Title of Invention	A NOVEL QUINAZOLINE DERIVATIVE
Abstract	ABSTRACT The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R^ is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof

Title of Invention

A NOVEL QUINAZOLINE DERIVATIVE

Abstract

ABSTRACT The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R^ is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof

Full Text	The present invention relates to a novel quinazoline derivative. Background Art Neuropeptide Y (hereinafter referred to as NPY) is a peptide which consists of 36 amino acid residues and was isolated from porcine brain in 1982. NPY is widely distributed in the central nervous system and peripheral tissues of humans and animals. It has been reported that NPY possesses a stimulating activity of food intake, an anti-seizure activity, a learning-promoting activity, an anti-anxiety activity, an anti-stress activity etc. in central nervous system, and it may be pivotally involved in the central nervous system diseases such as depression, Alzheimer's disease and Parkinson's disease. NPY is thought to be associated with the cardiovascular diseases, since it induces a contraction of smooth muscles such as blood vessels or cardiac muscles in the peripheral tissues. Furthermore, NPY is also known to be involved in the metabolic diseases such as obesity, diabetes, and hormone abnormalities (Trends in Pharmacological Sciences, Vol. 15, and 153 (1994)). Therefore, an NPY receptor antagonist is expected as a medicine for preventing or treating various diseases involved in the NPY receptor. Subtypes of Yl, Y2, Y3, Y4, Y5 and Y6 have now been identified as the NPY receptor (Trends in Pharmacological Sciences, Vol. 18, and 372 (1997)). It has been suggested that the Y5 receptor is at least involved it the feeding behaviour and its antagonist is expected as an anti-obestic agent (Peptides, Vol. 18, and 445 (1997)). Quinazoline compounds having similar structures to those of the compounds of the present invention and exhibiting an NPY receptor antagonistic activity are described in WO97/20820, WO97/20821, WO97/20823 and the like. In addition, it is described that urea derivatives having a sulfonamide group and amide derivatives having a sulfonyl group in W099/64349 and benzyl sulfonamide derivatives in EP1010691-A, have an NPY antagonistic activity. Compounds having similar structures to those of the compounds of the present invention are described in JP59-16871 -A and W097/15567. Their activities are quite different from that of the present invention and these documents do not suggest the present invention. Disclosure of Invention The object of the present invention is to provide a superior pharmaceutical composition for use as an NPY Y5 receptor antagonist and novel compounds having the activity. Best Mode for Carrying out the Invention 2 In the present specification, the term "halogen" includes fluorine, chlorine, bromine and iodine. Fluorine or chlorine is preferable. The term "protective group" in "optionally protected hydroxy" and "optionally protected hydroxy(lower)alkyl" includes all of hydroxy protecting groups usually used. For example, acyl such as acetyl, trichloroacetyl and benzoyl, lower alkoxycarbonyl such as t-butoxycarbonyl, lower alkylsulfonyl such as methane sulfonyl, lower alkoxy(lower)alkyl such as methoxymethyl, trialkylsilyl such as t-butyldimethylsilyl are included. The term "lower alkyl" includes Cl to CIO straight or branched alkyl. The examples of "lower alkyl" are methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, isopentyl, neopentyl, hexyl, isohexyl, n-heptyl, isoheptyl, n-octyl, isooctyl, n-nonyl and n-decyl. "Lower alkyl" represented by BA is preferably C3 to ClO alkyl, more preferably C3 to C6 alkyl and most preferably isopropyl or t-butyl. "Lower alkyl" in other cases is preferably Cl to C6 alkyl and more preferably Cl to C4 alkyl. The examples of substituents of "optionally substituted lower alkyl" represented by Z are, (1) halogen; (2) cyano; (3) the following groups (i) to (xvi), which are optionally substituted with one or more substituents selected from "a substituents group f$" defined below, (i) hydroxy, (ii) lower alkoxy, (iii) mercapto, (iv) lower alkylthio, (v) acyl, (vi) acyloxy, (vii) carboxy, (viii) lower alkoxycarbonyl, (ix) imino, (x) carbamoyl, (xi) thiocarbamoyl, (xii) lower alkylcarbamoyl, (xiii) lower alkylthiocarbamoyl, (xiv) amino, (xv) lower alkylamino or (xvi) heterocyclylcarbonyl; or (4) a group of the formula: wherein RlO and R2 are each independently hydrogen or lower alkyl and when this group has two or more of R2 and/or two or more of R-2, each R2O and/or each RH may be different, W is single bond, 0, S or NR12, Rl2 is hydrogen, lower alkyl or phenyl, is cycloalkyl, bicycloalkyl, cycloalkenyl, aryl or heterocyclyl, each of which is optionally substituted with one or more of substituents selected from "a substituents group a" defined below and s is an integer of 0 to 4. In the present specification, "a substituents group a" is a group constituting of (1) halogen; (2) oxo; (3) cyano; (4) nitro; (5) imino optionally substituted with lower alkyl or hydroxy; (6) the following groups (i) to (xxi), which are optionally substituted with one or more of groups selected from the substituents group p, (i) hydroxy, (ii) lower alkyl, (iii) lower alkenyl, (iv) lower alkoxy, (v) carboxy, (vi) lower alkoxycarbonyl, (vii) acyl, (viii) acyloxy, (ix) imino, (x) mercapto, (xi) lower alkylthio, (xii) carbamoyl, (xiii) lower alkylcarbamoyl, (xiv) cycloalkylcarbamoyl, (xv) thiocarbamoyl, (xvi) lower alkylthiocarbamoyl, (xvii) lower alkylsulfinyl, (xviii) lower alkylsulfonyl, (xix) sulfamoyl, (xx) lower alkylsulfamoyl and (xxi) cycloalkylsulfamoyl; (7) the following groups (i) to (v), which are optionally substituted with the substituents group (3, lower alkyl, lower alkoxy(lower)alkyl, optionally protected hydroxy(lower)alkyl, halogeno(lower)alkyl, lower alkylsulfonyl and/or arylsulfonyl, (i) cycloalkyl, (ii) cycloalkenyl, (iii)cycloalkyloxy, (iv) amino and (v) alkylenedioxy; and (8) the following groups (i) to (xii), which are optionally substituted with the substituents group 0, lower alkyl, halogeno(lower)alkyl and/or oxo, (i) phenyl, (ii) naphthyl, (iii) phenoxy, (iv) phenyl(lower)alkoxy, (v) phenylthio, (vi) phenyl(lower)alkylthio, (vii) phenylazo, (viii) heterocyclyl, (ix) heterocyclyloxy, (x) heterocyclylthio, (xi) heterocyclylcarbonyl and (xii) heterocyclylsulfonyl. The preferable examples of the substituents group a as substituents for B ring are halogen; nitro; hydroxy; optionally substituted lower alkyl wherein the substituents is halogen, cyano, phenyl, carboxy and/or lower alkoxycarbonyl; lower alkenyl; lower alkoxycarbonyl(lower)alkenyl; optionally substituted lower alkoxy wherein the substituents is halogen, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, lower alkylamino and/or cyano; acyl; hydroxyimino; lower alkylthio; lower alkylsulfinyl; sulfamoyl; optionally substituted amino wherein the substituents is lower alkyl, optionally protected hydroxy(lower)alkyl, phenyl and/or acyl; alkylenedioxy; cyanophenyl; heterocyclylphenyl; biphenylyl; phenoxy; phenylazo optionally substituted with lower alkyl; or