J5*)-6-(cyclopropylphenethylcarbainoyl)-7-{4-[2-(2,3,5-triraethyl-phenoxy)ethyI]phenyl}-3,9-diazabicycio[3.3.1]non-6-en-3-yl)-2,2-diniethy!-5-oxopentanoic acid;
{rac.y{IR*. J5*)-7-{4-[3-(2,3,6-triiluorophenoxy}propyl]phenyl}-3,9-dia2a'
bicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)ethylamide;
{rac.y{lR*. 5S*)-7-(4-[3-(2,3,6-trifluoropheiioxy)propyl]pbenyl}-3,9-diaza-
bicyclo[3.3.1]non-6-ene-3,6-dicarboxylic acid 6-J(2-chloroben2yl)cyc]opropyi-amide] 3-dimethyIamide;
i_rac.y{lR*, 5i'*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diaza-
bicyclo[3.3.1]Bon-6-eiie-3,6-dicarboxyIic acid 6-[(2-chlorob6nzyl)cycIopTopyl-amide] 3-diethyIaimde;
ijrac.y{}R'^. 5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyI]-7-{4-[3-(2,3,6-
trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.I]non-6-ene-3-carboxylic acid methyl ester;
{rac.y{lR*, 5-S*)-6-[(2-chloiobeDzyI)cyclopTopyicaibamoyl]-7-{4'[3-(2,3,6-
trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboxylic acid ethyl ester;

(rac.)-(lR*, 55*)-3-methanesuIfonyl-7-{4-[3-(2,3,6-trif]uorophenoxy)propyl]-phenyl}-3,9-diazabicycio[3.3.1]non-6-ene-6-carboxy!ic acid (2-chlorobenzyi)-cyclopropylamide;
[rac.yilR* 55*)-3-ethanesulfonyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-
phenyi}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)-cyciopropylamide;
(rac.y5-((JR*, J5*)-6-[(2-chlorobenzyl)cyclopropy]carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-diazabicyclo[3.3.I]non-6-en-3-yl)-5-oxo-pentanoic acid ethyl ester;
(rac.yA-aiR* J5*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-4-oXO-butyric acid;
(rac.)-3'[((lR*, 55*)-6-[(2-chlorobeiizyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-3-carbony!)-amino]propionic acid ethyl ester;
{rac.)4-[{{iR*, 5S*)-6-[(2-chlorobenzyI)cyclopropykarbamoyl]-7-(4-[3-(2,3,6-triiluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboiiyl)-amino]butyric acid ethyl ester;
(rac.y(IR*, 55*)-3-(3-carbamoylpropionyI)-7-{4-[3-(2,3,6-trifluoropheaoxy)-pTopyl]phenyl}-3,9-diazabicyclo[3.3.1]aon-6-ene-6-carboxyhc acid (2-chIoro-benzyl)cyclopropylamide;
{rac.y(lR*, 55'*)-3-(2-hydroxyacetyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]-phenyl} -3,9-diazabicyclo [3.3.1 ]non-6-ene-6-carboxylic acid (2-chIorob6nzyI)-cyclopropylamide;

(JS, 5ie)-3-((3i;)-3-hydroxybutyryl)-7-{4'[3-{2,3,6-trifluorophenoxy)propyl]-
pbenyl}-3,9-diazabicyclo[3.3.1]iion-6-ene-6-carboxylic acid (2-chlorobenzyl)-cyclopropyi amide;
l-.l-mixture ai {rac.)-{lR*, 5S*)-3-((ii?*, 2S*>2-hydtoxycyclopentanecatboTiyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyi]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyUc acid (2-chlorobenzyl)cyclopropylamide and {rac.)-{]R*, 5S*)-3-((75'*, 2^*)-2-hydroxycyclopentanecarbonyl>7-{4-[3-(2,3,6"trifluorophenoxy)-propyl]phenyi}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chloro-benzyI)cyclopropylainide;
{mc.)-(}R*. 5iS'*)-9-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3,3.1]non-6-ene-6-carboxylic acid (2-chlorobetizyl)cyclopropyI-amide;
(rac.yS-iUR*, 55*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl.)-5-oxo-pentanoic acid;
(rac.)-5-(ilR*. 5iS'*)-6-[(2-chlorobenzyI)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluoropheEoxy)propyl]plienyl}-3,9-diazabicycIo[3.3.1]iioii-6-en-9-yl)-5-oxo-pentanoic acid ethyl ester;
{rac.yS-aiR*. 55*)-6-[(2-chioTobenzyl)cyclopropylcarbamoyl]-7-{4-(;3-(2,3,6-trifluoropfaenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]aon-6-en-9-yl)-5-oxo-pentanoic acid methyl ester;
l:l-mixture of {rac.y{3R*)-5-{{}R*. 3S*>6-[(2-cMorob6nzyl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl>-3,9-dia2abicyclo-[3.3.1]nOD-6-en-9-yl)-3-hydroxy-5-oxo-pentanoic acid and (rac.)-(35'*)-5-((iJ?*, i5'*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-mfluoro-
phenoxy)propyi]phenyI}-3,9-diazabicycIo-[3.3.1]non-6-en-9-yl)-3-hydroxy-5-oxopentanoic acid;
(rac.)-5-({lR*. 55*)-6-[(2-chlorobenzyl)cycIopropyicarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en-9-yl)'2,2-dimethyi-5-oxopeBtanoic acid;
{rac.)-4 {rac.y{lR*, 55*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}'3,9-diaza-
bicyclo[3.3.1]non-6-ene-6,9-dicarboxylic acid 6-[{2-chlorobenzyl)cyclopropyl-amide] 9-dimethylainide;
{rac.y(lR*, 5^*)-6-[(2-chlorofaenzyl)cyc]opropylcarbamoyl]-7-{4-[3-(2,3,6-
trifluorophenoxy)propyl]phenyl} -3,9-diazabicycIo[3 -3.1 ]non-6-ene-9-carboxyIic acid methyl ester;
{rac.y{lR*. 55*)-6-[(2-chloroben2yl)cyclopropylcarfaamoyl]-7-{4-[3-(2,3,6-
trifluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-eiie-9-carboxylic acid ethyl ester;
irac.y3'[(JR*, 55*)-(6-[(2-chloroben2yl)cyclopropylcarbainoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl)-3,9-diazabicyclo[3.3.1]non-6-ene-9-caibonyl)-
aminojpropionic acid ethyl ester;
{rac.)~4-[i{lR*, 55*)-6-[(2-chlorobenzyI)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluoropheQoxy)propyl]pbenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)-
aminojbutyric acid ethyl ester;

{rac:)-(]}i*. J^*)-3-fomiyI-7-{4-[3-(2,3,6-trifluorophenoxy)propy]Jphenyl}-3,9-diazabicycIo[33.1]nQn-6-ene-6-carboxylic acid (2-ch!orobenzy!)cycIopropyI-amide;
(rac.)-3-[((/S*, 55'*)-6-[(2-chIoroben2yl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9'dia2abiGyclo[3.3.1]non-6-ene-3-carboQyt)-aminojpropionic acid;
(rac.)-3~[i(}R*, 55*)-6-[(2-chlorobenzyl)cyc]opropy]carbainoyl]'7-{4-[3-(2,3,6-trifluoroplienoxy)propyl]phenyl} -3,9-diazabicyclo[3.3.1 ]non-6-eae-9-carboayl)-aniino]propionic acid;
irac.)-A~[(i}R*, J5*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-{2,3,6-trifluorophenoxy)propyJ]phenyI}-3,9-diazabicycIo[3.3.1]non-6-ene-9-carbonyI)-aminojbutyric acid;
(rac.)-{lR*, 55*>-3-acetyl-7-{4'[2-(2,3,6-trifluorophenoxy)ethyI]phenyI}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxyiic acid (2-chlorobenzyl)cycIopropyl-amide;
(rac.y{lR*. 55*)-9-(4-carbamoylbutyryl>7-{4-[2-(2,3,6-t!ifluoTopheiioxy)-
propyl]phenyl}-3,9-dia2abicyclo[3.3.1]iion-6-ene-6-carboxylic acid (2-
chlorQbenzyi)cyclopropylainide;
(rac.)-{lR*, J5*)-9-(3-carbanioylpropioayl)-7-{4-[2-(2,3,6-trifluorophenoxy)-propyl]plienyl}-3,9-diazabicycio[3.3.1]non-6-ene-6-carboxylic acid (2-chloro-
benzyljcyclopropylamide;
(rac.y(JR*, 55'*)'9-(2-hydroxyacetyl)-7-{4'[2'(2,3,6-trifluorophenoxy)propyI]-phenyi}-3,9-diazabicycIo[3.3.1]noii-6-ene-6-carboxyIic acid (2'Chloiobenzyl)-cyclopropylamide;

(JR, ■?'S)-9-{(i5)-3-hydroxybutyryI)-7-{4-[2-(2,3,6-trifluoroplienoxy)propyl]-
phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxyIic acid (2-cIilorobenzyl)-cyclopropylamide;
5 {rac.)-(lR*, 55*)-9-methanesuIfonyl-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicycIo[3.3.1]non-6'ene-6-carboxylic acid (2-cIilorobenzyl)-cyclopropyiamide;
(racHIR*, 55*)-9-etlianesulfonyl-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-
) phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid (2-chJorobenzyl)-cyclopropylamide;
{rac.)-{m*, J5*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propy]]phenyl}-3,9-dia2abiGyclo[3.3.1]noTi-6-ene-6-cacboxylic acidcyclopropyl-(2-fluoro-5-iDethoxy-benzyl)ainide;
{rac.)-(JR*, J5'*)-3-acetyI-7-(4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid cyclopropyl-(3-methoxybenzyl)-amide;
irac.)'{JR*, 55*)-3-acetyl-7-{4-[3-(2,3,6-tiifluorophenoxy)propyl]phenyl}-3,9-dia2abicycIo[3.3.1]non-6-ene-6-caiboxylic acid cyclopropyl-(3,4-diinethoxy-benzyl)ainid6;
{rac.)-{lR*, 55*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]pIieiiyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chloro-3-trifluoroinethyI-beiizyl)cyclopropylamide;
(rac.)-(JR*, 55*)-3-acetyl-7-{4-[3-(2,3,6-triiluorophenoxy)propyl]phenyl}-3,9-dia2abicycIo[3.3.11iioa-6-ene-6-carboxylic acid benzo[l,3]dioxol-5-ylinethyl-cyclopropylamide;

(rac.y(JR*, J^*)-3-acetyl-7-{4-[3-(2,3,6-trifIuorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]iion-6-ene-6-carboxylic acid (2-cla]oro-6-fluorobenzyl)-cyclopropylamide;
(rac.)-(]R*. 55*)-3-acety]-7-{4-[3-{2,3,6-tTifluorophenoxy)propyI]phenyll-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-bromoben2yl)cyclopropyl-aniide;
{rac.)-(IR*, 55*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]rioii-6-ene-6-carbOKyUc acid cycIopropyl-(2,3-dimethyl-ben2yl)amide;
(rac.)-(IR'^, 5iS'*)-3-acetyl-7-{4-[3-(2,3,6-trifluoropheiioxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid cyclopropyl-(3,5-dif]uoro-benzyl)amide;
(rac.)-(lR*, 55'*)-3-acetyl-7-(4-[3-{2,3,6-trifluorophenoxy)propyi]plienyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2,3-dichloro-benzyl)amide;
{rac.)-(lR*, 5S*>3-acetyl-7-{4-i;3-(2,3,6-trifiuorophenoxy)propyl]plienyl}-3,9-dia2abicyclo[3.3.1]non-6-eiie-6-carboxylic acid cyclopropyl-(3-tri£luotoniethoxy-benzyl)amide;
(rac.yUR*, J5*)-3-acetyl-7-(4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1]noii-6-ene-6-carboxyIic acid cyclopropyl-(3-methylbea2yI)-amide;
irac.)-{lR*. 5i'*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propylJplieiiyl}-3,9-diazabicyclo[3.3.1]iion-6-ene-6-carboxytic acid (3-cblorobenzyl)cyclopropyl-amide;

(rac.)-(IR*. 5^*)-3-(5-morphoiin-4-yl-5-oxopentanoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyt]phenyl}-3,9-diazabicyclo[3.3.1]noTi-6-ene-6-carboxylic acid (2-clilorobenzyl)cyclopropylamide;
(rac,)-(7i?*, 55*)-3-(2-tetra2ol-l-ylacetyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-
propyl]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chloro-benzyQcycIopropylamide;
(rac.)-(IR*, J5'*)-3-(5-oxo-5-piperazin-l-yIpentanoyl)-7-{4-[3-(2,3,6-trifluoro-pb.enoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-eiie-6-carboxylic acid (2-chlorobenzyl)cycloprop ylamide;
l:l-raixture of (JR. 551-3-((25)-2-amino-3-hydroxypropionyl)-7-{4-[3-(2,3,6-trifluoTophenoxy)propyi]phenyl}-3,9-diazabicyc!o[3.3.1]non-6-ene-6-carboxyiic acid (2'Chlorobenzyl)cyclopropylamide and (IS. 5R)-3-({2S)-2-a]mno-3-hydroxypropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]pheny!}-3,9-diaza-bicyclo[3.3.1Jnoii-6-eDe-6-carboxylic acid (2-chlorobenzyl)cyclopropyIamide;
1:1-mixture of (IR. 5iS)'3-({25}-2-ainiDOpropionyI)-7- {4-[3-(2,3,6-trif]uoro-phenoxy)propyl]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzy])cyclopropylainJde and (IS, 5J;)-3-((25)-2-aminopropionyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]plienyl}-3,9-diazabicyclo[3.3.1]iioii-6-ene-6-caiboxylic sw;id (2-chloTobenzyl)cyclopropyIamide;
(rac.)-(IR*, 55*)~3-acetyI-7-{4-[2-(2,6-dicliloro-4-inethyIphenoxy)etlioxy]-
phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2,3-
dichlorobenzyOamide;
(rac.y(]R*. J5'*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-
phenyI}-3,9-dia2abicyc!o[3.3.1]non-6'ene-6-carboxylic acid cyclopropyl-(2,3-dimethylbenzyl)amide;

irac.)'{lR*. J5*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)etIioxy]-
phenyl}-3,9-diazabicyclo[3.3.1]nou-6-ene-6-carboxyUc acid (2-ch.loro-3-trifluoromethyl-ben2yl)cyclopropylamide;
(rac.)-(}R *, J5*)-3-acetyl-7- {4-[2-{2,6-dichloro-4-methylphenoxy)ethoxy]-
phenyl)-3,9-diazabicyclo[3.3.1]non-5-6ne-6-carboxylic acid (2-bromobenzyl)-cyclopropylamide;
(rac.)-(IR*, 55*)-3-acetyl-7-{4-[2-(2,6-dichIoro-4-methylphenoxy)ethoxy]-
phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid (2-chIorobenzyl)-cyclopropyiamide;
(rac.)-(JR*, 55*)-3-acetyl-7-{4-[2-(2,6-dichJoro-4-methyIphenoxy)ethoxy]-
phenyl)-3,9-dia2abicyclo[3,3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)-ethylamide;
(rac.XlR*. J6'*)-3-acetyl-7-{4-[2-(2,6'dich]oro-4-methylphenoxy)ethoxy]-
phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid (6-chlorobenzo-[l,3]dioxol-5-yImethyl)cyclopropylaimde;
{rac.)-{lR*, 5S*)'3-acetyl-7-{4-[2-(2,6-diciilOTo-4-inethylphenoxy)efeoxyV
phenyi}-3,9-diaza-bicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,5-diiflethoxybenzyl)aniide;
(rac.y(JR* 55*)-3-acetyl-7-{4-I2-(2,6-dichloro-4-methylphenoxy)eaoxy]-
phenyl}-3,9-diazabicyGlo[3.3.1]noii-6-eiie-6-carboxylic acid cycloptopyl-(3-tiiethoxyben2yl)amide;
(racHlR*, J6'*)-3-acetyI-7-{4-[2-(2-chIoro-5-fluorophenoxy)ethoxy]phenyI}-3,9-diazabicyclo[3.3.l]non-6-ene-6-carboxylic acid cyclopropyI-(2,3-dichloro-benzyl)ainide;

{rac.)'(IIi*, 5i'*)-3-acetyl-7-{4-[2-(2-chloro-5-f!uorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]Don-6-ene-6-carboxylic acid (2-ch]oro-3-trif]uoro-methylbenzyl)cyclopropy!ainide;
(rac.yU-R*, 55*)-3-acetyl-7-{4-[2-{2,6-dichloro-4-methy!phenoxy)etIioxy]-
phenyi}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid (3-chlorobenzyl)-cyclopropylamide;
(rac.)-{m*, 55*)-3-aGetyl-7-{4-[2-(2,6-diGliioro-4-metliylphenoxy)ethoxy]'
phenyl}-3,9-dia2abicyclo[3.3.1]non-6-eQe-6-carboxyUc acid cyclopropyI-(3-methyib6nzyl)aiTiide;
irac.)-{]R*, 55*>3-acetyl-7-{4-[2-(2,6-dichloro-4-methy]phenoxy)ethoxy]-
phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2-fluoro-5-methoxyben2yl}amide;
{rac.)-{IR * J6'*)-3-acetyl-7- {4-[2-(2-chIoro-4,5-diinethylpheiioxy)-
ethoxy]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxyHc acid cyclopropyi-(2,3-dichlorobenzyl)amide;
{rac.)-{lR*, 55*)-3-acetyl-7-{4-[3-(2-chloro-3,6-difiuorophenoxy)propyI]-
phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyI)-cyclopropylamide;
{racyQR*, 55*)-3-acetyl-7-{4-[2-C2-chIoro-4,5-dimethylphenoxy)ethoxy]-
phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-cUoro-3-fiifluoromethylbenzyOcyclopropylamide;
(rac.)-(/-R*, 5S*>3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)etlioxy]-
phenyl}-3,9-diazabicycio[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,4-diinethoxybenzyl)aimde;

{rac.yilR*. J5'*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)etIioxy]-
phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyI-(3-tri fluoromethox ybenzyl) amide;
irac.)-(IR*, 55*)-3'acetyl-7-{4-[2-(2,4,5-tricWoTOphenoxy)ethoxy]pheEyU-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chloro-3-trif]uoro-
methyibenzyi)cyclopropyl amide;
(rac.)-(IR*, 55'*)-3-acety!-7-{4-[2-(2,4,5-trichJorophenoxy)ethoxy]phenyI}-3,9-
diazabicycIo-[3.3.1]non-6-ene-6-carboxyIic acid cycIopropy]-(2,3-
dichIorobeiizy])anii de;
(rac.yOR* 55*)-3-acetyI-7-{4-[2-(2,3-dichIorophenoxy)ethoxy]phenyl}-3,9-
diazabieycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2,3-dimetliyl-ben2yl)amide;
{rac.)-{}R*. 55*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]plienyl>-3,9-
diazabicyclo-[3.3.1]non-6-6ne-6-carboxylic acid cyclopropyl-{2,3-
diinethylbenzyl)amide;
(rac.)-iIR*. 55*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)etfaoxy]-
pheiiyl)-3,9-diazabicyc]o[3.3.1]non-6-ene-6-carboxylic acid cycIopropyl-(2,3-dimethylb eiizyl)amide;
{rac.y(lR*, 55'*>-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyI}-
3,9-diaza-bicycio[3.3.1]non-6-efle-6-caiboxylic acid cyclopropyl-(2,3-
dichlorobenzyl)amide;
(rac.yOR*, 55*J-3-acetyl-7-{4-[2-(2-chloro-4,5-diinethylphenoxy)eihoxy]-
phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-broinobenzyl)-cyclopropylamide;

irac.)-{]R^ 55*>3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cycIopropyl-(2,3--
dicli!oroben2yl)amide;
5 (rac.)-(iil*, 5S*)-3-acet\'l-7-{4-[2-(2-chloTO-5-fluoTophenoxy)ethoxy]phenyl)-
3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid cyc]opropyl-(2,3-
dimethylbeiizy!)amide;
(rac.)-(lR. 55)-7-{4-[3-(2,3,6-trifluorophenoxy)propylphenyI}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxyhc acid (2-chlorobenzyl)cyclopropylamide;
(rac.y(JS, 5fl)-7-{4-[3-(2,3,6-trifluorophenoxy)propylphenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic acid (2-ch]oroben2yl)cyclopropylaitiide.
The compounds of general formula I and their phannaceutically acceptable salts may be used as ther^eutics e.g. in fomi of phamiaceutical compositions. They may especially be used in the treatment and/or prophylaxis of cardiovascular and renal diseases, Exan^les of such diseases are hypertension, coronary diseases, cardiac insufficiency, renal insufficiency, renal and myocardial ischemia, and renal failure. They can also be used to prevent restenosis after balloon or stent angioplasty, to treat erectile dysfunction, glomerulonephritis, renal colic, and glaucoma. Furthermore, they can be used in the th^apy and the prophylaxis of diabetic complications, complications of vascular or cardiac surgery or after organ transplantation, complications of cyclosporin treatment, as well as other diseases presently known to be related to the RAS.
In another embodiment, the invention relates to a method for the treatment and/or prophylaxis of diseases which are related to the RAS such as hypertension, coronary diseases, cardiac insufficiency, renal insufficiency, renal and myocardial ischemia, and renal failure, which method comprises administrating a compound as defined above to a human being or animal.

The invention further relates to the use of compounds of general formula I as defined above for the treatment and/or prophylaxis of diseases which are associated with the RAS such as hypertension, coronary diseases, cardiac insufficiency, renal insufficiency, renal and myocardial ischemia, and renal failui'e.
In addition, the invention relates to the use of compounds as defined above for the preparation of medicaments for the treatment andVor prophylaxis of diseases which are associated with the RAS such as hypertension, coronary diseases, cardiac insufficiency, renal insufficiency, renal and myocardial ischemia, and renal failure.
The compounds of formula I may also be used in combination with one or more
other therapeutically usefiil substances e. g. with other renin inhibitors, with ACE-
inhibitors, with angiotensln-receptor antagonists, with diuretics, with calcium
channel blockers, with eodothelin receptors antagonists or with other drugs
beneficial for the prevention or the treatment of cardiovascular events or renal
insufficiency. '
All forms of prodrugs leading to an active component comprised by general formula I above are included in the present invention.
The compounds of general fonnula I can be manufactured by the methods outlined below, by the methods described in the examples or by analogous methods.
Preparation of the precursors:
Precursors are compounds which were prepared as key intermediates and/or building blocks and which were suitable for fiirther transformations in parallel chemistry.

Bicyclononanone A was prepared from (4-benzyl-6-ethoxycarbonylmethyI-l-methylpiperazm-2-yl)acetic acid ethyl ester (Patent Application WO92/05174) as described in Scheme 1, Derivative A miglit also be present as enol form. Xn order to allow a coupling at the 7-position of bicyclononane A with aryl bromides, the vinyl triflate derivative B was prepared.

The bromoaryl components can be prepared as described in Scheme 2. A Mitsunobu coupling (-> compounds of type C) or the alkylation of an alcohol with a ben2ylic chloride (or bromide, -> compounds of type D) are often the most convenient methods. Derivatives E and F were prepared in one step from I-(3-chloropropoxymethyl)-2-methoxyben2ene (Vieira E. et al., Bioorg. Med. Chem. Letters, 1999, P, 1397) or 3-(5-bromopyridin-2-yIoxy)propan-l-ol (Patent AppUcation WO 98/39328) according to these methods. Other methods for the preparation of ethers or thioethers, like a Williamson synthesis, might be used as well (see e.g. March, J, "Advanced Organic Chemistry,", 3"^ ed., John Wiley and sons, 1985).


As shown in Scheme 3, these bromoaryl derivatives might then be coupled to triflate B in the presence of Pd(PPh3)4 or a related Pd(0)-compiex in order to obtain bicyclononenes G (for details see the corresponding examples). Protective group manipulation would lead to the bicyclononenes H, which can finally be reduced to the alcohol derivatives J.


If R^ is 0-SEM and X is CH, in compounds of type J, the SEM-protecting group can be cleaved under slightly acidic conditions, while the Boc-protecting group remains untouched as illustrated in Scheme 4. The phenolic moiety of bicyclononene K might then be alkylated to bicyclononene L. This alkohol intermediate would be transformed into the ester M, and the Boc-protecting group can finally be cleaved to yield precursor N.





















From precuTsois prepared as described above, the final compounds can be prepared using parallel chemistry techniques. For the specific examples, see the experimental part.
Diazabicyclononenes of type of N can be acylated, or alkylated, or sulfonated, using standard procedures (Scheme 19), and then directly deprotected to yield the final compounds (for numbering, see specific examples). In each case, purification by preparative HPLC might give the corresponding TFA salts or formate salts.

Precursors R, II or BB (with a L-substituent at the N(3)-position) might be transformed into the corresponding aryl ethers (Scheme 20), using the Mitsunobu reaction conditions. After deprotection, the final compounds are obtained.





Enantioselective synthesis;
The compounds of the present invention contain at least two chiral centers which, however, are not independent from each other. The synthetic methods presented so far might Lead to racemates. Both enantiomers might be prepared selectively starting from a ?7;ejo-bicyclononane derivative, like compound AD (Blount B. K., Robinson, R., J. Chem. Soc, 1932, 2485) or AE, prepared similarly to compound A with a subsequent decarboxylation (Scheme 25). For instance, compound AE might be stereoselecti\'ely acylated to bicyclononane derivatives AF or AG as already described elsewhere for similar compounds (Majewski M., Lasny R., J. Org. Chem., 1995, 60, 5825). Similarly, the other enantiomer might be prepared.




optionally in combination %\ith other therapeutically valuable substances, into a galenical administration form together with suitable, non-toxic, inert, therapeutically compatible solid or liquid carrier materials and, if desired, usual pharmaceutical adjuvants.
Suitable carrier materials are not only inorganic carrier materials, but also organic carrier materials. Thus, for example, lactose, com starch or derivatives thereof, talc, stearic acid or its salts can be used as carrier materials for tablets, coated tablets, dragees and hard gelatine capsules. Suitable carrier materials for soft gelatine capsules are, for example, vegetable oils, waxes, fats and semi-solid and liquid poyols (depending on the nature of the active ingredient no carriers are, however, required in the case of soft gelatme capsules). Suitable carrier materials for the production of solutions and symps are, for example, water, polyols, sucrose, invert sugar and the like. Suitable carrier materials for injections are, for example, water, alcohols, polyols, glycerols and vegetable oils. Suitable carrier materials for suppositories are, for example, natural or hardened oils, waxes, fats and semi-liquid or liquid polyols. Suitable carrier materials for topical preparations are glycerides, semi-synthetic and synthetic glycerides, hydrogenated oils, liquid waxes, liquid paraffins, liquid fatty alcohols, sterols, polyethylene glycols and cellulose derivatives.
Usual stabilizers, preservatives, wetting and emulsifying agents, consistency-improving agents, flavour-improving agents, salts for varying the osmotic pressure, buffer substances, solubilizers, colorants and masking agents and antioxidants come mto consideration as pharmaceutical adjuvants.
The dosage of compounds of formula I can vary within wide limits depending on the disease to be controlled, the age and the individual condition of the patient and the mode of administration, and will, of course, be fitted to the individual requirements in each particular case. For adult patients a daily dosage of about I mg to about 1000 mg, especially about 50 mg to about 500 mg, comes into consideration.

The pharmaceutical preparations conveniently contain about 1 - 500 mg, preferably 5 - 200 mg of a compound of formula I.
The following examples serve to illustrate the present invention in more detail. They are, however, not intended to limit its scope in any manner.
Examples
General remarJcs
The compounds were characterized at least by LC-MS and 'H-NMR. Only the LC-MS data are given here.

Abbreviations
AcCl Acetyl chloride
ACE Angiotensin Converting Enzyme
AcOH Acetic acid
Ang Angiotensin
aq. aqueous
9-BBN 9-BorabicycIo[3.3.1]nonane
Bn Benzyl
Boo rer/-Butyloxycarbonyl
BSA Bovine serum albumine
BuLi n-Butyllithium
GDI 1,1 -Carbonyldiimidazol
cone. concentrated
DIBAL Diisobutylaluminium hydride
DIPEA Diisopropylethylamine
DMAP 4-A^, A^-DimethylamLnopyridine
DMF N, JV-Dimethylfonmamide

DMSO Dimethyl sulfoxide
EDCHCl Ethyl-A^A^-dimethylaminopropylcarbodiimidehydrochloride
EIA Enzyme immunoassay
eq. equivalent
Et Ethyl
EtOAc Ethyl acetaie
FC Flash Chromatography
HOBt Hydroxybenzotriazol
KHMDS Potassium hexamethyldisilazide
LAH Lithium aluminium hydride
MeOH Methanol
MPLC Medium Pressure Liquid Chromatography
NMO /^-Methylmoipholine A^-oxide
org. organic
PG protecting group
Ph Phenyl
RAS Renin Angiotensin System
RP18 Reversed phase column, filled with Cig hydrocarbon
rt room temperature
SBM Trimethylsilylethoxymethyl
sol. Solution
TBAF Tetra-n-butylammonium fluoride
TBDMS rer/-Butyldimethylsilyl
TBDPS /er/-Butyldiphenylsilyl
tBuOH fert-Butanol
tBuOK Potassium rerNbutylate
Tf Triiluoromethylsulfonyl
TFA Trifluoroacetic acid
THF Tetrahydrofuran
TLC Thin Layer Chromatography
TMAD iV^//'JV'-Tetraraethylazodicarboxamide

Preparation of the precursors
(rac.)-(lR*, 55*)-9-Methyl-7-oxo-3,9'diazabicycIo[3.3.1Inonane-3,6-dicarbo-xylic acid i-tert-hxityl ester 6-ethyl ester (A)
(4-Benzyl-6-ethoxycarbonyimethyl-l-m6thyl-piperazin-2-yl)acetic acid ethyl ester (Patent WO 92/05174) (71.0 g, 0.196 mol) was dissolved in MeOH (400 mL). TFA (77.8 mL, 1.02 mol) was added and the flask was purged with nitrogen. Pd/C (10%, 50% mojyture, 3.6 g) was added. The flask was closed and purged with hydrogen (3x). After 1 day, the mixture was filtered through Celile and washed with MeOH. The solvents were removed londer reduced pressure and the foamy residue (92.7 g) was dried under high vacuum. A sol. of tBuOK (117.2 g, 1.04 mol) in toluene (3.07 L) was heated to reflux. A sol of the crude piperaziue formerly obtained, dissolved in THF (300 mL), was added dropwise over 50 min. The black mixture was stirred for 10 flirther min. and allowed to cool to rt. The mixture was cooled to 0 °C and AcOH (36.6 mL, 0.635 mol) was added. The solvents were removed under reduced pressure. This crude material was suspended in CH2CI2 (400 mL) and cooled to 0 °C. DIPEA(19.1 mL, 112mmol) was added. A sol. of B0C2O (24.3 g, 113 mmol) in CH2CI2 (200 mL) was added dropwise. The mixture was stirred for I h at 0 "C, then 1 h at rt. The mixture was washed with aq, 10% Na2C03 (2x). The org. extracts were dried over MgS04, filtered and the solvents were evaporated under reduced pressure. The residue was purified by FC (EtOAc/heptane 1:1 ^ EtOAc). The title compound was obtained as oil (24.5 g, 38%). Rf = 0.05 (EtOAc/heptane 1:1) or 0.56 (MeOH/CHiCli 1:9), LC-MS: Ri= 2.94; ES+: 325.19.
{rac.)-{lR*, 5>S'")-9-]VIethyl-7-trifluoromethanesulfonyIoxy-3,9-diazabicycIo-[3.3.11non-6-ene-3,6-dicarboxylic acid 3-(err-butyl ester 6-ethyl ester (B)
A sol, of bicycloDonanone A (2.22 g, 6.80 mmol) in THF (50 mL) was cooled to 0 °C and NaH (about 60% in mineral oil, 326 mg, about 8.2 mmol) was added. A gas evolution was observed. After 20 rain, Tf2NPh (3.22 g, 9.00 mmol) was

added. 10 min later, the ice bath was removed. After 3 h, the sol. was diluted with EtOAc and washed with brine (Ix). The org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification by FC (EtOAclieptane 3:1 -? EtOAc) yielded the title compound as an oil (2.50 g, 80%). Rf = 0.15 (EtOAc/heptane 1:1). LC-MS: R, = 4.73; ES+: 458.95.
Compounds of type C
3-(4-Bromophenyl)prop-l-yl 2-ch!oropheny! ether (CI)
To a sol. of 3-(4-bromophenyl)propan-]-oI (Glover S. A., et al; Tet>-ahedron, 1990, 46, 7247; 24.5 g, 0.114 mol) in toluene (600 mL) under nitrogen were added 2-chlorophenol (17.4 mL, 0.171 mmol), diisopropyl azodicarboxylate (33.1 mL, 0.171 mol) and tri-/7-butylphosphine (42.2 mL, 0.171 mol). The sol. was heated to reflux and stirred under reflux overnight. The sol. was allowed to cool to rt and the solvents were removed under reduced pressure. The residue was diluted in EtOAc and washed with aq. IM HCl (ix) and aq. IM NaOH (2x). The org. extracts were dried over MgS04, filtered and the solvents were removed under reduced pressure. Purification of the residue by FC (petroleum ether —>■ EtaO/petroleum ether 1:99 -> 1:19) led to the title compound (15.1 g, 41%). Rf = 0.70 (EtOAc/heptane 1:3).
2-(4-BromophenyI)eth-l-yI 2^^-trimefiiyIphenyl ether (C2)
A mixture of 2-(4-bromophenyl)ethanol (20.0 mL, 143 mmol), 2,3,5-trimethylphenol (31.1 g, 229 mmol), azodicarboxylic dipiperidide (72.1 g, 286 mmol) and tributylphosphine (88 mL; 357 mmol) in toluene (2.00 L) was heated to reflux for 2 h. The mixture was allowed to cool to rt. The mixture was filtered, washed with toluene and the solvents were partially removed under reduced pressure. The residue was diluted with Et20 and washed with aq. IM NaOH (2x). The org. extracts were dried over MgS04, filtered, and the solvents were removed

under reduced pressure. Purification of the residue by FC (petroleum ether -> Et20/petroleuin etiier 1:3) >-ielded the title compound (33.1 g, 73%). LC-MS: R, = 6.95.
l-Bromo-4-[3-{2-methoxyhenzyl)propoxy]benzene (E)
4-Bromophenol (4.32 g, 25.0 mmol) and l-(3-chloropropoxyniethyi)-2'methoxy-benzene (Vieka E., et al, Bioorg. Med. Chem. Letters, 1999, P, 1397,4.88 g, 22.7 inmoL) were dissolved in DMF (150 mL). Nal (1.50 g, 0.10 mmol) and CS2CO3 (16.3 g, 50.0 mmol) were added. The mixture was heated to 80 °C and stirred for 6 h, before it was allowed to cool to rt. After dilution with EtOAc (600 mL) the mixture was washed with water (Ix), aq. IM NaOH (ix). aq. IM HCI (Ix). The org. extracts were dried over MgS04 and filtered. 7he solvents were removed under reduced pressure. Purification of the residue by FC (EtiO/petroleum ether 1:9 -> 1:4) yielded the title compound (5.66 g, 71%). Rf = 0.60 (EtiO/heptane 1:1).
5-Bromo-2-[3-(2-methox}'benzyloxy)propoxy|pyridine (F)
3-(5-Bromopyridin-2-yloxy)propan-I-ol (Patent Application WO 98/39328, 1.05 g, 4.51 mmol) was diluted at rt m DMF (24 ml) and the sol. cooled to 0 "C. NaH (55 - 65 weight % in mmeral oil, 193 mg, 4.42 - 5.23 mmol) was added and the yellow mixture was stirred for 20 min. 2-Methoxybenzyl chloride (1.49 ml, 10.7 mmol) was added and the solution was allowed to warm to rt and was stirred for 4 h. The mixture was quenched with ice and diluted with BtOAc (20 ml), washed with brine and water, dried over MgS04 and filtered. The solvents were evaporated under reduced pressure. Purification of the residue by FC (Et20, heptane 1:39 -> 1:19) yielded the title compound (627 mg, 40%) as an oil. Rf = 0.07 (Et20 / heptane, 1:3).
Compounds of type G

(rac.y{lR*, 55*>9-Methy[-7-[4-(2-triniethyisiIanyiethoxymethoxy)pbenyIl-3,9-diazabicycIo[3.3,l]non-6-ene-3,6-dicarboxyIic add 3-/er^butyI ester 6-ethyl ester (Gl)
A sol. of [2-(4'bromophenoxymethQxy)ethyl]trimethylsilane (Blass B. E., et ai, Tetrahedron Lett., 2001, 42, 1611, 4.13 g, 13.6 mmol) in TPIF (30 mL) was cooled to -78 °C. BuLi (1.6 M in hexane, 9.1 mL, 14.6 mmol) was added. The sol. was stirred at-78 °C for 30 mini A sol. of ZnCb, prepared from ZnCla (2.23 g, about 16.4 mmol) dried under high vacuum for 2 h at 140 °C and THF (35 mL), was added and the resulting sol. was allowed to warm up to rt. A sol. of bicyclononene B (2.50 g, 5-45 mmol) in THF ( 5 mL) and then Pd(PPh3)4 (157 mg, 0.136 mmol) were added. After 10 min, the reaction mixture was heated to reflux. After 90 min, the reaction mixture was allowed to cool to rt and quenched with aq. IM HCl. The mixture was diluted with EtOAc and washed with aq. 10% Na2C03(lx). The org. extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by PC (MeOH/CHiCL 1:39 -^ 1:24 ^ 1:20) yielded the title compound as an oil (2.90 g,99%). Rf= 0.39 (MeOH/CHjCb 1:9). LC-MS: Rt = 4.35; ES+: 533.29.
{racyilR*, 5S*)-7-{4-[2-(tert-Bntyldiinethy\silanyloxy)ethyllpfaenyl}-9-me-thyI-3,9-dia2abicyclopJ.l]non-6-ene-3,6-dicarboxyIic acid 3-^erf-butyI ester 6-ethyl ester (G2)
A sol. of [2-(4'bromophenyl)ethoxy]-terf-butyldimethylsilane (Fuji Kl., et aL, Tetrahedron Lett, 1990, 3J, 6553, 21.8 g, 69.1 mmol) in THF (250 mL) was cooled to-78 °C. BuLi (1.55M in hexane, 44.6 mL, 69.1 mmol) was added. The sol. turned temporarily orange, then yellowish. After 30 min, ZnCl2 (IM in THF, 70 mL, 70 mmol, prepared as described for Gl) was added. The sol. was allowed to warm up to rt. Vinyl triflate B (12.91 g, 28.2 mmol) dissolved in THF (20 mL), and Pd(PPh3)4 (600 mg, 0.519 mmoi) were added. The sol- was stmred at rt for 90 min and aq. IM HCl (1 mL) was then added. The mixture was diluted in EtOAc and washed with aq. IM NaOH (Ix). The org. extracts were dried over MgS04,

filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (MeOH/CH2Cl2 1:49 -> 1:24 -> 3:47 -)■ 2:25) yielded the title compound (10.91 g, 71%). Rf - 0.65 (MeOH/CHjCb 1:9). LC-MS: R, = 5.32; ES+: 545.49.
{rac.)-(JR*, 55*)-7-{4-[3-(fert-Butyldimethylsilanyloxy)propyl]phenyl}-9-rae-tIiyl-3,9-dia2abicyclQ[3.3.1]QQtt-6-ene-3,6-dicarboKylic acid S-terf-butjl ester 6-tthyl ester (G3)
A sol. of [3-(4-broraophenyl)propoxy]-Zer/-butyldimethylsilane (Kiesewetter D. O., Tetrahedron Asymmetry, 1993, 4, 2183, 22.60 g, 68.6 nuiiol) inTHF (250 mL) was cooled to -78 °C. BuLJ (1.55M in hexane, 44.3 mL, 68.6 mmol) was added. The sol. turned orange, then dark green. After 30 rain, 2nCl2 (IM m THF, 69 mL, 69 mmol, prepared as described for G2) was added, whereas the sol. turned deep yellow. The mixture was allowed to warm up to rt. Vinyl triflate B (12.91 g, 28.2 mmol) in THF (20 mL) and then Pd(PPh3)4 (600 mg, 0.519 mmol) were added. The mixture was stured at rt for 90 min and aq. IM HCl (1 mL) was added. The mixture was diluted with EtOAc and washed with aq. IM NaOH (Ix). The org. extracts were dried over MgS04, filtered and the solvents were removed under reduced pressure. Purification of the residue by FC (MeOH/CH2C]2 1:49 -> 1:24 -> 3:47 -^ 2:23) yielded the title product (10.76 g, 70%). Rf = 0.60 (MeOH/CH2a2l:9). LC-MS: R4 = 4.95;ES+: 559.51.
{rac.)-{lR*, 5S*)-7-{6-13-(2-Methoxyben2yloxy)propoxy]pyridiii-3-yl}-9-me-thyl-3,9-diazabicycloj3.3.11ni>n-6-ene-3,6-dicarboxylic acid Z-tert-hutyl ester 6-ethyl ester (G4)
A sol. of bromop>TidinyI derivative F (300 mg, 852 /anol) in THF (10 ml) was cooled to -78 "C. BuLi (1.55M in hexane, 0.580 ml, 889 /imol) was added and the mixture was stined for 30 min. ZnCl2 (IM in THF, 0.94 ml, 0.94 mmol, prepared as described for G2) was added and the reaction mixture was allowed to

warm up to rt. Vinyl trifiate B (259 mg, 596 fmol) in THF (1 ml), was added, followed by Pd(PPh3):i (20.4 mg, 16.6 /jmol). The mixture was refluxed for 2 h. The reaction was terminated upon addition of ice. After dilution with EtOAc (125 ml), the reaction mixture was washed with 10% aq. Na^COa and the org. extracts were dried over MgS04 and filtered. The solvents were evaporated under reduced pressure. Purification of the residue by FC (CHiCb/MeOH: 39:1 -^ 29:1 -> 24:1-> 19:1-^9:1) led to title compound (197 mg, 54%). Rf = 0.35 (CHjCb/MeOH 9:1). LC-MS: R, = 4.06; ES+: 582.78.
irac)-{JR*, 5.S'*)-7-{4-[3-(2~Methoxyben2yloxy)propoxyIphenyl}-9-methyl-3,9-dia2abicycIo[3.3.I]non-6-ene-3,6-dicarboxyIic acid 3-/'ert-butyl ester 6-ethyl ester (G5)
A sol. of bromophenyl derivative E (5.60 g, 15.9 mmol) in THF (50 mL) was cooled to -78 °C. BuLi (1.55M in hexane, 10.3 mL, 15.9 mmol) was added. The sol. was stirred at -78 °C for 3D mm and ZnCb (IM in THF, 17.5 mL, 17.5 mmol, prepared as described for G2) was added. After warming up to rt, a sol. of vinyl trifiate B (3.63 g, 7.90 mmol) in THF (5 mL), followed by Pd(PPh3)4 (205 mg, 0.177 mmol), were added. The mixture was heated to reflux while turning black. After I h, the reaction mixture was allowed to cool to rt. Ice was added and the mixture was diluted in EtOAc. The org. extracts were washed with aq. IMNaOH (Ix) and dried over MgSO*- The solvents were removed under reduced pressure. Purification of the residue by FC (MeOH/CHaCla 1:49 ->■ 3:97 ^ 1:24 -»■ 1:19 -)• 1:9) yielded the title compound (4.57 g, 99%). Rf = 0.50 (MeOH/CH2Cl2 1:9). LC-MS: R, = 4.17; ES+: S%\ .60.
irac.)-{lR% 55*)-7-{4-[3-(2-ChloropheQoxy)propyl]phenyI}-9-methyI-3,9-di-azabicycIo[3.3.1Jnon-6-ene-3,6-dicarboxylic acid 3-fef/-butyl ester 6-ethyI ester (G6)
A sol. of bromophenyl derivative CI (16.0 g, 49.0 mmol) in THF (700 mL) was cooled to -78 "C. BuLi (1.55M in hexane, 34.8 mL, 54.0 mmol) was added. The

sol. was stined ai -78 °C for 30 min and ZnCl2 (IM in THF, 54.0 mL, 54.0 mmol, prepared as described for G2) was added. After -warming up to rt, a sol. of vinyl triflate B (15,0 g, 32.7 nrniol) m THF (50 mL), followed by Pd(PPii3)4 (945 mg, 0.818 mmol), were added. The sol. was heated to xellux. After 30 min, tire reaction mixture was allowed to cool to rt. ice was added and the mixture was diluted in EtOAc. The org. phase was washed with aq. IM NaOH (Ix) and dried over MgS04. The solvents were removed under reduced pressure. Purification of the residue by FC (MeOH/CH2Cl2 1:49 -> 3:97 -> 1:24 -^ 1:19 -» 1:9) yielded the title compound (10.5 g, 58%), LC-MS: R, = 4.41; ES+: 555.13.
(rac)-{lR*y 55'*)-7-{4-[2-(fer^ButyIdimethylsilanyloxy)ethoxylphenyl}-9-
methyI-3,9-diazabicycIo[3.3.11uon-6-eiie-3,6-dicarbi>xyIic acid 3-/er/-butyI ester 6-ethyl ester (G7)
BuLi (1.6 M in hexane, 218 mL, 350 mmoi) was added to a sol. of [2-(4-bromo-phenoxy)ethoxy]-rerf-butyIdimethylsilane (Merita, C; et al.al.; Heterocycles, 2000, 52, 1163; 129 g, 342 mmol) in THF (I.OL) at -78 °C. The mixture was stirred for 1 h at -78 °C, and ZnCb (IM in THF, 400 mL, 400 mmol, prepared as described for G2) was added. The mixture was allowed to warm up to rt. Bicyclononene B (78.4 g, 171 mmol) and PdCPPli3)4 (4.94 g, 4.28 mmol) were added. The mixture was heated to reflux for 0.5 h, and was allowed to cool to rt. Aq. IM HCl (2 mL) was added. The mixture was diluted with EtOAc (2 L) and washed with aq. IM NaOH (750 mL). The aq. extracts were extracted back with EtOAc (Ix). The combined org. extracts were dried over MgS04, filtered, and the solvents were removed mider reduced pressure. Purification of the residue by FC (MeOH/CHiCIa 1:49 -> 1:24 ^ 3:47 -^ 2:23) yielded the title compound (87.7 g, 91°/o). Rf= 0.60 (MeOH/CH2C12 1:9). LC-MS: Rt = 4.74; ES4-: 561.41.
irac.)-{lR*, 5.S*)-7-{4-[2-(/^/■^Buty!diphenylsUanyloxy)ethyI]pbenyl}-9-
methyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxyIic acid 3-fert-butyl ester 6-ethyl ester (G8)

BuLi (1.5 M in hexane, 13.4 mL, 20 mmol) was added to a sol. [2-(4-bromo-phenyl)ethoxy]-rer£-butyidiphenylsilane (8.79 g, 20.0 mmol, prepared &om 2-(4-bromophenyl)ethanol, TBDPS-Cl and imidazol in DMF) in THF (40 mL) at -78 °C. The mixture was stirred for 30 min at -78 °C, and ZnCh (IM in THF, 24 mL, 24 mmol, prepared as described for G2) was added. The mixture was allowed to warm up to rt. Bicyclononene B (3.67 g, 8.00 mmol) and Pd(PPh3)4 (231 mg, 0.20 mmol) were added. The mismre was heated to 40 °C for 40 min, and was allowed to cool to rt. Aq. IM HCl (2 itiL) was added. The mixtire was diluted with EtOAc and washed with aq. IMNaOH. The aq. extracts were extracted back with EtOAc (Ix). The combined org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (MeOH/CH2C]2 1:49 -> 1:24 -> 3:47 -^ 2:23) yielded the title compound (4.32 g, 81%). LC-MS: R,= 1.06; ES+: 669.49.
Compounds of type H
{rac.y(lR*, 55*)-7-[4-(2-TrlmethylsiIanylethoxyniethoxy)phenyl]-3,9-dia2abi-cyclo[3.3.1]non-6-ene-3,6,9-tricarborylic acid 3-i'^rf-butyI ester 6-ethyl ester 9-(2,2,2-trichIoro-l,l-dimethylefhyl) ester (HI)
p,P,p—Trichloro-i'er^butyl chloroformate (6.60 g, 27.5 mmol) was added to a sol. of bicyclononene Gl (2.93 g, 5.50 mmol) m 1,2-dichloroethane (60 roL). The sol. was heated to reflux. After 3 h, the reaction mixture was allowed to cool to rt, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAcAieptane 1:4 -> 1:3 ->■ 2:3 ~-> 1:1) yielded the title compound as an oil (3.31g,83%). Rf= 0.52 (EtOAc/heptane 1:1). LC-MS; Rt = 7.40; ES+: 742.52.
{racy{JR*, 55*)-7-{4-[2-(/ert-Butyldimethylsilanyloxy)ethyl]phenyl}-3,9-di-azabicyclo[3.3.1 Jnon-6-ene-3,6,9-tricarboxylic acid 3-/^rt-butyl ester 6-ethyl ester 9-(2,2^-trichloro-l,l-diinethylethyI) ester (H2)

As for tlie preparation of compound HI, from bicyclononene G2 (10.91 g, 20.0 mmol), P,p,p-trichIoro-/'e;-(-buty] chloroformate (24.0 g, 100 mmoi), and 1,2-dichloroethane (210 mL). Purification of the residue FC (EtOAc/heptane 1:9 -> 1:4 ->2:3) yielded the title compound (13.75 g, 94%). Rf = 0.64 (EtOAc/lieptane 1:1). LC-MS:Ri-7.66; ES+: 755.37.
irac.)'{lR\ 55*)-7-{4-[3-(/ert-Butyldiraethylsilanyloxy)propyl]phenyli-3,9'di-azabicycIo[3.3.1!QOtt-6-ene-3,6,9-tricarbox5'Iic acid 3-tert-butyl ester 6-ethyl ester 9-(2,2,2-trich!oro-l,l-dimethyletfayl) ester (H3)
As for the preparation of compound HI, from bicyclononene G3 (10.96 g, 19.6 mmol), p,p,j3-frichloio-re?'/-butyl chloroformate (23.5 g, 98.1 mmol), and 1,2-dichloroethane (210 mL). Purification of the residue by FC (EtOAc/heptane 1:9 ^ 1:4 -s- 2:3) yielded the title compound (13.50 g, 92%). Rf = 0.58 (EtOAc/heptane 1:1). LC-MS: Rt = 7.79; BS+: 769.49.
(rac.y(lR*, J5*)-7-{6-[3-(2-MethoxybenzyIoxy)propoxyIpyridin3-yi}-3,9-di-azabicycIo[3.3.1]non-6-ene-3,6,9-tricarboxyIic acid 3-/er/-butyI ester 6-etbyI ester 9-(2,2,2-trichIoro-l,l-dimethylethy() ester (H4)
As for the preparation of compound HI, from bicyclononene G4 (373 mg, 0.642 mmol), Pjp.p-trichloro-i'err-butyl chloroformate (770 mg, 3.11 mmol), and 1,2-dichloroethaue (8 mL). Purification of the residue by FC (EtOAc/heptane 1:9 -> 1:4 -> 1:3) yielded the title compound (382 mg, 77%). Rf = 0.47 (EtOAc/heptane 1:1). LC-MS: R, = 7.14; ES+: 770.50.
(rac.)-(IR*, 55*)-7-{4-[3-(2-Methox>'benzyIoxy)propoxylphenyI}-3,9-dia2abi-cyclo[3.3.11non-6'ene-3,6,9-tricarboxylic acid 3-tert-buti'l ester 6-ethyl ester 9-(2,2^-trichloro-l,l-diraethyIethyI) ester (H5)
As for the preparation of compound HI, from bicyclononene G5 (4.57 g, 7.87 mmol), p,p,p-trichloro-terr-hutyl chloroformate (9,44 g, 39.4 mmol), and 1,2-

dichloroethane (100 mL). Purification of the residue by FC (EtOAc/heptane 1:9 -> 1:4 -)■ l-.l) yielded the title compound (5,35 g, 88%). Rf = 0.46 (EtOAc/heptanel:!).
(rac.)-{lR*, 5S*)-7-{4-13-(2-Chlorophenox)')propyl]phenyl}-3,9-diazabicyclo-(3.3.1]non-6-ene-3,6,9-tricarboxyIic acid 3-to-J'-butyI ester 6-ethyI ester 9-(2,2,2-trichioro-l,l-dimethylethyl) ester (H6)
As for the preparation of compound HI, from bicyclononene G6 (10.51 g, 18.9 mmol), p,p,p-trichloro-?^r?-butyI chloroformate (22,7 g, 94.7 mmol), and 1,2-dichloroethane (350 mL). Purification of the residue by FC (EtOAc/heptane 1-.8 -> ]:4-j- 1:1) yielded tlie title compound (12.5 g, 88%).
{rac.y{}R% 5S*)-7-S4-l2-(te/^Butyldimethylsilanyloxy)ethoxy]phenyl}-3,9-diazabicyclo (3.3.1] noQ-6-ene-3,6,9-fricarboxyIic acid 3'tert'buty\ ester 6-ethyI ester 9-(2,2,2-trichloro-l,l-
As for the preparation of compound HI, from bicyclononene G7 (87.7 g, 156 mmol), fi,p,p-trichloro-rerr-butyl chloroformate (188 g, 784 mmol), and 1,2-dichloroethane (1.75 L). Purification of the residue by FC (EtOAc/heptane 1:19 -^ 1:3) yielded the title compound (111 g, 95%). Rf = 0.75 (EtOAc/heptane 1:1). LC-MS:Rt = 7.84.
irac)'{lR*, 55*)-7-{4-[2-(/er/-ButyldiphenyIsiIanyIoxy)ethyl]phenyI}-3^-
dia2abicyclo[3.3.11non-6-ene-3,6,9-tricarboxyIic acid 3-ferf-butyl ester 6-ethyl ester 9-(2;2,2-trichloro-l,l-diinethylethyl) ester (H8)
As for the preparation of compound HI, from bicyclononene G8 (4.32 g, 6.46 mmol), p,p,p-trichloro-?e/-/-butyl chloroforaiate (7.75 g, 32.3 mmol), and 1,2-dichloroethane (100 mL). Purification of the residue by FC (EtOAc/heptane 1:19 -^ 1:3) yielded the title compound (4.97 g, 90%). Rf = 0.75 (EtOAc/heptane 1:1). LC-MS-.Rt=1.35.

Compounds of type J
(rac.)-(JR*, 5xS'*)-6-HydroxyiiiethyI-7-[4-(2~trimethylsiIanyletho\ymethoxy)-phenyil-3,9-diazabicyclo[3.3.1]non-6-ene-3, 9-dicarboxyJic acid 3-/fr/-butyI ester 9-(2,2,2-tricliloro-l,l-dimethyletbyl) ester (Jl)
A sol. of bicyclononene HI (3.31 g, 4.58 mmol) in CH2CI3 (60 mL) was cooled to -78 °C. DIBAL (IM in toluene, 10.1 mL, 10.1 mmol) was added. The sol. was stirred for 30 min at -78 °C and was then allowed to warm slowly. DIBAL (5 mL) was added again after 1.5 h (-65 °C). Later, DIBAL was added successively in 5 mL-portions until TLC displayed no more starting material. Ice and water were then added at —50 "C. The cold bath was removed and the mixture warmed slowly to rt. More CH2CI2 was added and the mixture was washed with aq. IM HCl. The aq. phase was extracted with CH2CI2 (Ix) and the combuned org. extracts were dried over MgS04. After filtration and evaporation of the solvents under reduced pressure, the residue was purified by FC (EtOAc/heptane 1 ;4 -> 1 ;3 "> 2:3) to yield the title compound as an oil (L89 g, 60%). Rf ^ 0.50 (EtOAc/heptane 1:1). LC-MS; Ri^ 7.08; ES+: 661.38, 702.83.
(rac.y(lS*, 5iS*)-7-{4-2-(tert-ButyldimethylsiIanyloxy)ethyl]phenyI}-6-hydro-symethyI-3^-diazabicycIo(33.1]non-6-ene-3,9-dicarboxylic acid 3-tert~batyl ester 9-(2,2,2-trlchloro-l,l-diinethyIethyl) ester (J2)
To a sol. of bicyclononene H2 (1.57 g, 2.32 mmol) m CH2CI2 (40 mL) at -78 'C DIBAL (IM in toluene, 5.80 mL, 5.80 mmol) was added. The sol. was stirred at -78 °C for 1 h. Ice was added, and the mixture was allowed to warm up to rt. More CH2CI2 was added and the org. extracts were washed with aq. IM HCI (Ix), dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:3) yielded the title compound (868 mg, 59%). LC-MS: Rt = 7.38; ES+: 715.48.

(racyilR*, 55*)-7-{4-[3-(ter/-ButyIdlmefhyIsilanyIoxy)propyl]phenyl}-6-hy-droxymethyI-3,9-diazabicyclo(3.3.1]non-6-ene-3,9-dicarboxyIic acid 2i-tert-butyl ester 9-(2,2,2-trichloro-l,l-dimethylethyI) ester (J3)
A sol of bicyciononene H3 (2.39 g, 3.20 mmol) in CHiCta (55 mL) was cooled to -78 °C. DIBAL (IM in toluene, 8.00 mL, 8.00 mmol) was added and the mixture was stirred at -78 "C fot 1 h. Ice was added, and the mixture was allowed to warm up to rt. More CH2CI2 was added and the org. extracts were washed with aq. IM HCl (Ix), dried over MgSO^ and filtered. The solvents were removed under reduced pressure. Purification of tlie residue by FC (EtOAc/heptane 1:3) yielded the title compound (1.34 g, 59%). LC-MS: R, = 7.59; ES+: 727.54.
{rac.')-{lR*, 5iS*)-6-Hydroxyinethyl-7-{6-[3-(2-metboxybeiizyloxy)propoxy]-pyridiii-3-yl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxyUc acid 3-tert-butyl ester 9- A sol. of bicyciononene H4 (345 mg, 0.447 mmol) in CH2CI2 (10 roL) was cooled to -78 "C. DIBAL (IM m toluene, 1.92 mL, 1.92 mmol) was added. The mixture was stirred at -78 °C for 1 h and again two portions of DIBAL (0.50 mL, 0.50 mmol) were added successively. After 2 h, ice was added. The mixture was allowed to warm up to rt and was diluted with more CH2CI2. The org. extracts were washed with aq. 10% NaaCOa (2x), dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:4 -^ 1:3 -> 2:3 ~> 3:1) yielded the title compound (122 mg, 37%). Rf= 0.36 (EtOAc/heptane 1:1). LC-MS: Rt = 6.51; ES+: 728.49.
{rac)-(JIi% 5i?*)-6-HydroxymethyI-7-(4-hydroxyphenyI)-3^-diazabicycIo-[33.1Inon-6-ene-3,9-dicarboxyUc acid 3~/ert-butyl ester 9-(2,2,2-trichloro-l,l-dimethylethyl) ester (K)
To a sol. of bicyciononene Jl (1.89 g, 2.79 mmol) in THF/MeOH (1:1, 20 mL), a sol. of cone. H2SO4 (0.100 mL) in MeOH (10 mL) was added. The mixture was

stirred for 3 h at rt. The reaction mixture was diluted with EtOAc, washed with brine (Ix) and aq. sat. NaHC03 (Ix). The org, extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Crystallization of the residue from ElOAc/heptane led to the title compound (1.03 g, 67%). Rf = 0.14 (EtOAc/heptane 1:1). LC-MS: R, = 5.17; ES-: 547.06.
{rac.y{lR*, 55 *)-6-Hydrosym ethyl-7-{4-(3-(2-methoxybenzy Ioxy)propoxy]-phenyl}-3,9-diazabicycIo[3.3.1]non-6-eue-3,9-dicarboxyiic acid 3-/eri-butyl ester 9-(2,2,2-trichIoro-l,l-dimethylethyl) ester (L)
To a sol. of bicyclononene K (1.03 g, 1.87 mmol) in DMF (20 mL) were added Nal (280 mg, 1.87 mmol), CS2CO3 (609 mg, 1.87 mmol) and then l-(3-chJoropropoxymethyl)-2-methoxybenzene (Vieira E., et al, Bioorg. Med. Chem. Letters, 1999, 9, 1397, 400 mg, 1.87 mmol)- The mixture was stirred at 100 "C. After 1.5 h, another portion of CS2CO3 (609 mg, 1.87 mmol) and l-(3-chloropropoxymethyl)-2-methoxybenzene chloride (400 mg, 1.87 mmol) were added to complete the reaction. After 1.5 h later, the mixture was allowed to cool to rt and diluted with EtOAc. The org. extracts were washed with brine (Ix). The org. extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (ElO Ac/heptane 1:4 ->■ 1:3 -^ 2;3) yielded the title compound (1.00 g, 73%). Rf = 0.35 (EtOAc/heptane 1:1). LC-MS: Ri = 6.54.
{rac)-{lR*, 55*)-7-{4-[3-(2-Methoxyben2yIoxy)propoxy]phenyI}-6-[2-(2-me-thoxypfaenyI)acetoxymethyI]-3,9-diazabicycIo[33.1]non-6-ene-3,9-dicar-boxylic acid 3-/ert-butyl esfer 9-(2,2,2-trichloro-l,l-dimefliyIethyl) ester (M)
To a sol. of bicyclononene L (500 mg, 0.687 mmol) in CH2CI2 (10 mL) were added (2-methoxyphenyl)acetic acid (206 mg, 1.37 mmol), DMAP (cat. amount),
DIPEA (0.230 mL, 1.34 mmol) and EDC-HCl (134 mg, 0.700 mmol). The sol. was stirred at rt for 90 min, when a second portion of DIPEA (0.100 mL, 0.584 mmol) was added. After 3 h, the reaction mixture was diluted in more CH2CI2

and washed witii water (Ix). The org. extracts were dried over MgS04, filtered, and the solvents were remo\'ed under reduced pressure. Purification of the residue by FC (EtOAc/heptane i:4 -> 1:3 -> 2\2>) yielded the title compound (495 mg, 82%). Rf-0.42 (EtOAc/heptane 1:1). LC-MS: Rt = 7.33; ES+: 897.33.
irac.)-ilR*, 55*)-7-{4-13-(2-Methoxybenzyloxy)propoxyiphenyl}-6-[2-(2-nie-thoxyp heny l)acetoxymethy I] -3,9-diazabicycIo [3.3,1] no a-6-ene-9-carboxyIic acid 2,2^-trichloro-l,l-dimeth>iethyi ester hydrochloride salt (N)
A mixture of CH2CI2 (3 raL) and HCl/dioxane (4M, 1 mL) was slowly added to bicyclononene M (495 mg, 0.585 mmol) in an ice bath. The resulting sol. was stined at 0 °C. After 1 h, HCl/dioxane (4M, 0.5 mL) was added, and 1 h later the ice bath was removed. After 75 min, the solvents were removed under reduced pressure and the residue dried under high vacuum. The resulting foam was estimated to contain about 80% of the title compound according to LC-MS and was used without fiuther purification. LC-MS: Ri = 4.97; ES+: 774.97.
{rac)-{IR*, 55*)-6-[2-(2-Methoxyphcnyl)acetoxymethyll-7-{6-13-(2-methoxy-benzyIoxy)proposy]pyridm-3-yI}-3,9-diazabicyclo [3.3.1 Jnon-6-ene-3,9-dicar-boxylic acid 3-tert-butyl ester 9-(2;2^-trichIoro-l,l-dunefhyIefhyl) ester (O)
To a sol. of bicyclononene J4 (122 mg, 0.167 mmol) m CH2CI2 (5 mL) were added (2-methoxypheny!)acetic acid (50 mg, 0.328 mmol), DIPEA (0.126 mL,
0.740 Eomol), DMAP (cat. amount) and EDCHCl (34 mg, 0.173 ramol). The mixture was stirred at rt for 3 h, then diluted in CH2CI2, and washed with washed with water (Ix). The org. extracts were dried over MgS04 and filtered. The solvents were removed vmder reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:4 -> 1:3 ->■ 2:3 -> 1:1) yielded the title compound (108 mg, 74%). LC-MS: R, = 7.34; ES+: 876.54.

(/■flc.)-{7if% 55-^)-7-{6-[3-(2-Methoxybenzyloxy)propoxylpyridin-3-yl}-6-12-(2-me{hoxyph£ny!).'icetoxyniethyI]-3,9-diazabicyc!o[3.3.11non-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-dimethyIethyl ester dihydrochloride salt (P)
Bicyclononene O (114 mg, 0.130 mmol) was dissolved in CH2CI2 (2 ml.). The sol. was cooled to -40 °C and 4M HCi/dioxane (2 mL) was added. The sol. was stirred for 50 min while warming up slowly to 0 °C and then stirred for 1.5 h at 0 °C. The solvents were rapidly removed under reduced pressure. The residue was dried under high vacuum to give the title compoimd (156 mg) as a foam that was used without further purification. LC-MS: R, = 4.S6; ES+: 776.48.
Compounds of type Q
irac.)-(lR*, 55*)-7-{4-[2-(to-/-ButyIdimethylsilanyIoxy)etIiylJphenyl}-6-[2-(2-methoxyphcnyl)aceto_\ymethyl]-3,9-diazabicycIoI3.3.1]non-6-ene-3,9-dicar-boxylic acid 3-tert-butyI ester 9~(2,2,2-trichIoro-l,l-dimethylethyI) ester (Ql)
To a sol. of bicyclononene J2 (868 mg, 1.25 mmol) in CH2CI2 (20 mL) were added (2-methoxyphenyl)acetic acid (343 mg, 2.06 mmol), DIPEA (0.652 mL,
3.81 mmol), DMAP (cat. amount), and EDC-HCl (201 mg, 1.05 mmol). The
mixture was stirred at rt for 1 h and EDC-HCl (73 mg, 0.38 mmol) and DIPEA (0.163 mmol, 0.952 mraol) were added again. After 30 min. the reaction mixture was diluted with CH2CI2, washed with aq. IM HCl (Ix), and aq. sat. NaHCOa (Ix). The org. extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:3) yielded the title compound (948 mg, 90%). LC-MS: Rt = 7.98; ES+: 861.51.
(rac.)-(lR% 5,S*)-7-{4-[3-(fert-ButyIdimethylsilanyloxy)prDpyl]phenyl}-6-[2-(2-methoxyphenyl)acetoxymethyll-3,9-diazabicyc\o[3.3.11non-6-en£-3,9-dicar-boxylic acid 3-tert-hutyl ester 9-(2,2,2-trichIoro-l,l-dimethyIethyl) ester (Q2)

Toasol. ofbicyclononene J3 (1.34 g, 1.90 mmol) in CH2CI2 (30 mL), were added 2-methoxypheny!acetic acid (633 mg, 3.81 mmol), DIPEA (0.652 mL, 3.81
mmol), DMAP (cat. amount), and EDC'HCl (402 mg, 2.09 mmol). The sol. was
stirred at rt for 1 h and EDC-HCl (73 mg, 0.38 mmol) and DIPEA (0.163 mmol, 0.952 mmol) were added again. After 30 min., the reaction mixture was diluted with CH2CI2, washed with aq. IM HCl (Ix) and aq. sat. NaHCOa (Ix). The org. extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:3) yielded the title compound (1.47 g, 90%). LC-MS: Rt = 8.17; ES-f: 875.53.
Compounds of type R
{rac.)-(lR*, 55*)-3-AcetyI-7-{4-(2-hydroxyethyl)phenyl]-6-[2-(2-metboxy-
phenyl)acetoxymethyI]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid 2,2,2-trichIoro-l,i-dimethyIethyl ester (Rl)
Bicyclononene Ql (948 mg, 1.13 mmol) was dissolved in CH2CI2 (20 mL). The sol. was cooled to 0 "C and 4M HCl/dioxane (20 mL) was added. After 2.25 h the solvents were rapidly removed under reduced pressure, and the residue was immediately dried under high vacuum. The resulting foam was then dissolved in THF (55 mL) and cooled to -78 °C. DIPEA (0.774 mL, 4.51 mmol) and DMAP (cat. amount) were added, followed by the addition of acetyl chloride (0.064 mL, 0.91 mmol). After 2.5 h at -78 "C, MeOH (20 mL) was added, and the reaction mixture was allowed to warm to rt. The reaction mixture was diluted in EtOAc, washed with aq, 1 M HCl (Ix), and the org. extract were dried over MgS04 and filtered. The solvents were removed under reduced pressiu-e. Purification of the residue by FC (EtOAc/heptane 1:2) yielded the title compound (651 mg, 55%). LC-MS: R, = 5.47; ES+: 689.05.
irac.)-(lR*, 55*)-3-Acetyl-7-[4-(3-hydroxypropyl)phenyl]-6-[2-(2-methoxy-phenyl)acetoxymethylI-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-dimethylethyl ester (R2)

To a sol. of bicyclononene Q2 (1.47 g, 1.72 ramol) in CH2CI3 (25 riiL), 4M HCi/dioxane (25 mL) was added at 0 °C. After 2.25 h at 0 "C the solvents were rapidly removed under reduced pressure, and the residue was immediately dried under high vacuum. The resulting foam was then dissolved in THF (75 mL) and cooled to -78 °C. DIPEA (1.18 niL, 6.88 mmol) and DMAP (cat. amount) were added, followed by slow addition of acetyl chloride (0.098 niL, L38 nunol). After 2.5 h at - 78 °C MeOH (80 mL) was added, and the reaction mixture was allowed to warm up to rt. Afler dilution with EtOAc, the mixture was washed with aq. 1 M HCl (Ix) and the org. extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:2) yielded the title compound (651 mg, 55%).
Compounds of type S
(rflc.)-(Jfl*, 5S*)-3~Acetyl-7-{4-13-(2-mcthoxybenzyloxy)propoxylphenyl}-3,9-diazabicyclo[33.1]non-6-eoe-6,9-dicarboxyIic acid 6-ethyl ester 9-(2,2,2-trichloro-l,l-dimethylethyl) ester (SI)
A sol. of bicyclononene H5 (5.35 g, 6-95 nunol) in CH2CI2 (30 mL) was cooled to 0°C. 4M HCl/dioxane (30 mL) was added. The sol. was stirred at 0 °C for 3.5 h, the solvents were removed under reduced pressure and the residue dried at high vacu^Im. The resulting foam was dissolved in THF (100 mL) and cooled to -78 "C. DIPEA (5.80 mL, 34.7 mmol) was added. A sol. of acetyl chloride (0.494 mL, 6.95 nmaol) in THF (10 mL) was added slowly. The leacton mixture was stirred at -78 °C for 90 min, then allowed allowed to warm to rt and diluted in MeOH (5 mL), then in EtOAc. The org, extracts were washed with aq. IM HCl (2x), aq. sat. NaHCOa (Ix), dried over MgS04, filtered and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:4 -> 1:3 -» 1:1 -> EtOAc) yielded the title compound (3.67 g, 74%). Rf= 0.50 (EtOAc). LC-MS: 6.22;ES+: 7n.3L

(racy(lR*, 55*)-3-Acet>'I-7-{4-[3-(2-chIoropfaenoxy)propyl]phenyI}-3,9-di-azabicyclot3.3.1]non-6-ene-6,9-dicarboxylic acid 6-ethyl ester 9-(2,2^-trichIoro-l,l-dmiethylethyl) ester (S2)
As for compound SI, from H6 (10.8 g, 14.5 mmol), CH2CI2 (110 mL), 4M HCl/dioxane (110 mL), THF (220 mL), DIPEA (12.4 mL, 72.6 mmol), DMAP (89 mg, 0.73 mmol), acetyl chloride (1.24 mL, 17.4 mmol), and MeOH (5 mL). Purification of the residue by FC (EtOAc/heptane 1:3 -> 1:1 -^ EtOAc) yielded the title compound (8.59 g, 86%). Rf = 0.43 (EtOAc). LC-MS: 6.32; ES+: 684.99.
(racyilR*, 5>y*)-3-Acetyl-7-[4-(2-hydroxyethyI)phenyI]-3,9-diazafaicyclo-
(3.3.1]non-6-ene-6,9-dicarfaoxylic acid 6-ethyI ester 9-(2^,2-trichIoro-l,l-dimethylethyl) ester (S3)
As for compound SI, from H2 (3.00 g, 4.08 mmol), CH2CI2 (30 mL), 4M HCl/dioxane (30 mL), THF (60 mL), DMAP (25 mg, 0.204 mmol), DIPEA (2.74 mL, 16.4 mmol), acetyl chloride (0.343 mL, 4.08 mmol), and MeOH (5 mL). Purification of the residue by FC (EtOAc/heptane 1:1 -> EtOAc -> MeOH/EtOAc 1:9) led to the title compound (1.80 g, 79%). Rf= 0.20 (EtOAc).
(raay-ilR*, 55*)-3-AcetyI-7-[4-(2-hydroxyethoiy)pheiiyII-3,9-diazabicyclo-l33.1]non-6-ene-6,9-dicarboxyIic acid 6-etfayl ester 9-(2;2,2-trichIoro-l,l-dimethyletbyl) ester (S4)
As for compound SI, from H7 (5.80 g, 7.73 mmol), CH2CI2 (60 mL), 4M HCVdioxane (60 mL), THF (50 mL), DMAP (47 mg, 0.384 mmol), DIPEA (5.29 mL, 31.7 mmol), acetyl chloride (0.604 mL, 8.08 mmol), and MeOH (5 mL). Purification of the residue by FC (EtOAc/heptane 1:1 -> EtOAc -> MeOH/EtOAc 1:9) led to the title compound (3.07 g, 69%). Rf - 0.20 (EtOAc). LC-MS: R, = 4.80; ES+: 576.93.

{rac.)-iIR*, 55*)-3-Acetyl-7-[4-(3-UydrQsypropyl)pheny[l-3,9-diazabicyclQ-[3.3.1]non-6-ene-6,9-dicarboxyUc acid 6-ethyI ester 9-(2,2,2-trichIoro-l,l-dimethylethyi) ester (S5)
As for compound SI, from H3 (5.04 g, 6.74 mmol), CH2CI2 (80 niL), 4M HCl/dioxane (80 mL), TIIF (80 mL), without DMAP, DIPEA (4.62 niL, 27.0 mmol), acetyl chloride (0.430 mL,6.06 mmo!), and iVleOH (5 mL). Purification ofthe residue by FC (EtOAc/heptane 1:1 -> EtOAc -> MeOH/EtOAc 1:9) led to the title compound (3.23 g, 83%). Rf = 0.20 (EtOAc). LC-MS: Rt - 1.00; ES+: 575.13.
Compounds of type T
(i-ac.)-(lR*, 55*)-3-Acetyl-7-{4-(3-(2-methox7beuzyloxy)propoxylphenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6,9-dicarboxylic acid 9-(2,2,2-frichloro-l,l-dimethylethyl) ester (Tl)
To a sol. of bicyclononene SI (3.67 g, 5.15 mmol) in EtOH (27 mL) was added aq. NaOH (IM, 27 mL, 27 mmol). The mixture was heated to 80 °C for 3 h and then allowed to cool to rt. After adjustment ofthe pH to 1-2 with aq. IM HCl and extraction with EtOAc (2x), the combined org. extracts were dried over MgS04, filtered, and evaporated under reduced pressure. Purification ofthe residue by FC (EtOAc/heptane 1:1 -^ 3:1 -> EtOAc -^ MeOH/EtOAc 1:9) yielded the title compound (1.45 g, 41%). LC-MS; Rt = 5.50; ES+: 683.24.
(rac.)-(JR% 5;y*)-3-AcetyI-7-(4-|3-(2-chlorophcnoxy)propyl]phenyl}-3,9-
diazabicycIo[3.3.1]non-6-ene-6,9-dicarboxylic acid 9-(2,2,2-trichloro-l,l-dimethylethyl) ester (T2)
From bicyclononene S2 (8.59 g, 12.5 mmol) the title compound (4.29 g, 52%) was obtained after purification by FC (MeOH/CHiCli 1:99 -)■ 1:49 -> 3:97 ^ 1:24) as described for Tl. LC-MS: R, = 5.61; ES-: 655.24.

(racyilR*, 55*)-3-Acetyl-7-[4-(2-hydroxyethoxy)phenyl]-3,9-diaza-
bicyclo[3.3.11iion-6-ene-6,9-dicarboxyUc acid 9-(2,2^-trichloro-l,l-dimethyl-ethyl) ester (T3)
From bicyclononene S4 (3.07 g, 5.73 mmol) in EtOH (119 mL) and aq. IMNaOH (i 19 mL) the title compound (1.88 g, 60%) was obtained after purification by PC (MeOH/CH2Cl2 1:99 -^ 1:49 -> 3:97 -> 1:24) as described for Tl. LC-MS: R, = 4.32; ES+: 548.96.
{rac.)-{lR*, 5S*)-3-AcetyI-7-{4-[3-(j'^rt-butyldimethybiIanyIoiy)propyl]-
phenyl}-3,9-diazabicyeIo[33.1Jnon-6-ene-6,9-dicarboxyIic acid 9-(2,2,2-trichlorQ-l,l-dimethylethyl) ester (T4)
A mixture of bicyclononene AZl (1.60 g, 2.93 mmol), imidazol (797 mg, 11.7 mmol) and TBDMS-Cl (l.l g, 7.30 mmol) in DMF (20 mL) was stirred at rt overnight. Aq. sat. NH4CI was added and the mixture was extracted with hexane (3x). The combined org- extracts were dried over MgS04, filtered, and the solvents were evaporated under reduced pressiure. A mixture of this crude product and K2C03 (0.2 g) in THF (30 ml), MeOH (10 ml), and H2O (10 ml) was stirred at rt for 3 h. Aq. sat. NRjCl was added and this mixture was extracted with Et20 (3x). The combined org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. This yielded the title compound (1.85 g, 95%) that was used withour further purification.
{rac.)-{lR*, 55*)-7-{4-[2-(tert-8utyldiphenylsUanyloxy)ethyl]phenyI}-3,9-
diazabicyclo (33.1] non-6-ene-3,6,9-trlcarboxylie acid Z-tert-hnty\ ester 9-(2,2^-trichloro-l,l-dimethyIethyl) ester (T5)
As for compound T4, but fi:om bicyclononene AZ2 (crude, about 5.79 mmol), imidazol (1.2 g, 17.6 mmol) and TBDPS-Cl (4.84 g, 17.6 mmol) in DMF (50 mL), then K2CO3 (0.5 g), THF (60 mL), MeOH (20 mL), and H2O (20 mL). The crude
title compoimd (9.6 g, quantitative yield) was used further without purification. LC-MS:R,- 1.26.
Compounds of type U
{rac.y{lR*, 5S*)-3-Acetyl-7-(4-Uydroxypheayl)-6-(methyIp hen et hylcarba-raoyl)-3,9-diazabicycIo[3.3.1]non-6-ene-9-carboxyUc acid 2,2,2-trichloro-1,1-dimethylethyl ester (Ul)
To a sol. of bicyclononene Wl ( 0.93 g, 1.37 mmol) in CH2CI2 (10 niL) was added HCl/dioxane (10 mL) at 0 °C. After 15 min, the ice bath was removed. The reaction mixture was stirred at rt for 1 h and the solvents were removed under reduced pressure. After drying at high vacuum for 30 min., the resulting solid or foam was dissolved in THF (10 mL). DfPEA (0.983 mL, 5.48 mmol) and DMAP (cat. amount) were added. The sol. was cooled to -78 °C and a sol. of AcCl (0.0973 niL, 1.37 mmol) in THF (5 mL) was slowly added over 2 min. After 75 min at -78 °C MeOH (10 mL) was added and the mixture was allowed to warm up. After dilution in EtOAc, the reaction mixture was washed with aq. IM HCl (Ix) and aq. sat. NaHCOa (Ix). The org. extracts were dried over MgS04, filtered, and evaporated under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:3 -> 1:1 -> 3:1 -^ EtOAc -> MeOH/EtOAc 1:19 -^ 1:9) yielded the title compound (253 mg, 30%). Rf = 0.30 (EtOAc). LC-MS: Rt = 5.12; ES+: 622.31.
{rac.y{lR% 55*)-3-Acetyl-7-[4-(2-hydroxyethyl)phenyl]-6-(methylph6nethyl-
carbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid 2,2,2-
trichloro-l,l-dimethyIethyl ester (U2)
To a sol. of bicyclononene W2 (3.46 g, 4.88 mmol) m CH2CI2 (35 mL) was added HCl (4M in dioxane, 35 mL) at 0 "C. After I h the ice bath was removed, and stirring continued for 1 h at rt. The solvents were removed under reduced pressure and the residue dried under higb vacuum. The resulting foam was

dissolved in THF (50 mL). DIPEA (3.34 mL, 19.5 mmol) and DMAP (cat. amount) were added. The reaction mixture was cooled to -78 °C and AcCl (0.347 mL, 4.88 mmol) in THF (20 mL) was added dropwise. After 2 h at -78 °C, AcCl (0,100 mL, 1.41 mmol) was added again, followed by a third portion of AcCl (0.050 mL, 0.71 mmol) 1.5 h later. MeOH (10 mL) was added after 30 min. and the mixture was allowed to warm up to rt. After dilution with EtOAc and washing with aq. IM HCl (Ix) and aq. sat. NaHCOj (Ix), the org. extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue b}^ FC (EtOAc/heptane 1:1-^ EtOAc -> MeOH/EtOAc 1:9) yielded the title compound as a colorless foam (2.06 g, 65%). Rf = 0.15 (EtOAc). LC-MS:Rt = 5.l4;ES+:650.21.
{rac.)-{lR*, 5,y*)-3-Acetyl-7-[4-(3-hydroxypropyl)phenyl]-6-(methylphen-ethyIcarfaamoyI)-3,9-diazabicyclo[33.11non-6-eDe-9-carboxyUc acid 2,1,1-trichloro-l,l-dimethylethyl ester (U3)
To a sol. of bicyclononene W3 (3.18 g, 4.40 mmol) in CH2CI2 (30 mL) was added HCl (4M in dioxane, 30 mL) at 0 °C. After 1 h at 0 °C and 1 h at rt, die solvents were removed imder reduced pressure and the residue dried under high vacuum. The residue was dissolved in THF (45 mL), and DIPEA (3.02 mL, 17.6 mmol) and DMAP (cat amount) were added. The sol. was cooled to -78 °C and a sol. of AcCI (0.313 mL, 4.40 mmol) in THF (15 mL) was added dropwise over 5 min. After L25 h, AcCl (0.070 mL, 0.984 mmol) was added again. After 30 min. MeOH (10 mL) was added and the mixture was allowed to warm up to rt After dilution in EtOAc and washing with aq. IM HCl (Ix) and aq. sat. NaHCOs (Ix), the org. extracts were dried over MgSO^ and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:1 —>■ EtOAc -^ MeOH/EtOAc 1:9) yielded the tide compound (2.92 g, 66%) as a foam. Rf = 0.23 (EtOAc). LC-MS: Rt - 5.24; ES+: 664.29.