optionally substituted heterocyclyl wherein the substituents is optionally protected hydroxy, mercapto, halogen, lower alkyl, cycloalkyl, lower alkoxycarbonyl, amino, lower alkoxycarbonyl amino, carbamoyl, oxo, phenyl, lower alkoxyphenyl or heterocyclyl. More preferable examples are halogen; lower alkyl optionally substituted with halogen; or lower alkoxy optionally substituted with halogen. "A substituents group p" is a group consisting of halogen, optionally protected hydroxy, mercapto, lower alkoxy, lower alkenyl, amino, lower alkylamino, lower alkoxycarbonylamino, lower alkylthio, acyl, carboxy, lower alkoxycarbonyl, carbamoyl, cyano, cycloalkyl, phenyl, phenoxy, lower alkylphenyl, lower alkoxyphenyl, halogenophenyl, naphthyl and heterocyclyl. Examples of the substituents for "optionally substituted lower alkyl" represented by any other than Z (e.g., R1) are one or more substituents selected from the substituents group p. The lower alkyl may be substituted with these substituents at any possible positions. The lower alkyl part in "lower alkoxy", "lower alkoxycarbonyl", "lower alkoxycarbonyl(lower)alkyl", "lower alkylphenyl", "lower alkoxyphenyl", "lower alkylcarbamoyl", "lower alkylthiocarbamoyl", "lower alkylamino", "halogeno(lower)alkyl", "hydroxy(lower)alkyl", "phenyl(lower)alkoxy", "lower alkylthio", "phenyl(lower)alkylthio", "lower alkoxycarbonylamino", "lower alkoxycarbonyl(lower)alkenyl", "lower alkylsulfinyl", "lower alkylsulfonyl", "aryl(lower)alkoxycarbonyl", "lower alkylbenzoyl" and "lower alkoxybenzoyl" is the same as defined in the above "lower alkyl". Examples of substituents for "optionally substituted lower alkoxy" are one or more substituents selected from the substituents group p. Preferable examples are phenyl, lower alkylphenyl, lower alkoxyphenyl, naphthyl and heterocyclyl. The term "cycloalkyl" includes C3 to C8 cyclic alkyl and preferably C5 to C6 cyclic alkyl. Examples are cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl. Examples of substituents for "optionally substituted cycloalkyl" are one or more substituents selected from the substituents group a and the cycloalkyl may be substituted with these substituents at any possible positions. The term "bicycloalkyl" includes a group which is formed by excluding one hydrogen from a C5 to C8 aliphatic cycle containing two rings which possess two or more of atoms in common. Examples are bicyclo[2.1.0]pentyl, bicyclo[2.2.1]heptyl, bicyclo[2.2.2]octyl and bicyclo[3.2.1]octyl. The term "lower alkenyl" includes C2 to CIO, preferably C2 to C8 and more preferably C3 to C6 straight or branched alkenyl having one or more double bonds at any possible positions. Examples are vinyl, propenyl, isopropenyl, butenyl, isobutenyl, prenyl, butadienyl, pentenyl, isopentenyl, pentadienyl, hexenyl, isohexenyl, hexadienyl, heptenyl, octenyl, nonenyl and decenyl. The "lower alkenyl" part in "lower alkoxycarbonyl(lower)alkenyl" is the same as the above "lower alkenyl". Examples of the substituents for "optionally substituted lower alkenyl" are halogen, lower alkoxy, lower alkenyl, amino, lower alkylamino, lower alkoxycarbonylamino, lower alkylthio, acyl, carboxy, lower alkoxycarbonyl, carbamoyl, cyano, cycloalkyl, phenyl, lower alkylphenyl, lower alkoxyphenyl, naphthyl and/or heterocyclyl. The term "acyl" includes (1) Cl to CIO, preferably Cl to C6 and more preferably Cl to C4 straight or branched alkylcarbonyl or alkenylcarbonyl, (2) C4 to C9 and preferably C4 to C7 cycloalkylcarbonyl and (3) C7 to Cll arylcarbonyl. Examples are formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, pivaloyl, hexanoyl, acryloyl, propioloyl, methacryloyl, crotonoyl, cyclopropylcarbonyl, cyclohexylcarbonyl, cyclooctylcarbonyl and benzoyl. The "acyl" part in "acyloxy" is the same as the above. The term "cycloalkenyl" includes a group having at least one double bond at any possible positions in the above cycloalkyl. Examples are cyclopropenyl, cyclobutenyl, cyclopentenyl, cyclohexenyl and cyclohexadienyl. Examples of substituents for "optionally substituted cycloalkenyl" are one or more substituents selected from the substituents group p. Examples of substituents for "optionally substituted amino" are the substituents group p, optionally substituted benzoyl and/or optionally substituted heterocyclylcarbonyl wherein the substituents is hydroxy, lower alkyl, lower alkoxy and/or lower alkylthio. The term "aryl" includes a monocyclic of polycyclic aromatic carbocyclyl group and examples are phenyl, naphthyl, anthryl and phenanthryl. "Aryl" includes aryl fused with other a non-aromatic carbocyclyl group, for example, indanyl, indenyl, biphenylyl, acenaphthyl, tetrahydronaphthyl and fluorenyl. Phenyl is preferable. The aryl part in "aryl lower alkoxycarbonyl" is the same as the above. The term "optionally substituted aryl" and "optionally substituted phenyl" represented by Z include the above "aryl" and "phenyl" respectively, which may be substituted with the substLtuents group a or lower alkyl which may be substituted with one or more group selected from the substituents group a. Examples of the substituents for "optionally substituted aryl" and "optionally substituted phenyl" represented by any other than Z are one or more groups selected from the substituents group \|3. The term "carbocyclyl" includes the above "cycloalkyl", "cycloalkenyl", "bicycloalkyl" and "aryl". The term "non-aromatic carbocyclyl" includes the above "cycloalkyl", "cycloalkenyl" and "bicycloalkyl". The term "optionally substituted carbocyclyl" includes the above "optionally substituted cycloalkyl", "optionally substituted cycloalkenyl", "optionally substituted bicycloalkyl" and "optionally substituted aryl". The term "heterocyclyl" includes a heterocyclic group containing at least one heteroatom arbitrarily selected from 0, S and N. For example, 5- or 6-membered heteroaryl such as pyrrolyl, imidazolyl, pyrazolyl, pyridyl, pyridazinyl, pyrimidinyl, oxazolyl, oxadiazolyl, isothiazolyl, thiazolyl, thiadiazolyl, furyl and thienyl; fused heterocyclyl consisting of two rings such as indolyl, isoindolyl, indazolyl, indolizinyl, indolinyl, isoindolinyl, quinolyl, isoquinolyl, cinnolinyl, phthalazinyl, quinazolinyl, naphthyridinyl, quinoxalinyl, purinyl, pteridinyl, benzopyranyl, benzimidazolyl, benzisoxazolyl, benzoxazolyl benbzoxadiazolyl, benzisothiazolyl, benzothiazolyl, benzothiadiazolyl, benzofuryl, isobenzofuryl, benzothienyl, benzotriazolyl, imidazopyridyl, triazoropyridyl, imidazothiazolyl, pyrazinopyridazinyl, quinazolinyl, quinolyl, isoquinolyl, naphthyridinyl, dihydropyridyl, tetrahydroquinolyl and tetrahydrobenzothienyl; fused heterocyclyl consisting of three rings such as carbazolyl, acridinyl, xanthenyl, phenothiazinyl, phenoxathiinyl, phenoxazinyl and dibenzofuryl; and non-aromatic heterocyclyl such as dioxanyl, thiiranyl, oxiranyl, oxathiolanyl, azetidinyl, thianyl, pyrrolidinyl, pyrrolinyl, imidazolidinyl, imidazolinyl, pyrazolidinyl, pyrazolinyl, piperidyl, piperazinyl, morpholinyl, morpholino, thiomorpholinyl, thiomorpholino, dihydropyridyl, tetrahydrofuryl, tetrahydropyranyl, tetrahydrothiazolyl and tetrahydroisothiazolyl. "Fused heterocyclyl" fused with a ring other than a heterocycle (e.g., benzothiazolyl), may connect at any possible position. Substituents for "optionally substituted heterocyclyl" are the same as those for the above "optionally substituted aryl". Heterocyclyl parts in "heterocyclylcarbonyl", "heterocyclyloxy", "heterocyclylthio" and "heterocyclyl substituted phenyl" are the same as the above "heterocyclyl". The term "lower alkylene" includes a bivalent group comprising 1 to 6 of methylene, preferably 2 to 6 of methylene and more preferably 3 to 6 of methylene. For example, methylene, ethylene, trimethylene, tetramethylene, pentamethylene and hexamethylene are included. Tetramethylene is preferable. "Rl and R2 taken together may form lower alkylene" includes the case Lower alkylene part in "lower alkylenedioxy" is the same as the above "lower alkylene". Methylenedioxy or ethylenedioxy is preferable. The term "lower alkenylene" includes a bivalent group comprising 2 to 6 of methylene, preferably 3 to 6 of methylene and more preferably 4 to 5 of methylene and including at least one double bond. The term "cycloalkylene" includes a bivalent group which is formed by excluding one hydrogen from the above "cycloalkyl". A preferable example of cycloalkylene represented by X is 1, 4-cyclohexanediyl. The term "cycloalkenylene" includes a group containing at least one double bonds in the above cycloalkylene. The term "bicycloalkylene" includes a group which is formed by excluding one hydrogen from the above "bicycloalkyl". Examples are bicyclo[2. 1. OJpentylene, bicyclo[2. 2. l]heptylene, bicyclo[2. 2. 2]octylene, and bicyclo[3. 2. ljoctylene. The term "heterocyclediyl" includes a bivalent group which is formed by excluding one hydrogen from the above "heterocyclyl". Piperidinediyl, piperazinediyl, pyridinediyl, pyrimidinediyl, pyrazinediyl, pyrrolidinediyl or pyrrolediyl is preferable and piperidindiyl is more preferable. The term "arylene" includes a bivalent group which is formed by excluding one hydrogen from the above "aryl". Phenylene is preferable. The term "heteroarylene" includes aromatic groups in the above "heterocyclediyl". Examples are pyrrolediyl, imidazolediyl, pyrazolediyl, pyridinediyl, pyridazinediyl, pyrimidinediyl, pyrazinediyl, triazolediyl, triazinediyl, isoxazolediyl, oxazolediyl, oxadiazolediyl, isothiazolediyl, thiazolediyl, thiadiazolediyl, furandiyl and thiophenediyl. One or more groups selected from the substituents group p are examples of substituents for "optionally substituted lower alkylene", "optionally substituted lower alkenylene", "optionally substituted cycloalkylene", "optionally substituted cyclohexylene", "optionally substituted bicycloalkylene", "optionally substituted cycloalkenylene", "optionally substituted phenylene", "optionally substituted heterocyclediyl" and "optionally substituted piperidinylene". Halogen, hydroxy, lower alkyl, halogeno(lower)alkyl, lower alkoxy, amino, lower alkylamino, acyl, carboxy or The compounds of the present invention include any formable and pharmaceutical2 acceptable salts thereof. Examples of "the pharmaceutical2 acceptable salt" are salts with mineral acids such as hydrochloric acid, sulfuric acid, nitric acid and phosphoric acid; salts with organic acids such as para-toluenesulfonic acid, methane sulfonic acid, oxalic acid and citric acid; salts with organic bases such as ammonium, trimethylammonium and triethylammonium; salts with alkaline metals such as sodium and potassium; and salts with alkaline earth metals such as calcium and magnesium. The compounds of the present invention include solvates thereof. Hydrate is preferable and arbitrary numbers of water molecules may coordinate to the compound of the present invention. The compounds of the present invention include prodrugs thereof. Prodrug includes derivatives of the compounds of the present invention which have a chemically or metabolically decomposable group and can be converted into pharmaceutical2 active compounds of the present invention in vivo by solvolysis or under the physiological conditions. The methods for selecting and producing suitable prodrugs are described in Design of Prodrugs, Elsevier, Amsterdam 1985. When a compound (I) of the present invention has carboxy, examples of prodrugs are an ester derivative and an amide derivative, which can be produced by reacting a compound (I) having carboxy with a suitable alcohol or a suitable amine, respectively. When a compound (I) of the present invention has hydroxy, an example of prodrugs is an acyloxy derivative, which can be synthesized by reacting a compound (I) having hydroxy with a suitable acyl halide or a suitable acid anhydride. When a compound (I) of the present invention has amino, an example of prodrugs is an amide derivative, which can be synthesized by reacting a compound (I) having amino with a suitable acid halide or a suitable mixed acid anhydride. When the compound (I) of the present invention has an asymmetric carbon atom, it includes racemates, all of enantiomers and all of stereoisomers such as diastereomer, epimer and enantiomer thereof. When the compound (I) of the present invention having one or more double bonds forms an E isomer or Z isomer, the compound (I) includes both isomers. When X is cycloalkylene, the compound (I) includes both of cis isomer and trans isomer. For example, the compound (I) of the present invention can be synthesized by the following methods. wherein Hal is halogen, Q is an amino protecting group and the other symbols are the same as the above. Step A Compound 1 is reacted with Amino Compound 2 having the desired substituent Z and R7 in a suitable solvent at 0 °C to 50 °C for several minutes to several hours. As solvents, tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile, water, a mixture thereof etc. can be used. An activator such as thionyl chloride, acid halide, acid anhydride and activated ester can be used, if necessary. StepB Compound 3 is deprotected by the usual method and reacted with Sulfonyl Halide 4 having the desired substituent R2 in a suitable solvent at 0 °C to 50 °C for several minutes to several hours to give Compound (I-A) wherein n is 2. Tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile, water and the mixture thereof etc. can be used as a solvent. StepC Compound (I-B) wherein n is 1 can be synthesized by reacting Compound 3 with Sulfinyl Halide 5 having substituent R2-. The conditions for the reaction are the same as those of the above Step B. StepD Compound (I-B) obtained in Step C is oxidized by the usual method to give Compound (I-A) wherein n is 2. m-Chloroperbenzoic acid, peracetic acid, hydrogen peroxide, trifluoroperacetic acid, sodium periodate, sodium hypochlorite, potassium permanganate etc. can be used as an oxidizer and the reaction may be carried out at 0 °C to 50 °C. Examples of solvents are tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile, water, methanol, ethanol, isopropanol and mixture thereof. In case X is heterocyclediyl containing at least one N atom and the N atom connects to CONR2-Z in the compound (I), the following reaction may be employed to obtain wherein R is lower alkyl or aryl and L is a leaving group. StepC Compound 5 is reacted with Compound 6 in a similar manner to the above Step C to give Compound 