(raa)-(JR^ 5^*)-3-Acef>'I-7-[4-(2-hydroxyethoxy)phenyl]-6-(niethyl-
phenethylcarbanioyI)-3,9-diazabicyclo[3.3.1jnoD-6-ene-9-carbox>iic acid
2,2,2-trichIoro-l,l-dimethylethyl ester ftJ4)
A mixture of bicyclononene T3 (1.88 g, 3.42 nimol), methylphenethylamine (1.49 niL, 10.3 mmol), DMAP (41 mg, 0.34 mmol), DIPEA (2.33 mL, 18.0 nimol),
HOBt (46 mg, 0.34 mmo\) and EDC-HCS (1.64 g, 8.55 nimol) in CHClj (40 mL) was stirred overnight at rt. The mixture was diluted in CH2CI2 and washed with aq. IM HCl (2x) and aq. sat. NaHCOs. The organic extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/ heptane 1:4 -> 1:1 -^ 4:1 -> EtOAc) yielded the tide compound (1.33 g, 58%). LC MS: R, = 5.25; ES+; 666.08.
Compounds of type V
irac.yilR*, 55*)-7-(4-Hydroxyphenyl)-3,9-diflzabicycIo[3.3.1]ijon-6-ene-3,6,9-tricarboxylic acid 3-teri-butyl ester 9-(2,2,2~trichIoro-l,l-dimethyiethyI) ester (VI)
To a sol. of bicyclononene HI (4.18 g, 5.79 mmol) in EtOH (55 mL) aq. NaOH (IM, 55 mL, 55 ramol) Vi^as added. The mixture was stirred at 80 °C for 28 h before it was allowed to cool to rt and acidified to pH 1 with aq. IM HCl. After extraction with EtOAc (3x) the combined org. extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (MeOH/CHjCli 1:49 -^ 3:97 -> 1:24 ^ 1:19 -> 1:9 -^ 1:4) yielded the title compound (1.50 g, 40%). Rf = 0.29. LC-MS: Rt = 4.91; ES-: 561.12.
irac.)-(lR*, 55*^)-7-[4-(2-Hydroxyettiyl)phenyi]-3,9-diazabicycIo[3.3.1]non-6-ene-3,6,9-tricar boxy lie acid 3-/e/-/-butyl ester 9-(2,2,2-trichloro-l,l-dimefbyl-ethyl) ester {V2)

To a sol. of bicyclononene H2 (13.75 g, 18.7 mmol) in EtOH (180 mL) aq. NaOH (IM, ISO mL, 180 mmol) was added. The mixture was stirred at 80 "C for 8 h and then left at -5 °C overnight. The mixture was acidified to pH 1 with aq. IM HCl and extracted with EtOAc (3x). The org. extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (MeOii/CHaCb 1:49 -^ 3:47 -^ 1:24 -^ 1:19 -> 1:9 ^ 1:4) yielded the title compound, contaminated with {rac.)-(lR*, 5S*)'7-[4-(2-hydroxyethyl)phenyl]-3,9-diazabicyclo[3.3.1]non-7-ene-3,6,9-tricarboxylic acid 3-/er^butyl ester 9-(2,2,2-trichioTO-l,l-dimethylethyl) ester (7.09 g, 64%). Rf =0.40 MeOH/CH2Cl2 1:9). R, = 4.90; ES-: 589.16.
(roc.)-(JJt*, 5S*)-7-[4-(3-Hydroxypropyl)phenyll-3,9-diazabicyclol3.3.1]non-6-ene-3,6,9-tricarboxylic acid 3-tert-butyl ester 9-(2,2,2-trichIoro-l,l-dimethylethyl) ester (V3)
To a soL of bicyclononene H3 (13.50 g, 18.0 mmol) in EtOH (180 mL) aq. NaOH (IM, 180 mL, 180 mmol) was added. The mixture was heated to 40 °C and after 1 h to 80 °C. After 7 h, the mixture was left overnight at -5 °C. EtOH (100 mL) and aq. NaOH (IM, 50 mL, 50 mmol) were added and the sol. was heated to 80 "C for 6 h. After cooling to rt and adjustment of the pH to 1 with aq. IM HCl, the mixture was extracted with EtOAc (3x). The combined org. extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (MeOH/CHjCh 1:49 -> 3: 97 -> 1:24 -^ 1:19 -> 1:9 -^ 1:4) yielded flie title compound (4.80 g, 55%). Rf = 0.50 (MeOWCRjCh 1:9). Le-MS:Rt = 4.99; ES-: 603.20.
Compounds of type W
(rac.)-(lR*, 55*)-7-(4-HydroxyphenyI)-6-(methylphenethyIcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylic acid 3-tert~butyl ester 9-(2,2,2-trichIoro-l,l-dimethylethyl) ester (Wl)

To a susp. of bicyclononene VT (1.50 g, 2.66 mmol) in CHCI3 (30 mL) was added methylphenethylainijic (0.774 mL, 5.32 mmol). DMAP (32.5 mg, 0.266 mmol),
HOBt (36 mg, 0.266 mmol), and EDCTICI (765 mg, 3.99 mmol) were added successively. Airier 3 days at rt the mixture was diluted in CHjCU and washed with aq. IM HCI (Ix) and aq. sai. NaHCO^ (Ix). The org. extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane ]:9 -> 1:4 -> 3:7 -> 2:3 -> 1:1 -> 3:2 -> 7:3) yielded the title compound as a colorless solid (0.93 g, 51%). Rf = 0.25 (EtOAcAieptane 1:1). LC-MS: Ri - 5.86; ES-: 678.14.
{rac.)-{lR*, J5-)-7-[4-(2-Hydroxyethyl)plienyI]-6-(mefhyIphcnethylcarbamo-yl)-3,9-diazabicyclo|3.3.1]non-6-ene-3,9-dicarboxylic acid 3-/ert-butyI ester 9-(2,2,2-trichIoro-l,l-diraethylethyl) ester (W2)
To a sol. of bicyclononene V2 (7.09 g, 11.97 mmol) in CHCI3 (UO mL) were added A^-methylphenethylamine (3.48 mL, 24.0 mmol), DMAP (137 mg, 1.12
mmol), HOBt (151 mg, 1.12 mmol) and EDC-HCI (3.44 g, 18.0 mmol). The mixture was stirred at rt for 3 days, before it was diluted with CH2CI2 and washed witii aq. IM HCI (Ix) and aq. sat. NaHCOj (Ix). The org. extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue purified by FC (MeOH/CHzClz 1:49 -)■ 3:122 -^ 4:121 ->■ 1:24 -> 1:9 -^ 1:4) yielded the title compound (3.46 g, 41%). Rf = 0.26 (MeOH/CHzCIi 1:19). LC-MS; Rt = 5.87; ES+: 708.40.
{racy-ilR*, 55*)-7-J4-(3-Hydroxypropyi)phenyi]-6-(methyVphenethylcarba-inoyI)-3,9-diazabicyclo[3.3.1]aon-6-eBe-3,9-dicarboxyiic acid 'i-tert-hntyl ester 9-(2,2,2-trichIoro-l,l-dimefhylethyI) ester (W3)
To a sol. of bicyclononene V3 (7.59 g, 12.5 mmol) in CHCh (150 mL) were added methylphenethylamine (3.63 mL, 25.0 mmol), DMAP (153 mg, L25
mmol), HOBt (169 mg, 1.25 mmol) and EDC-HCI (3.80 g, 19.2 mmol). The mixture was stirred at rt for 3 days before it was diluted in CH2Ci2 and washed

with aq. IM HCl (Ix) and aq. sat. >^aHC03 (Ix). The org. extracts were dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (MeOH/CH2Cl2 1:49 ^ 3:97 ^ 1:24 ^ 1:9 ^ 1:4) yielded the title compound (3.18 g, 35%). Rf = 0.42 (MeOH/CHiCl; 1:19). LC-MS: Ri = 5.99; ES+: 744.50.
(rac.)-(lR*, 55*)-3-Acet\l-6-hydroxyiuethyl-7-{4-[3-(2-methoxybenzyloxy)-propoxylpheuyl}-3,9-diaiabicycIo(3.3.11noQ-6-eQe-9-carboxylic acid 2,2,2-trichloro-l,I-dimethylethyI ester (X)
To a sol. of bicyclononene SI (2.29 g, 3.21 mmol) in CHaCla (100 mL) was added BF3 EtiO (0.460 mL, 3.66 mmol) at -78 °C. The mixture was stirred at -78 °C for 30 rain and DIBAL (IM in toluene, 6.42 mL, 6.42 mmol) was added. After 75 min, ice was added and the mixture was allowed to warm up to rt. CH2CI2 was added and the mixture was washed with aq. IM HCl (Ix). The org. extracts were separated, dried over MgS04 and filtered. The solvents were removed under reduced pressure. Purification of the residue by FC (EtO Ac/heptane 1:2 —> 1:1 --> EtOAc) yielded the title compound (1.01 g, 47%).
(rac)'(IR*, 55*)-3-Acetyl-6-formyi-7-{4-[3-(2-methoxybeiizyloa;y)propoxy]-phenyl}-3,9-diazabicycIo[3^.1]non-6-ene-9-carbo3CyUc acid 2,2^-trichloro-1,1-dimethyIethyI ester (Y)
To a sol. of bicyclononene X (258 mg, 0.385 mmol) in CH2CI2 (5 mL) was added to 0 °C Dess-Martin periodane (170 mg, 0.401 mmol) at 0 "C. After 45 min. at 0 °C a second portion periodane was added. The sol. w^ stirred for 15 min before the solvents were removed under reduced pressure. Direct purification of the
residue by FC (EtOAc/heptane 2:3 -> 1:1 -^ 3:2 -^ 7:3) yielded the title compound (188 mg, 73%). Rf = 0.49 (EtOAc). LC-MS: R, = 6.18; ES+: 667.21.

(rac.)-(lR*, 55*)-3-Ace(yl-7-{4-[3-(2-mefhoxybenzyloxy)propox7]phenyl}-6-methylaminomethyl-3,9-diazabicyclo[3.3.1]Don-6-ene-9-carboxyUc acid 2,2,2-trichIoro-l,l-diraethylethyl ester (Z)
To a sol. of bicyclononene Y (334 mg, 0.50 mmol) in MeOH (10 ml.) methylamine (40S-o in'water, 0.215 mL, 2.5 mmol) was added. The raixiwe was stirred at rt for 1 h and then cooled to 0 °C. NaBRj (20 mg, 0.50 mniol) was added. The mixture was stirred at rt for 4 h before K2CO3 (263 mg) was added. After evaporation under reduced pressure the residue was distributed between EtOAc and water. The org. extracts were separated, dried over MgS04, and filtered. The sol^'ents were removed under reduced pressure. Purification of the residue by RP18-MPLC yielded the title compound (130 mg, 38%). LC-MS: Ri = 1.00; ES+: 682.14.
{rac.)-{lR*, 55*)-7-{4-[3-(2-ChIorophenoxy)propylIph£nyl}-3,9-diazabicyclo-[3.3.11non-6-ene-3,6,9-fricarboxylic acid i-teit-hntyX ester 9-(2^^-trichloro-1,1-dimethylethyl) ester (AA)
Bicyclononene H6 (1.71 g, 2.3 mmol) was dissolved in EtOH (50 mL). Aq. IM NaOH (50 mL) was added and the mixture was heated to 80 °C. The sol. was stirred for 5 h at 80 °C, then allowed to cool down to rt. After acidification to pH = 1-2 with aq. IM HCl the mixture was extracted with EtOAc (3x). The combined org. extracts were dried over MgS04, filtered and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 2:3 -> 1:2 ->■ 1:1) yielded the title compound (504 mg, 31 %). Rf = 0.30 (EtOAc/heptane 1:1). LC-MS: R, = 6.21; ES-: 712.34.
{rac.)-{lR% 55*)-7-{4-I3-(2-Chlorophenoxy)propyl]plienyl}-6-{I2-(2-chloro-phenyI)ethyI]methyIcarbamoyI}-3,9-diazabicycIo [3.3.1 ]non-6-ene-3,9-dicarboxylic acid 3-fer/-butyl ester 9-(2,2,2-trichIoro-l,l-dimethylethyl) ester (AB)

Bicyclononene AA (504 mg, 0.703 mmol) was dissolved in CHCb (25 mL). [2-(2-chlorophenyl)ethyl]meth;1amine (Jaques B.; Wallace R. G., Tetrahedron, 1977, 33, 581; 238 mg. 1.40 mmol), DIPEA (0.240 mL, 1.40 nrniol), DMAP (17
mg, 0.14 nnnol), HOBt (19 mg, 0.10 mmol) and EDC-HCI (135 mg, 1.40 mmol) were added. The sol. was stirred at rt overnight, The mixture was diluted with CH2CI2 and washed with water (Ix). The org. extracts were dried over MgS04 and the solvents were removed under reduced pressure. Purification of the residue by filtration through sihca gel yielded the title compound as a yellowish foam (336 mg, 55%).
(rac,)-(/fi% 5S*)-7-|4-l3-(2-ChIorophenoxy)propyI]phenyl}-6-{[2-(2-ch\oro-phenyI)ethyI]methylcarbamoyI}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbo-xylic acid 2^,2-trichloro-l,l-dimethyIethyl ester hydrochloride salt (AC)
Bicyclononene AB (336 mg, 0.378 mmol) was dissolved in CH2CI2 (3 mL). 4M HCl/dioxane (13 mL) was added and the mixture was stirred at rt for 2 h. The solvents were removed under reduced pressure. Drying the residue at high vacuum yielded the title compound as a colorless foam that was used without further purification. LC-MS: R, = 5.26; ES+: 765.85.
9-Methyi-7-oKO-3,9-dia2abicyclo[3.3.1]nonane-3-carboxylic acid tert-butyl ester (AE)
(4-Ben2yl-6-ethoxycarbonyImethyI-l-methylpiperazin-2-yl)acetic acid ethyl ester (Patent WO 92/05174) (71.0 g, 0.196 mol) was dissolved in MeOH (400 mL), TFA (77.8 mL, 1.02 mol) was added and the flask was purged with nitrogen. Pd/C (10%, 50% moisture, 3.6 g) was added. The flask was closed and purged with hydrogen (3x). After 1 day, the mixture was filtered through celite and washed with MeOH. The solvent was removed under reduced pressure and the foamy residue (92.7 g) was dried under iugh vacuimi. A sol. of tBuOK (117.2 g, 1.04 mol) in toluene (3.07 L) was heated to reflux. A sol. of the cmde plperazine formerly obtained, dissolved in THF (300 mL), was added dropwdse over 50 min.

The black mixture was stirred for 10 further min. and allowed to cool to rt. The mixture was cooled to 0 "C and AcOH (36.6 niL, 0.635 mol) was added. The solvents were removed under reduced pressure and the residue purified by FC (MeOH/CH2Cl2 1:9 ~> 1:4 -> 1:3). The fractions with an Rrvalue close to 0.10 (MeOVUCihCh 1:9) ■were collected and the solvent removed under reduced pressure. The residue was dissolved in aq. 5M HCI (2 L) and the reaction mixture heated to reflux overnight. The mixture was allowed to cool to rt, then cooled to 0 °C with an ice bath. The pH was brought to 12 by adding carefully solid KOH. This mixture was extracted with CH^CIi (3x). The combined org. extracts were dried over MgS04 and the solvents were removed under reduced pressure. The residue was suspended m CHsCb (400 ml.,) and cooled to 0 °C. DIPEA (19.1 mL, 112raraol) was added. A sol. of BociO (24.3 g, 113 mmol) in CH2CI2 (200 mL) was added dropwise. The mixture was stirred for 1 h at 0 "C, tlien 1 h at rt. The mixture was washed with aq. 10% Na2C03 (2x). The org. extracts were dried over MgS04, filtered and the solvents were evaporated under reduced pressure. The residue was purified by FC (EtOAc/heptane 1:1 -> EtOAc), The title compound was obtained as a solid that could be recrystallized from heptane (15.6 g,30%). Rf=0.45(MeOPl/CH2Cl2l:9). LC-MS: Rt= 1.55; ES+: 254.16.
(IR, 55)-9-MethyI-7-oxo-3,9-diazabicyclo[3.3.1]nonaDe-3,6-dicarboxylic acid 3-tert-buiyl ester 6-methyl ester (AF)
To a susp. of (-)-bis[(S)-l-plienylethyl]amine Tiydrochloride (226 mg, 0.864 mmol) in THF (3 mL) at 0 °C was added dropwise n-BuLi (1.6M in hexane, 1.136 mL, 1.S08 mmol). The mixture was stirred for 1 h at 0 °C, then cooled to -78 °C. A sol. of bicyclononane AE (200 mg, 0.786 mmol) in THF (2 mL) was added dropwise over 3 min. The reaction mixture was stirred for 3 h at -78 °C, then methylcyanoformat (0.081 mL, 1.02 mmol) was added. The reaction mixture was stirred for 30 mm. at -78 °C and a sol. of AgNOs (191 mg, 1.124 mmol) in H2O/THF (1:1, 2 mL) was added. After 10 min., H2O (1.5 mL) and AcOH (1.5 mL) were added and the reaction mixture was allowed to warm to rt. Ammoniac (25% in water) was added until the Ag-salt had completely dissolved. The

reaction mixture was extracted wdth EtOAc (Ix) and CH2CI2 (2x). The combined org. e?rtracts were dried over MgS04 and the solvents were removed under reduced pressure. Purification of the residue by FC (MeOH/CH2Cl2 1:14) yielded the title compound (167 mg, 68%). Rf =^ 0.37 (MeOH/CH2Cl2 1:9). LC-MS: Rt = 0.76; ES+: 313.10. ee = S2%.
(IR, 55)-9"Methyl-7-oxo-3,9-dia2abicyclo[3.3.1!nonane-3,6-dicarboxylic acid 6-benzyl ester 3-ter(-butyl ester (AG)
To a susp. of (-)-bis[(S)-l-plienylethyl]amine hydrochloride (226 mg, 0.864 mmol) inTHF (3 rtiL) atO "C was added dropvase «-BuLi(1.6Minhexane, 1.136 mL, 1.808 mmol). The mixture was stirred for 1 h at 0 °C, then cooled to -78 °C. A sol. of bicyclononane AE (200 mg, 0.786 mmol) in THF (2 mL) was added dropwise over 3 min. The reaction mixture was sdrred for 3 h at -78 °C, then methylcyanoformat (0.081 mL, 1.02 mmol) was added. The reaction mixture was stirred for 30 min. at -78 °C and a sol. of AgNOa (191 mg, 1.124 mmol) m H2O/THF (1:1, 2 mL) was added. After 10 min., H2O (1.5 mL) and AcOH (1.5 mL) were added and the reaction mixture was allowed to warm to rt. Ammoniac (25% in water) was added until the Ag-salt had completely dissolved. The reaction mixture was extracted with EtOAc (Ix) and CH2CI2 (2x). The combined org. extracts were dried over MgS04 and the solvents were removed under reduced pressure. Purification of the residue by FC (MeOH/CH2Cl2 1:14) yielded the title compound (150 mg, 49%). Rf = 0.50 (MeOH/CH2Cl2 1:9). LC-MS: Ri = 0.87; ES+: 389.09. 66 = 84%.
irac.)-{JR*, 55*)-3-Acetyl-7-{4-I2-(2-bromo-5-fluorophenoxy)ethyl]phenyI}-3,9-diazabicycIo[3J.l]non-6-ene-6,9-dicarboxylic add 6-cthyl ester 9-(2,2,2-trichloro-l,l-dimcthyIethyI) ester (AH)
A sol. of bicyclononene S3 (900 mg, 1.60 nmiol) in toluene (15 mL) was purged with N2 (4x). 2-Broino-5-fluorophenol (0.267 mL, 2.4 mmol), TMAD (344 mg, 2.00 mmol) and tributylphosphine (1.18 mL, 4.80 mmol) were added and the

reaction mixture was lieated to reflux for 1 h. The mixture was allowed to coo! to rt, and the sol%'ems were removed under reduced pressure. Purification of the residue by FC (ElOAc/heptane 1:24 -> 1:9 ^ 2:3 -^ 7:3) yielded tlie title compound (1.06 g, 90%). Rf- 0.58 (ElOAc). LC-MS: Rt= 6.52; ES+: 733.00.
Compounds of type AJ
(rac.)-(lR*, 56'*)-3-Acet>'I-7-{4-I2-(2-bromo-5-iluorophenoxy)ethyI]phenyI}-3,9-diazabicyclo(3.3.3|non-6-ene-6,9-dicarboxyIic acid 9-(2,2,2-trichloro-l,l-dimethylelhyl) ester (AJl)
A mixture of bicyclononene AH (1.06 g, 1.44 nimol) in EtOH (30 mL) and aq. IM NaOH (30 mL) was stined efficiently at 80 °C for 2.5 h. The mixture was allowed to cool to rt, acidified with aq. IM HCl, and extracted with EtOAc (3x). The combined org. phases were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane i:l -> 3:1 -^ EtOAc -^ MeOH/EtOAc 1:19 ^ 1:9) yielded the title compound (845 mg, 83%). Rf = 0.10 (EtOAc). LC-MS: Rt = 5.78; ES-: 702.81.
(rac.)-(iiZ*, 55*)-3-Acetyl-7-{4-[3-(2^,6-trifluorophenoxy)propylIphenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylic acid 9-(2,2,2-trithIoro-l,l~ dimethylethyl) ester (AJ2)
A soi. of bicyclononene ARl (296 mg, 0.39 ramol) in MeOH (10 mL) at 0 °C was purged with N2 (3x). Pd/C (10%, cat. amount) was added and the mixture was purged with H? (4x). The mixture was stirred under Hz for 2 h at 0 °C, and was filtered through Celite. The solvents were removed under reduced pressure and the residue was dried under high vacuum (200 mg, 80%). It was used without fiirther purification. LC~MS; Rt = 5.83.

(rac.)-(-?^%5^*)-3-Acetyl-7-{4-[3-(3-fluorophenoxy)propyl]phenyI}-3,9-diaza-bicyclo[3.3.1]non-6-cne-6,9-dicarboxylic acid 9-(2,2,2-trichloro-l,l-d'niethyl-ethyl) ester (AJ3)
As for compound AJ2, but from AR2 (205 mg, 0.25 mmoi), Pd/C (cat. amount) and MeOH (IQ mL). The crude material (100 mg, 56%) was used without further purification. LC-MS; R,= 5.81.
(rac.)-(IR*, 55*)-3-AcetyI-7-{4-[3-(2-bromo-5-fluoropfaenoxy)propyI]phenyl}-3,9-diazabicyclo[3,3.1]non-6-ene-6,9-dicarboxylic acid 9-(2,2,2-trichIoro-l,l-dimethylethyl) ester (AJ4)
As for compoxmd AJl, but &om bicyclononene BL (1.55 g, 2.07 mmol), EtOH (55 mL) and aq. IM NaOH (55 mL). Purification of the residue by FC (EtOAc/heptane 1:1 -> EtOAc -^ MeOH/EtOAc 1:9) yielded the title compound (1.17g,78%). Rf=0.20(EtOAc). Rt = 6.02; ES+: 721.12.
Compounds of type AK
{rac.)-(lR% 55*0-7-{4-[2-(2-Bromo-5-fluorophenoxy)ethyl]phenyl}-6-(methyl-phenethylcarbainayI)-3,9-diazabicyclo[33.1Jnon-6-ene-3,9-dicarboxylic acid 3-tert-butyl ester 9-(2^^-trichloro-l,l-dimethyIethyl) ester (AKl)
A sol, of bicyclononene W2 (1.68 g, 2.37 mmol) in toluene (50 mL) was purged with N2 (4x). 2-Bromo-5-fluorophenol (0,403 mL, 3.56 mmol), azodicarboxylic dipiperidide (897 mg, 3.56 mmol) and tributyl phosphine (1.62 mL, 7.12 mmol) were added. The mixture was heated to reflux for 2 h. The mixture was then allowed to cool to rt and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:19 -* 1:9 ^ 1:4 -> 1:1 -> 3:1) yielded the title compound (1.88 g, 90%). Rf = 0.80 (EtOAc). LC-MS: R, = 7.30.

{racyilR*, 55*)-6-l(2-ClilorobeuzyI)cyclopropyIcarbamoylj-7-{4-[3-(2,3,6-tri-fluorophenoxy)propyljpheuyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarbo-xylic acid 3-terl~hutyl ester 9-(2,2,2-trit:hIoro-l,l-diinetiiyIethyl) ester
(AK2)
A mixture of bicyclononcne AYl (12.15 g, 16 mniol), (2-chloroben2yl)-cyclopropylamine (9.0S g, 50 mmol), DIPEA (10.9 niL, 64 mmol), DMAP (488 mg, 4 nimol), HOBt (2.43 g, 18 mmol) and EDC-HCl (4.60 g, 24 mmol) in CH2C12 (250 mL) was stirred overnight, The mixture was diluted with CH2CI2, and washed with aq. IM PiCl (3x) and witli aq. sat. NaHCOj (Ix). The org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:5-> 1:3-> 1:2) yielded the title compound (9.10 g, 63%). LC-MS: Rt = 7.68.
(rac.)-(IR*, 55*)-6-(BenzylcyclopropylcarbaraoyI)-7-{4-[3-(2,3,6-trifluoro-phcnoxy)propyI]phcnyI}-3,9-diazabicyclo[3.3,l]non-6-ene-3,9-dicarboxyIic acid 3-to/-bufyl ester 9-(2,2,2-trichloro-l,l-dimetiiyIethyI) ester (AK3)
As for bicyclononene AK2, but fi'om bicyclononcne AYl (552 mg, 0.75 mmol), benzylcyclopropylamine (Loeppky, R. N.; et a!., J. Org. Chem., 2000, 65, 96; 221 mg, 1.50 mmol), DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol),
HOBt (101 mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol) in CHzClz (7 mL). Purification by FC yielded the title compound (570 mg, 88%). LC-MS: Rt -1.28.
(i-ac.y(lR*, 55*)-6-[(2-chIorobenzyl)ethylcarbamoyIl-7-{4-(3-(23,6-trifIuoro-phenoxy)propyll pheny I}-3,9-diazabicy do (3,3.1 lnon-6-ene-3,9-dicarboxy lie acid 3-te/-/-butyI ester 9-(2,2^-trichloro-l,l-dimethylethyl) ester (AK4)
As for bicyclononene AK2, but firom bicyclononene AYl (552 n^, 0,75 mmol), (2-chlQrobenzyl)ethylamine (Ishihara, Y; et al; Chem. Pharm. Bull., 1991, 39, 3225; 255 mg, 1.50 mraoL), DIPEA (Q.515 mL, 3.00 mmol), DMAP (23 mg, 0.19

mmol), HOBt (101 mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol) in CEiCh (7 mL). Purification by FC yielded the title compound (543 mg, 82%). LC-MS:R,-1.29.
(rac.)-(lR*, 55*)-6-[Cyelopropyl-(2-fluorobenzyI)carbamoylI-7-{4-[3-(2,3,6-trifluorophenoxy)p ropy 1] ph enyl} -3,9-diazabicy clo[3.3.1 ] non-6-ene-3,9-diearboxylic acid 3-iert-hu1y\ ester 9-(2,2,2-tricliloro-l,l-di methyl ethyl) ester (AK5)
As for bicyclononene AK2, but from bicyclononene AYl (552 mg, 0.75 mmol), cycbpropyl-(2-fluorobenzyl)amine (248 mg, 1.50 mmol), DIPEA (0.515 mL, 3-00
mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol) in CH2CI2 (7 mL). Purification by FC yielded the title compound (526 mg, 79%). LC-MS; Rt = 1.28.
{rac.)-{lR*, 5iS*)-€-ICyclopropyV-(3-tTifluoromethylbenzyi)tarbamoyl]-7-{4-[3-{23,6-trifluorophenoxy)propylIphenyl}-3,9-dia2ahicy do [3.3.1] non~6-ene-3,9-dicarbosylic acid 3-J'^n'-butyl ester 9-(2,2^-trichIoro-l,l-dimethyletliyl) ester (AK6)
As for bicyclononene AK2, but from bicyclononene AYl (552 mg, 0.75 mmol), cycIopropyl-(3-trifluoromethyl-benzyl)amine (Brabander, H. J.; et al; J. Org. Chem., 1967, 32, 4053; 323 mg, 1.50 mmol), DIPEA (0.51S mL, 3.00 mmol),
DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol) in CH2C12 (7 mL). Purification by FC yielded the title compound
(551mg,79%). LC-MS: Rt= 1.25.
{rac.)-(lR*, 5,S*)-6-[CyclopropyI-(2-methylbenzyl)carbamoyll-7-{4-[3-(2 ^,6-trifluorophenoxy)propyIJphenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylic acid 3-/^r/-butyl ester 9-(2^,2-trichloro-l,l-diiMethylethyl) ester
(AK7)

As for bicyciononene AK2, but from bicyclononene AYl (552 mg, 0.75 mmol), cyclopropyl-(2-mcthylbenzyl)-aminc (242 mg, 1.50 mraolj, DIPEA (0.515 mL, 3.00 mmol), DMA? (23 mg, 0.19 iiunol), HOBt (101 mg, 0.75 mmol) and
EDC-HCl (216 mg, 1.12 mmol) in CHzClo (7 mL). Purification by FC yielded the title compound (553 mg, 84%). LC-MS: R, = 1.29.
{rac.)-{IIi*, 55*)-6-{Cyc!opropyl-[2-(4-methoxyphcooxy)cthyI]carbamoy!}-7-{4-[3-(235^-trifluorophenoxy)propyllplienyl)-3,9-diazabicyclo(3.3.1}noB-6-ene-3,9-dicarboxyiic acid 3~tert-but\l ester 9-(2,2,2-trichloro-I,l-dimcthyl-ethyl) ester (AK8)
As for bicyclononene AK2, but from bicyclononene AYl (552 mg, 0,75 mmol), cyclopropyl-[2-(4-m6thoxy-phenoxy)ethyl]amine (311 mg, L50 mmol), DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 rag, 0.75 mmol)
andEDC-HCi(216mg, l.]2mmol) in CH2CI2 (7mL). Purification by FC yielded the title compound (566 mg, 82%), LC-MS: Rt- 1.28.
(rac.)~(JJi*, Ji**)-6-(Cyclopropyl-[2-(2-mcthoxyphenoxy)ethyl]carbamoyI}-7-{4-[3-(2,3,6-trifiu orophenoxy)propyl] phenyl}-3,9-diazabicyclo[3J'.l)non-6-ene-3,9-dicarboxyIic acid 3-/ert-butyl ester 9-(2,2,2-trichloro-l,l-dimethyl-ethyl) ester (AK9)
As for bicyclononene AK2, but ftom bicyclononene AYl (552 mg, 0.75 mmol), cyclopropyl-[2-(2-methoxy-phenoxy)ethyl]amine (311 mg, 1.50 mmol), DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol) inCH2Cl2(7mL). Purification by FC yielded the title corapound(570 mg, 82%). LC-MS; R;- 1.28.
(rac.)'ilJi*, 55*)-6-ICycIopropyK2-/«-tolyloxyethyI)carbamoyII-7-{4-[3-
(23,6-triflu ore ph en oxy)propyl]pheny l}-3,9-diazabicyclo [3.3.1] non-6-ene-3,9-dicarboxylic acid 3-tert-butyl ester 9-(2,2,2-trichloro-l,l-dimethyIethyI) ester (AKIO)

As for bicyclononene AK2, but horn bicyclononene AYl (552 mg, 0.75 mmol), cyclopropyl-(2-H;-tolyloxy-ethyl)amine (287 mg, 1.50 mmol), DIPEA (0.515 mL, 3,00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) and
EDC-HCl (216 mg, 1,12 mmol) inCHsCh (7 mL). Purification by FC yielded the title compound (506 mg. 74%). LC-MS: R,= 1.30.
{rac.)-(JJi*, 55*)-6-{Cjclopropyl-[2-(3,4-dimethylphenoxy)ctliyl]carbarnoyl}-7-{4-[3-(2,3,6-trinuorophenoxy)propyllphenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxy\ic acid 3-/ert-butyl ester 9-(2,2,2-trichl6ro-l,1-dimethyl-ethyl) ester (AKll)
As for bicyclononene AK2, but fi-om bicyclononene AYl (552 mg, 0.75 mmol), cyclopropyl-[2-(3,4-diraethyl-phenoxy)ethyl]amine (462 mg, 1.50 mmol), DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol)
and EDC-HCl (216 mg, 1.12 mmol) in CH2a2 (7 mL). Purification by FC yielded the title compound (693 mg, 100%). LC-MS:Ri= 1.28.
(mc)-(iii*, 5S*)-6-(Cyclopropylphenethylcarbamoyl)-7~{4-l3-(23,6-trifluoro-phenoxy)propyI]phenyl}-33-diazabicyclol33.1]non-6-eDe-3,9-dicarboxyIic acid 3-tert-butyI ester 9-(2^^-trichIoro-l,l-dimethylethyI) ester (AK12)
As for bicyclononene AK2, but from bicyclononene AYl (552 mg, 0.75 mmol), cyclopropylphenethylamine (Smith, P. W.; et al; J. Med Chem., 1998, 4J, 787; 242 mg, 1.50 mmol), DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19
mmol), HOBt (101 mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol) ia CH2CI2 (7 mL). Purification by FC yielded the title compound (510 mg, 77%). LC-MS: R, = 1.28.
(rac.)-(JR% 55*)-6-{[2-(2-Chlorophenyl)ethyl]cyclopropyIcarbamoyl}-7-{4-[3-(2^,6-trifluorophenoxy)propyl]phenyI}-3,9-diazabicycIo[3.3.1]non-6-ene-3,9-

dicarboxylic acid 3-teii-huty\ esfer 9-(2,2,2-trichIoro-l,I-[liinethylcthyl) ester
(AK13)
As for bicyclononene AK2, but from bicyclononene AYl (552 mg, 0,75 mniol), [2-(2-ch]orop]ienyl)ethyl]-cycIopropylamine (294 mg, 1.50 mmoi), DiPKA (0,515 niL, 3.00 mmol). DMAP (23 mg, 0,19 mmol), HOBt (101 mg, 0.75 mmol) and
EDC-HCl (216 mg, 1.12 mmol) in CH2CI2 (7 mL), Purification by FC yielded the title compoimd (540 mg, 79%). LC-MS: R, = 1.2S.
{)ac.)-(lR'', 5;S'")-6-{Cyc!opropyl-[2-(2,3-difluoropbenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trinuorophenoxy)propyl]phciiyl}-3,9-diazabicyclo[3.3.1]iion-6-ene-3,9-dicarboxylic add 3-ieii-buiyl ester 9-(2,2,2-tricbloro-l,l-dimethylethyl) ester {AK34)
As for bicyclononene AK2, but from bicyclononene AYl (552 mg, 0.75 nrunol), cyclopropyl-[2-(2,3-difluoro-phenyl)ethylJamine (296 mg, 1.50 mmol), DIPEA (0.515 niL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol) in CH2CI2 (7 mL). Purification by FC yielded the title compound (572 mg, 83%), LC-MS: R,= 1.28.
(rac,y(JR*, 55'*)-6-{CycIopropyl-[2-(4-fluoropheiiyl)ethyIJ carbamoyl}-?-{4-[3-(2^,6-trifluorophenoxy)propyI]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylic acid 3-tert-buty\ ester 9-(2,2,2-trichloro-l,l-dimethy!ethyl)
ester (AK15)
As for bicyclononene AK2, but from bicyclononene AVI (552 mg, 0.75 mmol), cyclopropyi-[2-(4-fluoro-phenyl)ethy!]amine (269 mg, 1.50 mmol), DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) and
EDC-HCl (216 mg, 1.12 mmol) in CH2CI2 (7 raL). Purification by FC yielded the title compound (533 mg, 79%). LC-MS: R, = 1.28.

(racHlR*, 55*)-6-[CycIopropyl-(2-tf-toIyIethyl)carbamoyI]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]pbenyl)-3,9-diazabicyclo[3.3,l]non-6-enc-3,9-dicarboxyiic acid 3-tert-butyl ester 9-(2,2,2-trichIoro-l,l-dimethyietbyI) ester (AK16)
As for bicyciononene AK2, but from bicyclononene AYl (552 mg, 0.75 mmol), cyclopropyI-(2-o-toIylethyl)-amine (263 rag, 1.50 mmol), DIPEA (0.515 mL, 3.00
mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) and EDC-HCI (216 mg, 1.12 mmol) in CH2CI2 (7 ml). Purification by FC yielded the title compound (562 mg, 84%). LC-MS: R, = 1.29.
(rac.)-{lR*, 55*)-^{Cyclopropyl-(3,5-dimefhoxybenzyl)carbamoyl}-7-{4-[3-(2^,6-trifluorophcaoxy)propylIpheoyl}-3,9-diazabicyclo[3J.l]non-6-ene-3,9-dicarboxylic acid 3-/ej(-butyl ester 9-(2,2,2-trichloro-l,l-diniethylethyl) ester (AK17)
As for bicyclononene AK2, but from bicyclononene AYl (552 mg, 0.75 mmol), cycIopropyl-(3,5-dimethoxy-ben2yl)aniine (311 mg, 1.50 mmol), DIPEA (0.515 inL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) and
EDC-HCI (216 mg, 1.12 mmol) in CH2CI2 (7mL). Purification by FC yielded the title compound (530 mg, 76%). LC-MS; Rt = 1.28.
(rac)-(lR*> 55*)-6-lCyclopropyl-(2-p-toIylethyi)carbamoyIl-7-{4-[3-(23,6-trifluo rophenosy)propyI] phenyl}-3,9-diazabicy do [33.1 ] non-6-ene-3,9-dicarboxylic acid 3-/ert-butyl ester 9-(2,2,2-trichIoro-l,l-dimethylefhyl) ester (AK18)
As for bicyciononene AK2, but from bicyclononene AYl (552 mg, 0.75 mmol), cyclopropyl-(2-_p-tolyIethyl)-amine (263 mg, 1.50 mmol), DIPEA (0.515 mL, 3.00
mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) and EDC-HCI (216 mg, 1.12 mmol) in CH2C12 (7 mL). Purification by FC yielded the title compound (530 mg, 79%). LC-MS: Rt= 1.30.

(rac,)-{lR*, 55*)-6-{Cyclopropyl-[2-(2-hydroxyethyl)beiizyllcarbamoyl}-7-{4-[3-(2,3,6-trifluorDphenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3.1]non-^-ene-3,9-dicarboxyHc acid 3-ier^butyl ester 9-(2,2,2-tricfaloro-l,l-dimethylethyl) ester (AK19)
As for bicyclonoaene AK2, but fi-ora bicyclononene AYl (1.30, 1.77 mmol), (2-allyIbenzyl)cyclopropyl-amine (992 mg, 5.30 mmol), DIPEA (1.01 mL, 7.08
mmol), DMAP (54 mg, 0.44 mmol), HOBt (263 mg, 1.95 mmol) and EDC-HCl (509 mg, 2.66 mmol) in CH2CI2 (25 mL). Purification by FC yielded the intermediate compound (1.49 g, 93%). LC-MS: R^ = 7.81. Then as for compound AT, but from the foraier intermediate compound (1.49 g,
1.65 mmol), NMO-HjO (245 mg, 1.82 mmol), and OSO4 (2.5% in teri-BuOU, 0.207 mL, 0.017 mmol) m THF (4 mL), tert-BuOH (2 mL) and water (1 mL). Purification of the residue by FC (EtOAc/heptane 1:4 -> 2:3 -> 3:2 ^ 4:1 -^ EtOAc) yielded the 2"'^ intermediate compound (866 mg, 56%). Rf = 0.50 (EtOAc). LC-MS: R,= 6.95.
Then as for compound AU, but from the 2"' intermediate compound (866 mg, 0.922 mmol) and NaI04 (217 mg, 1.01 mmol) m THF (8 mL) and water (2 mL). Purification of the residue by FC (EtOAc/heptane 1:4 -> 2:3) yielded the 3"* intermediate compound (751 mg, 90%). Rf = 0.75 (EtOAc). Finally as for compound AV, but from the 3"* intermediate compound (751 mg, 0.828 mmol) and NaBH4 (35 mg, 0.9 mmol) in MeOH (10 mL). Purificatioa of the residue by FC (EtOAc/heptane 2:3) yielded the title compound (599 mg, 80%). LC-MS: Rt = 7.30.
(rac.)-(lR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyI)cycIopropyIcarbamoyl]-3,9-diazabicyclo [3.3.1 ]non-6-ene-3,9-dicarboxyiic acid 3-teit-butyl ester 9-(2,2,2-trichloro-l,l-dimethyIethyl) ester (AK20)

As for bicyclononene AK2, but from bicyclononene AY2 (7.68 g, 9.86 mmol), (2-chlorobenzyOcyclopropyiamine (5.37, 29.6 mmol), DIPEA (6.75 mL, 39.4 mmol),
DMAP (301 mg, 2.47 mmol), HOBt (1.46 mg, 10.8 mmol) and EDC-HCl (2.84 g, 14.8 mmol) in CH2C12 (150 mL). Purification by FC (EtOAc/beptane 1:4 -> 3:7 -> 2:3 -> 1:1) yielded the title compound (3.7 g, 40%). Rf = 0.55 (EtOAc/heptane i-.l). LC-MS: R, = 7.97.
(rac.)-(lR*, 55*)-6-(BenzylcyclopropyIcarbamoyl)-7-{4-13-(2-bromo-5-fluoro-pheDOxy)propyllphenyl}-3,9-diazabicyclo[3.3.1]noii-6-ene-3,9-dicarboxyIic acid 3-tert-buty\ ester 9-(2;2,2-trichIoro-l,l-dimethylethyI) ester (AK21)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), benzylcyclopropylamine (Loeppky, R. N.; et al., J. Org. Chem., 2000, 65, 96; 1.27 g, 1.50 mmol), DIPEA (0.6S4 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol),
HOBt (135 mg, 1.00 mmol) and EDC-HCl (287 mg, 1.50 mmol) in CH3CI2 (10 mL). Purification by FC yielded the title compound (520 mg, 57%). LC-MS: Rt = 7.79.
(rac.)'(]R*, 55*)-7-{4-p-{2-Bromo-5-fluorophenoxy)propyl]phenyI}-6-[(2-chlorobenzyOethylcarbamoyl]-3,9-diazabicy do [3.3.1 ]non-6-en e-3,9-dicarbo-xylic acid 3-iert-butyl ester 9-(2^^-trichioro-l,l-dimethylefhyI) ester (AK22)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), (2-chlorobeozyl)ethylamine (Ishihara, Y; et ai; Chem. Pharm. Bull., 1991, 39, 3225; 254 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00 mmol), DMAP (30 rag, 0.25
mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (287 mg, 1.50 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (475 mg, 51%). LC-MS: Rt = 7.82.
(rac.)'(lR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyljphenyl}-6-
[cyclopropyI-(2-fluorobeiiryl)carbamoyll-3,9-diazabicyclo[3.3.1]non-6-ene-

3,9-dicarboxylic acid 3-teH-butyl ester 9-(2,2,2-trichloro-14-dimethylethyl) ester (AK23)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), cyclopropyl-(2-fluorobenzyl)armiie (247 mg, 1.50 mmol), DIPEA (0.684 mL, 4.QQ mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg. 1.00 mmol) and EDC-HCl (287 mg, 1.50 mmol) in CH^Cb (10 mL). Pxirification by FC yielded the title compound (465 mg, 50%). LC-MS: R, = 7.69.
irac.)-{lR*, 55'*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cycIo-propyl-(3-trifluoromethylbenzyl)carbaraoyl]-3,9-diazabicyclo[3J.ljnon-6-ene-3,9-dicarbosylic acid 3-^er/-butyi ester 9-(2,2,2-trichloro-l,l-dimethyl-ethyl) ester (AK24)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), cyc]opropyl-(3-trifluoromethyibenzyl)amlne (Brabander, H. J.; et al; J. Org. Chem., 1967, S2, 4053; 323 rag, 1.50 nraiol), DIPEA (0.684 mL, 4.00 mmol),
DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (287 mg, 1.50 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (345 mg, 35%). LC-MS: R, = 7.76.
{rac)-ilR\ 55*>7-{4-[3-(2-Bromo-5-fluorophenoxy)propyllphcayl}-6-
[cyclopropyI-(2-methyIbeiizyl)carbamoyI)-3,9-diazabicycIo[33.11non-6-ene-3,9-dicarboxylic acid 3-terf-butyl ester 9-(2,2,2-trichloro-l,l-dimefhyIethyl) ester (AK25)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), cyclopropyl-(2-methylbenzyl)amine (242 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (287 mg, 1.50 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (722 mg, 78%). LC-MS: R, = 7.77.

(rac.)'(lR*, 55*)-7-(4~[3-(2-Bromo-5-nuorophenoxy)propyI]phenyl}-6--{cyclo-propyl-[2-(4-methoxyphenoxy)ethyI]carbamoyl}-3,9-diazabicyclo[3.3.11non-6-ene-3,9-dicarb03[yUc acid 3-rerr-butyI ester 9-(2,2,2-trichloro-l,l-dimethyl-ethyl) ester (AK26)
As for bicyclononene AK2, but firom bicyclononene Ay2 (779 mg, 1.00 mmol), cyclopropyl-(4-methoxyphenoxymethyl)amine (311 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00 mmol), DM\P (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol)
and EDC-HCl (287 mg, 1.50 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (579 mg, 60%). LC-MS: R, = 7.64.
(rac.)-(JR*, 5iy*)-7-{4-[3-(2-Brorao-5-fluorophenoxy)propyI]phenyl}-6-[cycIo-propyl-(2-m-tolyloxyethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylic acid 3-/er/-butyl ester 9-(2,2,2-trichloro-l,l-dimethyIethyl) ester
(AK27)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), cyclopropyl-m-tolyloxymethylamine (311 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol) and
EDCHCl (287 mg, 1.50 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (340 mg, 36%). LC-MS: R, = 7.83.
{rac)-(lR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclo-prQpyl-[2-(3,4-dimefhylphenoxy)ethyllcarbamoyI}-3^-diazabicyclo [3.3.11-non-6-ene-3,9-dicarbosylic acid S-tert-butyl ester 9-(2^,2-trichloro-l,l-dimethylethyl) ester (AK28)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), cyclopropyl-(3,4-dimethylphenoxymethyi)amine (308 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol)
and EDC-HCl (287 mg, 1.50 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (470 mg, 49%). LC-MS". R, = 7.93.

(rac.)-(lR*, 55*)-7-{4-[3-(2-Broino-5-fluorophenoxy)propyl]phenyI}-6-(cycIo-P ro py Iphenethy lea rb amoyl)-3,9-diazabicy do [3 J, 1] iioa-6-ene-3,9-dicarho-xylic acid 3-^^rt-butyl ester 9-(2,2,2-trichloro-l,l-dimethylethyl) ester (AK29)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), cyclopropyl-phenethylamine (Smith, P. W.; el al; J. Med. Chem., 1998, 4], 787; 242 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00 mniol), DMAP (30 mg, 0.25
mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCI (287 mg, 1.50 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (449 mg, 49%). LC-MS:R,= 7.72.
(rac.y(IR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyI]piienyl}-^{[2-(2-chIorophenyl)ethyl]cycIopropylcarbamoyl}-3,9-diazabicyclo[3.3.11non-6-eue-3,9-dicarboxyiic acid 3-tert'huty] ester 9-(2,2,2-frichIoro-14-dimethyIetiiyl)
ester (AK30)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), [2-(2-chloro-phenyI)ethyl]cyclopropylamine (294 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 rag, l.OQ mmol) and
EDC-HCI (287 mg, 1.50 mmol) in CH2CI2 (10 mL). Pmification by FC yielded the title compound (605 mg, 63%). LC-MS: R[e= 7.89.
(rac)-{lR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclo-propyI-[2-(2^-difluorophenyI)ethyl]carbamoyI}-3,9-diazabicycIo [3.3.1 Inon-6-ene~3,9-dicarboxyUc acid 3-/ert-butyI ester 9-(2,2^-trichloro-l,l-dimethyl-ethyl) ester (AK31)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), cyclopropyl-[2-(2,3-difluorophenyl)ethyl] amine (296 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol)

and EDC-HCl (287 mg, 1.50 mmol) in CHsCl; (10 mL). Purification by FC yielded the title compound (670 rag, 70%). LC-MS: R, = 7.70.
(i-ac.)-(2R*, 55*)-7-{4-[3-(2-Bromo-5-nuorophenoxy}propyl]phenyl}-6-{cycIo-propyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicycIo[3.3.1]non-6-ene-3,9-dicarboxylic acid "i-tert-hat}'} ester 9-(2,2,2-trichloro-l,l-di)metbyl-ethyl) ester (AK32)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), cyclopropyl-[2-(4-fluorophenyl)ethyl]amine (269 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol) and
EDC-HCl (287 mg, 1.50 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (638 mg, 68%). LC-MS: Ri = 7.70.
(rac.)-(lR*, 5iS'*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyI]phenyl}-6-(cycIo-propyl-(2-o-tolyIethyl)carbamoyI]-3,9-diazabicyclo [3.3.1] non-6-ene-3,9-dicarboxylic acid 3-tert-bufyI ester 9-(2,2,2-trichIoro-l,l-dimethy!ethyI) ester
(AK33)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), cyclopropyi-(2-o-tolyletiiyl)amme (263 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00
mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (287 mg, 1.50 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (659 mg, 70%). LC-MS: Ri = 7.58.
1:1 Mixture of (raa)-(}R*, 55*)-7'{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-[((2ff*)-2-Iiydroxy-2-pheoylethyl)methyIcarbamoyll-3,9-diaza-bicycIo[3.3.1]noD-6-ene-3,9-dicarboxyIic acid 3-tert-butyl ester 9-(2,2,2-trichIoro-l,l-dimethylethyl) ester and (rac.)-(JR*, 55*)-7-(4-[3-(2-bromo-5-fIuorophenoxy)propyiIphenyl}-6-[((25*)-2-hydroxy-2-plienylethyI)methyl-carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxyIic acid 3-tert-butyl ester 9-(2,2,2-trichloro-l,l-dimethylethyl) ester (AK34)

As for bicyclononene AK2, but from bicyciononene AY2 (779 mg, 1.00 mmol), (rflc.)-2-meihylaniino-I-phenylethanoI (310 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol) and
EDC-HCl (287 mg, 1.50 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compounds (456 mg, 50%). LC-MS: R, = 7.42.
(rac.y{lR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-
(cy clop ropy l-{33-dimethosyben2yl)carbamoyl]-3,9-diazabicyclo 13.3.1 jnon-6-ene-3,9-dicar boxy lie acid 3-/^rt-butyI ester 9-(2,2^-trichloro-l,l-dimethyl' ethyl) ester (AK35)
As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), cyclopropyl-(3,5-dimethoxybenzyl)amine (311 mg, 1.50 mmol), DIPEA (0.684-mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (287 rog, 1.50 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (736 mg, 76%). LC-MS: Rt = 7.73.
{rac.)-[lR*, 55*)-7-{4-t3-(2-Bromo-5-fluorophenoxy)propyllphenyl>-6-Icydo-propyK2-iJ-toIyIethyl)carbamoyI]-3,9-dia2ablcyclo[33,l]oon-6-ene-3,9-dicar-boxylic acid 3-/ert-butyi ester 9-(2^^-trichloro-l,l-dimethylethyl) ester (AK36)
As for bicyclononene AK2, but &om bicyclononene AY2 (779 mg, 1.00 mmol), cyclopropyI-(2-/Ktolylethyl)amine (263 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00
mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol) and EDCHCI (287 mg, 1.50 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (718 mg, 77%). LC-MS: R, = 7.73.
(rac.)-(JR*, 55'*)-6-[(2-AlIylben2yl)cycIopropylcarbamoylI-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phcnyI}-3,9-diazabicyclo[3.3.1Jnon-6-ene-3,9-

diearbo-xylic acid 3-(ert-butyl ester 9-(2,2,2-trichloro-l,l-dimethy]etliyI) ester (AK37)
As for bicycloDonene AK2, but from bicyclononene Ay2 (1.45, 2.00 nunol), (2-allylbenzyl)cyclopropylamine (1.12 g, 6.00 mmol), DIPEA (1.37 mL, 8.00 mmol), DMAP (62 mg, 0.50 mmol), HOBt (298 mg, 2.20 mmol) and EDC-HCl (576 mg, 3.00 mmol) in CH2CI2 (20 mL). Purification by FC yielded the intermediate compomid (1.77 g, 93%). LC-MS: R, = 7.95. Then as for compound AT, but from the former intermediate compound (1.77 g,
1.86 mmol), NMO-HjO (516 mg, 3.82 mmol), and OSO4 (2.5% in tert-BuOR, 0.276 mL, 0.023 mmol) in THF (40 mL), lert-BuOH (20 mL) and water (10 mL). Purification of the residue by FC (EtOAc/heptane 1:4 -> 2:3 -^ 3:2 -^ 4:1 -> EtOAc) yielded the 2"" intemiediate compound (548 mg, 27%). Rf = 0.60 (EtOAc). LC-MS: Rt = 7.43; ES+: 980.18.
Then as for compound AU, but from the 2"^ intermediate compound (928 mg, 0.945 mmol) and NaI04 (222 mg, 1.04 mmol) in THF (8 mL) and water (2 mL). Purification of the residue by FC (EtOAc/heptane 1:4 ~> 2:3) yielded the 3"^ intemiediate compound (868 mg, 97%). Rf = 0.80 (EtOAc). Finally as for compound AV, but from the 3"^ intermediate compound (868 mg, 0.914 mmol) and NaBH4 (38 mg, 1.0 mmol) in MeOH (10 mL). Purification of the residue by FC (EtOAc/heptane 2:3) yielded the title compound (603 mg, 69%). LC-MS: Rt = 7.44.
(racyilS*, Xy*)-6-I(2-ChIorbenzyl)cyclopropyIcarbamoyl]-7-{4-[2-(2^,5-trimethy!phenoxy)ethyl]phenyl}-3,9-diazabicyclo [33.1] non-6-ene-3,9-dicar-boiylic acid 3-tert-butyl ester 9-(2,2,2-trichloro-l,l-dimethy\etbyl) ester
(AK38)
As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58 mmol), (2-chlorobenzyl)-cycIopropylaniine (211 mg, 1.16 mmol), DIPEA (0.397 mL, 2.32 mmol), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol) and

EDC-HCl (167 mg, 0.87 mmol) in CH2CI2 (8 mL). Purification by FC \ielded the title compound (312 mg, 62%). LC-MS: R, = 7.66.
(rac.yilR*, 55*)-6-(BeDzyleyclop ropy lcarbamoyl)-7-{4-[2-(2,3,5-trimethyl-phenoxj')ethyi]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-3,9-dicarboxjiic acid 3~tert-hutyl ester 9-(2,2,2-trichlorQ-l,l-dimethylethyl) ester (AK39)
As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58 mmol), benzyl-cyclopropylamine (Loeppky, R, N.; el al., J. Org. Chem., 2000, 65, 96; 171 mg, 1.16 mmol), DIPEA (0.397 mL, 2.32 mmol), DMAP (18 mg, 0.15
mmol), HOBt (86 mg, 0.64 mmol) and EDC-HCl (167 mg, 0.87 mmol) in CH2CI2 (8 mL). Purification by FC yielded the title compound (340 mg, 70%). LC-MS; Rt = 8.12.
(rac.)-(ifi*, 55*)-6-[(2-ChIorobenzyl)ethylcarbainoyll-7-{4-[2-(23,5-
triinethyl-phenoxy)ethyIl phenyl}-3,9-diazabicyclo{3J.lJnon-6-ene-3^-dicarboxylic acid 3-tert-butyl ester 9-(2,2,2-trichloro-l,l-diraetfayIethyl) ester (AK40)
As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58 mmol), (2-chlorobenzyl)-ethyIamine (Ishihara, Y; et al; Chem. Pharm. Bull, 1991, 39, 3225; 197 mg, 1.16 mmol), DIPEA (0.397 mL, 2.32 mmol), DMAP (18 mg, 0-15
mmol), HOBt (86 mg, 0.64 mmol) and EDC-HCl (167 mg, 0.87 mmol) in CHzClz (8 mL). Purification by FC yielded the title compound (374 mg, 74%). LC-MS-. Rt = 8.30.
{rac.y{lR*, 5S*)-6-(CyclopropyU(2-fluorobeiizyl)carbamoyll-7-{4-[2.(2^,5-tri-m ethy lphenoxy)ethyl jpheny l}-3,9-diaza bicy do [3.3.1] non-6-ene-3,9dicarfaoxy-lic acid 3-/£r/-butyl ester 9-(2,2,2-trichIoro-l,l-dimethylethyl) ester (AK41)

As for bicyclononene AK2, but &om bicyclononene AY3 (411 mg, 0.58 mmol), cyclopropyl-(2-fluoroben2yI)amine (192 mg, 1.16 mmol), DIPEA (0.397 mL, 2.32
mmol), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol) and EDC-HCl (167 rag, 0.87 mmol) in CH2CI2 (8 mL). Purification by FC yielded the title compoimd (350 mg, 70%). LC-MS: Rt = 8.13.
{rac.y{lR*, 55*)-6-[ Cyclop ropy l-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[2-(23,5-trimethylphenoxy)ethyl]phenyI}~3,9-diazabicycio[3.3.1]non-6-ene-3,9-dicarboxylic acid 3-/^rt-butyl ester 9-(2,2,2-trichIoro-l,l-dimethyletbyl) ester (AK42)
As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58 mmol), cyclopropyl-(3-trifluoromethylbenzyl)amine (Brabander, H. J.; et al.\ J. Org. Chem., 1967, 32, 4053; 250 rag, 1.16 mmol), DIPEA (0.397 mL, 2.32 mmol),
DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol) and EDC-HCl (167 mg, 0.87 mmol) in CH2CI2 (8 mL). Purification by FC yielded the title compound (294mg, 56%). LC-MS: Ri = 8.16.
{rac.)-{lR*, 55*)-6-iCyclopropyI-(2-methylbeDzyl)carbamoyl]-7-{4-I2-(2^^-trimethylphenoxy)ethyl] phenyl}-3^-diazabicyclo[3.3.1 ]iion-6-ene-3,9-dicar-boiylic acid 3-tert-butyl ester 9-(2,2^-trichloro-l,l-^«nethylethyI) ester
(AK43)
As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58 mmol), cyclopropyl-(2-methylben2yl)amine (187 mg, 1.16 mmol), DIPEA (0.397 mL, 2.32 mmol), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol) and
EDC-HCl (167 mg, 0.87 mmol) in CH2CI2 (8 mL). Purification by FC yielded the title compound (294 mg, 56%). LC-MS: R^ = 8.15.
{rac.y{lR*, 5S*)-6-{CycIopropyl-[2-(4-methoxyphenosy)ethyllcarbamoyl5-7-{4- [2-(2,3,5-trimethylph enoxy)ethyl] ph enyl) -3,9-diaza bicyclo [3.3.1 ] non-6-

cne-3,9-dicarboxylic acid 3-tert-batyl ester 9-(2,2,2-trichloro-14-dimethyl-ethyl) ester (AK44)
As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58 mmol), cyclopropyl-[2-(4-methoxyphenoxy)ethyl] amine (187 mg, 1.16 mmol), DIPEA (0.397 mL, 2.32 mmol), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol)
and EDC-HCl (167 mg, 0.87 mmol) in CH^Cii (8 mL). Purification by FC yielded the title compound (159 mg, 30%). LC-MS: R, = 7.93,
(rac.)-(2S*, 5iS'*)-6-{Cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoy!}-7-{4- (2-(2,3)5-triiii ethylphenoxy)ethyl] pheny I}-3,9-diaza bicyclo [3.3.1 ] non-6-ene-3,9-dicarboxylic acid S-tert-butyl ester 9-(2,2^-trichloro-l,l-dimefhyi-ethyl) ester (AK45)
As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58 mmol), cyclopropyl-[2-(3-methoxyphenoxy)ethyl]amine (287 mg, 1.16 mmol), DIPEA (0.397 mL, 2.32 mmol), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol) and EDC-HCl (167 mg, 0.87 mmol) in CH2CI2 (8 mL). Purification by FC yielded the tide compound (237 mg, 45%). LC-MS: R, = 7.69.
{rac)-(lR*, 55*)-6-ICyclopropyI-(2-/«-toIyloxyethyl)carbamoyI]-7-{4-[2-
(2^,5-trimethylphenoiy)ethyl]phenyI}-3,9-diazablcycIo[33.11non-6-enc-3,9-dicar-boxylic acid 3-tert-butyl ester 9-(2^^-trichIoro-l,l-dimethylethyI) ester (AK46)
As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58 mmol), cyclopropyl-(2-m-tolyloxyethyl)amine (222 mg, 1.16 mmol), DIPEA (0.397 mL, 2.32 mmoi), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol) and
EDC-HCl (167 mg, 0.87 mmol) in CH2CI2 (8 mL). Purification by FC yielded the title compound (185 mg, 36%). LC-MS: R( = 8.12.

(rac.)-{lR% 55*)-6-(CyclopropylphenethylcarbamoyI)-7-(4-[2-(2,3,6-
trimethyl-phenoxy)ethyllphenyl}-3,9-diazabicyclol3.3.11noii-6-ene-3,9-dicarboxylic acid 3-(^rt-but>I ester 9-(2,2,2-trichloro-l,l-dimethyIethyI) ester
(AK47)
As for bicyclononene AK2, but from bicyclouonene AY3 (590 mg, 0.83 mmol), cyciopropyl-phenethyiamine (Smith, P. W.; et al\ J. Med. Chem., 1998, 41, 787; 402 mg, 2.49 mmol), DIPEA (0.568 mL, 3.32 mmol), DMAP (25 mg, 0.21
mmol), HOBt (169 mg, 1.25 mmol) and EDC-HCl (239 mg, 1.25 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (309 mg, 44%). LC-MS:Rt = 8.01.
(mc.)-(ifi*, 55*)-6-((2-(2-Chloropheayl)ethyllcyclopropylcarbamoyl}-7-{4-[2-(2,3,6-trimetliylphcnoxy)ethyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylic acid 3-tert-buty\ ester 9-(2,2,2-trichloro-l,l-dimethyIethyl) ester
(AK48)
As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0.83 mmol), [2-(2-chIoro-phenyl)ethyl]cyclopropylamine (487 mg, 2.49 mmol), DIPEA (0.568 mL, 3.32 mmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg, 1.25 mmol) and
EDC-HCl (239 mg, 1.25 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (272 mg, 37%). LC-MS; R, = 8.20.
(rac.}-{JR*, 55*)-^-{CycIopropyI-[2-(23-difluorophenyl)ethyl}carbamoyl}-7-{4-[2-(2^,6-trimethylphenoxy)ethyI]phenyl}-3,9-dia2abicycIo [3.3.1 ]noii-6-ene-3,9-dicarboxyJic acid 3-tert-butyl ester 9-(2;2,2-trichIoro-l,l-dimethylethyl) ester (AK49)
As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0.83 mmol),
cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amine (491 mg, 2.49 uimol), DIPEA (0.568 mL, 3.32 mmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg, 1.25 mmol)

and EDC-HCl (239 mg, 1.25 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (309 mg, 42%). LC-MS: R, = 7,98.
(rac.)-(ifl*, 56:*)-6-{CycIopropyH2-(4-fluorophenyl)ethyllcarbamoyl}-7-{4-[2-(2,3,6-trimetliylph enoxy)ethyl] ph enyl}-3,9-dia2abicycIo [3.3.1 ] non-6-en e-3,9-dicarboxyIic acid 3-tert-hutyl ester 9-(2,2,2-trichioro-l,l-dimethyIethyl) ester (AK50)
As for bicyclonooene AK2, but fi'om bicyclononene AYS (590 mg, 0.83 nmiol), cyclopropyl-[2-(4-fluorophenyl)ethyI]amine (491 mg, 2.49 mmol), DIPEA (0.568 mL, 3.32 Ynmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg, 1.25 ramol) and
EDC-HCl (239 mg, 1.25 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (294 mg, 41%). LC-MS: R, = 7.93.
irac.)-iIR*, 5i'*)-6-[CycIopropyI-(2-o-tolylethyl)carbamoyll-7-{4-[2-(2,3,6-triiDethylphenoxy)ethyllphenyl}-3,9-diazablcyclo[3.3,l]non-6-ene-3,9-dicar-boxylic acid 3-tert-butyl ester 9-(2^2,2-trichloro-l,l-dimethylethyl) ester (AK51)
As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0,83 mmol), cyclopropyl-(2-o-tolyIethyl)amine (491 rag, 2.49 mmol), DIPEA (0.568 mL, 3.32
mmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg, 1.25 mmol) and EDC-HCl (239 mg, 1.25 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (258 mg, 36%). LC-MS: Rt = 8.16.
l:l-Mixture of (rac.)-IR*, J5*)-6-K('?^*)-2-hydroxy-2-phenyletbyl)methy!-carbamoyI]-7-{4-[2-(2^,6-trimethyiphenoxy)ethyl]phenyl}-3,9-diazabicycIo-[3.3.1]non-6-ene-3,9-dicarboxyIlc acid 3-tert-bntyl ester 9-(2,2,2-trichloro-l,l-dimethylethyl) ester and (rac.)-(IS*, 55*)-6-K(2.y*)-2-hydroxy-2-phenylethyl)methyIcarbamoyll-7-{4-[2-(2,3,6-trimethylpfaenoxy)ethyn-pheoyI}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxyIic acid 3-/er/-butyl ester 9-(2,2,2-trichloro-l,l-dimethylethyl) ester (AK52)

As for bicyclononene AK2, but from bicycloaonene AYS (590 mg, 0.83 mmol), (rac.)-2-raethyiamino-l-phenyIethanoi (377 mg, 2.49 mmol), DIPEA (0.568 mL, 3.32 mmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg, 1.25 mmol) and
EDC-HCl (239 mg, 1.25 mmol) in CH2CI; (10 mL). Purification by FC yielded the title compounds (117 mg, 17%). LC-MS: Rt = 7.50.
(rac.)-(JJi*, 55*)-6-(Cyclopropyl-(3,5-diraethoxybenzyl)carbamoyl]-7~{4-{2-(2^,6-trim eth yiphen oxy)ethyll pheDyl}-3,9-dia2abicyclo [3.3.1 ] non-6-ene-3,9-dicarboxylic acid 3-/er^butyI ester 9-(2,2,2-trichIoro-l,l-dimethyIethyI) ester
(AK53)
As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0.83 mmol), cyclopropyi-(3,5-dimethoxyben2yl)amine (516 mg, 2.49 mmol), DIPEA (0.568 mL, 3.32 mmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg, 1.25 mmol) and
EDOHCl (239 mg, 1.25 mmoi) in CH2CI2 (10 mL). Purification by FC yielded the title compound (258 mg, 35%). LC-MS: Rt = 7.80.
(rac.)-(lS*, 55*)-6-[Cyclopropyl-(2-/j-tolyIethyl)carbanioylJ-7-{4-[2-(23,6-trimetbyIphenosy)ethyl]phenyl}-3,9-diazabicyclo[33.1Inon-6-ene-3,9-dicarboxylic acid 3-/ert-butyI ester 9-(2^^-trichloro-l,l-dmiethylethyI) ester (AK54)
As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0.83 mmol), cyclopropyl-(2-p-tolylediyl)amiiie (426 mg, 2.49 mmol), DIPEA (0.568 mL, 3.32
mmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg, 1.25 mmol) and.EDC-HCI (239 mg, 1.25 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (235 mg, 32%). LC-MS: I^ = 8.16.
(rac)-(lR% J5'*)-6-{CycIopropyl-[2-(2-hydroxyethyI)benzyI]carbamoyI}-7-{4-[2-(2,3,6-trimethyIphenoxy)ethyl] phenyl}-3,9-diazabicyclo 13.3. l]non-6-ene-

3,9-dicarboxyUc acid 3-(£r/-butyl ester 9-{2,2,2-trichloro-l,l-dimetiiyIethyl) ester (AK55>
As for bicyclononene AK2, but &om bicyclononene AV3 (1.18 g, 1.66 mmol), (2-aUylbeczyl)cyclopropylamine (932 mg, 4.98 mmol), DIPEA (1.14 mL, 6.64
mmol), DMAP (51 mg, 0.42 mmol), HOBt (338 mg, 2.50 mmol) and EDC-HCl (478 mg, 2.50 mmol) in CH2a2 (20 mL). Purification by FC yielded the intermediate compound (613 mg, 42%). LC-MS: R, = 8.16. Then as for compound AT, but &om the former intermediate compound (613 mg,
0.697 mmol), NMOH2O (141 mg, 1.05 mmol), and OSO4 (2.5% in tert-BuOU, 0.175 mL, 0.014 mmol) in THF (8 mL), ;er;-BuOH (4 mL) and water (2 mL). Purification of the residue by FC (EtOAc/heptane 1:1 -> EtOAc) yielded the 2"'^ intennediate compound (348 mg, 55%). Rf= 0.05 (EtOAc/heptane 1:1). LC-MS: R, = 7.31.
Then as for compound ATJ, but from the 2"^" intermediate compound (348 mg, 0.381 mmol) and NaI04 (122 mg, 0.571 mmol) in THF (6 mL) and water (2 mL). Drying the residue under high vacuum yielded the 3' intennediate compound (269 mg, 80%) that was used without further purification. LC-MS: Rt = 7.29. Finally as for compound AV, but from the 3'"' intermediate compound (269 mg, 0.305 mmol) and NaBH4 (13 mg, 0.34 mmol) in MeOH (5 mL). Purification of the residue by FC (EtOAc/heptane 1:4 ->• 2:3 -» 3:2 -> 4:1) yielded the title compound (210 mg, 78%). LC-MS: Rt= 7.55.
(rac)-(JR*, 5^*)-6-I(2-ChlorobciizyI)cycIopropylcarbanioylJ-7-{4-[2-(2-
chloro-4,5-dimethyIphenosy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.11non-6-ene-3,9-dicarboxylic acid 3-tert-butyI ester 9-(2,2,2-trichIoro-l,l-dimethylethyl) ester (AK56)
As for bicyclononene AK2, but from bicyclononene Ay4 (596 mg, 0.80 mmol), (2-chioroben2yl)-cyclopropylamine (290 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl

(307 mg, 1.55 mmol) in CH2CI2 (5 mL). Purification by FC yielded the title compound (451 mg. 74%). LC-MS: R, = 1.30.
(rac.)-{iR*^ 55'*)-6-t(2-Ctilorobenzyl)ethyk3rbamoyli-7-{4-[2-(2-chloro-4,5-dimethyiphenoxy)ethoxy] phenyl}-3,9-diazabicyclo [3.3.1 ]non-6-ene-3,9-dicar-boxylic acid S-iert-hutyi ester 9-(2,2,2-trichloro-14-dimethylethyI) ester
(AK57)
As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0,80 mmol), (2-clilorobenzyl)-ethylamine (Ishihara, Y; et ai; Chem. Pharm. Bull, 1991, 39, 3225; 290 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21
mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (307 mg, 1.55 mmol) in CH2CI2 (5 mL). Purification by FC yielded the title compound (596 mg, 83%). LC-MS: Ri= 1.30.
(rac)-(iJ?*, 55*)-7-{4-i2-(2-CWoro-4,5-dimethylpheiioxy)ethoxylphenyl}-6-[cycIopropyl-(2-fluorobenzyI)carbamoyI]-3^-diazabicyclo[3J.l]noD-6-ene-3,9-dicarboxylic acid 3-/er/-butyl ester 9-(2^,2-trichioro-l,l-dimethylethyl)
ester (AK58)
As for bicyclononene AK2, but fi:om bicyclononene Ay4 (596 mg, 0.80 mmol), cyclopropyl-(2-fluorobenzyl)amine (264 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2
mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (307 mg, 1.55 mmol) in CH2CI2 (5 mL). Purification by FC yielded the title compound (519 mg, 73%). LC-MS: Rt = 1.29.
{rac)-{lR*, 55'*)-7-{4-{2-(2-CIiloro-4,5-dimethyIphenoxy)ethoxy]phenyl}-6-[cyclopropyI-(3-trifluoromethylbenzyl)carbamoyI]-3,9-diazabicyclo[3.3.1]-noD-6-ene-3,9-dicar boxy lie acid 3-ferf-butyl ester 9-(2,2,2-trichIoro-l,l-dimethylethyl) ester (AK59)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80 mmol), cyclopropyl-(3-trifluoromethylbenzyi)amine (Brabander, H. J.; et al; J. Org. Chem., 1967, 32. 4053; 344 mg, 1.60 mmol), DIPEA (0.548 mL. 3.2 mmol),
D^MP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (307 mg, 1.55 mmol) in CH2CI2 (5 mL). Purification by FC yielded the title compound (584mg, 78%). LC-MS: R, - L30.
{rac.)-{lR*, 55*)-7-(4-[2-(2-Chloro-4,5-diraethylphenoxy)ethoxylplieayl}-6-[cyclo pro pyl-(2-inethylbenzyl)carbamoyIl-3,9-diazabicycIo [3.3.1 In on-6-ene-3,9-dicarboxylic acid 3-tert-butyI ester 9-(2,2,2-trichloro-l,l-dimethyIethyI) ester (AK60)
As for bicyclononene AK2, but from bicyclononene Ay4 (596 mg, 0.80 mmol), cyclopropyl-(2-methyibenzyi)amine (258 mg, 1.60 mmol), DIPEA (0.54S mL, 3.2
mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (307 mg, 1.55 mmol) in CH^Cli (5 mL), Purification by FC yielded the title compound (569 mg, 48%). LC-MS: Rt = 1.30.
{rac.)-{lR*, 55*)-7-{4-12-(2-ChIoro-4,5-dimethylphenoxy)ethoxylphenyI}-6-{cyclopropyI-[2-(4-methoxyphenoxy)ethyIIcarbamoyl}-3,9-diazabicycIo-[3.3.1]non-6-ene-3,9-dicarboxylic acid 3-Cert-butyI ester 9-(2^^-trichloro-l,l-dimethylethyO ester (AK61)
As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80 mmol), cyclopropyl-[2-(4-methoxyphenoxy)etliyl]amine (332 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol)
and EDC-HCl (307 mg, 1.55 mmol) in CH2CI2 (5 mL). Purification by FC yielded the title compound (591 mg, 79%). LC-MS: R, = 1.28.
{rac.y{lR*, 55:*)-7-{4-[2-(2-Chloro-4,5-dimetbyiphenosy)ethoxylphenyl}-6-{cyclopropyl-[2-(3-methoxyphenoxj)ethyl]carbamoyl}-3,9-diazabicycIo-

[3.3.1]non-6-ene-3,9-dicarboxy]ic acid 3-terl-butyl ester 9-(2^,2~tricfaIoro-l,I-dimethylethyl) ester (AK62)
As for bicyclonoaene AK2, but fi:ora bicyclononeoe AY4 (596 mg, 0.80 mmol), cyclopropyl-[2-(3-methoxyphenDxy)ethyl]amine (332 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol)
and EDC-HCl (307 mg, 1.55 mmol) in CH2C!2 (5 mL). Purification by FC yielded the title compound (584 mg, 77%). LC-MS: Rt = 1.28.
(rac.)-ilR*y 55*)-7-{4-[2-(2-ChIoro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-lcycIopropyl-(2-ni-tolylDxyethyl)carbamoyll-3,9-dia2abicyclo(3.3.11noii-6-ene-3,9-dicarboxyIic acid 3-tert-buty\ ester 9-(2,2,2-triciiIoro-l,l-dimethylethyl) ester (AK63)
As for bicyclononene AK2, but from bicyciononene AY4 (596 mg, 0.80 mmol), cyclopropyl-(2-p-tolyloxyethyl)amine (306 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and
EDC-HCl (307 mg, 1.55 mmol) in CH2CI2 (5 mL). Purification by FC yielded the title compound (525 mg, 71%). LC-MS: Rt= 1.30.
(rac)-{lR*, 55*)-7-{4-I2- As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80 mmol), cyclopropyl-phenethylamine (Smith, P. W.; et al; J. Med. Chem., 1998, 41, 787; 258 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol),
HOBt (135 mg, 1.00 mmo!) and EDC-HCl (307 mg, 1.55 mmol) in CHjCh (5 mL). Purification by FC yielded the title compound (360 mg, 50%). LC-MS: R| = 1.30.

{rac.)-(lR\ 55*)-7-{4-[2-(2-Chloro-4,5-dimethyIphenoxy)ethox3'-]phenyI}-6-{[2-(2-chlorophenyl)ethyI]cycIopropylcarbamoyl}-3,9-diazabicycIo[3.3.1]noD-6-ene-3,9-dicarboxyIic acid 3-tert-hutyl ester 9-(2,2,2-trichIoro-l,l-dimethyI-ethyl) ester (AK65)
As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80 mmol), [2-(2-chloro-phenyl)ethyl]cyclopropylamiiie (313 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and
EDC-HCl (307 mg, 1.55 mmol) in CH2CI2 (5 mL). Purification by FC yielded the title compound (572 mg, 76%). LC-MS:Rt= 1.30.
(rac.)-(llt*, 5iS'*)-7-(4-[2-(2-ChIoro-4,5-dimethylphenoxy)ethoxylphenyI!-6-{cycIopropyl-[2-(2^-difluorophenyl)ethyI]carbamoyi}-3,9-diazabicyclo[3.3.1]-non-6-ene-3,9-dicarboxylic acid 3-tert-butyl ester 9-(2,2,2-trichloro-l,l-dimetbylethyl) ester (AK66)
As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80 mmol), cyclopropyI-[2-(2,3-diiluorophenyl)ethyI]amine (316 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol)
and EDC-HCl (307 mg, 1.55 mmol) in CH2CI2 (5 mL). Purification by FC yielded the title compound (584 mg, 79%). LC-MS: Rt = 1.29.
(rac.)-(JR*, 55*)-7-{4-[2-(2-Chloro-4,5-dimethyIphenoxy)ethoxy]phenyl}-6-{cyclopropyl- [2-(4-fluoropbenyl)etfayl] carbamoyl}-3,9-diazabicyclo [3^. 1] non-6-ene-3,9-dicarboxyUc acid 3-tert-butyl ester 9-(2,2,2-trichIoro-l,l-dimethyl-ethyl) ester (AK67)
As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80 mmol), cyclopropyI-[2-(4-fluorophenyl)ethyl]amine (287 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (307 mg, 1.55 mmol) in CH2CI2 (5 mL). Purification by FC yielded the title compound (616 mg, 84%). LC-MS: R, = 1.28.

(rac.)-(JR% J^*)-7-{4-I2-(2-Chloro-4,5-dimethylplienoxy)ethoxy]pheDy!}-6-[cyclopropyI-(2-(7-toIylethyI)carbamoyI]-3,9-dJazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylic acid 2>-teii-hut\\ ester 9-{2,2,2-trichloro-l,l-dimetbylethyl) ester (AK68)
As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80 mmoi), cyclopropyl-(2-o-toIyIethyl)araine (280 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2
mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (307 mg, 1.55 mmo!) in CH2CI2 (5 mL). Pmification by FC yielded the title compound (556 mg, 76%). LC-MS: Rt= 1.28.
l:l-Mixfure of (rac.)-{lR*, 55*)-7-{4-(2-(2-chloro-4,5-dimethylphenoxj)-ethoxy]phenyl}-6-[((2/(*)-2-hydroxy-2-phenyIethyl)methykarbainoyl]-3,9-diazabicycIo[3.3.1]non-6-ene-3,9-dicarboxyIic acid 3-fert-butyI ester 9-(2^,2-trichloro-l,l-dimetliylethyI) ester and (raayilR*, 55*)-7-{4-[2-(2-chloro-4,5-dimethy Iphenoiy)efhoxy]phenyI}-6-[((2.5 *)-2-hydro xy-2-phenyIethy l)inethyl-carbamoyl]-3,9-diazabicycIo[33.1]non-6-enc-3,9-dicarboxylic acid 3-tert-butyl ester 9-(2^,2-trichloro-l,l-dunethylethyl) ester {AK69)
As for bicyclonoQene AK2, but &om bicyclononene AY4 (596 mg, 0.80 mmol), (/■ac.)-2-methylamiiio-l-pheDyIetlianol (242 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and
EDC-HCl (307 mg, 1.55 mmol) in CH2CI2 (5 mL). Purification by FC yielded the title compounds (380 mg, 54%). LC-MS: R^ = 1.23.
(rac.y{lR*, 55*)-7-{4-[2-(2-Chloro-4,5-dimethyiphenoxy)ethoxy]phenyI}-6-[cycIopropyl-(3,5-dimethoxybenzyI)carbamoyll-3,9-diazabicyclo[3.3.1Jnon-6-ene-3,9-dicarboxylic acid 3-tert-hutyl ester 9-(2,2,2-trichIoro-l,l-diinethyl-ethyl) ester (AK70)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, O.SO mmol), cyclopropyi'(3,5-dimetiioxybenzyi)amine (332 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol). DMAP (25 rag, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and
EDC-HCl (307 mg, 1.55 mmol) in CH^Cia (5 mL). Purification by FC >-ielded the title compound (619 mg, 83%). LC-MS: R, = 1.28.
(rac.)'iJR*, 55*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-p-toIylethyl)carbamoyl]-3,9-diazabicyclo [3.3.1 ]non-6-ene-3,9-dicarboxylic acid 3-ter(-butyl ester 9-(2,2,2-tricb(oro-l,l-dimethylethyl) ester (AK71)
As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80 mmol), cyclopropyI-(2-p-tolyIethyI)amine (280 mg, 1.60 mmol), DIPEA (0.548 naL, 3.2
mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (307 mg, 1.55 mmol) in CHiCb (5 mL). Purification by FC yielded the title compound (619 mg, 83%). LC-MS: R, = 1.28.
(rac.)-{lR*, 55'*)-7-{4-[2-(2-Chloro-4,5-dimethyIphenoxy)ethoxylphenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)beiizyI]carbamoyl}-3,9-diazabicydo[3.3.1I-iiOD-6-eiie-3^-dicarboxylic acid 3-/ert-butyI ester 9-(2^^-trichloro-l,l-dimethyl-ethyl) ester (AK72)
As for bicyclononene AK2, but from bicyclononene AY3 (1.00 g, 1.34 mmol), (2-aIlylbenzyl)cyclopropylamine (752 mg, 4.02 mmol), DEPEA (0.918 mL, 5.26
mmol), DMAP (41 mg, 0.34 mmol), HOBt (199 mg, 1.47 mmol) and EDC-HCl (385 mg, 2.01 mmol) in CH2CI2 (15 mL). Purification by FC yielded the
intermediate compound (845 mg, 69%). Rf= 0.45 (EtOAc/heptane 1:1). LC-MS:
Rt = 7.85.
Then as for compound AT, but from the former intennediate compound (845 mg,
0.926 mmol), NMO-H.O (150 mg, 1.11 mmol), and Os04 (2.5% in (ert-BuOH, 0.173 mL, 0.014 mmol) in THF (8 mL), ten-BuOH (4 mL) and water (2 mL). Purification of the residue by FC (EtOAc/heptane 1:1 -> EtOAc ^ MeOH/EtOAc

1:9) yielded the 2"" intermediate compound (616 mg, 70%). Rf = 0.05 (EtOAc/heptanel:!). LC-MS: R, = 7.04.
Then as for compound AU, but from the 2"' intermediate compound (616 mg, 0.649 mmol) and NaI04 (208 mg, 0.973 mmol) in THF (6 mL) and water (2 mL). Drying the residue under high vacuum yielded the 3^^" intermediate compound (477 mg, S0%) that was used without further purification. LC-MS: R, = 7.43. Finally as for compound AV, but fiom the 3'^ intermediate compound (477 mg, 0.520 mmol) and NaBH4 (22 mg, 0.57 mmol) in MeOH (5 mL). Purification of the residue by FC (EtOAc/heptane 1:4 -^ 2:3 -^ 3:2 -> 4:1) yielded the title compound (210 mg, 78%). Rf-0.10 (EtOAc/heptane 1:1). LC-MS: Rt = 7.26.
irac.y{lR*, 55*)-7-{4-l2-(4-Bromophenosy)ethoxylphenyl}-6-[(2-chloro-
benzyl)cyclopropylcarbamoylJ-3,9-diazabicycloI33.1]non-6-ene-3,9-dicarbo-xylic acid 3-/ert-butyl ester 9-(2^,2-trichloro-l,l-dimethylethyl) ester tAK73)
As for bicyclononene AK2, but firom bicyclononene AYS (534 mg, 0.7 mmol), (2-chlorobenzyl)-cyclopropylamine (200 mg, 1.10 mmol), DEPEA (0.479 mL, 2.8
mmoi), DMAP (21 mg, 0.18 mmol), HOBt (113 mg. 0.84 mmol) and EDC-HCl (211 mg, 1.1 mmol) in CH2CI2 (7 mL). Purification by FC yielded the title compound (263 mg, 39%). LC-MS: Rt = 1.28.
(roc;)-(iiZ*, 55*)-6-(BenzyIcycIopropylcarbamoyl)-7-{4-[2-(4-bromophenoiy)-ethosylphenyl}-3,9-diazabicyclol3^.1]non-6-eiie-3,9-dicarboxyUc acid 3-tert-butyl ester 9-(2;2,2-trichIoro-l,l-dimethylethyl) ester (AK74)
As for bicyclononene AK2, but ftom bicyclononene AYS (534 mg, 0.7 mmol), benzylcyclopropyl-amine (Loeppky, R. N.; et al., J. Org. Chem., 2000, 65, 96; 162 mg, 1.10 mmol), DIPEA (0.479 mL, 2.8 mmol), DMAP (21 mg, 0.18 mmol),
HOBt (113 rag, 0.84 mmol) and EDC-HCl (211 mg, I.l mmol) in CH2CI2 (7 mL). Purification by FC yielded the title compound (263 mg, 39%). LC-MS: R, = 1.26.

(rac.y{lR*, 5^*).7-{4-[2-(4-Bromopheiioxy)ethoxy]phenyI}-6-[(2-chloro-
benzyl)ethylcarbamoyl]-3,9-diaEabicycloI3.3.1]non-6-ene-3,9-dicarboxylic acid 3~tert-hutyl ester 9-{2^,2-trichloro-l,l-dimethyIethyl) ester (AK75)
As for bicyclononene AK2, but from bicyclononene AYS (534 mg, 0.7 minol), (2-chlorobenzyl)-etliylamLne (Ishihara, Y; et al\ Chem. Pharm. Bull., 199U 39, 3225; 187 mg, 1.10 mmol), DIPEA (0.479 mL, 2.8 mmoi), DMAP (21 mg, 0.18
mmol), HOBt (113 mg, 0.84 mmol) and EDC-HCl (211 mg, 1.1 mmol) in CH2CI2 (7 mL). Purification by FC yielded the title compound (204 mg, 32%). LC-MS: Rt=1.28.
(rac.)-(lR*, 55*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-lcycIopropyI-{2-fluorobenzyl)carbamoyl]-3,9-diazabicycIo[3^.1]non-6-ene-3,9-dicarboxylic acid 3-tert-buty] ester 9-(2^,2-frichloro-l,l-dimethylethyl) ester (AK76)
As for bicyclononene AK2, but from bicyclononene AYS (534 mg, 0.7 mmol), cyclopropyl-(2-fluorobenzyl)amine (182 mg, 1.10 mmol), DIPEA (0.479 mL, 2.8
mmol), DMAP (21 mg, 0.18 mmol), HOBt (113 mg, 0.84 mmol) and EDC-HCl (211 mg, 1.1 mmol) in CH2CI2 (7 mL). Purification by FC yielded the title compound (233 mg, 37%). LC-MS: Rt= 1.27.
(r(7a)-(iJ?*, 55*)-7-{4-[2-(4-Broinophenoxy)ethoxy]phenyI}-6-[cyclopropyI-(3-trifluoromethylben2yl)carbamoyl]-3^-diazabicyclo[3J.llnon-6-ene-3^-dicarboxylic acid 3-tert-bntyl ester 9-(2,2^-trichIoro-14-diinethylethyl) ester
(AK77)
As for bicyclononene AK2, but from bicyclononene AYS (534 mg, 0.7 mmol), cyclopropyl-(3-trifluoromethylbenzyl)amine (Brabander, H. J.; et al; J. Org. Chem., 1967, 32, 4053; 237 mg, l.lO mmol), DIPEA (0.479 mL, 2.8 mmol),
DMAP (21 mg, 0.18 mmol), HOBt (113 mg, 0.84 mmol) and EDC-HCi (211 mg, 1.1 mmol) in CH2CI2 (7 mL). Purification by FC yielded the title compound (276 mg,41%). LC-MS: Ri= 1.27.

(racyilR*, 55'*)-7-{4-[2-{4-Bromophenoxy)ethoxylphenyl}-6-[cyclopropyl-(2-methyibenzyl)carbamoyl]-3,9-diazabicyclo{3.3.1]non-6-ene-3,9-dicarboxyiic acid 3-tert'hutyl ester 9-(2,2^-trichloro-l,l-dimethylethy!;) ester (AK78)
As for bicyclononene AK2, but from bicyclononene AYS (534 mg, 0.7 mmol), cyclopropyl-(2-methylben2yl)amine (17S mg, 1.10 mmol), DIPEA (0.479 mL, 2.8
mmol), DMAP (21 mg, 0.18 mmol), HOBt (U3 mg, 0.84 mmol) and EDC-HCI (211 mg, 1.1 mmol) in CH2CI2 (7 mL). Purification by FC yielded the title compound (171 mg, 27%). LC-MS: Rt = 1.26.
{racy(l-R*, 55*)~7-{4-[2-(4-Bromophenoxy)ethoxy]phenyI}-6-{cyclopropyl-[2-(4-ni etboxyphen oxy)ethy 1] carbamoyl} -3,9-diazabicyclo [3.3.1] noD-6-ene-3,9-dicarboxylic acid 3-tert-butyI ester 9-(2,2^2-trichIoro-l,l-dimethylethyl) ester
(AK79)
As for bicyclononene AK2, but from bicyclononene AYS (534 mg, 0.7 mmol), cyclopropyl-[2-(4-methoxyphenoxy)elhyl]amine (228 mg, 1.10 mmol), DIPEA (0.479 mL, 2.8 mmol), DMAP- (21 mg, 0.18 mmol), HOBt (113 mg, 0.84 mmol)
and EDC-HCI (211 mg, 1.1 mmol) in CH2CI2 (7 mL). Purification by FC yielded the title compound (190 mg, 29%). LC-MS: R^ = 1.26.
(rac)-(lR*, 5S*)-7-{4-I2-(4-BrQinopheiioxy)ethoxy]pbeByI}-6-{cycl(jpropyl-[2-(3,4-dimethyIpheno3iy)etbyl] carbamoyI)-3^-diazabicycIo [33.1] non-6-ene-3,9-dicarboxylic acid 3-/ej*/-butyl ester 9-(2,2^-trichloro-l,l-d'nietliylethyl) ester
(AKSO)
As for bicyclononene AK2, but from bicyclononene AYS (700 mg, 0.918 mmol), cyclopropyI-[2-(3,4-dimethyIphenoxy)ethyl]amxne (565 mg, 2.75 mmol), DIPEA (0.628 mL, 3.67 mmoL), DMAP (28 mg, 0.23 mmol), HOBt (136 mg, 1.01 mmol)
and EDC-HCI (264 mg, 1.38 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (199 mg, 23%). LC-MS: R, = 7.76.

(rac.)-(]R*, J5*)-7-{4-[2-(4-Bron!ophenoxy)ethoxylphenyl}-6-{[2-(2-chIoro-phenyl)ethyl]cyclopropykarbamoyl}-3,9-diazabicycIo[3.3.1]noa-6-ene--3,9-dicarboxylic acid 3-lert-hutyl ester 9-(2,2,2-tricbloro-l,l-dimethylethyI) ester (AK81)
As for bicyclononene AK2, but from bicyclononene AYS (700 mg, 0.918 mmol), [2-(2-chloro-phenyl)ethyl]cyclopropylamme (538 mg, 2.75 mmol), DIPEA (0.628 mL, 3.67 mmoi), DMAP (28 mg, 0.23 mmol), HOBt (136 mg, 1.01 mmol) and
EDC-HCl (264 mg, 1.38 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (256 mg, 30%). LC-MS: Rt = 7.70.
{rac.)-{lR*, 55'*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-12-(2,3-difluorophenyl)ethyl] carbamoyl}-3,9-dlazabicy do [3.3.1 ]non-6-ene-3,9-dicarboxylic acid 3-ter/-butyI ester 9-(2,2,2-trichloro-l,l-dimethylethyi) ester (AK82)
As for bicyclononene AK2, but from bicyclononene AYS (700 mg, 0.918 mmol), cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amine (542 mg, 2.75 mmol), DIPEA (0.628 mL, 3.67 mmol), DMAP (28 mg, 0.23 mmol), HOBt (136 mg, 1.01 mmol)
and EDC-HCl (264 mg, 1.38 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (245 mg, 28%). LC-MS: Rt = 7.55.
(rrtc.)-(iJ2*)55'*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyI}-6-{cycIopropyl-{2-(4-fluoropheayl)ethyllcarbamoyI}-3,9-diazabicyclo [3.3.1 ]non-6-ene-3,9-dicar-boxylic acid 3-/er^butyl ester 9-(2,2,2-trichloro-l,l-dimethylethyl) ester (AK83)
As for bicyclononene AK2, but from bicyclononene AYS (700 mg, 0.918 mmol), cyclopropyl-[2-(4-fluorophenyl)ethyl]amine (493 mg, 2.75 mmol), DIPEA (0.628 mL, 3.67 mmol), DMAP (28 mg, 0.23 mmol), HOBt (136 mg, 1.01 mmol) and

EDC'HCI (264 mg, 1.38 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (220 mg, 26%). LC-MS: R^ = 7.51.
(mc.)-(lR*, 5iS'*)-7-{4-{2-(4-Bromophenoxy)ethoxy]phenyI}-6-[cycIopropyl-(2-(7-toIyIethyI)earbamoyl]-3,9-diazabicyclo[3.3.1]non~6-ene-3,9-dicarboxyIic acid 3-tert-buty} ester 9-(2,2,2-trichloro-l,l-dimethyIcthyl) ester (AK84)
As for bicyclononene AK2, but from bicyclononene AYS (700 mg, 0.918 mmol), cyclopropyl-(2-o-tolylethyl)amine (482 mg, 2.75 mmol), DIPEA (0.628 mL, 3.67
mmol), DMAP (28 mg, 0,23 mmol), HOBt (136 mg, 1.01 mmol) and EDC-HCl (264 mg, 1.38 mmol) in CH3CI2 (10 mL). Purification by FC yielded the title compound (252 mg, 30%). LC-MS: Ri = 7.66.
(rac.)-(IR*, 5iy*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyI}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicycIo[3.3.1]non-6-ene-3,9-dicarboxy-lic acid S-tert-hutyl ester 9-{2^,2-trichloro-l,l-dimethylethyl) ester
(AK85)
As for bicyclononene AK2, but fi-om bicyclononene AYS (700 mg, 0.918 mmol), Cyclopropyl-(3,5-dmiethoxy-benzyl)-amine (570 mg, 2.75 nmiol), DIPEA (0.628 mL, 3.67 mmol), DMAP (28 mg, 0.23 mmol), HOBt (136 mg, 1.01 mmol) and
EDC-HCl (264 mg, 1.38 mmol) in CH2CI2 (10 mL). Purification by FC yielded the title compound (242 mg, 28%). LC-MS: R* = 7.42.
(rac.)-{lR*, 55*)-7-{4-[2-(4-Bromopheno3ty)ethoxy]phenyl}-6-IcycIopropyl-(2-/?-tolyIethyI)carbamoyI]-3,9-diazabicyclo[33.1]non-6-ene-3,9-dicarboxylic acid 3-fert-hutyl ester 9-(2,2,2-trichloro-l,l-dimethylethyI) ester (AK86)
As for bicyclononene AK2, but from bicyclononene AYS (700 mg, 0.918 mmol), cyclopropyl-(2-;7-tolylethyl)amine (482 mg, 2.75 mmol), DIPEA (0.628 mL, 3.67
mmol), DMAP (28 mg, 0.23 mmol), HOBt (136 mg, 1.01 mmol) and EDC-HCl

(264 mg, 1.38 raraol) in CH2CI2 (10 mL). Purification by FC yielded the titie compound (246 mg, 29%). LC-MS: Rt = 7.66.
(/■ac.)-(7.ff*, 55*)-7-(4-{2-(4-Bromophenoxy)ethoxy]phenyI}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl] carbamoyl}-3,9-dia2abicyclo [3.3.1] non-6-ene-3,9-dicarboxylic acid 3-/e;-/-butyl ester 9-(2,2,2-trichloro-l,l- As for bicyclononene AK2, but firom bicyclononene AY5 (1.00 g, 1.31 mmol), (2-aliylbenzyl)cyclopropylamine (752 mg, 4.02 mmol), DIPEA (0.918 mL, 5.26
mmol), DMAP (41 mg, 0.34 mmol), HOBt (199 mg, 1.47 mmol) and EDC-HCI (385 mg, 2.01 mmol) in CH2CI2 (15 mL). Purification by FC yielded the intermediate compound (875 mg, 72%). Rf= 0.45 (EtOAc/heptane 1:1). LC-MS; R, = 7.69. Then as for compound AT, but firom the former intermediate compound (875 mg,
0.939 mmol), NM0-H20 (152 mg, 1.13 mmol), and OSO4 (2.5% in fer(-BuOH, 0.236 mL, 0.019 mmol) in THF (8 mL), tert-BuOH (4 mL) and water (2 mL). Purification of the residue by FC (EtOAc/heptane 1:1 -> EtOAc -> MeOH/EtOAc 1:9) yielded the 2"' intermediate compound (310 mg, 34%). Rf = 0.05 (EtOAc/heptane 1:1). LC-MS: Ri = 6.86.
Then as for compound AU, but fi-om the 2"** intermediate compound (310 mg, 0.321 mmol) and NaI04 (139 mg, 0.481 mmol) in THF (6 mL) and water (2 mL). Drying the residue under hi^ vacuum yielded the 3^** intermediate compound (239 mg, 80%) that was used without further purification. LC-MS: Rt = 7.29. Finally as for compound AV, but firom the 3^^ intermediate compound (239 mg, 0.256 mmol) and NaBH4 (U mg, 0.28 mmol) in MeOH (5 mL). Purification of the residue by FC (EtOAc/heptane 1:4 -> 2:3 -^ 3:2 -> 4:1) yielded the title compound (170 mg, 71%). Rf= 0.10 (EtOAc/heptane 1:1). LC-MS: R, = 7.13.
Compounds of type AL

(rac.)-ilR*, 55*)-7-{4-[2-(2-Bromo-5-fluorophenoxy)ethyI]phenyI}-6-(methyI-
pbenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxyIic acid
2,2,2-trkhloro-l,l-duncthylethyl ester hydrochloride salt (ALl)
A sol. bicyclononene AKl (540 mg, 0.61 mmol)! in CHjCli (10 mL) was cooled to O^C. HCl/dioxane (4M, 10 mL) was added and the ice bath was removed. After 4 h stirring at it the solvents were removed under reduced pressure and the residue dried under high vacuum. The crude was used without tiarther purification.
irac.)-{lR*, 55*)-6-((2-Chlorobeiizyl)cyclopropylcarbamoyll-7-{4-[3-(2,3,6-trifluorophenoxy)propyI] phenyl}-3,9-diazabicy do [3.3.1 ]non-6-en e-9-carboxy-lic acid 2,2,2-trichloro-l,l-dimethyl-ethyl ester hydrochloride salt (AL2)
As for compound ALl but from bicyclononene AK2 (407 mg, 0.47 mmol) m CHzCl; (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 1.06; ES+: 796.34.
iracyilR*, 55*)-6-(BeiizyIcyclopropylcarbamoyl)-7-{4-I3-(2^,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[33.1Jnon-6-ene-9-carboxylic acid 2^,2-trichloro-l,l-dlmethy!-ethyI ester hydrochloride salt {AL3)
As for compound ALl but from bicyclononene AK3 (570 mg, 0.65 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 1.04; ES+: 766.34.
(racy(lR*, J5'*)-6-I(2-Chloroben2yl)ethytcarbamoyl]-7-{4-13-(23,6-trifluoro-phenoxy)propyl]phenyI}-3,9-diazabicycIo[33.11non-6-ene-9-carhoxyUc acid 2,2;2-trichloro-l,l-dimethylethyl ester hydrochloride salt (AL4)
As for compound ALl but from bicyclononene AK4 (about 0.55 mmol) in CHiCia (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R^ = 1.19; ES+: 786.25.

(mc.)'(lR*, 55*)-6-[CyclopropyI-(2-fluorobenzyl)carbamoyll-7-{4-(3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-dia2abicycIo[33.1]noa-6-eae-9-carbosylic acid 2,2,2-trichloro-14-dimcthyiethyI ester hydrochloride salt (AL5)
As for compound ALl but from bicyclononene AK5 (about 0.55 mmol) in CH2CI2 (5 mL) and HCVdioxaae (4M, 5 mL). LC-MS: Rv= 1.18; ES+: 782.28.
(rac.)'{lR*, 55 *)-6-lCy clop ropy l-(3-trifluoromethylbeiizy])carbamoyl]-7-{4-[3-(23,6-trifluoropheDOXy)propyI]pheoyl}-3,9-diazabicyclo[33.1]Don-6-ene-9-carboxyllc acid 2,2,2-trichloro-l,l-dimethylefhyl ester hydrochloride salt
(AL6)
As for compound ALl but from bicyclononene AK6 (about 0.55 mmol) in CH2CI2 (5 mL) and HCI/dioxane (4M, 5 mL). LC-MS: R^ = 1.20.
0-ac.)-(lR*, 55*)-6-[Cyclopropyl-(2-methylbeiizyI)carbamoyll-7-{4-[3-(23,6-trifluorophenoxy)propyl]phenyI}-3^-diazabicyclo[3.3.1]non-6-ene-9-carboxy-lic acid 2»2,2-trichloro-l,l-diinethylethyl ester hydrochloride salt (AL7)
As for compound ALl but from bicyclononene AK7 (about 0.55 mmol) in CH2CI2 (5 mL) and HCI/dioxane (4M, 5 mL). LC-MS: Rt = 1.21; ES+: 778.30.
(rac.)-(iiJ*, 5iS*)-6-[CyclopropyH4-methoxyphenoxymethyl)carbamoyl]-7-{4-l3-(23,6-trifluorophenoxy)propyl]phenyl)-3,9-diazabicyclo [3.3.1] no D-6-ene-9-carboxyIic acid 2,2,2-trichIoro-l,l-dimethylethyl ester hydrochloride salt
(AL8)
As for compound ALl but from bicyclononene AK8 (about 0,55 mmol) in CH2CI2 (5 mL) and HCiydioxane (4M, 5 mL). LC-MS: Rt = 1.21.

(_rac.y(lS% 55*)-6-[Cyclopropyl-(3-methoxyphenoxymethyI)carbamoyI]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyi}-3,9-diazabicy do [3.3.1] non-6-ene-9-carboxylic acid 2,2,2-trichIoro-l,l-dimethyIethyI ester hydrochloride salt
(AL9)
As for compound ALl but from bicyclononene AK9 (about 0.55 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R^= 1.18.
(mc.)'(lR*, 55'*)-6-(Cyclopropyl-m-tolyloxymethyicarbamoyi)-7-(4-[3-(2^,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclol3.3.1]non-6-cne-9-carboxy-lie acid 2^^-tricbIorQ-l,l-dimetliylethyl ester hydrochloride salt (ALIO)
As-for compound ALl but from bicyclononene AKIO (about 0.55 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 1.24.
{rac.)-{lR*^ 55'*)-6-lCyclopropyl-(3,4-dimethylpheiioxymethyl)carbamoyl]-7-{4-l3-(2y3,6-trifluo ropheaoxy)prQpy!l pheny l}-3,9-diazabicy do {3.3. lluoii-6-ene-9-carboxyUc acid 2^,2-trichloro-l,l-dimethyIethyI ester hydrochloride salt (ALU)
As for compound ALl but from bicyclononene AKll (about 0.55 nunol) in CH2Ci2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 1.28.
(rfla)-(iJi:*, 55*)-6-(Cydopropylphenethylca^bamoyl)-7-{4-[3-(2^,6-tI^fl^oro-phe^oxy)propyl]phenyl}-3,9-diazabicyclo[3J.lInon-6-ene-9-carboxylic acid 2,2,2-trichIoro-l,l-dimethylethyl ester hydrochloride salt (AH2)
As for compound ALl but from bicyclononene AK12 (about 0.55 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R, == I.IS; ES+: 778.30.
(/■flc.)-(7/f* 55'*)-6-{[2-(2-Chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifIuoropiienoxy)propyI]pheiiyl}-3,9-diazabicydo[3.3.1]non-6-ene-9-

carboxylic acid 2,2,2-trichloro-l,l-dimethyIetiiyl ester hydrochloride salt (AL13)
As for compound ALl but from bicyclononene AK13 (about 0.55 mmol) in CHiCh (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS; R, = 1.21.
(rflc.)-(^-'?*, 55*)-6-{CycIopropyl-[2-(2,3-dinuorophenyl)efhyIlcarbamoyl}-7-{4-[3-(2,3,6-triiluorophenox>')propyIIphenyl}-3,9-diazabicycIop.3.1Jnon-6-ene-9-carbosylic acid 2,2v2-trichIoro-l,l-dimethyIethyl ester (AL14)
As for compound ALl but from bicyclononene AK14 (about 0.55 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt =1.21.
{rac.)-{lR*, 55*)-6-{Cyclopropyl-[2-(4-nuoropheiiyI)ethyl]carbamoyl}-7-{4-[3-(23i6-trifluorophenox5')propyl}pfaenyl}-3,9-diazabicyclo [3.3.1 ]non-6-ene-9-carboxyUc acid 2,2,2-trichloro-l,l-diniethylethyl ester hydrochloride salt
(AL15)
As for compound ALl but from bicyclononene AK15 (about 0.55 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R^ = 1.18; ES+: 796.28.
(rac)-iJS% 5iS'*)-6-(CyclopropyI-{2-o-tolyiethyl)carbamoyI]-7-{4-[3- As for compound ALl but from bicyclononene AK16 (about 0.55 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R, =^ 1.21; ES+: 794.30.
{rac.)-(lR% 55*)-6-[Cyclopropyl-{3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trinuorophenoxy)propyllpheoyI}-3,9-diarabicyclo [3.3. lino Q-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-dimethyIethyl ester hydrochloride salt (AL17)

As for compound ALl but from bicyclononene AK17 (about 0.55 nunol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 1.16.
(_rac.)~(lR*, 55*)-6-[Cyclopropy|-(2-/?-tolyIethyI)carbamoyl]-7-{4-[3-(2^,6-tri-fluorophenoxy)propyI]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-9-carboxjiic acid 2,2^-trich!oro-l,l-dimethylethyl ester hydrochloride salt (AL18)
As for compound ALl but from bicyclononene AKI8 (about 0.55 mmol) in CH2CI2 (5 n^) and HCl/dioxane (4M, 5 mL). LC-MS: R, = 1.22; ES+-. 792.30.
(rac.)-{JR% 55*)-6-{CyclopropyI.[2-(2-hydroxyethyl)ben2yI]carbamoyl}~7-{4-[3-(23,6"trinuorophenoxy)propyl|phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid 2^,2-trichloro-l,l-dimethylethyl ester hydrochloride salt (AL19)
As for compound ALl but from bicyclononene AK19 (about 0.55 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R^= l.Ol.
(racy(lR% 55*)-7-{4-[3-(2-Bromo-5-fluoropbenoxy)propyllphenyl}-6-[(2-chloroben2yl)cyclopropylcarbamoyI]-3,9-diazabicyclo[33.1]non-6-ene-9-carboxylic acid 2^^-trichIoro-l,l-dimetfayletbyI ester hydrochloride salt (AL20)
As for compound ALl but from bicyclononene AK20 (about 0.55 mmol) in CH2CI3 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 5.26; ES+: 806.26.
(rac.y{lR*, 5S*)-6-(Beiizyleyclopropylcarbamoyl)-7-{4-l3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxyUc acid 2,2,2-trichioro-l,l-dimethylethyl ester hydrochloride salt (AL21)

As for compound ALl but from bicyclononene AK21 (519 mg, 0.54 mmol) in CH2C13 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R, = 1.06.
(racyilR", 55*)-7-{4-13-(2-Bromo-5-nuorophenoxy)propyIlphenyl}-6-l(2-chlorot>enzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.11non-6-ene-9-carboxylic acid 2,2,2-frichloro-l,J-dimethyIethyl ester hydrochloride salt (AL22)
As for compound ALl but from bicyclononene AK22 (about 0.8 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 5.30; ES+; 828.33.
{racyilR*, 5^*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl|phenyl}-6-[cycIo-propyI-(2-fluorobenzyI)carbamoyl|-3,9-dia2abicycIo[3.3.1jnon-6-ene-9-carbo-xylic acid 2^^2-trichIoro-l,l-dimethyIethyl esfer hydrochloride salt (AL23)
As for compound ALl but from bicyclononene AK23 (about 0.8 mmol) in CHiCIi (5 mL) and HCl/dioxane (4M, 5 mL).
{racWlR*, 55'*>-7-{4-(3-(2-Bromo-5-fluorophenoxy)propyllphenyI)-€-[cyclo-propyl-(3-trifiuororaethylbenzyl)carbanioyll-3,9-diazabicycIo[33.11nGo-6-ene-9-carboxylic acid 2^,2-tricfaloro-l,l-dimethylethyl ester hydrochloride salt (AL24)
As for compound ALl but from bicyclononene AK24 (about 0.8 mmol) in CH2CI2 (5 mL) and HCydioxane (4M, 5 mL). LC-MS; R, ^ 5.33; ES+: 820.40.
(racyilR*, 55*)-7-{4-[3-(2-Bronio-5-fluorophettory)propyl]phenyl}-6-[cyclo-propyl-(2-methylben2yi)carbamoyl]-3,9-dia2abicycio[3.3.1]non-6-ene-9-carboxylic acid 2,2,2-trichIoro-l,l-dimethyIethyf ester hydrochloride salt
(AL25)
As for compound ALl but from bicyclononene AK25 (about 0.8 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL), LC-MS: R, - 1.06.
{racHJR*, 5^*)-7-{4-I3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cycIo-propyl-[2-(4-methoxypfaenox>')ethyl]carbamoyI}-3,9-diazabicycIo[3.3.1]non-6-ene-9-carboxyIic acid 2,2,2-trichIoro-l,l-dimethylethyI ester hydrochloride salt (AL26)
As for compound ALl but from bicyclononene AK26 (about 0.8 nunol) in CHsCb (5 mL) and HCI/dioxane (4M, 5 mL). LC-MS: R, = 5.08; ES+: 866.40.
irac.)-{JR*, 5^*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclo-propyl-(2-m-tolyloxyethyl)carbamQyll-3,9-diazabicyclo[3J!.l]noii-^-ene-9-carboxylic acid 2,2,2-tricliloro-l,l-dimetliylethyI ester hydrochloride salt
(AL27)
As for compound ALl but from bicyclononene AK27 (about 0.8 mmol) in CH2CI2 (5 mL) and HCI/dioxane (4M, 5 mL). LC-MS: Rt = 1.07.
(rac.)-(lR*, J5*)-7-{4-(3-(2-Bromo-5-fluorophenoxy)propyllpheiiyl}-6-{cyclo-propyl-[2-(3,4-dimethy lphenory)ethyl] carbamoy i}-3,9-dia2abicy CIG[3.3. 1] -non-6-ene-9-carboxylic acid 2,2^-trichloro-l,l-dimethylefbyi ester hydrochloride salt (AL28)
As for compound ALl but from bicyclononene AK28 (about 0.8 mmol) in CH2CI2 (5 mL) and HCI/dioxane (4M, 5 mL). LC-MS: Rt = 1.08.
-(JR*, J5*)-7-{4-(3-(2-Broiiio-5-fluorophenoxy)propyl]pheoyl}-6-(cyclo-
propylphenethylcarbamoyl)-3,9-diazab!cyclof3.3.1]non-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-dimethylethyl ester hydrochloride salt (AL29)
As foT compound ALl but from bicyclononene AK29 (about 0.8 ramol) in CH2CI2 (5 mL) and HCI/dioxane (4M, 5 mL). LC-MS: R, - 5.25; ES+: 820.38.

(rac.)'iJR*, 55*)-7-{4-I3-(2-Bromo-5-fluorophedoxy)propyl]phenyI}-6-{[2-(2-chIorophenyi)ethyI]cyclopropylcarbamoyI}-3,9-dia2abicyclo[3.3.1]non-6-ene-9-carboxylic acid 2^,2--trichIoro-l,l-dimethyIefliyl ester hydrochloride salt (AIJO)
As for compound ALl but from bicyciononene AK30 (about 0.8 mmol) in CH2CI2 (5 niL) and HCI/dioxane (4M, 5 mL). LC-MS: R^= 5.35; ES+: 854.30.
(rac.y(JR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclo-p ropy l-[2-(2 3-d iflu orophenyl)ethy i] carbamoyl}-3,9-diazabicy do [3.3.1 ] n on-6-ene-9-carboxjlic acid 2^,2-trichloro-l,l-dimethylethyI ester hydrochloride salt (AL31)
As for compound ALl but from bicyciononene AK31 (about 0.8 mmol) in CH2CI2 (5 mL) and HCI/dioxane (4M, 5 mL). LC-MS: Rt = 5.40; ES+: 856.38.
(rac.)-(lJi*, 55*)-7-(4-[3-(2-Bromo-5-fluoropheooxy)propyl]phenyl}-6-{cyclo-propyI-[2-(4-fIuorophenyI)ethyl] carbamoyl}-3,9-diazabicycIo [3.3.1] non-6-ene-9-carboxyUc acid 2,2^-trichloro-l,l-dimethyIethyl ester hydrochloride salt (AL32)
As for compound ALl but from bicyciononene AK32 (about 0.8 mmol) in CHzCii (5 mL) and HCydioxane (4M, 5 mL). LC-MS: R, = 5.28; ES+; 838.40.
(racHJR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyIJphenyl}-6-Icyclo-propyl-(2-o-toIylethyI)carbam oyl] -3,9-diazabicy clo [3.3.1] non-6-ene-9-^:arbo-xyiic acid 2^,2-trichloro-l,l-dimethyIethyl ester hydrochloride salt (AL33)
As for compound ALl but from bicyciononene AK33 (about 0.8 inmo!) in CH2CI2 (5 mL) and HCI/dioxane (4M, 5 mL). LC-MS: R, = 5.36; ES+: 834.42.

l:l-IVIixture of (rac.)-{lR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propylI-phenyl}-6-[((2i;*)-2-hyd roxy-2-plienylethy I)methylcarfaamoy l]-3,9-d iaza-bicyclo[3.3.1Jnon-6-ene-9-carboxyIic acid 2,2,2-trichloro-l,l-dimefliylethyI ester hydrochloride salt and (rac.yilR*, 5^*)-7-{4-[3-{2-Bromo-5-fluoro-phenoxy )propyl] phenyl}-6-[((25*)-2-hy droxy-2-phenylethy l)methy i-carbamoyl]-3,9-diazabicyclol3.3.1]iion-6-ene-9-carboxylic acid 2,2,2-tri-chloro-1,1-dimethyIethyl ester hydrochloride salt (AL34)
As for compound ALl but from bicyclononenes AK34 (about 0.3 mmol) in CH2CI2 (5 niL) and HCl/dioxane (4M, 5 niL). LC-MS: R, = 0.99.
{rac)-(JR*, J5*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyI]phenyl)-6-[cyclo-propyl-(3,5-dimethoxybeazyI)carbamoyl)-3,9-diazabicycIo[3.3.11non-6-eiie-9-carboxylic acid 2,2,2-trichIoro-l,l-dimethylethyl ester hydrochloride salt
(AL35)
As for compound ALl but from bicyclononene AK35 (about 0.8 mmol) in CHzCli (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 5.23; ES+: 866.40.
(rac.)-(iJ?*, 5S*)-7-{4-I3-(2-Bromo-5-flaorophenoxy)propylJphenyl}-6-[cyclo-propyI-(2-^-tolylethyl)carbamoyl]-3^-dia2abicyclo[33.1]non-6-ene-9-carbo-^Iic acid 2^,2-tnchIoro-l,l-dimethylethyl ester hydrochloride salt (AL36)
As for compound ALl but from bicyclononene AK36 (about 0.8 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt= 5.59; ES+: 834.42.
{rac.)-{lR\ 5S*)-7-{4-[3-(2-Bronio-5-fiiiorophenoxy)propyIlphenyl}-6-tcydo-pro pyI-I2-(2-hyd roxy ethy Ob enzy I] carba moyl}-3,9-diazabicy cio [3.3.1] non-6-ene-9-carboxyIic acid 2,2,2-trichloro-l,l-dimethylethyl ester hydrochloride salt (AL37)

As for compound ALl but from bicyclononene AK37 (about 0.8 mmol) in CH2CI2 (5 mL) and HCi/dioxane (4M, 5 niL). LC-MS: Rt= 1.01.
(rac.)-(lR% J5*)-6-[(2-ChlorobettzyI)cycIopropylcarbaaioyl]-7-{4-(2-(2»3,6-trimefhyiphenoxy)ethyl]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-9-carboxy-lic acid 2,2,2-trichloro-l,l-diinethyIethyI ester hydrochloride salt (AL38)
As for compound ALl but from bicyclononene AK38 (312 mg, 0.35 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R, = 1.08; ES+: 774.33.
(rac.)-(lR*, 5iS'*)-6-(BenzylcyclopropyIcarbamoyI)-7-{4-[2-(2^,6-trimethyl-pheiioxy)ethyl]phenyI}-3,9-diazabicyclo[3.3.1JnGa-6-ene-9-carboxylic acid 2,2,2-trichIoro-l,l-dimethylethyl ester hydrochloride salt (AL39)
As for compound ALl but from bicyclononene AJ09 (340 mg, 0.40 mmol) in CH2CI2 (5 mL) and HCVdioxane (4M, 5 mL). LC-MS: R^- 1.05; ES+: 740.42.
{rac.)-{lR\ J^*)-6-I(2-ChIorobenzyl)ethy!carbamoyl]-7-{4-[2-(23,6-
trimethyl-phenoxy)ethyI] phenyl}-3,9-diazabicyclo [33,1 Jiion-6-ene-9-carboxylic acid 2,2^-trichloro-l,l-dimethylethyl ester hydrochloride salt
(AL40)
As for compotmd ALl but from bicyclononene AK40 (374 mg, 0.43 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R^ = 1.07; ES+: 762.34.
(racHlR*, 55*)-6-[Cyclopropyl-(2-fluorobenzyI)carbamoyl]-7-{4-(2-(2,3,6-trimethylphenosy)ethyllphenyl}-3,9-dia2abicyclo[33.1)non-6-ene-9-carboxy-lic acid 2,2,2-trichloro-l,l-dimethylethyl ester hydrochloride salt (AL41)
As for compound ALl but from bicyclononene AK41 (350 mg, 0.41 mmol) In CH2CI2 (5 mL) and HCl/dioxane (4M. 5 mL). LC-MS: Rt - 1.06; ES+: 758.38.

{rac.)-{lR*, 5iS'*)-6-[Cydopropyl-(3-trifluoromethylbenzyI)carbamoyI]-7-{4-{2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicy do [3.3.1 ]nQa-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-dimethyIethyl ester hydrochloride salt
(AL42)
As for compound ALl but from bicyclononene AK42 (294 mg, 0.32 mmol) in CHiCh (5 mL) andHCVdioxane (4M, 5 mL). LC-MS: R,= 1.08.
{rac.)-ilR% 55*)-6-(CycIopropyI'(2-raethyIbenzyI)carbamoyII-7-{4-[2-(2,3,6-trimethylplienoxy)etbyIlphenyl}-3,9-diazflbicyclo[3.3.11noa-6-ene-9-carboxy-lic acid 2,2,2-trichloro-l,l-dimethylethyI ester hydrochloride salt {AL43)
As for compound ALl but from bicyclononene AK43 (322 mg, 0.38 mmol) in CH2CI2 (5 mL) and HCl/diosane (4M, 5 mL). LC-MS: Rt = 1.08; ES+: 752.39.
(rac.)-(IR*, 55*)-6-{CycIopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyI}-7-{4-[2-(2»3)6-trimethyIphenoxy)ethylJphenyl}-3,9-diazabicyclo[33.1]non-6-ene-9-carboxyIic acid 2;2^-trichIoro-l,l-dimethyIethyI ester hydrochloride salt (AL44)
As for compoimd ALl but from bicyclononene AK44 (159 mg, 0.18 mmol) in CH2CI2 (5 mL) and HCVdioxane (4M. 5 mL). LC-MS; R, = 1.07.
(rac)-{lR*i 55*)-6-{CyclopropyI-[2-(3-methoxypheno3y)ethylIcarbamoyl}-7-{4-12-(23)6-triiiiethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxyIic acid 2^,2-trichloro-l,l-dimethyIethyl ester (AL45)
As for compound ALl but from bicyclononene AK45 (237 mg, 0.26 mmol) in CH2CI2 (5 mL) and HCi/dioxane (4M, 5 mL). LC-MS: R^ = 1.00.
(rac.)-(JR*, 55*)-6-(CycIopropyl-(2-m-tolyIoxyethyI)carbamoyl]-7-{4'[2-
(2^,6-trimethyIphenoxy)ethyl]phenyI}-3,9-diazabicyclo[3.3.1]noD-6-ene-9-

carboxy-lic acid 2,2,2-trichloro-l,l-dimethylethyI ester hydrochloride salt (AL46)
As for compound ALl but from bicyclononene AK46 (185 mg, 0.21 mmol) in i CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R, = 1.09; ES+: 784.40.
(rac,y(IR*, 55:*)-6-(Cyc!opropylpUcnethylcarbamoyi)-7-{4-{2-(2,3,6-
frimethyI-phenoxy)ethyl]phenyI}-3,9-diazabicycIoI3.3-I]non-6-ene-9-carboxylic acid 2,2^-tricbloro-l,l-dimethylethyJ ester hydrochloride salt (AL47)
As for compound ALl but from bicyclononene AK47 (about 0.3 mmo!) in CH2CI2 (5 mL) and HO/dioxane (4M, 5 mL). LC-MS: Rt = 1,09; ES+: 754.44.
(rtfc.)-(iif*, J5*)-6-{[2-(2-ChlorophenyOethylIcyclopropylcarbamoyl}-7-{4-[2-(2,3,6-triQiethylphenoxy)cthyI]phenyl}-3,9-diazabicycIo[3.3.1InoD-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-diinethyletfayi ester hydrochloride salt
(AL48)
As for compound ALl but from bicyclononene AK48 (about 0.3 namol) in CH2CI3 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 1.10; ES+: 788.41.
{rac.)-{lR*, 5S*V6-{CyclopropyH2-(23-difluorophenyl)ethyllcarbamoyl)-7-{4-(2-(23>6-trimethylphenoxy)ethyl]-pheiiyi}-3,9-diazabicyclot3.3.11noii-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-dimethylethyl ester hydrochloride salt (AL49)
As for compound ALl but from bicyclononene AK49 (about 0.3 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R,= 1.09; ES+: 788.41.
(rac.)-
carboxylic acid 2,2,2-trichIoro-l,l-dimethyIethyJ ester hydrochloride salt (ALSO)
As for compound AS.l but from bicyclononene AK50 (about 0.3 ramol) in CH2CI2 (5 mL) and HCiydioxane (4M, 5 mL). LC-MS: R, = 1.09; ES+: 772.41.
(racHlR*, 5^*)-6-[CyclopropyH2-o-tolylethyI)carbanioyII-7-{4-(2-(2,3,6-trimethylphenoxy)ethyl]plienyl}-3,9-diazabicycloI3.3.1Jnon-6-ene-9-carboxy-lic acid 2,2,2-trichIoro-l,l-dimethylethy! ester hydrochloride salt (AL51)
As for compound ALl but from bicyclononene AK51 (about 0.3 mmol) in CH2CI2 (5 mJL) and HCl/dioxane (4M, 5 mL). LC-MS: R, = LIO; ES+: 768.44.
l;l-Mixturc of {rac.).-{lR*, 5S*>6-l((25*)-2-hydroxy-2-pheny\etbyl)methyL carbamoyl]-7-{4-[2-(23,6-tri methyIphenoxy)ethyll phenyl}-3,9-diazabicy clo-[3.3.1]non-6-ene-9-carfaoxyIic acid 2,2,2-trichIoro-l,l-dimethyIethyl ester hydrochloride salt and (rac.)-(JR*, 55*)-6-[((25*)-2-hydroxy-2-phenyIethyl)-methyIcarbamoyI]-7-{4-I2-(23,6-trimethylphenoxy)ethyl]phenyI}-3,9-diaza-bicyclo[3.3.1]non-6-ene-9-carboxyUc acid 2,2,2-trichloro-l,i-dimethylethyI ester hydrochloride salt (AL52)
As for compound ALl but from bicyclononene AK52 (about 0.3 nmiol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC~MS: Rt = 1.02; ES+: 744.44.
(racy{lR*, 5S*)-6-lCyclopropyl-(3,5-dimethoiybeazyl)carbamoyll-7-{4-[2-(2^,6-triinethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid 2,2,2-trichIoro-l,l-dimethylethyl ester hydrochloride salt
(AL53)
As foi compound ALl but &om bicyclononene AK53 (about 0.3 ramol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R, = 1.07.

(rac.)-(^R*y •>'S'*)-6-[CyclopropyI-(2-p-toIyIethyl)carbamoyl]-7-{4-[2-(2,3,6-tri-methylphenox>')ethyl]phenyI}-3,9-diazabieydo{3.3.1]non-6-ene-9-carboxyIic acid 2,2,2-trichIoro-l,l-dimethy[ethyI ester hydrochloride salt (AL54)
As for compound ALl but &om bicyclononene AK54 (about 0.3 mmol) in CH2Cl2(5mL)andHCl/dioxane(4M, 5mL). LC-MS: R^= l.IO; ES+: 768.44.
(rac.)-(lR% 55*)-6-{Cyclopropyl-[2-(2-hydroxyethyI)benzylJcarbaraoyl}-7-{4-[2-(2,3,6-trimethylphenoxy)ethyi]pheiiy!}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-dimethyIethyI ester hydrochloride salt (AL55)
As for compound ALl but &om bicyclononene AK55 (about 0.3 mmol) in CH2CI2 (5 mL) and HCI/dioxane (4M, 5 mL). LC-MS: Rt = 1.03; ES+: 784.44.
(racHlR*, 5^*)-6-[(2-ChIorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-{2-
chloro-4,5-diinethylphenoxy)ethoxylpheDyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbox5'Iic acid 2,2,2-trichIoro-l,l-dimethylethyl ester hydrochloride salt (AL5&)
As for compound ALl but from bicyclononene AK56 (about 0.5 mmol) in CH2CI2 (5 mL) and HCI/dioxane (4M. 5 mL). LC-MS; Rt = 1.08; ES+: 785.26.
(rac.)-(lR% 55*)-6-[(2-Chlorobeiizyl)ethyIcarbamoyIl-7-{4-[2-(2-chloro-4^ dimethyIphenoxy)ethoxy]phenyl}-3,9-diazabicyclol3.3.1Jnon-6-ene-9-carbo-xyiic acid 2^^-trichIoro-l,I-dhnethyIethyl ester hydrochloride salt (AL57)
As for compound ALl but from bicyclononene AK57 (about 0.5 mmol) in CH2CI2 (5 mL) and HCI/dioxane (4M, 5 mL). LC-MS: R, = 1.06.
{rac.y(lR*, 55*)-7-{4-I2-(2-ChIoro-4,5-dimethylphenoxy)ethoxylphenyl}-6-{cycIopropy[-(2-fluorobeiizyI)carbamoy[I-3,9-diazabicyclo[3.3.1]non-6-ene-9-

carboxylic acid 2,2a-trichloro-l,l-dimethyIethyi ester hydrochloride salt
(AL58)
As for compound ALl but from bicyclononene AK58 (about 0.5 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R, = 1.06.
(rac.)-{IR% 5^*)-7-{4-(2-(2-Chloro-4,5-dimethylpheiioxy)ethoxylphenyl}-6-[cyclopropyl-(3-trifluoromethylbeiizyl)carhamoyf]-3,9-diiw;abicyclo[3.3.11-non-6-ene-9-carbosylJc acid 2,2,2-trichloro-l,l-dimethylethyl ester hydrochloride salt (AL59)
As for compound ALl but from bicyclononene AK59 (about 0.5 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R, = 1.08.
(racHJR*, 55'*)-7"{4-[2-(2-ChIoro-4,5-dimethyIphenoxy)ethoxylpfaenyi}-6-(cydopropyl-{2-methylbenzyl)carbamoyl]-3,9-diaKibicyclo[33,Ilnon-6-eue-9-carboxylic acid 2,2,2-tricfaloro-l,l-dimethyIethyl ester hydrochloride salt
(AL60)
As for compoimd ALl but from bicyclononene AK60 (about 0.5 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R, = 1.07; ES+: 788.40.
(rac)-(2R% 55*)-7-{4-p-(2-Chloro-4,5-dimethylphenoxy)ethoxylphenyI}-6-{cyclopropyl-[2-(4-methoiyphenoxy)ethyllcarbamoyl}-3^-diazabicycIo-l3.3.1]non-6-eiie-9-carboxylic acid 2,2,2-trichloro-l,l-dimethylethyl ester hydrochloride salt (AL61)
As for compound ALl but from bicyclononene AK61 (about 0.5 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 1 -06.
(rac.)-(lK% 55*)-7-{4-[2-(2-Chloro-4,5-dimefhyIphenoxy)ethoxy]phenyl)-6-{cy clopro py I- [2-(3-meth oxyph enoxy )ethy llcarbam oyl} -3,9-

)

diazabicyclo[3.3.1Jnon-6-ene-9-carboxyIic acid 2,2,2-trJchIoro-l,l-
dimethylethyl ester hydrochloride salt (AL62)
As for compound ALl but from bicyclononene AK62 (about 0-5 mmol) in CH2CI2 (5 mil and HCl/dioxane (4M, 5 mL). LC-MS: R, = 1.07.
(rac.)'(lR*, 55*)-7-{4-|2-(2-Chloi'o-4,5-dimethyIpheiioxy)ethox5iphenyl}-6-[cyc[opropyI-(2-m-tolylos:;'ethyl)carbamoyli-3,9-diazabicyclo(3,3.1]aon-6-ene-9-carbosyiic acid 2,2,2-trichloro-l,l-dimethyIethyl ester hydrochloride salt (AL63)
As for compound ALl but from bicyclononene AK63 (about 0.5 mmo!) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS; R, = 1.08.
(rac.)-(JR*, 55 *)-7-{4-[2-(2-ChIoro-4,5-dimefhylphenoxy)ethoxy]phenyl}-6-(cyclop ropylph enethy lea rbamoy I)-3,9-diazabicy do [3.3.1] non-6-en e-9-carbo-xylic acid 2,2,2-trichIoro-l,l-dimethyIethyI ester hydrochloride salt (AL64)
As for compound ALl but from bicyclononene AK64 (about 0.5 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 1-07; ES+: 788.39.
{rac.)-{lR*, 55*)-7-{4-[2-(2-ChIoro-4,5-dimethylphenoxy)ethoxylphenyl}-6-{[2-(2-cbloropheiiyl)ethyIlcyclopropylcarbamoyI)-3,9-diazabicyclo[3.3.1]non-6-€ne-9-carboiylic acid 2;2,2-trichloro-l,l-dimethylethyl ester hydrochloride salt (AL65)
As for compound ALl but from bicyclononene AK65 (about 0.5 mmol) in
CH2CI2 (5 mL) andHO/dioxane (4M, 5 mL). LC-MS; Rt = 1.08.
(rae.)-(i/?*, 55*)-7-{4-[2-(2-Chloro-4,5-dimethylpheQOxy)ethoxy]phenyl}-6-{cyclopropyI-[2-(2,3-difluorophenyl)ethyl]carbamoyI}-3,9-diazabicycIo-

l3.3.1]non-6-ene-9-carboiylic acid 2,2,2-trichloro44-dimethylethyl ester hydrochloride salt (AL66)
As for compound ALl but from bicyclononene AK66 (about 0.5 mmo!) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 1.06.
(irac.)-(llt% 55*>-7-{4-[2-(2-ChIoro-4,5-dimethylphenoxy)ethoxy]pheny!}-6-(cyclopropyl-[2-(4-fluoroph enyl)ethyl] carbamoyl}-3,9-diaza bicy do {3.3.1 ]non-6-ene-9-carboxylic acid 2^,2-trichlorQ-l,l-dimethylethyl ester hydrochloride salt (AL67)
As for compound ALl but from bicyclononene AK67 (about 0.5 mmol) in CH2CI2 (5 mL) and HCI/dioxane (4M, 5 mL). LC-MS: R, = 1.06.
{rac)-{lR*, 55*)-7-{4-l2-(2-Chloro-4,5-dimethylpfaeooxy)ethoxy]phenyi}-6-jcyclopropyl-(2-tf-tolylethyl)carbamoyI]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid 2^^-trichloro-l,l-dimethylethyI ester (AL68)
As for compound ALl but from bicyclononene AK68 (about 0-5 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Ri ^ 1.08.
l:l-Mixtore of irac.)-{lR% 55*)-7-{4-I2-(2-cUoro-4^-dimethylpheiioxy)-
ethoxy]phenyl}-6-[((2if*)2-hydroiy-2-phenylethyl)methylcarbamoylJ-3,9-
diazabicycIo[3.3.1)non-6-ene-9-carboiyUc acid 2^^-trichioro-l,l-dimefhyl-
etbyl ester hydrochloride salt and (rac.)-(JR*, 55*)-7-{4-[2-(2-chIoro-4,5-
dimethylphenoxy)etboxy]phenyl}-6-(((25*)2-bydroxy-2-phenyletfayl)inethyl-
carbamoylJ-3,9-diazabicyclo (3.3.1] non-6-ene-9-carboxylic acid 2,2,2-
trichloro-l,l-dimethylethyl ester hydrochloride salt (AL69)
As for compound ALl but from bicyclononene AK69 (about 0.5 ramo!) in CHiCb (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Ri= 0.99; ES+: 780.37.

(raa)-(JJi*, i5'*)-7-(4-(2-(2-ChIoro-4,5-dimethyIphenox5')ethoxyjpheiiyIi-6-[cyc!opropyI-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabkyclDl3.3,l]non-6-ene-9-carboxjIic acid 2,2,2-trichloro-l,l-dimethylethyl ester hydrochloride salt (AL70)
As for compound ALl but from bicyclononene AK70 (about 0.5 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R, = 1.06.
(rac.)-ilS^, J5*)-7-{4-I2-(2-Chloro-4,5-diniethyiphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-/»-tolyIetliyI)carbamoyI]-3,9-dia2abicycIo[3J.l]non-6-enc-9-carboxylic acid 2^^-trichIoro-l,l-dimethylethyI ester hydrochloride salt
(AL71)
As for compound ALl but from bicyclononene AK71 (about 0.5 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt= 1.08.
irac)-(JJt*, 55*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropy I-(2-(2-hydroxy ethyl) benzyll carbamoyl}-3,9-diazabicyclo [3.3.1]-non-6-ene-9-carfaoxyIic acid 2»2,2-trichioro-l,l-dimetfaylethyl ester hydrochloride salt
As for compound ALl but &om bicyclononene AK72 (about 0.5 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 1.01.
{racJ)-{IR*, 5.y*)-7-{4-[2-(4-Broniopheaoxy)ethoxyIpheayl}-6-[(2-chIoro-
ben2yl)cyclopropylcarbamoyl]-3^-diazabicyclo [3.3.1)non-6-eD e-9-carboxy lie acid 2,2,2-trichloro-l,l-dimethyl-ethyl ester hydrochloride salt (AL73)
As foT compound ALl but fi:om bicyclononene AK73 (0.28 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 4.98; ES+: 824.32.

irac.)-(}R*, 5^*)-6-(Ben2yIcyciopropylcarbamoyI)-7-{4-f2-(4-bromophenoxy)-ethoxy]phenyi}-3,9-diazabicyclo [3.3.1 J noii-6-ene-9-car boxy lie acid 2,2,2-trichloro-l,l-dimethyIefhyl esfer hydrochloride salt (AL74)
As for compound ALl but from bicyclononene AK74 (D.27 mmol) in CH2CI2 (5 mL) and HCVdioxane (4M, 5 mL). LC-MS: Rt = 1.03; ES+; 792.36.
(rac.HJR*, 55'*)-7-{4-[2-(4-Bromophenoxy)ethoxylphenyI}'6-[(2-chIoro-
beB2yl)ethyIcarbamoyl}-3,9-diazabicyclo{33.11non-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-dimethylethyl ester hydrochloride salt (Al,75)
As for compound ALl but from bicyclononene AK75 (0.22 mmol) in CH2CI2 (5 mL) andHCl/dioxane(4M, 5 mL). LC-MS: R, = 4.92; ES+: 812.35.
{rac.)-{}R*, 5S*)-7-{4-12-(4-Bromophenoxy)ethoxy]phenyl}-^-leyeJopropyH2-fluorobeazyl)carbamoyI]-3,9-dia2abicycIoi3J.l]non-6-ene-9-carboiylic acid 2,2,2-trichloro-l,l-dimethyIethyl ester hydrochloride salt (AL76)
As for compound ALl but from bicyclononene AK76 (0.26 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: Rt = 4.78; ES+: 808.40.
(rfla)-(7if*, 5>S*)-7-{4-[2-(4-Bromophcnoxy)ethosy]phenyI}-6-IcyclopropyI-(3-trifIuoromethyIbenzyI)carbamoyI]-3,9-dlazabicyclo[33.1]non-6-ene-9-carbo-xylic acid 2,2,2-trichloro-l,l~diniethylethyl ester hydrochloride salt (AL77)
As for compound AH but from bicyclononene AK77 (0.29 nmiol) in CH2Ci2 (5 mL) and HO/dioxane (4M, 5 mL). LC-MS: R, = 4.97; ES+: 858.42.
{rac.)'(lR% 55'*)-7-{4-I2-(4-Bromophenoxy)ethoxyiphenyI}-6-[cyclopropyl-(2-methylben2yl)carbamoyIl-3,9-diazabicyclo[33.1Inon-6-ene-9-carboxyUc acid 2,2,2-tricbloro-l,l-dimethylethyl ester hydrochloride salt (AL78)

As for compound ALl but from bicyclononene AK78 (0.28 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: 11,= 5.Q1; ES+: 804.42.
(rflc.)-(iif*, 55*)-7-S4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-I2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxj'Iic acid 2,2,2-trichloro-l,l-dimethylethyl ester hydrochloride salt (AL79)
As for compoiind ALl but from bicyclononene AK79 (0.2 ramol) in CH2CI2 (5 mL) and HCI/dioxane (4M, 5 mL). LC-MS: R, - 5.03; ES+: 850.44.
(rac)-(/if*, 5S*)-7-{4-[2-(4-BromopheaQxy)ethoxylphenyl}-€-{cyclQpropyl-[2-(3,4-dimethylphenoxy)ethyllcarbainoyl}-3,9-dJazabicycIol3J3.11non-6-eiie-9-carboxylic acid 2,2,2-tricbloro-l,l-dimethyiethyl ester hydrochloride salt As for compound ALl but from bicyclononene AKSO (0.21 mmol) in CH2CI2 (5 mL) and HCi/dioxane (4M, 5 mL). LC-MS: R, = 5.11; ES+: 848.43.
(racHJR*, 55*>7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{[2-(2-chloro-phenyl) ethy II cyclo pro pyIcarbamoyl}-3,9-diazabicycIo (3.3.1 Inon-6-ene-9-carboxyllc acid 2.^^-trichloro-l,l-dimethylethyl ester hydrochloride salt (AL81)
As for compound ALl but from bicyclononene AK81 (0.27 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: B* = 5.09; ES+: 838.36.
(/■flc.)-(ii;*, 55*)-7-^4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluo^ophenyI)ethyI]carbamoyl}-3,9-diazabicyclo(3.3.1]non-6-ene-9-carboxyUc acid 2,2,2-trichloro-l,l-dimethy!ethyl ester hydrochloride salt
(AL82)
X

As for compound ALl but from bicyclononene AK82 (0.26 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R, = 4.44; ES+-. 840.42.
(/•flc)-(7J?* 55*)-7-{4-[2-(4-Bromophenox3')efhoxyIphenyl}-6-{cyclopropyI-12-(4-fluorophenyI)ethyI] carbarn oyl}-3,9-diazabicyclo[3.3. l]non-6-ene-9-carbo-xylic acid 2,2,2-tnchloro-l,l-diinethyl£thyl ester hydrochloride salt (AL83)
As for compound ALl but from bicyclononene AK83 (0.24 mmol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R^ = 4.89; ES+: 822.39.
(rac)-{lR*, 55*)-7-{4-[2-(4-Bromopheaosy)ethoxylphe0yl)-6-lcyciopropyl-(2-o-tolylethyl)carbamoyI]-3,9-diazabicyclo[3.3.1]noD-6-ene-9-carboxylic acid 2,2^-trichIoro-l,l-dimethyIethyI ester hydrochloride salt (AL84)
As for compound ALl but from bicyclononene AK84 (0.27 nunol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL).
(rac.)~(JR*, 55'*)-7-{4-[2-(4-Bromophenoxy)ethoxy]pheQyl}-6-[cycIopropyl-(3,5-dimethoxybeiizyl)carbainoyl]-3,9-diazabicycloP3.11iion-6-ene-9-carboxylic acid 2^^-trichIoro-l,l-dimethylethyI ester hydrochloride salt (AL85)
As for compound ALl but from bicyclononene AK85 (0.25 mmol) in CH2CI2 (5 mL) and HCydioxane (4M. 5 mL). LC-MS: R^= 4.76; ES+: 850.40.
irac)-(JR*, 55*)-7-{4-{2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyi-(2-j3-toIylefhyl)carbamoylJ-3,9-diazabicyclo[33.1]non-6-ene-9-carboxylic acid 2,2,2-trichloro-l,l-dimethyIethy! ester hydrochloride salt (AL86)
As for compound ALl but from bicyclononene AK86 (0.27 nunol) in CH3CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R,= 4.99; ES+: 820.78.

(/■(ic.)-(-/-ff*, 55*)-7-{4-[2-(4-Bromophenoxy)ethoxyJphenylJ-6-(cyclopropyJ-[2-(2-hydroxyethyl)benzy]IcarbamoyI}-3,9-diazabicycIo[3.3.1Inoa-6-ene-9-carboxylic acid 2^^-tricIi(oro-l,l-diinethylethyl ester hydrochloride salt (AL87)
As for compound ALl but from bicyclononene AK87 (0.18 ramol) in CH2CI2 (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R,= 4.58; ES+-. 834.43.
(rac)-(lR*, J5*)-7-Hydrosy-9-methyI-3,9-diazabicycIo[3.3,l]non-6-ene-3,6-dicarboxylie acid 6-henzyi ester 3-/ert-butyl ester (AM)
Ti(0Et)4 (2.92 mL, 13.9 mmol) was added to a sol. of bicyclononane A (13.0 g, 39.8 mmol) in benzyl alcohol (90 mL). The mixture was heated to 125 °C and itirred at this temperature for 28 h. The mixture was allowed to cool to rt and aq. 10% HCl (180 mL) was added. The mixture was extracted with Et^O (3x). The ■.ombined org. extracts were washed with aq. NaHC03 (2ii), with brine (Ix). The ng. extracts were then dried over MgS04, filtered, and the solvents were removed irst under reduced pressure, then under high vacuum. Purification of the residue y FC (EtOAc/heptane 1:1 -> 3:1 -> EtOAc) yielded the title compound (9.90 g, 4%). LC-MS: Rt= 1.39; ES+: 389.25.
■ac)'(lR*, 55*)-9-Methyl-7-trifluoromefhanesuIfonyIoxy-3,9-dlazabicyclo-!.3.1]iion-6-«ne-3,6-dicarboxylic acid 6-benzyI ester 3-/ert-butyI ester (AN)
aH (55% m oil, 2.20 g, 50.5 mmol) was added to a sol. of bicyclononane AM 5.69 g, 40.4 mmol) in THF (290 mL) at 0°C. After 15 min. TfaNPh (19.2 g, i .7 mmol) was added and the mixture was stirred overnight while warming up to [ce was added and the mixture was diluted with EtOAc, and washed with aq. )% NasCOs. The org. extracts were dried over MgS04, filtered, and the solvents 2re removed imder reduced pressure. Purification of the residue by FC tOAc/heptane 1:1 -> 3:1) yielded the title compound (17.1 g, 81%). Rf = 15 (EtOAc/heptane 1:1). LC-MS: Rt= 5.62; ES+: 521.37.

Compounds of type AO
(rac.)-(JR% 55*)-7-{4-[3-(/£//-ButyldimethylsiIanyloxy)propyllphe!iyl}-9-
methyI-3,9-diazabicycIo[3.3.1]non-6-ene-3,6-dicarboxylic acid 6-beazyl ester 3'tert-butyl ester (AOl)
BuLi (1.5M in hexane, 3.81 mL, 5.71 mmol) was added to a sol. of p-(4-bromophenyJ)propoxy]-/ert-butyldimethylsilane (Kiesewetter D. 0., Tetrahedron Asymmetry, 1993, 4, 2183, 1.88 g, 5.71 mmol) m THF (33 mL) at ~78 °C. After 30 min ZnCb (IM in THF, 6.97 mL, 6.97 mmol, prepared as described for compoxmd Gl) was added and the mixture was allowed to warm up to rt. Bicyclononene AN (1.65 g, 3.17 mmol) and Pd(PPh3)4 (92 mg, 0.080 mmol) were added. The mixture was heated to 40 °C and stirred at this temperature for 30 min. The mixture was allowed to cool to rt and aq. IM HCI (1 mL) was added. The mixture was diluted with EtOAc and washed with aq. IM NaOH (Ix). The org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (MeOH/CHiCli 1:49 -> 3:97 ^ 2:48 ->■ 5:95) yielded the title compound (L78 g, 90%). LC-MS; Rt = 5.55; ES+: 681.30.
(rac)-(JR*, 55*)-9-MethyI-7-{4-12-(23,5-trimethyIphenosy)ethyI]phenyI}-3,9-dia2abicyclo[3.3.1Jnon-6-ene-3,6-dicarboxylic acid 6-beiizyl ester 2-tert-huty\ ester (A02)
BuLi (I.6M in hexane, 19.40 mL, 31.0 mmol) was added to a sol. of compoxmd C2 (9.90 g, 31.0 mmol) in THF (100 mL) at -78 °C. Aiter 30 min ZnCh (0.83M in THF, 43.8 mL, 37.2 mmol, prepared as described for compound Gl) was added and the mixture was allowed to warm up to rt. Bicyclononene AN (9.90 g, 19.0 mraol) and Pd(PPh3)4 (550 mg, 0.475 mmol) were added. The mixture was heated to reflux for 1 h. The niixture was allowed to cool to rt and aq. IM HCI (1 mL) wag added. The mixture was diluted with EtOAc and washed with aq. IM NaOH

(Ix). The org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (MeOHyCH.Cls 1:49 ^ 3:97 -> 2:48 -> 5:95) yielded the title compound (6.20 g, 54%). LC-MS:R,-5.I0;ES+; 611.59.
Compounds of type AP
irac)-{lR*, 5,y*)-7-{4-(3-(/ert-BufyIdimethyIsiIanylox5')propyllphenyl}-3,9-diazahicycIo(3.3.11non-6-eQe-3,6,9-tricarboxyUc acid 6-benzyl ester 3-fert-butyl ester 9-(2,2,2-trichloro-l,l-dimethyIethyl) ester (API)
A sol. of bicyclononene AOl (1.78 g, 2.87 mmol) and 2,2,2-trichloro-re/-/-butyl chloroformate (3.44 g, 14.4 mmo!) in CH2CICH2C! (35 mL) was heated to reflux for 2 h. The mixture was allowed to cool to rt and the solvents vi'ere removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:8 -^ 1:1) yielded the title compound (1.88 g, 81%). LC-MS: Rt= 8.34.
(rac)-(lR*, 55*)-7-{4-(2-(2,3,5-Triniefhylphenoxy)ethyllphenyl}-3,9-dia2a-bicycIo[3.3.1]non-6-ene-3,6,9-tricarboxyIic acid 6-beii2yl ester 3-tert-bntyl ester 9-(2^,2-trichIoro-l,l-dimethyIethyl) ester (AP2)
As for compound API but from bicyclononene A02 (22.4 g, 36.7 mmol) and 2,2,2-trichloro-ferf-butyl chloroformate (44 g, 184 mmol) in CH2CICH2CI (400 mL). Purification of the residue by FC (EtOAc/heptane 1:8 -^ 1:1) yielded the title compound (19.2 g, 65%). LC-MS: R, = 7.95.
[rac.)-{}R*y 55 *)-3-Acetyl-7-[4-(3-hydroxy propy I)phenyll-3,9-diaiabicyclo-r3.3.1]non-6-ene-6,9-dicarboxyIic acid 6-benzyl ester 9-(2,2,2-trichloro-l,l-iimethyl ethyl) ester (AQ)

HCl/dioxane (4M, 20 mL) was added to a sol. of bicyclononene API (1.88 g, 2.32 mmol) in CH2CI2 (20 mL) was cooled to 0 °C. The ice bath was removed and the mixture was stkred for 3 h at rt. The solvents were removed under reduced pressure and the residue was dried under high vacuum. This residue was then dissolved in THF (30 mL) and the sol. was cooled to -78 "C. DMAP (cat. amount), DIPEA (1.60 mL, 9.28 mmol) and AcCl (0.165 mL, 2.32 mmol) were added. The mixture was stirred for 15 min at -78 °C and MeOH(10 mL) was added. The mixture was allowed to warm up to rt, was dissolved in EtOAc and washed with aq. IM HCl (Ix) and aq. sat. NaHCOj (Ix). The org. Extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1...4 -> 1:1 -> EtOAc -> MeOH/EtOAc 1:9) yielded the title compound (936 mg, 63%). LC-MS: R, = 5.47; ES+: 637.06.
Compounds of type AR
[racO-(i-R%55*)-3-Acetyl-7-{4-I3-(23,6-trinuorophenoxy)propyi]phenyI}-3,9-iiazabicyclo 13.3.1] no n-6-ene-6,9-dicarboxylie acid 6-benzyl ester 9-(2,2^-trichIoro-l,l-dimethyIethyI) ester (ARl)
K mixture of bicyclononene AQ (468 mg, 0.73 mmol), 2,3,6-trifIuorophenol (216 ng, 1.46 mmol), azodicarboxylic dipiperidide (277 mg, 1.10 mmol) and tributyl ihosphine (0.541 mL, 2.19 mmol) in toluene (I5 mL) was heated to reflux for 20 1. The mixture was allowed to cool to rt and the solvents were removed imder educed pressure. Purification of the residue by FC (EtOAc/heptane 1:49 -> 1:19 -s- 1:9) yielded the title compound (297 mg, 53%). LC-MS: R, = 6.87; ES+: 67.04.
'acy{lR*, 5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluoropheaoxy)propyllphenyl}-,9-diazabicycIo[3.3.11non-4-ene-6,9-dicarboxylic acid 6-benzyl ester 9-(2>2,2-ichloro-l,l-dimethylethyl) ester (AR2>

As for the bicyclononene ARl, but from bicyclononene AQI (468 mg, 0.73 mmol), 2-bromo-5-fluorophenoi (0.163 mL, 1.46 mmol), azodicarboxylic dipiperidide (277 mg, 1,10 mmoi) and tributyl phosphine (0.541 mL, 2.19 mmol) in toluene (15 mL). Purification of the residue by FC (EtOAc/heptane 1:49 -> 1:19 ->■ 1:9) yielded the title compound (205 mg, 35%). LC-MS: Rt - 7.06.
(rflC.)-(iif%55*)-3-Aeetyl-6-[(2-aUylbenryl)cyclopropylcarbamoylI-7-(4-[3-(2-b romo-5-fluo rop henosy)pro py 1] p henyl}-3,9-diazab icyclo [3.3.1 ]nou-6-eBe-9-carboxylic acid 2^,2-trichloro-l,l-dimethylethyl ester (AS)
A mixture of bicyclononene AJ4 (225 mg, 0.300 mmol), (2-alIylbeQzyl)-cyclopropylamine (168 mg, 0.900 mmol), DIPEA (0.300 mL, 1.80 mmol), DMAP (10 rag, 0.082 mmoi), HOBt (41 mg, 0.300 mmol) and EDC.HCl (86 mg, 0.450 mmol) in CH2CI2 (3 mL) v,ias stined foi 2 days. EDCHCl (29 mg, 0.150 mmol) was added again after 24 h and 30 b. The mixture was diluted with CH2CI2 and washed with aq. IM HCi (Ix). The org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressme. Purification of the residue by FC (EtOAc/heptane 1:4 -?■ 3:7 -^ 2:3 ^ 1:1 -> 3:2 -^ 7:3 -> 4:1) yielded the title compound (185 mg, 67%). Rf= 0.63 (EtOAc). LC-MS: Rt = 7.40,
Ill-Mixture of (rac.)-(JJR*, 55*)-3-acetyl-7-{4-I3-(2-bromo-5-fluorophenoxy)-propyIlphenyl}-6-{cycIopropyl-(2-((2i?*)-23-dihydroxypropyi)faen2yIl-carbainoyI}-3,9-diazab icy clo [33.1] non-6-ene-9-carboxylic acid 2^^-trichloro-l,l-dimefhyIethyl ester and (rac)-(lR*, 55*)-3-acetyl-7-{4-[3-(2-
bromo-5-nuorophenoxy)propylIphenyl}-6-{cycIopropyI-l2-((25*)-23-dihydroxypropyl)bea2yl]carbamoyl}-3,9-diaza bicycio [3,3.1] non-6-ene-9-
carboxylic acid 2,2,2-trichIoro-l,l-dimethylethyI ester (AT)
A mixture of bicyclononene AS (281 mg, 0.316 mmol), NMO-H^O (44.8 mg, 0.332 mmol), and OsO* (2.5% in lerJ-BuOH, 0.0396 mL, 0.00316 mmol) in THF (4 mL), tert-BnOH (2 niL) and water (1 mL) was stirred overnight. NM0-H20 (10 rag, 0.074 mmol) and OSO4 (0.010 raL, 0.008 mmon were added 3oai.i «n
the mixture was stirred again for 3 b. The solvents were removed under reduced pressure, and the residue was diluted with EtOAc, washed with aq. IM HCl (Ix), and with aq. sat. NaHC03 (Ix). The org. extracts were dried over MgS04, fdtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:4 -^ 2:3 -> 3:2 -^ 4:1 ~> EtOAc -> MeOH/EtOAc 1:9) yielded the title compounds (207 mg, 71%). Rf = 0.20 (EtOAc). LC-MS:R4= 6.23; ES+: 922.59.
(rac.)-(lR*, 55*)-3-Acety 1-7-{4-[3-(2-bromo-5-fiuorophenoxy)propyIlphenyl}-6~(cyclopropyI-[2-(2-oxoethyl)benzyllcarbamoyl}-3,9-diazabicydo[3.3.1]noo-6-ene-9-carboxyiic acid 2,2,2-trichloro-l,l-dimethylethyl ester (AU)
A mixture of bicyclononenes AT (167 mg, 0.181 mmol) and NalO^ (40 mg, 0.187 mmol) in THF (3 mL) and water (1 mL) was stirred at rt for 1 h. NaJ04 (20 mg, 0.01 mmol) was added again and the mixture was stirred for 3 h. The mixture was diluted wdth EtOAc and washed with aq. sat. NaHCOs (IK). The org. extracts were dried over MgS04, fiUered, and the solvents were removed under reduced pressure. The residue was dried under high vacuum and the title compound (156 mg, 97%) was used without further purification. LC-MS: Rt = 6.87; ES+: 891.78.
irac)-{JR*, 55'*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyIlphenyI}-
6-{cycloprQpyl-{2-(2-hydroiyethyI)benzyllcarbanioyl}-3,9-
diazabicycVol33.1]-non-6-ene-9-earboxylic acid 2^»2-trichloro-l,l-
dimetbylethyl ester (AV)
A mixture of bicyclononene AU (44.6 mg, 0.05 mmol) and NaBIli (about 2 mg, about 0.05 mmol) in MeOH (1 mL) was stirred at rt for 90 min. The mixture was diluted with EtOAc and washed with aq. IM HCl (Ix). The org. extracts were Iried over MgSOi, filtered and the solvents were removed under reduced pressure. The residue was used without further purification.
I^ompounds of type AW

{rac.)'(lR*, 55'*)-7-[4-(3-Hydroxypropyl)phenyI]-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylic acid 3-tert-buty\ ester 6-ethyI ester 9-(2,2,2-trichloro-l,l-diiiiethylethyI) ester (AWl)
TBAF (28.8 g, 91.4 mmol) was added to a sol. of bicyclononene H3 (45.6 g, 60.9 imnol) in THF (900 mL) at 0 °C. After 20 min, the ice bath was removed. After stirring the mixture at rt for 5 h, it was diluted with EtOAc and washed with water (2x), The org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:4-> 1:1) yielded the title compound (27.6 g, 72%). Rf=0.22 (EtOAc/heptane I; 1). LC-MS: R, ^ 6. U; ES+: 655.23.
{rac.)-{JR*, J5*)-7-[4-(2-Hydroxyethoxy)phenyI]-3,9-diazabicycIo[33.1]non-6-ene-3,6,9-tricarboxylic acid 3-/er^butyl ester 6-ethy! ester 9-(2,2^-(richloro-l,l-dimethylethyl) ester {A'W2)
As for compomid AWl but fi-om bicyclononene H7 (44.4 g, 59.2 nmiol) TBAF (28.0 g, 88.9 imnol) and THF (600 mL). Purification by FC (EtOAc/heptane 1:3 -> 1:1 -> EtOAc) yielded the title compound (23.67 g, 63%). R^ = 0.20 (EtOAc/heptane 1:1). LC-MS: R, = 6.02; ES+; 635.36.
Compounds of type AX
{racy{lR*y 55*)-7-{4-p-(23,6-Trifluorophenoxy)propyllphenyli-3,9-diaza-bicycloI3.3.1]non-6-ene-3,6,9"tricarboxyIic acid 3-tert~huty\ ester 6-ethyl ester 9-(2,2,2-trichloro-l,l-dimethyIethyl) ester (AXl)
A mixture of bicyclononene AWl (20.22 g, 32.0 mmol), 2,3,6-trifluorophenoI (9.50 g, 64.0 mmol), azodicaiboxylic dipiperidide (16.15 g, 64.0 mmol) and ttibutyl phospbine (85%, 27.9 mL, 96-0 mmol) in toluene (800 ml) was heated to reflux for 2 h. The mixture was allowed to cool to rt and the solvent removed

under reduced pressure. Purification of the residue was purified by FC (EtOAc/heptane l:J9-> 1:9-^ 1:4) yielded the title compound (21.7 g, 89%). Rf = 0.60 (EtOAc/heptane 1:1). LC-MS: R, - 1.25; ES+: 765,22.
{rac.y(lR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyllphenyI}-3,9-
diaza-bicyclo(3.3.1]non-6-eoe-3,6,9-tricarboxylic acid 3-(^r/-butyl ester 6-ethyl ester 9-(2,2,2-trichloro-l,l-dimethylethyl) ester (AX2)
As for AXl, but from bicyclononene AWl (27.63 g, 43.6 mmol), 2-bromo-5-fluorophenol (9.70 mL, 87.2 mmol), azodicarboxylic dipiperidide (22.0 g, 87.2 mmol), tributyl phosphine (32.2 mL, 13! mmol), and toluene (550 ml). Purification of the residue by FC (EtOAc/heptane 1:19 -> 1:9 -^ 1:4) jaelded the title compound (31.67 g, 90%). Rf = 0.60 (EtOAc/heptane 1:1). LC-MS: R, = 7.63.
{rac.)-{lR*, 5S*)-7-(4-l2-(2-Chloro-4,5-dimethyVphenoxy)ethoxylphenyl}-3,9-diazabicydo (3.3,1 ]non-6-ene-3,6,9-tricarboxylic acid 3-/ert-butyl ester 6-ethyl ester 9-(2^,2-trichIoro-l,l-dimethyIethyl) ester (AX3)
As for AXl, but from bicyclononene AW2 (11.83 g, 18.6 mmol), 2-chloro-4,5~ dimethylphenol (5.83 mL, 37.2 mmol), azodicarboxylic dipiperidide (9.39 g, 37.2 mmol), tributyl phosphine (85%, 16.2 mL, 55.8 mmol), and toluene (300 ml). Purification of the residue by EC (EtOAc/heptane 1:19 -> 1:9 -^ 1.3 -> 1:1) yielded the title compomid (13.35 g, 93%). Rf= 0,50 (EtOAc/heptane 1:1). LC-MS: Rt= 7.60.
irac)-{lR*, 55*)-7-{4-[2-(4-Bromophenoxy)ethoxyiphenyl}-3,9-diazabicyclo-[3.3.I]non-6-eDe-6,9-dicarboxyIic acid 6-etfayl ester 9-(2,2,2-trichIoro-l,l-dimethylethyl) ester (AX4)
As for AXl, but from bicyclononene AW2 (11.83 g, 18.6 mmol), 4-bromophenoI (6.43 mL, 37.2 mmol), azodicarboxylic dipiperidide (9.39 g, 37.2 mmol), tributyl

phosphine (85%, 16.2 ml, 55.8 nmol), and toluene (300 ml). Purification of the residue by FC (EtOAc/heptane 1:19 -> 1:9 -> 1:3 -> 1:1) yielded the title compound (13.6 g, 92%). Rf= 0.50 (EtOAc/heptane 1:1). LC-MS: R, = 7.49.
Compounds of type AY
{rac.y{lR*, 55*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyllphenyl}-3,9-diaza-bicydo[3J.l]non-6-ene-3,6,9-tricarboxylic acid 3-tert-butyI ester 9-(2,2,2-trichloro-l,l-dimethyIethyI) ester (AYl)
A mixture of bicyclononene AXl (15.76 g, 20.7 mmol) in EtOH (600 mL) and aq. IM NaOH (600 mL) was stirred for 7 h at 80 °C. The mixture was allowed to cool to rt and the solvents were partially removed under reduced pressure. The residue was diluted with EtOAc and aq. IM HCl was added to pH 1 - 2. The phases were shaken, separated and the aq. phase was extracted with EtOAc (2x)-The combined org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:4 -> 1:2 -^ 1:1) yielded the title compound (12.15 g, 80%). LC-MS: Rt= 1.16; ES+: 737.21.
irac.)-{lR*, 5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propylIphenyl}-3,9-
diaza-bicyclo[33.1]non-6-ene-3,6,9-tricflrboxylic acid 3-te/t-buiyl ester 9-(2^;2-trichloro-l,l-dinietbyIethyl) ester (AY2)
As for compound AYl, but from bicyclouonene AX2 (29.67 g, 36-8 mmol), EtOH (700 mL) and aq. IM NaOH (700 mL). Purification by FC (EtOAc/heptane 1:1 -^ EtOAc ^ MeOH/EtOAc 1:9) yielded the title compound 26.67 g (94%). LC-MS: R, - 6.89; ES+: 749.92.
(rac.)-(lR*, 5,y*)-7-{4-[2-(2^,5-Trimethylpbenoxy)ethyl]phenyl}-3,9-diaza-bicycio [3.3,1 ]non-6-ene-3,6,9-tncarboxylie acid 3-^^/-/-butyl ester 9-(2,2,2-trlchloro-l,l-dim^ethylethyI) ester (AY3)

Under N2 Pd/C (10%, 1.92 g) was added to a sol. of bicyclononene AP2 (19.2 g, 24.0 mmol) in MeOH (390 inL) cooled to 0 "^C. The mixture was purged with H2 (4x) and stirred at 0 °C under Hi for 7 h. The mixture was filtered through Celite, diluted with EtOAc and washed with aq. IM HCl (Ix). The org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification by FC (EtOAc/heptane 1:3 -^ 1:1 -> EtOAc -> MeOH/EtOAc 1:9) yielded the title coitipound (4.26 g, 25%). LC-MS: Rt= 7.10.
{rac.)-ilR*, 55*)-7-{4-(2-(2-Chloro-4,5-dimethylphenoxy)ethoxyJphenyl}-3,9-diazabicyclo (3.3.1] non-6-ene-3,6,9-tricarbosyHe acid 3-(gr*-butyl ester 9-(2,2^-trichloro-i,l-dimethyIethyl) ester (Ay4)
As for compound AYl, but from bicyclononene AX3 (13.35 g, 17.2 mmol), EtOH (670 mL) and aq. IM NaOH (670 mL). Purification by FC (EtOAc/heptane 1:1 -» EtOAc -). MeOH/EtOAc 1:9) yielded the title compound 12.3 g (96%). Rf = 0.75 (EtOAc). LC-MS: R, = 6.94.
irac)-{lR*, 55*)-7-{4-[2-(4-Bromophenoiy)efhoxy]pIienyI}-3,9-diazabicycIo-[3-3.1 Inon-6-ene-6,9-dicarboxylic acid 9-(2,2;i-trichloro-14-dimefhylefhyl) ester (AYS)
As for compound AYl, birt from bicyclononene AX4 (13.6 g, 17.2 mmol), EtOH (680 mL) and aq. IM NaOH (680 mL). Purification by FC (EtOAc/heptane 1:1 -> EtOAc -> MeOH/EtOAc 1:9) yielded the title compound 12.2 g (93%). Rf = 0.75 (EtOAc). LC-MS; Rt = 6.75.
Compounds of type AZ
(rac.)-(//f*, 55 *)-3-Acetyl-?-14-(3-hydroxypropy Opheay l]-3,9-diazabicy clo-[3,3.1]non-6-ene-6,9-dicarbosyUc acid 9-(2,2,2-trichloro-l,l-dimethylethyl)
ester (AZl)

A mixture of bicyclononene S5 (3.23 g, 5.60 mmol) in EtOH (50 mL) and aq. IM NaOH (50 mL) was stirred at 80 °C for 5 h. The mixture was allowed to cool to rt and diluted with EtOAc. The mixture was brought to pH 2 with aq. IM HCl and extracted with EtOAc (3x). The combined org. extracts were dried o\'er MgS04, filtered, and the soVvents were removed under reduced pressuie. Purification by FC (MeOH/CHsCb 1:19 -> 1:9 -> 1:4) yielded the title compound (1.40 g, 46%). LC-MS: R, = 0.89; ES+; 547.28.
(racH^R*, 55*}-7-[4-(2-Hydroxyethyi)phenyl]-3,9-diazabicydo[33.1jooii-6-ene-3,6,9-tricarboxylic acid 3-/^rt-butyl ester 9-(2,2,2-trichloro-l,l-dimethyl-ethyl) ester (AZ2)
As for compotmd AZl but from bicyclononene H8 (4.96 g), EtOH (150 mL) and aq. IM NaOH (150 mL). The crude material was used further without purification.
Compounds of type BA
(rac.)-(JJi*, 55*)-3-Acetyl-7-{4-I3-(tert-butyldimethylsilanyloxy)propyl]-
phenyl}-6-((2-chlorobejizyl)cyrfopropylcarbamoyl]-3,9-diazabicyclo[33.1]-non-6-ene-9-carboxylic acid 2^,2-trichloro-l,l-diinethylethyl ester (BAl)
A mixture of bicyclononene T4 (1.85 g, 2.79 mmol), (2-chIorobenzyl)-cyclopropylamine (1.52 g, 8.37 mmol), DMAP (85 mg, 0.70 mmol), DIPEA (1.91
mL, 11.2 mmol), HOBt (377 mg, 2.79 mmol) and EDC-HCl (803 mg, 4.19 mmol) in CH2CI2 (50 mL) was stirred at rt for 18 h. The mixttire was diluted with more CH2CI2 and washed with aq. IM HCl (Ix) and aq. sat. NaHC03 (Ix). The org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:4 ^-1:3 —*■ 1:2-> l:l)yielded the title compound (LI6g, 50%). LC-MS: R, = 1.37.