7. StepE Thus obtained Compound 7 is treated with a base in a suitable solvent to give Compound 8. For example, barium hydroxide, sodium hydroxide, potassium hydroxide, hydrazine or lithium propanethiolate=can be used as a base. As a solvent, tetrahydrofuran, dimethylformamide, dioxane, acetone, acetonitrile, methanol, ethanol, propanol, water, the mixture thereof or the like can be used. The reaction can be carried out at 0 °C to 100 °C for several minutes to several tens hours. StepF Compound 8 is reacted with Compound 9 having a leaving group and a desired substituent in a suitable solvent in the presence or absence of a base at 0 °C to 100 °C for several minutes to several days to give Compound (I-B1). Examples of the leaving group are phenoxy, chloro and trichloromethyl. Examples of the base are triethylamine, pyridine, diisopropylethylamine, sodium hydroxide, potassium carbonate and sodium hydrogencarbonate. Examples of the solvent are tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile, methanol, ethanol and the mixture thereof. StepD Compound (I-B') is reacted in a similar manner to the above Step D to give Compound (I-A'). wherein each of the symbols is the same as the above. Step G and Step B Compound 10 is reacted with Compound 11 under the same reaction condition as that in Step B. Thus obtained Compound 12 is reacted in a similar manner to the above Step B to give Compound (I-C) wherein n=2. Step C and Step D To synthesize Compound (I-D), Compound 12 obtained in Step G may be reacted in similar manners to the above Step C and Step D. (Compound wherein Y=OCONR7) wherein each of symbols is the same as the above. StepH Compound 13 is reacted with Isocianate Compound 14 having a substituent Z in a suitable solvent in the presence or absence of a suitable catalyst at 0 °C to 100 °C for several minutes to several days to give Compound 15. Examples of the solvent are tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile and the mixture thereof. Step C and Step D Thus obtained Compound 15 is reacted in similar manners to Step C and Step D to give Compound (I-E) of the present invention. (Compound wherein Y=CSNR7 or NR7CS) Compound (I) wherein Y is CSNR7 or NR7CS can be synthesized by reacting Compound (I) wherein Y is CONR7 or NR7CO synthesized in any one of the above methods with the Lawesson's reagent or phosphorus pentasulfide in a suitable solvent at 30 °C to 100 °C for several minutes to several hours. Examples of the solvent are tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile and the mixture thereof. Amino groups may be protected with a suitable protecting group in the usual manner at a suitable step. For example, phthalimide, lower alkoxycarbonyl, lower alkenyloxycarbonyl, halogenoalkoxycarbonyl, aryl(lower)alkoxycarbonyl, trialkylsilyl, lower alkylsulfonyl, halogeno(lower)alkylsulfonyl, arylsulfonyl, lower alkylcarbonyl and arylcarbonyl can be used as the protecting group. After protection of the amino group, the compound is subjected to the above-mentioned reactions and the obtained compound is deprotected by treatment of an acid or a base in a suitable solvent at a suitable stage. Examples of a solvent is tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile and the mixture thereof. Examples of a base are hydrazine, pyridine, sodium hydroxide and potassium hydroxide and examples of an acid are hydrochloric acid, trifluoroacetic acid and hydrofluoric acid. All of the compounds of the present invention have an NPY Y5 antagonistic activity and the following compounds are specifically preferable. In the formula (I), a compound wherein SA is optionally substituted lower alkyl or optionally substituted cycloalkyl (hereinafter referred to as "R1 is Rl-1"), a compound wherein R1 is C3 to CIO alkyl or C5 to C6 cycloalkyl, each of which is optionally substituted with halogen (hereinafter referred to as "R1 is Rl-2"), a compound wherein R1 is C3 to CIO alkyl optionally substituted with halogen (hereinafter referred to as "R* is Rl-3"), a compound wherein R1 is isopropyl or t-butyl (hereinafter referred to as "R1 is Rl-4"), a compound wherein R2 is hydrogen or Cl to C3 alkyl (hereinafter referred to as "R2 is R2-1"), a compound wherein R2 is hydrogen (hereinafter referred to as" R2 is R2-2"), a compound wherein X is optionally substituted lower alkylene, optionally substituted wherein is optionally substituted cycloalkylene, optionally substituted phenylene, optionally substituted piperidinylene, optionally substituted thiophenediyl or optionally substituted furandiyl (hereinafter referred to as "X is X-3"), a compound wherein X is (i) C2 to C6 alkylene or (ii) cycloalkylene or phenylene, each of which is optionally substituted with halogen, hydroxy, lower alkyl or halogeno(lower)alkyl (hereinafter referred to as "X is X-4"), a compound wherein X is C2 to C6 alkylene or to C5 to C6 cycloalkylene (hereinafter referred to as "X is X-5"), a compound wherein X is C3 to C6 alkylene or 1,4-cyclohexylene (hereinafter referred to as "X is X-6"), a compound wherein Y is CONR7, CSNE7, NR7CO or NR7CS and R7is hydrogen or Cl to C3 alkyl (hereinafter referred to as "Y is Y-l"), a compound wherein Y is CONH, CSNH or NHCO (hereinafter referred to as "Y is Y-2"), a compound wherein Y is CONH (hereinafter referred to as "Y is Y-3"), a compound wherein Z is optionally substituted lower alkyl, optionally substituted carbocyclyl or optionally substituted heterocyclyl (hereinafter referred to as "Z is Z-1"), a compound wherein Z is -(CR8 R2r-W-CCRiORi2s-V wherein R8, R2, RlO and R1 are each independently hydrogen or lower alkyl and when Z has two or more of R8, two or more of R°, two or more of R0 and /or two or more of R11, each of R8, R2, RlO an(j R11 may be different, Wis single bond, 0, S or NR12, Rl2 is hydrogen, lower alkyl or phenyl, V is hydrogen, optionally substituted cycloalkyl, optionally substituted bicycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl, r is an integer of 1 to 4 and s is an integer of 0 to 4 (hereinafter referred to as "Z is Z-2"), a compound wherein Z is -(CH2)r-W-(CH2)s-V wherein W is single bond, 0, S or NR12 R12 JS hydrogen or lower alkyl, V is optionally substituted aryl or optionally substituted heterocyclyl wherein the substituents is halogen, hydroxy, lower alkyl, halogeno(lower)alkyl, lower alkoxy, lower alkenyl, amino, lower alkylamino, acyl, carboxy, lower alkoxycarbonyl, phenyl or monocyclic heteroaryl, r is an integer of 1 to 4 and s is an integer of 0 to 4 (hereinafter referred to as "Z is Z-3), a compound wherein Z is -(CH2)r-W-(CH2)s-V wherein W is single bond, O, S, NH or NMe, V is optionally substituted phenyl or optionally substituted heteroaryl wherein the substituents is halogen, lower alkyl, halogeno(lower)alkyl, lower alkoxy, amino or lower alkylamino, r is an integer of 1 to 3 and s is an integer of 0 or 1 (hereinafter referred to as "Z is Z-4"), a compound wherein Z is optionally substituted carbocyclyl, wherein the substituent is halogen; hydroxy; optionally substituted lower alkyl wherein the substituents is halogen, hydroxy, carboxy, lower alkoxycarbonyl, cyano and /or phenyl; lower alkenyl optionally substituted with lower alkoxycarbonyl; optionally substituted