(rac.)-(lR% i5*)-7-{4-[2-(fer^Butyldiphenylsilany!ox>)ethyI]pheQyl)-6-[(2-chlorobenzyI)cyclopropylcarbamoylJ-3,9-diazabicyclo(3.3.]]non-6-ene-3,9-dicarboxyiic acid 3-^^rt-butyl ester 9-(2^,2-trichIoro-l,l-dimethy]ethyI) ester (BA2)
As for compound BAl, bur &om bicyclononene T5 (crude, about 5.79 mmol), (2-chlrobenzyOcyclopropylamine (3.10 g, 17.1 mmol), DIPEA (3.9 mL, 22.8 mmol).
DIvIAP (140 mg, 1.14 mmol), HOBt (770 mg, 5.70 mmol), and EDC-HCl (1.64 g, 8.55 mmol), in CH2CI2 (50 mL). Purification of the residue by FC (EtOAc/heptane 1:8 "> 1:4) yielded the title compound 3.35 g (58%). Rf = 0.55 (EtOAc/heptane 2:3). LC-MS: Rt= 1.40.
(/•flc)-(i.ff*, J5*)-3-AcetyI-7-{4-[2-(fert-butyldiphenylsiIanyloxy)ethyIIphenyl}-6-[(2-chIorobenzyl)cyclopropylcarbanioyl]-3,9-dia2abicycloI3.3.1Jnon-6-ene-9-carboxyHc acid 2^,2-trichIoro-l,l-dimethyIethyI ester (BA3)
As for compound SI, from BA2 (1.45 g, 1.45 mmol), CH2CI2 (10 mL), 4M HCI/dioxane (10 mL), THF (20 mL), without DMAP, DIPEA (4.62 mL, 27.0 mmol), acetyl chloride (0.903 mL,9.55 mmol), and MeOH (5 mL). Purification of the residue by FC (ErOAc/heptane 1:1 -»■ EtOAc -> MeOH/EtOAc 1 ;9) led to the title compound (1.34 g, 75%). Rf =0.30 (EtOAc/heptane 1:1). LC-MS: Rt = 1.39.
Compounds of type BB
irac.)-{lR% 55*)-3-Acefyl-6-[(2-cIiIorobenzyI)cyclopropyIcarbamoyl]-7-[4-(3-hydroxypropyI)phenyl]-3,9-diazabicyclo[3.3.1]non-6-eiie-9-carboxyHc acid 2^,2-trichloro-l,l-dlmethylethyl ester (BBl)
A mixture of bicyclononene BAl (1.16 g, 1.40 mmol) and TBAF (884 rag, 2.80 mmol) in THF (10 mL) was stirred at rt for 90 min. The mixture was diluted with BtOAc and washed with water (2x) and brine (Ix). The org. extracts were dried

over MgS04, filtered, and the solvents were removed under reduced pressure. Purification by FC (MeOH/CH2Cl2 1:49 -^ 1:9) yielded the title compound (990 mg,98%), Rf- 0.47 (MeOH/CH.Cb 1:9). LC-MS: Rt-l.ll.
(rac.)--(JR*, 55'*)-3-Acetyl-6-[(2-chlorobenzyl)cyclopropylcarbamoyI]-7-[4-(2-
hydroxyethyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxyIic acid
2,2,2-trichloro-l,l-dimethyleth>'I ester (BB2)
As for compound BBl, but from BA3 (1.99 g, 2.21 mmol), TBAF (IM in THF, 4.5 mL, 4.5 mmol) in THF (15 mL). Purification by FC (EtOAc/heptane 1:5 -> 1:1 -> EtOAc) yielded the title compound (1.00 g, 68%). Rf = 0.38 (EtOAc/heptane 1:1). LC-MS: Ri= 1.09; ES+: 698.02.
(racyilR*, 55*)-6-K2-Cblorobenzyl)cyclopropylcarbamoyll-7-{4-l3- Zn (1.63 g, 24.9 mmol) was added to a sol. of bicyclononene AK2 (2.25 g, 2.50 mmol) in THF (30 mL) and AcOH (10 mL) under efficient stirring. The mixture was stirred efficiently for 2.5 h, then filtered and washedwith THF. The filtrate was diluted with EtOAc and washed witti aq. IM NaHO (2x). The org. extracts were dried over MgS04, and filtered. Ev^orating the solvents under reduced pressure yielded the title compound that was used without further purification.
(JR, 55)-9-Methyl-7-trifluoromethaiiesulfonyloxy-3,9-diazabicycio[33.1]non-6-ene-3,6-dicarboxylic acid 6-benzyl ester 3-ter/-butyI ester (BD)
A sol. of bicyclononene AG (1.13 g; 2.91 mmol) in THF (8 ml) was added to a suspension of NaH (ca 60%, 175 mg; 4.36 mmol) in THF (2 ml) at 0°C. After 30 min TfjNPh (1.56 g; 4.36 mmol) was added and the mixture was stirred at rt for 12 h. Ice (5 g) was added and THF was evaporated. The aq. residue was extracted with EtOAc (3x). The combine org, extracts were dried over MgS04, filtered, and

the solvents were removed under reduced pressure. Puriciation of the residue by FC (EtOAc/cyclohexane 1:1 -> EtOAc) yielded the title compound (1.28 g, 84%). Rf=0.53(EtOAc),
{IR, 55)-7-{4-[3-(ter/-Buty!dimethylsilanyloxy)propyllphenyl}-9-methyI-3,9-diazabicyc[o[33.11noii-6-ene-3,6-dicarbosyUc acid 6-benzyl ester 3-(ert-butyl ester (BE)
BuLi (1.6 M in hexane, 3.82 mL, 5.98 mmol) was added to a sol. of [3-(4-bromophenyl)propoxy]-/err-butyldiinethyIsiIane (Kiesewetter D. O., Tetrahedron Asymmetry, 1993, 4, 2183; 1.97 g; 5.98 mmol) in THF (4ml) at -78°C. After 30 min, ZaCli (IM in THF, 7.2 ml; 7.2 mmol) was added and the mixture was alloed to warm up to rt. A sol. of bicyclononene BD (1.24 g: 2.39 mmol) in TPIF (7 ml) and Pd(PPh3)4 (69 mg; 0.060 mmol) were added after each other and the mixture was heated to 40°C for 35 min. The reaction mixture was allowed to cool to rt, sat. solution of NH4CI was added, and the mixture was extracted with EtOAc (3x). The combined org. extracts were dried over MgS04,filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/cyclohexane 1:1 -> EtOAc) yielded the title compound (1.22 g, 82%). Rf = 0.27 (EtOAc). LC-MS: R, = 5.68; ES+ = 621.30.
[JR, 55)-7-{4-I3-(/crt-Batyldimethylsilanyloxy)propyl]phenyI}-3,9-diaza-
bicyclol33.il non-6-ene-3,6,9-tricarboxylic acid 6-benzyl ester 3-/erf-butyl ester 9-(2^^-trichloro-l,l-dimethyIethyI) ester (BF)
\ mixture of bicyclononene BE (1.66 g, 2.67 mmol) and p,p,P-trichloro-/er/-butyl
;hlorofoiiuate (13.4 g, 240 mmol) in 1,2-dichloroethane (10 ml) was heated to ■eflux for 4 h. The mixture was allowed to cool to rt and the solvents were emoved under reduced pressure. Purification of the residue by FC itOAc/cyclohexane 1:4) yielded the title compound (1.75 g, 83%). Rf = 0.43 ElOAc/cyclohexane 1:4). LC-MS: R, = 8.30.

(}J{, 55)-7-{4-(3-Hydroxypropyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarbosylic acid 6-beiizyl ester 3-/ert-butyl ester 9-(2,2^-trichloro-l,l-dimethylethyl) ester (BH)
A sol. of bicyclononene BF (1.59 g, 1.96 mmol) in CH2CI2 (3 ml) was cooled to 0°C and HCl/dioxane (4M, 10 ml) was added. The mixture was stirred for 2 h at 0°C and subsequently for 3 h at rt. After the solvents were removed under reduced pressure the crude was dried under high vacuum. The cresidue was dissolved in THF (5 ml). DMAP (12 mg, 0.098 mmol) and DIPEA (1.34 ml; 7.849 mmol) were added and the mixture was cooled to -78 °C. AcCI (0.153 ml; 2.16 mmol) was added and reaction mixture was sthred at -78 °C for 30 min. After addition of MeOH (1 ml) and warming-up to rt, aq. HCl (IM, 10 ml) was added and reaction mixture was extracted with EtOAc (3x). The combined org. extracts were washed with aq. sat. NaHCOs (Ix), and the org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC EtOAc/cyclohexane 1:3 ^^ 1:1) yielded the title compound (280 mg, 22%). Rf=0.38 (EtOAc). LC-MS: R( = 5.43; ES+ = 637.17.
(IR, 5.S)-7-[4-(3-Hydroxypropyl)phenyl]-3,9-diazabicyclo[33.11noa-6-ene-3,6,9-tricarboxyIic acid 3-tert-butyl ester 9-(2,2,2-tricliloro-l,l-diinefhyI-ethyl) ester (BI)
A mixture of bicyclononene BH (140 mg; 0.219 mmol) and Pd/C (10%, 25 mg) m MeOH (4 ml) was stitted at rt under H2 for 2 h. The mixture was filtered through Celite, washed with MeOH, and the solvents were evaporated under reduced pressure. The crude product (110 mg) was directly used in the next reaction without purification. Rf= 0.15 (EtOAc). LC-MS; Rt = 4.41; BS-: 545.02.
(IS, 55)-7-[4-(3-Hydroxypropyl)phenyi]-6-(methylphenethyIcarbamoyl)-3,9-diazab icy do [3.3.1] non-6-ene-3,9-dicarboxy lie acid 3-(e/(-butyl ester 9-(2,2,2-trichIoro-l,l-dimethyIethyl) ester (BJ)

A mixture of bicyclononene BI (95 mg; 0.17 mmol), phenethylmethylamine (0.48 mi; 0.34 mmol); HOBt (6.0 mg, 0.042 mmol), EDC-HCl (49 mg; 0.255 mmol) and DMAP (5.0 mg; 0.042 mmol) in CHCI3 (6 ml) was stiired at rt for 14 h. Aq HCl (IM) was added and the mixture was extracted with CH^Cb (3x). The org. phase was washed with aq, sat. NaHCOj (Ix), the combined org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/cyclohexane 1:1-+ EtOAc) yielded the title compound (64 mg, 44%). Rf = 0.25 (EtOAc). LC-MS: R, = 5.37; ES+r 664.29.
(IR, 55)-7-{4-(3-(2-Bromo-5-fluorophenoxy)propyllphenyl}-6-(methyl-
phene(hyIcarbamoyI)-3,9-diazabicycIo[3.3.1]Don-6-ene-3,9-dicarboxylic acid 3-teii-butyl ester 9-(2,2,2-trichloro-l,l-dimethyI-ethyI) ester (BK)
A mixture of bicyclononene BJ (60 mg; 0.090 mmol), 2-bromo-5-fluorophenoI (34 mg, 0.18 mmol), azodicarboxylic dipiperidide (34 mg; 0.135 mmol) and tributylphosphine (67 mg; 0.270 mmol) in toluene (2 ml) was heated to reflux for 20 h. The solvent was removed under reduced pressure. Purification of the residue was by FC EtOAc/cyclohexane 2:1 ~> 4:1) yielded the title compound (58 mg,76%). Rf=0.60(EtOAc). LC-MS: R, = 7.01; ES+ = 836.07.
(rac.)-(lR*, 55*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenosy)-
propyl]phenyI}-3,9-dia2abicyclo(33.1]non-6-ene-6,9-dicarboxylic acid 6-efhyl ester 9-(2^,2-trichIoro-l,l-dimethyIetbyI) ester (BL)
HCI/dioxane (4M, 20 mL) was added to a sol. of bicyclononene AX2 (2.00 g, 2.47 mmol) in CH2CI2 (20 mL) cooled to 0 °C. The ice bath removed and the mixture was stirred at rt for 2 h. The solvents were removed under reduced pressure and the foamy residue dried under high vacuum. A mixture of this residue, DMAP (15 mg, 0.123 mmol) and DIPEA (1.69 mL, 9.88 mmol) m THF (40 mL) was cooled to -78 °C, and AcCi (0.186 mL, 2.47 mmol) was added. The mixture was stirred for 20 min at -78 °C and MeOH (5 mL) was added. The mixture was

allowed to warm up to rt, was diluted with EtOAc and washed with aq. IM HCl (Ix). The org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:4 -^ 1:1 -^ EtOAc) yielded the title compound (1.55 g, 83%). Rf= 0.50 (EtOAc).
Compounds of t>'pe BM
3-Acetyl-7-{4-(2-(2-bromo-5-fluorophenox>')ethoxy]pheoyI}-3,9-diaza-bicycIo[3J3.1]noii-6-ette-6,9-dicarboxyIic acid 6-ethyl ester 9-(2,2^-trichloro-1,1-dimefhyIethyI) ester (BM2)
Tributylphosphine (3.84 mL, 15.6 nraiol) was added to a sol. of bicyclononene S4 (3.00 g, 5.19 mmol), 2-bromo-5-lluorophenol (1.15 mL, 10.4 mmol) and azodicarboxylic dipiperidide (1.97 g, 7.79 mmol) in toluene (30 mL). The mixture was heated to reflux for 2 h and allowed to cool to rt. The solvents were removed under reduced pressure. Purification by FC (EtOAc/heptane 1:1 —> 2:1 ^ 3:1) yielded the title compound (2.70 g, 69%).
3-AcetyI-7-{4-[2-(2-c!iloro-4,5-dimethyIphenoxy)ethoxyJphenyi}-3,9-diaza-bicycio [3.3.1] noii-6-ene-6,9-dicarbosyIic acid 6-ethyI ester 9-(2^^-trichloro-1,1-dimethyIethyl) ester (BM3)
As described for compoxmd BM2, but from bicyclononene S4 (3.00 g, 5.19 mmol), 2-chloro-4,5-dimethylphenol (1.64 g, 10.5 mmol), azodicarboxylic dipiperidide (L98 g, 7.86 mmol) , tributylphosphine (3.90 mL, 15.7 mmol) and toluene (50 mL). Purification by FC yielded the title compound (2.82 g, 75%).
3-Acetyl-7-{4-[2-(2,6-dichIoro-4-methylphenosy)ethoxylphenyl}-3,9-diaza-bicyclo[3.3.1Jnon-6-ene-6,9-dicarboxyIic acid 6-etfayl ester 9-(2,2,2-trichIoro-1,1-dimethylethyI) ester (BM4)

As described for compound BM2, but &om bicyclononene S4 (3.00 g, 5.19 mmol), 2,6-dichloro-4-methylphenol (1.84 g, 10.38 mmol), azodicarboxylic dipiperidide (1.97 g, 7.79 mmol) , tributylphosphine (3.84 mL, 15.6 mmol) and toluene (50 mL). Purification by FC yielded the title compound (2.76 g, 72%).
3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]pbenyl}-3,9-diazabicyclo-[3.3.1]Don-6-ene-6,9-dicarbox\iic acid 6-ethyl ester 9-(2,2^-trichloro-l,l-dimethylethyl) ester (BM5)
As described for compouad BM2, but &om bicyclononene S4 (3.20 g, 5.54 mmol), 2,3-dichiorophenoI (1.80 g, 11.1 mmol), azodtcarboKyUc dipiperidide (2,10 g, 8.31 mmol) , tributylphosphine (4.11 raL, 16,6 mmol) and toluene (50 mL), Purification by FC yielded the title compound (2.22 g, 55%).
3-AcefyI-7-{4-[2-(4-chloro-2-methylpheooxy)ethoxylpbenyI}-3,9-dia2a-bicyclo[3.3.1]non-6-ene-6,9-dicarboxyIic acid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethyIethyl) ester (BM7)
\s described for compound BM2, but from bicyclononene S4 (3.00g, 5.19 mmol), ^chloro-2-methylphenol (1.48 g, 10.4 mmol), azodicarboxylic dipiperidide (1.97 ;, 7.79 mmol) , tributylphosphine (3.84 mL, 15.6 mmol) and toluene (50 mL). Purification by FC yielded the tide compound (1.36 g, 37%).
i-AcetyI-7-{4-[2-(2,4,5-trichJorophenosy)ethorj']pIienyI}-3^-diazabicycl(>-3J.lJnon-6-ene-6,9-dicarboxyiic acid 6-ethyI ester 9-(2^,2-trichIoro-I,l-limethylethyl) ester (BM9)
IS described for compound B]VI2, but from bicyclononene S4 (3.00 g, 5.19 mmol) ,4,5-triclilorophenoI (2.05 g, 10.4 mmol), azodicarboxylic dipiperidide (1.97 g, .79 mmol) , tributylphosphine (3.84 mL, 15.6 mmol) and toluene (50 mL). urification by FC yielded die title compound (2.76 g, 72%).

3-AcetyI-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyI}-3,9-dia2a-bicyclo[3.3.1]non-6-ene-6,9-dicarboxyIic acid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethyIethyI) ester (BMIO)
As described for compound BM2, but from bicyclononene S4 (3.18 g, 5.50 mmol) 2-chloro-5-fluorophenol (1.61 g, 11.0 mmol), azodicarboxylic dipiperidide (2.08 g, 8.25 mmol) , tributylphosphine (4.10 mL, 16.6 mmol) and toluene (50 mL). Purification by FC yielded the title compound (2.67 g, 69%).
Compounds of type BN
3-Acetyl-7-{4-[2-(2-bromo-5-fluoropheiioxy)ethoxy]phenyl}-3,9-diaza-bicyclo[3.3.1]noii-6-ene-6,9-dicarboxylic acid 9-(2,2,2-trichloro-l,l-dimethyl-ethyl) ester (B1SI2)
A mixture of bicyclononene BM2 (2.69, 3.58 mmol) in aq. IM NaOH (30 mL) and EtOH (70 mL) was stirred for 1 h at 85 °C. The mixture was allowed to cool to rt and the solvents were partially removed under reduced pressure. The residue was acidified to pH 2 with aq. IM HCl and this mixture was extracted with EtOAc (3x). The combined org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. The crude title compound (2.96 g, quantitative yield) was used further without purifiaition.
3-Acetyl-7-{4-[2-(2-chloro-4^-dimethyIphenoxy)ethQrylphenyl}-3,9-diaza-bicyclop3.1Inoii-6-ene-6,9-dicarboxylic acid 9-(2^,2-trichioro-l,l-dimethyl-ethyl) ester (BN3)
As described for compound BN2, but from bicyclononene BM3 (2.82 g, 3.94 mmol), aq. IM NaOH (30 mL) and EtOH (70 mL). The crude title compound (2.59 g, 96%) was used further without purification.

3-Acetyi-7-{4-[2-(2,6-dichIoro-4-niethylphenoxy)ethoxy]phenyJ}-3,9-dia2a-bicycIo[3.3.1]noD-6-ene-6,9-dicarboxyIic acid 9-(2^,2-trichIoro-l,I-dimefhyl-ethyl) ester (BN4)
As described for compound BN2, but from bicyclononene BM4 (2.75 g, 3.73 mmol), aq. IM NaOH (30 mL) and EtOH (70 mL). The crude dtle compound (2.63 g, quantitative yield) was used fiirther without purification.
3-Acetyl-7-{4-[2-(23-dicblorophenoxy)ethoxyJ phenyl)-3,9-diazabicyclo-I33.11non-6-ene-6,9-dicarboxylic acid 9-(2^^-trichloro-l,l-dimethylethyl) ester (BN5)
As described for compound BN2, but from bicyclononene BM5 (2.22 g, 3.07 mmol), aq. IM NaOH (30 mL) and EtOH (70 mL). The crude title compound (1-59 g, 75%) was used further without purificatioa.
3-Acetyl-7-(4-[2-(4-chloro-2-iBethylphenoxy)ethoxylpheayl}-3,9-diaza-bicycIo[3.3.1]noii-6-ene-6,9-dicarboxylic acid 9-(2,2^-trichloro-l,l-dimethyl-ethyl) ester (BN7)
As described for compound BN2, but from bicyclononene BM7 (1.35 g, 1.92 mmol), aq. IM "NaOH (30 mL) and EtOH (70 mL). The crude title compound (1.25 g, 97%) WE^ used fiirther without purification.
3-AcetyI-7-{4-[2-(2,4,5-trichIorophenoxy)ethoxy]phenyI}-3^-diazabicycIo-{33.1]non-6-ene-6,9-dicarboxyIic acid 9-(2^,2-trichIoro-l,l-dimethyIethyl) ester (BN9)
As described for compound BN2, but from bicyclononene BM9 (2,31 g, 3.05 mmol), aq. IM NaOH (30 mL) and EtOH (70 mL). The crude title compound (2.19 g, 99%) was used further without purification.

3-Acetyl-7-{4-[2-(2-chloro-5-fluoropIienoxy}ethoxy]phenyl}-3,9-diazabicyclo-(3.3.1]nDn-6-ene-6,9-dicarboxyIic acid 9-(2,2,2-trichIoro-l,l-dimethylefhyl) ester (BNIO)
As described for compound BN2, but from bicyclononene BMIO (2.82 g, 3.94 mmol), aq. IM NaOH (30 mL) and EtOH (70 niL). The crude title compound (1.90 g, 74%) was used further without purification.
Preparation of the final compounds
Typical procedure (A) for the acylation:
To a solution of bicyclononene in anhydrous EtOAc was added vacuum dried-Amberlyst 21 (1.5 g/mmole of bicyclononene) or another suitable scavenger, followed by the addition of the desired acid chloride (1.5 eq.). After shaking the suspension for 3 h, an aliquot water was added and shaking was continued for 1 h. The resin was then removed by filtration, washed with EtOAc and the filtrate was evaporated to yield the intermediate amide.
The synthesis of the sulfonamide, carbamate or urea derivatives was performed in analogy to the above-described procedure, by using the corresponding sulfonyl chloride, chloroformate or carbamoyl chloride respectively.
Typical procedure (B)for amide formation from acid chlorides:
To a sol. of the acid chloride (1 eq.) in CH2CI2 (2.5 mL/mmol) at 0 "C. the amine (3 eq.) was added. The mixture was stirred for 3 h while warming up slowly to rt. If necessary, more CH2CI2 was added, then the reaction mixture was washed with aq. sat. NaHCOs (Ix) and aq. IM HCi (Ix). The extracts were dried over MgSOj and the solvents were removed under reduced pressure. The obtained product was used without further purification.

Typical procedure (C) for an amide coupling with CDI
To a sol. of tlie carboxylic acid {1 eq.) in CH2CI2 (4 mL/mmol) CDI (I eq.) was added. The sol. or suspension was stirred for 2 h at rt, then cooled to 0 °C. The amine (6 eq.) was added and the sol. or suspension was stirred for 2 h while warming up slowly to rt. The sol. or suspension was washed with water (Ix). The org. extracts were evaporated under reduced pressure and the obtained residue was used further without purification.
Typical procedure (D)for the reduction of an amide to an amine with LAH
To a sol of the amide (1 eq.) was dissolved in THF (3 mL/mmol) LAH (IM in THF, 3 eq.) was added carefully. The mixture was stirred at rt for 30 min, then heated to 60 °C for 3 h before it was allowed to cool down to rt, then to 0 °C. For X g of LiAlH4 initially added, was added x g of water, then x g of aq. 15% NaOH, and finally 3x g of water again. The resulting mixture was stirred overnight, filtered, and the precipitate washed with EtOAc. The filtrate was evaporated under reduced pressure and the residue diluted in a small amount of MeOH. The sol. was passed through a pad of SCX silica gel (sulfonic acid). Elution started with MeOH, followed by NHj/MeOH. The amines eluted with the second second eluent. The solvents were removed under reduced pressure. The isolated amines were either used without further purification or purified by HPLC, depending on the purity.
Typical procedure (E) for the cleavage of the 2,2,2-trichloro-l,l-dimethylethylcarbamate protecting group:
The crude product from another typical procedure was dissolved in THF/AcOH (1:0.1) and treated with zinc (20 eq.). The suspension was stirred for 5 h and filtered through celite, which was washed with EtOAc. The filtrate was evaporated under reduced pressure and the residue was purified by HPLC.

Typical procedure (F)for the formation of aryl ether (Mitsunobu reaction)
The bicyclononene (0.05 mmol) was dissolved or suspended in toluene (1.00 mL). The phenol derivative (0.075 mmol) in toluene (0.50 mL) was added. TMAD (0.075 mmol) in toluene (0.50 mL) was added, followed by tribut>-lphosphine (0.15 mmol). The reaction mixt^e was stirred for 2 h at rt and then 2 h at 60 °C. Sometimes, it was necessary to add a second portion of tributylphosphine and to stir overnight. Sometimes, THF was necessary as cosolvent to dissolve the reactants. The reaction mixture was allowed to cool to rt, then water was added. The mixture was extracted with EtOAc, and the org, extracts were evaporated under reduced pressure.
Typica! procedure (G)for an amide coupling
To a sol. of bicyclononene (0.05 mmol) in CHCI3 (2 mL) the desired carboxylic acid (0.10 mmol) was added. DIPEA (0.10 mmol), DMAP (0.01 mmol), HOBt
(0.01 mmol), and EDCHCl (0.05 mmol) were added and the reaction mixture was
stirred overnight. Sometimes, it was necessary to add another portion of acid,
DMAP, HOBt and EDC-HCI and to continue stirring for 24 h. CH2CI2 was added md the mixture was washed with water. The org. extracts were separated, dried 3ver Na2S04 and filtered. The solvent was removed under reduced pressure.
Typical procedure (H)for an amide coupling
To a sol. of the bicyclononene (0.05 mmol) CHCls or CH2CI2 (2 mL) the desired tmine (commercially available or prepared following known, standard irocedures) (0.10 mmol) was added. DIPEA (0.10 mmol), DMAP (0.01 mmol), lOBt (0.01 mmol) and EDC-HCI (0.05 mmol) were added. ■ The reaction mixture vas stirred overnight. Sometimes, it was necessary to add another portion of mine, DMAP, HOBt and EDC-HCi and to continue stirring the sol. for 24 h. ]H2Cl2 was added and the mixture was washed with water. The org. extracts

were separated, dried over Na2S04 and filtered. The solvents were removed under reduced pressure.
Typical procedure (J) for reductive amination
To a solution of aldehyde (leq.) in MeOH (0.5 mL/mmol) was added an amine (1.2 eq.). The solution was stirred for 2h. Sodium borohydride (1.2 eq.) was added portionwise at O^C and then stirring was continued, at rt, for 4h. A solution of NaOH IN was added and the MeOH was evaporated. The mixture was extracted with EtOAc twice and the organic layer was washed with brine, dried over Na2S04 and filtered. The solvent was removed under reduced pressxire. The isolated amines were either used without further purification or purified by flash chromatography (EtOAc/heptane; 2/8), depending on the purity.
Typical procedure (K)for an anhydride coupling
To a sol. of the bicyclononene (0.05 nmiol) in CH2CI2 (0.4 mL) was added DIPEA (0.1 mmol) followed by the anhydride (0.06 mmol) m CH2C12 (0.4 mL) at 0°C. After stirring for 3h at ri, the solvent was evaporated under reduced pressure.
Typical procedure (L)for protecting group (BOC and TBDMS) cleavage
To a sol. of the bicyclononene (0.05 mmol) in CH2CI2 (0.5 mL), cooled to O^C, was added 4M HCl/dioxane(0.5 mL) The ice bath was removed and the solution was stined for lh30 to 3h, depending on the compound. The solvents were evaporated under reduced pressure without heatmg.
Typical procedure (M) for the saponification of esters
A mixture of the ester (1 eq.) and LiOH (2 eq.) in THF was stirred at rt for 2 h. The solvents were removed under reduced pressure and the residue was extracted on isolute sorbent (0.25 g pre-washed with 0300 mL aq. IM HCl, elution with 2

mL CH2Ci2). The solvent was removed under reduced pressure and the residue was used without fUrther purification.
Preparation of amines (2-ChlorobenzyI)cycIopropyIamine
Synthesized according to typical procedures B and D irom 2-chlorobenzoyl chloride and cyclopropylamine.
Benzy Icy do propylamine
See Loeppky, R. N.; et al, J. Org. Chem., 2000, 65, 96.
(2-Chlorobenzyl)ethylamiiie
See Ishihara, Y; et al; Chem. Pharm. Bull., 1991, 39, 3225.
CycIopropyI-(3-trifluorometbylbenzyl)ainiDe
See Brabander, H. J.; el al; J. Org. Chem., 1967, 32,4053.
Cyclopropylphenethylamine
See Smith, P. W.; ef al; J. Med. Chem., 1998, 41, 111.
IVIethyl(3-pIienoxypropyl)ainine
Synthesized according to typical procedures C and D from. 3-phenoxypropionic icid and methylamine.
2-/j-Tolyloxj ethyl)mef hylamine

Synthesized according to typical procedures C and D from 2-/)-tolyIoxyacetic acid and methylamine.
[2-(3-Chlorophenyl)ethyl]amine
Synthesized according to typical procedures C and D from 3-chlorophenyIacetic acid and methylamine.
[2-(2-MethoxyphenyJ)ethyl] amine
Synthesized according to typical procedures C and D from 2-methoxyphenylacetic acid and methylamine.
(2-A)lylben2yI)cyclo propylamine
BuLi (1.55 M in hexane, 14.7 mL, 22.7 mmol) was added to a sol. of l-bromo-2-(dimethoxymethyl)ben2ene (5.00 g, 21.6 mmol) in EtiO (50 mL). The mixture
was stirred for 30 min at -78 °C and MgBri-EtsO (5.87 g, 22.7 mmol) was added. The mixture was allowed to warm up to 0 °C over 15 min and Cul (420 mg, 2.16 mmol) was added. The mixture was stirred at 0 °C for 5 min and allyl bromide (1.92 mL, 22.7 mmol) was added. The mixture was stirred overnight while warming up to rt. Aq. IM HCl (1 mL) was added and the mixture was diluted with Et20, and washed with aq. IM HCl (Ix). The org. Extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. The residue was dissolved in acetone (20 mL) and water (10 mL), and TosOH (cat. amount) was added. The mixture was stirred for 5 h at rt, and the solvents were partially removed under reduced pressure. The residue was diluted with Et20, and washed with aq. IM HCl (Ix), and aq. sat. NaHCOa (Ix). The org. extracts were dried over MgS04, filtered, and the solvents were removed under reduced pressure. Purification of the residue by FC (EtiO/petroIeum ether 1:49 -> 24:1)

yielded 2-allylbenzaldehyde (1.06 g, 34%). This compound was transformed into the title compound following typical procedure J with cyclopropylamine.
Cyclop ropyl(2-fluorobeiizyl)amine
Synthesized according to typical procedure J from 2-iluorobeiiza!dehyde and cyclopropylamine.
CycIopropyI-(2-methylbeiizyl)amiae
Synthesized according to typical procedure J from 2-methylbenzaldehyde and cyclopropylamine.
Cyclopropyl-[2-^4-methoxypheQOxy)ethyIlamine
Synthesized according to typical procedures C and D from (4-methoxyphenoxy)-acetic acid and cyclopropylamine.
Cyclopropyi-I2-(3-methoxyphenoxy)ethyl]amine
Synthesized according to typical procedures C and D from (3-methoxyphenoxy)-acetic acid and cyclopropylamine.
CyclopropyI-(2-fl-toIyIoxyethyi)ainine
Synthesized according to typical procedures C and D from o-tolyloxyacetic acid and cyclopiopylamine.
Cyclopropyl-[2-(3,4-dimethylpheQoxy)ethyl]amine
Synthesized according to typical procedures C and D from (3,4-dim6thyl-phenoxy)acetic acid and cyclopropylamine.

[2-(2-Chlorophenyl)ethyI]cyclopropyIamine
Synthesized according to typical procedures C and D from (2-chlorophenyi)-acetic acid and cyclopropylamine.
Cyclopropyl-[2-(23-difluorophenyl)ethyl]amine
Synthesized according to typical procedures C and D from (2,3-difluoiopbenyl)-aceric acid and cyclopropylamine.
Cyclopropyl-I2-(4-fluoropbenyI)ethyl]amine
Synthesized according to typical procedures C and D from (4-fluorophenyl)acetic acid and cyclopropylamine.
CycIopropyI-{2-o-tolylethyl)amme
Synthesized according to typical procedures C and D from o-tolylacetic acid and cyclopropylamine.
CycIop^opyI-(2-J!^•tolyIethyI)anline
Synthesized according to typical procedures C and D from ^tolylacetic acid and cyclopropylamine.
CycIopropyI-(3,5-dimethoxybenzyI)amine
Synthesized according to typical procedure J from 2,5-dimethoxybenzaldehyde and cyclopropylamine.
(2-ChIorobenzyI)niethylamine

See Kihara, M; et al.; Heterocycles, 1989,29, 957.
(2-Chlorobeiizyl)isopropylamine
Synthesized according to typical procedure J from 2-chloroben2aldehyde and isopropylamine.
CycIopropyI-(2-fluoro-5-methoxybenzyI)amiDe
Synthesized according to typical procedure J from 2-fluoro-5-methoxybenzaJdehyde and eyelopropyi amine.
CyclopropyI-(3-metboxybenzyl)amine
Synthesized according to typical procedure J from 3-methoxybenzaldehyde and cyclopropylaimne.
Cyclopropyl-(3,4-dimethoKybeiizyl)aiiiine
Synthesized according to typical procedure J ftom 3,4-dimethoxybenzaldehyde and cyclopropylamine.
(2-Chloro-3-trjfluoromethylbeiizyl)cyclopropyIamiiie
Synthesized according to typical procedure J from 2-chIoro-3-trifluoromethylbenzaldehyde and cyclopropylamine.
(6-ChIorobenzo[13Idioxoi-5-ylmethyI)cycIopropyiamine
Synthesized according to typical procedure J from 6-chlorobenzo[l,3]dioxole-5-carbaldehyde and cyclopropylamine.

Cyclopropyl-(5-fluoro-2-methosybeiizyl)amine
Synthesized according to typical procedure J from 5-fluoro-2-methoxybenzaldehyde and cyclopropyl amine.
(2-Cliloro-6-fluorobenzyl)cyclo propylamine
Synthesized according to typical procedure J from 2-chloro-6-fluorobenzaldehyde and cyciopropylamine.
(2-Bromobenzyl)cyclopropylamiDe
Synthesized according to typical procedure J from 2-bromobenzaldehyde and cyciopropylamine.
Cyclopropyl-{2,6-difluorobenzyl)ainine
Synthesized according to typical procedure J from 2,6-difluorobenzaldehyde and cyciopropylamine.
Cyclopropyl-(2^-dim etJiyIbenzy])ajnuie
Synthesized according to typical procedure J from 2,3-diniethylbenzaldehyde and
cyciopropylamine.
Cyclopropyl-(3-fluoro-2-methylbeiizyl)amine
Synthesized according to typical procedure J from 3-fluoro-2-methylbenzaldehyde and cyciopropylamine.
Cyclopropyl-(3,5-difluorobenzyl)amine

Synthesized according to typical procedure J from 3,5-difluorobenzaldehyde and cyclopropylamine.
(2-Cbloro-3,6-difluorobenzyl)cyclopropylainine
Synthesized according to typical .procedure J from 2-chJoro-3,6-difluorobenzaidehyde and cyclopropylamine.
(2,3-DichIorobenzyl)cyclopropyIamine
Synthesized according to typical procedure J from 2,3-dichlorobenzaldehyde and cyclopropylamine.
CycIopropyl-(3-trifluoromethoxybenzyl)amine
Synthesized according to typical procedure J from 3-trifluoromethoxy-benzaldehyde and cyclopropylamine.
CyclopropyI-(3-iBethylbenzyl)amme
Synthesized according to typical procedure J from 3-methylbenzaldehyde and cyclopropylamine.
Cyclopropyl-(23-d)[fluorobenzyl)amine
Synthesized according to typical procedure J from 2,3-difIuorobenzaldehyde and
cyclopropylamine.
(3-ChIorobeazyl)cy clop ropy lamine

Synthesized according to typical procedure J from 3-chlorobenzaldehyde and cyclopropylamine.
CycIopropy)-(4-fluorobeDzyl)amine
Synthesized according to typical procedure J from 4-fluorobenzaidehyde and cyclopropylamine.
Preparation of other reagents
4-Carbamoylbutyric acid
See Melnyk, O., et al.; J. Org. Chem., 2001, 66,4153.
me5o-3,4-Dihydroxytartaric acid anhydride
A mixture of mejo-3,4-Diydroxytartaric acid (1.00 g, 6.67 mmol) and trifluoroacetic acid anhydride (5 mL) was stirred for 2 h at rt. The solvents were removed under reduced pressure and the residue was used as crude product without fiuther purification.
Succinamic acid
See Bellier, B., et al.; J. Med. Chem.. 2000, 43, 3614.
Specific examples
Example 1
(rac.)-(2-Methoxyphenyl)acetic acid {IR*, 55*)-3-[2-(4-chIorophenyI)acetyIl-7-{4-[3-(2-methoxybenzyloxy)propoxy] phenyl}-3,9-diazabicyclo [3.3.1] non-6-en-6-yI methyl ester trifluoroacetate salt

Synthesized according to typical procedure A from bicyciononene N and 4-cliJorophenylacetyl chloride, then according to tj'pical procedure E. LC-MS: Rt= 4,57; ES^: 725.35.
Example 2
(mc.)-(2-]VIethoxyphenyI)acetic acid (IR*, 55'*)-7-(4-[3-{2-methoxybenzyl-oxy)propoxy]phenylJ-3-(quinoialine-2-carbonyI)-3,9-diazabicyclo[3.3.1]non-6-eo-6-yl methyl ester trifluoroacetate salt
Synthesized according to typical procedure A from bicyclononene N and 2-quinoxaloyl chloride, then according to typical procedure E. LC-MS: R, = 4.55; ES+-. 728.94.
Example 3
(rac.)-(2-Methoxyphenyl)acetic acid (7J?*, 55*)-7-{4-|3- Synthesized according to typical procedure A from bicyclononene N and phenylmethanesulfonyi chloride, then according to typical procedure E. LC-MS:
Rt = 4.75; ES-I-: 727.74.
Example 4
(/■flc.>(2-MethoxypheDyl)acetic acid {IR", 55*)-7-{4-l3-(2-methoxyben2yl-oxy)propoxy]phenyl}-3-(2-thiopheo-2-ylacetyl)-3,9-diazflbicyclol3J.l]non-6-
en-6-yl methyl ester trifluoroacetate salt

252
Synthesized according to typical procedure A from bicyclononene IS' and thiophen-2-ylacel.yl cliJoride, then according to typical procedure E. LC-MS: R, = 4.52; ES+: 696,91.
Example 5
(rflc. )-(2-Melhoxyi)henyl)iicctic acid (Hi*, 55*)-3-(bcnz()[ft]thiophcne~3-carhoiiyI)-7-{4-[3-(2-n!cthoxybciizyloxy)propoxy]pheiiyl}-3,9-dia/:ibicycIo-[3.3.1]non-6-ci»-6-yI methyl ester trifluoroacetate salt
Synthesized according to typicai procedure A from bicyclononene N and benzothiophene-3-carbonyI chloride, then according to t>'pical procedure E. LC-MS: R, = 4.76; ES+: 733.80.
Example 6
(rac.)'(lR*, 5^*)-7-{4-[3-(2-Methox>-beuzylosy)propoxyIphenyI}-6-(2-(2-me-thoxyphenyl)acetuxymethyll-3,9-diazabicyclo[3.3.1jnou-6-ene-9-carboxylic acid 2^,2-trichloro-l,l-dimethylethyI ester trifluoroacetate salt
Prepared as compound N, but then purified by HPLC. LC-MS: Ri = 5.30; ES+: 774.97.
Example 7
(rac.yilR*, 55*)-3-Acetyi-7-{4-[3-(2-methoxybenzy!oxy)propoxy]pbenyl}-3,9" diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid |2-(2-ehlorophenyl)ethylI-methylamide trifluoroacetate salt
Synthesized according to typical procedures H and E from bicyclononene Tl and [2-(2-chlorophenyI)ethyl]raethylamine (Jaques B.; Wallace R. G., Tetrahedron, 1977, 33, 581). LC-MS: Ri = 0.89; ES+: 632.40.

Example 8
(/•(ic.)-(2-Methoxyphenyl)acetic acid (JR*, 55*)-3-acetyl-7-{4-[3-(2-mefhoxy-ben2yloxy)propoxy]phenyl}-3,9-diazabicyc\ot3.3.11non-6-eii-6-ylmethy\ ester trifluoroacetate salt
Synthesized according to typical procedures A and E ftom bicyclononene IV and acetyl chloride. LC-MS:Ri = 0.93;ES+: 615.29.
Example 9
{rac)-{lR*, 55*)-3-AcetyI-7-(4-[3-{2-methoxybeii2yIoxy)propoxy]phenyI}-3,9-diaiabicyclop.3.1iflon-6-eae-6-carhoxyUc acid l2^(4-methoxyphenyl)ethyll-methylamide trifluoroacetate salt
Synthesized according to typical procedures H and E from bicyclononene Tl and [2-(4-metiioxyphenyl)ethyI]niethylainine (Ho C. Y,; Kukla M. J., Tetrahedron Lett. 1997, 38, 2799). LC-MS: R, = 0.83; ES+: 628.44.
Example 10
(rac)-(2-MethoxyphenyI)acetic acid (IR*, 55*)-3-[2 Synthesized according to typical procedures A and E from bicyclononene P and 4-
chlorophenylacetyl chloride. LC-MS; Rt = 1.03; ES+: 726.44.
Example 11

(rtrc.HlJi*, 5^*)-3-Acctyl-7-{4-[3-(2-metlH)x>'benz}'loxy)propox7]pheDyl}-3,9-di:izabi{;ycIo[3.3.1]non-6-cne-6-c:irboxyIic acid (2-(4-chloroplieny!)ethyl]-methylamide trifluoroacetate salt
Syntliesized according to t)'pica] procedures H and E from bicyclononene Tl and [2-(4-chIorophenyl)cthyI]methylamin6 (You Q., et ai, Chem.. Res. Chin. Univ., 1992, S, 468), LC-MS: R, - 0.90; ES+: 632.40.
Example 12
{rac.)'{lR*, 5;S*)-3-Acctyl-7-{4-[3-(2-methoxybenzyIoxy)propoxy]plienyl}-3,9' diazabicyclo[3.3.1]non-6-eue-6-carboxylic acid [2-(3-dilorophenyI)ethyi]-mefhylamide trifluoroacetate salt
Synthesized according to typical procedures H and E from bicyclononene Tl and [2-(3-clilorophenyI)ethyl]methylamine. LC-MS: Rt= 0.92; ES+; 632.37.
Example 13
(rac.)-(lR% 55*)-3-Acefyl-7-{4-[3-(2-methoxybenzyloxy)propoxyJphenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid ethylphenethylamide tri¬fluoroacetate salt
Synthesized according to typical procedures H and E from bicyclononene Tl and ethylphenethylamine (Cossy J., Rakotoarisoa, H., Tetrahedron Lett., 2000, 47, 2097). LC-MS: R,- 0.89; ES+: 612.46.
Example 14
irac.)-(lR*, 55*)-3-Acetyl-7-(4-{3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid [2-(3-methoxyphenyi)ethyI]-methylamide trifluoroacetate salt
Syndaesized according to typical procedures H and E from bicyclononene Tl and [2-(3-methox>-pheuyL)ethyl]metliy!amine. LC-MS; Ri= 0.88; ES+: 628.41.
Example 15
(mc.)-(2-Me(hoxyphenyI)acetic acid (]R% 55*)-7-{4-[3-(2-metfaoxybenzy-loxy)propox>]phenyl}-3-methyl-3,9-diazabicyclo[3.3.1jDon-6-en-6-ylmethyl ester trifluoroacetate salt
A sol. of bic>'clononene N (0.05 mmol) in CH2Ci2 (2 mL) was cooled to 0 °C. DIPEA (0.10 mniol) and methyl iodide (0.10 mmol) were added. The mixture was stirred at 0 "C for 2 h, then ovemight at rt. Methyl iodide (0.50 mmol) and DIPEA (0.15 mmol) were added again and stirring was continued for 4 h at rt. EtOAc was added and the mixture was washed with water. The org. extracts were separated, dried over MgS04 and filtered. The solvents were removed under reduced pressure and the residue was porcessed further according to general procedure E. LC-MS: Rt = 4.04; ES+: 587.38.
Example 16
(rac.)-(JR% 55*)-3-AcetyI-7-{4-(3-(2-methoxybenzyIoxy)propoxylphenyl}-3^-diaiabicyclo[33.11tton-6-ene-6-carboxylic acid [2-(3,4-dunethoxyplienyI)-ethyl]meihylamide trifluoroacetate salt
Synthesized according to typical procedures H and E from bicyclononene Tl and 2-(3,4~dimethoxyphenyl)ediyl]methylamine. LC-MS: R, = 0.89; ES+: 644.48.
i^xample 17

(rac.)-(2-Methoxyphenyl)acetic acid {JR*, 5A'*)-7~{4-[3-(2-methoxybenzyI-oxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.11non-6-cn-6-yImethyl ester tri-lluoroacetatesalt
Synthesized according to tj'pical procedure E from bicyclononene N. LC-MS: Ri = 0.S3;ES+: 573.29.
Example 18
{rac.)-N'({lR*, 55*}-3-Acet}I-7-{4-[3-(2-methoxybenzj'loxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6~ylmethyl)-2-(2-jnethoxypheayl)-A'-methyl-acetamide trlfluoroacetate salt
Synthesized according to typical procedures G and E from bicyciononene Z and (2-methoxyphenyl)acetic acid. LC-MS: R, = 3.98; ES+: 62S.63.
Example 19
{rac.y{lR*, 55*)-3-AcetyI-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]noii-6-ene-6-carboxylic acid methyl(3-phenylp ropy I) amide trifluoroacetate salt
Synthesized according to typical procedures H and E from bicyclononene Tl and 7V-methyI(3-phenylpropyl)aniine (Lavastre I.; et al, Bull. Soc. Chiin. Fr., 1995,
132,188). LC-MS: Rt = 0.88; ES+: 612.45.
Example 20
(rac.)-(lR*, 55'*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicycVo[3.3.11iioii-6-ene-6-carboxylic acid [2-(2-methosyphenyI)ethyl]-methylamide trifluoroacetate

Synthesized according to typical procedures H and E from bicyclononene Tl and [2-(2-methoxyphenyl]ethyl]methylamine. LC-MS: R, = 0.88; ES+; 62S.45.
Example 21
(rac.y(JR*, 55'*)-3-Acetyl-7~{4-[3-(2-methoxybenzyIoxy)propoxy]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-eQe-6-carboxylic acid benzylmethylamide trifluoro-acetate
Synthesized according to typical procedures H and E from bicyclononene Tl and N-methylbenzj'lamine. LC-MS: Rt = 0.84; ES+: 684.41.
Example 22
(rac.)-(2-Methoxyphenyl)acetic acid (IR^, 55*)-3-acetyl-7-{4-[3-(2-chloro-phenoxy)propyIlphenyl}-3,9-diazabicyclo[33.1]non-6-en-6-ylmethyl ester trifluo roacetate
Synthesized according to typical procedures F and E from bicyclononene R2 and 2-chlorophenoI. LC-MS: R, = 0.89; ES+: 589.34.
Example 23
(rac)-(2-Methoxyphenyl)acetic acid (IR*, 55*)-3-acetyl-7-{6-[3-(2-methoxy-benzyIoxy)propoxy]pyridiii-3-yl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyI ester trifluoroacetate salt
Synthesized according to typical procedures A and E from bicyclononene P and acetyl chloride. LC-MS: R, = 0.90; ES+: 616.44.
Example 24

(;-flf:.)-(2-Methoxyphenyl)acetic acid {1R% 5^*)-3-acetyI-7-{4-[3-(2-bromo-phenosy)propyl]phenyI}-3,9-diazai)icyclo[3.3.1]noo-6-en-6-ylmethyl ester trifluoroacetate salt
Synthesized according to tj'pica! procedures F and E from bicyclononene R2 and 2-bromophenol. LC-MS: R,= 0.92; ES+; 633.26.
Example 25
(rQc,)-(2-Methoxyphenyl)acetic acid (1R% 5^*>3-[2-(4-chIorophenyl)ethyll-7-{4- [3-(2-m ethoxybenzyloxy )prop oxy] phenyl} -3,9-diazabicycIo [3.3.11 non-6-en-6-yI- methyl ester trifluoroacetate salt
To a sol. of bicyclononene N (0.05 mmol) m CH2CI2 (2 mL) NaBHaOAc (0.065 mmol) and (4-chlorophenyl)acetaldehyde (Zhuangyu Z., e( al. Synthesis, 1991, 539, 0.065 mmol) were added. The mixture was stirred overnight. The solvent was removed under reduced pressure and the residue treated according to typical procedure E. LC-MS: Rt = 4-88; ES+: 711.47.
Example 26
(/•(zc)-(2-MethoxyphenyI)acetic acid (IR*, 55*>-3-acetyI-7-{4-[2-(3-chloro-
phenosy)ethyllpheiiylJ-33-diazabicyclo[3.3.1]BQn'6-eii-6-ylmethyl ester
trifluoroacetate salt
Synthesized according to typical procedures F and E from bicyclononene Rl and
3-chlorophenol. LC-MS: Rt ^ 4.17; ES+: 575.62.
Example 27

(mc.H2-MethoxyphenyI)acetic acid fJif*, 55*>3-acety\-7-{4-[3-(3-chlorophenoxy-)propyi]phenyI}-3,9-diazabicyclo[3.3.11noo-6-en-6-yImethyl ester trifluoro-acetate salt
Synthesized according to tj'pical procedures F and E from bicyclononene R2 and S-chlorophenoL LC-MS: R:i= 0.90; ES+; 589.33.
Example 28
(rac.K2-MethoxyphenyI)acetic acid {JR*, 5S*)-3-acetyI-7-{4-[2-(2-chloro-
pheooxy)ethyI]phenyI}-3,9-diazabicyclo|3.3.1]noo-6-en-6-ylmethyl ester
trifluoroacetate salt
Synthesized according to typical procedures F and E from bicyclononene Rl and 2-chlorophenoI. LC-MS: Rt= 0.94; ES+: 575.34.
example 29
'rac.)-{IR% 55*)-3-AcetyI-7-{4-[3-(2-methosybenzyIoxy)propoxylphenyl}-3,9-iiazabicyclo[3^.1]non-6-ene-6-carboxylic acid phenethylamide trifluoro-icetate salt
iynthesized according to typical procedures H and E from bicyclononene Tl and )henethylamine. LC-MS: R i^xample 30
rflc.)-(2-Methoxyphenyl)acetic acid {!&% 55*)-3-acetyl-7-[4-{3-phenoxy-iropyI)phenyl]-3,9-diazabicyclo[3.3.1]noii-6-eD-6-ylmethyI ester trifluoro-cetate salt

Synthesized according to typical procedures F and E from bicyclononene R2 and phenol. LC'MS: R, = 0.87; ESH-; 555.31.
Example 31
l:l-Mixture of (2R)' and {2S)-N-({1R*, 55'*)-3-ace(yl-7-{4-[3-(2-methoxyben-zyIoxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl)-A'-mc-thyl-2-phenyIpropionamide trifluoroacetate salt
Synthesized according to typical procedures G and E fr-oni bicyclononene Z and (rac.)-2-phenylpropiomc acid. LC-MS: Rt = 0.87; ES+: 612.42.
Example 32
(rac.)-{]Ji*, 55*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-di3zabicyclol3.3.1]non-6-ene-6-carboxylic acid 12-(2-methoxyphenyl)ethyl]-amide trifluoroacetate salt
Sjmthesized according to typical procedures H and E from bicyclononene Tl and 2-(2-methoxyphenyl)ethylaimne. LC-MS: Rt = 4.06; ES+: 614.35.
Example 33
(rac.)-(IR*, 55*)-3-Acetyl-7-{4-[2-(2-chIorophenoxy)efhyl]phenyl}-3,9-diaza-bicyclo[3.3.1JnoD-6-ene-6-carboxylic acid mcthylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2-ch)orophenol. LC-MS: Rt = 0.84; ES+: 558.24.
Example 34

irac.)-UR% 55*)-3-Acetyl-7-{4-[2-{2-ethoxyphenoxy)ethyl]phenyl}-3,9-diaza-bicyclo{3.3.11i\on-6-ene-6-carboxyHc acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2'ethoxyphenol. LC-MS; R, = 0.84; ES+: 568.30.
Example 35
(rrtc.)-(i-ff*, J5*)-3-Acetyl-7-{4-I2-{2-acetylphenoxy)ethylJphenyI}-3,9-diaza-bicycIo[3.3.1]non-6-cne-6-carboxylic acid oiethylpheoethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2-acetyIphenol. LC-MS: Rt = 1.13; ES+: 566.29.
Example 36
(rac.)-{lJt*, 55*)-3-Acetyl-7-(4-[2-tf-toluoxyethyIjphenyl}-3,9-diazablcyclo-[3 J.ll-noQ-6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2-methyipheno\. LC-MS:Rf = 1.1S;ES+-. 53S.27.
Example 37
(rac.)-(lR*, 5>9*)-3-Acetyl-7-(4-[2-(3-methosyphenoxy)ethyl]pbenyl}-3,9'di-a2abicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 3-methoxyphenol. LC-MS: R,= 1.15; ES+: 554.28.
Example 38

{rac.y(lR*, 55'*)-3-Acetyl-7-{4-[2-(3-trilluoromethoxyphenoxy)ethyl]phenyI}-3,9-diazabicyclo[3.3.1)non-6-eue-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 3-trifiuoromethoxyphenol. LC-MS; R,- 1.19; ES+: 608.28.
Example 39
(rac.)-(IR% 55*)-3-Acetyl-7-{4-[2-m-toIuoxyethyl]pheiiyl}-3,9-diazabicyclo-[3.3.1]-non-6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 3-mediylphenol. LC-MS: R,= 1.17; ES+: 538.26.
Example 40
{rac.y(lR*, 5^*>-3-Acetyl-7-{4-[2-{3-isopropyIphenoxy)efhyl]phenyl}-3,9-di-azabicycIo[3.3.1]non-6-ene-6-carboxylic acid methylpheoethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 3-isopropylphenol. LC-MSi Rt = 1.19; ES+: 608.28.
Example 41
(rac.)'{lR*, 55'*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyIlphenyl}-3,9-diaz-bicyclo{3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide trifluoro-acetate salt

Synthesized according to typical procedures F and E from bicyclononene U3 and 2-chlorophenol. LC-MS: Rt = 0.87; ES+: 572.13.
Example 42
(/■flc.}-(i-ff*, 55*)-3-Acetyl-7-{4-[3-(2-bromophenoxy)propyI]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 2-bromophenol. LC-MS: Rt= 0.79; ES+: 616.11.
Example 43
(rflc.)-(iff*, ■55*)-3-Acetyl-7-{4-[3-(2-fiuorophenoxy)propyllphenyI}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-'carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 2-fluorophenol. LC-MS: Rt = 0.75; ES+: 556.20.
Example 44
{rac.)-{lR*, 55*)-3-Acetyl-7-{4-[3-(2-acetylpheDOxy)propyI]phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6'Carboxylic acid methylphenethylamide formate salt
Synthesized accordmg to typical procedures F and E from bicyclononene U3 and 2-acetylphenol. LC-MS: Rt = 0.71; ES+: 580.20.
Example 45

(rac.y(ll{*, 5^*)-3-Acet>I-7-{4-[3-i)-toIuoxypropy]Jphenyl}-3,9-dia2abicycIo-[3.3.1]non-6-ene-6-carboxy]ic acid methylphenethylainidc trifluoroacetate salt
Synthesized according to tj-pical procedures F and E from bicyclononene U3 and 2-methylphcno]. LC-MS: Rt = 0.90: ES+: 552.20.
Example 46
rac.)'(JR% 55*)-3-Acetyi-7-{4-[3-(3-methoxyphenoxy)propyI]phei]yl}-3,9-di-izabkycloI3.3.1]noii-6-eije-6-carboxylic acid methyl ph en ethylamide tri-luoroacetate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and -methoxyphenol. LC-MS: R,-0.86; ES+-. 568.21.
jxaraple 47
-ac.yiJR*, 5.S*)-3-Acetyl-7-{4-[3-m-toluoxypropyIlphenyl}-3,9-diazabicyclo-i.3.I]non-6-€ne-6-carboxylic acid methylphenethylamide formate salt
ynthesized according to typical procedures F and E ftom bicyclononene U3 and ■metliylphenoi. LC-MS: Rt - 0.79; ES+: 552.21.
xample 48
ac.)-(lR*, 55*)-3-Acetyi-7-{4-(3-(3-chlorophenoxy)propyI]phenyI}-3,9-di-
^abicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide
ifluoroacetate salt
mthesized according to typical procedures F and E fiom bicyclononene U3 and chlorophenol. LC-MS: R, = 4.44; ES+: 572,32.

Example 49
(rac.yi^R*, 55*)-3-Acetyl-7-{4-[2-{3-bromopheDOxy)ethyI]phenyI}-3,9-dia2a-bieyclo[3.3.1]non-6-ene-6-carboxyIic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 3-bromophenol. LC-MS: R, = 0.78; ES+: 602.10.
Example 50
(rac.)-ilR*, 55*)-3-Acet>'l-7-{4-[2-{2,3-dichlorophenoxy)ethyllpheDyl}-3,9-di-azabicyclo[33.1]non-6-ene-6-carbox7lic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 23-dichlorophenol. LC-MS: R^ = 0.78; ES+: 592.10.
Example 51
{rac.)~iJR*, 55*)-3-Acetyl-7-{4-[2-(2-chloro-3-trif!uoromethylphenoxy)ethyll-phenyI}-3,9-diazabicyclo[33.1]non-6-ene-6-carboxylic acid methylphenethyl¬amide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and
2-chloro-3-trifluoromethylphenol. LC-MS: Rt = 0.80; ES+: 626.11.
Example 52
{rac.yilR*, 55'*)-3-AcetyI-7-{4-[2-(2,3-difIuorophenoxy)ethyllpheQyl}-3,9-di-azabicyclo[3J.lloon-6-ene-6-carboxylic acid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononene U2 and 2,3-difluorophenoL LC-MS: R,= 0.74; ES+: 560.13.
Example 53
{rac.y(lR*, 5S*)-3-Acety!-7-{4-[2-(2,3-dimethylphenoxy)ethyl]phenyl}-3,9-di-a2abicyc\ol3.3.1]non-6-ene-6-carboxyiic acid methylphenethylamidc formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2,3-dimethylphenoI. LC-MS: R, = 0.79; ES+: 559.19.
Example 54
{rac.)-{JR% 55'*)-3-Acetyl-7-{4-[2-{2-ethylphenoxy)cthyliphenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxyIJc acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyciononene U2 and 2-ethylphenol. LC-MS: Rt = 0.80; ES+: 552.19.
Example 55
(rac.)-(JR*, 55'*)-3-AcetyI-7-{4-[3-(3-bromophenoxy)propyl]phenyI}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxyIic acid methylphenethylamide tri-fluoroacetate salt
Synthesized according to typical procedures F and E from bicyclononene XJ3 and 3-bromophenol. LC-MS: Rt ^ 0.92; ES+: 616.05.
Example 56

(rac.y(IR*, 55*)-3-Acety]-7-{4-[3-{2,3-dichlorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphen ethyl amide tri-fluoroacetate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 2,3-dicMorophenol. LC-MS: R, = 0.93; ES+: 606.12.
Example 57
(rac.)-(lR*, 55*)-3-Acetyl-7-{4-[3-(2-chIoro-3-trifluorometfayIphenoxy)-
propyl]phenylJ-3,9-dia2al)icycloI3.3.1]non-6-ene-6-carboxyUc acid methyl-phenethylamide trifluoro acetate salt
Synthesized according lo typical procedures F and E from bicyclononene U3 and 2-chloro-3-trifluoromethylphenol. LC-MS: R, = 0.93; ES+: 640.10.
Example 53
'rac.)-(JR*, 55'*)-3-Acetyl-7-{4-[3-(23-dinuorophenoxy)propyl]phenyI}-3,9-liazabicyclol33.11non-6-ene-6-carboxylic acid methylphenethylamide tri-luoroacetate salt
iynthesized accortUng to typical procedures F and E ftom bicyclononene U3 and !,3-difIuorophenol. LC-MS: R,- 0.88; ES+: 574.17.
(Example 59
rac.y(2R*, 55*)-3-Acetyl-7-{4-[3-(2,3-dimethylphenoxy)propyl]phenyI}-3,9-liazabicyclo[3.3.1]Qon-6-ene-6-carbQxyUc acid methylphenethylamide rifluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononene 1)3 and 2,3-dimethylphenoI. LC-MS: Rt= 0.93; ES+: 566.22.
Example 60
(mc.)-(ii^*, 55*)-3-AcetyI-7-{4-[3-(2-ethylphenoxj')propy]phenyl}-3,9-diaza-bicyclo[3.3.11aon-6-ene-6-carboxyIic acid methylphenefhylamide trifluoro-acetate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 2-ethyiphenoI. LC-MS: R, = 0.93; ES+: 566.22.
Example 61
(rac.)-(lR*, 55'*)-3-Accty 1-7-{4-{3-(2-isopropylphenoxy)propy 11 phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxyIic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 2-isopropylphenol. LC-MS: Rt= 0.86; ES+: 580.22.
Example 62
(rac.y{lR*, 55 *)-3-Acetyl-7-{4-[3-(2-/crt-butylp!ienoxy)propyl] phenyl}-3,9-diazabicycIo[3.3.1]non~6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 2-/erNbutylphenol. LC-MS: Rt = 0.89; ES+: 594.24,
Example 63

(rac.)-{lR*, 55*)-3-Acetyl-7-{4-[3-(4-chloro-2-methoxyphenoxy)propyl]phe-nyl}-3,9-diazabicyclo[3.3.11non-6-ene-6-carboxylic acid methylphenethyl-amide formate salt
Synthesized according to typical procedures F and E from bicyclononene "U3 and 4-chloro-2-methoxyphenol. LC-MS: R,-0.77; ES+i 602.14.
Example 64
{rac.)-{lR*, 55*)-3-Acetyl-7-{4-[3-(2,4-dichlorophenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3.1Inon-6-ene-6-carboxylic ac'*! inHhyiphenethylamide formate salt
Synthesized according to typical procedures F and E from, bicyclononene U3 and 2,4-dichlorophenol. LC-MS: R,= 0.84; ES+: 606.08.
Example 65
(rac.Hi^*. 55*)-3-AcetyI-7-{4-[3-{4-fluo^ophe^oxy)propyIlpheayI}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononene U3 and 4-fluorophenoi. LC-MS: Rt= 0.76; ES+: 556.19.
Example 66
irac.)-{lR*, 55*)-3-Acetyl-7-{4-[3-(2-(ert-butyl-4-methylphenoxy)propyll~
pheny]}-3,9-diazabicyc]op.3.1]DOD-6-ene-6-earboxylic acid metbylpheDetbyl-amide formate salt
Synthesized according to typical procedures F and E firom bicyclononene U3 and 2-rerr-butyl-4-methyIphenoI. LC-MS: R, -0.93; ES+: 608.25.

Example 67
(rac.y(lR*, 55*)-3-Acetj'l-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxjiic acid methylphenethylatnide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 2-bromo-5-fiuorophenoI. LC-MS: R, = 0.80; ES+; 634.05.
Lxample 68
(rac.y(lR*, 55*)-3-Acetyl-7-{4-[3-(2,5-difluoropI]enoxy)propyl|phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxyHc acid methylphenethylamide for¬mate salt
Synthesized according to typical procedures F and E fiom bicyclononene U3 and 2,5-difluorophenoi. LC-MS: R, = 0.76; ES+: 574.14.
Example 69
{rac.)-(lR*, 55*)-3-Acetyl-7-{4-[3-(2-chloro-5-methylpheiiosy)propyl]-
phenyl}-3,9-diazabicyclo[33.1]non-6-ene-6-carbosylic acid methylphenethyl¬amide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 2-chloro-5-methylphenoL LC-MS: R, = 0.82; ES+: 586.16.
Example 70

(rac.)-(lR*, 55*)-3-Acet}'l-7-{4-[3-(2,5-dimethylphenoxy)propyl]pfaenyl}-3,9-diazabicycIo[3.3.11non-6-ene-6-carboxylie acid methylphenethylamide formate salt
Synthesized according to t>'pical procedures F and E Irom bicyclononene U3 and 2,5-dimethylphenol. LC-MS: R, = 0.83; ES+: 566.20,
Example 71
(mc.)-(i-R*, 55*)-3-Acetyi-7-{4-[2-{2-isopropylphenoxy)ethyl]pheoyl}"3,9-di-a2abicyclof3.3.1]non-6-ene-6-carboxylic acid methylphenethyi^'ntde for^nat*" salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2-isopropylpheno!. LC-MS: R, = 0.82; ES+: 566.22.
Example 72
(rac.)-(llt*, 55*>-3-Acetyl-7-{4-I2-(2-ter/-butyIphenoxy)ethyl]phenyl}-3,9-di-azabicyclo[33.1]non-6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2-/e/•^butylphenoI. LC-MS: Ri = 0.85; ES+: 580.26.
Example 73
irac.)-{JR*, 55*)-3-Acet5'l-7-{4-[2-{2-propionylphenoxy)ethyllphenyI}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononene U2 and 2-propionylphenol. LC-MS: R, = 0.72; ES+: 580.21.
Example 74
(rac.)-(lR\ 5S*)-3-Acet>'l-7-{4-[2-(2,4~dichloropbenoxy)ethyIlphenyll-3,9-di-azabicycJo [3.3.1] D on-6-eiie-6-carboA'yIic acid metbylplienethyiamide formate salt
Synthesized accordi;",g lo t'j'pical procedures F and E from bicyclononene U2 and 2,4-dichlorophenol. LC-MS: R, = 0.80; ES+: 592.09.
Example 75
(rac.yilR*, 55*)-3-Acetyl-7-{4-12-(2-/ert-butyl-4-methylphenoxy)ethyl]phe-nyl}-3,9-diazablcyc!o[3.3.1]noii-6-ene-6-carboxyIic acid methylphenethyl¬amide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2-/e/-/-butyl-4-methylphenol. LC-MS: Rt = 0.88; ES+: 594.27.
Example 76
irac.)-{IR*, 55'*)-3-Acetyl-7-{4-t2-(4-methoxyphenoxy)ethyI]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 4-methoxyphenol. LC-MS: Rt= 0.71; ES+: 554.18.
Example 77

{rac.y(lR-, 55*)-3-Acetyi-7-{4-[2-(2-bromo-5-nuorophenoxy)ethyl]plienyI}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carbox\Iic acid mefhylphenethyJamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2-bromo-5-fluoropheno!. LC-MS: Rt = 0.76; ES+: 620.09.
Example 78
(mc.)-(;" , 5o*^;-3-Acctyl-7 ;4-^2-{2,5-dinuo^ophenoxy)ethyl]phenyl}-3,9-di-azabicyclo[33.^]noD-6-ene-6-carboxyUc acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2,5-difluorophenol. LC-iMS: Rt = 0.73; ES+: 560.17.
Example 79
{rac.y{lR*, 5>S*)-3-Ac€tyl-7-{4-[2-(2-chloro-5-methylphenoKy)ethyllphenyli-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxyIic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2-chloro-5~methylphenol. LC-MS: Rt = 0.78; ES+: 572.13.
Example 80
{rac.)-{lR*, 55*)-3-Acetyl-7-{4-(2-(2-methoxy-5-methylphenoxT)ethyI!phe-nyl}-3,9-diazabicyclo(3.3.11noii-6-ene-6-carboxyIic acid methylphenethyl¬amide formate salt

Synthesized according to typical procedures F and E from bicyclononene U2 and 2-methoxy-5-methylphenol. LC-MS: Ri - 0.72; ES+; 568.19.
Example 81
(rac.)-(iif* 55*)-3-Acetyl-7-{4-[2-(2,5-dimethylpIienoxy)ethyl]phenyl}-3,9-di-azabicyclo[3.3.11iion-6-ene-6-carboxylic acid raethylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2,5-dimethylphenol. LC-MS: R, = 0.90; EZ i: 552.24.
Example 82
(raC.yUR*, 55*)-3-AcetyI-7-{4-[2-(2-chlorophenoxy)ethoxy]phenyl}-3,9-di-azabicyclop.3.1]noii-6-ene-6-carboxyIie acid metbylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene Ul and 2-(2-chlorophenoxy)ethanol. LC-MS: Rt = 0.75; ES+: 574.15.
Example 83
(racHlR*, J5*)-3-Acetyl-7-{4-[2-(3-methylphenoxy)ethoiy]phenyI}-3^-di-azabicydo [3.3.1] Don-6-ene-6-carbo%ylic acid metbylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene Ul and 2-(3-methyIphenoxy)ethanol. LC-MS: Rt = 0.76; ES+: 554.18.
Example 84

(rac.)-(lR*, 5>5*)-3-AcetyI-7-{4-12-(2-chlorophenyl)ethoxylphenyl}-3,9-diaza-blcyclo[3.3.1]non-6-ene-6-carboxyIic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene Ul and 2-(chlorophen\-l)ethanoI. LC-MS: R, - 0.77; ES+: 558.13.
Example 85
{rac.y{lR*, 55*)-3-AcetyI-7-{4-[2-(3-chiorophenyi)ethoxyiphenyI}-3,9-diaza-bicycIo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene Ul and 2-(3-chlorophyl)ethanol. LC-MS: R, = 0.77; ES+: 558.14.
Example 86
{rac.)-(lR*, 55*)-3-Acetyl-7-{4-[2-(2-methoxypheDyl)ethoxy]pheiiyl}-3,9-di-azabicyclo[33.11non-6-ene-6-carboxyIic acid methylphenethylamide trifluo-roacetate salt
Synthesized according to typical procedures F and E &om bicyclononene Ul and 2-(2-methoxyphyl)ethanol. LC-MS: Rt = 0.85; ES+: 554.21.
Example 87
{rac.yilR*, 55'*)-3-Acetyl-7-(4-[2-(2,5-dichIoropheooxy)ethyIIphenyl}-3,9-di-azabicyclo[33.1]non-6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2,5-dichlorDphenol. LC-MS: Rt = 0.79; ES+: 592.07.

Example 88
(rac.)-(lJi*, 55*)-3-Acetyl-7-(4-[2-(2,3,6-trifluorophenoxy)ethyI]phenyi}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2,3,6-trifluorophenol. LC-MS: Ri = 0.74; ES+: 578.14.
Example 89
(rac.y(lR% 5^*)-3-Acetyl-7-{4-[2-(3,5-dimethylphenoxy)ethyl]phcnyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxyHc acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 3,5-dmiethylphenol. LC-MS: Rt= 0.80; ES+: 552.20.
Example 90
{rac.y{lR*, 55*)-3-Acetyl-7-E4-12-(3-chlorophenosy)etbyl]phenyl}-3,9-di-
azabicycIo3.3.1jnon-6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 3-chlorophenol. LC-MS: ^ = 0.77; ES+: 558.15.
Example 91
{rac.y{lR*, 55*)-3-Acetyl-7-{4-t2-(3-trifluoromethylphenoxy)ethyIlphenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononene U2 and 3-trifluoromeihylphenol, LC-MS: R, = 0.78; ES+: 592.17.
Example 92
{rac.)-{lR*, 55*)-3-Acet5!-7-{4-[2-(4-rert-hutyl-2-methylpbenoxy)etbyI]-
phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethyl-amide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 4-rerr-butyl-2-methylphenol. LC-MS: R, = 0.88; ES+; 594.22.
Example 93
(rac.yilR*, 55*)-3-Acetyl-7-{4-[2-(3,4-dichlorophenoxy)ethyl]phenyI}-3,9-di-azabicyclo[33.1jnon-6-eDe-6'Carboxyllc acid methylphenethylatnide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 3,4-dichlorophenol. LC-MS: Rt = 0.81; ES+: 592.12.
Example 94
{rac.)-{lR*, 55*)-3-AcetyI-7-{4-[2-(4-bromo-3-methyIphenoxy)efhyI]phenyl}-3,9-diazabicycio(3.3.1]non-6-ene-6-carboiyiic acid methyiphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 4-bromo-3-methylphenol. LC-MS: Ri = 0.81; ES+-. 616.12.
Example 95

(rac.y(lR*, 5^*)-3-Acetyl-7-(4-[2-(3,4-dimethylphenoxy)ethyllphenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 3,4-dimethyIphenol. LC-MS: Rt = 0.78; ES+: 552.18.
Example 96
yrac.y{iR\ 5^^-)-3-At;ciyI-7-{4-[2-(3,5-dichIorophenoxy)ethy!]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-eae-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 3,5-dichlorophenol. LC-MS: Ri = 0.82; ES+: 592.10.
Example 97
(_rac.)-(lR% 55'*)-3-Acetyl-7-{4-{2-(3^-dimethylphenoxy)ethyiJphenyl}-3,9-di-azabicyclo[3.3.1]noa-6-ene-6-carboxyUc acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 3,5-dimethylphenol. LC-MS: R* = 0.79; ES+: 552.20.
Example 98
{rac.)-{lR*, 5S*)-3-Acetyl-7-{4-i2H3,5-diraethoxypheQOxy)ethyl]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxy!ic acid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononene U2 and 3,5-dimethox\-phenol. LC-MS: Rt= 0.72; ES+: 584.19.
Example 99
(rac.)-(lR*, J5*)-3-Acetyl-7-{4-[2-{2-chloro-4,5-diraethyIphenox>')ethyliphe-nyl}-3,9-diazabicyclo[3.3.1]iion-6-ene-6-carboxyUc acid methylpheaethyl-amide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2-dichlorG-4,5-dLncthy:phcnoI. LC-MS: R, = O.S 1; ES+: 586.17.
Example 100
(mc.)-(i-«*, 55*)-3-Acetyl-7-{4-[2-(2.3,5-triinethylphenoxy)etliyl]phenyi}-3,9-diaxabi6yclo[33.1]noD-6-eQe-6-carboxylic acid methylpfaenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2,3,5-trimethylphenoI. LC-MS: R^ = 0.82; ES+: 566.21.
Example 101
(rac.)-iJR*, J5'*)-3-Acetyl-7-{4-13-(2,5-dichlorophenoiy)propyl]phenyl}-3,9-diazabicyclo[3,3.11non-6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 2,5-dichlorophenol. LC-MS: Rt = 0.83; ES+: 606.12.
Example 102

(rac.)-(lR% 55*)-3-Acetyl-7-{4-[3-(2-acetyI-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.11non-6-ene-6-carboxylie acid methyiphencthyf amide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 2-acetyI-5-fluorophenol. LC-MS: Rt = 0.73; ES+: 598.18.
Example 103
(racHi-R*, 55*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-dia2abicycIo[3.3.1]non-6-ciie-(;-carboxyIic acid methylpheDethylamide trifluoroacetate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 2,3,6-trifluorophenol. LC-MS: R, = 0.88; ES+: 592.19.
Example 104
(rac.)-(]R*, 55*)-3-AcetyI-7-{4-{3-(2,4-dimethylphenoxy)propyIl phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxyIic acid metliylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 2,4-dimethylphenol. LC-MS: R^ = 0.83; ES+: 566.22.
Example 105
{rac.)-{lR*, 55*)-3-AcetyI-7-{4-[3-(2-tert-butyl-6-methylphenoxy)propyl]phe-ByI}-3,9-diazabicyclo[3.3.1]noo-6-ene-6-carboxylic acid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononene U3 and 2-/ert-butyl-6-methylphenol, LC-MS: R, - 0.88; ES+: 608.27.
Example 106
{rac.y{lR*, 55*)-3-Acet}J-7-(4-[3-(4-te/'/-butyI-2-methylphenoxy)propylJphe-nyi}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid m ethyl pheoethyl-amide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 euid 4-/err-butyl-2-methyIphenoI. LC-MS: R, - G.93; EE+: 608.25.
Example 107
{rac.)-{lR*, 5S*)-3-Acetyl-7-{4-[3-(3,4-dichl(irophcnoxy)propyl]phenyl}-3,9-diaz;abicyclot3.3.1Iaon-6-eae-6~carhoxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 3,4-dichlorophenol. LC-MS: R( = 0.84; ES+: 606.12.
Example 108
{rac.y{lR*, 55*)-3-Acefyl-7-{4-[3-(4-bromo-3-methylphenoiy)propyIJphe-nyl}-3,9-diazabic5'clo[3.3.1]non-6-ene-6-carboxylic acid methylphenethyl-amide formate salt
Synthesized accordmg to typical procedures F and E from bicyclononene U3 and 4-bromo-3-methylphenol. LC-MS: R^ = 0.85; ES+: 630.11.
Example 109

(rac.y{JR*, 5S'*)-3-Acetyl-7-{4-[3-(3,4-diraethyIpheiiDxy)propyI]phenyI}-3,9-diazabicycIo[3.3.1}non-6-ene-6-carboxyiic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene US and 3,4-dimethylphenol. LC-MS: R, = 0.82; ES+: 566.20.
Example 110
(rac.)-{lR*, 55*)-3-Acetyl-7-{4-[3-(3,5-dichlorophenoxy)propyl]phenyI}-3,9-diazablcyclo[3.3.1]non-^-ene-6-carboxyIic acid inethylpheE:;thyl:;!::!de-formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 3,5-dichIorophenol. LC-MS: Rt = 0.87; ES+: 606.13.
Example 111
irac.)-{lR*, 55*)-3-Acetyl-7-{4-l3-(3^dimethylphenoxy)propyl]phenyl}-3,9-diazabicycIo[33.1]non-6-ene-6-carboxylic acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and 3,5-dimethylphenol. LC-MS: R, = 0.82; ES+: 566.21.
Example 112
(rac.)-{lR*, 55*)-3-AcetyI-7-{4-[3-{2-ch]oro-4,5-dimethylphenoxy)propyl]phe-nyl}-3,9-diazahicyclo[3.3.11non-6-ene-6-carboxylic acid methylphenethyl¬amide formate salt

Synthesized according to typical procedures F and E from bicyclononene U3 and 2-chloro-4,5-dimethylphenol. LC-MS: R, = 0.85; ES+: 600.18.
Example 113
{rac.)-{lR*, 55*)-3-Acetyl-7-{4-[3-(23,5-trimethylphenoxy)propyl]phenyl}-3,9-diazabicyclQ[3.3.1]noD-6-ene-6-carboxylic acid methyiphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene U3 and
2,3,5-trimediylphenol. LC-MS: Rt = 0.86; ES+: 580.23. ..... .^....
Example 114
(/■ac.)-Acetic acid {IR*, 55*)-2-{7-{4-I3-(2-chlorophciioxy)propyl]phenyli-6-{[2-(2-chlorop henyl)ethyl] met hylcarbamoy I}-3,9-diaza bicycio [3.3.1] non-6-eii-3-yl)-2-oxoethyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AC and acetic acid chlorocarbonyhnethyl ester. LC-MS: Rt= 1.01; ES+: 664.14.
Example 115
(rac.)-(ijR*, 55*)-7-{4-[3-(2-Cfaloropbenoxy)propyl]phenyl}-3-(2-cyanoacetyl)-3,9-diazabicycIo[33.1]non-6-ene-6-carboxyIic acid [2-(2-chIoropheDyl)ethyl]-methylamide formate salt
Synthesized according to typical procedures K and E from bicyclononene AC and cyanoacetic acid. LC-MS; R^ - 1.02; ES+: 631.13.
Example 116

(rac.)-{llt*, 55*)-3-(2-Acetylaminoacetyl)-7-{4-[3-(2-cfalorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non"6-ene-6-earboxylic acid [2-(2-cUIoro-phenyl)ethyl]methylamide formate salt
Synthesized according to typical procedures K and E from bicyclononene AC and acetylaminoacetic acid. LC-MS; Rt = 0.96; ES+: 663.14.
S-xample 117
1:1 Mixture of (IR, 55)-3-((-/5)-2-acetyIamino-4-methyipentanoyI)-7-{4-[3-(2-chloroph enoxy) propyl] phenyl}-3,9-diazablcyclo [3.3.1 ] non-6-ene-6-carboxy lie add E2-(2-chlorophenyl)etbyI]methylainide formate salt and (IS, 5R)-3-{(4S)-2-acetyl-amino-4-metliyIpentanoyl)-7-{4-[3-(2-chiorophenoxy)propyl]plie-nyl}-3,9-diazabicyclo[3.3.1]non-6-enc-6-carbosylic acid [2-(2-chlorophenyl)-ethyl]methylamide formate salt
Synthesized according to typical procedures K and E from bicyclononene AC and acetyl leucine. LC-MS: R^ = 1.05; ES+: 719.19.
Example 118
(racyilR*, 55*)-3-Acetyl-7-{4-[3-(2-chloropfaenoxy)propyl]phenyl}-3,9-di-azab icy clo [3.3.lino n-6-ene-6-carboxyUc acid [2-(2-chloropheDyl)ethyll-methylamide formate salt
Synthesized accordmg to typical procedures G and E from bicyclononene T2 and [2-(2-chlorophenyl)ethyl]methylamine (Jaques B.; Wallace R. G., Tetrahedron, 1977, 33, 581). LC-MS: Rt = 0.90; ES+: 606.08.
Example 119

(racyilR*, 55*)-3-AcetyI-7-{4-[3-(2-chlorophenoxy)propyI]pfaenyl}-3,9-di-azabicycIo[3,3.1]non-6-ene-6-carboxylic acid (2-hydroxybeiiz>i)niethylainide formate salt
Synthesized according to typical procedures G and E &om bicyclononene T2 and 2-methyIarainom.ethyIphenol (Ross S. D., et al; J. Org. Chem., 1966, 3!, 133). LC-MS: R,= 0.83;ES+: 574.10,
Example 120
(tac'j-ilJi*, 55*)-3-AcetyI-7-{4-[3-(2-chIoropfaenoxy)propylJphenyl}-3,9-di-azabicyclo[3.3.11non-6-ene-6-carboxyIic acid (2-chlorobenzyl)cycIopropyl-amide formate salt
Synthesized according to typical procedures G and E &om bicyclononene T2 and (2-chlorobenzyl)cycIopropylanune. LC-MS: R, = 0.92; ES+: 617.94.
Example 121
1:1 Mistnre of {rac.)-{lR*, 55*)-3-acetyl-7-{4-[3-(2-chlorophenoiy)propyll-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid J(5JI*)3-(2-ch!oro-phenyl)butyl]methylamide formate salt and (rac)-(lR*, 55*)-3-aeetyl-7-{4-[3-(2-chlorophenoiy)propyll-phenyI}-3,9-diazabicyclol3.3.11iH>n-6-ene-6-carbo-lylic acid [(55'^)~3-(2-chloropheayI)bu(yl]methylamide formate salt
Synthesized according to typical procedures G and E fiom bicyclononene T2 and (rflc.)-methy!(3-phenylbutyl)amine (Meyers A. I., et al.; J. Am. Chem. Soc, 1982, 104, 877). LC-MS: Ri = 0.91;ES+: 600.13.
Example 122

{rac.y(lR*, 55*)-3-Acetyl-7-{4-[3-(2-chIorophenoxy)propyI]phenyl}-3,9-di-azabicycIo[3.3.1Inon-6-ene-6-carboxylic acid methyl-(4-piienylbutyl)amide formate salt
Synthesized according to typical procedures G and E from bicyclononene T2 and methyl{4-phenylbutyl)amine (Neale R. S., et ah; J. Org. Chem., 1965, 30, 3683). LC-MS: Rt= 0.91; ES+: 600.20,
Esample 123
(racy{lR*, 55*>-3-Acetyl-7-{4-[3- Synthesized according to typical procedures G and E from bicyclononene T2 and rnethyl(3-phenoxypropyl)amine. LC-MS: R( = 0.88; ES+: 602.09.
Example 124
(rac)-{lR*, 55*)-3-Acetyl-7-{4-[3-(2-chIorophenoxy)propyl]phenyl}-3^-di-azabicyclo]3.3.1]non-6-ene-6-carboxylic acid metfayl-(4-phenylpentyI)amide formate salt
Synthesized according to typical procedures G and E from bicyclononene T2 and methyl(5-phenylpentyl)aniine (Neale R. S., et al.;J. Org. Chem., 1965, 30, 3683). LC-MS; R, = 0.95; ES+: 614.12.
Example 125
(rac.)-(JK* 5S*)-3-Acetyl-7-14-[3-(2-chIorophenoxy)propyllpheiiyl>-3,9-di-azabicyclo[3.3.1]noD-6-ene-6-carboxylic acid (3-ben2o[l,31dioxol-5-ylpropyl)-methylamide formate salt

Synthesized according to typical procedures G and E from bicyclononene T2 and (3-benzo[i,3]dioxol-5-ylpropyl)methylamine (Dallacker, et al; Chem. Ber., 1971, 104, 2517). LC-MS: Rt = 0.86; ES+: 630,10.
Example 126
(racyiJR*, 5>5*)-3-Acetyi-7-{4.[3-(2-chlorophenoxy)propyl]phenyl}-3,9-di-azabicyclol3.3.1]non-6-ene-6-carboxyIic acid [2-(4-methoxypIieDOxy)ethyl]-methylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene T2 and [2-(4-methox>phenoxy)ethyI]methyianiine. LC-MS: R, = 0.84; ES+: 618.03.
Example 127
(rac)-(i^* 55*)-3-Acetyl-7-{4-[3-(2-chIorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid [2-(4-chIorophenoxy)ethyI]-metbylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene T2 and [2-(4-chlorophenoxy)ethyl]methylamine. LC-MS: Rt= 0.90; ES+; 622.03.
Example 128
(rac.)-(lR*, 55*)-3-AcetyI-7-{4-[3-(2-chlorophenoxy)propyl]pheDyl}-3,9-
diazablcycIo[3.3.1]noD-6-ene-6-carboxylic acid methyl-(2-^-tolyIoxyethyl)-amide formate salt
Synthesized according to typical procedures G and E from bicyclononene T2 and (2-/7-toly!oxyethyl)methyiaraine. LC-MS: Ri= 0.89; ES+: 602.08.

Example 129
(rac.)-(lR*, 55*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyI]pheQyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carboxylic acid diethylamide formate salt
Syntliesized according to tyf>icai procedures G and E from bicyclononene T2 and diethylaraine. LC-MS: R,= 0.79; ES+: 510.06.
Example 130
(rac.)-{lR*, 55'*)-3-Ace(yl-7-{4-(3-(2-chloropheilOAj)pro^yllpheily!}-3,*»-di-azabicycIo[3.3.1]non-6-ene'6-carboxylic acid metbyI-(2-pyridin-2-ylethyl)-amide formate salt
Synthesized according to typical procedures G and E from bicyclononene T2 and
ethyl(2-pyridin-2-ylethyl)amine. LC-MS: R, = 0.89; ES+: 602.08.
Example 131
{IS, 5;f)-3-Acetyl-7-{4-p-(23,6-trinuorophenoxy)ethyl]phenyI}-3,9-diaza-bicyclo[33.1]non-6-ene-6-carboxylic acid methylphenethylamide
Synthesized according to typical procedures F and E fi:om bicyclononene BJ and 2,3,6-trifluorophenol. LC-MS: Rt = 0.94; ES+: 592.19. ee=80%.
Example 132
l:l-Mixture of irac.)-{lR*r 55*>3-acetyl-7-(4-[3-(2-bromo-5-fluoropbenoxy)-propyi]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclo-propyl-[2-((2ii*)-2,3-dihydroxypropyl)benzyll amide trifluoroacetate salt and (rac.y(lR*, 5iS'*)-3-acetyl-7-(4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-

3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxyIic acid cyclopropyl-[2-{(2iS'*)-2,3-dihydroxypropyl)benzy!l amide trtfluoroacetate salt
Synthesized according to typical procedure E from bicyclononene AT. LC-MS: R,-3.99; ES+: 720.49.
Example 133
irac.)-(lR*, 55*)-3-AcetyI-7-{4-[3-(2-bromo-5-fluoropheDoxy)propyIJphenyI}-
3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxy]ic acid cycIopropyl-[2-(2-
-hydroxyethyl)benzylJamide trifluoroacetate salt
Synthesized according to typical procedure E from bicyclononene AV. LC-MS; Rt= 3.94; ES+: 692.77.
Example 134
(rac.}-(lR*, 5iS'*)-3-AcetyI-7-{4-[3-(2-bromo-5-fluorophenoxy)propylJphenyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid benzylcyclopropylamide formate salt
Synthesized according to typical procedures H and E frt)m bicyclononene AJ4 and benzylcyclopropylamine. LC-MS: Rt = 0.89 ES+: 646.41.
Example 135
{rac)'{lR*, 55*)-3-Acetyl-7-{4-I3-(2-bromo-5-fluoro-phenoiy)propyl]-
phenyI}-3,9-diazabicydo[3.3.l]non-6-eBe-6-carboxylie acid (2-chlorobenzyi)-ethylamide formate salt
Synthesized according to typical procedures H and E Irom bicyclononene AJ4 and(2-chlorobenzyi)ethyIair[ine. LC-MS: R, = 0.91 ES+: 668.44.

Example 136
irac.)-(lR*, J5*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-enc-6-carboxj'lic acid cyclopropyK2-fluoro-beiizyl)ainide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ4 and (2-fluoroben2yl)cyclopropyJamine. LC-MS: Rt= 0.90 ES+; 664.46.

Example 15

I-

(racy{lR*, 55*)-3-AcetyI-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyI}-3,9-diazabicyclo[3.3.1]noii-6-ene-6-carboxylic acid cyclopropyl-(2-methyl~ benzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ4 and (2-methylbenzyl)cyclopropylamine. LC-MS: Ri = 0.92 ES+: 660.47.
Example 138
{rac)-{lR*, J5*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyllphenyl}-3,9-diazabicyclo [33,l]non-6-€ne-6-carboxyIic acid cy c!opropyI-t2-(4-nietfaoxyphenoxy)ethyll amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ4 and cyclopropyl[2-(4-methoxyphenoxy)ethyl]aniine. LC-MS: Rt = 0.90 ES+:
706.44.
Example 139

(rac.)-(lR*, 55*)-3-Acetyl-7-{4-[3 Synthesized according to typical procedures H and E from bicyclononene AJ4 and cyclopropyl[2-(3-methylphenoxy)ethyijaraine. LC-MS: Rt = 0.93 ES+: 690.47.
Example 140
(rac.)-\iii*i Jj";-3-AcetyI-7-{4-[3-(2-bronio-5-fluoropheiioiy)propyl]phenyI}-339-diazabic>"c!o(3.3.1]non-6-cne-6-carboxylic acid cyclopropyl-[2-(3,4-diinethyIphenoxy)ethyIlamide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ4 and cyclopropyl|;2-(3,4-diniethylphenoxy)elhyl]amine. LC-MS: Rt = 0.94 ES+-. 704.48.
Example 141
(rac)-{lR*, 55*)-3-Acetyl-7-{4-[3-{2-bromo-5-fluorophenoxy)propyiJphenyl}-3,9-diazabicyclo{33.1Jnon-6-ene-6-carboxyIic acid cyclopropylpheuethyl-amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ4 and cyclopropylphenethylamine. LC-MS: R, = 0.90 ES+: 660.50.
Example 142
{rac.)-{lR*, 55*)-3-Acety 1-7-{4-[3-{2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclol3.3.11oon-6-ene-6-carboxylic acid [2-(2-chlorophenyl)ethyl]-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononene AJ4 and [2-(2-chloroplienyl)ethyl]cyclopropylamine. LC-MS: Rt = 0.92 ES+: 694.44.
Example 143
{rac.)-{lR*, 55*)-3-AcetyI'7-{4-[3-(2-bromo-5-fluorophenoxy)propyi]phenyI}-3,9-diazabicycloI33.1]non-6-ene-6-carboxylic acid cyclopropyl-[2-(23-difluorophenyl)ethyl]aniide formate salt
Synthesized aucoiJing to typical piot;edtucs H and E from bicyclononene AJ4 and [2-{2,3-diiluorophenyl)ethyl]cyclopropylamine. LC-MS: Rt = 0.91 ES+: 696.47.
Example 144
{rac.y{lR*, 55*)-3-Acefyl-7-(4-[3-(2-bromo-5-fluoropheBioxy)propyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyHc acid cyclopropyl-l2-(4-fluoro-phenyl)ethyl] amide formate salt
Syntiiesized according to typical procedures H and E from bicyclononene AJ4 and [2-C4-fluorophenyl)ethyl]cyclopropylamine. LC-MS: R* = 0.91 ES+: 678.53.
Example 145
{racyilR*, 55*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluoropheDOxy)propyl]phenyl}-
3,9-diazabicyclo[3.3.1]noii-6-ene-6-carboxylic acid cyclopropyl-(2-o-
toIy]ethyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ4 and [2-(2-methyIphenyI)ethyl]cycIopropylaniine. LC-MS: Rt - 0.92 ES+: 674.55.

Example 146
l:l-Mixture of (rac.)-(lR*, 55*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyi]phenyI}-3,9-diazabicyelo[3.3.1]aon-6-ene-6-carboxylic acid iX2R*)-2-hydroxy-2-phenylethyl)methylamide formate salt and (rac.)-{lR*, 55*)-3-acet}i-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyI)-3,9-diazabicycl-o[3.3.1]noQ-6-ene-6-carboxylic acid {(2S*)-2-hydroxy-2-phenylethyI)methyl-amide formate salt
Synthesized according to typical procedures G and E from blcyclononeQe AJ4 and a-(methylaniinomcdiyi)boii^yl a:vo;-.bl.-XC-MS: Rt = 0.85 ES+: 650.49.
Example 147
(rac.)-{lR*, 5xS'*)-3-Acetyl-7-{4-[3-(2-bromo-5-fiuoropheiioxy)propyIJphenyl}-3,9-diazabicyclo[3.3.1]noD-6-ene-6-carboxylic acid cyclopropyl-(3-trifluoro-methy!benzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ4 and (3-trifluoromethylbenzyl)cyclopropylamine. LC-MS: R, = 0.93 ES+: 714.40.
Example 148
irac)-(lR*, 5^*)-3-Acetyl-7-{4-[3-(2^,6-trifluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo(3.3.1Jnon-6-ene-6-carboxyIic acid cycIopropyl-(2-o-tolyIethyl)-amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ4 and [2-(2-metliylphenyl)et!iyl]cyc!opropylamine. LC-MS: Rt = 0.90 ES+: 632.51.
Example 149

{racYilR", 55'*)-7-{4-[3-(2,3,6-Trinuorophenoxy)propylphenyI}-3,9-diaza-bicycIo[3.3.1]non-6-ene-6-carboxylicacid (2-chloi'obeazyl)cyclopropylamide
Synthesized according to typical procedure E from bicyclononene AL2 and purification by FC. LC-MS: R, = 0.84 ES+: 596.30.
Example ISO
(rac.)-5-{(iJ?*, 5^*)-6-I(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(23,6-
trifluoroph en oxy)propylphenyl}-3,9-diazabicycIo 13.3.1 ]non-6-en-3-yI)-5-oxo-
pentanoic acid formate salt _
Synthesized according to typical procedures K and E from bicyclononene AL2 and glutaric anhydride. LC-MS: R, = 0.87 ES+: 710.42.
Example 151
{rac.y(lR*, 55*H-I(2-Chlorobenzyl)cyclopropylcarbamoylJ-7-{4-[3- Synthesized according to typical procedure L from bicyclononene AK2 and. LC-MS: Rt= 1.06 ES+: 798.34.
Example 152
(rac)-iJR*, 55*)-6-[(2-Chlorobenzyl)ethylcarbamoyll-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl] phenyl)-3,9-diazabicycIo [33. l]non-6-ene-9-carboxyUc acid 2,2,2-trichloro-l,l-dimethylefhyI ester hydrochloride salt
Synthesized according to typical procedure L from bicyclononene AK4 and. LC-MS: R,= 1.19 ES+; 7g8.25,

Example 153
{rac.y(lR% 55*)-6-[(2-Fluorobenzyl)cyciopropykarbamoyI]-7-{4-(3-(2^,6-trifiuoropheDoxy)propyl] phenyl)-3,9-diazabicyclo [3.3.1] non-6-ene-9-carbo-xylic acid 2,2^-trichloro-l,l-dimethylethyl ester hydrochloride salt
Synthesized according to typical procedure L from bicyclononene AK5. LC-MS: Rt=1.18ES+: 784.27.
Example 154 ■ "./ -^--'
{rac.)-(lR*, 5^*)-6-[(2-Methylbenzyi)cyclopropylcarbamoyl]-7-{4-[3-(2^,6-triflaorophen oxy)propyl] phenyl} -3,9-dlazah icy do [3.3. llnon-6-ene-9-carbo-xylic acid 2,2^-tricfaloro-l,l'dimethylethyI ester hydrochloride salt
Synthesized according to typical procedure L from bicyclononene AK7. LC-MS: R,= 1.21 ES+: 780.29.
Example 155
(racH^R*, J5'*)-6-[Cyclopropyl-(2-o-toIylethyI)carbamoyl]-7-{4-[3-(23,6-trifluorophenoxy)propyl]phenyl}-3,9-diaza bicycle [3.3.1] non-6-ene-9-carbo-
xylic acid 2,2^-tricbloro-l,l-dimethylethyI ester hydrochloride salt
Synthesized according to typical procedure L from bicyclononene AK16. LC-MS: Rt= 1,21 ES+: 794.30.
Example 156

(rac.)-{lS*, 55*)-6-[CyelopropyI-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(23j6-trifluoroplienoxy)propyl]pheiiyi}-3,9-diazabicycio[33.1jDOD-6-ene-9-carboxylic acid 2,2,2-trichIoro-l,l-dimethyletbyl ester hydrocbloride salt
Synthesized according to typical procedure L from bicyclononene AK17. LC-MS:Rt=1.16.
Example 157
{rac.)-{JR*, 55*)-6-[CydopropyI-(2-p-tolyiethyl)carbainoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo [3.3.1] non-6-ene-9-carbt>-xylic acid 2^,2-trichloro-l,l-dimethylethyl ester hydrochloride salt
Synthesized according to typical procedure L from bicyclononene AK18. LC-
MS:Rt= 1.22 ES+: 794.30.
Example 158
{racy5-{{lR*, 55*)-6-[(2-Chlorobenzyl)cycIopropylcarbamoyll-7-{4-[3-(23,6-trifluorophenoxy)propyllphenyl}-3^-diazabicyclo [3 J. 1 ] non-6-eii-3-yI)-2^-dimethyI-5-oxo-pentanoic acid formate salt
Synthesi2ed according to typical procedures K and E from bicyclononene AL2 and 2,2-dimethylglutaric anhydride. LC-MS: Rt = 0.91 ES+: 738.52.
Example 159
(rac.yS-iilR*, 55*)-6-[(2-Chloroben2yl)cyclopropylcarbamoyl]-7-(4-[3-(2,3,6-trlfluorophenoxy)propyl]phenyl}-3,9-diazabicyc!o[3.3.1jnon-6-en-3-yl)-5-oxo-pentanoic acid methyl ester formate salt

Synthesized according to typical procedures A and E from bicycloBonene AL2 and glutaric acid monomethylester chloride. LC-MS: I^ = 0.93 ES+: 724.49.
Example 160
l:l-Mixture of (IR, 5S)-3'((}S, ^7;)~4-hydroxypyrroIidine-2-carbonyi)-7-{4-J3-{23,6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicycIo[3.3.1]noa-6-ene-6-carboxyUc acid (2-chlorobenzyl)cyclopropylamide formate salt and {IS, 5fl)-3-((iS, 4il)-4-hydrDxypyrrolidine-2-carbonyl)-7-{4-{3-(2^,6-trifluoro-phenoxy)propyllphenyI)-3,9-diaxabicyclo{3.3.11noa-6-ene-6-carboxylic acid (2-chIoruben2yl)cycIopropylamide formate salt
Synthesized according to typical procedures G, E and L from bicyclononene AL2
and BOC-L-hydroxyproline. LC-MS: R, = 0.80 ES+: 709.38..
Example 161
(rac.)-(i^% 55*)-3-(4-CarbamDylb«tyTyl)-7-{4-I3-{23,6-trifluorophenoxy)-propylIphenyl)-3,9-diazabicyclo(3.3.1)noB-6-eiie-6-carb«xyUc acid (2-chloro-benzyl)cyclopropylafflide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL2 and 4-carbamoylbutyric acid. LC-MS: Rt = 0.86 ES+: 709.38.
Example 162
irac.y{lR*, 55*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3.6-trinuorophenoxy)-propyl] phenyl}-3,9-diazabicyclo[3.3.11non-6-enc-6-carboxylic acid benzyl-
cyclopropylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL3 and 4-carbamoylbutyric acid. LC-MS: Rt = 0,84 ES+: 675.49.

Example 163
[rac.y{lR-^, 55*)-3-(4-CarbaraoylbutyryI)-7-{4-{3-(2,3,6-trifluorophenoxy)-propyl|phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid (2-chloro-benzyl)ethylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL4 and 4-carbamoylbutyric acid. LC-MS: Rt = 0.86 ES+: 697.40.
Example 164 -
{rac.)-(lR*, 55'*)-3-(4-CarbamoyIbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[33.11non-6-ene~6-carboxylic acid cyclo-propyl-(2-fluorobea2yI)amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL5 and 4-carbamoylbutyric acid. LC-MS: R, = 0.85 ES+: 693.43.
Example 165
{racy-ilR*, 55*)-3- propyllphettyl}-3,9-diazabicyclo [33.1] non-6-ene-6-carboxy lie acid
cyclopropyl-{3-trifluoromethyIbenzyI)amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL6 and 4-carbamoylbutyric acid. LC-MS: %, = 0.88 ES+: 743.4L
Example 166

{rac.)-(lR*, 55'*)-3-(4-CarbamoylbutyryI)-7-{4-[3-(23,6-trifluorophenoxy)-propy!]phenyJ}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cycio-propyl-{2~methylbenzyl)amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL7 and 4-caTbamoylbutyric acid. LC-MS: Rt = 0.86 ES+: 689.47.
Example 167
irac.)-(lR% 55*)-3-(4-CarbamoyIbutyryl)-7-{4-[3-(23,6-trinuorophenox)0-propylJpIitiiy:}-3,3-diazabicyi:c[3J.IInoQ-6-ene-6-carboxyiic acid cycio-propyl-[2-(4-methoxyphenoxy)ethyl]amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL8 and 4-carbamoyibutyric acid. LC-MS: Rt = 0.85 ES+: 735.47.
Example 168
(rac.y{JR*, 55*)-3-{4-CarbamoylbutyryI)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl] phenyl}-3,9-diazabicyclo [3.3. l]non-6-ene-6-carboxy lie acid cyclo-propyl-[2-(3-methoxyphenoxy)ethyl] amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL9 and 4-carbamoylbutyric acid. LC-MS: Rt = 0.86 ES+: 735.47.
Example 169
(racHlR*, 55*)-3-{4-Carbamoylbutyryl)-7-{4-l3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclo-propyl-(2-Hi-tolyloxyethyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononene ALIO and 4-carbamoy!butyric acid. LC-MS; Rt = 0.87 ES+: 719.46.
Example 170
(rac.)'QJf*> i5*)-3-{4-Carbamoylbutyryl)-7-{4-[3-(23,6-trinuorophenoxy)-propyI]phenyI}-3,9-diazabicyc!o[3.3.1]non-6-ene-6-carboxylic acid cyclo-propyl-(2-(3,4-dimethyiphenoxy)ethyllamide formate salt
Synthesized according to typical procedures G and E from bicyclononene ALII and 4-carbamoylbutyric acid. LC-MS: Rt^0.S9E5-i-:'733.49. '
Example 171
(rac.)-(lR*, 55*)-3-(4-CarbamoylbutyryI)-7-(4-[3-(2»3,6-trinuorophenoxy)-propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclo-propylphenethylamide formate salt
Synthesized according to typical procedures G and E from bicycloaonene AL12 and 4-carbamoylbutyric acid. LC-MS: Rt = 0.85 ES+: 689.48.
Example 172
{rac)-{2R*, 55*)-3-{4-Carbamoylbutyryl>7-{4-i3-{2^,6-tiifluorophenoxy)-propyI]phenyI}-3,9-diaza-bicycIo[3.3.1]non-6-ene-6-carboxyiic acid [2-(2-ch1oro-phenyl)ethyl]cyclopropylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL13
and 4-carbamoylbutyric acid. LC-MS: Ri = 0.87 ES+: 723.43,
Example 173

(racyilR*, 55*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(23,6-trinuorophenoxy)-propyl]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyHc acid cyclo-propyI-[2-(2.3-difluorophenyl)ethyI]amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL14 and 4-carbamoylbutyric acid. LC-MS: Rt ^ 0.86 ES+: 725.45.
Example 174
{rac.)-(lR*, 55*)-3-(4-CarbamoyIbutyryl)-7-{4-[3-(23,6-trifluorophenoxy)-p ropyl] pheByl}-3,9-diazabicy do [3.3:1 ]::an-6-ene-6-carbo™]:c acid cyclo-propy i- [2-{4-fIuoroph enyl)ethyl] amide
Synthesized according to typical procedures G and E from bicyclononene AL15 and 4-carbamoylbutyric acid. LC-MS: Rt = 0.86 ES+: 707.44.
Example 175
(racH^R*, 55*)-3-(4-CarbamoylbutyryI)-7-{4-[3-(23,6-trifluorophenoiy)-
propyl]phenyl}-3,9-diazabicycIo[33.1]non-6-ene-6-carboxyiic acid
cyclopropyl-(2-o-tolylethyl)amide formate salt
Synthesized accordiog to typical procedures G and E from bicyclononene AL16 and 4-carbamoylbutyric acid. LC-MS; Rt = 0.87 ES+: 703.47.
Example 176
(rac.)-(lR*, 55*)-3-(4-Carbamoylbutyryl)-7-{4-I3-(2,3,6-trifluorophenoiy)-propyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carbosyiic acid cyclo-propyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononene AL17 and 4-carbamoyIbutyric acid- LC-MS: R, = 0.85 ES+: 735.47.
Example 177
(rac.)-(lR*, 55*)-3-(4-CarbamoyIbutyryl)-7-{4-[3-(2,3,6-trifIuorophenoxy)-propyl]phenyI}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclo-propyl-(2-p-tolykthyl)amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL18 and 'f-carbamoylbutyric acid- LC-MS; Rf = 0.87 ES+: 703.46.
Example 178
l:l-Mixture of (IR, 5S)-3-i(lS, ^^)-4-hydroxypyrrolidinc-2-carbonyl)-7-{4-[3-(23)6-trifluoroph en oxy)propyl] phenyi}-3,9-diazabicyclo [3.3.1 lnon-6-ene-6-carboxyiic acid bcnzylcyclopropylamide formate salt and {IS, 5R)-3-{{lS, ■^iJ)-4-hydroxypyrrolldine-2-carbonyl)-7-{4-I3-(23)6-trifluorophenoxy)-prDpyI]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid bcnzyl¬cyclopropylamide formate salt
Synthesized according to typical procedures G, E and L from bicyclononene AL3 and BOC-L-hydroxyproline. LC-MS: R* = 0.78 ES4-: 675.47.
Example 179
l:l-Mixture of {IR, 5S)-3~{{1S, 4J?H-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(23,6-trifluorophenoxy)propyIphenyl}-3,9-dlazablcyclo[3,3.1]non~6-ene-6-carboxylic acid (2-chlorobenzyl)ethylamide formate salt and (JS, 5R)-3-{{lS, •^i;)-4-hydroxypyrrolidine'2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propylphenyl}-3,9-diazabicyclo[3.3.11non-6-ene-6-carboxylic acid (2-chloro-benzyl)ethylamide formate salt

Synthesized according to typical procedures G, E and L from bicyclononene AL4 and BOC-L-hydroxyproline. LC-MS: R, = 0.79 ES+: 697.40.
Example 180
l:l-Mixture of {IR, 55)-3-((75, ./^)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(23»6-trinuorophenoxy)propyl]phenyl}-3,9-diazabicyclo{3.3.1]non-6-ene-6-carboxylic acid cyciopropyI-(2-fluorofaenzyI)araide formate salt and (IS, SR)-3-i{IS, 4i?)-4-hydrosypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluoro-pI.tJiGKy)propyllphenyI}-3,9-dia2abicyclo[33.1]non-6-ene-6-carbpsyUc acid cyclopropyl-(2-fluorobeii2yl)aDiide formate salt
Synthesized according to typical procedures G, E and L from bicyclononene AL5 and BOC-L-hydroxyproline. LC-MS; R, = 0.78 ES+i 693.44.
Example 181
l:l-Mixture of (IR, 5S)-3-({lS, ■^i?)-4-hydroxypyrroIidine-2-carbonyl)-7-{4-I3-(2356-trifluoropheDoxy)propyl]phenyl}-3,9-diazabicyclo[33.1]non-6-ene-6-carboxylic acid cycIopropyl-(3-trifluoromethylbenzyI)amide formate salt and (IS, 5R)-3-(iJS, ^Ji)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(23,6-trifluorophenoxy)propyl] phenyl}-3,9-diazabicyclo [3 J.i] aon-6-ene-6-carboxyiic acid cyclopropyl-(3-trifluoromethyIbenzyl)amide formate salt
Synthesized according to typical procedures G, E and L from bicyclononene AL6 and BOC-L-hydroxyproline. LC-MS: R* = 0.81 ES+: 743.42.
Example 182
l:l-Mixture of (IR, 5S)'3-((1S, 4J?)-4-hydroxypyrroUdine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propy!]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-

6-carboxyIic acid cyclopropyl-(2-metliylbenzyI)amide formate salt and (IS, 5R)-3-{(lS, '/^)-4-hydroxypyrroUdme-2-carbonyI)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl|phenyl}-3,9-dia2abicyclo(3.3.1]non-6-ene-6-carboxyIic acid cyclopropyl-(2-methyIenzyl)amide formate salt
Synthesized according to typical procedures G, E and L from bicyclononene AL7 and BOC-L-hydroxyproline. LC-MS: Rt = 0.79 ES+: 689.47.
Example 183
Iri-MlAiure of (IR, SSj-Z-ix^S, '/i;)-4-hydroxypyrroIidine-2-carbonyl)-7-{4-
[3-(23>6-trifluorophenoxy)propyllphenyl}-3,9-diazabicyclo 13.3.1] non-6-ene-
6-carboxylic acid cyciopropyl-(2-m-tolyloxyethyI)amide formate salt and {IS,
5R)-3-iilR '/5-4-hydroxypyrroUdine-2-carbonyl)-7-{4-[3-(23,6-trifluoro-
phenoxy)propyl]pbenyl}-3,9-diazabicyclo[33-l]non-6-ene-6-carboxylic acid cycIopropyI-(2-m-tolyIoxyethyl)amide formate salt
Synthesized according to typical procedures G, E and L from bicyclononene ALIO and BOC-L-hydroxyproline. LC-MS: Rt = 0.81 ES+: 719.45.
Example 184
l:l-Mixt«re of (IR, 5S}-3-(ilS, ^iJ)-4-hydroxypyrroIidine-2-carbonyI)-7-{4-[3-(23,6-trifluorophenoxy)propyI]pfaenyI}-3,9-diazabicyclo[33.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,5-dimethoxybenzyl)aDiide fromate salt and (JS, 5R)~3-{(1S, ^jR)-4-hydroxypyrroIidine-2-carbonyl)-7-{4-[3-(2^,6-trifluoroplienoxy)propyI]phenyl}-3,9-diazabicycIo [3.3.1] non-6-ene-6-carbo-xylic acid cycIopropyl-(3,5-dimethoxybenzyl)amide formate salt
Synthesized according to typical procedures G, E and L from bicyclononene AL17 and BOC-L-hydroxyproline. LC-MS: R, = 0.78 ES+: 735.48.

Example 185
l:l-Mixture of {IR, 5S)-5-{{lS, •/if)-hydroxypyrroUdine-2-carbonyI)-7-{4-[3-(2,3,6-trifluorophenoxy)propy!]phenyI}-3,9-diazabicyclo(3.3.1]non-6-ene-6-carboxylic acid cycJopropy)-(2-/?-tolyJertiy])amide formate salt and {JS, 5J?)-3-({IS, 4fl)-hydroxypyrrolidine-2-carbonyi)-7-{4-[3-{2,3,6-trifluorophenosy)-propyllphenyl)-3,9-dia2abicycIo[3.3.11non-6-ene-6-carboxyIic acid cyclo-propyl-(2-p-toly!ethyl)-aniide formate salt
Synthesized according to typical procedures G, E and L irom bicyclononene AL18 and DOC-L-l,ydrox)-prbline. LC-MS: R, = 0.81 ES+: 703.48."
Example 186
l:l-MLvture of (rac.)-i3R*)-5-{(lR*, 55*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[3-(23,6-trifIuoropheQoxy)propyl]phenyl}-3,9-diazabicyclo-p.3.I]non-^en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and {rac)-(55*)-5-({ifl% J5*)-6-l(2-ch|orobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifIuoropheno^)propylJphenyl}-3,9-diazabicyclo-[3 3.1] non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL2 and 3-(fert-butyldimethylsilyloxy)glutaric anhydride. LC-MS: Ri = 0.86 ES+: 726.40.
Example 187
l:l-Mixture of {rac.)-i3R*)-5-(ilS*, 55*)-6-(bettzylcyclopropylcarbamoyl)-7-{4- [3-(2,3,6-trifluo rop henoxy)propyll phenyl} -3,9-diazabicyclo [3.3.1] nott-6-eo-3-yl)-3-hydroxy-5-oxopeQtanoic acid formate salt and (rac.)-(3S*)S-({IR*, 55 *)-6-(benzy ley ciopropyl carbamoyl)-?-{4-[3-(2,3,6-triftuorophenoxy)-
propyI]phenyl}-3,9-diazabicyclo[3.3.1]iion-6-en-3-yl)-3-hydroxy-5-oxo-pentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL3 and 3-(ren'-butyldimethylsilyloxy)glutaric anhydride. LC-MS: Rt = 0.84 ES4-: 692.45
Example 188
l:l-Mixture of (rac.)-(_3R*)-5-(iJR*, 5Jf*)-6-[(2-chlorobenzyI)ethyl-carbam oyl] -7- {4-[3-(2^ ,6-trifl«oropLenoxj )propy:j phenylj -3,9-diazabicyc!o-[3.3.1]non-6-eii-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and (rac.)~ (3S*)-5-(ilR*, 55*)-64(2-chloroben2yl)ethyIcarbamoyl]-7-{4-[3-(23,6-tri-fluoropbenoxy)propy I] phenyl}-3,9-diazabicyclo [3.3.1 lQon-6-eii-3-yl)-3-hydroiy-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL4 and 3-(/er^butyldimethyIsilyioxy)glutaric anhydride. LC-MS: Rt = 0.86 ES+: 714.38
Example 189
l:l-Mixture of {rac.H3R*)-5-{(lR*, 55*)-6-[cyclopropyI-(2-fluorobe0zyl)-carbamoyl]-7-{4-I3-(23.6-trifluoropheno3y)propyllphenyI}-3^-diazbicyclo-|33.1Inon-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and (rac)-(3S*)-5-i{lR*, 55*)-6-[cyclopropyI-(2-fluorobenzyl)carbamoyIJ-7-{4-(3-(2^,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazbicycIo-p.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL5 and 3-(rer^butyIdimethylsilyloxy)glutaric anhydride. LC-MS: R| = 0.84 ES+: 710.42

Example 190
l:l-IVrixture of (rac.)-(3R*')-5-({IR*, 5^*)-6-[cyclopropyl-(3-trifluoroiijethyl-
benzyl)carbamoyll-7-{4-[3-(23,6-trifluorophenoxy)propyIiphenyl}-3,9-dia2a-
bicyclo[3.3.1]non-6-en-3-yI)-3-hydroxy-5-oxopentanoic acid formate salt and
(rac.)-(55*)-5-((ii?*, 55*)-6-[cyclopropyl-(3-trifluorometliylbeDzyl)-
carbamoyl]-7-{4-[3-(2,3)6-trifluoropheDOxy)propyl]phenyl}~3,9-diazabicydo-[3.3.1]nOQ-6-en-3-yl)-3-hydrosj'-5-Qxopentaiioic acid formate salt
Synthesized according to typical yrocedaca K^ Ii cud L -from bicyclonoaene AL6 and 3-(rerr-butyldimethylsiIyIoxy)glutaric anJiydride. LC-MS: Rt = 0.88 ES+: 760.39
Example 191
l:l-Mixture of (rac)-(ifi*)-5-((ifl* 55'*)-6-tcyclQpropyl-(2-methylhen2yl)-
carbamoy!]-7-{4-{3-(23>6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo-
(3,3.11noa-6-ea-3-yl)-3-hydroxy-5-oxopentattoic acid formate salt and (rac.)-
(3S*)-5'({IR*, 55*)-6-[cyclopropyK2-methylbeiizy!)carbamoyl]-7-{4-[3-
(23>6-trifluoropheiioxy)propyl]pheayli-3,9-diazabicyclo-[33.1]non-6-en-3-yI)-3-hydroiy-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL7 and 3-(^erf-butyldimethylsilyloKy)glutaric anhydride. LC-MS: R^ = 0.86 ES+: 706.44
Example 192
l:l-Mixture of irac.)-{3R*)-5-({lR*, 55*>6-{cyclopropyl-[2-(4-methoxy-phenoxy)ethylJcarbamoyl}-7-{4-[3-(2,3,6-trifluoropheiioxy)propyl]phettyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate

salt and (rac.)-(3S*y5-i(lR*, 55*)-6-{cycIopropyl-[2-(4-mefhoxyphenoxy)-ethyl] carbamoyl}-7-{4-[3-(2,3»6-tiifluo rophenoxy)propy IJpIienyI}-3,9-diaza-bicyclo[3.3.1]non-6-en-3-yI)-3-hydrosy-5-oxopentaDoic acid formate salt
Synthesized according to typical procedures K, E and L &0DI bicyclononene AL8 and 3-(/er/-butyIdiniethylsilyIoxy}glutaric anhydride. LC-MS; R, - 0.85 ES+: 752.43
Example 193
l:l-Mixture of (rflcH^J?*)-5-((/J?* 55*}-6-{cyclopi-epyl-t2 (3-me*!?oxy-
phenoxy)ethyl]carbamoyl}'7-{4-[3-(23)6-trifluoropheDoxy)propylJphenyl}-
3,9-diazabicyclo[3.3.1Inon-6-en-3-yI)-3-hydroxy-5H)iopentanoic acid formate
salt and irac,y(3S*y5-{{tR*, 55 *)-6-{cy do propyl-[2-(3-methoxyphenoxy)-
ethyl]carbamoyl}-7-{4-[3-(23»6-trinuorophenoxy)propyI]pheBiyI}-3,9-
diazabicydo [3.3.1 ]non-6-en-3-yi)-3-hydroxy-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL9 and 3-(i'erf-butyldimethylsilyloxy)glutaric anhydride. LC-MS: Rt = 0.85 ES+: 752.44
Example 194
l:l-Mixture of (rflc)-(3/E*)-5-((/J?* 55*)-6-[cyclopropyH2-m-toIyloxyethyl)-carbamoyll-7-{4-P-(23,6-trifluorophenoxy)propyllphenyl}-3,9-diazabicyclo-[33.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and {rac.y (3S*y5-i(lR*, 55*)-6-[cydopropyl-(2-/«-toIyloxyethyl)carbamoy!]-7-{4-[3-(23,6-trinuorophenoxy)propyll phenyl}-3,9-diazab icy do-i3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopeDtanoic acid formate salt

Synthesized according to typical procedures K, E and L from bicyclononene ALIO and 3-(fe7-^buty!dimethylsilyloxy)glutaric anhydride. LC-MS: Rt = 0.87 ES+: 736.45.
Example 195
l:l-Misture of Synthesized according to typical procedures K, E and L from bicyclononene ALII and 3-(/e/'/-butyldimethyIsilyloxy)glufaric anhydride. LC-MS: Rt = 0.89 ES+: 750.47
Example 196
1:1-Mixture of (rac.)-(3S *)-5-(ilR *, 55*)-(6-(cycIopropylphenethyl~
carbamoyl)-7-{4-[3-{2,3,6-trifluorophenoxy)propyllphenyi}-3,9-diazabicyclo-
l33.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and {rac)-
{3S*)-5-{(lR*, 55*)-5-(6-(cyclopropyIphenethyIcarbamoyl)-7-{4-(3-(23,6-
trifluorophenoxy)propylJphenyl}-3,9-diazabicycIo-[33.1]non-6-en-3-yI)-3-hydroxy-S-oxopentanoic acid formate salt
Syntbesized according to typical procedures K, E and L from bicyclononene AL12 and 3-(i'er^butyldimethylsiiyloxy)glutaric anhydride. LC-MS: Rt = 0.85 ES+: 706.43
Example 197

l:l-Mixture of (rac.y{3R*)-5-((JR*, 55*)-6-{I2-(2-chlorophenyl)ethyl]-cyclopropyIcarbamoyl}-7-{4-[3-(23,6-trifluorophenoxy)propylIphenyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and {rac.)-(SS*)-5-i(lR% 55*)-6-{[2-(2-chlorophenyl)ethyl]cydopropyI-carbamoyl}-7-(4-[3-(23,6-trifliio ro phenoxy)propy llphenyli-3,9-diazahicy clo-[3.3.1]non-6-en-3-y!)-3-hydroxy-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL13 and 3-{(eri'-butyldiniethyIsiIyloxy)glutaric anhydride. LC-MS; R( = 0.87 ES+: 740.40
Example 198
l;l-Mixt«re of {rac.)-(3R*)-5-({lR*, 5S*)-6-{cyclopropyl-[2-(23-difluoro-phenyl)ethyI]carbamoyl}-7-{4-{3-(23j6-trifluorophenoiy)propyI]phenyI}-3,9-diazabicycIoI3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and (rac)-i3S*)-5-((lR*, 55*)-6-{cyclopropyI-[2-(2^-difluorophcnyl)ethyl]-carbamoyI}-7-{4-I3-(23,6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo-[33.11non-6-en-3-yI)-3-hydroxy-5-oxopentanoic acid formate salt
Synthesized according to typical procediures K, E and L ftom bicyclononene AL14 and 3- Example 199
l:l-Mixture of {rac.)-(3R*)-5-i(lR*, 55*)-6-{cyclopropyl-[2-(4-fluorophenyl)-
ethy 1] carbamoyl} -7- t4-[3-(23,6-trifluorophenoxy)propyl][pheoy \}-3,9-diaxa-
bicyclo[3.3.1]noo-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and
{rac.)-{3S*yS-{(lR*, J5*)-6-{cycIopropyl-{2-(4-fluorophenyI)ethyl]-
carbamoyl}-7-{4-[3-(2,3,6-trlfluorophenoxy)propyl]phcnyI}-3,9-diazabicycIo-[3.3.1]non-6-en-3-yI)-3-hydroxy-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K, E and L from bicyclononene AL15 and 3-(rerf-butyldimethylsilyioxy)glutaric anhydride. LC-MS: R, = 0.86 ES+: 724.43.
Example 200
l:l-Mixture of {rac.)-(3-R*)-HU-R% 55*)-6-[cyclopropyI-(2-o-toIylethyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]pheny!}-3,9-diazabicycIo-I3.3.1]aon-6-€n-3-yI)-3-hydroxy-5-oxopentanoic acid formate salt and {rac.)-(3Sy3-i(lK*, 5i:;*)-6-[c>clopropyl-(2-(»-toIyIethyOcarbamoyl]-7-{4-p-(23,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-eD-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL16 and 3-{/er/-butyldrmethylsilyloxy)glutaric anhydride. LC-MS: Rt = 0.87 ES+: 720.45
Example 201
1:1-Mixture of {rac)-i3R *)-5-{{lR * 55*)-6-[cyclopropyl-(3,5-dimethoxy-benzyl)carbamoyi]-7-{4-[3-{2^,6-trifluoropheooxy)propyI]phenyI}-3,9-diaza-bicyclol33.11non-6-en-3-yI)-3-hydrosy-5-oxopentanoic acid formate salt and (rac.H^5*)-5-((i.R*, 55^-(cycIopropyH3,S-dmiethoxybeiizyI)carbamoyI]-7-{4-[3-(2^,6-trifluoropheDOxy)propyI]phenyI}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene
AL17 and 3-(^erf-butyldiraethylsLlyloxy}glutaric anhydride. LC-MS; R, = 0.S5 ES+: 752.42
Example 202

l:l-Mixture of (rac.)-(3R*y5-{(IR*, 55*)-6-[cycIopropyl-(2-/;-tolyletbyl)-carbamoyl] -7- {4- {3-(2,3,6-trifluoro p henoxy)propy 1] pheny I}-3,9-d iazabicy clo-[3.3.1]non-6-£n-3-yl)-3-hydroxy-5-oxopeQtanoic acid formate salt and (rac.)-(3R *)-5-(ilR * 55*)-6-[cycIopropyt-(2-p-tolylethyl)carbamoyl]-7-(4-l3-(2,3,6-trifluorophenoxy)propyi]pbenyl}-3,9-diazabicyclo-[3.3,l]non-6-en-3-y!)-3-hydroxy-5-OKopentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene
AL18 and 3-(j'^rC-butyIdiinethylsilyloxy)glutaric anhydride. LC-MS: Rt = 0.87
ES+: 720.43 - ■ -- ■■'--- - - .
Example 203
(rac.)-(lR*, 55*)-3-AcetyI-7-{4-[3-{2»3,6-trifIuoropheaoxy)propyI]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid benzylcyclopropylamide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL3 and acetyl chloride. LC-MS: Rt = 0.88 ES+: 604.53
Example 204
(rac)-(lR*, 55'*)-3-Acety!-7-{4-p-(2^,6-trifluorophenoxy)propyllphenyI}-3,9-diazabicycloI33.1]non-6-ene-6-carboxyIic acid (2-chIorobenzyl)ethyIamide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL4 and acetyl chloride. LC-MS: R, = 0.90 ES+: 626.48
Example 205

{rac.)-{lR*, 55*)-3-ActtyI-7-{4-(3-(2,3,6-trifluorophenoxy)propyIlphenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl(2-fluorobenzyl)-amide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL5 and acetyl chloride. LC-MS: R, = 0.89 ES+: 622.53
Example 206
(rac.y(lR*, 55*)-3-Acetyl'7-{4-[3-(2,3,6-trifluorophenoxy)propyiIphenyI}-3,9-diazabicycloI33.1Jnon-6-eirc^6^ca"bbiy;;c acid 2ycIoprcpyI-(2-methylbeiizyI)-amide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL? and acetyl chloride. LC-MS: R, = 0.90 ES+-. 618.54
Example 207
(racH^R*, 55*)-3-Acetyl-7-{4-[3-(2^,6-trlfluoropIienoxy)propyl)phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl[2-(4-methoxy-phenoxy)ethyl] amide formate salt
Synthesized according to typical procedures A and E from bicyclononene ALS and acetyl chloride. LC-MS: R( = 0.89 ES+; 664.54
Example 208
irac.)'(lR*, 55*)-3-AcetyI-7-{4-[3-{2^,6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.11non-6-eae-6-carboxyUc acid cyclopropyl[2-(3-methoxy-phenoxy)ethyI]amide formate salt

Synthesized according to typical procedures A and E from bicyclononene AJL9 and acetyl chloride. LC-MS: Rt = 0.89 ES+: 664.53
Example 209
(rac.)-(iJf* 5S*)-3-Acetyl-7~{4-I3-{2,3,6-trinuorophenoxy)propyl]phenyl)-3,9-diazabicycIo[3.3.1Jnoii-6-ene-6-carboxylic acid cyclopropyl[2-(3-methyl-phenoiy)ethyI] amide formate salt
Synthesized according to typical procedures A and E from bicyclononene ALIO
and acetyl chloride. LC-MS: Rt= 0.91 ES+: 648.53 ' '
Example 210
irac)-{lR*, 55*)-3-Acetyl'7-{4-[3-(23,6-triiluoropIienoxy)propyl]phenyl)-3,9-diazabicyclo(3.3.1]non-6-ene-6-carboxylic acid cyclop ropy Iph en ethylamide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL12 and acetyl chloride. LC-MS: Rt = 0.89 ES+: 618.54
Example 211
(ra£L)-(iif* 55'^-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.1Inon-6-ene-6-carboxyIic acid cyclopropyl(33-dimetIioxy-benzyl)amide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL17 and acetyl chloride. LC-MS: Ri = 0.88 ES+: 664.55
Example 212

(rflc.)-(JR*, 55*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyllphenyl}~3,9-
diazab icy do [3.3.l]noDi-6-ene-6-carboxylic acid cyclopropyl(2-/j-
tolylethy])aniide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL18 and acetyl chloride. LC-MS: Ri = 0.91 ES+: 632.54
Example 213
(mc.)-5-((JR% 5S*)-6-(BenzyleyclopropyIcarbamoyl)-7-{4-[3-(23,6-trifluoro-pheDOxy)propyl]phenyl}-3,9-dlazabicycio|33.1Inon-6'en-3-yl)-5-cTe*^ent«- ■ ■ noic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL3 and glutaric anhydride. LC-MS; Ri = 0.86 ES+: 676.54
Example 214
iracyS-dlR*, 55*)-6-[(2-Chloroben2yI)ethyIcarbamoyI]-7-{4-[3-(2^,6-
trifluorophenoxy)propyl]phenyI}-3,9-dia2abicycIp[3.3.1Jnon-6-en-3-yl)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene ALA and glutaric anhydride. LC-MS: R, = 0.88 ES+: 698-46
Example 215
(>'ac.y5-((lR*, 55>6-ICyclopropyl-(2-fluorobenzyl)carbamoyI]-7-{4-[3-
(2,3,6-trinuorophenoxy)propyI]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K and E from bicyciononene AL5 and glutaric anhydride. LC-MS: R( = 0.86 ES+: 694.51
Example 216
(rac.)-5~((lR*, 55*)-6-[CyclopropyI{3-trifluoromethy!beazyl)carbamoyI]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl] phenyl}-3,9-diazabicyclo [3.3.1 ]non-6-en-3-yl)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyciononene AL6 and giiaVmc anhydride. LC-MS: R, = 0.89 ES+: 744.51
Example 217
(rac.)-5-{(lR*, 55*)-6-lCyclopropyI(2-methylbenzyl)carbamoyl]-7-{4-[3-
(2,3)6-trifluorophenoiy)propyl]phenyI}-3,9-diazabicyclo [3.3.1] non-6-en-3-yl)-5-oxo-pentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyciononene AL7 and glutaric anhydride. LC-MS: Rt = 0.88 ES+: 690.54
Example 218
{rac.yS'{(lR*, 55'^^-{CycIopropyI[2-(4-metlioxyphenoxy)ethyl]carbamoyl}-7-{4-l3-(2^,6-trifluorophenoxy)propyllphenyl}-3,9-diazabicyclo[33.11noii-6-en-3-yI)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyciononene AL8
and glutaric anhydride. LC-MS: Rt = 0.87 ES+: 736.54
Example 219

(rac.)-5'((]R*, 55*)-6-{CyclopropyI[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3i6-trinuorophenoxy)propylJphcnyI}-3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-5-oiopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL9 and glutaric anhydride. LC-MS: R, = 0.87 ES+: 736.55
Example 220
(rac.y5'iilR% 55'*)-6-{Cyclopropyl[2-(3-methylphenoxy)ethyI]carbamoyi}-7-{4 [3-(2,3,6 triflucrophenoiy)propyl]phenyl}-3,9-diazabicyclo(33.1jHoii-6-en-3-yl)-S-oxopentaaQic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene ALIO and glutaric anhydride. LC-MS: R, = 0.89 ES+: 720.53
Example 221
(rac.)-5-{(lR*, 55*)-6-{Cyclopropyl-[2-(3,4-dimethylphenoxy)ethylI-
carbamoyI}-7-{4-[3-{23,6-trifluorophenoxy)propyl]phenyi}-3,9-diazabicyclo-[3.3.1 ]non-6-en-3-yl)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene ALII and glutaric anhydride. LC-MS; Ri = 0.90 ES+: 734.57
Example 222
(mc.)-5-((iif*, 55*)-6-(Cyclopropylphenethylcarbamoyl)-7-{4-I3-(2,3,6-
trifluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid formate salt

Synthesized accordmg to typical procedures K and E from bicyclononene AH2 and glutaric anhydride. LC-MS: R, = 0.87 ES+: 690.52
Example 223
(mc.yS'iilR*, 55*)-6-{(2-{2-Chlorophenyl)ethyI]cyclopropyIcarbamoyl}-7-{4-[3-(2y3»6-trifluorophenoxy)propyllpheiiyl}-3,9-diazabicy do [3.3.1 lnon-6-en-3-yI)-5-o.topentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL13 and glutaric anhydade.tG-:,ISrP^'^ 0.89 ES't-:-724.49
Example 224
(rac>5-((2R*, 55*)-6-(CyclQpropyl-[2-(2>3-difluoropliettyl)efhyIlcarbamoyl}-7-{4-p-(23,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicycIoI33.1]non-6-en-3-yl)-5-oxQpeataaoic acid formate salt
Synthesiasd according to typical procedures K and E fi:om bicyclononene AL14 and glutaric anhydride. LC-MS: R, = 0.88ES+: 726.51
Example 225
(rac)-5-((IR*, 55*)-6-{Cyclopropyl[2-(4-fluorophenyl)ethyI]carbamoyl}-7-{4-[3-(23,6-trifluorQpliettoiy)propyi]pheayl}-3,9-diazabicyclQ [3 3 .llttoii-6-ea-3-yl)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL15 and glutaric anhydride. LC-MS; Rt = 0.87 ES-i-: 708.50
Example 226

)propyl]phenyl}-3,9-diazaMcycloI3.3.11non-6-en-3-yt)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from, bicyclononene AL16 and glutaric anhydride. LC-MS: R,= 0.88 ES+: 704.54
Example 227
(rac.)-5-((i-ff*, 55*>6-[CyclopropyI(3,5-dimethoxybenzyi)carbaraoyl]-7-{4-[3-(2^,6-trifluoropheKosy)j'ropy!lpbenylJ-3iy-(*«*cabicyclo[33.1Jnon-6-en-3-yl)-5-oxopeDtanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL17 and glutaric anhydride. LC-MS: Rt = 0.86 ES+: 736.55
Example 228
(rac.)'5-({JR*, 55*)-6-(Cyclopropyl(2-;)-tolylethyl) carbamoyl]-?-{4-[3-(2^,6-trifIuoroplienoxy)propyI]phenyl}-3,9-dia2abicycIo[3.3.1Jnon-6-ed-3-yI)-5-oio-pentanoic acid formats salt
Synthesized according to typical procedures K and E from bicyclononene AL18 and glutaric anhydride. LC-MS: Rt = 0.88 ES+: 704.54
Example 229
(roc.)-5-((ii!*, 5S*)-6-(BenzylcyclopropykarbainoylV7-{4-l3-(23,6-trifluoro-pfaeaosy)p ropy l]pheoyl}-3,9-diazabicyclo [3.3.llnon-6-en-3-yl)-5-oxopen-tauoic acid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononene AL3 and glutaric acid monomethylester chloride. LC-MS: R, = 0.91 ES+: 690.55
Example 230
(rac.)-5-i(JS*, 55*>6-[(2-Chlorobenzyl)ethyIcarbamoyI]-7-{4-[3-(2,3,6-
triflHorophenoxy)propyt]phenyi}-3,9-diazabicycIo[3.3.1]non-6-en-3-yI)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL4 and glutaric acid monomethylester chloride. LC-MS: Rt = 0 ^SHS^-'-H'S^^ ■
Example 231
(rac)-5-((iil* 5S*)-6-[Cyclopropyl-(2-fiuorobenzyl)carbamoyl)-7-{4-[3-
(23,6-trifluorophenosy)propyl]phenyl}-3,9-diazabicycIo[3J.i]oon-6-eii-3-yl)-5-oxopentaDoic acid methyl ester formate sait
Synthesized according to typical procedures A and E from bicyclononene AL5 and glutaric acid monomethylester chloride. LC-MS: Rt = 0.91 ES+: 708.51
Example 232
(racy5-((lJl*, 55*)-6-[CycIopropyl(3-trifluoromethyIbenzyI)carbamoyI]-7-{4-[3-(2^,6-trifluorophenoiy)propyi]phenyI}-3,9-dia2ab icy clo [3.3.1] noii-6-en-3-yl)-S-oxopentaBoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL6 and glutaric acid monomethylester chloride. LC-MS: Rt = 0.94 ES+: 758.51
Example 233

irac.)-5-{ilR*, 55*)-6-[CycIopropyl(2-mefhylben2yl)carbanioyIl-7-{4-[3-
(23»6-trifluoropfaenoxy)propyl]phenyl}-3,9-dia2abicycIo[3.3.1Inon-6-en-3-yI)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL7 and glutaric acid monomethylester chloride. LC-MS; R, = 0.92 ES+: 704.54
Example 234
{racyS-iilR*, ^i?*)-6-{Cyclopropyl(2-(4-methoxyphenoxy)ethyl]carbamoyl)-7-{4-[3-(2^,6-trifluoropheiioxy)propylJphenyl}-5,'9^-'ti3zabicyelo[? 3:,ijn'»n-'i-eo-3-yl)-5-oxopeDtanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL8 and glutaric acid monomethylester chloride. LC-MS: Ri == 0.92 ES+: 750.54
Example 235
{rac)-B-mR*, 55*)-6-{Cyclopropyl[2-(3-methoxyphenoxy)etfayI]carbamoyI}-7-{4-[3-(23)6-ti*'fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3-3.1]non-6-ea-3-yI)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyciononene AL9 and glutaric acid monomethylester chloride. LC-MS: Rt = 0.92 ES+: 750.56
Example 236
{rac.yS-({lR% 55*)-6-{Cyclopropyll2-(3-methylplienoxy)ethyl)carbamoyl}-7-(4-(3-(23,6-triflaorophenoxy)propyllphenyl}-3,9-diazabicyclol3.3.1)non-6-en-3-yl)-5-oxopentanoic acid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononene ALIO and glutaric acid monomethylester chloride. LC-MS: Rt = 0.93 ES+: 734.58
Example 237
(racyS'iilR*, 55*)-6-{Cyclopropyl[2-(3,4-dimethyIphenoxy)ethyl]-
carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]nQa-6-ea-3-yl)-5-osopeiitaiioic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene ALU '^d^gltnarice-rid monomethylester chloride. LC-MS; R = 0.95 ES+: 748.57--
Example 238
{rac)-5-i(lR*, 55*)-6-{CycIopropyIphenethylcarbamoyl)-7-{4-(3-(2^,6-
trifluorophenoxy)pr opyl] phcnyl}-3,9-diazabicy clo [3.3.11noD-6-eii-3-yl)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL12 and glutaric acid monomethylester chloride. LC-MS: Rt = 0.91 ES+; 704.55
Example 239
{racyS-iilR*, 5S*)-6-(I2-(2-Chlorophenyl)ethyl]cydopropylcarbamoyl}-7-{4-(3-(2^,6-trifluoroplienoxy)propyllphenyl}-3,9-diazabicyclo[3_3.1]non-6-en-3-yI)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL13 and glutaric acid monomethylester chloride. LC-MS; Rt = 0.93 ES+: 738.53
Example 240

(rac.y5-i{lR*, 5S*>6-{CydopropyI[2-(2,3-difluQropheuyI)ethyllcarbamoyl}-7-{4-t3-(23,6-trifluorophenQxy)propyllphcnyl}-3,9-diazabicyclo[3J.lliiott-6-en-3-yl)-5-oxopeatanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL14 md glutaric acid monomethylester chloride. LC-MS: Rt = 0.92 ES+; 740.54
Example 241
rac.y-S-aJR*, 55*)-6-{CycIopropyl[2-(4-fluorophenyl)ethyl]carbamoyI}-7-{4-^-(2,5;'*-*"^1oTophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3ilJaon-6-e'E"5-'t)-S-oxopeiitanoic acid methyl ester formate salt
lynthesized according to typical procedures A and E from bicyclononene AL15 nd glutaric acid monomethyiester chloride. LC-MS: Rt = 0.92 ES+; 722.54
:xample 242
ac.)-5-({lR*, 5^*)-6-{Cyclop ropyl [2-(2-methyIphenyI)ethylI carbamoy I}-7-l-I3-(2»3)6-trifluoropheno3:y)propyl]phenyI)-3,9-diazabicycIoI3J.l]non-6-en-■yl)-5-oxopeQtanoic acid methyl ester formate salt
ynthesized accoiding to typical procednres A and E from bicyclononene AL16 id glutaric acid monomethylestet chloride. LC-MS; Rt= 0.93 ES+: 718,56
!tample 243
itc.)-5-{{lR*, 55*)-6-lCyclopropyl~(3,5-dimetlioxybenzyl)carbamoyll-7-{4--(23,6-trifluorophenoxy)propyI] phenyl}-3,9-diazabicy do [3.3.11 non-6-en-3-1-5-0X0pentauoic acid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononene AL17 and glutaric acid monomethylester chloride, LC-MS: Rt = 0.91 ES+: 750.55
Example 244
(rac.)-5-i(lS*, 55 *)-6-(Cyclop ropyl [2-(4-methylphenyl)ethyllcarfaamoyl}-7-{4- [3-(2,3,6-trifluorophenoiy)propy I j phenyl}-3,9-diazabicy do [3.3,1] non-6-en-3-yI)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL18 and glutaric aciu'moiiOmethyrestcr ^I^btidi: LC-MS: R^ = 0.93 ES+: 718.56
Example 245
{rac.)-5-(ilR*, 55*)-6-(Beiizylcyclopropylcarbamoyl)-7-{4-13-(23,6-trifluoro-phenoxy)propyllphenyl}-3,9-diazabicycloI33.1Inon-6-en-3-yl)-2,2-dimethyl-5-oxopentaaoic acid methyl ester formate salt
Synthesized according to typical procedures K and E from bicyclononene AL3 and 2,2-dimethylglutaric anhydride. LC-MS: Rt = 0.90 ES+: 704.53
Example 246
(racyS'iiJR*, 55*)-6-[(2-ChlorobenzyI)ethylcarbamoyl]-7-{4-[3-(2^,6-
trifluorophenoxy)propyllphenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimetbyl-S-oxopentanolc acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL4 and 2,2-dim.ethylglutaric anhydride. LC-MS: Ri ^ 0.91 ES+: 726.53
Example 247

(rflc.)-5-((i/?*, 55*)-6-[Cyclopropyl-(2-fluorobenzyl>carbamoyll-7-{4-f3-
(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-diazabicycIo[33.1]non-6-en-3-yl)-2,2-dimethyl-5-oxo-pentanoic formate salt
Synthesized according to typical procedures K and E from bicyclononene AL5 and 2,2-dimethyIglutaTic anhydride. LC-MS; Rt = 0.90 ES+: 722.54
Example 248
(rac.)-5-((/R *, 5vS*>-6-[Cyclopropyl-(3-trifluoromethylbenzyl)carbaniOylj-7-{4-[3-(2,3,6-trifliiorophcaoxy)pr::py!]ph?nyI}-3,9-dia2abicycIo[3.3.1]non-6-en-3-y\)-2,2-dimethyl-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K. and E from bicyclononene AL6 and 2,2-dimethylglutaric anhydride, LC-MS: R, = 0.93 ES+: 772.51
Example 249
(rac.)-5-((IR*, 55*)-6-[Cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-I3-
(2^,6-trifiuorophenoxy)propyl]pheiiyl}-3,9-diazabicyclop3.1]noii-6-en-3-yl)-2^-dimethyl-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E ftom bicyclononene AL7 and 2,2-dkQethylglutaric anhydride. LC-MS: Ri = 0.91 ES+; 718.57
Example 250
(rac.)-5-{{lR*, 5>S*>6-{CyclopropyI-I2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-(3-(23,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.11non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K aad E from bicyclononene AL8 and 2,2-dimethylglutaric anhydride. LC-MS: Rt = 0.90 ES+: 764.55
Example 251
(rac.)-5'({ljR*, 5i5*)-6-{Cyclopropyl-[2-(3-niethoxyphenoxy)ethyljcarbamoyl}-7-{4-[3-(23)6-trifluoro-phenoxy)propylIpheiiyl}-3,9-diazabicyclo[33.1]non-6-en-3-yl)-2,2-diinethyl-5-oxopeiitanoie acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL9 and 2,2-dimethyiglutaric anhydride. LC-MS: Ri=^ 0.90 ES+: 7t'1.54 ■
Example 252
{rac.)-5-((ifl*, 55*)-6-{Cyclopropyl-p-{3-methylphenoxy)ethyllcarbamoyl)-7-{4-[3-(2^,6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicycIo[3.3.1]noii-6-en-3-yI)-2^-dimethyl-5-oxopentanoic acid formate salt
Synthesized accocding to typical procedures K and E from bicyclononene ALIO and 2,2-dhiiethylglutaric anhydride. LC-MS; Rt = 0.92 ES+: 748.58
Example 253
{rac)'5-{iIR*, 55*)-6-{CycIopropyl-[2-(3,4-dimethylphenoiy)ethylI-
carbamoyI}-7-{4-[3-{2^,6-trifluorophenoxy)propyI]phedyl}-3,9-diazabicycIo-[3.3.1]noa-6-en-3-yI)-2,2-dimethyl-S-osopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene ALII and 2,2-dimethylglutaric anhydride. LC-MS: Rt = 0.93 ES+: 762.58
Example 254

(racyS-aiR*^, 55*)-6-(CyclopropylphenethylcarbamoyI)-7-{4-[3-(2,3,6-
trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-2,2-dimethyl-S-oxo-pentaooic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL12 and 2,2-dimethylgiutaTic anhydride. LC-MS: R, = O.90 ES+: 718.56
Example 255
(rac)~5'({JR*, 55'*)-6-{[2-(2-ChIorophenyI)ethyI]cyclopropyIearbamoyl}-7-{4-[3-(2^,6-trifluorophenoxy)propyl]pbenyI}-3,**-rtiaz';b!fyel'»[? ?;li*win-r6-en-3-yl)-2,2-dimethyl-5-oiopeQtanoic acid formate salt
Synthesized according to typical procedxores K and E from bicyclononene AL13 and 2,2-dmiethyIglutaric anhydride. LC-MS; R| = 0.92 ES+: 752.50
Example 256
(rac)-5-((lR% 55*)-6-{(2-(2^-Difmoropheny0efhyl]cyclopropylcarbamoyl}-7-{4-p-(23,6-trifluorophenoxy)propyllphenyl}-3,9-diazabicycIo[33.11non[-6-eii-3-yl)-2^-dimethyI-5-oxopeiitanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL14 and 2,2-dimethylglutaric anhydride. LC-MS: Rt = 0.91 ES+: 754.53
Example 257
(rac)-5-((ii?*, 55*)-6-{l2-(4-Fluorophenyl)ethyIlcycIopropylcarbamoyl)-7-(4-[3-(23,6-trlfluorophenoxy)propyl]phenyI}-3,9-dia2abicyclo[3.3.11non-6-en-3-
yi)-2,2'dimethyl-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL15 and 2,2-dimethylglutaric anhydride. LC-MS: Rt = 0.91 ES+: 736.56
Example 258
(rac.)-5-((;R* 55*)-6-{[2-(2-Methytphenyl)ethyIlcyclopropyIcarbamoyI}-7-{4-[3-(23,6-trifluoropheaoxy)propyllphenyI}-3,9-diazabicyclo[3.3.1]aon-6-eu-3-yO-2,2-dimethyI-S-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL16 mti 2,2-dimethylglutaric anhydride. LC-MS: Rt = 0.92 ES+; 732.59
Example 259
rac)-5-(ilR*, 5>y*)-6-[Cyclopropyl-(3,S-dimethoxybenzyl)carbamoyI]-7-{4-3-(2^,6-trifluorophenoiy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-i)-2,2-dunethyI'5-oxopentanoic acid formate salt
lynihesized accordmg to typical procedures K and E from bicyclononene AL17 nd 2,2-dimethylglutaiic anhydride. LC-MS: R, = 0.90 ES+: 764.54
'.xample 260
-ac.)-5-((^it*, 55*)-6-{[2- ynthesized according to typical procedures K and E from bicyclononene AL18
id 2,2-dimethyIgIutaric anhydride. LC-MS: R, = 0.92 ES+: 732.58
sample 261

1

l:l-Mixture of {rac.H2R\ 3S*)~4-((ifl* 55*)-6-I(2-chlorobenzyl)ethyl-carbamoy!]-7-(4-[3-(2,3,6-trifluorophenosy)propyIlphenyi}-3,9-diazabicycio-[3.3.1]noti-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid formate salt and {rnc.)-{2S*, 3R*)-4-{{JR*, 5S*>-6-l(2-chlorobenzyI)ethylcarbaraoyl]-7-{4-[3-(2,3,6-trifluoropheiioxy)propyllphenyl}-3,9-diazabicyclo-[3.3.11iion-6-en-3-yl)-2,3-dibydrox>-4-oxobut>Tic acid formate salt
Synthesized according to typical procedures K and E fi-ora bicyclononene AL4 and fneso-2,3-dihydroxysuccinic anhydride. LC-MS: Ri - 0.85 ES+: 716.45
Examph262
1:1-Mixture of {rac.y{2R * iS*)-4-((ifi % 55*)-6-[cyclopropyl-(2-fluorQ-bettzy l)carbamoylj[-7- (4- [3-(23 56-tritluo rop beuoxy)propy IJp heay 1} -3,9-diaza-bicycIo[33.11non-6-ea-3-yl)-2y3-dihydroxy-4-oxobutyric acid formate salt aad (rac)-(2S*, 3R*)'4-{{JR% 55*)-6-{cycIopropyH2-fluorobeiizyl)carbamoyIl-7-{4-[3-(23i6-trifluorophenoiy)p ropy 11 phenyl}-3,9-diazabicyclo-(33.1 lnon-6-en-3-yl)-23-dihydroxy-4-oxobutyric acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL5 and meJo-2,3-dihydroxysuccinic anhydride. LC-MS: Rt = 0.83 ES+: 712.44
Example 263
l:l-Mixture of (rac.)-(2S*, 3S*y4~({lR*, 5>S*)-6-[CyclopropyH3-trifluoromefhyiben2yl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-pheDyl}-3,9-diazabicyclo-[3.3.1]non-6-cn-3-yl)-23-^ihydroxy-4-oxobutyric acid formate salt apd {rac.)-{2S*, 3R*)'4~i(lR*, 55*)-6-Icyclopropyl-(3-trifluoromethylbenzyI)carbamoyIJ-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-pheQyl}-3,9-dia2abicy do-[3.3. llnon-6-en-3-yI)-23-dihydroiy-4-0x0 butyric acid fromate salt

Synthesized according to typical procediu-es K and E from bicyclononene AL6 and me^o-2,3-dihydroxysuccinic aniiydride. LC-MS: R, = 0.87 ES+: 762.42
Example 264
l;l-Mixture of irac.)-i2R*, 55*)-4-({7if* 55*)-6-[cycIopropyK2-inethyl-henzy l)carhamoy li-7-(4-l3-(23,6-trifluorQpb.ettQicy)prQpy llpfaenyl}-3,9-diaza-bicycIo[3.3.1]non-6-en-3-yl)-2,3-dihyd^oxy-4-oxobutyric acid formate salt and (rac.)-(2S*, 3R*)-4-((lR*, 5iS*)-6-[cycIopropyH2-methyIbenzyI)carbamoyI]-7-{4-[3-(23,6-trifluorophenoxy)propyl] phenyl}-3,9-dlazabicycIo-[3.3.1] non-6-en-3-yI)-23- Synthesized according to typical procedures K and E from bicyclononene AL7 and niejo-2,3-dihydroxysuccinic anhydride. LC-MS: Rt = 0.85 ES+: 708.46
Example 265
l:l-Mixture of (rac)-(2iJ*, i5*)-4-((Jif* 55*)-6-{cyclopropyI-I2-(2,3-difIuoro-phenyl)ethylJcarbamoyl}-7-{4-[3-(2^,6-trifIuorophenoxy)propyllphenyl}-3,9-diazabicyclo[33.1]non-6-en-3-yl)-23-dihydroxy-4-oxobutyric acid formate salt and (racy(2S*, 3R*)-4-{ilR*, 55*)-6-{cyclopropyl-[2-(23-difluoro-phenyl)ethyljcarbamoyl}-7-{4-[3-(2^,6-trifluoropheno]^)propyllphenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-23-dihydroxy-4-oxobutyric acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL14 and mc5o-2,3-dihydroxysuccimc anhydride. LC-MS: R, = 0.85 ES-!-: 744.46
Example 266
l:l-Mixture of irac.)-(2R^ 3S*)'4-i(_IR*, 55*)-6-{cycIopropyl-l2-(2-methyl-phenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-

diazabicyclo[3.3.1Jiion-6-en-3-yI)-2,3-dihydroxj'-4~oxobutyric acid formate salt and irac.)-{2S% 3R'^)-HU^% 55*)-6-{cyclopropyI-[2-(2-methyIphenyl)-ethyllcarbamoyi}-7-{4-[3-{2,3,6-trifluoropheiioxy)propyl)pheflyl)-3,9-diaza-bicyclo(3.3.Ilnou-6-en-3-yl)-2,3-dihydroxy-4-oxohutyric acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL16 and me5o-2,3-dihydroxysuccmic anhydride. LC-MS: R, - 0.86 ES+: 722.52
Example 267
I:l-Mlxture Gf (,ac)-(2R* 3^*)M'^((ii!*, 55*)-6-[cyclopropyl-(3^dimethoxy-benzyl)carbamoyI]-7-(4'[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diaza-bicycIo[3.3.1]noo-6-en-3-yI)-2^-dihydroxy-4-oxobutyric acid formate salt and irac.y{2S*, 3R*)~4-({1R*, J5*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)-carbamoyl]-7-{4-[3-(2^,6-trifIuorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1] noD-6-en-3-yl)-23-dihydroxy-4-oxobutyric acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL17 and meJo-23-dihydroxysuccmic anhydride. LC-MS: R, = 0.84 ES+: 754.50
Example 268
l:l-Mixture of iracy{2R*, 35*)-4-((Jfl* 55*)-6-{cyclopropyl-I2-(4-methyl-phenyI)eUiyl}carbamoyl}-7-{4-t3-(2y3^-trifluorophenoxy)propyllpheayl}-3,9-diazabicyclo[3.3.1Jnon-6-en-3-yI>23-dihydroxy-4-oxobutyric acid formate salt and (rac.H2S*, 3R*)-4-(ilR*, 55*)-6-{cyclopropyl-[2-{4-methylphenyl)-ethyl] carbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propy 1] phenyl}-3,9-diaza-bicyclo(3.3.1]non-6-en-3-yl)-23-dihydroxy-4-oxobutyric acid formate salt
Synthesized according to typical procedures K. aad E from bicyclononene AL18 and m^TO-2,3-dihydroxysuccinic anhydride. LC-MS: R^ = 0.86 ES+: 722.49

Example 269
l:l-Mixture of (rac.)-(3R*)-5-((JJi*, 55*)-6-[(2-chiorobenzyI)cyclopropyl-carbamoyI]-7-{4-[3-(2,3,5-trimethylphenoxy)efhyI]phenyl}-3,9-diazabicyclo-[3.3.1]noa-6-en-3-yl)-3-hydrox}-5-oxopeiitanoic acid formate salt and (rac.)-i3S*)'5-((28*, 55*)-6-[(2-chloroben2yI)cyclopropy!carbamoyl]-7-{4-[3-(2,3,5-trimethy!phenoxy)ethyl] phenyl]-3,9-diazabicy do-[3.3.1] non-6-en-3-yl)-3-hydroxy-5-QXopentaaoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AIJ38 and 3-{rert-butyldimethyIsilyloxy)giutaric anhydride." LU-MS: Rt = 0.88 ES+: 700.52
Example 270
l:l-Mixture of (_rac.y(3R*)-5-i(lR*, 55*)-6-[(2-chlorobenzyl)ethyi-
carbaraoylI-7-{4-[3-(23,S-trimethylphenoxy)ethyI]phenyl}-3,9-diazabicyclo-
[33.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and (rac)-
(JS*)-5-((/R* 55*)-6-[(2-chIorohenzyI)efhylcarbamoyIl-7-{4-[3-(23^-tri-
methylphenoxy)ethyl]phenyl}-3^-diazabicycIo[33.11non-6-en-3-yl)-3-hydroxy-S-oxopentanoic acid formftte salt
Synthesized according to typical procedures K, E and L from bicyclononene AL40 and 3-(/er/-butyldimethylsilyloxy)glutaric anhydride. LC-MS: Rt = 0.88 ES+: 688.54
Example 271
(rac.)-5-{iJR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyI]phenyi}-6-
{cy clopr opy l-t2-(2-hy dr Qxyethyl)beMyli carbamoyl}-3,9-diazahicyclQ [3,3.11-non-6-en-3-yi)-5-oxo-peDtanoic acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL37 and glutaric anhydride. LC-MS: R, = 0.86 ES+: 762.42
Example 272
(rac.)-5-((IJi*, 55*)-7-(4-[3-(2-Bromo-5-fluorophenoxy)propyl]phe»iyl}-6-
{cyc\opropyl-[2-(2-hydroxyethyl)benzyl] carbamoyl}-3,9-dia2abicy clo[33.1)-non-6-en-3-yi)-5-oxo-pentanoic acid mefhyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL37 and glutaric acid monomethyl ester chlc-nde.- LC-MS:-"Rt - 0.2S ES-^: 776.43
Example 273
(rac.)-(JR*, 55*)-7-{4-[3-(2-Bromo-5-nuoropheDOxy)propyl]phenyl}-3-(4-
carbamoylbutyryl)-3,9-diazabicyclo[3.3.11non-6-ene-6-carboxylic acid cyclo-propyI-[2-(2-hydroxy£thyi)beiizyl]amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL37 and 4-carbamoylbutyric acid. LC-MS: R, = 0.82 ES+; 761.45
Example 274
(rac>(i/f* 55*)-3-Acetyl-7-{4-I3-(2^,6-trinuorophettoxy)propyllphenyl}-3,9-dia2abicyc!o[3.3.1]non-6-ene-6-carboxyIic acid cyclopropyl-[2-(2-hydroxy-ethyl)benzyl] amide formate salt
Synthesized according to typical procedures A and E irom bicyclononene AL19 and acetyl chloride. LC-MS: R, - 0.84 ES-I-: 648.50
Example 275

(rac)-5-((7fi* 55'*)-6-(Cyclopropyl-(2-(2-hydro£yethyl)beiiiyllcarbamoyl}-7-{4-[3-{2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicydo[3.3.1]Qon-6-eii-3-yl)-5-oxo-pentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL19 and glutaric anhydride. LC-MS: Rt = 0.85 ES+; 740.42
Example 276
(rac.y5'((IR*, 55*)-6-{Cyclopropyl-[2-(2-hydroiyetbyI)beiizyl]carbamoyI}-7-{4-|j-(2r3)6-trifluorophenoxy)propyI]phenyI}-3,9-dia2;abicycIop3.1Jii&a-6-eE-3-yl)-5-Oiopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E ftom bicyclononene AL19 and glutaric acid monomethylester chloride. LC-MS: Ri = 0.87 ES+: 734.52
Example 277
(rac)-5-i(IS*, 55*)-6-{CycIopropyl-[2-(2-hydroxyetbyr)benzyl]carbamoyl}-7-{4-[3-(2 3,6-trifluorophenoxy)propyllpheny l}-3,9-diazabicyclo (3 J,llnoa-6-en-3-yI)-2^-dimetliyl-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL19 and 2,2-dimetfaylglutaric anhydride. LC-MS: R Example 278
irac.y(lR*, 55*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(23,6-trlfluoroplieaoxy)-propylIphenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxyIic acid cyclo-propyl-[2-(2-hydroxyethyl)benzyIlamide formate salt

Synthesized according to typical procedures G and E from bicyclononene AL19 and 4-carbamoylbutyric acid. LC-MS: R, = 0.81; ES+: 719.52.
Example 279
{mc.)-5-{(lR*, 55*)-7-{4-[3-(2-Bromo-5-i]uorophenoxy)propyl]phenyI}-6-[{2-chIorobenzyl)ethylcarbamoyll-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoic acid formate salt
Synthesized according to typical procediires K and E from bicyclononene AL22
::nd glutaric anhydride. LC-MS: R^ = 0.89; ES+: 740.38. -r .-•-■ —
Example 280
{rac.)-5-{(lR*, 55*)-7-{4-[3-(2-Bronio-5-fluorophenoxy)propyI]phenyI}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyll-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL23 and glutaric anhydride. LC-MS: Rj = 0.88; ES+: 736.41.
Example 281
(raayS-iilR*, 5S^-7-{4-[3-(2-Bromo-5-fluorophenosy)propyl]phenyl}-6-
{cyclopropyl-(3-trifIuoromethyIbenzyl)carbamoyl]-3,9-diazabicy do [3.3.1]-non-6-eii-3-yl}-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL24
and glutaric aniiydride. LC-MS: R,= 0.91; ES+; 736.38.
Example 282

(rac.yS-iilR*, 55*)-7-{4-[3-(2-Bromo-5-nuoropbenoxy)propylIphenyI}-6-[cyclopropyI-(2-methylbenzyl)carbamoyI]-3,9-diazabicyclo [3.3.1] no n-6-en-3-yI}-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL25 and glutaric anhydride. LC-MS: Rj = 0.89; ES+; 732.45.
Example 2S3
(racyS'iilR*, 55'*)-7-{4-I3-(2-Bromo-5-nuorophenoxy)propylIphenyi}-6-{cyclopropyl-l2-('*-niethoxyphttnoxy)ethyllcarbamoyl}-3,9-diaxabicyclo-[3J.I]non-6-en-3-yl)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL26 and glutaric anhydride. LC-MS: R^ = 0.89; ES+: 778.41.
Example 284
(rflc)-5-({JiI*, 55*)-7-{4-I3-(2-Bromo-5-flnorophenoxy)propyllpheiiyl}-6-
(cycIopropyl-[2-(3-metliylph en oxy)ethyl]carbamoyl}-3,9-diaza bicycle [3.3.1]-noii-6-en-3'yl)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL27 and glutaric anhydride. LC-MS; Rt = 0.91; ES+: 762.42.
Example 285
(rac.)-5-{{JR*, 55'*)-7-(4-[3-(2-Bromo-5-fluorophenoiy)propyl]pheiiyl}-6-{cyc!opropyl-[2-(3,4-dimethylpbenoxy)ethyl]carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL28 and glufaric anhydride. LC-MS; Ri = 0.92; ES+: 776.45.
Example 2S6
(rflc.)-5-[(ii?* 55*)-7-{4~[3-(2-Bromo-5-fluorophenoxy)propyI]pheuyI}-6-
(cy clop ropylphenef bylcarbamoy l)-3,9-diazabicyclo [3.3.1 ]non-6-en-3-yI]-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL29 and glutcric anliyiidc. LC-Mt:': R, = 0.89; ES+: 732.44.
Example 287
(rac.)-5-((IR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-([2-(2-chIorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicycIo[33.1]nQn-6-en-3-yl)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene ALSO and glutaric anhydride. LC-MS: R^ = 0.90; ES+: 766.35.
Example 288
(rac)-5-((iJ?* 55*)-7-{4-[3-(2-Bromo-5-nuoroplienoxy)propyI]pheny!}-6-{[2-(2^-difluorophenyl)ethyIJcyclopropylcarbamoyi}-3,9-diazabicyclo [3.3.1] non-6-en-3-yI)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL31 and glutaric anhydride. LC-MS: R^ = 0.90; ES+: 768.35.
Example 289

(rac.)'5'((lR% 55*)-7-{4-[3-(2-Brorao-5-fluorophenoxy)propyl]phenyI}-6-{[2-(4-fluorophenyl)ethyl]eyclopropyIcarbamoyl}-3,9-diazabicycIo{3.3.1]non-6-en-3-yl)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL32 and glutaric anhydride. LC-MS: Rt = 0.89; ES-i--. 750.40.
Example 290
(rac.)-5-((IR*, 55*)-7-{4-[3-(2-Bromo-5-nuorophenoxy)propyI]phenyl}-6-{[2-(2-methyIphenyI)ethyI]cyclopropylcarbamoyijr-5,>-diiizal>icycIo[33.1]non-6-en-3-yl)-5-oxopeatanoic acid formate salt
Synthesized accordmg to typical procedures K and E from bicyclononene AL33 and glutaric anhydride. LC-MS: Ri = 0.90; ES+: 746.43.
Example 291
(rac.>-5-{(ifl*, 5S*)-7-{4-[3-(2-Bromo-5-fluoropheB03ty)propyllphenyl}-6-[cyclopropyl-(3,5-dimethoxybeiizyl)carbamoyl]-3^-diazabicycIo[3.3.1]non-6-en'3-yl}-5-oxopeDtanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL35 and glutaric anhydride. LC-MS: Rt = 0.88; BS+; 778.40.
Example 292
irac.)-5-({JR*, 5i5*)-7-(4-[3-(2-Bromo-5-nuorophenoxy)propyllphenyl}-6-U2-(4-methylphenyl)ethylIcycIopropyIcarbamoyI}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K and E from, bicyclononene AL36 and glutaric anhydride, LC-MS: R, = 0.90; ES+: 746.43.
Example 293
irac.)-5-{(lR*, 5.?*)-7-{4-[3-(2-Bromo-5-fluoropheDoxy)propyl]phenyl}-6-[(2-chloroben2>i)ethyIcarbamoyI]-3,9-diazabicyclo [3.3.1 lnon-6-en-3-y I}-5-oxo-pentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL22 and glutaric acid monomethylester chlonde. LC-MS: Rt = 0.94; ES+: 754.37.
Example 294
{rac.)-5-{{lR*, 55*)-7-{4-l3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-lcyclopropyl-(2-nuorobeiizyl)carbamoyl]-3,9-diazabicyclop.3.1]noD-6-eo-3-yl}-5-oiopentanoic acid metbyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL23 and glutaric acid monomethylesterchloride. LC-MS: Rt = 0.93; ES+: 750.39.
Example 295
(rac)-5-{(lR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyI}-6-(cyclopropyI-(3-trifluoromethy!beii2yI)carbamoyIJ-3,9-dia2a bicycle (3.3.1 ] -non-6-ea-3-yl}-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL24 and glutaric acid monomethylester chloride. LC-MS: Ri = 0.96; ES+: 801.40,
Example 296