lower alkoxy wherein the substituents is halogen, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, lower alkylamino, cycloalkyl, cyano and /or heterocyclyl; cycloalkyl; cycloalkyloxy; acyl; lower alkylthio; carbamoyl; lower alkylcarbamoyl; cycloalkylcarbamoyl; hydroxy imino; optionally substituted amino wherein the substituents is lower alkyl, optionally protected hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, acyl, lower alkylsulfonyl, arylsulfonyl and/or phenyl; phenyl optionally substituted with halogen, cyano, phenyl and /or heterocyclyl; lower alkylsulfinyl; lower alkylsulfamoyl; cycloalkylsulfamoyl; nitro; cyano; alkylenedioxy; phenylazo optionally substituted with lower alkyl; phenoxy; oxo; optionally substituted heterocyclyl wherein the substituents is optionally protected hydroxy, mercapto, halogen, lower alkyl, cycloalkyl, lower alkoxycarbonyl, acyl, amino, lower alkoxycarbonylamino, carbamoyl, oxo, phenyl, lower alkoxyphenyl, halogenophenyl, heterocyclyl and /or oxo; heterocyclylsulfonyl optionally substituted with lower alkyl; heterocyclyloxy; heterocyclylcarbonyl optionally substituted with lower alkyl (hereinafter referred to as "Z is Z-5), a compound wherein Z is optionally substituted phenyl wherein the substituents is halogen; hydroxy; lower alkyl optionally substituted with halogen, hydroxy, lower alkoxycarbonyl, cyano and /or phenyl; lower alkoxycarbonyl(lower)alkenyl; lower alkoxy optionally substituted with halogen, lower alkoxy, lower alkoxycarbonyl, cycloalkyl and /or heterocyclyl; cycloalkyl; cycloalkyloxy; acyl; lower alkylthio; carbamoyl; lower alkycarbamoyl; amino optionally substituted with lower alkyl, hydroxy(lower)alkyl, acyl, lower alkylsulfonyl and /or phenyl; phenyl optionally substituted with halogen, cyano, phenyl and /or heterocyclyl; lower alkyl sulfamoyl; cycloalkylsulfamoyl; nitro; alkylenedioxy; phenylazo optionally substituted with lower alkyl; phenoxy; oxo; heterocyclyl optionally substituted with hydroxy, halogen, lower alkyl, lower alkoxycarbonyl, amino, carbamoyl, phenyl, halogenophenyl, heterocyclyl and /or oxo; heterocyclyloxy; and/or heterocyclylsulfonyl optionally substituted with lower alkyl (hereinafter referred to as" Z is Z-6"), a compound wherein Z is optionally substituted phenyl wherein the substituents is halogen; lower alkyl optionally substituted with halogen, hydroxy, lower alkoxycarbonyl and/or phenyl; lower alkoxy optionally substituted with halogen and/or cycloalkyl; cycloalkyl; cycloalkyloxy; acyl; lower alkylthio; lower alkylcarbamoyl; amino optionally substituted with lower alkyl, hydroxy(lower)alkyl, acyl and/or phenyl; phenyl optionally substituted with piperidyl; cycloalkylsulfamoyl; alkylenedioxy; phenoxy; morpholinyl or morpholino, each of which is optionally substituted with lower alkyl; piperidyl optionally substituted with hydroxy, lower alkyl, lower alkoxycarbonyl, phenyl, halogenophenyl and/or oxo; pyrrolidinyl optionally substituted with hydroxy, carbamoyl and/or oxo; piperazinyl optionally substituted with phenyl or pyrimidinyl; dihydropyridyl; pyrrolyl; pyrrolinyl; imidazolyl optionally substituted with halogen and/or lower alkyl; pyrazolyl; thienyl; thiadiazolyl; furyl; oxazolyl; isoxazolyl; tetrazolyl optionally substituted with lower alkyl and/or phenyl; indolinyl; indolyl; tetrahydroquinolyl; benzothiazolyl optionally substituted with lower alkyl; tetrahydroisothiazolyl optionally substituted with oxo; benzopyranyl optionally substituted with oxo; tetrahydropyranyloxy; tetrahydrofuryloxy; morpholinosulfonyl optionally substituted with lower alkyl; and/or piperidylsulfonyl optionally substituted with lower alkyl (hereinafter referred to as "Z is Z-7"), a compound wherein Z is optionally substituted phenyl wherein the substituents is halogen, lower alkyl, halogeno(lower)alkyl, lower alkoxy, cycloalkyloxy, lower alkylcarbamoyl, phenyl, lower alkyl morpholino and/or tetrahydropyranyloxy (hereinafter referred to as "Z is Z-8"), a compound wherein Z is optionally substituted heterocyclyl wherein the substituents is halogen, hydroxy, lower alkyl, halogeno(lower)alkyl, lower alkoxy, mercapto, lower alkylthio, acyl, carboxy, lower alkoxycarbonyl, amino, lower alkylamino, phenyl, naphthyl, phenylthio optionally substituted with halogen, phenoxy optionally substituted with halogen, oxo, and/or heterocyclyl optionally substituted with lower alkyl (hereinafter referred to as "Z is Z-9"), a compound wherein Z is thienyl, pyrazolyl, thiazolyl, thiadiazolyl, pyridyl, pyrimidinyl, pyrazinyl, triazinyl, indolyl, isoindolyl, indolinyl, isoindolinyl, indazolyl, benzopyranyl, benzoxazolyl, benzothienyl, benzothiazolyl, benzothiazolinyl, benzothiadiazolyl, quinolyl, isoquinolyl, dihydrobenzofuryl, carbazolyl, acridinyl or dibenzofuryl, each of which is optionally substituted with substituents selected from the group of lower alkyl; halogeno(lower)alkyl; lower alkoxy; lower alkoxycarbonyl; acyl; lower alkoxycarbonyl(lower)alkyl; mercapto; phenyl, naphthyl, phenylthio or phenoxy, each of which is optionally substituted with halogen; furyl; nitro; oxo; and morpholino optionally substituted with lower alkyl) (hereinafter referred to as "Z is Z-10"), a compound wherein Z is thienyl, thiazolyl, thiadiazolyl, pyridyl, pyrazinyl, indolyl, isoindolinyl, benzopyranyl, quinolyl, carbazolyl, dibenzofuryl, benzopyranyl, benzothienyl or benzothiazolyl, each of which is optionally substituted with one or more substituents selected from the group of lower alkyl, halogeno(lower)alkyl, lower alkoxy, lower alkoxycarbonyl, acyl, phenyl, naphthyl, phenylthio, lower alkyl morpholino and oxo) (hereinafter referred to as "Z is Z-ll), a compound wherein R1 is Rl-2, R2 is R2-2, n is 2 and a combination of X, Y and Z, i.e., (X, Y, Z), is any one of the followings. (X, Y, Z) = (X-3, Y-2, Z-l), (X-3, Y-2, Z-2), (X-3, Y-2, Z-3), (X-3, Y-2, Z-4), (X-3, Y-2, Z-5), (X-3, Y-2, Z-6), (X-3, Y-2, Z-7), (X-3, Y-2, Z-8), (X-3, Y-2, Z-9), (X-3, Y-2, Z-10), (X-3, Y-2, Z-ll), (X-3, Y-3, Z-l), (X-3, Y-3, Z-2), (X-3, Y-3, Z-3), (X-3, Y-3, Z-4), (X-3, Y-3, Z-5), (X-3, Y-3, Z- 6), (X-3, Y-3, Z-7), (X-3, Y-3, Z-8), (X-3, Y-3, Z-9), (X-3, Y-3, Z-10), (X-3, Y-3, Z-ll), (X-4, Y-2, Z-l), (X-4, Y-2, Z-2), (X-4, Y-2, Z-3), (X-4, Y-2, Z-4), (X-4, Y-2, Z-5), (X-4, Y-2, Z- 6), (X-4, Y-2, Z-7), (X-4, Y-2, Z-8), (X-4, Y-2, Z-9), (X-4, Y-2, Z-10), (X-4, Y-2, Z-ll), (X-4, Y-3, Z-l), (X-4, Y-3, Z-2), (X-4, Y-3, Z-3), (X-4, Y-3, Z-4), (X-4, Y-3, Z-5), (X-4, Y-3, Z- 6), (X-4, Y-3, Z-7), (X-4, Y-3, Z-8), (X-4, Y-3, Z-9), (X-4, Y-3, Z-10), (X-4, Y-3, Z-ll), (X-5, Y-2, Z-l), (X-5, Y-2, Z-2), (X-5, Y-2, Z-3), (X-5, Y-2, Z-4), (X-5, Y-2, Z-5), (X-5, Y-2, Z- 6), (X-5, Y-2, Z-7), (X-5, Y-2, Z-8), (X-5, Y-2, Z-9), (X-5, Y-2, Z-10), (X-5, Y-2, Z-ll), (X-5, Y-3, Z-l), (X-5, Y-3, Z-2), (X-5, Y-3, Z-3), (X-5, Y-3, Z-4), (X-5, Y-3, Z-5), (X-5, Y-3, Z- 6), (X-5, Y-3, Z-7), (X-5, Y-3, Z-8), (X-5, Y-3, Z-9), (X-5, Y-3, Z-10) or (X-5, Y-3, Z-ll), the pharmaceutically acceptable salt, solvate or prodrug thereof. The NPY Y5 receptor antagonist of the present invention is effective for all of the diseases in which NPY Y5 is involved and it is especially useful for preventing and/or treating obesity and suppressing food