(rac.)-5-{{lR*, 55*)-7-{4-[3-(2-Bromo-5-nuorophenoxy)propyi]phenyI}-6-[cyclo pro pyl-{2-methylbenzyl)c a rbamoy 11-3,9-dia2abicycIo [3.3.1 lnon-6-en-3-yI}-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL25 and glutaric acid monomethylester chloride. LC-MS: R, = 0.94; ES+: 746.43.
Example 397
(rac.)-5-((JIt*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-
{cyclopropyI-[2-{4-methoxyphenoiy)ethyl]carbamoyl}-3,9rdii.SaMc>cli-[3.3.I]Don-6-en-3-yI)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical piocedures A and E from bicyclononene AL26 and glutaric acid monomethylester chloride. LC-MS: R, = 0.93; ES+: 793.40.
Example 298
(rac)-$-{{lR*, 5^*>7-{4-[3- {cyclopropyl-[2-(3-methyIphenoxy)ethyljcarbamoyI}-3,9-diazabicyclD[33.1J-non-6-en-3-yl)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL27 and glutaric acid monomethylester chloride. LC-MS: Rt = 0.95; ES+: 776.41.
Example 299
irac.)-5-((2R*, 5^*)-7-{4-[3- {cyclopropyl-[2-(3,4-dimethyIphenoxy)ethyllcarbamoyI}-3,9-diazabicyclo-(3.3.1]noa-6-eQ-3-yI)-5-oxopentanoic acid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononene AL28 and glutaric acid monomethylester chloride, LC-MS: Ri = 0.97; ES+: 791.40.
Example 300
(rac.)-5-[(IJ{*, 55*)-7-{4-[3-(2-Bromo-5-fluoropheiioxy)propylJphenyI}-6-
(cydQpropylpheaethylcarbainoyl)-3,9-diazabicyclo[3.3.1]nQn-6-en-3-ylJ-5-oxo-pentaiioic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL29 and glutaric acid monomethylester chloride. LC-MS: Rt = 0.9^/, c?+i746.43-.- ■
Example 301
irac.)-5-((IR*, 55*h7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyI}-6-{{2-(2-chlorophenyl)ethylIcycIopropylcarbamoyI}-3,9-dia2abicycIo(33.IJaon-6-en-3-yI)-5-oxopeDtanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL30 and glutaric acid monomethylester chloride. LC-MS: Ri = 0.95; ES+: 780.38.
Example 302
(rac.y5-i{lR*, J5*)-7-{4-I3-fluorophenyl)ethyIIcycIopropyIcarbamoyl}-3,9-diazabicyclo(3.3.11non-6-en-3-yl)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL31 and glutaric acid monomethylester chloride. LC-MS: Rt = 0.94; ES+; 782.40.
Example 303

(rac.)-5-((lR*, 55*)-7-{4-[3-(2-Bromo-5-nuorophenoxy)propyI]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropyIcarbamoyl}-3,9-diazabicycIo[3J.l]oon-6-cD-3-yl)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL32 and glutaric acid monomethylester chloride. LC-MS: R,= 0.94; ES+; 764.41.
Example 304
irac.)-5-((lR*, 55*)-7-(4-[3-(2-Bromo-5-fluorophenoxy)propyI]phenyl}-6-{I2-(2-inetiiylpbcnyl)eiiiyiJfcyviopropylcarbamoyl}-3,9-diazabicyclol3-3.1]non-6-eii-3-yI)-5-oxopentaQoic acid methyl ester
Synthesized according to typical procedures A and E from bicyclononene AL33 and glutaric acid monomethylester chloride. LC-MS: R, = 0.95; ES+: 760.43.
Example 305
{rac.)-5-{(JR*, 55*)-7-{4-I3-(2-Broiuo-5-fluoropbenoxy)propyI]phenyI}-6-[cyclopropyH3,5-dimethoxybeazyl)carbamoyl]-3,9-diazabicycIo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AXi35 and glutaric acid monomethylester chloride. LC-MS: Rt = 0.93; ES+: 793.40.
Example 306
{rac.)-S-((lR*, 55*)-7-{4-l3-(2-Bromo-5-nuorophenoxy)propyllphenyl)-6-{I2-(4-methylphenyl)ethyl]cycIopropylcarbamoyi}-3,9-diazablcyclo[33.1]oon-6-en-3-yl)-5-oxopentanoic acid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononene AL36 and glutaric acid monomethyiester chloride. LC-MS; R, = 0.95; ES^: 760.42.
Example 307
{rac.)-5-{UR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenz>'l)ethylcarbamoyI]-3,9-diazabicyclo [3.3.1] non-6-en-3-yl}-2,2-di-methyl-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL22 auJ 2,2-dimetI.ylgiutiric anhydride. LC-MS: Y^ = 0.93; ES+: 768.36.
Example 308
(rac.)-5~{(JR*, 55'*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl)-6-[cy clopropy l-(2-fluoro ben2yl)carbaiii oylj -3,9-diazabicydo [3.3.1 ] non-6-en-3-yl)-2,2-dimethyI-5-oxo-pentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL23 and 2,2-diinethylglutaric anhydride. LC-MS: R, = 0.92; ES+: 764.39.
Example 309
irac.}-5-{(lR*, 55*)-7-{4-[3-(2-Bromo-5-fluoropheiioxy)propyIlphenyI}-6-{cyclopropyl-(3-trifluoromethyIbenzyi)carbamoyl]-3,9-diazabicycloI3.3.1]-Qon-6-en-3-yl}-2^-diniethyl-5-oxopentanoic acid formate salt
Synthesized accoiding to typical procedures K and E from bicyclononene AL24
and 2^-diinethylgIutaric anhydride. LC-MS: Ri = 0.94; ES+: 815.40.
Example 310

(rac.)-5-{{JR*, 55 *)-7-{4-[3-(2-Bromo-5-fluoroph en oxy)p ropyl]phenyI}-6-
[cyclQpropyl-(2-methylben2:yl)carbamoyll-3,9-diazahicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethy 1-5-0X0-pentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL25 and 2,2-dimethylglutaric anhydride. LC-MS: R, = 0.93; ES+: 760.43.
Example 311
(rac.y5'((lR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyI]phenyl}-6-{cycIopropyl-[2-(4-methbxypuenoxy)ethyij-cariuaflioyi}-3,9-diazabicyclo-[3.3.1)non-6-en-3-yl)-2,2-dimethyI-5-oxopentaQoic acid formate salt
Synthesized according to typical procedures K and E &om bicyclononene AL26 and 2,2-diraethylglutaric anhydride. LC-MS: Rt = 0.92; ES+: >805.
Example 312
(rac.y5-{(lR*, J5'*)-7-{4-[3-(2-Bromo-5-fluorophenoiy)propyIlphenyI}-6-{cyclopropyl-[2-(3-m ethylphenoxy)ethyl]-carbamoy I}-3,9-diazabicy do [3.3.1]-nott-6-en-3-yl)-2^-dimethyl-5-oxopentaiioic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL27 and 2,2-dimethylglutaric anhydride. LC-MS: Ri = 0.94; ES+: 790.47.
Example 313
{rac.)-5-{(lR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cycIopropy!-[2-(3,4-dimethylphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo-
[3.3.l]non-6-en-3-yl)-2,2-dimethyl-5-0xopentanoic acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL28 and 2,2-diniethylglutaric anhydride. LC-MS: R, = 0.95; ES+: 805.4.
Example 314
5
{rac.)-5~[{IR*, 55*)-7-{4-[3-(2-BrQmo-5-fiuorophenoxy)propyllpheayl}-6-(cyclop ropyIphenethyIcarbamoyI)-3,9-diaza bicy do [3.3.11 n on-6-en-3-ylI-2,2-dimethyI-5-oxopentanoic acid formate salt
I Synthesized according to typical procedures K and E from bicyclononene AL29 and 2,2-dimethylgIutaiic anhydddfe-hC-MS:?.; = 0.92; ES+: 760.43.
Example 315
(mc)-5-{(ii?% 55*)-7-{4-[3-{2-Bromo-5-fluorophenoxy)propyIIphenyl}-6-{[2-(2-chlorophetiyl)ethyI] cyclop ropylcarbamoyl}-3,9-diazabicy do [33.1] iion-6-eo-3-yl)-2^-dimethyl-5-oxopentanoic add formate salt
Synthesized according to typical procedures K and E from bicyclononene AL30 and 2;2-dimethylglutaric anhydride. LC-MS: R^ = 0.94; BS-i-: 794.41.
Example 316
irac)-S-({IR*, 5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2^-dlfluorophenyI)ethyl]cyclopropylcarbamoyl)-3,9-diazabicydo[3.3.11non-6-en-3-yl)-2^-dimethyl-5-oxopentaiioic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL31
and 2,2-dimethyIgIutaric anhydride. LC-MS: Ri = 0.93; ES+: 796.44.
Example 317

(rac.)'5-({lR^, 55*)-7-{4-[3-{2-Bromo-5-fluorophenoxy)propyI]pheiiyIJ-6-{[2-{4-fluorophenyl)ethyIIcyclopropyIcarbamoyJ}-3,9-diazabicycIo[3.3.11non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid formate salt
Synthesized according to typical procednies K and E from bicyclononene AL32 and 2,2-diniethyIglutaric aniiydride. LC-MS: Rt = 0.93; ES+: 778.42.
Example 318
iraa)-5-i(lR*, J5*)-7-{4-I3-(2-Brorao-5-nuorophenoxy)propyl]pheoyl}-6-{{2-(2-mefhyIphenyI)ethylIcycIopropylcarbamoyI}-3^-diiz&l!)icycIo[3.3.Iiaoh-ii-en-3-yl)-2,2-dimethyl-5-osopentanoic acid formate salt
Syathesized according to typical procedures K and E from bicyclononene AL33 and 2,2-dimethylgIutaric anhydride. LC-MS: R^ = 0.94; ES+: 774.46.
Example 319
(rflc>5-{(JjR*, 5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propylJphenylJ-6-(cyclopropyl-(3^-dimcthoxybeiizyI)carbamoyl]-3,9-diazabicycloI3J.l]non-6-ea-3-y!}-24-dimethyl-5-oxQpeiitaaQic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL35 and2,2-dimetbylglutaric anhydride. LC-MS: Rt= 0.92; ES+: >805.
Example 320
(racyS-dlR*, 55*)-7-{4-t3-(2-Bromo-5-fluorophenoxy)propyllphenyI)-6-([2-(4-metbylphenyl)ethyi] cyclop ropylcarbamoyl}-3,9-diazabicyclo [3.3.1 Jiion-6-ea-3-yl)-2,2-dimethyl-5-oxopentanoic acid formate salt

Synthesized according to t>pical procedures K and E from bicyclononene AL36 and 2,2'dimethylglutaric anhydride. LC-MS: Ri - 0.94; ES+: 774.44.
Example 321
l:l-Misture of irac.y{2R*, 3S*)-4-{U-R*, 5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyllphenyl)-6-[(2-chloroben2yi)ethylcarbaffloyl]-3,9-diazabi-cyclo[33.1]non-6-en-3-yl}-23-diliydroxy-4-oxobutyric acid formate salt and (rac.)-(25*. 5J?*)-4-{(Jif* 55*)-7-{4-[3-(2-bromo-5-fluorophenDxy)propyl]-phenyI}-6-[(2-chlorobenzyl)ethylcarbainoyl]-3,9-diazabicyclo-[3J.l]non-^-en-3-yI}-2,3-dihydroxy-4-oxobutyric acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL22 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R, = 0.87; ES-;-: 758.33.
Example 322
l:l-Mixture of (Mc.)-{2i?* 55*)-4-{Uif*, 55*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyi]pbenyl}-6-[cycIopropyl-(2-fluorobenzyl)carbamoyl]-3,9-dlazabicycIo[3>3.1jQon-6-en-3-yI}-2r3-dihydroxy-4-oxobutyric acid formate salt and (rac)'(2S*, 3R*)-4-{ilR*, 55*)-7-{4-I3-(2-bromo-5-fiuoro-phenoiy)propyl]phenyl}-6-[cycIopropyH2-fluorobenzyl)carbamoyl]-3,9-diazabicycIo[3.3.11iion-6-eii-3-yli-2^-dihydroxy-4-oxobutyric acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL23
and (S,R)-2,3-dihydroxy3uccimc anliydride. LC-MS: Rt = 0.85; ES+-. 754.37.
Example 323
l:l-Mixture of (mc.)-(2ff* i5*)-4-{(7ii% 55*)-7-{4-I3-(2-bromo-5-nuoro-pheno.\y)propyiJpheny!}-6~[cyciopropyl-(3-trifIuoromethylbenz>l)-

carbamoyl]-3,9-diazabicyc!G[3.3.11noii-6-en-3-yl}-23-dihydroxy-4'OXobutyric acid formate salt and (rac.)-{2S*. 3R*y4-{(lR*, 55*)-7-{4-[3-(2"bromo-5-fluorophenoxy)propyIl-phenyl}-6-(cyclopropyl-(3-trifluoromethylbenzyI)-carbamoyiI-3,9-diazabicycIo[3.3.1]noii-6-en-3-yI}-2,3-dihydrox>'-4-oxobutyric acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL24 and (S,R)-2,3-dihydroxysuccinJc anhydride. LC-MS: R, = 0.89; ES+: 805.4.
Example 324
l:l-Mixture of 9-dia2abicyclo[3.3.1]non-6-eD-3-yI)-23-dihydroxy-4-oxobutyric acid formate salt and (rac.H2S*, 3R*)-4-{(lR*, 55*)-7-{4-[3- Synthesized according to typical procedures K and E from bicyclononene AL25 and (S,R)-2,3-dihydroxysuccimc anhydride. LC-MS: Rt = 0.87; ES+: 750.39-
Example 325
l:l-Mixture of (fac)'(2R*, 3S*)-4-((JR*, 55*>7-{4-I3-(2-bromo-5-nuoro-
phenoxy)prDpyl]phenyl}-6-{cyclopropyl-(2-(4-methoxyphenoxy)ethyl]-
carbamoyI}-3,9-dia2abicycIo[33.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric
acid formate salt and (rac)-(2S*, 3R*)A-(UR*, 55'*)-7-{4-[3-(2-bromo-5-
fluoro-phenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]-
carbamoyl}-3,9-diazabicycloJ3.3.1]non-6-eo-3-yl)-2,3-dihydroxy-4-oxobutyric
acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL26 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS; R, = 0.86; ES+: 796.42.
Example 326
l:l-Mixture of (rac.)-(2R*, 3S')-4-((IR*, i5'*)-7-{4-[3-(2-bromo-5-nuoro-p henoxy) pro pyllphenyl}-6-{cyclop ropy 142-(3-methyIp henoxy)ethy II-carbamoyl}-3,9-diazabicyclol3.3.1]non-6-en-3-yl)-2,3-dihydrox>'-4-oxobutyric acid formate salt and (rac.)-(2S*, 3R*)-4-i{IJt% 5^*)-7-{4-[3-(2-bronio-5-fluorophenoxy)propyllpheiiyl}-6-{cycIopropyl-[2-(3-methylphenoxy)etbyi]-carIjaaii>>i}-3,9-diazai;/icyclo[3.3.1Jnon-6-en-3-yl)-2^-dihydroxy-4-oxobutyric acid formate salt
Synthesized according to typical procedures K and E &om bicyclononene AL27 ind (S;[l)-2,3-dihydroxysuccimc anhydride. LC-MS: R, = 0.88; ES+: 780.38.
Lxample 327
:1-Mixture of irac)-{2R*, 3S*)'4-(iJR*, 55*)-7-{4-(3-(2-broino-S-fluoro-ih enoxy)propyIl phenyl}-^- jcy clop ropyl-[2-{3,4-dimethyIpheDoxy)ethy I] -arbamoyl}-3,9-diazabicycIo[33.1]iion-6-en-3-yl)-23-dihydroxy-4-oxobutyric cid formate salt and {rac.)-{2S*, 3R*)-4-{{IR*, 55*)-7-{4-[3-(2-bromo-S-luorophenoxy)-propyl]phcnyI}-6-{cycIopropyI-[2-(3,4-dimethylpheno:Q')-thyIIcarbainoyl}-3,9-diazabicyclo(33.11tton-6-en-3-yI)-2^-dihydroxy-4-irobutyric acid formate salt
ynthesized according to typical procedtires K and E from bicyclononene AL28 id (S,R)-2,3-dihydroxysuccimc anhydride. LC-MS: R, = 0.89; ES+: 794.44.
(ample 328

I:l-Mixture of {rac.)-(2R*, 3S*)~i-[(lR*, 55*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyI] phenyl}-6-(cyclopropyIphenethyIcarb amoyI)-3,9-d iazabi-cyclo [3.3.1] no n-6-en-3-yI]-2,3-dihydroiy-4-oxo butyric acid formate salt and {rac)-{2S*, 3R*y4-\{lR^ 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyll-phenyI)-6-(cycIop ropy lphenethylcarbamoyl)-3,9-diazabicyclo [3,3.1 ]non-6-en-3-yl]-2,3-dihydroxy-4-oxobutyric acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL29
and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS-. Rt = 0.86; ES+: 750.36.
Example 329 -
l:l-Mixture of irac)-(2R*, 3S*)-4'i(lR*, 55*)-7-{4-[3-(2-bromo-5-nuoro-
phenoicy)propyl^plienyli-6-{t2-(2-chloroplieayl)ethylIcyclQpropylcarbamoyli-
3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-23-dihydroxy-4-oxobutyric acid
formate salt and (rac.)-{2S% J7f*)-4-((i/(*, 55*)-7-{4-[3--(2-bromo-5-fluorophenoxy)propyl]-phenyi)-6-{[2-(2-chlorophenyl)efhyI]cycIopropyl-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2^-dihydroxy-4-oiobutyTic acid formate salt
Synthesized according to typical procedures K and E fcom bicyclononene ALSO and (S^)-2,3-dihydroxysuccmic anhydride. LC-MS: R, = 0.88; ES+: 784.34.
Example 330
l:l-Mixture of iracy{2R% 3S*}A-{{1R*, 5S*)-7-{4-[3-(2-bromo-5-fluoro-
pheDOxy)propyl]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cycIopropyIcarbamoyl}-
3,9-dia2abicyclol3.3.1]non-6-en-3-yl)-23-dihydroxy-4-oxobutyric acid
formate salt and (rac.)-(2S% 3R*)-4-{ilR*, 55*)-7-{4-[3-(2-bromo-5-fluoropheno xy) propyl j-phenyl}-6-{ [2-(4-nuorophenyl)ethyl]cyclo pro pyl-carbamoyl}-3,9-diazablcyclol3.3.11nott-6-en-3-yl)-2,3-dibydroxy-4-oxobutyric acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL32 and (S,R>2,3-dihydroxysuceinic anhydride. LC-MS: R^ ^ 0.85; ES-^: 768.34.
Example 331
l:l-Mixture of (rac.)-{2R% 3S*)-4~((IS*, 55'*)-7-{4-p-(2-bromo-5-fluoro-phenoxy)propyI]phenyI}-6-{[2-(2-niethylphenyI)ethyIlcyclopropyI-carbamoy 1}-3,9-dia2abicy do (33.1] Qon-6-en-3-yl)-2,3-dihy dro3t\-4-Qxobutyric acid formate salt and {rac)-{2S*, 3R*y4-{{}R*, 55*)-7-{4-13'(2-bromo-5-nuorophenoxy)propyijpueny i}-6- {I2-(2-me iliylpL^nyl) ethyl] cyclopropyl-carbamoyI}-3,9-dia2abicycIo-[3.3.1]non-6-en-3-yI)-2,3-dihydroxj-4-oxobutyric acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL33 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS; R,= 0.88; ES+: 764.41.
Example 332
l:l-Mixture of (rac.)-(2R*, 3S*)-4-[(IR*, 55*)-7-{4-[3-{2-broino-5-fluoro-
phenoxy)p ropyl] phenyl}-6-[cyclopropyI-(3,5-dimethoxy benzy l)carbamoy 1]-
3,9-diazabicyclop.3,lJnon-6-eD-3-yI}-23-dihydroxy-4-oxobutyric acid
formate salt and (racYi^S*, 3S*)-4'{(1R*, 5S*)-7-{4-[3-{2-bromo-5-fluoro-
phen.osy)propyl]phehyl}-6-[cycIopropyl-(3^-dlmethoxybeiizyI)carbamoyll-
3,9-diaxabicyclol3.3.1]non-6-cii-3-yl}-23-dihydroxy-4-oxobatyric acid
formate salt
Syntliesized according to typical procedures K and E from bicyclononene AL35 and (S,R)-2,3-dihydroxysuccinic anliydride. LC-MS: R, = 0.86; ES+: 797.38,
Example 333

l:l-Mbtture of {rac.)-(2R*, 3S*y4~{{}R-^, 5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl] phenyl}-6-{[2-(4-mcthyIph enyl)ethyllcy clopropyJ-carbarooyI}-3,9-diazabicycIo[33.1]non-6-en-3-yl)-2^-dihydroxy-4-oxobutyric acid formate salt and {rac.)-{2S-^, 3R*)~4-((1R*, 55*)-7-{4-{3-(2-bromo-5-fluorophenoxy)propyll-phenyl}-6-{[2-(4-methylphenyl)ethyllcycIopropyl-carbaiiioyl}-3,9-dia2abicycIo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid formate salt
Synthesized according to typical procedures K and E &om bicyclononene AL36 and (S,R)-2,3-dihydroxysuccimc anhydride. LC-M5; R, = 0.87; ES+: 764.38.
Example 334
irac.y{lR*, 55*)-7-{4-[3-{2-Bromo-5-fluorophenoxy)prapyl]phenyl>-3-(4-
carbainoylbutyryO-3,9-diazabicyclo[33,ljDon-6-ene-6-carboxyUc acid (2-chIorobeiizyI)etfayIainide formate salt
Synthesized according to typical procedures G and E ftom bicyclononene AL22 and 4-carbamoylbutyric acid. LC-MS: Rj = 0.87; BS+: 739.49.
Example 335
[racyilR*, 5S*)-7-{4-13-(2-Bromo-5-fluorophenoxy)propyl]pheiiyl}-3-(4-
carbamoyIbutyryl)-3,9-diazabicycIo[33.1Jnon-6-eDe-6-carboxyUc acid
cyclopropyl-(2-fluorobeDzyl)amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL23 and 4-carbamoylbutyric acid. LC-MS: Rt = 0.86; ES+: 735.50.
Example 336

(rac.)'{lR*, 55*)-7-{4-[3-(2-Bromo-5-fluorophenQxy)propyl]pheByl}-3-(4-
carbamoylbutyryl)-3,9-diazabicyclo[3.3.l]non-6-eue-6-carboxylic acid
cycIopropyI-(2-methylbenzyi)amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL25 and 4-carbamoylbutyric acid. LC-MS: Rt = 0.88; ES+: 731.55.
Example 337
irac.)-(lS*, 55*)-7-{4-p-(2-Bromo-5-fluorophenoxy)propyI]phenyl}-3-(4-
carbamoylbutyryI)-3,9-diazabicyclo[33.1]non-6-c«t 5-carboxyI:c - ^eid cyclopropyI-[2-(4-raethoxyphenoiy)ethyI]amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL26 and 4-carbamoylbutyric acid. LC-MS: R, = 0.86; ES+: 777.52.
Example 338
{rac)-iJR*, 5i5*>-7-(4-[3-(2-Bromo-5-fluorophenoxy)propylJplienyI}-3-(4-
carbamoy!butyryl)-3,9-diazabicycIo [33.1] noil-6-ene-6-carboiylic acid
cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]amide formate salt
Synthesized according to typical procedxu^s G and E from bicyclononene AL28 and 4-carbamoylbutyric acid. LC-MSi Rt = 0.90; ES+: 775.55.
Example 339
{rac.)-{lR*, 55*)-7-(4-[3-(2-Bromo-5-fluorophenoxy)propyIlpheayl}-3-(4-
carbamoylbutyryl)-3,9-diazabicycIo[3.3.11non-6-ene-6-carboxyIic acid [2-(2-chlorophenyl)ethyl]cyclopropylamide formate salt

Syntiiesized according to typical procedures G and E from bicyclononene AL30 and 4-carbamoylbutyric acid. LC-MS: R( = 0.89; ES+: 765.46.
Example 340
(rac.)-(Jif*, 55*)-7-{4-{3-(2-Broino-5-fluorophenoxy)propylIphenyl}-3-(4-
carbamoylbutyryl)-3,9-dia2abicycIo[3.3.1Inon-6-cne-6-carboxyIicacid [2-(2,3-difluorophenyl)ethyI]cyclopropylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL31 and 4-carbamOylbatyric acid. LC-MS: R, = 0.88; ES+: 767.48.
Example 341
(rac.)-(lli*, 55*)-7-{4-[3-{2-Bromo-5-fluorophenoiy)propyl]phenyI}-3-(4-
carbamoyIbutyryI)-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxyUc acid I2-(4-fluorophenyl)ethyl]cyclopropylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL32 and 4-carbamoylbutyric acid. LC-MS: Ri = 0.87; ES+; 749.52.
Example 342
{rac)-(lR*, 55*)-7-{4-[3-(2-Bromo-5-nuorophenoiy)propyl]phenyI)-3-(4-carbamoyIbutyryl)-3^-diazabicycio[3J.l]non-6-ene-6-carboxyIic acid [2-(2-methylpbenyl)ethyl] cyclop ropylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL33 and 4-carbamoyIbutyric acid. LC-MS: Ri - 0.89; ES+: 745.54.
Example 343

(rac.)-(JS% 55*)-7-{4-{3-(2-Bromo-5-nuorophenoxy)propyllpUenyl}-3-(4-
carbamoylbutyiyl)-3,9-diazabicyclo 13.3.1 ]Don-6-ene-6-carboxy lie acid
cyclopropyI-(3,5-din]ethoxybenzyl)amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL35 and 4-carbamoylbutyric acid. LC-MS; R, = 0.S6; ES+: 777.53.
Example 344
{racy{JR*, 55*)-7-(4-[3-(2-Bromo-5-fluorGphenoxy)propyl]phenyl}-3-(4-earbauxOjlbi.tyi7l)-3,9-dia2abicycIo[3.3.1]noo-6-eQe-6-carboxyIic acid [2-{4-methylphenyl)etliyl]cyclopropylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL36 and 4-carbamoylbutyric acid. LC-MS: Rj = 0.88; ES+: 745.54.
Example 345
l:l-Mixtureof(racH5^*)-5-{UiJ*, 55*)-7-{4-[3-(2-bromo-5-flaoropheiiosy)-
)ropyl]phenyl}-6-I(2-chlorobenzyI)ethyIcarbamoyl]-3,9-diazabicyclol3^.1)-
ion-6-eii-3-yl}-3-hydroxy-5-oiopentaDoic acid formate salt and (rac.)-(3S*)-
-{(i/i* J5*)-7-{4-[3-(2-broiiio-5-fluoropheiioxy)-propyllpheiiyl}-6-[(2-
faIorobenzyl)ethylc3rbamoyl]-3,9-diazabicyclo [3.3.1] don-6-en-3-yl}-3-ydroxy-S-oxopentanoic acid formate salt
yntiiesized according to typical procedures K, E and L from bicyclononene L22 and 3~(i'er/-butyldim6thylsilyIoxy)glutaric anhydride. LC-MS; Rt = 0.87;
S+-. 756.44.
sample 346

l:l-Mixture of (i'ac.)-(3R*)-5-{(lR*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-
propyI]phenyI}-6-[cycIopropyl-(2-fluorobenz>'l)carbamoyI]-3,9-diazabicyclo-
[3.3.1]non-6-en-3-yI}-3-bydroxy-5-osopentanoic acid formate salt and (rac.)-
(3S*)-5'{(1R% 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyI]pbenyI}-6-
[cycIopropyi-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclD[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopenfanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL23 and 3-((erf-butyldimethy!siIylosy)g[utaric anhydride. LC-MS: Rt = 0.86; ES+; 752.46.
Example 347
l:l-Mixture of {rac.)-(3R*)'5-{(lR*, 55*)-7-{4-[3- Synthesized according to typical procedures K, E and L from bicyclononene AL24 and 3-(re^^blItyld^methylsilyloxy)gllItaric anhydride. LC-MS: Rt = 0.89; ES+: 803.40.
Example 348
l;l-Mixture of {rac.)-{3R*)-5-{{}R*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyilphenyl}-6-lcyclopropyl-(2-methylbenzy!)carbanioyll-3,9-dia2a-bicyclo[33.llnon-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid formate salt and {rac,)'{3S*y5-{ilR*, 5^*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyllphenyl}-6-[cycIopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabjcyclo-[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid formate salt
5

Synthesized according to typical procedmes K, E and L &om bicyclononene AL25 and 3-(;'e/-?-butyldimethyIsiIyloxy)glutaric anhydride. LC-iMS: R, = 0.87; ES+: 748.52.
Example 349
l:l-Mlxture of (rac.)-{3R*)-5-{ilR*, 5ir*)-7-{4-t3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{cyclopropyl-I2-(4-methoxyphenoxy)ethyl}carbamoyl}-3,9-diazabicycIo[3.3.1]noa-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and (rac.)-(3S*)-5-{/JR*, 5^*)-'T-{M3-{?-bromo-5-fluorophenoKy)propyi]-pheByl}-6-{cycIopropyl-i2-(4-methoxypheaoxy)ethyllcarbaraoyl}-3,9-diaza-bicycIo[33.1]noD-6-en-3-yl)-3-hydroxy-5-oxopentaooic acid formate salt
Synthesized according to typical procedures BC, E and L from bicyclonotiene AL26 and 3-(/er/-butyldimethylsi]yloxy)glutaric anhydride. LC-MS: Rt = 0.86; ES+: 794.40.
Example 350
l:l-Miiture of {rac)-{3R*)-5-(iIR*, 5^*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyIlphenyI}-6-{cycIopropyl-[2-(3-methylphenoxy)ethyIIcarbamoyI}-3,9-diazabicyclo[33.1]non-6-en-3-yI)-3-hydroxy-5-oxopentanoJc acid formate salt and (raa)-{3S*)-5-((IR*, 55*)-7-{4-[3-(2-bromo-5-fluoropheiioxy)propyl]-phenyl)-6-{cyclopropyI-[2-(3-methyIphenoxy)ethyl]carbamoyI}-3,9-diazabi-cyclol33.11noa-6-en-3-yI)-3-hydroxy-5-oxopentattoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL27 and 3-(/err-butyidimethylsilyIoxy)glutaric anhydride. LC-MS: Ri = 0.89;
ES-V: 778.52.
Example 351

l:l-Mixture of irac.)'(3R*)-5-((JR*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoiy)-propyI]phenyl}-6-{cyclopropyI-[2-(3,4-dimethyIphenoxy)ethyI]carbamoyl}-3,9-diazabicydo[3.3.1 ]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and {tac.)-{3S*)-S-{{lR*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{cyclopropyl-[2-(3,4-dimetbyIphenoxy)ethyl]carbaraoyl}-3,9-diaza-bicyclo[3,3.1]-non-6-en-3-yI)-3-hydroxj'-5-oxopeiitanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL28 and 3-(fer/-butyldimethylsilyioxy)gIutaric anhydride. LC-MS: Rt = 0.90;
ES+: 792.42. ' --■■■>
Example 352
l:l-Mixture of (rac.)-i3R*)'5-[(lR*, 55*)-7-{4~[3- Synthesized according to typical procedures K, E and L from bicyclononene AL29 and 3-(ter(-butyldimethylsiIylQxy)glutaric anhydride. LC-MS; R* = 0.86; ES+: 748.50.
Example 353
l:l-MLxture of (rac.y(3R*)-5-(ilR*, J5*)-7-{4-I3-(2-bromo-5-nuorophenoxy)-propyl]piienyI}-6-{[2-(2-chIorophenyl)ethyl)cyclopropyIcarbamoyi}-3,9-diaiabicyclio[3.3.11non-6-en-3-yl)-3-hydroxy-5-oxopeatanoic acid formate salt and (rac.y(3R*)-5-((JR*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyI]-

phenyl}-5-{[2-(2-chlorophenyI)ethy]]cycIopropyIcarbamoyl}-3,9-dia2a-bicyclop J.llnon-6-en-3-yl)-3-hydroxy-5-QxopentaQoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene 5 AL30 and 3-(fcr/-butyldimethylsilyloxy)glutaric anhydride. LC-MS: Rt = 0.88; ES+: 782.49.
Example 354
I l:l-Mixture of (rac.)-(3R*y5-({}Jt*, 5J*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyllphenyl}-6-{[2-(2^-difluorophenyl)et(jyiiP*fJopr(*nyicarbaTnoyi}-^,9-diazabicyclo(3.3.11iion-6-en-3-yl)-3-hydroxy-5-osopentanoic acid formate salt and (rac)-(3i?*)-5-((iif* 55*)-7-t4-l3-(2-broino-5-fluoropfaenosy)propyll-phenyl}-6-{(2-(2^-dif]uorophcnyl)ethyI] cyclop ropylcarbamoyi }-3,9-diazabi-cyclo(33.11aon-6-en-3-yl)-3-hydroxy-5-osopentanoic acid formate salt
Synthesized accordiag to typical procedures K, E and L from bicyclononene AL31 and 3-(/ert-butyldimethylsilyloxy)glutaric anhydride. LC-MS; R* = 0.88; ES4-: 784.53.
Example 355
l:l-Mixfure of (rac.y(3R*)-5-(iJR*, 55*)-7-{4-[3-(2-bromo-5-fIuoropheDOiy)-propyl]pheayl>-6-{[2-(4-fluoropheiiyI)ctfayllcyclopropylcarbamoylJ-3,9-diaza-bicyclop3.1]non-6-eii-3-yl)-3-hydroxy-5-oxopeiitanoic acid formate salt and {racy{3R*)-5-{{lR*, 5>S*)-7-{4-I3-(2-bromo-5-auorophett03cy)propyllphenyI}-6-{[2-(4-fluorophenyl)ethyl]cyclopropyIcarbamoyI}-3,9-diazabicyclo[3.3.1]-ii«a-6-eii-3-yl)-3-hydroxy-5-oxopeataQoic acid formate salt
Synthesized according fo typical procedures K, E and L from bicyclononene AL,32 and 3-('^^'-butyldimethylsilyloxy)giutaric anhydride. LC-MS; Rt = 0.87; ES+: 766.47.

Example 356
l:l-Mixture of (rac.)-{3R*)-S-((lR*, 55*)-7-{4-[3-{2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{{2-(2-methylphenyI)ethyl]cyclopropylcarbainoyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yI)-3-hydroxy-5-oxopentanoic acid formate salt and (rac.y{3J{*)-5'((lR*, 5,S'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyI]-phenyI}-6-{[2-(2-methylphenyI)ethyI]cycIopropylcarbantoyI}-3,9-dia2abi-cycIo[3.3.IInon-^-en-3-yI)-3-hydroiy-5-oxopentanoic acid formate salt
Synthesized according to typical procedm-es K, E and L ftom bicyclononene AL33 and 3-(rer/-butyldiniethylsilyloxy)glutaric anhydride. LC-MS: R, = 0.88;
ES+: 762.55.
Example 357
l:l-Mixt«re of (rac.)'(3R*)-5-{(lR*, 5,y*)-7-{4-[3-(2-bromo-5"fluorophenos:y)-propyl]phenyi}-6-[cyc!opropyi-(3,5-dimethoxybenzyI)carbamoyl]-3,9-diaza-bicyclo[33.1]non-6-eii-3-yI}-3-hydroxy-5-oxopentanoic acid fonnate salt and irac)-i3S*)-5-{(lR% 55*)-7-{4-[3-(2-bromo-S-fluorophenoxy)propyl]phenyl}-6-Icyclopropyl-(3,5-dimethoxybenzyl)carbamoyI]-3,9-diazabicydo-[3.3.11non-6-en-3-yl|-3-hydroxy-5-oxopentanoic acid fonnate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL35 and 3-(/err-butyldimethylsilyloxy)glutaric anhydride. LC-MS: Rt - 0.86; ES+: 794.38.
Example 358
l:l-Mixtttre of {rac.)-(3R*)'5-{(lR*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyI]phenyl}-6-{[2-(4-methylphenyl)ethyI]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.I]non-6-en-3-yl)-3-bydroxy-5-oxopentanoic acid formate salt

and (rac.)-(3R*y5-(lim*, 55*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyI}-6-{[2-(4-methylphenyl)ethyllcyclopropylcarbamoyl}-3,9-diazabi-cydo[3.3.1]non-6-en-3-yI)-3-hydroac>-5-oxopenfanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicydononene AL36 and 3-(fer/-butyldimethylsilyIoxy)gImaric anhydride. LC-MS: R, = 0.8S; ES+: 762.55.
Example 359
l:i-Mi-rture -f (rac.)-{3R*yS-{(JR% 55>6-{cyclopropyl-I2-(2-hydroxyi;byi;-
beazylJcarbamoyl}-7-{4-[3-(23,6-trifluorophenoxy)propyl]phenyl}-3,9~diaza-
bicyclQ[33,ljaon-6-eii-3-yl)-3-hydroxy-5-oiopentaaQic acid formate salt and
(rac.)-{3S*)-5-{{lR*, J5*)-6-{cyclopropyl-l2-(2-hydroxyethyl)benzyl]-
carbamoyl}-7'{4-[3-{2,3,6-trifluorophenos:y)propyIJpIienyl}-3,9-diazflbicycIo-[3.3,l|non-6-ett-3-yI)-3-hydroxy-5-oxopeataiiQic acid formate salt
Synthesized according to typical procedures K, E and L from bicydononene AL19 and 3-('err-butyldiinethyIsilyloxy)gIutaric anhydride. LC-MS: Rt = 0.81;
ES+: 736.54.
Example 360
(racyiJR*, 5,S*)-3-AcetyI-7-{4-I2-(2^,5-trimetbylpheiioxy)ethyIlphenyI}-3,9-diazabicycIo[3.3.11non-^-eDe-6-carboiyIic acid (2-chIorobenzyl)cyclopropyi-amide formate salt
Synthesized according to typical procedures A and E from bicydononene AL38
and acetyl chloride. LC-MS: R, - 0.93; ES-t-: 612.52.
Example 361

(rac.)-(lR*, 55*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]plienyI}-3,9-diazabicyclo[3.3.11noii-6-ene-6-carboxylic acid (2-ch\orobenzyl)ethylamide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL40 and acetyl chloride. LC-MS: Rt = 0.93; ES+: 600.50.
Example 362
{rac.)-{lR*, 5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethyIphenoxy)ethyllphenyl}-3,9-diazabicyclo[3.3.ijnoii-b-ene-6-»:arbox>'Uc acid (2-fluorobenzyI)cycIopropyl-amide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL41 and acetyl chloride. LC-MS: Rt = 0.91; ES+: 596.53.
Example 363
(racXlR*, 55'*)-3-Acetyl-7-{4-[2-(23,5-trimethylphenoxy)ethyIlphenyI}-3,9-diazabicydol3.3.1]noii-6-ene-6-carboxylic acid (S-trifluoromethylbenzyl)-cyctopropylamide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL42 and acetyl chloride. LC-MS: Rt = 0.95; ES+: 646.54.
Example 364
(rdC-Xiif*, 5S*)-3-AcetyI-7-{4-I2-(23,5-trimethylplienoxy)ethyllphenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-mefhylbenzyI)cyclopropyl~ amide formate salt

S^thesized according to typical procedures A and E from bicyclononene AL43 and acet>-l chloride. LC-MS: R, = 0.93; ES+: 592.56.
Example 365
irac.)-(JR*, 55*)-3-AcetyI-7-{4-(2-(2,3,5'trimethylphenoxy)ethyI]phenyl}-3,9-dlazabicyclo[3.3.11non-6-ene-6-carboxyIic acid cyclopropyI-[2-(4-methoxy-phenoxy)etfayl]aiiiide formate salt
Syntliesized according to typical procedures A and E from bicyclononene AL44 and acetyl c^Dride. LC-MS: Rt = 0-.93; bS+: 638.58.
Example 366
(rac)-5-((ifl*, 55*)-6-[(2-ChIorobenzs'I)cyclopropylcarbamoylJ-7-{4-l2-(2^^ trimetbylpheaoxy)etfayllp henyl J -3,9-dia2abicycIo (3.3.11 non-6-en-3-y I)-5-oxo-pentanoic acid formate salt
Synthesized according to typical procedures K and E Jrom bicyclononene AL38 and glutaric anhydride. LC-MS: Rj = 0.91; ES+: 684.54.
Example 367
{racys-iillt*, 55*)-6-(BeiizyIcycIopropyIcarbamoyI)-7-{4-[2-{2^^-trimethyl-phenoxy)efhyl]phenyl)-3,9-diazabicycIo[3.3.1Jiion-6-en-3-yl)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL39
and glutaric anhydride. LC-MS: R^ = 0.89; ES+: 650.57.
Example 368

(racyS-aiR*, 55*)-6-l(2~ChIorobeiizyl)ethylcarbamoyl]-7-{4-[2-(2,3,5-
trimethylphenoxy)ethyl}phenyJ}-3,9-diazabicyclo|3.3.1]non-6-en-3-yr)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL40 and glutaric anhydride, LC-MS: R, = 0.90; ES+: 672.55.
Example 369
(rac.)-5-((iiI*, 55*)-6~((2-FluorobenzyI)cyclopropyicarbamoyl]-7-{4-l2-(2;3,5-triniethylphenoxy)ethyl]phenyi}-3,9-diazabicyi;lo[3.3.1]nou-6-en-3-yl)-5-oxo-pentanoic acid formate salt
Synthesized according to typical piocedures K, and E from bicyclononene AL41 and glutaric anhydride. LC-MS: Rt = 0.89; ES+: 668.57.
Example 370
{racy5-{(JR*, 55'*)-6-[(3-Trifluoromethylbeiizyl)cycIopropykarbamoyll-7-{4-[2-(23,5-trimethylpheiioxy)ethyllphenyli-3 ^-diazabicyclo [3.3.11iioa-6-en-3-yl)-5-oxo-pentaaoic acid fonnate salt
Synthesized according to typical procedures K and E from bicyclononene AI142 and glutaric anhydride. LC-MS: Rt= 0.92; ES+: 718.52.
Example 371
(rac.)-5-((JJi*, 55*)-6-[(2-Methylbenzyl)cyclopropylcarbamoyI]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyIlpheDyI}-3,9-diazabicycIo[3.3.1|non-6-en-3-yl)-5-oxo-peatanoic acid formate salt

Synthesized according to typical procedures K and E from bicyclononene Al-43 and glutaric anhydride. LC-MS: Rt = 0.90; ES+: 664.59.
Example 372
(rac.)-5-({IR*, 55'*)-6-{Cyclopropyl-[2-(4-niethoxj'phenoxy)ethyllcarbainoyl}-7-{4-[2-(23,5-trimethyIphenoxy)ethyl]pheHyI}-3,9-diazabicyclo[3.3.Iinon-6-en-3-yl)-5-oxopenlanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL44
and glutaric anhydride. LC-MS: Rt = 0.89; ES+: 710.56. ->.
Example 373
{rac.)-5-{(lR*, 55*)-6-{Cyclopropyl-|2-(3-methoxyphenoxy)ethyllcarbamoyl}-7- {4-l2-(2 3,5-trimethylpb enoxy)ethyl] phenyl} -3,9-diazabicycio [3.3.11 non-6-en-3-yl)-5-oxopenfanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL45 and glutaric anhydride. LC-MS: Ri = 0.90; ES+: 710.54.
Example 374
(racyS-iilR*, 55*)-6-{CyclopropyI-l2-(3-methylphenoxy)ethyl]carbaiaoyl}-7-{4-[2-(23>5-trimethyIplienoxy)ethyIlphenyl}-3,9-dia2abicyclo(33.1]noii-6-eB-3-yI)-5-oxopentanoic acid formate salt
Synthesized according to typical procediures K and E from bicyclononene AL46 and glutaric anhydride. LC-MS: R, = 0.92; ES+: 694.57.
Example 375

{yacyS'iilR*, 5S'*)-6-K2-Chlorobenzyl)ethy\carbamoyI]-7-{4-(2-(2,3,5-
f rimethylph en oxy) ethyll phenyI}-3,9-diazabicy do [3.3.1 lnon-6-en-3-yl)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from "bicyclononene AL40 and glutaric acid niononiethylester chloride. LC-MS; Rt=0.96; ES+: 686.54.
Example 376
(rac)-5-((ifi*, 55*>-6-lCycIopropyl-(2-fluorobeiizyt)carbamoylJ-7-{4-p-
(2^^-trimethyIphenoxy)ethy(]phenyI}-3,9-diazabicycIo{33.1]non-o-en-3-yl)-5-oxopentanoic acid methyl ester
Synthesized according to typical procedures A and E from bicyclononene AL41 and glutaric acid monomethylester chloride. LC-MS: Rt = 0.94; ES+: 682.57.
Example 377
{rac)-5-(i]R*, 55*}-6-[CyclopropyI-(2-methyIbenzyl)carbamoylI-7-{4-[2-
(2^4-trimethylphenoxy)ethyl]phenyI}-3,9-dia2abicycIo[33.1]non-6-eii-3-yl)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL43 and glutaric acid monomethylester chloride. LC-MS: R) = 0.96; ES+: 678.6L
Example 378
(rac)-5~i(IR*, 55*H-[(2-ChIorobenzyl)cycIopropylcarbamoyll-7-{4-I2-(2,3,5-trimethyIphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3,3.1]non-6-en-3-yI)-2^-dimethyi-5-oxopentanoic acid formate salt

Syntliesized according to typical procedures K and E from bicyclononene AL3S and 2,2-dimethylglutaric anhydride. LC-MS: R, = 0.94; BS+: 712.51.
Example 379
(rac.y5~(ilR*, 5^*)-6-(Benzj'lcyciopropyIcarbamoyl)-7-(4-[2-(23,5-trimethyi-pheno}[y)ethyl]phenyI}-3,9-diazabicyclo[3.3.11non-6-en-3-yl)-2,2-dimetliyl-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL39 and2,2 dimethylglutaric anhydride. LC-MS: R, = 0.93; ES+: 678.60. ^"- '
Example 380
(rac)-5-((JR*, 5^*)-6-[(2-ChIoroben2yI)ethylcarbamoyI]-7-{4-[2-(23>
frimetliylphenoxy)ethyl]phenyl}-3,9-diazabicyclo [3.3.1 Jnon-6-en-3-yl)-2,2-(limethyl-5-oxopentaDoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononeae AL40 and 2,2-dimethylglutaric anhydride. LC-MS: R, = 0.94; ES+; 700.52.
Example 381
(racyS-dlR*, 55*)-6-ICycIopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[2-
(33,5-trimethylphem>xy)ethyllpheayI}-3,9-dia2abicyclo[33.11non-6-en-3-y!)-2,2-dimethyI-5-oxopentaDoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL41 and 2,2-diiiiethylglutaric anhydride. LC-MS; R, = 0.93; ES+: 696.57.
Example 382

{rac.)-5-{(lR*, 5S*)-6-|Cyc]opropyl-(2-methylbeDzyl)carbamoyl)-7-{4-I2-
(2,3,5-f rim ethylphenoxy)etliyl] phenyl}-3,9-dia2abicycio [3.3.1 ]n on -6-eD-3-yl)-2,2-dimethyl-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL43 and 2,2-dimethylglutaric anhydride. LC-MS: R, = 0.94; ES+; 692.60.
Example 383
Ill-Mixture of (mc)-(JJ(*)-4-((iJe* jL5*)-6-[cycIopropyI-(2-methylbeozyI)-
carbamoyll-7-{4-I2-\i,53-t«i>"BtbyIphenosy)ethyl]pheayl}-3,9-diazabicyclo-
[3.3.1]non-6-eii-3-yI)-2,3-dihydroxy-4-oxobufyric acid formate salt and (raa)-
i3S*)-4-i(JR*, 5^*)-6-(cyclopropyI-(2-methyIbenzyl)carbamoyI]-7-{4-[2-
(23^trimethy\phenosy)ethyl]pheiiyl}-3,9-diazabicyclot3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oiobutyric acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL43 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R, = 0,87; ES+: 682.57.
Example 384
(rac>(ifi* 55*)-3-(4-CarbamoyIbutyryl)-7-{4-[2-(2^^-trimetliylphenoxy)-ethyI]phenyl}-3,9-diazabicyclo [3-3.1] non-6-ene-6-carboiylic acid benzyl-cyclopropylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL39
and 4-carbamoyIbutyric acid. LC-MS: Ri = 0.87; ES+: 649.59.
Example 385

(racHIR*, 55*)-3-(4-CarbamoyIbutyryl)-7-(4-[2-(23,5-trimethyIphenosy)-ethyllphenyi}-3,9-diazabicyclo[3.3.1lDon-6-ene-6-earbox}'lic acid (2-chIoro-beQzyl)ethytamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL40 and 4-carbamoyIbutyric acid. LC-MS: Rt = 0.88; ES+: 671.56.
Example 386
{rac.)-(lR*, 55*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2,3,5-trimetUylphenoxy)-ethylJpiicnyl}-3,9-dia7abicyciop;'* !i]non-6-ene-6-carboxyljc acid cyclopropyl-(2-fluorobeDzyl)amide formate salt
Synthesized according to typical procedures G and E irom bicyclononene AL41 and 4-carbamoyIbutyric acid. LC-MS: Rt = 0.87; ES+: 667.6.
Example 387
(rac)-(Jit*, 5S*)-7-{4-13-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3,9-
diazabicycio(33.1]non-6-ene-6'CarboxyIic acid (2-chlorobenzyl)cthylaiiiide formate salt
Synthesized according to typical procedure E from bicyclononene AK22. LC-MS: Rt = 0.84; ES+: 628.36.
Example 388
7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo(3.3.1J-non-6-ene-6-carboxylic acid cyeIopropyI-(3,5-dimethoxybenzyI)^niide formate salt

Syntiiesized according to typical procedure E from bicyclononene AK35. LC-MS; Rt= 0.84; ES+: 666.43.
Example 389
7-{4-[3-(2-Bromo-5-fluorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.1]-noD-6-ene-6-carboxylic acid cyclop ropy l-(2-mefhyIbenzyl)amide formate salt
Synthesized according to typical procedure E from bicyclononene AK25. LC-MS;Rt = 0.85; ES+: 618.41.
Example 390
7-{4-[3-(2-B rem o-5-nuorDpheiioxy)propyll phenyl j-3,9-diazabicyclo [33.1]-non-6-ene-6-carboiylic acid cyclopropyl-[2-(4-methoxypheno3ty)ethyl] amide formate salt
Synthesized according to typical procedure E from bicyclononene AK26. LC-MS:Rt= 0.84; ES+; 664.43.
Example 391
l:l-Mixture of (IR, 55)-7-{4-[3-(2-bromo-5-fluoropheiioxy)propyl]phenyl}-3-((25, 4R)-4-bydroxypyrroUdme-2-carbonyl)-3^-diazabicyclo|33.1]iion-6-ene-6-carboxyIic acid cyclopropyI-(3,5-dimethoxybeiizyl)amide formate salt and (IS, 5fi)-7-{4-[3-(2-bromo-5-fluoropheaoxy)propyI]phenyl}-3-((25, 4R)-4-hydroKypyrroUdine-2-carboayl)-3»9-dia2abicycIol3.3.11nQa-6-eQe-6-carbosy-lic acid cyclopropyI-(3,5-dimethoxybenzyl)amide formate salt
Synthesized according to typical procedures G, E and L from bicyclononene AL35 and BOC-L-hydroxyproline. LC-MS: Ri = 0.80; ES+: 777.50.

(rac.)-5'{(lR*, 5j;'*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyI}-6-[(2-cbloroben2yl)cyclopropyIcarbamoyl]-3,9-diazabicycIo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyciononene AL20 and glutaric anhydride. LC-MS: R[ = 0.89; ES-i-: 752.43.
Example 393
(rac.y5-{iIR% 55*)-7-{4-[3-(2-Bromo-5-fluoropheDOxy)propyllphenyl}-6-[(2-chlorobenzyl)cyciopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopeatanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyciononene AL20 and glutaric acid monomethylester chloride. LC-MS: Rt = 0.95; ES+: 766-42.
Example 394
(rac)-5-K^^*» 5S*)-7-{443-(2-Bromo-5-fluorophenoxy>propyllphenyli-€-K2-chlorobenzyI)cyciopropyIcarbamoylI-3,9-diazabicycIo[3,3.11non-6-en-3-yl}-2^-dimethyl-S-oxopeiitaDoic acid formate salt
Synthesized according to typical procedures K and E from bicyciononene AL20 and 2,2-dimethylglutaric anhydride. LC-MS; R, = 0.93; ES+: 780.46.
Example 395
l:l-Mixture of (rac.)-(ift*)-4-{(i^*, 55*)-7-{4-13-(2-bromo-5-fluoropheiioxy)-propyl]pheayl)-6-[(2-chlorobenzyl)cyeIopropylcarbainoyl}-3,9-diazabicyclo-13.3.1]non-6-en-3-yt}-23-dihydrox\-4-os:obutyric acid formate salt and {rac.y

(,3S*)-4~{(1R*, 55*)-7-{4-[3-(2-bromo-5-nuorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarb am oyI]-3,9-diazabicyclo-[3.3.1] non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric acid formate salt
Synthesized accordmg to typical procedures K and B from bicyclononene AL20 and me5o-dihydroxysuccinic anhydride. LC-MS: R, = 0.87; ES+: 770.37.
Example 396
(roa)-5-{(iff*, 5^*H-[3-(2-Bromo-5-fluorophenoxy)propyI]phenyI}-3-(4-
carbamoy!butyryl)-3,9-diazabicydo[3J.l]non-6-ene-6-carbox.yuc acid (2-' cblorobeiizyl)cyclopropylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL20 and 4-carbamoylbutyric acid. LC-MS: R, ^ 0.88; ES+: 751.44.
Ei;ample 397
{rac)-5'((lS*, 55'*)-6-(BeiizylcycIopropylcarbamoyl)-7-(4-[3-(2-bromO'5-
fluorophenoxy)propyI]pheniyl}-3,9-diaiabicycio[3.3.11non-6-en-3-yi)-5-oxo-pentanoic acid formate salt
Synthesized accocding to typical procedures K. and E from bicyclononene AL21 and glutaric anhydride. LC-MS: R, = 0.88; ES+: 718.46.
Example 398
(rac.)-5-((lR*, 5S*)-6-(BenzykycIopropylcarbamoyl)-7-{4-[3-(2-bromo-5-
fluoroplienoxy)propyIIphenyl}-3,9-diazabicycIo[3.3.1]noo-6-en-3-yl)-5-oxo-pentanoic acid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyciononene AL21 and glutaric acid monomethylester chloride. LC-MS; R, = 0.93; ES+: 732.49.
Example 399
1: l-Mixtnre of {rac. )-(2R * 3S*)-4-({lR *, 55*)-6-(benzylcycIopropyl-carbamoyI)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyI]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-en-3-yl)-2^-dihydroxy-4-oxobutyric acid formate salt and (rac.y{2S% 3R*y4-{{2R% 55*)-6-(ben2ylcydopropylcarbamoyI)-7-{4-[3-(2-bromo-5-fluoropheQO]cy)propyl]pUeByl}-3,9-diazabicyclo[3.3.11non-6-ett-3-yI)-23-difaydroxy-4-oxobutyric acid formate salt
Synthesized according to typical procedures K and E from bicyciononene AL21 and (S,R)-23-dihydroxys\iccinic anhydride. LC-MS". R, = 0.86; ES+-. 736.43.
Example 400
irac.)'{lR*, 55*)-7-{4-[3'(2-Bromo-5-fluorophenoxy>propyllphenyi}-3-(4-
carbamoyIbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid
benzylcyclopropylamide formate salt
Synthesized according to typical procedures G and E from bicyciononene AL21 and 4-carbamoylbutyric acid. LC-MS: R^ = 0.86; ES+: 717.46.
Example 401
l:l-Mixture of (rac,)~5-{(lR*, 55*)-7-{4-t3-(2-bromo-5-fluoroplienoxy)-propyI]phenyl}-6-[((2^*)-2-hydroxy-2-pheiiylethyl)methylcarbamoyl]-3,9-diazabicycIo[3.3.1]aon-6-en-3-yI}-5-oxopentanoic acid formate salt and {rac.)-5-KiR*, 5S*)-7-{4-13-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-U(25*)-2-hydroiy-2-pheayIethyl)methylcarbanioyl]-3,9-diaiabicyclo[3.3.11non-6-eii-3-yl}-5-Gxopentanoic acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL34 and glutaric anhydride. LC-MS: R, = 0.85 ; ES+: 722.46
Example 402
l:l-Mixture of (rac.)-5-{(iR*, 55*)-7-{4-P-(2-bromo-5-fluorophenoxy)-propyi]phenyi}-6-[((2ff*)-2-hydroxy-2-phenyIethyI)methylcarbamoyl]-3,9-diazabicycio [3.3.1] non-6-en-3-yI}-5-oxo pen tanoic acid methyl ester formate salt and {r(ic.)-5-{{}R*, 55*)-7-{4-[3-(2-bromo-5-nuorophenoxy)propyl]-phenyl}-6-[((2A"'*>-2-iiydroxy-2-phenyIethyl)methyIcarbamoyIl-3,9-dia2a-bicycI-[3.3.1]non-6-^n-3-yI}-5-oxopentaDoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL34 and glutaric acid raonomethylester chloride. LC-MS: Rt = 0.88 ; ES+: 736.46
Example 403
l:l-Mixtnre of (rac.)-5-[(lR*, 5J*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyllpbenyl}-6-(((2i{*)-2-hydroiy-2-phenylethyl)methylcarbamoyl]-3,9-dia2abicycloI3.3.1]non-6-en-3-yl}-2^-dimethyl-5-oxopentanoic acid formate salt and (rac.)-5~{(IR*, 55^7-{4-[3-(2-bromo-5-fIuorophenoxy)propyll-pfaenyl}-6-[((25'*)-2-hydrory-2-phenyiethyl)methylcarbamoyl]-3,9-diaza-bicyclo [3 J.lInon-6-en-3-yl}-2,2-dimetliyl-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL34 and 2,2-dimethylglutaric anhydride. LC-MS: Rt= 0.88 ; ES+-. 750.47
Example 404
I:l-Mixture of {rac.)'(JR*, 55*)-7-{4-[3-(2-bromo-5-fIuorophenoxy)propyI]-phenyl}-3-(4-carbamoyibutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6~earboxy-

lie acid ((2ii*)-2-hydroxy-2-phenylethyl)methylaniide formate salt and (rac.)-(IR*, J'S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyI]-phenyI}-3-(4-carba-moyibut>TyI)-3,9-diazabicycIo[3.3.1]non-6-ene-6-carbox}'lic acid ((2R*)-2-hydroxy-2-phenylethyl)metliylamide formate salt
Syntliesized according to typical procedures G and E from bicyclononene AL34 and 4-carbamoyIbutyiic acid. LC-MS: R, = 0.82 ; ES+: 721.46
Example 405
i:l-Mixti»re of ('■'"■)-{.''*>-5-{ Synthesized according to typical procedures K, E and L from bicyclononene AL20 and 3-(i'err-butyLdimetliylsilyloxy)glutaric anhydride. LC-MS: JU = 0.88 ; ES+: 768.40
Example 406
l:l-Mixture of (rac.)-{3R*)-5'{(lR*, 55*)-6-(benzylcyclopropyIcarbamoyl)-7-
{4-[3-(2-bromo-5-{luorophenoxy)propyllphenyl}-3,9-diaiabicyclol3.3.11non-
6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and (rac.)-(35*)-5-
((JR*, 55*)-6-(beiizyIcyclopropyIcarbamoyI)-7-{4-I3-(2-bromo-5-fluoro-
phenoxy)propyl]phenyl}-3,9-diaza bicycle [3.3.1] noD-6-eo-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K, E and L from bicyclononene ALU and 3-(rerf-butyldimethylsilyloxy)glutaric anhydride. LC-MS: Rt = 0.86 ; ES+-. 734.47
Example 407
{racyilR*, 55*)-7-{4-[2-(2-Chloro-4,5-dimethylphenosy)ethoxylpheny!}-3,9-diazabicyclo[3.3.11aon-6-eiie-6-carboxyIic acid [2-(2-chlorophenyl)ethyll-cyclopropylamide formate salt
Synthesized according to tytjlcal pioceduie E Tiv/iii bicyclononene AK65. LC-MS: R, = 0.84 ; ES+: 620^45
E^tample 408
(rac)-(lR*, 55*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxyJphenyl}-3,9-diazabicyclo [3.3.1] noD-6-enc-6-car boxy lie acid cyclopropyl-(3,5-dimethosy-benzyl)amide formate salt
Synthesized according to typical procedure E from bicyclononene AK70. LC-MS; R, = 0.84 ; ES+: 7632.32
Example 409
(racyilR*, 55*)-7-{4-[2- Synthesized according to typical procedure E from bicyclononene AK71. LC-MS: R^ = 0.85 ; ES+: 600.29
Example 410

{rac.)-(lR*, 55*)-3-Acetyl-7-{4-I2-(4-bromophenoxy)etho\-y]phenyl}-3,9-
diazabicyclo[3.3,l)non-6-ene-5-carboxylic acid (2-chlorobeoz>i)cyclopropyl-amide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL73 and acet>I chloride. LC-MS: R, = 0.90 ; ES+: 664.33
Example 411
{raayilR*, 55*)-3-Acet3^7-{4 [2 (4-br3EOpheaoTy)ethosylphenyl}-3,9-
dia2abicyclo[33.1]non-6-ene-6-carbosylic acid cyclopropyl-(3,5-dimethoxy-beiizyl)amide formate salt
Syn^esized according to typical procedures A and £ from bicyclononene ALSS and acetyl chloride. LC-MS: El, = 0.88 ; ES+: 690.36
Example 412
irac.y5'{(lR*, 55*)-7-{4-[2-(4-BromopheQoxy)ethoxy!phenyl}-6-[(2-chloro-benzyi)cyclopropylcarbamoylJ-3^-diazabicycIo [3.3.1 lnon-6-en-3-yl}-5-oxo-pentaooic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL73 and glutaric anhydride. LC-MS; R Example 413
(rac.)-5-({lR*, 5^*)-6-(BenzylcyclopropyIcarbamoyl)-7-{4-[2-(4-bromo-
pbenoxy)ethoxy]plienyI}-3,9-diazabicydo[3.3.1]non-6-en-3-yl)-5-oxopenta-noic acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL74 and giutaric anhydride. LC-MS: R, = 0,85 ; ES+: 702.33
Example 414
(rac.y5-{(IR*, 55*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyI}-6-[cyclopropyI-(2-fluorobeDzyI)carbamoyll-3,9-diazabicyclo[3.3.1]non-6-eii-3-yI}-5-oso-pcntanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL76
and giutaric anhydride. LC-MS; R,== 0.86 ; ES+: 720.33 " * •■■.■..^..-....,.,,
Example 415
(rac.)-5-{(JR*, J5*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl~ (3-trifluoromethylbenzyl)carbamoyI]-3,9-diazabicycIoI33.11non-6-en-3-yl}-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL77 and giutaric anhydride. LC-MS: R^ = 0.89 ; BS+: 770.27
Example 416
(rac)-5-{(ii?* 55*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cycIopropyI-(2-methyIbenzyI)carbamoyl]-3,9-diazabicycIo[3.3.1Jnon-6-eDi-3-yI}-5-oxo-peDtanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL78 and giutaric anhydride. LC-MS: R, = 0.87 ; ES+: 716.34
Example 417

{tacyS-lilR*, 55*)-7-{4-[2-(4-BromopIienoxy)ethoxyIphenyI}-6-{cyclo-
propyl[2-{3,4-dimetbylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]noii-6-en-3-yl}-5-oxo-peatano(c acid formate salt
Synthesized according to typical procedures K and E from bicyclononene ALSO and glutaric anhydride. LC-MS: Rt = 0.90 ; ES+: 760.37
Example 418
(rac.)-5-{(lS*, 5^*)-7-{4-[2-(4-Bromophenoxy)ethoxyIphenyl}-6-{[2-(2-
chlorophenyl) ethyl] cyclopropylcarbamoyl}-3,9-diazabicyc;oP3.1 J non-6-csi-3-yl}-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL81 and glutaric anhydride. LC-MS; R, = 0.88 ; ES+: 750.31
Example 419
irac.)-5-{(2R*, 55*)-7-{4-f2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cycIo-
propyl[2-(4-fluorophenyl)ethyl] carbamoyl}-3,9-diazabicyclol33. lJnon-6-en-3-yl}-5-oio-pentaiioic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL83 and glutaric anhydride. LC-MS: Rt = 0.87 ; ES+: 734.34
Example 420
(rac.)-5-{(IR*, 5^*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclo-
propyl-[2-(2-methylphenyl)ethylIcarbamoyl}-3,9-diazabicyclo[3.3.I]n(jn-6-en-3-yl}-5-osopentano\c acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL84 and glutaric anhydride. LC-MS: R, = 0.88 ; ES+: 730.37
Example 421
irac.)-5'{{lR*, 5iS*)-7-{4-[2-(4-Broinophenoxy)ethoxy]phenyl}-6-[cycIopropyl-(3^-dimethoxybenzyI)carbamoyl)-3,9-diazabicyclo[3.3.11aon-6-en-3-yl}-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL85 and glutaric anhydride. LC-MS: R, = 0.86 ; ES+: 762.31
Example 422
(rac.)-S-{{lR*, 55'*)-7-{4-[2-(4-Bromophenoiy)ethoxy]pheDyI}-6-{cycIo-
propyI-[2-(4-methylphenyl)efhyl]carbamoy]}-3,9-diazabicyclo[3.3.1]aon-6-en-3-yI}-5-oxQpeataaQic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL86 and glutaric anhydride. LC-MS: Rt = 0.88 ; ES+: 730.37
Example 423
(fffc.)-5-{(iJ?* 55*)-7-{4-[2-(4-Bromophenoxy)ethoiy]phenyI}-6-(cycIopropyI-(2-fluorobenzyI)carbamoyI]-3,9-diazabicyclo[3J.l]uon-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL76 and 2,2-dimethylglutaric anhydride. LC-MS; Rt = 0.89 ; ES+: 748.35
Example 424

(rac)'5-((IR*, 55*>7-{4-(2-(4-Bromophenoxy)ethoxy]pheflyl}-6-S12-(2-
chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo [3.3.1] non-6-en-3-yl)-2,2-dimethy 1-5-0X0pentanoic acid formate salt
Synthesized according to t>'pical procedures K and E from bicyclononene AI.81 and 2,2-dimethyIglutaric anhydride, LC-MS: R^ = 0.91 ; ES+; 778.33
Example 425
{rac.yS--({lR*, 55'^-7-{4-I2-(4-Bromophenoa:y)ethoiy]phenyl)-6-{cyclopropyl-[2-(2,3-difluorophepyi)*'fhyI]carbamoyI}-3,9-diazabicycIop3.1]non-6-en-3-yl)-2,2-dimethy\-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL82 and 2,2-dimethylglutaric anhydride. LC-MS: R, = 0.91 ; ES+; 780.36
Example 426
(rac.)-5-({lS*, 55*)-7-{4-|2-(4-Bromophenoxy)etlioxy]plienyl}-6-{cyclopropyl-[2-(2-methylpheijyI)etbyllcarbamoyl}-3,9-diazabicyclot3J.llnon-6-en-3-yI)-2^-dimethyl-5-oxopen[taiioic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL84 and 2;2-dimethyiglutaric anhydride. LC-MS: Rt= 0.92 ; ES+: 7758.39
Example 427
(rac.)-5-{(i/i* 55*H~{4-[2-(4-Bromopbenoxy)ethoxy]phenyl}-6-[cycIopropyl-(3,5-diniethoxybenz>l)carbamoyll-3,9-diazabicyclo[3.3.11noa-6-ea-3-yl}-2,2-dimethyI-5-oxopentanoic acid formate salt
5S^

,r^^^-**««2S^ -^cvTvmmin
Synthesized according to typical procedures K and E from bicyclononene AL85 and 2,2-dimethylglutaric anhydride, LC-MS; Rt = 0.89 ; ES+: 790.39

5

Example 428
irac.)-5-iilR*, 55*)-7-j4-p-(4-Bromophenoxy)ethoxy]phenyI}-6-{cyclopropyl-(2-(4-raethylphenyl)ethyl]carbamoyI}-3,9-diazabicyelo[3.3.1]non-6-en-3^i)-2^-diinethyl-5-oxopcntanoic acid formate salt

10 Synthesized according to typical procedures K and E from bicyclononene AL86 and 2,2-dimethylglutaric aiiliydriJe. LC-MS: Rt-0.91 ;ES+; 758.38
Example 429
^ 15 (rac.)-(JR*, 5^*)-7-{4-(2- butyryI)-3,9-diazabicyclo [3.3.1 jo on-6-cne-6-carboxylic acid benzyl-
cyclopropylamide fonnate salt
Synthesized according to typical procedures G and E from bicyclononene AL74 20 and 4-carbamoylbutyric acid. LC-MS: Rt = 0.85 ; ES+: 735.34
Example 430
{rac)-(JR% 5.S'*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-
25 butyryl)-3,9-diazabicyclo[33.11aoa-6-eae-6-carboryUc acid (2-chlorobenzyI)-
^ ethylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AXHS and 4-carbamoylbutyric acid. LC-MS: R, = 0.85 ; ES+: 723.32 30
Example 431
S^S

{rac.)-{lR*, 5^*)-7-{4-[2-(4-Broraophenoxy)ethoxy]phenyi}-3-(4-carbamoyI-b«tyr>'i)-3,9-diazabicyclo[3.3.1}non-6-ene-6-carboxylic acid cyclopropyl-(2-fluorobenzyl)amide formate salt
Synthesized according to t>'pica] procedures G and E from bicyclononene AL76 and 4-carbamoylbutyric acid. LC-MS: R, = 0.84 ; ES+; 719.33
Example 432
(rac.}-(JR*, 5^*)-7-{4-p-{4-Bromophenoxy)efhoxy]phenyI}-3-(4-carbainoyl-butyryl)-3^-diazabicycI(,{33.IJnon-6-che-C-c«rbcx>:;c acid cycIopropyl-[2-(4-raethoiyphenoxy)ethyl]amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL79 and 4-carbamoyIbutyric acid. LC-MS: Rt = 0.84 ; ES+: 761.34
Example 433
(rac.)-{JIi*, 55'*)-7-{4-[2-(4-Bromophenoxy)ethoiylphenyI}-3-(4-carbamoyl-butyryl)-3,9-diazabicycIo[3^.1]non-6-eDe-6-carboxy|ic acid [2-(2-chloro-pheRyl)etliyl]cyclopropylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL81 and 4-carbamoylbutyric acid. LC-MS: R^= 0.86 ; ES+: 749.32
Example 434
{rac.y{lJ{*, 5^*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl>-3-(4-carbamoyl-butyryl)-3,9-diaiabicyclQ[3.3.1]noQ-6-ene-6-carboKyUc acid cyclopropyH3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononene AL85 and 4-carbamoylbutyric acid. LC-MS: Ri = 0.84 ; ES+: 761.35
Example 435
{rac.)-{lR*, 55*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyI}-3-(4-carbamoyl-butyryl)-3,9-diazabicycIo[3.3.11non-6-ene-6-carboxylic acid cyclopropyI-[2-(2-hydroxyethyl)benzyI]amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL87
and 4-carbamoylbutyric acid. LC-MS: Rt = 0.80 ;ES:. 745.40 ' ' -
Example 436
{rac.y{lR*, 55*)-7-{4-t2-(2-Chloro-4,5-dimethylphenoxy)ethoxylphenyl)-3-formyl-3,9-diazabicyclo[3.3.11non-6-ene-6-carboxylic acid (2-chlorobeazyl)-etbylamide formate salt
Synthesized according to typical procedure E from bicyclononene AK57. Obtained as side-product after purificytion by HPLC. LC-MS: R, =^ 0.91 ; ES+: 622.25
Example 437
{rac.)-{lR*, 55*)-7-{4-[2-(2-Chloro-4,5-dimethylphenory)ethoxy]phenyl}-3-formyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cycIopropyl-(2-o-tolylethyI)ainide formate salt
Synthesized according to typical procedure E from bicyclononene AK68. Obtained as side-product after purification by HPLC. LC-MS: R, = 0.92 ; ES+: 628.31

Example 438
(rac.y(lR*, 55*>7-{4-[2-{2-Chloro-4,5-dimethyiphenox>)ethoxy]phenyl}-3-formyI-3,9-diazabicyclop.3.1]non-6-cDe-6-carboxylic acid c> ciopropyl-(3,5-dimefhox5benzyI)amide formate salt
Synthesized according to typical procedure E from, bicyclononene AK70. Obtained as side-product after purification by HPLC. LC-MS: R, = 0.9O ; ES+: 660.30
Example 439
{racyilR*, 5^*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-pheny!}-3,9-diazabieyclo[33.1JDon-6-ene-6-carboxylic acid (2-chlorobeiizyI)-cyclopropylamide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL56 and acetyl chloride. LC-MS: R, = 0.93 ; ES+: 648.37
Example 440
iracH^R*, 5^*)-3-Acetyl-7-{4-[2-(2-Chloro-4,5-dimetliylphenoxy)ethoxyl-phenyl}-3,9-diazabicyclo[33.1]non-6-ene-6-carboxylic acid (2-chlorobeiizyI)-ethylamide formate salt
Synthesized according to typical procedures A and E &om bicyclononene A1.57 and acetyl chloride. LC-MS: R, = 0.92 ; ES+: 636.37
Example 441

(rac.)-ilJi*, 5^*)-3-Acetyl-7-{4-[2-(2-chIoro-4,5-dimethylphenoxy)etlioxyI-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid cyclop ropy I-(2-fluorobenzyI)amide formate salt
Synfliesized according to typical procedures A and E from bicyclononene AL58 and acetyl cliloride. LC-MS: Rt = 0,90 ; ES+: 632.41
Example 442
irac.)-{lli*, 55*)-3-Acetyl-7-{4-(2-(2-chIoro-4,5-dimethylphenoxy)efhoxy]-pheayij-J,y-dia/.a"uicyclo[3.3.1]flon-6-ene-6-carboxylic acid cyclQpropyl-(2-metbylbenzyl)amide formate salt
Syntiiesized according to typical procedures A and E from bicyclononene AL60 and acetyl chloride. LC-MS: Rt = 0.91 ; ES+: 628.43
Example 443
irac.y{lR*, 5S*)-3-Acetyi;-7-{4-12-(2-ch!oro-4,5-diniethylphenoxy)ethoxyl-phenyI}-3,9-diazabicyclo[3.3.1]noo-6-ene-6-carboxylic acid cyclopropyl-(3,5-dimethoxybenzyI)amide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL70 and acetyl chloride. LC-MS: R, = 0.91; ES+: 674.44
Example 444
irac.y(JR*, 55*)-3-Acetyl-7-(4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy)-phenyI}-3,9-diazabicyclo[3.3.1]non-6-enc-6-carboxylic acid cycIopropyl-(2-/)-tolylethyl)amide formate salt

Synthesized according to typical procedures A and E from bicyclononene AL71 and acet>-l chloride. LC-MS: R, = 0.92 ; ES+: 642.44
Example 445
(rac.)'5-{illi*, 55*)-6-[(2-ChIoroben2yl)cyclopropyIcarbamoyl]-7-{4-[2-{2-chloro-4p-dimethyiphenoxy)ethoxy]piienyl}-3,9-diazabicyclo[3.3.11non-6-en-3-y!)-5-osopentaiioic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL56 i«id felalcjic anhydridU LC-MS: R, = 0.90 ; ES+: 720.36
Example 446
(rac)'5-{(IR*, 55*)-6-l(2-Chlorobenzyl)ethylcarbamoyll-7-{4-[2-{2-chloro-4,5-diniethyIphenoxy)ethosy]phenyI}-3,9~diazabicycIo[3.3.1]Qon-6-en-3-yl)-5-oxo-pentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL57 and glutaric anhydride. LC-MS: R[ = 0.89 ; ES+: 708.35
Example 447
{rac.)-5-{(JR*, 5,y*)-7-{4-I2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]pheDyI}-6-[cyclopropyI-(2-nuorobenzyl)carbamoyIJ-3,9-diazabicycIo[33.1]noo-6-eii-3-yl}-5-oxopeiitanoic add formate salt
Synthesized according to typical procedures K and E from bicyclononene AL58 and glutaric anhydride. LC-MS: Ri = 0.88 ; ES+: 704.37
Example 448

{rac.y5-{(JR% 5^*)-7-{4-[2-(2-ChIoro-4,5-dimethylphenoxy)ethoxy]phenyI}-6-[cyciopropyI-{3-trifluoromethyIbeuzyl)carbainoyl]-3,9-diazabicycIo[3.3.1]-non-6-en-3-yl}-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL59 and glutaric anhydride. LC-MS: R^ = 0.91 ; ES+: 745.38
Example 449
{racy5-{(JR*, 55*)-7-{4-[2-(2-ChIoro-4,5-dimefhyIphenosy)ethoxyIphenyI}-6-[cyclopropyI-(2-mfctiiylbei«-j;)c&,lJamoyJI'3,9-diazabicycIo[33.1Inon-6-en-3-yl}-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclonoaene AL60 and glutaric anhydride. LC-MS: Rt = 0.89 ; ES+; 700.41
Example 450
(rac.).5-{(ii?* 55*)-7-{4-p-(2-Chloro-4,5-dimetbylphenoxy)ethoxylphenyl}-6-|cycIopropyH2-(4-metboxypheBioxy)ethyl]carbamoyl)-3,9-diazabicyclo-*[3.3.1Jiion-6-en-3-yi)-5-oxopcntanoic acid fonnate salt
Synthesized according to typical procedures K and E ftom bicyclononene AL61 and glutaric anhydride. LC-MS: R4 = 0.88 ; ES+; 746.42
Example 451
(mc>5-((iif* 55*)-7-{4-12-(2-Chloro-4,5-diinethylpbenoxy)ethoxy]pbenyl}-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyI]carbamoyl}-3,9-diazabicyclo-
[3,3.1]aott-6-en-3-yl)-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K and E from bicyciononene AL62 and glutaric anhydride. LC-MS: Rt = 0.88 ; ES+: 746.41
Example 452
(/■(ic.)-5-((ifl* 5■S*)-7-{4-[2-(2-Chloro-4,5-dimcthylphe^oxy)ethoxy]pheIlyI}-6-{cyc!opropyl-[2-(3-methyIphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.11-non-6-en-3-yl)-5-oKopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL63 and glutaric anhydride. LC-WS: R,—0.91 ;ES+: 730.44
Example 453
(r(ic.)-5-[(7Jf* 5^*)-7-{4-[2-(2-Cbloro-4,5-dimethylphenoxy)ethoxy]pheDyI}-6-(cyclopropyIphenethyIcarbamoyi)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxo-pentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL64 and glutaric anhydride. LC-MS: R, = 0.88 ; ES+: 700.41
Example 454
(rflc:)-5-((i5*. ■J5*)-7-{4-[2-(2-ChIoro-4,5-dilnethylpheaoxy)ethoxy]pheDyl}-6-{[2-(2-chlo^ophenyI)ethylJcyc^opropyl-ca^bamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yI)-5-oxopettfanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL65 and glutaric anhydride. LC-MS: R, = 0.90 ; ES+: 734,39
Example 455

(rflc.)-5-((ii?* 55*)-7-{4-[2-(2-Chlo^o-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyelopropyl-I2-(2,3-difluo^ophenyl)ethyl]carbamoyl}-3,9-diazabicycloI3.3.1]-Don-6-en-3-yI)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL66 and gintaric anhydride. LC-MS: R, = 0.90 ; ES+; 736.41
Example 456
{rac.)-5-((i-R*, 55*)-7-{4-12-(2-Chloro-4,5-dimethylphenoxy)ethoxylphenyl}-6-{cyclopropyi-(2-(4-fluoropbenyl)ethyllcarbfiaicyll-3,9-dUzabicydQt33.il-non-6-en-3-yl)-5~oxopentaiioic acid formate salt
Synthesized according to typical piocedures K and E from bicyclononene AL67 and glutaric anhydride. LC-MSi Rt = 0.89 ; ES+-. 718.40
Example 457
(rflc)-5-((ifi*, 55*)-7-{4-{2-(2-Chloro-4,5-dimethy[pheaory)etfaoxylphenyl}-6-{cy clopropyl- (2-(2-niethylpheny l)ethy IJcarbamoy li-3,9-dia2abicyclo [33.11-aon-6-en-3-yl)-5-oxopetttanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL68 and glutaric anhydride. LC-MS: Rt= 0.90; ES+: 714.43
Example 458
{rac.)~5-{{lR*, 55 *)-7-{4-[2-(2-ChIoro-4,5-dimethylphenosy)ethoiy] phenyl}-6-[cyclopropyI-{3,5-dimethoxyben2yI)carbamoyI]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentaooic acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL70 and glutaric anhydride. LC-MS: R^ - 0.89 ; ES+: 746.41
Example 459
(rflc)-5-((i^* 55*)-7-{4-[2-(2-Chloro-4,5-diinethylphenoxy)ethoxy]phenyI}-6-{cyciopropyI-{2-(4-methylphenyl)ethylIcarbamoyI}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yI)-5-oiopentanoic acid formate salt
Syn^esized according to typical procedures K and E from bicyclononene AL7i and glutaric anhydride. LC-MS:Rt = 0.90 ;ES+-?H.41 -
Example 460
(racyS'iilR*, 5.y*)-6-[(2-ChIorobenzyl)cyclopropylcarbamoyl]-7-(4-[2-(2-cliloro-4^dimethylphenoxy)ethoxylphenyl}-3,9-diazabicyclo[3.3.1|non-6-en-3-yi)-5-oxopeataaoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL56 and glutaric acid monomethylester chloride. LC'MS: Ri = 0.95 ; ES+: 734.37
Example 461
{racyS-iilR*, 55*)-6-[(2-Chlorobenzyl)etfaylcarbamoyll-7-{4-[2-(2-chIoro-4,5-diK»ethyIpheiioxy)ethoxylpheiiyl}-3,9-diazabicyclo[3.3.1Inon-6-eii-3-yl>5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL57 and glutaric acid monomethylester chloride. LC-MS: Rt = 0.94 ; ES+: 722.37
Example 462

irac.)-5-{{lR*, 55*)-7-{4-[2-(2-ChIoro-4,5-dimethylphenoxy)ethoxyI phenyl}-6-[cydopropyI-(2-nuorobenzyI)carbamoyI]-3,9-diazabicycIoI3.3.1]Don-6-en-3-yl}-5-oxopentaDoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL58 and glutaric acid monomethylester chloride. LC-MS: Rt = 0.93 ; ES+: 718.40
Example 463
irac.)'5-{(JR*, 55'*)-7-(4-[2-{2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-5^[cycii.pr&pj)-(3-trifluoromethylbenzyl)carbamoyll-3,9-diazabicyclo(3u2.T:j'-iioii-6-en-3-yl}-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL59 and glutaric acid monomethylester chloride. LC-MS: R^ = 0.96 ; ES+: 768.38
Example 464
(raayS-iilR*, 55*)-7-{4-[2-(2-Chloro-4,5-dimethylpheDoiy)etfaoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl) carbamoyl]-3,9-diazabicyclo [33.1 lnon-6-en-3-yl}-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicycloaoaerie AIJ60 and glutaric acid monometbylester chloride. LC-MS: Rt = 0.94 ; ES+: 714.43
Example 465
(/■flc.)-5-[Ci/;* 55*H-{4-l2-(2-Chloro-4,5-dimethylphenoxy)ethoxylphenyi}-6-(cyclopropylphenethyIcarbamoyI)-3,9-diazabicyclo[3.3.1jnon-6-en-3-yIJ-5-oxopentanoic acid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononene AL64 and giutaric acid monomethylester chloride. LC-MS: R, = 0.93 ; ES+; 714.41
Example 466
(TO£:.)-5-((ifl* JS*)-7-{4-I2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]plienyl}-6-{[2-{2-chloropheayl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo(3.3.1]noD-6-en-3-yl)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL65 aliu g'iuta.;^ acid monomethylester chloride. LC-MS: Ri = 0.93 ; ES+: 748.39 : ■ '
Example 467
(rac)-5-((i/f*, 55*)-7-{4-(2-(2-ChIoro-43-dimethylpheiioxy)ethoxy|phenyl}-6-{(2-(2,3-difl"orophenyl)etfay!lcyclopropylcarbamoyl}-3,9-diazabicycloI3.3.11-non-6-en-3-yl)-5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL66 and giutaric acid monomethylester chloride. LC-MS: Rt = 0.94 ; ES+: 750.40
Example 468
(r(ic.)-5-((^fi* 55*)-7-{4-[2-(2-ChIoro-4,5-dimethylphenoxy)ethoxyIphenyl}-6-{[2-(4-fluorophenyI)etIiyI]cyclopropyIcarbamoyl}-3,9-diazabicydo [3.3.1] non-6-eD-3-yI)-S-oxopeDfanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL67 and giutaric acid monomethylester chloride. LC-MS: Rt = 0.93 ; ES+: 732.44
Example 469