intake. Moreover, the antagonist is effective for preventing and/or treating the diseases in which obesity acts as a risk factor, for example, diabetes, hypertension, hyperlipemia, atherosclerosis and acute coronary syndrome. In addition, the NPY Y5 receptor antagonist of the present invention has a low affinity for NPY Yl and Y2 receptors, and has a high selectivity for NPYY5 receptor. NPY causes a sustained vasoconstrictive action in the periphery and this action is mainly via Yl receptor. Since Y5 receptor is not involved in this action at all, the NPY Y5 receptor antagonist has a low risk of inducing side effects based on the peripheral vasoconstriction, and is expected to be suitably used as a safe medicine. The NPY Y5 receptor antagonist shows an anti-obestic effect by suppressing food intake. Therefore, it is one of the features that this antagonist does not induce side effects, e.g., an indigestion caused by an anti-obestic agent which inhibits digestion and absorption, and a central side effect such as anti-depression caused by a serotonin transporter inhibitor showing an anti-obesity effect. A compound of the present invention can be administered orally or parenterally as an anti-obestic agent or anorectic agent. In the case of oral administration, it may be in any usual form such as tablets, granules, powders, capsules, pills, solutions, syrups, buccal tablets and sublingual tablets. When the compound is parenterally administered, any usual form is preferable, for example, injections (e.g., intravenous, intramuscular), suppositories, endermic agents and vapors. Oral administration is particularly preferable because the compounds of the present invention show a high oral absorbability. A pharmaceutical composition may be manufactured by mixing an effective amount of a compound of the present invention with various pharmaceutical additives suitable for the administration form, such as excipients, binders, moistening agents, disintegrators, lubricants and diluents. When the composition is of an injection, an active ingredient together with a suitable carrier can be sterilized to give a pharmaceutical composition. Examples of the excipients include lactose, saccharose, glucose, starch, calcium carbonate and crystalline cellulose. Examples of the binders include methylcellulose, carboxymethylcellulose, hydroxypropylcellulose, gelatin and polyvinylpyrrolidone. Examples of the disintegrators include carboxymethylcellulose, sodium carboxymethylcellulose, starch, sodium alginate, agar and sodium lauryl sulfate. Examples of the lubricants include talc, magnesium stearate and macrogol. Cacao oil, macrogol, methylcellulose etc. may be used as base materials of suppositories. When the composition is manufactured as solutions, emulsified injections or suspended injections, dissolving accelerators, suspending agents, emulsifiers, stabilizers, preservatives, isotonic agents and the like may be added. For oral administration, sweetening agents, flavors and the like may be added. Although the dosage of a compound of the present invention as an anti-obestic agent or anorectic agent should be determined in consideration of the patient's age and body weight, the type and degree of diseases, the administration route etc., a usual oral dosage for an adult is 0.05 to 100 mg/kg/day and preferable is 0.1 to 10 mg/kg/day. For parenteral administration, although the dosage highly varies with administration routes, a usual dosage is 0.005 to 10 mg/kg/day, preferably, 0.01 to 1 mg/kg/day. The dosage may be administered in one to several divisions per day. The present invention is further explained by the following Examples and Experiments, which are not intended to limit the scope of the present invention. Examples Example 1 Synthesis of Compound (1-7) Step 1 Sodium carbonate (995 mg, 9.38 mmol) was dissolved in 30 ml of water and starting material amino acid (1.0 g, 8.53 mmol) and N-carbethoxyphthalimide (2.49 g, 11.4 mmol) were added thereto. The mixture was stirred at room temperature overnight. The pH of the mixture was adjusted to 1 by adding cone, hydrochloric acid. Precipitated crystals were washed with water and dried to give the desired compound (1.72 g, 82 % yield). iH-NMR (CD3OD) 6 ppm: 1.59-1.77 (m, 4H), 2.34 (t, 2H, J = 6.3 Hz), 3.69 (t, 2H, J = 6.6 Hz), 7.78-7.87 (m, 4H). The compound obtained in Step 1 (1.0 g, 4.0 mmol) was dissolved in 5 ml of dichloromethane at room temperature. Oxalyl chloride (0.459 ml, 5.2 mmol) and trace amounts of DMF were added to the mixture under ice-cooling and the mixture was reacted under ice-cooling and at room temperature, each for 30 min. After the solvent was removed under reduced pressure, 5 ml of dichloromethane was added. Under ice- cooling, 4-butylaniline (664 mg, 4.4 mmol) and triethylamine (0.564 ml, 4.4 mmol) were added thereto and the mixture was reacted for 30 min. at room temperature. The reactant was poured into water and extracted with chloroform. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give the desired compound (1.49 g, 97 % yield). !H-NMR (CDC13) 5 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.27-1.39 (m, 2H), 1.51-1.62 (m, 2H), 1.72-1.84 (m, 4H), 2.40-2.46 (m, 2H), 2.56 (t, 2H, J = 7.5 Hz), 3.76 (t, 1H, J = 5.7 Hz), 7.12 (d, 2H, J = 7.8 Hz), 7.33 (s, 1H), 7.42 (d, 2H, J = 8.1 Hz), 7.71-7.73 (m, 2H), 7.83-7.86 (m, 2H). After the compound obtained in Step 2 (1.49 g, 3.9 mmol) was dissolved in 30 ml of ethanol, hydrazine monohydrate (0.591 mg, 11.8 mmol) was added and the mixture was reacted at 50 °C for 3 hours. The solvent was removed, 1 mol/1 aqueous NaOH was added and the solution was extracted with ethyl acetate. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure to give the desired compound (808 mg, 83 % yield) !H-NMR (CD3OD) 6 ppm: 0.93 (t, 3H, J = 7.2 Hz), 1.28-1.40 (m, 2H), 1.50-1.62 (m, 4H), 1.67-1.77 (m, 2H), 2.37 (t, 2H, J = 7.5 Hz), 2.56 (t, 2H, J = 7.8 Hz), 2.68 (t, 2H, J = 7.2 Hz), 7.11 (d, 2H, J = 8.1 Hz), 7.42 (d, 2H, J = 8.4 Hz). Step 4 The compound obtained in Step 3 (808 mg, 3.25 mmol) was suspended in 5 ml of dichloromethane under ice-cooling and isopropylsulfonyl chloride (696 mg, 4.9 mmol) and triethylamine (494 mg, 4.9 mmol) were added. After the mixture was reacted under ice-cooling for an hour, the reactant was poured into water and extracted with chloroform. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give the desired compound quantitatively. !H-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.27-1.40 (m, 2H), 1.36 (d, 6H, J = 6.6 Hz), 1.51-1.69 (m, 4H), 1.77-1.86 (m, 2H), 2.38 (t, 2H, J = 7.2 Hz), 2.56 (t, 2H, J = 7.5 Hz), 3.12-3.21 (m, 3H), 4.38 (t, 1H, J = 5.7 Hz), 7.11 (d, 2H, J = 8.4 Hz), 7.36-7.41 (m, 3H). Example 2 Synthesis of Compound (I-10) The desired compound was synthesized in a similar manner to Step 4 in Example 1 except that tert-butylsulfinyl chloride (689 mg, 4.9 mmol) and triethylamine (494 mg, 4.9 mmol) were added to the compound obtained in Step 3 in Example 1. !H-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.22 (s, 9H), 1.30-1.37 (m, 2H), 1.51- . 1.68 (m, 4H), 1.76-1.86 (m, 2H), 2.31-2.40 (m, 2H), 2.56 (t, 2H, J = 7.5 Hz), 3.15-3.26 (m, 3H), 7.11 (t, 2H, J = 8.7 Hz), 7.42 (d, 2H, J = 8.1 Hz), 7.54 (s, 1H). Example 3 Synthesis of Compound (I-11) The compound obtained in Example 2 (352 mg, 1.0 mmol) was dissolved in 5 ml of dichloromethane under ice-cooling and mCPBA (259 mg, 1.5 mmol) was added to the 5 solution. The solution was reacted at room temperature for an hour and the insoluble material was filtered off. The filtrate was washed with 1 mol/1 NaOH, Na2S2C>5 and water, successively, and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give the desired compound (338 mg, 92 % yield). ) iH-NMR (CDC13) Sppm: 0.91 (t, 3H, J = 7.5 Hz), 1.29-1.39 (m, 2H), 1.39 (s, 9H), 1.51-1.68 (m, 4H), 1.76-1.84 (m, 2H), 2.37 (t, 2H, J = 7.5 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.19-3.26 (m, 2H), 4.20 (t, 1H, J = 5.7 Hz), 7.11 (t, 2H, J = 8.1 Hz), 7.42 (d, 2H, J = 8.7 Hz), 7.46 (s, 1H). Example 4 Synthesis of Compound (1-72) Step 1 Starting material amino acid (a mixture of cis isomer and trans isomer) (1.0 g, 8.53 mmol) was dissolved in 7.5 ml of methanol. Thionyl chloride (1.0 ml, 13.7 mmol) was added to the mixture under ice-cooling and the mixture was stirred at room temperature overnight. After the mixture was concentrated under reduced pressure, diethylether was added and precipitated crystals were obtained by filtration. The crystals were washed with diethylether and dried to give the desired compound (1.25 g, 93 % yield). l-H-NMR (CDCI3) Sppm: 1.50-2.60 (m, 9H), 3.08-3.36 (m, 1H), 3.67 (s, 3H, C02Me of cis isomer), 3.71 (s, 3H, C02Me of trans isomer), 8.15-8.55 (m, 3H). Step 2 The desired sulfonamide (a mixture of cis isomer and trans isomer) was synthesized from starting material methyl ester in similar manners to Step 3 in Example 1 and Example 2. cis isomer iH-NMR (CDCI3) 6 ppm: 1.39 (s, 9H), 1.52-1.99 (m, 8H), 2.43-2.53 (m, 1H), 3.42-3.55 (m, 1H), 3.69 (s, 3H), 3.85 (d, 1H, J = 9.0 Hz). Step 3 Starting material sulfonamide (19.4 g, 70.0 mmol, a mixture of cis isomer and trans isomer) was dissolved in 30 ml of methanol. To the mixture, 28 % sodium methoxide (284 ml, 140.0 mmol) was added and refluxed with stirring under ice-cooling. After the solvent was removed, the residue was diluted with chloroform, and 1 mol/1 HC1 was added with stirring under ice-cooling until pH of an aqueous layer reached 3. The aqueous layer was extracted with chloroform and the organic layer was washed with water and dried over magnesium sulfate anhydride. The obtained crude crystals were recrystallized from hexane-ethyl acetate to give the desired sulfonamide (trans isomer, 7.75 g, 40 % yield). trans isomer !H-NMR (CD3OD) 5ppm: 1.16-1.32 (m, 2H), 1.39 (s, 9H), 1.44-1.52 (m, 2H), 1.98-2.09 (m, 2H), 2.14-2.29 (m, 3H), 3.18-3.37 (m, 1H), 3.63 (d, 1H, J = 9.0 Hz), 3.67 (s, 3H). Step 4 Starting material methyl ester (4.77 g, 17.2 mmol) was dissolved in 95 ml of methanol and 1 mol/1 NaOH (43 ml, 43.0 mmol) was added with stirring under ice-cooling. The mixture was stirred at room temperature overnight and concentrated under reduced pressure. After 1 mol/1 HC1 was added with stirring until pH of the mixture reached 3 under ice-cooling, the precipitated crystals were collected by filtration, washed with water and dried. The obtained crude crystals were recrystallized from hexane-ethylacetate to give the desired carboxylic acid (4.20 g, 93 % yield). !H-NMR (CDCI3) 5ppm: 1.18-1.35 (m, 2H), 1.39 (s, 9H), 1.46-1.63 (m, 2H), 2.01-2.14 (m, 2H), 2.14-2.32 (m, 3H), 3.18-3.35 (m, 1H), 3.80 (d, 1H, J = 9.6 Hz). Step 5 A starting material carboxylic acid (5.86 g, 22.3 mmol) was dissolved in 88 ml of dichloromethane at room temperature. To the mixture, oxalyl chloride (2.34 ml, 26.7 mmol) and catalytic amount of DMF were added under ice-cooling and stirred at room temperature for an hour. After the solvent was removed under reduced pressure, dichloromethane (115 ml), substituted aniline (5.05 g, 24.5 mmol) and triethylamine (4.65 ml, 33.4 mmol) were added. The mixture was stirred at room temperature for 2.5 hours, the ice-cooling water was poured thereto, and the mixture was extracted with chloroform. An organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and ethyl acetate and hexane were added to the residue. The precipitated crystals were collected with filtration to give the desired amide (7.00 g, 70 % yield). !H-NMR (CDC13) 5ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.17-1.42 (m, 2H), 1.40 (s, 9H), 1.60-1.78 (m, 2H), 1.98-2.43 (m, 7H), 3.20-3.43 (m, 3H), 3.67 (d, 1H, J = 9.6 Hz), 3.74-3.86 (m, 2H), 6.86 (d, 2H, J = 9.0 Hz), 7.04 (s, 1H), 7.38 (d, 2H, J = 9.0 Hz). Example 5 Synthesis of Compound (1-2) Step 1 After starting material diamine (461 mg, 2.5 mmol) was suspended in dichloromethane under ice-cooling, an acid chloride (500 mg, 2.5 mmol) and triethylamine (773 mg, 7.5 mmol) were added and the mixture was reacted for 30 min. Water and dichloromethane were added to the reactant and insoluble materials were filtered off. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure to give the desired compound as a residue (100 mg, 15 % yield). iH-NMR (CDCI3) 6 ppm: 0.93 (t, 3H, J = 7.2 Hz), 1.30-1.42 (m, 2H), 1.57-1.67 (m, 2H), 2.66 (t, 2H, J = 7.8 Hz), 3.50 (brs, 1H), 6.57 (s, 1H), 6.68 (d, 2H, J = 8.7 Hz), 7.26 (d, 2H, J = 8.4 Hz), 7.39 (d, 2H, J = 8.7 Hz), 7.68 (s, 1H), 7.75 (d, 2H, J = 8.1 Hz). Step 2 t The desired compound was synthesized in a similar manner to Step 4 in Example 1. !H-NMR (CDCI3) 5 ppm: 0.94 (t, 3H, J = 7.5 Hz), 1.34-1.44 (m, 2H), 1.40 (d, 6H, J = 6.6 Hz), 1.59-1.68 (m, 2H), 2.69 (t, 2H, J = 7.8 Hz), 3.24-3.35 (m, 1H), 6.49 (s, 1H), 7.23-7.32 (m, 4H), 7.6 (d, 2H, J = 8.7 Hz), 7.79 (d, 2H, J = 8.1 Hz), 7.85 (s, 1H). Example 6 Synthesis of Compound (1-31) Step 1 A starting material diamine (8.37 g, 73.3 mmol) was dissolved in 30 ml of dioxane at room temperature and a solution of B0C2O (2 g, 9.2 mmol) in dioxane (30 ml) was added. The mixture was reacted at room temperature for 3 days and the solvent was removed. Water was added to the residue and the mixture was extracted with chloroform. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure to give the desired compound as a residue (1.8 g, 92 % yield based on B0C2O) !H-NME (CDCI3) 6 ppm: 1.07-1.26 (m, 6H), 1.44 (s, 9H), 1.84-2.00 (m, 4H), 2.58-2.67 (m, 1H), 3.37 (brs, 1H), 4.43 (brs, 1H). Step 2 The desired compound was synthesized in a similar manner to Step 1 in Example 5. !H-NMR (CDCI3) 5 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.26-1.42 (m, 6H), 1.45 (s, 9H), 1.54-1.68 (m, 2H), 1.99-2.12 (m, 4H), 2.64 (t, 2H, J = 7.8 Hz), 3.43 (brs, 1H), 3.90-4.00 (m, 1H), 4.48 (d, 1H, J = 5.7 Hz), 5.95 (d, 1H, J = 8.4 Hz), 7.21 (d, 2H, J = 8.4 Hz), 7.65 (d, 2H, J = 8.4 Hz). Step 3 A starting material Boc compound (2.08 g, 5.55 mmol) was dissolved in 20 ml of ethyl acetate under ice-cooling and 20 ml of 4mol/l HCl/AcOEt was added. The mixture was reacted at room temperature for an hour and the solvent was removed under reduced pressure to give the desired compound as a residue (1.7 g, 98 % yield). iH-NMR (CD3OD) 6 ppm: 0.93 (t, 3H, J = 7.2 Hz), 1.29-1.41 (m, 2H), 1.50-1.66 (m, 6H), 2.02-2.18 (m, 4H), 2.66 (t, 2H, J = 7.8 Hz), 3.13 (brs, 1H), 3.82-3.94 (m, 1H), 7.26 (d, 2H, J = 8.7 Hz), 7.72 (d, 2H, J = 8.4Hz). Step 4 The desired compound was synthesized in a similar manner to Step 4 in Example 1. !H-NMR (CDCI3) 6 ppm: 0.92 (t, 3H, J = 7.5 Hz), 1.21 (s, 9H), 1.28-1.62 (m, 8H), 2.07-2.14 (m, 4H), 2.64 (t, 2H, J= 7.8 Hz), 3.11 (d, 1H, J= 5.1 Hz), 3.20 (brs, 1H), 3.90-4.04 (m, 1H), 6.06-6.14 (m, 1H), 7.21 (t, 2H, J = 8.1 Hz), 7.67 (t, 2H, J = 8.4 Hz). 