(rac,)-5-((/fl* 55*)-7-{4-[2-(2-ChIoro-4,5-diraethylpheaQxy)ethQxyIpheuyO-6-(l2-(2-methylphenyI)ethyl]cyclopropylearbamoyl)-3,9-diazabicycloI3.3.1Jnon-6-en-3-yl)~5-oxopentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E trom bicyclononene AL68 and glutaric acid monomethylester chloride. LC-MS: Ri = 0.95 ; ES+: 728.45
Example 470
(rac)-5-{(iJf* 5^*)-7-{4-[2-(2-Chloro-4,5-dimethyIphenoxy)ethoxy]phenyI}-6-[cycIoproE>y'-(3-5-dimethnxyb'*'Ty')c''bamoyIJ-3,9-diazabicycIof3.3.1]non-6-en-3-yli-5-oxopeBtanoic acid methyl ester formate salt
Synthesized according lo typical procedures A and E from bicyclononene AL70 and glutaric acid monomethylester ciiloride. LC-MS: Rt = 0.93 ; ES+; 760.40
Example 471
(rac)-5- Synthesized according to typical procedures A and E from bicyclononene AL71 and glutaric acid monomethylester chloride. LC-MS: R, = 0.95 ; ES+; 728.43
Example 472
(rac.)-5-((i/!* 5>S*)-6-[(2-Chlorobeozyl)cyc!opropyIcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimefhylphenoxy)ethoxy] phenyl}-3,9-diazabicyclo [3.3.1] non-6-en-3-yI)-2^-dimethyl-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K and E ftom bicyclononene AL56 and 2,2-dimethylglutaric anhydride, LC-MS: Rt= 0,93 ; ES+: 74S.40
Example 473
(_rac.)-5-((JR*, 5^*)-6-((2-ChlorobeiizyI)ethylcarbamoyll-7'{4-[2-(2'CMoi-o-4,5-dimetfayIphenoxy)ethoxylphenyl}-3,9-diazabicycio [3.3.1] no n-6-en-3-yI)-2,2-dimefhyI-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL57 and 2,2- Example 474
(rac.)-5'{{lR*, 55*)-7-{4-[2-(2-Chloro-4,5-dimethyIphenoxy)ethoxylphenyl}-6-[cyclopropyl-(2-fluorobenzyI)carbamoylJ-3,9-diazabicyclo[33.1]non-6-en-3-
yl}-2,2-dimetby]-5-oxopentatioic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL58 and 2^-dimethylg!utaric anhydride. LC-MS: R, = 0.91 ; ES+: 732.45
Example 475
(racyS-iiJR*, 55*)-7-{4-[2-(2-Chloro-4^-dimethylplienoiy)ethoxy]phenyI>-6-[cyclop ropy I-(2-methylbeiizyl)carfaamoyI]-3,9-diazabicy do [33.1 Inon-6-en-3-yl}-2,2-dimethyl-5-oxopentanolc acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL60 and 2,2-diniediyIglutaric anhydride. LC-MS: R, = 0.93 ; ES+: 728.48
Example 476

(rac.)-5-I(yi?* 5^*)-7-{4-[2-(2-ChIoro-4,5-dimethyIpheaoxy)ethoxjiphenyI}-6-(cyclopropylphcnethy)carbamoyI)-3,9-diazabicydo[3.3.1]non-6~en-3-yII-2,2-dimethyl-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E ftom bicyclononene AL64 and 2,2-dimethyigIutaric anhydride. LC-MS: R, = 0.92 ; ES+: 728.49
Example 477
(rac.)-5-((iif*, 55*)-7-{4-[2-(2-Chlor-4,5-diniethylphenoxj')ethoiy]phenyl)-6-{{2-(2-chlQrophenyl)ethylI<::yclopropyicarbamoy d:azafc:cytio acid formate salt> Synthesized according to typical procedures K and E fi-om bicyclononene AL65 and 2,2-dimethylglutaric anhydride. LC-MS: R( = 0.93 ; ES-i-: 762.42
Example 478
(wc.)-5-((i-R*, 5S*)-7-{4-I2-(2-ChIoro-43-dimethylpbenoxy)etho3y)phenyl)-6-{I2-{23-difIuoropheByl)ethyl]cyclDpropyicarbamoyl}-3,9-dia2abicycloI3.3.1]-non-6-en-3-yl)-2^-dimethyI-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL66 and 2^-dimetfayIglutaric anhydride. LC-MS: R^ = 0.93 ; ES+: 764.44
Example 479
(mc)-5-((/i2* 5S*)-7-{4-t2-(2-Chloro-4,5-dimethylphenoxy)eth(»sylphenyl}-6-((2-(4-fluoropfaenyI)ethyIlcy clop ropy IcflrbamoyI}-3,9-diazabicyclo [3.3.1 ]non-6-en-3-yI)-2,2-dimethyI-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL67 and 2,2'dimelhylglutaric anhydride. LC-MS: R, = 0.92 ; ES+: 746.48
Example 480
(/■acVS-CC-^-ff*, 55*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxyIplienyl}-6-([2-(2-methylphenyl)etliyl]cyclopropylcarbamoyl}-3,9-diazab!cyclo [3,3.1 Inon-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL68 and2,2-diniethylglutaric anhydride. LC-MS: R,-0.93 ; ES+; 742.51 --■ -
Example 481
(rac.)-5~{(lR*, 5>S*)-7-{4-[2-(2-Chloro-4,5-dimethylphcnoiy)efhoxyJpIienyl}-6-[cycIopropyH3,5-dimethoxybcnzyl)carbamoyll-3,9-diazabicy do (3.3.1 JDOD-6-eo-3-yl}-2,2-dimethyl-5-osopentaijoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL70 and2^-dimethyIglutaric anhydride. LC-MS: Rt= 0.92 ; ES+; 774.45
Example 482
(rafc>5-((JJ?*, 5S*)-7-{4-[2-(2-Chloro-43-dimethylphenoxy)etbosylphenyl}-6-{[2-(4-methyIphenyl)ethyiIcycIopropylcarbamoyO-3,9-diazabicyclo [3.3.1] non-6-en-3-yI)-2,2-dimethyl-5-K)xopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene Ai:71
and 2,2-dimethylglutaric anhydride. LC-MS: R, = 0.93 ; ES+: 742.51
Example 483

(rac.)-(lR*, 5'y*)-3-(4-Carbainoylbutyryi)-7-{4-[2-(2-chIoro-4,5-dimethyI-
phenoxy)ethoxyIphenyI}-3,9-diazabicycIo[3.3.11non-6-ene-6-carboxylic acid (2-chIorobenzyl)cyclopropylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL56 and 4-carbamoyIbutyric acid. LC-MS: Rt = 0.88 ; ES+: 719,43
Example 4S4
(rac.)-(lR% 5iS'*)-3-(4-CarbamoyIbutyryI)-7-{4-[2-(2-chloro-4,5-dimethyl-
pheui)xy)ethoxy]phenyl}-3,9~diazabicycIo[3,3.1]non-6-ene-6-carboxylic" acid (2-chIorobenzyI)ethyiaiiiide formate salt
Synthesized according to typical procedures G and E from bicyclononene ALS7 and 4-carbamoyIbutyric acid. LC-MS: R, - 0.S7 ; ES+: 707.39
Example 485
(racy(IR*r 55*)-3-(4-CarbamoyIbutyryI)-7-{4-(2-(2-chIoro-4,5-dimethyl-pbeno3cy)ethoxylpheDyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyI-(2-fluorobeiizyl)amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL58 and4-carbamoyIbutyric acid. LC-MS: Rt = 0.86 ;ES+: 703.43
Example 486
{rac.)-(lR*, 55*>3-(4-Carbamoylbutyryl)-7-{4-|2-(2-cWoro-4,5-dimethyl-
pheno3£y)ethoxy]phenyl}-3,9-diazabicyclol3.3.1]noa-6-eae-6-carboxylic acid
cycle pro py l-(3-trifIuoro me thy lbenzyl)amide formate salt

Synthesized according to tj'pical procedures G and E from bic>-clononene AL59 and 4-carbaraoy!butyric acid. LC-MS: R, = 0.89 ; ES+; 753.44
Example 487
irac.y{JR*, 55*)-3'(4-CarbamoyIbutj'ryI>7-H-i2-(2-chloro-4,5-diniethyI-
pbenox>)ethoxy]pheny]}-3,9-diazabicycloI3.3.11non-6-ene-6-carboxylic acid cyclopropyl-{2-niethylbenzyl)amide formate salt
Synihesized according to typical procedures G and E from bicyclononene AL60
and 4-carbamoylbutyiic acid. LC-MS: R, = 0.87 ; ES+: 699.47 . ,.,-. ^.». -
Example 48S
(rac.)-{iR*, 55*)-3-(4-CarbamoyJbutyryl)-7-{4-I2-(2-chloro-4,5-diniethyl-
phenoxy)ethoxy}phenyl}-3,9-diazabicycIa[33.11non-6-eDe-6-carboxylic acid cycIopropyl-j2-(4-metboxyphenoxy)ethyl] amide formate salt
Synthesized according to typical procedures G and E &om bicyclononene AL61 and 4-carbamoylbutyric acid. LC-MS: Rt= 0.86 ; ES+: 745.46
Example 4S9
(racHIK*, 55*)-3-(4-CarbanioyIbutyi7l)-7-t4-l2-(2-cfaIoro-4,5-dimethyI-
pheooxy)etboxy]phenyl}-3,9-diazabicycIo[33.11non-€-eoe-6-carb Synthesized according to typical procedures G and E from bicycLononene AL64 and 4-carbamoyIbutyric acid, LC-MS: R, = 0.86 ; ES+: 699.44
Example 490

(racHJJi*, 55'*)-3-{4-CarbamoylbutyryI)-7-{4-f2-(2-cfaloro-4,5-dimethyI-
phenoxy)ethoxy]phenyl}-3,9-diazabicycIo[3.3.11non-6-ene-6-carboxylic acid [2-(2-chlorophenyl)ethy[|cyclopropylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL65 and 4-carbamoylbutyric acid- LC-MS: Rt = 0.88 ; ES+: 733.42
Example 491
(racH^R*, 55*}-3-(4-CarbamoylbutyryI)-7-{4-[2-(2-chIoro-4,5-dimethyI-
phenoiyi^thox^jpiienylj 3,9-dhiabicydo[33.1]non-6-ene-6-carboxyIit acid cyclopropyI-[2-{2,3-difluoropbenyl)ethyl] amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL66 and 4-caibamoyibutyric acid. LC-MS: Rt = 0.88 ; ES+: 735.43
Example 492
{racyilR *, 55*)-3-(4-Carbamoy lbutyryl)-7-{4-I2-(2"ChIoro-4,S-dimethy 1-
pheooiy)ethoxy]plienyl}-3,9-diazabicyclo[33.1]non-6-ene-6-carboiylic acid cyclop ropyl-[2-(4-fluorophenyI)ethylJ amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AXJ67 and 4-carbamoylbutyric acid. LC-MS: Ri = 0.87 ; ES+: 717.43
Example 493
(mc.>(Ji{* 55*)-3-(4-Carbamoylbutyryl)-7-S4-[2-(2-chloro-4,5-dimethyl-
phenoxy)ethoxyJphenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclop ropyl-(2-o-tolyletbyl)amide formate salt

Synthesized according to typical procedures G and E from bic\-clononene AL68 and 4-carbamoylbutyric acid. LC-MS: R^ = 0.88 ; ES+: 713.46
Example 494
(racHJR*, J5*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chIoro-4,5-dimethyl-
phenox>)ethoxylphenyi}-3,9-dia2abicyclo{3.3.1]noa'6-ene-6-carboxyIic acid cyclopropyl-(3,5-dimethosybenzyl)amide formate salt
Synthesized according to typical procedures G and E &om bicyclononene ALTO and 4-caitainoylbatyni acid.^ie.-MS;".^ = 0.S7 ; ES+; 745.45
Example 495
(rac-HlR*, 55*)-3-(4-CarbamoyIbutyryl)-7-{4-[2-(2-chloro-4,5-dimetbyl-
plienoxy)ethoxyJplienyl)-3,9-diazabicyclol3.3.1lQon-6-ene-6-carboxylic acid cyclopropyl-{2-;7-tolylethyI)amidc formate salt
Synthesized according to typical procedures G and E from bicyclononene AL71 and 4-carbamoylbutyric acid. LC-MS: R^ = 0.88 ;ES+: 713.46
Example 496
l:l-Mixfnre of (rac)-{3S*)'5-{(lR*, 55*)-6-l(2-chlorobenzyl)cyclopropyI-carbamoyl]-7-{4-l2-(2-chloro-43-diinethylpheiioxy)ethoxylphenyl)-3,9-dia2a-bicyclo(33.1]non~6-en-3-yI)-3-hydroxy-5-oxopeiitanoic acid formate salt and
(rac.)-(3S*)-5-(ilR*, 5>S'*)-6-[(2-chIorobenz>-I)cyclopropyI-carbamoyll-7-{4-t2-(2-chloro-4,5-dimethylphenoiy)ethoxy]pheByl}-3,9-diazabicycIo [3.3.1] non-6-eii-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K, E and L from bicyclononene AL56 and 3-(rert-butyldimethyisilyloxy)glutaric anhydride. LC-MS: Ri = 0.88 ; ES+: 736.43
Example 497
l:l-Mixture of (rac.)-(i/?*)-5-((iif* 5^*)-6-K2-clilorobeiizyl)ethyl-
carbamoyl]-7-{4-[2-(2-cliloro-4,5-dimethylphenoxy)ethoxyiphenyI}-3,9-diaza-
bicyclo[3.3.1]-non-6-eii-3-yl)-3-hydroKy-S-oxopentanQic acid formate salt and
(rac.)-(3S*)-5-((l}i*, 55'*)-6-[(2-cblorobenzyl)ethylcarfaamoyl]-7-{4-[2-(2-
chloro-4,5-dimefhylphenoxy)ethoxy]pnenyI}-3,9-diazabicyciot3,3.1]-non-6-en-3-yl)-3-hydroxy-5-oxopeiitanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL57 and 3-(fer/-butyIdimethyIsilyloxy)glutaric anhydride. LC-MS: Ri = 0.87 ; ES+: 724.40
Example 498
l:l-Mixture of (racy(3R*)-5-{(lR*, 55*)-7-{4-[2-(2-chIoro-4,5-dimethyI-phenoxy)ethoxylphenyl)-6-lcyc\opropyV-(2-flttorobenzyl)carbamoyll-3,9-diazabicyclo[33.1]non-6-en-3-yI}-3-hydroxy-5-oxopeiitanoic acid formate salt and (rac.)-(3S*y5-{(lR*, 5.S'*)-7-{4-[2-(2-chloro-4,5-dmiethyiphenoxy)-ethoxy]pheDyl)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo-[3.3.1Jnon-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL58 and 3-(ferNbutyldiniethylsilyloxy)glutaric anhydride. LC-MS; Rt = 0.86 ;
ES+: 720.43
Example 499

l-.l-Mixture of (rac.)-(5fl*)-5-{(ii?% 55*)-7-{4-[2-(2~chIoro-4,5-diroethyl-phenoxy)ethoxy}phenyl}-6-lcyclopropyl-(3-trifluoromethylben2yl)-carbamo¥l]-3,9-dJazabicyclo[3.3.1)non-6-eo-3-yi}-3-hydrox)'-5-oxopentanoic acid formate salt and (mc.)-(3S*)-5-{(Ji;*, 5S*)-7-{4-I2-(2-chloro-4,5-dim ethylphenoxy)ethoxy] phenyl}-6-(cj'clopropy l-{3-trifluorm ethylobenzyl)-carbamoyll-3,9-diazabicycl-o[3.3.1)non-6-en-3-yl}-3-hydroxy-5-oxopentaaoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene
AL59 and 3-(ferf-butyldimethylsilyloxy)giutaric anhydride. LC-MS: Rt = 0.89 ;
ES+: 770.40 "-" ^ " ' -' ' .
Example 500
l:l-Mixture of {rac-)-{3R*)-5-({lR*, 55*)-7-{4-{2- Synthesized according to typical procedures K, E and L from bicyclononene AL61 and 3-(rert-butyldiniethylsilyloxy)glutaric anhydride. LC-MS: Rt = 0.86 ; ES+: 762.46
Example 501
l:l-Mixture of (rac.H3R*)-5-[(lJt*, 55*)-7-{4-[2-(2-chloro-4,5-dimetiiyI-phenoxy)ethoxy]pheQyl}-6-(cyclopropyiphenethylcarbamoyl)-3,9-diaza-bicyclo[3.3.1Inon-6-en-3-yI]-3-hydroxy-5-oxopentanoic acid formate salt and {rac.H3S*y5-[(lR*, 5^*)-7-{4-[2-(2-chloro-4,5-diraethylphenoxy)ethoxyJ'

phenyl}-6-(cyclopropylphenethykarbflmoyl)-3,9-diazabicycIo[3.3.1]noo-6-en-3-yl]-3-hydrosy-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL64 and 3-(/err-butyldimethylsilylox>0glutaric anhydride. LC-MS: Ri = 0.86 ; ES+: 716.46
Example 502
l:l-Mlxture of irac.)-(3R*y5-{{lR% J5-^-7-{4-I2-{2-chloro-4,5-dimethyl-pijciioxy)ethoiy] pheDyl}-6- {[2-(2-chlo rophenyl)ethyl] cyclopropylca rbamoyi)-3,9-dia2abicyclo [3.3.1] non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and {rac)-{3R*yS-{{lR*, 5S*)-7-{4-[2-{2-chloro-4,5-dimethylphenoiy)-ethoiy]phenyIJ-6- {t2-(2-ch.loropheny l)ethyll cy clopropylcarb amoy lJ-3,9-diazabicycJol3.3.11non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K, E and L &om bicyclononene AJj65 and 3-(rerf-butyldimethylsilyloxy)g[utaric anhydride. LC-MS: Ri = 0.88 ; ES+-. 750.41
Example 503
I:l-Mixture of (rac)-(iK*)-5-((Zfi% JS*>7-{4-[2-(2-Chloro-4,5-dimethyI-pheiioxy)etlio^lphettyl}-6-{cyclopropyl-[2-(2^-di£Iuoropheiiyl)ethyll-carbamoy l}-3,9-diazabicy do [3.3.1 lnon-6-en-3-yI)-3-hydroxy-5-oiopentanoic acid formate salt and (rac.)-{3S*y5-(ilR*, 56'*)-7-(4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxylpheayI}-6-{cyclo propyl-[2-(2,3-difluoro phenyl)-ethyllcarbamoyl} -3,9-diazabicyclo [3.3.1 lnon-6-en-3-y l)-3-hy droiy-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K, E and L from bicyclononene AL66 and 3-(/err-butyIdimethylsilyloxy)glutaric anhydride. LC-MS; Ri = 0.88 ; ES+: 752.45
Example 504
l:l-ML\Tiire of {raa)-(3R*)~5-((lR% 5i'*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenos:} ")ethoxy]phenyI}-6-{cyclop ropy I-[2-(4-fluorophenyl)e thy IJ-carbamoyl}-3,9-d»azabicyclo[3.3.i]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid formate salt and (rac.)-(3S*)-5-((IR% 5i'*>7-{4-[2-(2-chIoro-4,5-diiiiethyIphenoxy)ethoxylphenyI}-5-{cycIopropyl-[2-(4-fluoropheny!)riI:>Il- ' carbamoyl}-3,9-dia2abicycloI33.11non-6-en-3-yl)-3-hydro5y-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL67 and 3-(/er/-butyldimethylsilyloxy)glutaric anhydride. LC-MS; Rt = 0.87 ;
ES+: 734.47
Example 505
l:l-Mixture of irac)-(3R*)-S-{(lR*, J5*)-6-{(2-chlorobenzyl)cyclopropyI-carbarooyI}-7-{4-[3-{2^,6-trifluorophenoxy)propyllphenyl}-3^-diazabicyclo-(33,l]non-6-en-9-yl)-3-hydroxy-5-oio-pentanoic acid formate salt and (rac.)-(J5*)-5-({iJ?*, 55*)-6-[(2-chIorobenzyl)cycIopropylcarbamoyII-7-{4-[3-(2^,6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo-P3.11non-6-en-9-yI)-3-liydroxy-5-oxo-pentanoic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene BC
and 3-{rer^butyldimethylsilyloxy)gIutaric anhydride. LC-MS: Rt = 0.88 ; ES+: 726.32
Example 506

(rac.)-5~((ll{*, 55*)-6-((2-Chlorobenz)-I)cyclopropyIcarbamoylJ-7-(4-[3-(23,6-trifluorophenoxy)propyi]pbenyI|-3,9-diazabicyclo[3.3.I]non-6-en-9-yi)-2,2-dimethyl-S-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene BC and 2,2-dimethyIglutaric anhydride. LC-MS: Rt = 0.95 ; ES+: 738.37
Example 507
(raa)A'{i}F.*, 5S*) £ [(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(23,6-trifluorophenoxy)propyllphet3iy!il-3,9-diazabicyclol33.11non-6-en-9-yl)-4-oxo-butyric acid
Synthesized according to typical procedxires K and E &oin bicyclononene BC and succinic anhydride. LC-MS: Rt = 0.90 ; ES+: 696.32
Example 5t>8
{rac.)'(lR*, 55'*)-7-{4-I3-(2»3,6-Trifluorophenoxy)propyI]phenyi}-3,9-diaza-bicycIol33.1]non-6-ene-6,9-dicarboiyUc acid 6-l(2-chloroben2yl)cyclapropyi-amid^ S-diraetbylamide formate salt
Synthesized according to typical procedures A and E from bicyclononene BC and dimethylcaibamoyl chloride. LC-MS: Rt = 0.94 ; ES+: 667.38
Example 509
{rac.)-{lR*, 55" *)-6-[(2-Chlorobeitzyl)cyc!opropy [carbamoyl]-7-(4-[3-(2,3,6-trifluorophenoxy)propyIlpbenyI}-3,9-diazabicyclo[3.3.1]aon-6-ene-9-carboxylic acid methyl ester formate salt

Synthesized according to typical procedures A and E irom bicyclononene BC and methyl chlorofommte. LC-MS-. Rt= 0.96 ; ES+-. 654.34
Example 510
{rac)-{lR*, 55*)-6-[(2-Chlorobeii2yI)cycIopropylcarbaoioyIl-7"{4-[3-(2,3,6-trinuoropheaoxy)propyIlphenyI}-3,9-diazabicycIo[3.3.1]non-6-ene-9-carboxylic acid ethyl ester formate salt
Synthesized according to typical procedures A and E fiom bicyclononene BC and eth>-l cblcr^formate. LC-MS: R. - 0.98 ; ES+: 668.37
Example 511
{racy3-[{2R% 5>S'*)-(6-I(2-Chlorobenzyl)cyclopropylcarbaiiioyl]-7-{4-l3-
(23»6-trilluorophenoxy)propyl]pheiiyl}-3,9-diazabicj'clo[3,3.1]non-6-ene-9-carbonyl)araino]propioDJc acid ethyl ester formate salt
Synthesized according to typical procedures A and E firom bicyclononene BC and ethyl 4-isDcyanatopropionate. LC-MS: R, = 0.95 ; ES+: 739.36
Example 512
l:l-Mixture of (raaH3R*)-S-{(IS*, 55*)-7-{4-p-(2-chIoro-4^dimethyl-
phenory)ethoxy]phenyIJ-6-[cycIopropyl(2-tf-tolyIethyI)carbamoyl]-3,9-diaza-
bicyclo{33.11nQa-6-en-3-yl}-3-hydroxy-5-oxopentanoic acid and (rac.)-(3S*)-
5-{(iR*, 55*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxylphenyl}-6-
[cyclopropyl(2-o-tolylethyl)carbamoyI]-3,9-diazabicycIo[3.3.1]non-6-eii-3-yl}-3-hydroxy-5-oxopentanoic acid
Synthesized according to typical procedures K, E and L from bicyclononene AL68 and 3-(re7-f-butyidimethy]silyloxy)gIutaric anhydride. LC-MS: R, = 0.88 ; ES+: 730.49
Example 513
l:l-Mixture of {rac)'{3R*)-5-{{lR*, 55*)-7-{4-[2-(2-chIoro-4,5-diinethyK phenoxy)eth oxyjphenyi}-6-( cyclop ropyl-{3,5-dim ethoxy ben2yl)ca rbamoyi]-3,9-diazabicycIo[3.3.1]non-6-en-3-yl}-3-bydroxy-5-oxopent3noic acid formate salt and (rac)-(i5*)-5-{{iiI* 55*)-7-{4-l2-(2-chloro-4,5-dimetbylphcnoxy)-ethoxy]phenyl}-6-[cycIopropyI(3,5 dinictI;oiybciizyl}caibamoyI]-3,9-diaza-bicyelQi33.ilnon-6-en-3-yl}-3-hydroxy-5-osopentaiioic acid formate salt
Synthesized according to typical procedures K, E and L from bicyclononene AL70 and 3-(/e?-/-biJtyldiniethylsilyloxy)glutaric anhydride. LC-MS: R, = 0.87;
ES+: 762.47
Example 514
l:l-Mixture of (rac.H^fl*)-5-{(lfl* 5S*)-7-{4-12K2-ehloro-4,5-dimethyl-phenoxy)ethoxyJphettyl}-6-[cyclopropyl{2-p-toIyIetbyI)carbamoyIi-3,9-diaza-bicyclop3.11non-6-eu-3-yl}-3-hydroxy-5-QXopentanoic acid formate salt and (rac)-i3S*y5-{ilR*, 55*)-7-{4-I2- Synthesized according to typical procedures K., E and L from bicyclononene AL71 and 3-(rerf-butyidimethylsilyloxy)glutaric anhydride. LC-MS: Rt = 0.88 ; ES+; 730.49
Example 515

l:l'MiKture of (IR, 5,S)-7'{4-[2-(2-chloro-4,5-dimethyIphenoxy)etfaoxyl-
phenyl}-3-((2.S', ■/Ji)-4-hydroxypyrroliditte-2-carbonyI)-3,9-dia2abicycIo-
[3.3.1]non-6-ene-6-carboiyIic acid (2-chlorobenzyl)cyclopropyIainide formate salt and {IS, 5R)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxylphenyi}-3-((2S, ^i?V4-hydroxypyrrolidine-2-carbonyI)-3,9-dia2abicyclo[3.3.1)non-6-ene-6-carbosyHc acid (2-chlorobenzj'I)cyclopropylamide formate salt
Synthesized according to typical procedures G, E and L from bicyclononene AL56 and BOC-L-hydroxyproline. LC-MS: R( = 0.81 ;ES+: 791.37
Example 516
l:l-Mixture of {IR, 5^-7-{4-[2-(2-chloro-4>dimethyIphenoxy)ethoxy]-
phenyl}-3-((25', '/fl)-4-hydroxypyrroIidine-2-carbonyl)-3,9-dia2abicyclo-
[3.3.1lD.on-6-ene-6-carboxyUc acid cycIopropyl-(2-inethylbeBzyl)amide
formate salt and {IS, 5Jf)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-
phenyl}-3-((25, ^if)-4-hydroxypyrroIidine-2-carbonyI)-3,9-diazab(cyclo-
[3.3.1]non-6-ene-6-carbo3;ylic acid cyclopropyl-(2-methylbenzyl)amide, formate salt
Synthesized according to typical procedures G, E and L from bicyclononene AL60 andBOC-L-hydroxyproline. LC-MS; R4= 0.81; ES+: 699.45
Example 517
iracHJR*, 55*)-3-Acetyl-7-{4-(2-(2,3,5-triiiiethylphenoxy)ethyIIphenyl}-3,9-diazabicyclo[3.3.1Inon-6-eDe-6-carboxylic acid cyclopropylpheoethylamide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL47 and acetyl chloride. LC-MS: R, = 0,92 ; ES+: 592.52

Example 518
(rac.)-(lR*, 55*)-3-Acetyl-7-{4-[2-(2,3,5-triniethylphenoxy)ethyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxyIic acid p-{2-chlorophcnyI)ethyI]-eyclopropylamide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL48 and acetyl chloride. LC-MS: R^- 0.94 ; ES+: 626.51
Example 519
(rac.)-(lR*, 55*)-3-Acetyl-7-(4-[2-(23,5-trimethylpheooxy)ethyl]phenyl}-3,9-diazabicyclo[33.1Inon-6-ene-6-carboxylic acid cycIopropyl-[2-(2^-difluoro-phenyl)ethyllamide formate salt
Synthesized according to typical procedures A and E from bicyclononene Ai49 and acetyl chloride. LC-MS: R, = 0.93 ; ES+: 628.54
Example 520
{racHi^** 55*)-3-AcetyI-7-{4-I2-(23^-trimethylpheQOxy)ethyl]phenyl}-3,9-diazabicycIo[33.11non-6-ene-6-carboxyIic acid cycIopropyI-(3,5-dimethoxy-benzyl)amide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL53 and acetyl chloride. LC-MS: Rt = 0.92 ; ES+: 638.54
Example 521
(rac.)-[lR*, 5S*)-3-acetyl-7-{4-^2-(2,3,5-Trimethylpheooxy)ethyHpUeuyl)-3,9-dia2:abicycIo[3.3.1]non-6-ene-6-carboxylic acid cycIopropyI-(2-;)-tolylethyi)-amide formate salt

Synthesized according to typical procedures A and E from bicyclononene AL54 and acet>-l chloride. LC-MS: R, = 0.94 ; ES+: 606.54
Example 522
{rac.y{lR*, 5S*)-3-Acetyl-7-(4-p-(2,3,5-trimethyIpbenoxy)ethyllpheByI}-3,9-diazabicyclo[3.3.1]non-6-eoe-6-carboxylic acid cycIopropyl-[2-(2-hydroxy-ethyl)benzyl] amide formate salt
Synthesized according to typical procedures A and E from b:cycloi'.bneii:f:*^5£' and acet\-l chloride. LC-MS: Rt = 0.87 ; ES+: 622.55
Example 523
{raayiJR*, 55*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethyIphenoxy)ethoiyI-phenyl}-3,9-dlazabicycIo[3.3.1)non-6-ene-6-carboxyIic acid cyclopropyI-[2-{2-hydroxyethyl)beazyl] amide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL72 and acetyl chloride. LC-MS: Ri= 0.85 ; ES+: 658.47
Example 524
(racyS-iUR*, 55*)-6-(CycIopropylphenethyIcarbamoyl)-7-{4-[2-(2^,5-
trlmethyIphenoxy)ethyIlphenyl}~3,9-diazabicyclo [3.3.1 lnon-6-en-3-yl)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL47 and gtoaric anhydride. LC-MS-. Rt = 0.90 ; ES+-. 664.56
Example 525

(rac.)-5-(ilR*, 55*)-6-{[2-(2-ChIorophenyI)ethyl]cyclopropylcarbamoyl}-7-{4-[2-(2^,5-trim etbylpheaoxy)ethyl] phenyl}-3,9-diazabicyclo [3.3.1 ]non-6-en-3-yl)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL48 and glutaric anhydride. LC-MS: Rt = 0.91 ;ES+: 698.45
Example 526
(rac.)-5-uiJ?% Ji3*)-6-{CyclopropyI-[2-(2^-dinuorophenyI)ethyI]carbamoyl}-7-{4-[2-{2^,5-trimethyIphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ea-3-yI)-5-oxopeDtaQoic acid
Synthesized according to typical procedures K and E from bicyclononene AL49 and glutaric anhydride. LC-MS; Rt = 0.90 ; ES+: 700.50
Example 527
irac)-5-((lR*, 55*)-6-{CycIopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-l2-(23,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1iaon-6-en-3-yl)-S-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene ALSO and glutaric anhydride. LC-MS: Ri = 0.90 ; ES+: 682.54
Example 528
(rac.)S-((lJi*, 55*)-6-[CyclopropyH2-o-toIylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethyIpheD,oxy)ethyl]phenyl}-3,9-dia2abicycIo[3.3.11non-6-en-3-yl)-5-oxo-pentanoic acid

Synthesized according to typical procedures K and E from bicyclononene AL5I and glutaric anhydride. LC-MS: R, = 0.91 ; ES+: 678.55
Example 529
l-.l-Mixture of {rac.)-S-{{lR*, 5S*)-6-[cyciopi-opyK(2i?*)-2-hydroxy-2-phenylethyl)carbamoyl}-7-(4-(2-(2,3,5-trimethyIphenox;)ethyIlphenyI}-3,9-diazabicydo[3.3.1]non-6-en-3-yI)-5-oxopentanoic acid formate salt and (rac.)-S-{{1R*, 55*>-6-leyclopropyl-((25*>-2-hydroxy-2-phenylethyl)carbamoyl]-7-{4-[2-(23»5-trimethylphenox5')ethyl|phenyI}-3,9-diazabicyclo[3.3,l]non-6-en-3-yI) 5-cxopCElanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL52 and glutaric anhydride. LC-MS: Rt = 0.85 ; ES+: 654.50
Example 530
(rac.)-5-((ifi*, 55*)-6-ICyclopropyl-{3,5-dimethoxybenzyI)carbamoyll-7-{4-[2-(2^,5-trimethylpheDOxy)ethyl]phenyI}-3,9-diazabicyclo[33.1]non-6-en-3-yl)-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL53 and glutaric anhydride. LC-MS: R Example 531
(mc.)-5-i(lR*, 55*)-6-[CyclopropyH2-/)-tolylethyl)carbamoyl]-7"{4-[2-(23,5-trimethylphenoxy)ethyl]pheQyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyciononene AL54 and glutaric anhydride. LC-MS: R^ - 0.91; ES+: 678.56

Example 532
(j-ac.)-5-((ifl*, 55*)-6-{CjcIoprop>i-J2-(2-hydroxyethyl)benzyl]carbamoyl}-7-5 {4-[2-{2,3,5-trimethylphenoxy)ethyI]phenyI}-3,9-diazabicydo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid
Synthesized according to typical procedures K and E from bicyclononene AL55 and giutaric anhydride. LC-MS: Rt= 0.85 ; ES+i 694.53 10
Example 533
(rac)-5- Synthesized according to typical procedures K and E from bicyclononene AL72 and giutaric anhydride. LC-MS: Rt = 0.84 ; ES+: 730.46
20 Example 534
iracyS-iilR*, 55*)-6-{CycIopropylphenethylcarbamoyI)-7-{4-[2-(23^tri-methylphenoxy)ethyIlphenyl)-3,9-diazabicyclo [3.3.1 ] iion-6-en-3-yI)-2^-di-methyl-5-oxopeDtanoic acid formate salt
25
Synthesized according to typical piocedures K and E from bicyclononene AL47 and 2,2-dmiethylglutaric anhydride. LC-MS: R, = 0.93; ES+: 692.55
Example 535
30

irac.)-5-i{lR*, 55*)-6-{[2~(2-Chlorophenyl)ethyllcyclopropylcarbamoyl}-7-{4-[2-(23,5-trimethyIphenoiy)ethyI]phenyl}-3,9-diazabicyclo [3.3.1 ] non-6-en-3-yl)-2,2-diinethyI-5-oxop(;ntanoic acid formate salt
Synthesized according to typical pTOcedutes K and E ftom bicycSononene AL48 and 2,2-dimethylglutaric anhydride.. LC-MS: R, = 0.95 ; ES+; 726.48
Example 536
(rac.)-5-((lfl* 5S*)-6-{Cyclopropyl-12-(2,3-difluorophenyl)ethyl]carbamoyli-7-{4-[2-(2,3,5-trimethyJp'"'n"^)f*h;'I]phe!iyl}-?,'»-di:.zabicyclo(3.3.1]noa-6-en-3-yI)-2,2-dimethyI-5-oxopentanoic acid formate salt
Synthesized accordii^ to typical procedures K and E from bicyclononene AL49 and 2,2-dimethylglutaric anhydride. LC-MS; R, - 0.94; ES.+-. 728.51
Example 537
(rac.)-S-{i_lR*, 5iS'*)-6-{Cyclopropyl-(2-(4-fluorophcnyl)ethyIlcarbamoyl}-7-{4-[2-(23.5-triittethylphenoxy)ethyl]pfaenyI}-3,9-diazabicyclo[33.1Inon-6-*n-3-yl)-2,2-dimethyZ-5-oxopeatauoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene ALSO and 2^-dimethyIgiutaric anhydride. LC-MS; Rt= 0.94; ES+; 710.51
Example 538
(racyS-iilR*, 55*)-6-[Cyclopropyl-(2-o-tolyIethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethyIphenoxy)ethyllphenyl}-3,9-diazabicycio[3.3.11non-6-en-3-yl)-2,2-dimetbyI-5-oxopentano)c acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL51 and 2,2-dimethylglutaric anhydride. LC-MS; Rt= 0.95 ; ES+: 706.54
Example 539
(rac,)-5-({JR*, 55*)-6-[Cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-t2-(2,3,5-triinethylpheaoxy)ethyUpheayl}-3,9-diazabicyclQ[33.11nQB-6-en-3-yI)-2,2-dimethyI-5-oxopentanoic acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL53 and 2,2-dimethylglutaric anhydride. LC-MS: Rt = 0.95 ; Ea-r /.so.55
Example 540
(rac.)-5-((lR*, 55*)-6-[Cyclopropyl-(2-;7-toIylethyI)carbamoyI]-7-{4-[2-(23,5-trimethylphenoxy)ethyl)phenyI}-3,9-diazabicycIo{33.11non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid fonnate salt
Synthesized according to typical procedures K and E from bicyclononene AL54 and 2,2-dimethylglutaric anhydride. LC-MS: R, = 0.95 ; ES+: 706.53
Example 541
(rac.)-5-((i/t* 55*)-7-{4-[2-(2-Chloro-4,5-dimethylpheDOxy)ethoxylplienyI}-6-{cycIopropyl-[2-{2-hydroxyethyI)benzylIcarbamoy]}-3,9~dia2abicyclo[3.3.1I-iion-6-en-3-yI)-2,2-dimethyl-5-oxopentanoic acid fonnate salt
Synthesized according to typical procedures K and E from bicyclononene ^72
and 2,2-dimethylglutaric anhydride. LC-MS: R,= 0.87 ; ES+: 758.46
Example 542

■>

(rac.)'(JR*, 55*)-3-(4-CarbamoyIbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethy][]phenyl}-3,9-diazabicyclol3.3.11iion-6-ene-6-carboxj'lic acid cyclopropyl-pheaethylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL47 and 4-carbamoyIbutyric acid. LC-MS: Rt = 0.88 ; ES+: 663-55
Example 543
(mc.H-'J?*, 5^*)-3-(4-CarbaiuoylbutyryI)-7-{4-[2-(23,5-trimetliyIphenoxy)-efhyl]phenyI}-3,9-diazabicyclo[3.3.1]noo-6-ene-6-cai boxylic acid [i-v2-cliiui u-phenyl)etbyl]cyclopropylamide formate salt
Synthesized according to typical procedures G and E &om bicyclononene AL48 and 4-carbamoylbutyric acid. LC-MS: R, = 0.90 ; ES+: 697.49
Example 544
(rac)-(i«* JS*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2^^-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[33.11non-6-ene-6-carboxylic acid cyclopropyl-[2-(23-difluorophenyl)ethyl]amide formate salt
Syntiiesized according to typical procedures G and E from bicyclononene AL49 and4-carbamaylbutyric acid. LC-MS-. Rt= 0.89 ; ES+: 699.49
Example 545
(rac,)-(2R% 55*)-3-(4-Carbamoylbutyryl)-7-{4-12-(2,3,5-trimetbylpliettoxy)-etbyllphenyl}-3,9-diazabicycIo[3.3.11non-6-ene-6-carboxylie acid cyclopropyl-
[2-(4-fluorophenyl)ethy!lamide formate salt

Synthesized according to typical procedures G and E &dm bicyclononene ALSO and 4-carbamoylbutyric acid. LC-MS; Ri= 0.88 ; ES+: 681.54
Example 546
{rac.)-{lR*, 55*)-3-(4-Carbamoy]butyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyllphenyI}-3,9-diazabicycIo[3.3.11non-6-ene-6-carboxyIic acid cyclopropyl-(3,5-dimefhoxybenzyl)ainide formate salt
%k
Synthesized according to typical procedures G and E firom bicyclononene AL53
and 4-carDamoyiDutyric acid. LC-MS: Rt = 0.87 ; ES+: 709.50
Example 547
(racHlR*, 55'*)-3-(4-Carbamoylbutyryl)-7-{4-I2-(23,5-trimethylpheDOxy)-efhyI]phenyI}-3,9-diazabicyclo[3.3.1Jnon-6-ene-6-carboxylic acid cyclopropyl-(2-^-toIylethyl)aDiide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL54 and 4-<:arbamoylbutyric acid. lc-ms: rt="0.89;" es> Example 548
{racH^R*, 55*)-3-(4-CarbamoyIbutyryl)-7-(4-[2-(2^,S-trmiefhylphenoxy)-ethyIIphenyl}-3,9-d!a2abicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-I2-(2-hydroxyethyl)benzyl]amide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL55 and 4-carbamoylbutyric acid. LC-MS: R, = 0.83 ; ES+: 693.53
Example 549

(rac,)-(JR*, 55*)-3-(4-CarbainoyIbutyryl)-7-{4-[2-(2-cIjIoro-4,5-dimethyI-
phenox>)cthoxy]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-[2-(2-hydrosyethyi)benzji]amide formate salt
Synthesized according to typical procedures G and E from bic\"cloaQnene AL72 and 4-carbamoylbutyric acid. LC-MS: Ri = 0.82 ; ES+: 729.48
Example 550
(rac.)-Acetic acid (IR*, 5S*)-2-(2-{l(3-acetyl-7-{4-[2-(2,3,5-trimetbyl-piienui*)cihyIi|juenyl}-3,9-diazabicyclo[3.3.11nQD-6-ene-6-carbottyl)cyclo-propylamino]methyI}phenyl)ethyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL and acetyl chloride. LC-MS: R. = 0.93 ; ES+: 664.55
Example 551
(raa)-Acetic acid (IR*, J^*)-2-(2-{[(3-acetyl-7-(4-[2-(2-cbloro-4,5-dimefhyl-phenosy)efhoxylphenyI}-3,9-diazabicyclo[3^.1Jnon-6-ene-6-carbonyl)cycIo-propylamino]methyl}phenyl)etbyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL72 and acetyl chloride. LC-MS: Rt = 0.91 ; ES+: 700.44
Example 552
{rac.)~{lR*, 55*)-7-{4-(2-(233-Trimethylphenoxy)ethyllphenyll-3,9-diaza-bicyclo[3.3.11non-6-ene-6-carbo.\ylic acid cy do propyl-[2-{4-fluorophenyl)-etbyljamide formate salt

Synthesized according to typical procedure E fi-om bicyclononene AK50. LC-MS: R,-0.86 ;ES+: 568.50
Example 553
irac.)-(IS*, 5^*)-7-{4-I2-(2,3,5-Trimetliylphenoxy)efhyllphenyli-3,9-diaza-bicyclo(3.3.1 ]non-6-ene-6-carboxyIic acid cycIopropyl-(3,5-dimethoxybenzyI)-amide formate salt
Synthesized according to typical procedure E from bicyclononene AK53. LC-MS: Rt = 0.85; EC+-: 595.55
Example 554
(rac)-Acetic acid (JR*, 55*)-2-(2-{[(3-acetyl-7-{4-[2-(4-bromophenoxy)-ethoxy] phenyl}-3,9-diazabicy do [3.3.1 J non-6-ene-6-car bo nyl)cycIopropyl-amino]methyl|phenyl)etbyl ester formate salt
Synthesized according to typical procedures A and E from bicycloaonene AL87 and acetyl chloride. LC-MS: R, = 0.89 ; ES+: 716.35
Example 555
1:1 Mixture of (rac)'5-{i2R*, 55*)-7-{4-[2-(2-chIoro-4,5-dimethylphenoxy)-ethQxylplienyl}-6-(((2R*)-2-hydroxy-2-ph.eayIethyl)methylcarbamoyn-3,9-diazabicycIoI3.3.1]noii-6-en-3-yi}-2^-dimethyl-5-oxopentanoic acid formate salt and (racy5-{(lR*, 55*)-7-{4-I2-(2-chloro-4,5-dimetbylpfaenoxy)-ethoxy] pheny l)-6- [((2S*)-2-hy dr oxy-2-phenyletbyl)methylcarbamoyl) -3,9-diazabicy clo [3.3-1] no tt-6-en-3-yl}-2,2-dimethyI-5-oxo pen tanoic acid formate salt

Synthesized according to typical procedures K and E from bicyclononene AL69 and 2,2-dimethylglutaric anhydride. LC-MS: Ri = 0.88 ; ES+: 71 S.47
Example 556
(rac.)-(lJi*, 55*)-3-Acetj'I-7-{4-[3-(2-bromo-5-fluorophenoxy)propyIlphenyI}-3,9-diazabicyclo[3.3.1]iioii-6-eDe-6-carboxyUc acid (2-cbIorobeii2yI)cyclo-propylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL20 and acetyl chloride. LC-MS. R( = Z.GZ, ES+; 680.28.
Example 557
{rac.)-{lR*, 55*)-7-{4-[3-(23,6-Trifluorophenoxy)propylIphenyl}-3,9-diaza-bicycIo[33.1]noD-6-«ne-6-carboxylic acid benzylcyclopropylamide formate salt
Synthesized according to typical procedure E from bicyclononene AK3. LC-MS: R, = 0.S3;ES+-. 562.38
Example 558
{racyilR*, 55*)-7-{4-[3- SjTithesized according to typical procedure E from bicyclononene AK4. LC-MS: Rt = 0,84 ;ES+: 584.35
Example 559

(rac.)-(i/f* 5^*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyI]pIienyl}-3,9-diaza-bicycIo(3.3.Hpon-6-ene-6-(;arboxyiic acid cyclopropyI-(2-fluorobeazyl)ainide formate salt
Synthesized according to typical procedure E &om bicyclononene AK5. LC-MS: Rt=0.83;ES+: 580.38
Example 560
irac.)~{lR*, 55*)-7-{4-[3-(2»3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diaza-bicyclo[3.3.11aon-6-ene-6-carboxylic acid i.-yclupi'0p>i-(3-triiiuur6iatthyl-benzyl)amide
Synthesized according to typical procedure E from bicyclononene AK6. LC-MS: R,= 0.86 ;ES+: 630.43
Example 561
{rac)-{lR*, 5.S'*)-7-{4-[3-(2^,6-Trifluorophenoxy)propyl]phenyl}-3,9-dia2a-bicyclo[33.1Jnon-6-ene-6-carboiyIic acid cyclopropyl-(2-methylbenzyl)amide formate salt
Synthesized according to typical procedure E from bicyclononene AK7. LC-MS: Rt= 0.84 ;ES+: 576.42
Example 562
{rac,)-(JR*, 55*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-eae-6-carboxylic acid cycIopropyl-[2-(4-methoxy-phenoxy)ethyl]amide formate salt

Synthesized according to typical procedure E from bicyclononene AK8. LC-MS: Rt= 0.83 ;ES+: 622.45
Example 563
{rac.)-ilR*, 55*)-7-{4-[3-(2,3,6-Trinuoi'ophenoxy)propyl)phenyi}-3,9-diaza-
bicyclot3.3.1inoii-6-ene-6-carbosyIic acid [2-(2-chlorophenyl)ethyll-
cyclopropylamide formate salt
Synthesized according to typical procedure E from bicyclononene AK13. LC-MS: Rt= 0.86 ;ES+: 610.39
Example 564
(rac.)-(ii;*, 5S*)-7.{4-(3-(23,6-Trifluoropbenosy>propyllphenyl}-3,9-diaza-bicycIo[3,3.11noii-6-ene-6-carboxylic acid cyclopropyl-[2-(2,3-difluoro-phenyI) ethyl] amide formate salt
Synthesized according to typical procedure E from bicyclononene AK14. LC-MS: R, = 0.85 ; ES+: 612.44
Example 565
(rac)-(lR*, J5*)-7-{4-[3-(23,6-Trifluorophenoxy)propyllphenyl}-3,9-diaza-bicycIo[33.1Inon-6-ene-6-carboxylic acid cyclopropyl-(2-o-tolylethyl)amide formate salt
Synthesized according to typical procedure E from bicyclononene AK16. LC-MS: Rt = 0.85 ; ES+: 590.42
Example 566

(racHIR*, 55*)-7-{4-p-(2,3,6-Trinuorophcnoxy)propyl]phenyI}-3,9-diaza-bicycIo[3.3.1Jnon-6-ene-6-carboxylic acid cycIopropyl-(2-;j-tolylethyl)ainide formate salt
Synthesized according to typical procedures G and E from bicyclononene AK18. LC-MS: Ri = 0.85 ; ES+: 590.42
Example 567
irac.)-(JR% 55*)-3-AcetyI-7-{4-[3-(23-difluorophenoxy)propyl]phenyI}-3,9-diazabicycloli3.1]Doii-6-ene-6-carboxyIic acid (2-chIorobchzyI)cyclopropyt^ amide formate salt
Synthesized according to typical procedures F and E from bicyclononene BBl and 2,5-difluorophenoI. LC-MS: Rt = 0.89 ; ES4-: 614.40
Example 568
(racyilR*. 55*)-3-Acetyl-7-{4-[3-(2»3-dichlorophenoiy)propyI]phenyI}-3,9-diazabicycIo[33.1)non-6-ene-6-carboxylic acid (2-chloroben2yl)cycIopropyI-amide formate salt
Synthesized according to typical procedures F and E from bicyclononene BBl and 2,3-dichorophenoI. LC-MS: R| = 0.94; ES+: 654.32
Example 569
(rac.)-(JR*, 55*)-3-Acetyl-7-{4-[3-(2-chloro-S-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]Don-6-ene-6-carboxylic acid (2-chlorobeozyl)cyclo-propylamide formate salt

Synthesized according to typical procedures F and E from bicyclononene BBl and 2-chlora-5-fluorophenol. LC-MS: R, = 0.93 ; ES+: 636.36
Example 570
irac,)-{lR*, 55'*)-3-AcetyI-7-{4-[3-(3-cyanopyridin-2'ylox>-)propyIlpheoyl}-3,9-diazabicydop3.1Jnon-6-eiie-6-carboxyUc acid (2-ch\orobenzyl)cyc\o-propylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene BBl and
2-hydiOxymt;udnonitrile. LC-MS: Ri = 0.86 ; ES+: 610.42 " '"
Example 571
{racyilR*, 5S*)-7-{4-(3-(23,6-Trifluorophenoxy)propyl]phenyl}-3,9-diaza-bicyclo[3.3.11non-6-ene-3,6-dicarboxylic acid 6-[(2-chlorobenzyI)c:yclopropyl-amide] 3-dimethylainide formate salt
Synthesized according to typical procedures A and E firom bicyclononene AL2 and dimethylcarbamoyl chloride. LC-MS: R^ = 0.91 ; ES+: 667.42
Example 572
{rac)-{lR*, 55*)-7-{4-[3-(23,6-Trifluorophenoxy)propyI]phenyl}-3^-diaza-bicycloi33.1Jnon-6-ene-3,6-dicarboxyUc acid 6-[(2-chlorobenzyl)cyclopropyl-amide] 3-diethylamide formate salt
Synthesized according to typical procedures A and E from bicyclononene AL2 and diethylcaibamoyl chloride. LC-MS: R, = 0.95 ; ES+: 695.44
Example 573

{rac.)-(lS*, 5S*)-6-[(2-Chlorobenz>l)cyclopropylcarbamoyIJ-7-{4-|3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-diazabicyclo [3.3.1 Jnon-6-ene-3-carboxylic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL2 and methyl chloroformate. LC-MS: R, = 0.91 ; ES+: 654.37
Example 574
{rac)-{lR*, 55 *)-6-l(2-Chlorobenzyl)cyclopropylcarbamoylJ-7-{4-l3-(2^,6-trifluoropheuoxy)propyljphenyI}-3,9-dia2abicyclo[33.1Inon-6-ene-3-carbo-xylic acid etfayl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL2 and ethyl chloroformate. LC-MS; Rt = 0.93 ; ES+: 668.40
Example 575
{racy{JR*, 55*)-3-MethanesulfonyU7-{4-{3- Synthesized according to typical procedures A and E from bicyclononene AL2 and methylsulfonyl chloride. LC-MS; R, = 0.92 ; ES+: 674.37
Example 576
{rac.)-{JR*, 55*)-3-EthanesuifonyI-7-(4-[3-(2,3,6-trifIuorophenoxy)propylI-pbeiiyl}-3,9-diazabicyclo[3.3.11non-6-eiie-6-carboxylic acid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures A and E from bicyclononene AL2 and ethylsulfonyl chloride, LC-MS: R, - 0.93 ; ES+: 688.36
Example 577
(racyS-iilR*, 55*>6-[(2-ChlorobenzyI)cyclopropylcarbainoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl] phenyl}-3,9-diazabicy do [3.3.1 lnon-6-eD-3-y l)-5-oxo-pentanoic acid ethyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL2 and glutaiic acid monoetliylestc._c'^or:dc. LC-MS: ^ = 0.94 ; ES+: 738.41
Example 578
{rac)-4~mR*, 5.S*)-6-[(2-ChIorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(23,6-trifluorophenosy)propyl|[pheoyl)-3,9-diazabicyclo[3.3.11noa-6-eo-3-yl)-4-Qxo-butyric acid formate salt
Synthesized according to typical procedures K and E from bicyclononene AL2 and succinic anhydride. LC-MS: R^ = 0.87 ; ES+: 696.36
Example 579
(rac)-3-l((ii{*, 55*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyll-7-{4-[3-
(23t6-trifluorophenoiy)propyllphenyI)-3,9-dia2abicyclo[3.3.1Juon-6-ene-3-carbonyO^^'Dolpropionic acid ethyl ester formate salt
Synthesized accordmg to typical procedures A and E from bicyclononene AL2 and ethyl 4-isocyanatopropionate. LC-MS: Rt = 0.93 ; ES+: 739.41
Example 580

(rac.)4-l((lR*, J5*)-6-[(2-Chlorobenzjl^yclopropyicarbamoyI]-7-{4-I3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carbonyl)amiao]butyric acid ethyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene AL2 and ethyl 4-isocy3natobutyrate. LC-MS: R, = 0,93 ; ES+: 753.39
Example 581
irac.)'iJR*, 5^*)-3-(3-Carbamoyipropionyl)-7-{4-[3-(2^,6-trinuorophettoxy)-propyl]phenyl}-3,9-diazabicyclo[33.1]nnn-6-enf!-6-carhoxj'Jw" 9*iJ {2-chloro-benxyl)cydoprDpylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL2 and succinamic acid. LC-MS: Rt = 0.85 ; ES+: 695.38
Example 582
(racH^R*, 5S*)-3-(2-Hydroxyacetyl)-7-{4-[3-(2^,6-trifluorophenoxy)-
propylIphenyl}-3,9-diazabicycIo[3J.llnon-^-ene-6-carborylic acid (2-chloro-beDzyl)cyclopropylamide formate salt
Synthesized according to typical procedures G and E from bicyclononene AL2 and glycoUc acid LC-MS: R Example 583
(75, 5«)-3-((ifi)-3-Hydroxybutyryl)-7-{4-[3-(23,6-trifluorophenoxy)propyll-ph€nyl}-3,9-diazabicycloI3.3.1]non-6-ene-6-carboiyKc acid (2-chlorobeozyl)-
cyclopropylamide

Synthesized according to typical procedures G and E from bic>xIononene AL2 and (ii?)-3-hydroxybutyric acid. LC-MS: R,= 0.88; ES+: 682.40.
Example 584
l:l-Mixture of (rac,)-(lR*, 5S*)-3-(lilR*, 25*)-2-hydroxycyclopeiitane-carbony I)-7- {4- [3-(23)6-trifluorop hen osy)propyll phenyl} -3,9-diazabicy cio-[3.3.1]non-6-ene-6-carboxylic acid (2-cbIorobenzyl)cycIopropyIamide formate salt and (rac.)-(lR*, SS*)-3-((lS*, 2i?*)-2-hydroxycycIopenianecarboDyl)-7-{4-[3-(23»6-trifluorophenosy)propyl]phenyI}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboiyHc acid {2-chlorobenzyl)cyclopropyIaija;Jc forsi-tesai*
Synthesized according to typical procedures G and E from bicyclononene AL2 and cis-2-hydroxy-l-cycIopentane carboxylic acid. LC-MS: Rj = 0.91; ES+: 708.39.
Example 585
(rac)-(JJf* J5*)-9-Acetyl-7-{4-(3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo [3.3.1] 000-6-60e-6-carboxylie acid (2-chlorobeiizyl)cycIopropyI-amide formate salt
Synthesized according to typical procedures A and E from bicyclononene BC and acetyl chloride. LC-MS: ^ = 0.92; ES+: 638.34.
Example 586
{rac.)-5-((JR*, 55*)-6-[(2-Chlorobenzyl)cyclopropylearbamoyll-7-{4-[3-(2,3,6-trinuorophenoxy)propyi]phenyl}-3,9-dia2abicyeloI3.3.1]non-6-en-9-yl)-5-oxo-pentanoic acid formate salt

Synthesized according to typical procedures K and E from bicyclononene BC and glutaric anhydride. LC-MS: R, = 0.91; ES+i 710.33.
Example 587
{rac.)-5-(i2}f% 5^*)-6-[(2-ChIorobenzyl)cyclopropyIcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-dia2abicycIo [3.3.1 ]non-6-en-9-yl)-5-oxo-pentanoic acid methyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene BC and gluranc acid monomethylester chloride. LC-MS: Rt = 0.95; ES+: 724.i3. "': " "
Example 588
{rac.y5-((lR*, 5>y*)-6-[(2-ChIorobenzyl)cyclopropylcarbamoyl]"7-{4-[3-(23,6-triiluorophenoxy) propyl] plienyl}-3,9-diazabicy do [33.l]non-6-en-9-y l)-5-oxo-pentanoic acid ethyl ester formate salt
Synthesized according to typical procedures A and E from bicyclononene BC and glutaric acid monoethylester chloride. LC-MS: Rt = 0.97; ES+: 738.38.
Example 589
irac)-4-[(ilR*, 55*>6-[(2-ChIorobeiizy!)cyclopropyIcarbamoyI]-7-{4-[3-
(2^,6-trifluoropheiu>3y)propyllphenyl}-3,9-diazabicyclo[3.3.11non-6-ene-9-carbooyl)-aminoIbutyric acid ethyl ester
Synthesized according to typical procedures A and E from bicyclononene BC and ethyl 4-isocyanatobutyrate. LC-MS: Rt = 0.95; ES+: 753.37.
Example 590

(rac.)-(lll*, 55*)-3-Formyl-7-{4-[3-(2,3,6-trifluorophenox>-)propyI]phenyi}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid (2-chloroben!yl)cyclo-propylamide
Syntliesized according to typical procedure E from bicyclononene AK2. Obtained as side-product after purification by HPLC. LC-MS; Rt = 0.89; ES+: 624.36.
Example 591
(rac)-3-[({IS% 55*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-
(2^,6-'tfi;iuorophenoxy)propyIlphenyl}-3,9-diazabicyclo[33.11non-6r£c; 3 -car bony I)ainino] propionic acid formate salt
Synthesized according to typical procedures M and E from Example 579, then typical procedure E. LC-MS: Ri = 0.87; ES+: 711.31.
Example 592
(rac)-3-[((lR*, 55*)-6-[(2-ChlorobeiizyI)cyclopropylcarbamoyI]-7-(4-[3-
(2»3i6-trifluorophenoiy)propyl]plienyl}-3,9-diazabicyclo[33.1]non-6-ene-9-carboayl)amiao{propiQiiic acid formate salt
Synthesized according to typical procedures G, M and E from bicyclononene BC and ethyl 4-isocyanatopropionate. LC-MS: Rt = 0.88; ES+: 711.33.
Example 593
irac)-4-[(ilR% 5^*)-6-[(2-Chlorobeii2yl)cyclopropylcarbamoyl]-7-{4-I3-
(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-dlazabicyclo[3.3.11non-6-ene-9-carbonyl)aminolbutyric acid formate salt

Synthesized according to typical procedures M and E from Example 580. LC-
MS:Rt= 0.89; ES+: 725.35.
Example 594
(rac.)-(JR*, 55*)-3-acetyl-7-{4-[2-(2,3,6-TrifluorophenoX}')ethyl]phenyi}-3,9-dia2abicyclo[3.3.11non-6-ene-6-carboxylic acid (2-chlorobenzyl)cyclopropyI-amide formate salt
Synthesized according to typical procedures F and E &om bicyclononene BB2 and 2,3,6-tritmbrophenoi. Lc-MS: RV^ 0.89; ES+: 624.37.
Example 595
irac.y(lR*, 55*)-3-AcetyI-7-{4-[2-(23-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1Inon-6-ene-6-carboxylic acid (2-chIorobenzyl)cyclopropyl-amide formate salt
Synthesized according to tj^ical procedures F and E from bicyclononene BB2 and 2,3-dimethylphenol. LC-MS: R, = 0.91; ES+: 598.42.
Example 596
(racy(JR*, 55*)-3-Acefyl-7-{4-[2-(2,5-dimetliylphenoiy)efhyI]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid (2-cblorobeiizyl)cyclopropyl-amide
Synthesized according to typical procedures F and E from bicyclononene BB2 and
2,5-dimethyIplienoI. LC-MS: R, = 0.91; ES+: 598.43.
Example 597

(racyilR-^, 55*)-3-Acetyl-7-{4-[2-(2-chioro-4,5-dimethylphenoxy)ethyI]-
phenyI]-3,9-diazabicyclo{3.3.1]non-6-eae-6-carboxylic acid (2-chlorobenzyI)-cyclopropylamide formate salt
Synthesized according to typical procedures G and E firom bicyclononene BB2 and 2-chloro-4,5-dimethyIphenoi. LC-MS: R, = 0.93; ES+: 632.39.
Example 598
(rac.)-{2R% 55 *)-3-Acetyl-7-{4-I2-(2,4-dichlorophenoxy)ethyl] phenyl}-3,9-dia2abicycic[3.3.1Jno2-6-ecc 6-c£r!boxyIic acid (2-chlorobenzyl)cyclopropyI-amide formate salt
Synthesized according to typical procedures F and E from bicyclononene BB2 and 2,4-dicbJorophenol. LC-MS; Rt = 0.91; ES+: 640.32.
Example 599
(racH^R*, 55*)-3-Acetyl-7-{4-{2-(23-dichIorophenoxy)ethyl]phettyI}-3,9-diazabicycIoI33.1]noii-6-eiie-6-carboxyIic acid (2-chlorobenzyl)cycIopropyl-amide formate saVt
Synthesized according to typical procedures F and E from bicyclononene BB2 and 2,3-dichloroplienol. LC-MS: Rt = 0.91; ES+: 640.34.
Example 600
(rac.yilR*, 55*)-3-Acetyl-7-{4-[2-{2,6-difluorophenoxy)ethyllphenyl}-3,9-diazabicyelo [3.3,1] Don-6-ene-6-carboxylic acid (2-chlorobeiizyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononene BB2 and 2,6-difliiOTophenol. LC-MS: Ri = 0.S8; ES+: 606.39.
Example 601
{rac.)-(lR*, 55*)-3-Aeetyl-7-{4-[2-(2,5-difluorophenoxy)ethyI]phenyl}-3,9-diazabicycIo[3.3.I]non-6-ene-6-carboxylic acid (2-chIorobeazyI)cyclopropyI-amide fromate salt
Synthesized according to typical procedures F and E from bicyclononene BB2 and
2,5-difluorophenol. LC-MS: R, = 0.is»; BS+: 6U6.40. '" '
Example 602
{rac.)-{lR*, 55*)-3-Acetyl-7-{4-[2-(3,5-dichlorophenoxy)ethyl]phen3i}-3,9-diazabicyclD[3.3.1]Don-6-ene-6-carboxylic acid (2-chIorobenzy!)cyclopropyl-amide
Synthesized according to typical procedures F and E from bicyclononene BB2 and 3,5-dichlorophenol. LC-MS: Rt = 0.93; ES+; 638.32.
Example 603
{rac)-(lR*, 55*)-3-Acetyl-7-{4-[2-(2-chloro-5-methylphenoxy)ethyl|phenyl}-
3,9-diazabicyclo [3.3.1 ]non-6-ene-6-carboxyIic acid (2-chloroben2yl)-
cyclopropylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene BB2 and 2-chJoro-5'methylpheno[. LC-MS: R, = 0.91; ES+: 618.40.
Example 604

{rac.)-(lll*, 55*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethyljphenyI}-
3,9-diazabicyclo[3.3.1]aon-6-ene~6-carboxylic acid (2-chloroben2yl)-
cyclopropylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene BB2 and 2-chloro-5-fluorophenol. LC-MS: Rt= 0,89; £S+: 622.33.
Example 605
irac.)-(IR*, 55*)-3-Acetyl-7-{4-{2-(23,6-trichlorophenoxy)ethylIphenyl}-3,9-dia2abicycIo[3.3.1]non-6-ene-6-carlboiyIic add {2-cli:GrGben=5 l)cyclopropyI-amide formate salt
Synthesized according to typical procedures F and E from bicyclononene BB2 and 2,5,6-trichlorophenol. LC-MS: Rt = 0.93; ES+: 674.27.
Example 606
(rac.)-{llt*, 5^*)-9-(4-Carbamoylbutyryl)-7-{4-[2-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-dia2abicyclo[3.3.11non-6-ene-6-carboxyIic acid (2-chlorobenzyOcyclopropylamide formate salt
Synthesized according to typical procedures G and E &om bicyclononene BC and 4-carbamoylbutyric acid. LC-MS: R^ = 0.88; ES+: 709.39.
Example 607
{rac.)'iJR*, 55*)-9-(3-Carbamoylpropionyl)-7-{4-[2-(2,3,6-trifluorophenos:y)-propyl]phenyI}-3,9-dia2abicyclo[3.3.11non-6-ene-6-carboxylic acid (2-chIoro-ben2yI)cycIopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononene BC and succinamic acid. LC-MS: R, = 0.88; ES+: 695.36.
Example 608
{rac.yilR^, 55*)-9-(2-Hydroxyacetyl)-7-{4-I2-{2,3,6-trinuoKipheaoxj')-
propyllpheayl}-3,9-diazabicycIo[33.1Inoii-6-ene-6-carboxylic acid (2-chloro-beiizyl)cyclopropylaniide formate salt
Synthesized according to typical procedures G and E from bicyclononene BC and
glycolic acid. LC-MS: R, = 0.90; ES+: 654.37. - '
Example 609
(IR, 55)-9-((5^-3-Hydroxybutyryl)-7-{4-[2-{23,6-trifluorophenoxy)propylI-phenyl}-3,9-diazabicycIo[3J.l]non-6-ene-6-carboxyIic acid (2-chlorobenzyl)-cyclopropylamide formate salt
Synthesized according to typical piocedures G and E from bicyclononene BC and (5i?)-3-hydroxybutyric acid. LC-MS; Rt = 0.91; ES+; 682.41.
Example 610
(rac.)-{JR*, 55*)-9-Methanesulfonyl-7-{4-[2-(2^,6-trifluorophenoiy)propyll-phenyl}-3,9-diazabicycIo[33.1]non-6-ene-6-carboxyIic acid (2-chlorobeiizyI)-cyclopropylamide formate salt
Synthesized according to typical procedures A and E from bicyclononene BC and methylsulfonyl chloride. LC-MS: Rj = 0.95; ES+: 674.38.
Example 611

(rac.)-{IR*, 55*)-9-Ethanesulfonyl-7-{4-[2-{2,3,6-trifluorophenoxy)propyll-phenyi}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylie acid (2-chlorobenz>'I)-cyclopropylamide formate salt
Synthesized according to t>'pical procedures A and E from bicyclononene BC and ethylsulfonyi chloride. LC-MS: R, = 0.97; ES+: 688.37.
Example 612
(mc.)-(iif*, 55*)-3-Acetyl-7-(4-[3-(23,6-trinuorophenoxy)propyllphenyl}-3,9-diazabicycIo[3.3.11aon-6-ene-6-carboxylic acid cycioprcpyl-{2-fluoit, 5-methoi'ybenzyl)aniide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and cyclopropyl(2-fluoro-5-methoxybenzyl)amin6. LC-MS: Rt = 0.89; ES+: 652,31.
Example 613
(rac.)-(i-ff*, 55*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicycio{3-3.1JQon-6-ene-6-carboxylic acid cyclopropyl-(3-methoxy-beDzyI)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and cyclopropyi(3-methoxybenzyl)amine. LC-MS; Rt = 0.88; ES+: 634.34.
Example 614
{rac.)-(IR% 5.S*)-3-Acetyl-7-{4-13-(2,3,6-trinuorophenoxy)propyl]phenyI}-3,9-diazabicyclo[3.3,llnon-6-ene-6-carboxylic acid cyclopropyl-(2-niethoxy-l)enz>i>amide formate salt

Synthesized according to typical procedures H and E from bicyclononene AJ2 and cyclopropyl(2-methoxybenzyl)araine, LC-MS: R, = 0.S9; ES+: 634.32.
Example 615
{fac.)-(m% 55*)-3-Acetyl-7-{4-[3-(2,3,6-trinuorophenoxy)propyl)phenyl}-3,9-diazabicyclo[3.3.1]noa-6-ene-6-carbox\iic acid eye lop ropy l-(3,4-dim ethoxy-benzyl)ainide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and cyclopropyl(3,4-dimetiioxybenzyl)amine. LC-MS: R| = 0.86; ES+: 664.34.
Example 616
{rac,)-(lR*, 55*)-3-Acetyl-7-{4"[3-(2,3,6-trifluorophenoxy)propyI]phenyl}~3,9-d!azabicycIo[3.3.1]non-6-ene-6-carboxylic acid (2-cbloro-3-trifluoromethyl-benzyl)cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and (2-cbloro-3-trifluoromeliiylbenzyl)cyclopropylamine. LC-MS; R[ = 0.94; ES+: 706.20.
Example 617
(rac)-(JR*, 55*)-3-AcetyI-7-{4-[3-(23,6-trifluorophenoa:y)propyl]phenyl}-3,9-diazabicyclo[3.3.11noii-6-eBe-6-carboxyUc acid beazo[131dioxol-S-ylmethyl-cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and (6-chloroben2o[l,3}dioxol-5-ylmethyl)cycloprQpy!amine. LC-MS: Ri= 0.91; ES+: 682.2S.

Example 618
{rac.)'(JR\ 5^*)-3-Acetyl-7-(4-13-(2^.6-trinuoropheno\y)propyllpliettyli-3,9-diazabicyclo[3.3.1]non-6-£ne-6-carbox>Iic acid cycIopropyl-(5-fluoro-2-methos>benizyl)amidc formate salt
Synthesized according to tvpical procedmes H and E iirom bicyclononene AJ2 and eyelopropyI(2-meihoxy-5-flitorobenzyl)amine. LC-MS: Rt = 0.90; ES+: 652,32.
Example oi9
(racHJlR*, 55*)-3-Acetyl-7-{4-(3-(23,6-trifiuoropheDoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-eae-6-carbox>lic acid (2-chloro-6-fluorobenz>d)-cyclopropylainide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and cyclopropyl(2-chioro-6-fluorobenzyl)arainc. LC-MS: R, = 0.89; ES+: 656.30.
Example 620
(rac)-(JR*, 55*)-3-AcetyI-7-{4-[3-(2,3,6-trifluoropheooxy)propylIplienyl}-3,9-diazabicyclo(3.3.1]non-6-ene-6-carboxylie acid (2-bromobenzyl)cyclopropyI-amide formate salt
Synthesized according to typical pcocedures H and E firom bicyclononene AJ2 and cyclopropyl{2-bromobenzyl)amine. LC-MS: Ri = 0.91; ES-i-: 684.23.
Example 621

(rac.)-(lR*, 5.y*)-3-Acetyl-7-{4-[3-{2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-diazabicycIo[3.3.1]noD-6-ene-6-carbox5lic acid cycIopropy]-(2,6-difluoro-benzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and cyclopropyl(2,6-difluorobenzyl)aniine, LC-MS: R, = 0.88; ES+: 640.29.
Example 622
(rac)-(IR*, 5.y*)-3-AcetyI-7-{4-[3-(2^,6-trifluorophenoxy)propyllpheiiyI}-3,9-diazabicycloI33.1]non-6-ene-6-carboxyIic acid cytiopropyI-(2,3-dmiethyl-beiizyl)amide formate salt
Synthesized according to typical procedures H and E &om bicyclononene AJ2 and cycIopropyl{2,3-dimethylbenzyl)aniine. LC-MS: Rt = 0.92; ES+: 632.35.
Example 623
(racH^if*, 55'*)-3-Acety^-7-{4-[3-(23,6-trifluoropheaoxy)propyI]phenyIJ-3,9-diazabicyclo[3.3.1]noD-6-ene-6-carboxylic acid cyclopropyl-(3-fluoro-2-methylbenzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and cycIopropyl(2-methyl-3-fluorobenzyl)amine. LC-MS: R, = 0.91; ES4-: 636.31.
Example 624
{rac.)-{lJi*, 55*)-3-Acetyl-7-{4-[3-(2,3>6-trifluoroph€noxy)propyl]phenyl}-3,9-diazabicyclo[3.3,lliion-6-ene-6-carboxyUc acid cyclop ropy l-(3,5-difluQro~ benzy\)amide formate salt

Synthesized according to typical procedures H and E from bicyclononene AJ2 andcyc[opropyl(3,5-ditluorobenzj-l)ainine. LC-MS: R, = 0.93; ES+: 672.23,
Example 625
irac.y(JR*, 5^*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenox>0propyI]phenyi}-3,9-diazabicyclo[3.3.11non-6-ene-6-carboxylic acid (2-chIoro-3,6-difluoroben2yI)-cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and cyclopropyl(2-cliJoro-3,6-d;riUonjl:>tnzyl)aniine. LC-M3: Rt = 0.90; ES+: 674.25.
Example 626
{rac.)'{lR*, 55*)-3-Acetyl-7-{4-[3-(2,3,6-triflmiropheQoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.11non-6-ene-6-carboxjiic acid cyclop ropy I-(23-dichIoro-benzyOamide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and cyclopropyl(2,3-dichlorobenzyl)amiiie. LC-MS: R(- 0.93; ES+: 672.25.
Example 627
(rac.)-(JR*, 55'*>3-AcetyI-7-{4-f3-(2,3,6-trifluorophenoxy)propyiIphenyI}-3,9-diazabicyclol3.3.11oon-6-eoe-6-carboxylic acid cyclopropyH3-trifluoro-methoxybenzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and cyclopropyl(3-trifluorometho>:ybenzyl)amine. LC-MS: Rt = 0.93; ES+: 688.28.

Example 628
{rac.)-{lR*, 5>S'*)-3-AcetyI-7-{4-[3-(2,3,6-trinuorophenoxy)propyllphenyl}-3,9-diazabicyclo[3.3.11non-6~ene-6-carboxylic acid cycIopropyl-(3-methyIbenzyl)-amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and cydopropyI(3-methylbenzyl)ainine. LC-MS: Rt = 0.90; ES+: 618.36.
Example 629
(rac.)-(JR*, 55*)-3-AcetyI-7-{4-[3-(23,6-trifluorophenoxy)propyllphenyI}-3^-diazabicyclo[33.1jnon-6-ene-6-carboxylic acid cyclopropyI-(2,3-difluoro-benzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and cyclopropyl(2,3-difluorobenzyl)amine. LC-MS: Rt = 0.90; ES+: 640.29.
Example 630
{rac.)-{JR*, 55*)-3-Acetyl-7-{4-[3-(23,6-trifluorophenoxy)propyi]phenyl}-3,9-(liazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (3-chlorobeiizyI)cyclopropyI-amide formate salt
Synthesized according to typical procedures H and E from bicyclononene AJ2 and cyclopropyl(3-chlorobenzyl)amine. LC-MS: Rt = 0.91; ES+: 638.27.
Example 631
(rac.)-{lR% 55*)-3-Acetyl-7-{4-l3-(2,3,6-trinuorophenoxy)propyllphenyl}-3,9-diazabicycloi3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(4-nuorobenzyl)-amide formate salt

Synthesized according to typical procedures H and E from bicyclononene AJ2 and cyclopropy](4-fluorobenzyl)amine. LC-MS; R, = 0.89; ES-: 622.34.
Example 632
{rac.)-{lR*, 55*)-3-Acetyi-7-{4-[3-(2-bromo-5-fluoropUenoxy)ethyilplienyl}-
3,9-dia2abicyclo[3.3.1Jnon-6-ene-6-carbox>lic acid (2-chlorobeaz\l)-
cyclopropylamide
Synthesized according to typical procedures H and E firomi bicyclonoucue AJl and (2-chlorobenzyl)cycIopropylamine. The title compound was purified by FC. LC-MS; Ri - 4.17; ES+: 666.07.
Example 633
(rac)~(ljR*, 55*)-3-Acefyl-7-{4-[3-(2-chlorophenoxy)propyI]pheDyl}-3,9-
diazabicyclol3.3.1]non-6-ene-5-carbosy-lic acid {2-chlorobenzyI)cyclopropyl-amide formate salt
Synthesized according to typical procedures H and E from bicyclononene T2 and (2-chloroben2yl)cyclopropylamine. LC-MS: Rt= 0.92; ES+: 617.94.
Example 634
(rac.)-{lR*, J^*)-3-Acetyl-7-{4-|3-(2-chIorophenoxy)propyl]phenyl}-3,9-
diazabicyclo(3.3.1|aon-6~ene-6-carboxyUc acid [2-(4-metlioxyphenoxy)ethyl]-methylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene T2 and cyciopropyl-[2-(4-methoxyphenoxy)ethyl]amine. LC-MS: R, = 0.S4; ES+: 618.03.

Example 635
(rac.)-{lR*y 55*)-3-Acetyl-7-(4-[3-(2-chlQroplienoxy)propyllpIieDyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carbox>"lic acid mcthyl-(3-trifluorometbyl-benzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene T2 and cyclopropyI-(3-trifluoromethylbenzyi)aniine. LC-MS: Rf = 0.89; ES+: 626.06.
Hlxainple 636 -
{rac)-^R*, 55*)-3-Acetyl-7-(443-(2-chlorophenoxy)propyl]phenyl}-3,9-
diaza-bicyclo [33.1 ]non-6-ene-6-carboxy lie acid (2-(3,4-dimethylplienoxy)-ethyljmethylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene T2 and cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]amine. LC-MS: Rt = 0.91; ES+; 616.13.
Example 637
(rac)-{lR*, 55'*)-3-Acetyl-7-{4-(3-(2-chloropbeao3y)propyIIphenyI}-3,9-
diazabicyclo{3J.l]aon-6-ene-6-carboxyUc acid (33-dimethosyben^l)methyl-amide formate salt
Synthesized according to typical ptoceduTes H and E from bicyciononeoe T2 and cyclopropyl-(3,5-dimethoxyben2yI)amine. LC-MS: R, = 0.84; ES+: 618.11.
Example 638

(rac.)-{JR% 5iy*)-3-AcetyI-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3,I]noQ-6-eDe-6-carbox7lic acid {2-chIorobenzyl)cyclopropyl-amide trifluoroacetate salt
Synthesized according to t\pical procedures H and \l from bicyclononene AJ2 and (2-chlorobenzyl)cyc]opropyIamine. LC-MS: R, - 1.00: ES^; 638.14.
Example 639
{rat. )-(/i?*,55*)-3-AcetyI-7-{4-[3-(3-fluorophenoxy)propyIlpheayl}-3,9-diaza-bicytio[3.3.ijuOB-u-t:iie-6-tarboxyIic acid (2-chlorobenzyl)cycIopropyIamide trifluoroacetate salt
Synthesized according to typical procedures H and E from bicyclononene AJ3 and (2^hlorobenzyl)cycIopropylamine. LC-MS: R, = 0.99; ES+: 638.14.
Example 640
(rac.)-(JJ{*, 55*)-5-[7-{4-[2-(2-Bromo-5-fluoropheDoxy)ethyIiphenyl}-6-
(methylphenethyIcarbamoyI)-3,9-diazabicydo [3.3.1 lnon-6-en-3-yI]-2,2-dimethyl-5-oxo-pentanoic acid trifluoroacetate salt
Synthesized according to typical procedures K and E from bicyclononene ALl and 3,3-dimethyldihydropyran-2,6-dione. LC-MS: Rt = 0.95; ES+; 710.13.
Example 641
(rac.)-{IR*, 55>3-Acetyl-7-{4-[3-(2-chlorDphenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid (2-chlorobeiizyl)isopropyl-amide trifluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononene T2 and
(2-ch!orobenzyl)isopropylamine. LC-MS; Rt= 1.03; ES+; 620.20.
Example 642
{rac.)-{lR% 55*)-3-Acetyl-7-{4-|3-(23,6-trichlorophenoxy)ethyllphenyl>-3,9-diazabicyclo[3.3.1]non-6-eiie-^-carbos:j'Uc acid methyl phenethylamlde trifluoroacetate salt
Synthesized according to typical procedures F and E from bicyclononene U2 and 2,3,6-trichJorophenol. LC-MS: R( = l.OU; JiS+: 6ZD.99.
Example 643
{racy{lR*, 55*)-3-AcetyI-7-{4-I3-(2-chloropheiioxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chIorobeiizyI)ethyIamide formate salt
Synthesized according to typical procedures H and E from bicyclononene T2 and (2-chlorobenzyl)ethyIamine. LC-MS: Rt = 0.89; ES+: 606.07.
Example 644
{racWR*> 55*)-3-Acetyl-7-{4-[2-(3,4-dichlQrophenoxy)ethoxylpheiiylJ-3,9-diazabicyclot3.3.1]noii-6-cne-6-carboxyUc acid methylphenethylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene XJ4 and 3,4-dichlorophenol. LC-MS: R, = 0.86; ES+: 608.01.
Example 645

(rac.y{lR% 55*)-3-Acefyl-7-{4-[2-(2-chloro-4,5-dimethyIphenoxy)ethox>-I-phenyI}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxjIic acid methylpfaenethyl-amidie formate salt
5 Synthesized according to typical procedures F and E from bicyclononene U4 and 2-chloro-4,5-dimethylphenol. LC-MS: R, = 0.87; £5+: 602.07,

}

Example 646
(racH^R*, 55*)-3-Acetyl-7-{4-[3-(2-chIoropbenoxy)propyiIphcnyl}-3,9-
diazabicyclo[3.3.11non-6-eue-ii-t;arb9AyIic acid (2-culoroben2yI)methyIamide formate salt
Synthesized according to typical procedures F and E from bicyclononene T2 and (2-chlorobenzyl)methylamine. LC-MS: R,= 0.87; ES+: 591.99.
Example 647
(rac.)-(lR*, 5,S*)-3-IVIethyl-7-{4-[3-(23,6-trifluorophenoxy)propyi]phenyI}-
3,9-diazabicyclo[3.3.1]Don-6-ene-6-carboxylic acid (2-chIorobenzyI)-
cyctopropylaraide formate salt
A mixture of bicyclononene AL2 (1 eq.), DIPEA (3 eq.) and methyl iodide (10 eq.) in CH2CI2 was stirred at rt overnight. The solvents were removed under reduced pressure and the residue treated according to typical procedure E. LC-
]vIS:R,-0.89; ES+: 610.32.
Example 648
(mc.)-(ii?*, 55*)-3-Ethyl-7-{4-(3-(2,3,6-trifluorophcnoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxjIic acid (2-ehIorobenzyl)cyclopropyl-amide formate salt

A mixture of bicyclononene AL2 (1 eq,), DIPEA (3 eq.) and ethyl iodide (10 eq.) in CHjCb was stirred at rt overnight. The solvents were removed under reduced pressure and the residue treated according to typical procedure E. LC-MS: Rt = 0.91; ES+: 624.33.
Example 649
(rac.)-(lK*, 55*)-3-(2-Amino acetyl)-?-{4-[3-(2,3,6-trifluo rophcnoxy)propy I]-phenyI}-3,9-dia2abicydo [3.3.1 ]non-6-ene-6-carboxylie acid (2-chlorobenzyI)-cyclopropylamide formate salt
Synthesized according to typical procedures G, L and E from bicyclononene AL2 and Boc-glycine. LC-MS: R, = O.SO; ES+: 653.32.
Example 650
(rac)-(ii?* 55*)-3-(3-AminopropioQyl)-7-{4-[3-(2^,6-trifluorophenoxy)-
propyI]phenyl}-3,9-diazabicyclo 13.3.1 Jnon-6-ene-6-carboxylic acid (2-chlorobenzyl)cyclopropylamide formate salt
Synthesized according to typical procedures G, L and E from bicyclononene AL2 andBoc-p-alanine. LC-MS*. Ri= 0.80; ES-*-. 667.32.
I^xample 651
(rac.)-(lJi*, 55'*V3-(5-MorphoIin-4-yl-5-oxopeotanoyI)-7-{4-[3-(2,3,6-
trif]uorophenoxy)propyl]phenyl}-3,9-diazabicyelo{3.3.1Inon-6-ene-6-carbo-lyiic acid {2-chlorobenzyl)cyclopropylainide formate salt

Synthesized according to typical procedure H, from bicyclononene AL2 and glutaric anhydride, then according to typical procedure K and E from morpholine. LC-MS:R,-0.89; ES+: 779.31.
Example 652
{rac.)-(JS*, 5^*)-3-(2-Tetrazol-l-ylacetyl)-7-{4-[3-(2,3,6-trmuorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[33,llttou-6-eoe-6-carboxylic acid (2-chloro-beiizyi)cyclopropyIainide formate salt
Synthesized according to typical procedures G and E L:or^ bicyclononene AL2 and (5//-tetrazol-5-yl)acetic acid. LC-MS: R, = 0.91; ES+: 706.23.
Example 653
{rac.)-{iR*, 5S*)-3-(5-Oxo-5-piperazin-l-ylpentanoy0-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]plienyl}-3,9-diazabicyclo[33.1]non-6-ene-6-carboxyIic acid (2-chlorobeii2yI)cyclopropylamide formate salt
Synthesized according to typical procedure H, from bicyclononene AL2 and glutaric anhydride, then according to typical procedure K, L and E from Boc-piperazine. LC-MS: R| = 0.78; ES+: 778.37.
Example 654
l:l-Mixture of (IR, 55)-3-((25)-2-ammo-3-hydroxypropionyI)-7-{4-[3-(2,3,6-trifluoropheaoxy)propyl]phenyl}-3»9-dia2abicyclo[3.3.11non-6-ene-6-carbo-xyiic acid (2-chIorobeiizyl)cycIopropylamide formate salt and (IS, 5R)-3-((2iS)-2-amino-3-hydroxypropionyl)-7-{4-|3-{2,3,6-trifluorophenoxy)propyI]-phenylJ-3,9-diaza-bicyclo[3.3.1]noQ-6-ene-6-carboxylic acid (2-cblorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures G^ L and E from bicyclononene AL2 and BoG-serine. LC-MS: R, = 0.79; ES+: 68334.
Example 655
Ill-Mixture of (IR, 55)-3-((25)-2-aminopropionyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyI]phenyI}-3,9-diazabicyclo[33.11non-6-ene-6-carboxyIic acid (2-chIorobenzyI)cyclopropylainide formate salt and (IS, 5R)-3-({2S)~2--aminopropionyI)-7-{4-[3-(23t6-trifluorophenosy)propyllphenyI}-3,9-diaza-bicycIo[3.3.11non-6-ene-6-carboxylic acid (2-chIorobenzyl)cycIop ropy lam ide formate salt
Synthesized according to typical procediires G, L and E from bicyclononene AL2 and Boc-alanine. LC-MS: R, = O.80; ES+-. 667.32.
Example 656
{rac)-{lR*, 55*)-3-AcetyI-7-{4-(2-(2,6-dicbioro-4-methylphenoxy)ethoxyl-phenyI}-3,9-diazabicyclo[3.3.1Jnon-6-eoe-6-carboxyiic acid cyclop ropyl-{2^-dichlorobenzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN4 and (23-dichloroben2yl)cyclopropylanune. LC-MS: Rt= 0.96; ES+: 702.09.
Example 657
{rac)-{lR*, 55'*)-3-AcetyI-7-{4-[2-(2,6-dichloro-4-fflethyIphenoxy)efhoxy]-phenyI}-3,9-diaz:abicycIo[3.3.1Jnon-6-ene-6-carboryIic acid cycIopropyI-(2,3-dimetbylbeozyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN4 and cyclQprQpyK2,3-dimethylbenzyl)amine. LC-MS: R, = 0.94; ES+: 662.27.

Example 658
(rac.)~(JJt*, 5^*)-3-Acet>'l-7-{4-i2-(2,6-dicliIoro-4-methy|phcnoxy)ethoX}'I-pbenyl)-3,9-diazabicyclo[3.3.1]non-6-cne-6-carboxylic acid (2-chloro-3-trinuoi-oinethyl-benzj'l)cyc[opropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN4 and (2-chloro-3-trifIuoromethylbenzyl)cyclopropylamine. LC-MS: R[ = 0.96; ES+: 736.08.
Example 659
(rac,}-(JR% 5^*)-3-AcetyI-7'{4-[2-(2,6-dichloro-4-methylpheDOxy)ethoxy]-pheHyI}-3,9-diazabicycloJ3.3.11non-6-€ne-6-carboxyHc acid (2~broinobenzyl)-cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN4 and (2-bromobenzyl)cyclopropylaniine. LC-MS: Ri == 0.92; ES-H: 682.20.
Example 660
irac.)-(JIt*, 55*)-3-Acetyl-7-{4-[2-(2,6-dichIoro-4-raethylphenoxy)ethoxyl-phenyl}-3,9-dia2abicyclo(33.1]non-6-ene-6-carboxyIic acid (2~chIorobenzyl)-cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN4 and (2-ch]orobenzyl)cyclopropylamine. LC-MS: Rt = 0.93; ES+: 668.20.
Example 661

{rac.y{lR\ 5,S")-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyI}-3,9-diaEabicycio[3.3.1|non-6-ene-6-carboxyUc acid (2-cIiIorobenzyl)-etfaylamjde formate salt
Synthesized according to typical procedures H and E &om bicyclononene BN4 and (2-chlorobenzyl)ethylamine. LC-MS: Rt = 0.93; ES+: 656.20.
Example 662
{rac.y(lR*, 54*)-3-AcefyI-7-{4-[2-{2,6-dichloro-4-methyIpheB0xy)ethoxy]-phenyI}-3,9-diaza-^ii.>v;lo[3.5.1juou-6-eiic-u-carboxylic acid (6-chlorobenzo-[l,3]dioxol-5-yImethyl)cyclopropyIamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN4 and (6-chIoroben2o[l,3]dioxoI-5-ylmethyl)cyclopropylaniine. LC-MS: Rt = 0.93;
ES+: 712.15.
Example 663
{racyilR*, 5^*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methyIphenoxy)ethoxy]-phenyl}-3,9-diaza-bicyclo(3.3.1]non-6-ene-6-carboiylic acid cyclopropyI-(3^-dimethoxybenzyl)aiiude formate salt
Synthesized according to typical procedures H and E firom bicyclononene BN4 and cyclopropyl-(3,5-dimethoxybenzyI)amine. LC-MS: R, = 0.92; ES+: 694.20.
Example 664
(rac.y{lR*, 55*)-3-Acetyl-7-{4-(2-{2,6-dicliloro-4-methyIphenoxy)ethoxyj-phenyl}-3,9-diazabicyclo[3.3.1lDon-6-eDe-6-carboxylic acid cyclopropyi-(3-methoxybenzyl)aniide formate salt

Synthesized according to typical procedures H and E from bicyclononene BN4 and cyclopropyl-{3-methoxybenz>'l)amine. LC-MS: R, = 0.91: ES+: 664.25.
Example 665
{rac.y{lR*, 5^*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorDphenosj')ethoxy]phenyl)-3,9-diazabicyc[o[3.3.11non-6-ene-6-carboxyUc acid cyclop ropy I-(2,3-dichloro-benz\i)ainide formate salt
Synthesized according to typical procedures H and E from bicyclononene BNIO and cyclopropyI-(2,3-dichlofoben^;'Vdini,^«: XC-IvfS: R, = 0.92; ES+: 672.22.
Example 666
irac.)~{lR*, J.S'*)-3-Acetyl-7-(4-[2-(2-chIoro-5-fIuorophenosy)ethoxy]phenyl}-3,9-diazabicycIo[3.3,llQon-6-eQe-6-carboxyIic acid (2-ch[oro-3-trifluoro-metiiyibenzyi)cyclopropy]amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BNIO and (2-chloro-3-trifluoromethyIbenzyl)cyclopropylamine. LC-MS; R( = 0.93; ES+: 706.09.
Example 667
{rac.y{lR*, 55'*)-3-Acetyl-7-{4-[2-(2,6-dicfaloro-4-iaethyIphenQxy)ethoxyi-phenyI}-3,9-diazabicyclo[3.3.11aon-6-ene-6-carboxyUc acid (3-chlorobeQ2yl)-cycIopropy\amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN4 and (3-chlorobenzyl)cyclopTopy\amine. LC-MS'. Ri = 0.93; ES+: 66S.2L
Example 668

{raa)-{lR*, 55*)-3-Acefyl-7-{4-[2-{2,6-dichloro-4-methyIphenoxy)ethoxy]-pfaenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxjiic acid cyclop ropy l-(3-methylbenzyl)aniide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN4 and cyclopropyi-(3-methylbenzyl)amine. LC-MS: R, = 0.93; ES+; 648.23.
Example 669
(rac.y{JR*, 5.5*)-3-Acetyl-7"(4-12-(2,6-dicliloro-4-meihyipiit;uoxy)eiaosy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carbosylic acid cyclopropyH2-fluoro-5-methoxybeazyl)amide forpiate salt
Synthesized according to typical procedures H and E from bicyclononene BN4 and cyclopropyU(2-fluoro-5-methoxybeiizyl)amine. LC-MS: Rt = 0.92; ES+: 682.20.
Example 670
{racy(lR*, 55*)-3-AcetyI-7-{4-I2-(2-chloro-4,5-dimethylphenoxy)-
ethoxy]phenyl}-3,9-diazabicyclo[33.1]non-6-ene-6-carboiyIic acid
cyclopropyl-(23-dicbIorobeiizyI)aiaide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN3 and cyclopropyl-(2,3-dichlorobenzyl)amine. LC-MS: Rt = 0.95.; ES+: 684.20.
Example 671
(rnc.)-(i/(* 55*)-3-AcetyI-7-{4-[3-(2-chloro-3,6-difluorophenoxy)propyl]-
phenyI}-3,9-diazabicyclo[3.3.1]noD-6-ene-6-carboxylic acid (2-chloroben2yl)-cy clop ropy lamide formate salt

S\-nthesized according to typical procedures F and E from bicyclononene BBl and 2-chloro-3,6-difluorophenol. LC-MS: R, = 0.93.; ES+: 654.2S.
Example 672
(rac.)-{IR*, 5^*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dim€thylphenoxy)ethoxy]-phedyl}-3,9-diazabicyclop.3.11non-6-ene-6-carboxylic acid (2-chloro-3-trilluoromethylbenzyl)cyclopropylamide formate salt
SynthesiMd according to typical procedures H aad L clgnoriene liNS
and (2-chloro-3-trifluoromethylben2yl)cyclopropylamine. LC-MS: Rt = 0.96; ES+: 716.18.
Example 673
(racHiR*, 55'*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-aiethylphettoxy)ethoxyl-phenyI}-3,9-dia2abicyclo[3.3.l]noa-6-ene-6-carboxylic acid cyclopropyI-(3,4-ditnethoxybenzyl)ainide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN4 andcyclopropyl-(3,4-dimethoxybenzyl)anmie. LC-MS: Rt = 0.89; ES+: 694.23.
Example 674
(racy-ilR*, 55'*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methyIphenoxy}ethoxy]-phenyl}-3,9-diazabicyclop.3.1]non-6-ene-6-carboxylic acid cycIopropyl-(3-triflnoromethoxybenzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN4 and cyclopropyl-(3-trifluoromethoxybenzyi)amine. LC-MS: Rt " 0.95; ES+: 718.13.

Example 675
irac.)-(JR% J5*)-3-Acetyl-7-{4-[2-(2,-(,5-trichIorophenoxy)ethoxylphenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyiic acid (2-chIoro-3-trifluoro-niethylbenzyl)cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN9 and (2-chloro-34rifluoromethylbenzyl)cyclopropylamine. LC-MS: Rt = 0.97; ES+: 758.08.
Example 676
(r(ic)-(iV?* 55*)-3-Acetyl-7-{4-[2-(2,4,5-trichIorophenoxy)ethoxylphenyl}-3,9-diazabicyclo-(3.3.11nofl-6-ene-6-carboxyUc acid cycIopropyH^^-dichlorobenzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN9 and cyclopropyl-(2,3-dichlorobenzyl)amine. LC-MS: Rt = 0.96; ES+; 724.02.
Example 677
{rac)-(lM*, 55'*>3-Acetyl-7-{4-[2-(2^-dichl6rophenoxy)etlioxyIpIienyl}-3,9-diazabicycIo[3J.llDan-6-eDe-6-carboxylic acid cyclopropyI-(2^-dlmethyl-beiizyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN5
and cyclopropy]-(2,3-dimethylbenzyl)amine, LC-MS; R, = 0.92; ES+: 648.25.
Example 678

(rac.}-(JR*, 5i'*)-3-Acetyl-7-{4-[2-(2,4,5-trichloropheno\7)ethoxy]phenyl}-
3,9-diazabicydo-[3.3.1Inon-6-ene-6-carboxyIic acid cycIopropyH2,3-
dimethylhenzyl)amide formate salt
S>Tithesized according to typical procedures H and E from bicyclononene BN9 and cyclopropyl(23-dimethylbenz>-l)am5ne. LC-MS: R,= 0.95; ES+: 684.12.
Example 679
(rac,)-(JR% 55*>3-Acefyl-7-{4-[2-(2-chlorD-4,5-dimethylpbenoxy)ethoxy]-phcnyl}-3,9-di;;2abicyclo[3.3.1}non-6-eQc-6-carboxyIic acid cyclopropyl (2,3-diniethylbeazyl)ainide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN3 and cyclopropyl-(2,3-dinietiiyIbenzyl)amine. LC-MS: Rt = 0.94; ES+; 642.31-
Example 6S0
{racyilR*, 55*)-3-Acetyl-7-(4-I2-{2-bromo-5-fluorophenoiy)ethoxyJphei)yI}-
3,9-diaza-bicycIo(3.3.1]non-6-eoe-6-carboxyIic acid cyclopropyI-{2,3-
dichtorobenzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN2 and cyclopropyl-(2,3-dichlorobenzyl)aniine. LC-MS: Rt = 0.92; ES+: 718.05.
Example 681
{rac.y{lR*, 5S*)-3-Acetyl-7-{4-[2-(2-cWoro-4,5-dimethylphenoxy)ethoxyl-phenyI}-3,9-dia2a-bicyclo[3.3.1]non-6-ene-6-carboxyIic acid (2-bromobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedxires H and E &om bicyclononene BN3 and (2-bromobenzy!)cyciopropylamine. LC-MS: R, = 0.94; ES+; 694.15.
Example 682
(rac.)-ilR% 55*)-3-Acefyl-7-{4-[2-(23-dichIorophenoxy)ethoxy]phenyl}-3,9-
diazabicyclo{3.3.11non-6-ene-6-carbosyIic acid cyclopropyl-(2,3-
dichIorobenzyl)amide formate sah
Synthesized according to typical procedures H and E from bicyclononene BN5 and cyclopropyi-i^z,J-aicmorobenzyl)amin6. LC-MS: Rt = 0.93; ES+: 690.06.
Example 683
{rac)-(lR*, 55*)-3-Acetyl-7-(4-[2- 3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyUc acid cyclopropyl-(2^-
dimethylbenzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BNIO and cyclopropyI-(2,3-dimethylben2yl)amine. LC-MS: R, = 0.91; ES+: 632.31.
Example 684
{rac.}-{JR% 55*)-3-AcetyI-7-{4-[2-(2,4,5-trichlorophenoiy)ethoxy]phenyl}-
3^-dia2abicycIo[33.1|non-6-eae-6-carboxyIic acid (2-chlorobenzyl)-
cyclopropylamide formate salt
Synthesized according to typical procedures H and E ftom bicyclononene BN9 and (2-chIorobenzyl)cyclopropyIamine. LC-MS: Rt = 0.94; ES+: 690.07.
Example 685
{rac.)-ilR*, 5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fiuorophenoxy)ethoxy]phenyi}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid (2-chIoro-3-trifluoro-nie(hylbenzyi) cyclop ropy laniidc formate salt
Smthesized according to typical procedures H and E from bicyclononene BN2 and (2-chIoro-3-trifluoromethyIbenzyl)cycIopropyiamine. LC-MS: R, = 0.93; ES+-. 752.06.
Example 686
{rac.y{lR*, 'J5*)-3-Acety;-7-{4-|i-(S,4^j-trichIorophenoxy)efhoxyIphcnyl}-3,9-diazabicycIo-[3.3.1]noi)-6-ene-6-carboxylic acid (2-bromobenzyI)-cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN9 and (2-bromobenzyI)cyc[opropylamine. LC-MS: R, = 0-95; ES+: 733.99.
Example 687
(rac)-(lR* 5S*)-3-Acetyl-7-{4-(2-(2-broino-5-fluorophenosy)ethoxylphenyI}-3,9-diazabicycIo[33.1]non-6-enfr-6-carboxylicacidcyclopropyl-{23-dijnethyl-beiizyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN2 and cyclopropyl-(2,3-dimethylben2yI}amine. LC-MS: Rt = 0.91; ES+: 678.22.
Example 6S8
{rac.)-{iR*y 55'*)-3-Acetyl-7-{4-[2-{2,3-dichlorQphenQxy)ethoxylphenyl}-3,9-diazabicyclo[3.3.1]non-6-eDe-6-carboxylic acid (2-chloro-3-trifluoroinethyl-benzyOcycIopropylamide forraate salt

Synthesized according to typical procedures H and E from bicyclononene BN5 and (2-chloro-3-trifluoromethylbenzyl)cyclopropyIamine. LC-MS: Rt = 0.94; ES+; 724.13.
Example 689
irac.)-{lR*, 55*)-3-AcetyI-7-{4-[2-{2-chloro-4,5-dimethyIphenoxj')ethoxy]-pheay!}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid (3-chlorobenzyl)-cyclopropylamide formate salt
Synthesized according to typical proceduiet, M and E from iiicyclcnsnene BN3 and (3-chJorobenzyl)cyclopropylamine. LC-MS: Rt = 0.93; ES+: 648.26.
Example 690
(rac)-(lR*, 55*)-3~Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)etIioxy]phenyi}-3,9-diazabicyclo[3.3.1]noo-6-ene-6-carboxylic acid (2-chlorobeiizyl)ethyl-amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN9 and (2-chlorobenzyI)ethylamine. LC-MS: R, = 0.94; ES+-. 678.12.
Example 691
{rac.)-{JR*, J5*)-3-Acetyl-7-{4-[2-(2-chloro-5-nuorophenoxy)ethoxylplienyl}-3,9-diazabicyclo[33.1]non-6-ene-6-carboxyIic acid (2-bromobenzyl)cyclo-propylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BNlO and(2-bromobenzy!)cyclopropylamine. LC-MS: R,= 0.90; ES+: 684.11.
Example 692

{rac,y{JR\ 5,S*)-3-Acetyl-7-{4-[2-(4-chioro-2-meth>lphenox>)ethoxyI-
phenyl}-3,9'diazabicyclo(3.3.1]non-6-eue-6-carboxyUc acid cyclop ropy (-{2,3-dichlorobenzyl)ainide formate salt
Syntliesized according to typical procedures H and E &om bicyclononene BN7 and cyclopropy]-(2,3-dichlorobenz;-l)amine. LC-MS: Rt = 0.9-f; ES+: 670.17
Example 693
{rac)-(lR*, 55*V3-Acetyi-7-{4-[2-(2-chloro 4^-dt^ct:;ylphcnoiy)ethoxy]-phenyl}-3,9-diazabicydo[3.3.1]noii-6-ene-6-carboxyHc acid cyclopropyl-(3-niethoxybenzyI)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN3 andcyclopropyl-(3-metlioxyben2yl)amine. LC-MS: R, = 0.91; ES+; 644.32.
Example 694
{racy{lR*, J5*)-3-Acetyl-7-{4-{2-(2-bromo-5-nuoropheaoxy)ethoiy]-
phenyl}-3,9-diazabicyclo[3.3.1)non-6-ene-6-carboa[yUc acid (2-bromobenzyl)-cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN2 and cyclopropyl(2-bromobenzyl)amme. LC-MS: Rt = 0.91; ES+: 728.04.
Example 695
{rac.y{lR*, 5S *)-3-Acety 1-7-{4-12-(4-ch;or o-2-methy lphcnosy)ethoxy 1-
phcnyI)-3,9-dia2abicyclo[3.3.11non-6-ene-6-carboxylic acid cyclopropyl-(2,3-dimethylbenzyl)amide formale salt

Synthesized according to typical procedures H and E from bicyclononene BN7 and cyclopropy!(2,3-dimethyiben2yl)amine. LC-MS: R, = 0.93; ES+; 628.30.
Example 696
irac.)-{IR*, 55*)-3-AcetyI'7-{4-(2-(2,4,5-trichlorophenoxy)ethoxy]pheDyl}-3,9-diaza bicycle [33. l]iioii-6-ene-6-carboxyIic acid cyclopropyi-(3-methosy-benzyl)ainide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN9 axid cyJopropyi-(3-methoxyben2yl)amine. LC-MS: Rt = 0.92; ES+: 686:i4.
Example 697
(rac.)-(JR*, 55*)-3-Acetyi-7-{4-[2- Synthesized according to typical procedures H and E fi-om bicyclononene BN3 and cyclopropyi-(2-fluoro-5-methoxybenzyl)aniine. LC-MS: R( = 0.91; ES+: 662.29.
Example 698
(racyilR*, 55*)-3-AcetyI-7-{4-[2-(4-chIoro-2-metfayIphenoxy)ethoxyl-
phenyI)-3,9-diazabicyclo[3.3.11non-6-ene-6-carboxylic acid (2-bromobenzyl)-cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN7 and (2'bromoben2yl)cyclopTopylamine. LC-MS; R, = 0.93; ES+: 680.15.
Example 699

(rac)-(JR% 55*)-3-AcetyI-7-{4-[2-(2-chloro-5-fluorophenoxy)ethox}^]phcnyl}-
3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyfic acid (2-chlorobenzyI)-
cyclopropylamide formate salt
SjTithesized according to typical procedures H and E from bicyclononene BNIO and (2-chlorobenzyl)cyclopropylaraine. LC-MS: Rt = 0.90; ES+: 638.22.
Example 700
(iUc.riJR-, 5Ly*)-3-Acetj'l-7-{4-[2-{2,4,5-tricblorophenoxy)ethoxjJplie. 3,9-diazabicyclo[3.3.11iion-6-ene-6-carboxylic acid cyclopropyl-(3,5-
dimethoxybenzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN9 andcyclopropyl-(3,5-dimethQsybenzyI)ainine. LC-MS; R,= 0.93; ES+; 716.14.
Example 701
(racXiit*, 55*)-3-Acetyl-7-{4-[2-(23-dichlQropheaoxy)ethoxylpheiiyli-3,9-diazabicyclol3.3.11non-6-ene-6-carboxyUc acid (2-bromobenzyl)cycloprQpyl-amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN5 and (2-bromobensyl)cyclopropylamine. LC-MS: Rt= 0.91; ES+: 700.07.
Example 702
(racyilR*. 55*)-3-Acetyl-7-{4-12-(2-chloro-4,5-dimethylpheooxy)ethoxyl-pbenyl}-3,9-diazabicyclol3.3.11oon-6-ene-6-carboxylic acid {6-chloro-benzoIl,3]dioxol-5-yImethyI)-cyclopropylainide formate salt

Synthesized according to typical procedures H and E from bicyclononene BN3 and (6-chlorobenzo[;i,3]dioxoI-5-ylmethyl)cycIopropylamine. LC-MS: Ri = 0.93; ES+: 694.17.
Example 703
(rac.)-(lR*, 55*)-3-Acetyl-7-{4-[2-(2,3-dicIilorophenoxy)ethoxylphenyl}-3,9-diazabicycIo[3.3.1]non-6-eDe-6-carboxylic acid (2-chloroben2yl)cycIopropyI-amide formate salt
Synthesized" accuiiilug i.^ topical procediu-es H and E from bicyclononene BN5 and (2-chlorobenzyi)cyclopropylamine. LC-MS: Rt = 0.91; ES+: 656.19.
Example 704
{rac)-{}S*, 5S*)-3-Acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-
pbeoyI}-3,9-diazabicycIo[3J.l]non-6-ene-6-carboxyIic acid (2-cbIoro-3-trifluoromeffayIbenzyl)cycIopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN7 and (2-ctiloro-3-tiifiuoiometh.ylben2yi)c>clopropylaniine. LC-MS: Rt = 0.95; ES+: 702.17.
Example 705
{rac.)-{lR*, 5.S'*)-3-Acetyl-7-{4-[2-(2-cIiloro-4^-dimethylplienoxy)ethoxyl-phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cycIopropyH3-methylbenzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN3 and cycIopropyl-(3-methylbenzyl)ainine. LC-MS: Rt = 0.92; ES+; 628.32.

Example 706
(rac.yiJR% 5^*)-3-Acetyl-7-{4-(2-(2,3-dichIorophenox>)ethoxylphenyI}-3,9-diazabicyclo[3.3.1]noa-6-cDe-6-cinboAylic acid (2-chlorobenzyl)ethylamide formate salt
Synthesized according to typical procediu-es H and E irom bicyclononene BN5 and (2-clilorobenzyl}etiiy[amine. LC-MS: Rt = 0.90; ES+; 642.19.
Example 707
{rcic.)-(lR*, 55*)-3-Acetyl-7-{4-l2-(2-chloro-5-fluorophenoxy)ethoxylphenyl}-3,9-diazabicyclo[3.3.11non-6-ene-6-carboxyIic acid cyclopropyl-(2-fluoro-5-methosybenzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BNIO and cyclopropyl-{2-fluoro-5-methoxybenzyl)amiiie. LC-MS: Ri = 0.88; ES+: 652.26.
Example 708
(rac.)-(lR% 5.y*)-3-Acetyl-7-{4-[2-(4-chloro-2-mcthyiphenoxy)ethoxyI-
phenyI}-3,9-diazabicyclo[33.1]non-6-ene-6-carboxylic acid (2-chIorobenzyI)-cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN7 and cyclopropyI(2-chlorobenzyl)amine. LC-MS: Rt = 0.92; ES+: 634.22.
Example 709

{rac.)-(}R*, 55*)-3-Acetyl"7-{4-12-(2-bromo-5-fluorophenoxy)ethoxy]-
phenyI}-3,9-diazabicycJo(3.3,llnon-6-ene-6-carboxyiic acid cycIopropyl-(3,5-dimethoxyben2yI)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN2 andcycIopcopyi-(3,5-dimethoxybenzyl)amine. LC-MS: Rt= 0.88; ES+: 708.14-
Esample 710
irac.}-{lR*, 5S*)-3-Acetyi-7-{4-(2-(2-cfaloro-5-fluorophenoxy)ethoxyl-
phenyl}-3,9-diazabicycIo[3.3.1]oon-t-Cu^-6-caiuOxyIiL- aciii cycIopropyI-(3-methoxyben2yl)amide formate salt
SjTithesized according to typical procedures H and E feom bicyclononene BNlO and cyclopropyl-(3-raethoxyben2yl)amine, LC-MS: Rt = 0.87; ES+: 634.27.
Example 711
irac)-{lR*, 5i9*)~3-Acetyl-7-{4-[2-(2,4,5-frichIoropbeDOx)')ethoxy]phenyl}-
3^-diazabicyclo[33.1]noD-6-ene-6-carbosyUc acid (3-cfaloroben2yI)-
cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN9 and (3-chIoroben2yI)cyclopropylamine. LC-MS: Rt = 0.94; ES+: 690.09.
Example 712
{rac.y{iR*, 5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy-ethoxy}-phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxyIic acid cyclop ropy I-(3,5-difluorobenzyl) amide formate salt

Synthesized according to typical procedures H and E from bicyciononene BN4 and c\-clopropyl-(3,5-difluorobeii2yl)amine. LC-MS: Ri = 0.93; ES+; 670.22.
Example 713
{racy^R", 55*)-3-Acetjl-7-{4-[2-(2,4,5-tricUIorophenoxy)ethox>'lph€nyll-3,9-diazabicyclo[33.1]non-6-ene-6-carboxy]ic acid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyciononene BN9 and cyclopropyJ-(2-fluoro-5-methoxyl-'fr>,:yl)ainine. IC-A-^S: Ri ^ 0.93; ES+; 7Q2.40.
Example 714
{rac.y{lR*, 55*)-3-Acetyi-7-{4-I2-(2,4,5-trichloropheiioxy)ethoxy]phenyl}-
3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,4-
dimetho3£ybeiizyI)amide formate salt
Synthesized according to typical procedures H and E from bicyciononene BN9 and cycIopropyl-(3,4-dimethoxyben2yl)araine. LC-MS: Ri= 0.90; ES+: 716.10.
Example 715
iracy{lR*, 55*)-3-AcetyI-7-{4-[2-(2-chloro-5-fiuorophenoxy)ethosy]phenyl}-3,9-dia2abicycIo[3.3.1inon-6-ene-6-carboxyIic acid (6-cfaIoro-benzo[l,31-dioxol-5-ylmethyl)cycIopropylamide formate salt
Synthesized according to typical procedures H and E from bicyciononene BNIO and (6-chlorobenzo[!,3Jdioxol-5-ylmethyl)cyclopropylamine. LC-MS: Rt = 0.90'., ES+; 684.19.

Example 716
(rac.)'(JS*, 5,S'*)-3-AcefyI-7-{4-[2'(2-bromo-5-fluorophenoxy)ethoxy]phenyl]-
3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid (3-chIorobenzyl)-
cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN2 and (3-ch]orobenzyl)cyclopropylamine. LC-MS: Rt = 0.90; ES+: 682.16.
Example 717
{rac.y{lR*, 5^*)-3-Acetyl-7-{4-[2-(2,3-dichIorophenoxy)ethoxy]pbeDyl}-3,9-diazabicycIo[3.3.I]non-6-ene-6-carboxyIic acid cyclopropyl-(3,4-dimethoxy-be[izyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN5 and cyclopropyH3,4-dimethoxybenzyl)amine. LC-MS: Rt = 0.97; ES+: 758.08.
Example 718
{rac)-{lR*, 55*)-3-AcetyI-7-{4-[2-(2-chIoro-5-fluorophenoxy)etho3ty]phenyl}-3,9-diazabicycloI3J.lJnon-6-ene-6-carboiyIic acid (2-chIorobenzyI)-ethylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BNIO and (2-chIorobenzyl)ethylamme. LC-MS: Rt = 0.»9; ES+: 626.25.
Example 719
(rac.)-(lS*, 5^*)-3-AcetyI-7-{4-[2-(4-chloro-2-methyIphenoxy)ethoxy!-
phenyl}-3,9-diazabicyclo(3.3.1lDon-6-ene-6-carboxyIic acid cyclopropyI-(3»5-dimethoxybenzyl)amide formate salt

Syntliesized according to typical procedures H and E from bicyciononene BN7 and cyclopropyl-(3,5-dimethoxybenzyI)arain6. LC-MS: R, = 0.90; ES+; 660.29.
Example 720
(rachUR*, 5S*)-3-Acetj^l-7-{4-[2-(2,4^-trichlorophenoxy)ethoxylphenyl}-3,9-diazab icy cio (3.3.1] non-6-ene-6-car boxy lie acid cyclopropyl-(3-inethyl-beiiz>i)amide formate salt
oynthesized according to typical procedures H and E from bicycloiiofifenfc BN9aiiu cyclopropyi-(3-methyIbenz>'I)amine. LC-MS: Rt = 0.94; ES+: 670.22.
Example 721
irac)-{lR% 55'*)-3-Acet>'l-7-{4-[2-(23-dichloropheaoiy)ethoxy]phenyl}-3,9-diazabicycIo[3J.l]non-6-ene-6-carboxyUc acid cyclopropyl-(2-fluoro-5-methoxybenzyI)amide formate salt
Synthesized according to typical procedures H and E from bicyciononene BN5 and cyclopropyl-(2-fluoro-5-methoxybenzyl)amine. LC-MS: Rt = 0.89; ES+: 668.25.
Example 722
{raayilR*, 55*)-3-Acetyl-7-{4-[2-(2-chloro-4^-dimethylpIienoxy)ethoxyl-pheQyl}-3,9-diazabicyclo(3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,5-difluorobenzyl)amide formate salt
I
Synthesized according to typical procedures H and E from bicyciononene BN3 and cyclopropyl-(3,5-difluorobeiizyl)amine. LC-MS: Rt = 0.92; ES4-: 650,23.

Example 723
{rac.HJR', 55*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl)-3,9-dia2abieyclo[3.3.1]non-6-ene-6-carboxyUc acid cyclopropyl-(3,5-dimetboxy-benzyl)ainide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN5 and cyclopropyI-(3,5-dimethoxyben2yl)amine. LC-MS: Rt = 0.89; ES+: 680.22.
Example 724
irac.y(]R*, 55*)-3-Acetyi-7-{4-[2-(2-chloro-5-fluorophenoiy)ethoxyl-
pheDyl}-3,9-diazabicydo[33.1]non-6-ene-6-carboxylic acid (2-cfalorobenzyI)~ cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BNIO and cyclopropyl(3-chlorobenzyl)amine. LC-MS: Rt = 0.90; ES+: 638.22.
Example 725
{rac.)-{lR*, 55 *)-3-Acetyl-7-{4-[2-{2-bromo-5-fluorophenoiy)ethoxyl-
phenyl}-3^-diazabicyclo [3.3.1] non-6-ene-6-carboxylic acid (2-chlorobeiizyl)-cyclopropylamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN2 and (2-chlorobenzyl)cyclopropylamine. LC-MS: R, = 0.90; ES+: 684.12.
Example 726
{rac.)-ilR*, 55*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-pheiiyl}-3,9-diazabicyclo(3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3,4-dimethoxybenzyl)amide formate salt

Srathesized according to typical procedures H and E from bicyclononene BN3 and cyclopTopyl-(3,4-dimethoxybenzyl)amine. LC-MS: R, = 0,88; ES+: 674.31.
Example 727
(rac.)-(lR*, 5i'*)-3-Acet}'[-7-(4-[2-(2-chloro-4,5-dimethy|pheiiosy)ethoxjl-phenylJ-3,9-diazabicyclo[3-3.11noii-6-ene-6-carboxylic acid cyclopropyl-(3-trifluoromethoxybenzyl)amide formate salt
Synissizci^ jcccidir.g to topical procedures H and E from bicyclononene BN3 and cyclopropyl-(3-trifluoromethoxybenzyl)amine. LC-MS: Ri = 0.95; ES+: 698.22.
Example 728
{rac.y{lR*, 5S*)-3-Acetyl-7-{4-(2'(2-chloro-5-fluoropbeniOxy)etboxylplieByl}-
3,9-diazabicyclol3.3.1]Don-6-ene-6-carboxylic acid cydopropyl-(3-
methylbeiizyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BNIO and cyclopropyI-(3-methylbenzyl)amine. LC-MS; Rt = 0.89; ES+: 618.28.
Example 729
(rac.)-ilR*, 55*)-3-AcetyI-7-{4-l2-(2-chloro-5-nuorophenosy)ethoxyJphenyl>-
3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid cyclopropyI-(3,S-
dimethoxybeD2yI)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BNIO and cyclopropyI-(3,5-dimethoxybeQzyl)amine. LC-MS: R, = 0.88; ES+: 664.27,

Example 730
{rac.y{lR*, 55*)-3-Acetyl-7-{4-(2-(2,3-dichlorophenoxy)ethoxyIphenyI}-3,9-diazabicycIo(3.3.1]non-6-ene-6-carboxylic acid cycIopropyl-(3-methyI-benzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN5 and cyclopropyl-(3-methylfaenzy])amine. LC-MS: Rt = 0.90; ES+: 634.21.
Example 731
{racy{lR*, 55'*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxyJpheoyl}-3,9-dia2abicyclo[33.1]noD-6-ene-6-carboxyIic acid cyclopropyl-(2-fluoro-5-metboxybenzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN2 and cyciopropyI-(2-fiuoro-5-methoxybenzyl)amine. LC-MS: Rt = 0.89; ES+: 696.14.
Example 732
(rac.y(lR*, 55*)-3-Acetyl-7-{4-I2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[33.1]non-6-ene-6-carboxylic acid (2-chlorobeiizyl)etbyl-amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN2 and (2-chlorobenzyl)ethylamine. LC-MS: Rt= 0.90; ES+: 672.14.
Example 733

ii-ac.y{lR*, 5;5'*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoiy)ethoxy|pheiiyl}-3,9-diazabicycIo[3.3.1]Don-6-ene-6-carboxyUc acid (6-chIorobenzo[l,3]dioxoI-5-ylmethyOcyciopropylamide formate salt
Synihesized according to typical procedures H and E from bicyclononene BN5 and (6-chIorobenzo[l,3]dioxol-5-ylnietliyl)cyclopropylamine. LC-MS: Ri = 0.91; ES+: 700.12.
Example 734
{rac.)-(lR*, 55 *)-3-Acetyl-?-i-i-[2-(A,3-uichlorophtu JAy)c.hoxyJphenyl)-3,9-diazabicycIo[3.3.1]noa-6-ene-6-carboxylic acid (3-chIoroben2yl)cyclopropyI-amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN5 and (3-chIorobenzyl)cyclopropylamine, LC-MS: Rj = 0.91; ES+: 656.19.
Example 735
[racHIR*, 55'*)-3-Acetyl-7-{4-[2-(4-chIoro-2-methyIphenoxy)ethoxyJ-
pheayl}-3,9-diazabicyclo[33.1]noa-6-ene-6-carboxylic acid (6-chIoro-beiiZQ[131dioxoL-5-ylmethyl)cyc!opropylamide formate salt
Synthesized according to typical procedures H and E from bicyciononene BN7 md (6-chlorobeozo[l,3}dioxol-5-ylmethyl)cyclopropylainine. LC-MS: Ri = 0.92; BS+: 678.20.
Example 736
rac.)-(lR*, 55*)-3-Acetyl-7-(4-(2-(2-bromo-5-fluorophenoxy)ethoxyJphenyl}-(,9-diazabicyclo[3.3.1]non-6-ene'6-carboxyIic acid cyclopropyl-(3-methoxy-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononene BN2 and cyclopropy[-(3-methoxybenzyl)amine. LC-MS: R, = 0.88; ES+; 678.20.
Example 737
(rac.)-(lR^ 55*)-3-AcetyI-7-{4-[2-(4-chloro-2-methyIphenoxy)ethoxy]-
phenyI}-3,9-diazabicycIo[3.3.1]iion-6-ene-6-carboxylic acid (2-chIorobenzyI)-ethylamide formate salt
Synthesized according to typical procedures H and E from biuycionouene BN7 and (2-chlorobenzyl)ethylaniine. LC-MS: Rt = 0.91; ES+: 622.26.
Example 738
(rac)-(JR*, 55*)-3-Acetyi-7-{4-[2-(4-cb!oro-2-metliyIphenoxy)ethoxy|-
phenyl}-3,9-dia2abicyclo [3.3.1] non-6-ene-6-carboiylic acid cyclopropyl-(3-methylbeQzyl)amide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN7 andcyclopropyl-(3-methylbenzyl)amine. LC-MS:Ri = 0.91;ES+: 614.32.
Example 739
(rac.)-(lR*, 55*)-3-Acety!-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclol3.3.1]noii-6-ene-€-carboxylic acid (6-chlorobenzo[131dioxol-S-ylmethyI)cyclopropyIamide formate salt
Synthesized according to typical procedures H and E from bicyclononene BN9 and (6-chiorobenzo[l,3]dioxol-5-yhnethyl)cyclopropyIamine. LC-MS: Ri = 0.94; ES+: 734.06.

{rac.yilR, 55)-7-{4-I3-(2,3,6-Trifluorophenoxj')pr()pylphenyl}-3,9-diaza-
bicyclo[3.3.1]nOD-6-ene-6-carboxyIic acid (2-chIorobenz>'I)cyclopropylamide
From Example 149, separated by chiral preparative HPLC.
Example 741
{rac.)~(IS, 5fl)-7-{4-[3-{2,3,6-TrifIuorophenoxy)propyiphenyl}-3,9-diaza-
bicyc[oI3.3.1]non-6-ene-6-carboxylicacid (2-chloroben2yI)c}"clopropyl3.r.ide
From Example 149, separated by chiral preparative HPLC.
Example 742
{rac)-ilR% 55*)-3-Acetyl-7-{4-[3-(2,6-dicliIoro-4-metbylphenoxy)propyl]-phenyl)-3,9-diazabicyclo{3.3.11non-6-ene-6-carboxylic acid (2-chlorobenzyl)-cyclopropylamide formate salt
Synthesized according to typical procedures F and E from bicyclononene BBl and 2,6-dichloro-4-methyiphenol. LC-MS: Rt= 0.96; ES+: 666.35.
Example 743
{rac.)-{lR*, 55*)-7-{4-[3-(2-Bromo-5-nuoropheuoxy)propyllphenyl}-3,9-
diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)cyclopropyl-amide
Synthesized according to typical procedure E from bicyclononene AX-20. LC-MS: R, - 0.86; ES+: 640.21.

The following assay was carried out in order to detennine the activity of the compounds of general formula I and their salts.
Inhibition of human recombinant renin by the compounds of the invention
The enzymatic in vitro assay was performed in 384-well polypropylene plates (Nunc). The assay buffer consisted of 10 mM PBS (Gibco BRL) including 1 mM EDTA and 0.1% BSA. The incubates were composed of 50 fiL per well of an enzyme mix and 2.5 pL of renin inhibitors in DMSO. The enzyme mix was premixed at 4°C and consists of the following components:
• human recombinant renin (0.16 ng/niL) • synthetic human angiotensin(l-14) (0.5
MM)
• hydroxyquinoline sulfate (1 mM)
The mixtures were then incubated at 37°C for 3 h.
To determine the enzymatic actiWty and its inhibition, tiie accumulated Ang I was detected by an enzyme immunoassay (EIA) in 384-weU plates (Nunc). 5 pL of the incubates or standards were transferred to immuno plates which were previously coated with a covalent complex of Ang I and bovine serum albumin (Ang I -BSA). 75 jiL of Ang I-antibodies in essaybuffer above including 0.01% Tween 20 were added and a primary incubation made at 4 °C overnight. The plates were washed 3 times with PBS including 0.01% Tween 20, and then incubated for 2 h at rt with an antirabbit-petoxidase coupled antibody (WA 934, Amersham). After washing the plates 3 times, ^cperoxidase substrate ABTS (2.2'-azino-di-(3-ethyl-benzthiazolinsulfonate), was added and the plates incubated for 60 min at room temperature. After stopping the reaction with 0.1 M citric acid pH 4.3 the plate was evaluated in a microplate reader at 405 nm. The percentage of inhibitton was calculated of each concentration point and the concentration of renin inhibition was determined that inhibited the enzyme activity by 50% (IC50). The ICso-values of all compoimds tested are below 100 nM. However selected compounds exhibit a very good bioavailibility and are metabolically more stable than prior ari compounds.


WE CLAIM :

A and B independently represent -0-; -S-; -SO-; or -SO2-;
U represents aryl; or heteroaryl;
T represents -CONR'-; -(CH2)pOCO-; -(CH2)pN(R')CO-; -(CH2)pN(R')S02-; or -C00-;
Q represents lower aikylene; or lower alkenylene;
M represents hydrogen; cycloalkyl; aryl; heterocyclyl; or heteroaryl;
L represents -R^; -COR^; -COOR^; -CONR^R^; -S02R^; -SO2NRV; or -C0CH(Aryl)2;
R' represents hydrogen; lower alkyl; lower alkenyl; lower alkinyl; cycloalkyl; aryl; or cycloalkyl-lower alkyl;
R^ and R^' independently represent hydrogen; lower alkyl; lower alkenyl; cycloalkyl; or cycloalkyl-lower alkyl;

R^ represents hydrogen; lower alkyl; lower alkenyl; cycloalkyl; aryl; heteroaryl; heterocyclyl; cycloalkyl-lower alkyl; aryl-lower alkyl; heteroaryl-lower alkyl; heterocyclyl-lower alkyi; aryloxy-lower alkyl; heteroaryloxy-lower alkyl, wherein these groups may be unsubstituted or mono-, di- or tri-substituted with hydroxy, -OCOR^, -COOR^, lower alkoxy, cyano, -CONR^R^', -CO-morpholin-4-yl, -CO-((4-lower alkyl)piperazin-I-yl), -NH(NH)NH2, -NRV' or lower alkyl, with the proviso that a carbon atom Is attached at the most to one heteroatom in case this carbon atom is sp^-hybridized;
R and R"*' independently represent hydrogen; lower alkyl; cycloalkyl; cycloalkyl-lower alkyl; hydroxy-lower alkyl; -COOR^; or -CONH2;
m is 1 and n is 0, or m is 0 and n is 1;
p is the integer 1, 2, 3 or 4; r is the integer 3, 4, 5, or 6; s is the integer 2, 3, 4, or 5; t is the integer 1,2,3, or 4; u is the integer 1, 2, or 3; and V is the integer 2, 3, or 4;
and pharmaceutically acceptable salts thereof.
2. The compounds of general formula I as claimed in claim 1 wherein X, W, V, U, T, Q, L, and M are as defined in claim 1 and
n is 0, and mis 1,
and pharmaceutically acceptable salts thereof
3. The compounds of general formula I as claimed in claim 1 wherein X, W, V, U, T, Q, M^ m, and n are as defined in claim 1 and
L represents -COR^"; -COOR^"; or -CONR^"R^"; and
R^" and R^" independently represent lower alkyl; or lower cycloalkyl-lower alkyl, wherein lower alkyl and lower cycloalkyl-lower alkyl are unsubstituted or mono-substituted with halogen, -CN, -OH, -OCOCH3, -CONH2, -COOH, or -NH2, with the proviso that a carbon atom is attached at the most to one heteroatom in case this carbon atom is sp"'-hybridized,
and pharmaceutically acceptable salts thereof.

4. The compounds of general formula I as claimed in claim 1 wherein X, W, V, U, L, m,
and n are as defined in claim 1 and
T represents -CONR'-;
Q represents methylene; and
M represents hydrogen; aryl or heteroaryl;
and pharmaceutically acceptable salts thereof.
5. The compounds of general formula I as claimed in claim I wherein X, W, U, L, T, Q, M,
m, and n are as defined in claim 1 and
V represents -CH2CH2O-; -CH2CH2CH2O-; or -OCH2CH2O-; and phannaceutically acceptable salts thereof.
6. The compounds of general formula I as claimed in claim 1 wherein V, U, T, Q, M, L, m,
and n are as defined in claim 1 and
X and W represent a -CH- group;
and pharmaceutically acceptable salts thereof.
7. The compounds of general formula I as claimed in claim 1 wherein X, W, V, Q, T, M,
L, m, and n are as claimed in claim 1 and
U is a mono-, di-, or tri-substituted phenyl wherein the substituents are halogen; lower alkyl or lower alkoxy;
and pharmaceutically acceptable salts thereof.
8. The compounds as claimed in claim I selected from the group consisting of:
(2-methoxyphenyl)acetic acid (JR*, 55*)-7-{4-[3-(2-methoxybenzyIoxy)-propoxy]phenyI}-3-(2-thiophen-2-ylacetyl)-3,9-diazabicyclo[3.3.1]non-6-en-6-yl-methyl ester;
(2-methoxyphenyl)aceticacid(iJ?*,5S*)-3-[2-(4-chlorophenyl)acetyl]-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester;

(2-methoxyphenyl)acetic acid (IR*, i5'*)-7-{4-[3-(2-methoxybenzyIoxy)-propoxy]phenyl}-3-(quinoxaline-2-carbonyI)-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl ester;
(/y;*,55*)-3-acetyl-7-{4-[3-{2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid[2-(2-chlorophenyl)ethyi]methyl-amide;
(2-methoxyphenyl)aceticacid(//;*55*)-3-(benzo[;']thiophene-3-carbonyl>7-{4-[3-(2-methoxyben2yloxy)propoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-6-yl-methyl ester;
(2-methoxyphenyl)acetic acid {IR*, 5S*)-3-acetyl-7-{4-[3-(2-methoxy-benzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyIester;
(2-methoxyphenyl)acetic acid (JR*, ^5*)-7-{4-[3-(2-methoxybenzyIoxy)-propoxy]phenyl}-
3-phenylmethanesulfonyl-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl ester;
{7^*55*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-
diazabicyclo [3.3.1]non-6-ene-6-carboxyiic acid [2-(4-methoxyphenyl)ethyl]-methyIamide;
(7;;*5i?*)-3-acetyl-7-{4-[2-(2-chloro-5-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid methylphenethylamide;
(7if*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethyl]phenylJ-3,9-diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid methylphenethylamide;
(2-methoxyphenyl)acetic acid (IR*. J5*)-3-[2-(4-chIorophenyl)acetyl]-7-{6-[3-(2-methoxybenzyloxy)propoxy]pyridin-3-yl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl ester;

(7/;*55*)-3-acetyl-7-(4-[2-(2,5-dimethylphenoxy)ethyl]phenyl}-3,9-di-azabicyclo[3.3.1] non-6-ene-6-carboxylic acid methylphenethylamide;
(ii;*55'*)-3-acetyl-7-{4-[3-(2-methoxybenzyIoxy)propoxy]phenyI}-3,9-diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid [2-(4-chlorophenyI)ethyl]methy]-amide;
(/^*,i5*)-3-acetyl-7-{4-[3-(2-methoxybenzy!oxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1 ]non-6-ene-6-carboxylic acid [2-(3-chlorophenyl)ethyl]methyI-amide;
(i^*,55*)-3-acetyl-7-{4-[3-(2-methoxybenzyioxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid ethylphenethylamide;
(7^*,J5*)-3-acetyI-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid [2-{3-methoxyphenyI)ethyl]methyl-amide;
(/i?*,5S*)-3-acety!-7-{4-[3-(23,6-trifluorophenoxy)propy[lphenyl)-3,9-diazabicyclo[3,3.1]non-6-ene-6-carboxyIic acid methyiphenethylamide;
(7^*5iS'*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(]R *, 55*)-3-acetyl-7- {4-[3-(2-bromo-5-fluorophenoxy)propyl]pheny 1} -3,9-diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid methylphenethylamide;
(2-methoxypheiiyl)acetic acid (iJ?*, 5S*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyi}-3-methy l-3,9-diazabicyclo[3.3.1 ]non-6-en-6-ylmethyl ester;
(7J?*,^5*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylicacid[2-(3,4-dimethoxyphenyl)ethyl]-methylamide;

(7^*55*}-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(7^* 55'*)-3-acetyI-7-{4-[3-(2,5-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyl:c acid methylphenethylamide;
UR*. ^5*)-3-acetyl-7-{4-f2-(2,3-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
^-((Ji?*.5S*)-3-acetyl-7-(4-[2-(2-chloTO-4,5-dimethylphenoxy)elhyl]phe-nyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(2-methoxyphenyl)acetic acid (IR*, J5*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3,9-diazabicyclo[3.3. l]non-6-en-6-ylmethyl ester;
A^-{(//;*55*)-3-acetyl-7-{4-[3-(2-methoxybenzyIoxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl)-2-(2-methoxyphenyl)-A'-methyl-acetamide;
iV-((/^*5S*)-3-acetyl-7-{4-[2-(2-rer(-butyl-4-methyIphenoxy)ethyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(JR*, 55*)-3-acetyI-7-{4-f2-(2,5-difluorophenoxy)ethyl]phenyI}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(;^*J)S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3. l]non-6-ene-6-carboxyUc acid methyl(3-pheny!propyl)amide;

(IR*, i5*)-3-acetyl-7-{4-[3-(2,3-dichlorophenoxy)propyllphenyl}-3,9-di-azabicyclo[3.3,l]non-6-ene-6-carboxylic acid methylphenethylamide;
(;ii*,JS'*)-3-acetyl-7-{4-[3-(2-acetylphenoxy)propyl]phenyl}-3,9-dia2abi-cycIo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(;^*i5*)-3-acetyI-7-{4-[3-(2-methoxyben2yIoxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid [2-(2-methoxyphenyl)ethyl]methyl-amide;
(/-ff*,55*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid benzylmethylamide;
(iii*,55*)-3-acetyl-7-{4-[3-(2,5-difluorophenoxy)propyl]phenyl}-3,9-di-azabicyclo[3.3.1]non-6-ene-6-carbQxylic acid methylphenethylamide;
{/^*55*)-3-acety!-7-[4-(2-o-toJyloxyethyl)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(7V;*,55*)-3-acetyl-7-{4-[2-(3-isopropylphenoxy)ethyl]phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;
(;^*,55*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabi-cyclo[3.3.1]non-6-ene-6-caiboxylic acid (2-chlorobenzyl)cyclopropylam!de;
(7ye*,55*)-5-[7-{4-[2-(2-bromo-5-fluorophenoxy)ethyl]phenyl}-6-(methyl-phenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxo-pentanoicacid;

(7^*,55*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3. l]non-6-ene-6-carboxyIic acid (2-chlorobenzyl)cyclopropyl-amide;
(7Jf*,55*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl-phenyl}-3,9-diaza-bicycIo[3.3.1]non-6-ene-6-carboxylic acid (2-clilorobenzyl)cycIopropylamide;
5-((7J?*55*)-6-[(2-chIorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propy!phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid;
(7J?*,55*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyI]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1 ]non-6-ene-9-carboxylic acid 2,2, 2-trichloro-1,1 -dimethylethyl ester;
5-((/i?*55*)-6-[(2-chIorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxo-pentanoic acid;
5-((i^*J5*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyI]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid methyl ester;
(7^.55)-3-((/5,4^)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)cyclopropylamide;
{;5',Jfi)-3-((^'5,4^)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-
trifluorophenoxy)propyl]pheny]}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)cyclopropyl-amide;

{;/;*55*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid (2-chloro-benzyl)cyclopropylamide;
(/7;*,55*)-3-(4-carbamoylbutyryl)-7-{4-[3K2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid benzyl-cyclopropylamide;
(7^*55*)-3-(4-carbamoylbutyryI)-7-{4-[3-{2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid {2-chloro-benzyl)ethylamide;
(//i*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyllpheny!}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluorobenzyl)amide;
(//f*,i5*)-3-(4-carbamoylbutyryl)'7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acidcyclopropyl-(3-trifluoromethylben2yI)amide;
(77;*,55*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diaza-bicyclo[3.3.l]non-6-ene-6-carboxylic acidcyclopropyl-(2-methylbenzyl)amide;
(;ii*J5*)-3-(4-carbamoyIbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid cyclopropyl-phenethylamide;
(ifi*,J5'*)-3-(4-carbamoy]butyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl)-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylic acid [2-(2-chloro-plienyl)ethyI]cyclopropylamide;
(;i;*J5*)-3K4-carbamoyibutyryl)-7-{4-[3-(2,3,6-trifiuorophenoxy)-propyI]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-6-carboxylicacidcyclopropyl-(3,5-diinethoxybenzyl)amide;

(iJ?*)-5-(a/;*55*)-6-[(2-chloroben2yl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
{J5*)-5-((77;*55*)-6-[(2-chloroben2yl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,6-trinuoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-y!)-3-hydroxy-5-oxopentanoic acid;
(i^*)-5-((M*,J5*)-6-(benzylcyclopropylcarbamoyI)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
(55*>5-((;Vi*55*)-6-(benzylcyclopropylcarbamoyI)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl)-3,9-diazabicyclo[3.3,l]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
(i/;*>5-((7^*55*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifiuorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
(J5*)-5-((77;*,55*)-6-[(2-chlorobenzyI)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.l]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
(i^*)-5-((;7i*55*)-6-[cyciopropyl-(2-fluorobenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazbicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;

(i5*)-5-((7J;*55'*)-6-[cyclopropyl-(2-fluorobenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl} -3,9-diazbicyclo-[3.3. l]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
(i^*)-5-({7J?*55*)-6-[cyclopropyl-(3-trifluoromethyl-benzyl)carbanioyl]-7-{4-[3-{2,3,6-trifluorophenoxy)propyI]-phenyl}-3,9-dia2a-bicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
(J5*)-5-((7if*,55*)-6-[cyclopropyi-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
(3J?*)-5-((JJ?*5S*)-6-[cyclopropyl-(2-methylbenzyl)-carbamoyl]-7-{4-[3-(2,3,6-
trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yi)-3-hydroxy-5-oxopentanoic acid;
(55*)-5-((/7;*55*)-6-[cyclopropyl-(2-metiiylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluoro-
phenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic
acid;
(i/;*)-5-((7^*,55*)-6-{cyclopropyi-[2-(4-methoxy-phenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
(i5*)-5-((;^*55*)-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-diazabicycio[3.3.I]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;

(i^*)-5-{(M*,55*)-6-[cyclopropyl-{2-m-tolyloxyethyl)-carbamoyl]-7-{4-[3-(2,3,6-trif]uorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
(5S*)-5-((/R*,5S*)-6-[cyclopropyl-(2-m-tolyloxyethyl>-carbamoyl]-7-{4-[3-(2,3,6-trifluoro-
phenoxy)propyl]phenyl}-3,9-dia2abicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic
acid;
(J/f*)-5-((7;e*5S*)-6-{[2-{2-chlorophenyl)ethyl]-cyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
(i5*)-5-((^^*^5*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.I]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
(i^*)-5-((7^*55*)-6-[cyclopropyl-(3,5-dimethoxy-benzyl)carbamoyl]-7-{4-[3-(2,3,6-txi£luorophenoxy)propyl]pheayl}-3,9-diaza-bLcyclo[3.3.1]non-6-en-3-y[)-3-hydroxy-5-oxopentanoic acid;
(i5*)-5-((7i;*55*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic acid;
(7/?*J5*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3. i]non-6-ene-6-carboxylic acid (2-chlorobenzyl)ethylamide;
(7i;*,JS*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3. l]non-6-ene-6-carboxylic acid cyclopropyl(3,5-dimethoxy-benzyl)amide;

5-({;j;*,55*)-6-(benzylcyclopropyIcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyI]phenyI}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid;
5-((;^*,55*)-6-[(2-cblorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid;
5-((yfi*,55*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.I]non-6-en-3-yl)-5-oxo-pentanoicacid;
5-((7;;*,55*)-6-[cyclopropyl(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]plienyl}-3,9-diazabicyclQ[3.3.1]non-6-eii-3-yl)-5-oxopentanoicacid;
5-{(;/i*55*)-6-[cyclopropyl(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid;
5-((7/;*55*)-6-([2-(2-chlorophenyl)ethyI]cyclopropylcarbamoyl}-7-{4-[3'(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid;
5-((/^*i5*)-6-[cyclopropyl(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;
5-((7^*J5*)-6-[cyc!opropyl{2-p-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluoropIienoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-5-oxo-pentanoic acid;
5-((J^*55*)-6-[{2-chlorobenzyl)ethylcaTbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;

5-((;^*55*)-6-[cyclopropyl-(2-fluorobenzyI)carbamoyl]-7-{4-[3-(2,3,6-
trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yi)-5-oxo-pentanoic acid
methyl ester;
5-((7i;*,55*)-6-[cyclopropyl-(3,5-diniethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-
trif]uorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
5-((/ii*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic
acid;
5-({7^*55*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyI-5-oxopentanoic acid;
5-((7ii*,55'*)-6-[cyclopropyl-(2-methyIbenzyI)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
5-((;^*J5*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoy!]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
(2ii*.3S*)-4-((/i?*,5S*)-6-[cyclopropyl-(2-methylbenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid;
i2S*,3R*)-4-((lR*, 55*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluoro-

phenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric acid;
5-{(i^*, 5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-{2-
fluoroben2yl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid;
5-{(IR*, J5*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cycIopropyl-[2-(3-
methylphenoxy)ethyl]carbamoyl}-3,9-dia2abicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic acid;
5-[(JR* J5*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyI}-6-
{cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.l]aon-6-en-3-y[]-5-oxo-pentanoic acid;
-7-{4-[3-(2-bromo-5-fluoropheiioxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyI}-3,9-diazabicyclo[3.3.1]non-6-en-3-yI)-5-oxopentanoic acid;
-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyi]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid;
-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{f2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3,l]non-6-en-3-yl)-5-oxopentanoic acid;
-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]pheny!}-6-{[2-(4-methyIphenyl)etbyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yi)-5-oxopentanoic acid;
5-{(/-R* 5S*)-7'{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyi}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.I]non-6-eii-3-yl}-5-oxopentanoicacid;
492

5-{(JR*, 55'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-
dimethoxybenzyI)carbanioyI]-3,9-diazabicyclo[3.3.1]non-6-en-3-yI}-5-oxopentanoic acid
methyl ester;
5-{{lR*, 5S*)-7-{4-[3-(2-bromo-5-fluorQphenQxy)pTOpyl]pheny[}-6-[cyclopropyl-(2-
f]uorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxo-pentanoic
acid;
5-{{}R*, 55*)-7-(4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyI-(2-
methyIbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.l]non-6-en-3-yL}-2,2-dimethyl-5-oxo-pentanoic
acid;
5-[(lR* J5*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-
(cyciopropylphenelhylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-2,2-dimethyl-5-oxopentanoic acid;
-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-
methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
5-{i!R*. J5'*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-{3,5-
dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5~ oxopentanoic acid;
t {2R*, 3S*)A-{{1R*, 5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-
(3,5-dimethoxybenzyl)carbainoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric acid;
(25* 3R*)-4-{(JR*. 55*)-7-{4-[3-{2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyi-

(3,5-dimethoxybenzy[)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric acid;
-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3. l]non-6-en-3-yl)-5-oxo-pentanoic acid;
-6-[(3-trifluoromethylbenzyi)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-triniethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid;
-6-[(2-methylbenzyl)cyclopropylcarbamoyI]-7-{4-[2-{2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid;
-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;
-6-[cyclopropyl-{2-fluorobenzyl)carbamoyl]-7-{4-t2-(2,3,5-trimelhylphenoxy)6thyl]phenyI}-3,9-diazabicyclo[3,3,l]non-6-en-3-yl)-2,2-diniethyl-5-oxopentanoic acid;
5-{(}R* J5*)-7-{4-[3-(2-bromo-5-nuorophenoxy)propyl]phenyl}-6-[(2-
chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-eii-3-yl}-5-oxopeEtanoic
acid;
5-{i}R* 5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-
chlorobenzyl)cyclopropylcarbamoyI]-3,9-diazabicyclo[3.3.I]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic acid;
5-{(IR*, 55*)-4-[3-(2-bromo-5-fluorophenoxy)propyI]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid(2-chloro-benzyl)cyclopropylamide;

-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3,3.I]non-6-en-3-yl)-5-oxopentanoic acid methyl ester;
(iR*, 55'*)-3-acetyl-7-{4-[2-(2-chloro-4,5-diinethylphenoxy)ethoxy]-phenyl}-3,9-
dia2abicyclo[3.3.1]non-6-ene-6-carboxyIic acid{2-chlorobenzyl)-cyclopropylaraide;
-6-[(2-chlorobenzyl)cyclopropylcarbanioyl]-7-{4-[2-(2-chioro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3,l]non-6-en-3-yl)-5-oxopentanoicacid;
5-{(JR*, 55'*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]pheny]}-6-[cyclopropyI-(2-
ii)ethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid;
5-{(/^* J5*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyI}-6-[cyclopropyl-(3,5-dimethoxybenzyI)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic acid;
-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-{2-chloro-4,5-ditnethylpiienoxy)ethoxy]phenyl}-3,9-dia2abicyclo[3.3,l]non-6-en'3-yI}-2,2-dimethyl-5-oxopentanoic acid;
-6-[(2-chlorobenzyl)etiiylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;
5-{ilR*, J5*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)etiioxy]phenyl}-6-[cyclopropyl-(2-
fluorobenzyl)carbamoyl]-3,9-diazabicycIo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic
acid;
-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[2-(23,5-triniethyIphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;

-6-[cyclopropyl-(2-/7-tolylethyl)carbamoyI]-7-{4-[2-(2,3,5-trimethyIphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid;
-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethy!)benzyI]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic acid;
-6-{cyclopropylphenethylcarbamoyl)-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic acid;
(//?* 55*)-7-(4-[3-(2,3,6-trifluoropheaoxy)propyllphenyl}-3,9-diaza-bicyc[o[3.3.11non-6-ene-6-carboxylic acid (2-chlorobenzyl)ethylamide;
(IR*, J5*}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyi}-3,9-diaza-bicyclo[3.3.1]non-6-ene-3,6-dicarboxyIic acid 6-[(2-chIorobenzyl)cyclopropyl-aniide] 3-dimethylamide;
(!R*, i5*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diaza-bicycio[3.3.1]non-6-ene-3,6-dicarboxylic acid 6-[(2-chlorobenzyi)cyclopropyl-amide] 3-diethylamide;
(JR*, J5*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-
trifluoi:ophenoxy)propyllphenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboxylic acid methyl ester;
(]R*, 55*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-
trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboxylic acid ^thyl
ester;
(]R*, 55*)-3-methanesulfonyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropy!amide;

(JR* 55*)-3'ethanesulfonyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)-cyclopropylamide;
-6-[(2-chlorobeiizyI)cyclopropylcarbamoyl]-7-{4-[3-(2,3>6-trifluorophenoxy)propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic acid ethyl ester;
HOR*, J5*)-6-[(2-chlorobenzyl)cyclopropyIcarbamoyl]-7-{4-[3-(2,3,6-
trifluorophenoxy)propy[]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-4-oxo-butyricacid;
3-[((ifl*, 55*)-6-[(2-chlorobenzy])cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-
trifluorophenoxy)propyl]phenyI}-3,9-dia2abicycIo[3.3.1]non-6-ene-3-carbonyl)-amino]propionic acid ethyl ester;
4-[((7^*, 55*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-
trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carbonyl)-amino]butyric acid ethyl ester;
(//;* 5S*>3-(3-carbamoy[propioayl)'7-{4-[3-(2,3,6-trifluorophenoxy>propyl]phenyl}-3,9-dia2abicyclo[3.3.1]non-6-ene-6-carboxylicacid{2-chloro-benzyI)cyclopropylamide;
(IR*, 55*)-3-(2-hydroxyacetyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]-phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxyIic acid {2-chlorobenzyl)-cyclopropylamide;
(JS, 5^)-3-{(i^)-3-hydroxybutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]-phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)-cyclopropylamide;
(JR*. 5S*y3-(iIR*, 25*>2-hydroxycyclopentanecarbonyl)-7-{4'[3-(2,3.6-
trifluorophenoxy)pTopyl]phenyl}-3,9-diazabicycio[3.3.1]non-6-ene-6-carboxyUc acid

(2-chIorobenzyi)cyclopropylamide;
{IR*, 5S*)-H0S*. 2i;*)-2-hydroxycyclopentanecarbony0-7-{4-[3-(2,3,6-trifluorophenoxy)-
propyl]phenyl}-3,9-diazabicyclo[3.3.I]non-6-ene-6-carboxylic acid (2-chloro-
benzyl)cyclopropylamide;
(IR*. 55*)-9-acetyI-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)cycIopropyl-amide;
-6-[{2-chlorobenzyI)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicycio[3.3.1]non-6-en-9-yI)-5-oxo-pentanoic acid:
-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3. l]non-6-en-9-yl)-5-oxo-pentanoic acid ethyl ester;
-6-[{2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-5-oxo-pentanoic acid methyl ester;
(ii? *)—6-[{2-chlorobenzy l)cyc!opropy 1-carbamoy l]-7- {4-[3-(2,3,6-trifiuorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-9-yl)-3-hydroxy-5-oxo-pentanoic acid;
(i5*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-
phenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-9-yl)-3-hydroxy-5-oxo-pentanoic
acid;
-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-{2,3>6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-2,2-dimethyl-5-oxopentanoicacid;

4-((;^*, ^5*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4'[3-(2,3,6-
trifIuorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-4-oxo-butyric acid;
{IR*. 55*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diaza-bicyclo[3.3.1]non-6'ene-6,9-dicarboxylic acid 6-[(2-chlorobenzyl)cyclopropyl-amide] 9-dimethylamide;
(/«*, 55*)-6-[(2-chlorobenzy[)cycloprQpylcarbamoyI]-7-{4-[3-(2,3,6-
trifluorophenoxy)propy!]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxyIic acid methyl
ester;
(JR* ^5*)-6-[(2-chlorobenzyl)cycIopropylcarbamoyl]-7-{4-[3-(2,3,6-
trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid ethyl
ester;
■ HVR*. 55*)-(6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-(4-[3-{2,3,6-
trifluorophenoxy)propyl]phenyi}-3,9-dtazabicyclo[3.3.l]non-6-ene-9-carbonyl)-amino]propionic acid ethyl ester;
4-[((7^*, 55*)-6-[(2-chlorobenzyl)cycIopropylcarbamoyl]-7-{4-[3-(2,3,6-
trifluorophenoxy)propyl]phenyl} -3,9-diazabicyclo[3.3.1 ]non-6-ene-9-carbonyl)-amino]butyric acid ethyl ester;
(JR*, 55*)-3-fonnyI-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide;
W 3-[((/ii* 55*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-(4-[3-(2,3,6-
trifluorophenoxy)propyl]phenyl}-3,9-diazabicycIo[3.3.1]non-6-ene-3-carbonyl)-amino]propionic acid;
499

H(U^*> 55*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-
trifluorophenQxy)propyl]phenyl}-3,9-diazabicyclop.3.1}non-6-ene-9-carbonyI)-aminojpropionic acid;
4-[((//i'*, 55*)-6-[(2-chlorobenzyl)cyclopropy[carbamoyll-7-{4'[3-(23,6-
trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.11non-6-ene-9-carbonyl)-amino]butyric
acid;
OR*, 55*)-3-acetyl-7-{4-[2-(2,3,6-trifluorophenoxy)ethyllphenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)cyclopropyI-amide;
OR*. J5*)-9-(4-carbamoylbutyryl)-7-{4-[2-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diaza-bicycIo[3.3. i]non-6-ene-6-carboxylic acid (2-chlorobenzyl)cyclopropylamide;
OR*. J5'*)-9-{3-carbamoylpropionyl)-7-{4-[2-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diaza-bicyclo[3.3.1]non-6-ene-6-carboxylicacid(2-chloro-benzyl)cyclopropylamide;
OR*, 55*)-9-(2-hydroxyacetyl)-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diaza-bicyclo[3.3. l]non-6-ene-6-carboxylic acid {2-chloroben2yl)-cyclopropylamide;
OR, 55)-9-((i5)-3-hydroxybutyryl)-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-
diazabicycIo[3.3.1 ]non-6-ene-6-carboxylic acid (2-chlorobenzyl)-cyclopropyIamide;
OR*. 55*)-9-methanesulfonyI-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-
diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid (2-chlorobenzyl)-cyclopropyIamide;
OR*. J5*)-9-ethanesulfonyl-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-
dia2abicyclo[3.3.1]non-6-ene-6-carboxylicacid(2-chloroben2yI)-cycIopropylamide;

{IR*. 55*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(2-fluoro-5-methoxy-
benzyl)ainide;
(IR*, J5*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-(3-methoxybenzyl)-amide;
(IR*. 55*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyI]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid cyclopropyl-{3,4-dimelhoxy-benzyI)amide;
(IR*, 55'*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]noii-6-ene-6-carboxylic acid (2-chloro-3-trifluoromethyI-
benzyl)cycIopropylamide;
(!R* 55*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid benzo[l,3]dioxol-5-y]methyl-
cyclopropylamide;
UR*. ^";S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyI}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid(2-chIoro-6-fiuorobenzyl)-cyclopropylamide;
(]R*, 55'*)-3-acetyl-7-{4-[3-(2,3,6-lrifluorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid(2-bromobenzyl)cyc]opropyl-amide;
(]R* 55*)-3-acetyI-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]aon-6-ene-6-carboxyUcacidcyclopropyl'(2,3-dimethyl-benzyl)amide;
(IR*, 55*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylicacidcyclopropyl-(3,5-difluoro-benzyl)amide;

0R*> J5*)-3-acetyl-7-{4-[3-{2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]noii-6-ene-6-carboxyiic acid cyclopropyI-(2,3-dichloro-benzyl)amide;
(/^* J5*)-3-acetyl-7-(4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylicacidcyc[opropyl-(3-trifluoromethoxy-benzyl)amide;
OR*, 5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-
dia2abicyclo[3.3.1]non-6-ene-6-carboxyIicacidcyclopropyl-(3-methylbenzyl)-amide;
UR*, 5,S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diaza-
bicyclo[3.3.1]non-6-ene-6-carboxylic acid (3-chlorobenzyl)cyclopropy]-amide;
(!R*, J6'*}-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyI}-3-(4-carbamoyIbutyryl)-3,9-diazabicyc!o[3.3.1]non-6-ene-6-carboxyUc acid cycIopropyl-(3,5-dimethoxybenzy!)amide;:
(}R*, 55*)-3-(5-morpholin-4-yl-5-oxopentanoyl)-7-{4-[3-(2,3,6-trifluoro-
phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-
chlorobenzyl)cyclopropylamide;
(JR* 55*)-3-(2-tetrazol-l-ylacetyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-
diazabicyclo[3.3.1 ]non-6-ene-6-carboxyIic acid (2-chIoro-ben2yl)cyclopropylamide;
{IR*, 5S*)-3-(5-oxo-5-piperazin-l-ylpentanoyl)-7-{4-[3-(2,3,6-trifluoro-
phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-
chloroben2yl)cyclopropylamide;
(JR, 55)-3-((25)-2-amino-3-hydroxypropionyl)-7-{4-[3-(2,3,6-
trifluorophenoxy)propyI]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)cyclopropylamide;

OS, 5^)-3-((25)-2-amino-3-hydroxypropionyl).7-{4-[3-(2,3,6-
trifIuorophenoxy)propyl]phenyl} -3,9-diaza-bicyclo[3.3.1 ]non-6-ene-6-carboxylic acid (2-chloroben2>'l)cyclopropylamide;
(JR. 55)-3'((25)-2-aminopropionyi)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl)-3,9-
diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid (2-chloroben2yl)cyclopropyIamide;
(JS, 5^)-3-((26)-2-aminopropionyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyI}-3,9-
diazabicyclo[3.3. l]non-6-6ne-6-carboxyHc acid (2-chloroben2yl)cyclopropyIamide;
{IR*. 5S*)-3-acetyl-7-{4-p-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxyUcacidcyclopropyl-(2,3-dichloroben2yl)amide;
(//?*, 55*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyJ.}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acidcyclopropyl-(2,3-dimethyIbenzyl)amide;
(IR*, J5'*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyJ}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chIoro-3-trifluoromethyl-
benzyl)cyclopropylamide;
(IR*, 55*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-
dia2abicycIo[3.3.1]non'6-ene-6-carboxylicacid(2-bromobenzyl)-cyclopropylamide;
(IR*, J5*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methyiphenoxy)ethoxy]-phenyl}-3,9-
diazabicyclo[3.3.I]non-6-ene-6-carboxylicacid(2-chlorobeiizyl)-cyclopropylamide;
(]R*, 5S'*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methy)phenoxy)ethoxy]-phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid(2-chlorobenzyl)-ethylamide;

(IR*, ■55*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-niethylphenoxy)ethoxy]-phenyl}-3,9-diaza-
bicyc]o[3.3.1]non-6-ene-6-carboxylic acid (6-chlorobenzo-[l,3]dioxol-5-
ylmethyl)cycIopropyIamide;
{IR*, 5S*)-3-acetyl-7-{4-(2-(2,6-dichbro-4-methyiphenoxy)ethoxy]-phenyl}-3,9-dia2a-
bicyclo[3.3.1]non-6-ene-6-carboxylicacidcycIopropyl-(3,5-dimethoxybenzyl)amide;
U^*. 55*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxyl-phenyl}-3,9-
dia2abicyc!o[3.3.1 ]non-6-ene-6-carboxyl!c acid cyc!opropy!-(3-methoxybenzyl)amide;
OR*, J5*)-3-acetyl-7-{4-[2.(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-
dia2abicyclo[3.3.1]non-6-ene-6-carboxyiicacidcyclopropyl-(2,3-dichloro-benzyI)amide;
OR*, J5*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid (2-chloro-3-trif]uoro-
methylbenzyl)cyciopropylamide;
OR*, ^5*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methy]phenoxy)ethoxy]-phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid(3-chlorobenzyl)-cyclopropyIamide;
(}R*, 5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methy!phenoxy)ethoxy]-phenyl}-3,9-
diazabicyclo[3.3.1]non-6-ene-6-carboxyHc acid cyclopropyl-{3-inethylbenzyl)amide;
QR*, 55*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-
dia2abicyclol3.3.1]non-6'ene-6-carboxyUcacidcyclopropyl-(2-fluoro-5-methoxybenzyl)amide;
(JR*, 55*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-3,9-
diazabicycIo[3.3.1]non-6-ene-6-carboxylicacidcycIopropyl-(2,3-dichlorobenzyl)amide;

(^^*- -5'5*)-3-acetyl-7-{4-[3-(2-chloro-3,6-difluorophenoxy)propyl]-phenyl}-3,9-
diazabicyclo[3.3.11non-6-ene'6-carboxyiicacid(2-chIorobenzyl>cyclopropylamide;
(^^* •55*)-3-acetyI-7-(4-[2-(2-chloro-4,5-dimethyIpiienoxy)ethoxy]-pheny[}-3,9-
diazabicyclo[3.3. l]nQn-6-ene-6-carboxyHc acid (2-chloro-3-
trifluoromethylbenzyl)cyclopropylamide;
ilR*. 5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-
diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid cyclopropyl-(3,4-dimethoxybenzyl)amide;
{iR*. 5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-
dia2abicyclo[3.3. lJnon-6-ene-6-carboxylic acid cyclopropyl-(3-trifluoromethoxybenzyI)amide;
{]R*, 5S*)-3-acetyl-7-{4'[2-(2,4,5'trichiorophenoxy)ethoxy]phenyl}-3,9-
diazabicyclo[3.3.1 ]non-6-ene-6'Carboxylic acid (2-chloro-3-trifluoro-
methylbenzyl)cyclopropylamide;
(!R*, ^'5'*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-
[3.3.l]noa-6-ene-6-carboxylic acid cyclopropyl-(2,3-dichloroben2yl)amide;
(JR*, 55*)-3-acetyl-7'{4-[2-(2,3-dichiorophenoxy)ethoxy]phenyI}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxyUc acid cyclopropyl-(2,3-dimethyl-ben2yl)amide;
(JR*, 55*)-3-acetyl-7-|4-[2-(2,4,5-trichlorophenoxy)ethoxy]plienyl}-3,9-diazabicycIo-
[3.3. llnon-6-ene-6-carboxyUc acid cyclopropyl-(2,3-dimethylbetizyl)amide;
(7j?* 55*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-
diazabicyclo[3.3. l]non-6-ene-6-carboxy!ic acid cyclopropyI-(2,3-dimethyIbenzy0amide;

(]R*, J5*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diaza-
bicyclo[3.3.1]non-6-ene-6-carboxylicacidcyclopropyl-(2,3-dichiorobenzyl)amide;
UR*, 55*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diaza-
bicyclo[3.3.1]non-6-ene-6-carboxy!ic acid (2-broraobenzyl)-cyclopropylamide;
(]R*, 55'*)-3-acetyl-7-{4-[2-{2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.I]non-6-ene-6-carboxylic acid cyclopropyl-{2,3-dichlorobenzyl)amide;
OR*. J5*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-
diazabicyclo[3.3. l]non-6-ene-6-carboxylic acid cyclopropyi-(2,3-dimethylbenzyl)amide;
(IR, 55)-7-{4-[3-(2,3,6-trifluorophenoxy)propyIphenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic acid (2-chlorobenzyl)cycIopropylamide; and
{75, 57i)-7-{4-[3-(2,3,6-trifluorophenoxy)propylphenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic acid (2-chIorobenzyl)cyclopropylamide.
9. Pharmaceutical compositions containing a compound as claimed in any one of claims 1 to 8 and usual carrier materials and adjuvants.


Documents:

2435-chenp-2004 abstract.pdf

2435-chenp-2004 claims.pdf

2435-chenp-2004 correspondences others.pdf

2435-chenp-2004 correspondences po.pdf

2435-chenp-2004 description (complete)-1.pdf

2435-chenp-2004 description (complete)-2.pdf

2435-chenp-2004 description (complete)-3.pdf

2435-chenp-2004 description (complete)-4.pdf

2435-chenp-2004 description (complete)-5.pdf

2435-chenp-2004 description (complete)-6.pdf

2435-chenp-2004 description (complete)-7.pdf

2435-chenp-2004 description (complete)-8.pdf

2435-chenp-2004 description (complete)-9.pdf

2435-chenp-2004 description (complete).pdf

2435-chenp-2004 description (complete)duplicate-1.pdf

2435-chenp-2004 description (complete)duplicate-2.pdf

2435-chenp-2004 description (complete)duplicate-3.pdf

2435-chenp-2004 description (complete)duplicate-4.pdf

2435-chenp-2004 description (complete)duplicate-5.pdf

2435-chenp-2004 description (complete)duplicate-6.pdf

2435-chenp-2004 description (complete)duplicate-7.pdf

2435-chenp-2004 description (complete)duplicate-8.pdf

2435-chenp-2004 description (complete)duplicate-9.pdf

2435-chenp-2004 description (complete)duplicate.pdf

2435-chenp-2004 form-18.pdf

2435-chenp-2004 form-26.pdf

2435-chenp-2004 form-3.pdf

2435-chenp-2004 form-5.pdf

2435-chenp-2004 others.pdf

2435-chenp-2004 pct search report.pdf

2435-chenp-2004 pct.pdf

2435-chenp-2004 petition.pdf


Patent Number 231326
Indian Patent Application Number 2435/CHENP/2004
PG Journal Number 13/2009
Publication Date 27-Mar-2009
Grant Date 04-Mar-2009
Date of Filing 27-Oct-2004
Name of Patentee ACTELION PHARMACEUTICALS LTD.
Applicant Address Gewerbestrasse 16, CH-4123 Allschwil,
Inventors:
# Inventor's Name Inventor's Address
1 BEZENCON, Olivier Durrenmattweg 53, CH-4123 Allschwil,
2 BUR, Daniel Im Rosengarten 24, CH-4106 Therwil,
3 FISCHLI, Walter Obertorweg 64, CH-4123 Allschwil,
4 REMEN, Lubos Kurzelängeweg 28, CH-4123 Allschwil,
5 RICHARD-BILDSTEIN, Sylvia 34a, Rue D'ottmarsheim, F-68170 Rixheim,
6 WEBER, Hans-Peter Seewenweg 45, CH-4146 Hochwald,
7 WELLER, Thomas Hoelzlistrasse 58, CH-4102 Binningen,
PCT International Classification Number C07D 471/08
PCT International Application Number PCT/EP2003/03721
PCT International Filing date 2003-04-08
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 PCT/EP02/04705 2002-04-29 EUROPEAN UNION