5 Example 7 Synthesis of Compound (1-32) The desired compound was synthesized from the compound obtained in Example 6 in a similar manner to Example 3. !H-NMR (CDCI3) 5 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.27-1.65 (m, 8H), 1.40 (s, 9H), 2.10-1 2.23 (m, 4H), 2.65 (t, 2H, J = 7.5 Hz), 3.23-3.35 (m, 1H), 3.49 (s, 1H), 3.88-4.02 (m, 1H), 5.84-5.92 (m, 1H), 7.13 (t, 2H, J = 8.4 Hz), 7.65 (d, 2H, J = 8.1 Hz). Example 8 Synthesis of Compound (1-5) Step 1 The desired compound was synthesized in a similar manner to Step 2 in Example 1. !H-NMR (CDCI3) 6 ppm: 0.94 (t, 3H, J = 7.5 Hz), 1.30-1.42 (m, 2H), 1.50-1.65 (m, 2H), 2.61 (t, 2H, J = 7.8 Hz), 7.20 (d, 2H, J = 7.2 Hz), 7.48-7.51 (m, 3H), 7.72 (s, 1H), 7.88-7.90 (m, 1H). Step 2 To a mixture of a starting material nitro compound (593 mg, 1.95 mmol) and tin (358 mg, 3.0 mmol), 30 ml of 6 mol/1 HC1 and 6 ml of THF were added and reacted at 50 °C for 3 hours. After cooling, the solvent was removed and the residue was neutralized 10 % with NaOH and extracted with chloroform. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give the desired compound (110 mg, 21 % yield). !H-NMR (CDC13) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.26-1.39 (m, 2H), 1.49-1.59 (m, 2H), 2.50 (t, 2H, J = 7.8 Hz), 4.37 (s, 1H), 6.65 (d, 2H, J = 8.4 Hz), 6.97 (d, 2H, J = 8.4 Hz), 7.14 (d, 1H, J = 8.4 Hz), 7.43 (d, 1H, J = 8.7 Hz). Step 3 The desired compound was synthesized in a similar manner to Step 4 in Example 1. 1 J-H-NMR (CDCI3) 6 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.28-1.41 (m, 2H), 1.46 (d, 6H, J = 6.9 Hz), 1.53-1.63 (m, 2H), 2.59 (t, 2H, J = 7.8 Hz), 3.35-3.44 (m, 1H), 7.15 (d, 2H, J = 8.7 Hz), 7.38 (s, 1H), 7.45 (d, 2H, J = 8.7 Hz), 7.57 (s, 1H). Example 9 Synthesis of Compound (1-4) Step 1 The desired compound was synthesized in a similar manner to Step 4 in Example 1. iH-NMR (CDCI3) 5 ppm: 1.44 (d, 6H, J = 6.9 Hz), 3.33-3.43 (m, 1H), 3.88 (s, 9H), 6.24-6.26 (m, 1H), 7.11-7.14 (m, 2H). Step 2 The desired compound was synthesized in a similar manner to Step 4 in Example 4. !H-NMR (CDCI3) 6 ppm: 1.44 (d, 6H, J = 6.3 Hz), 3.33-3.45 (m, 1H), 6.25-6.28 (m, 1H), 7.27-7.28 (m, 1H), 7.51 (s, 1H). Step 3 The desired compound was synthesized in a similar manner to Step 2 in Example 1. !H-NMR (CD3OD) 6 ppm: 0.92 (t, 3H, J = 6.9 Hz), 1.28-1.41 (m, 2H), 1.46 (d, 6H, J = 6.3 Hz), 1.53-1.63 (m, 2H), 2.58 (t, 2H, J = 7.8 Hz), 3.33-3.43 (m, 1H), 6.27-6.29 (m, 1H), 7.14-7.16 (m, 3H), 7.50 (d, 2H, J = 8.4 Hz), 7.90 (s, 1H). Example 10 Synthesis of Compound (1-28) Step 1 The desired compound was synthesized in a similar manner to Step 1 in Example 1. iH-NMR (CDCI3) 5ppm: 1.37-1.52 (m, 3H), 1.74-1.79 (m, 2H), 2.07-2.13 (m, 2H), 2.28-2.42 (m, 2H), 3.72-3.81 (m, 1H), 4.09-4.20 (m, 1H), 7.68-7.73 (m, 2H), 7.81-7.85 (m, 2H). Step 2 4-butylphenyl isocyanate (2.85 g, 16.3 mmol) was dissolved in 30 ml of THF, and a starting material alcohol (1.0 g, 4.08 mmol) and bis(tributyltin)oxide (972 mg, 1.63 mmol) were added. After the mixture was stirred overnight, the solvent was removed, water was added and the solution was extracted with chloroform. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give the desired compound (332 mg, 19 % yield). !H-NMR (CDCI3) 5ppm: 0.92 (t, 3H, J = 6.9 Hz), 1.30-1.40 (m, 2H), 1.48-1.62 (m, 4H), 1.79-1.83 (m, 2H), 2.21-2.25 (m, 2H), 2.37-2.50 (m, 2H), 2.57 (t, 2H, J = 7.8 Hz), 4.11-4.22 (m, 1H), 4.77-4.87 (m, 1H), 6.49 (s, 1H), 7.11 (d, 2H, J = 8.7 Hz), 7.28 (d, 2H, J = 8.7 Hz), 7.69-7.73 (m, 2H), 7.80-7.84 (m, 2H). Step 3 The desired compound was synthesized in similar manners to Step 3 in Example 1 and Example 2. iH-NMR (CDC13) Sppm: 0.91 (t, 3H, J = 7.2 Hz), 1.21 (s, 9H), 1.30-1.62 (m, 8H), 2.08 (d, 4H, J = 11.1 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.04 (d, 1H, J = 4.8 Hz), 3.20-3.30 (m, 1H), 4.65-4.76 (m, 1H), 6.57 (s, 1H), 7.10 (d, 2H, J = 8.7 Hz), 7.26 (d, 2H, J = 8.1Hz). The desired compound was synthesized in a similar manner to Example 3. iH-NMR (CDCI3) Sppm: 0.91 (t, 3H, J = 7.2 Hz), 1.23-1.62 (m, 8H), 1.40 (s, 9H), 2.12 (d, 4H, J = 14.4 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.28-3.40 (m, 1H), 3.90 (s, 1H), 4.60-4.73 (m, 1H), 6.57 (s, 1H), 7.10 (d, 2H, J = 8.4 Hz), 7.25 (d, 2H, J = 8.4Hz). Example 12 Synthesis of Compound (1-114) Lawesson's reagent [2,4-bis(4-methoxyphenyl)-l,3-dithia-2,4-diphosphetane-2,4- disulfide] (132 mg) was added to a solution of 100 mg of Compound (I-110) synthesized in a similar manner to Example 1 in toluene (2.7 ml) and the mixture was stirred at 80 °C for 3 hours. The reactant was concentrated under reduced pressure and the residue was purified by silica gel chromatography (ethyl acetate: n-hexane=l:l) to give pale yellow crystals (82.3 mg, 79 %). The crystals were recrystallized from methylene chloride-diisopropyl ether to give the desired compound as colorless needles (50.5 mg, 48 %). Example 13 Synthesis of Compound (1-120) Step 1 Ethyl 4-amino-l-piperidinecarboxylate (300 mg) and triethylamine (258 mg) were dissolved in 5 ml of dichloromethane. To the mixture, 2 ml of solution of t-butylsulfinyl chloride (222 mg) in dichloromethane was added and the mixture was stirred at room temperature for 4 hours. The solution was partitioned into an aqueous solution of potassium hydrogen sulfate and ethyl acetate. The organic layer was washed with brine and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give 378 mg of 4-t-butylsulfiny amino-1-ethoxycarbonyl piperidine. Step 2 In a mixture of 5 ml of 2-propanol and 5 ml of water, 378 mg of 4-t-butylsulfinylamino-1-ethoxycarbonyl piperidine was suspended and 1.77 g of barium hydroxide was added. The mixture was refluxed with stirring and heating for 4 hours. The mixture was diluted with methanol and the insoluble material was filtered off. The solvent was removed under reduced pressure to give 4-t-butylsulfinylaminopiperidine. Without purification, the obtained material was dissolved in 5 ml of THF, and 984 mg of N-phenoxycarbonyl-4-butyl aniline and 236 mg of diisopropyl ethylamine were added, followed by stirring at room temperature overnight. An aqueous solution of potassium hydrogen sulfate was added to the mixture and the mixture was extracted with ethyl acetate. The organic layer was washed with brine and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give 291 mg of 4-t-butylsulfinylaminopiperidine-1-carboxlic acid(4-t-butylphenyl)amide. !H-NMR (CDC13) 5 ppm:0.89(t, 3H, J = 7.3Hz), 1.19(8, 9H), 1.25-1.38(m, 4H), 1.40-1.60(m, 4H), 1.89-2.03(m, 3H), 2.52(t, 2H, J = 7.7Hz), 2.89-3.04(m, 2H), 3.14(d, 1H, J = 5.2 Hz), 3.37(m, 1H), 3.96(m, 2H), 6.67(s, 1H), 7.05(d, 2H, J = 8.5Hz), 7.22(d, 2H, J = 8.5Hz). Step 3 In a mixture of 2 ml of methanol and 2 ml of methylene chloride, 291 mg of 4-t-butylsulfinyl aminopiperidine-1-carboxlic acid(4-t-butylphenyl)amide was dissolved. To the mixture, 570 mg of 80%-MMPP (magnesium monoperoxyphthalate hexahydrate) was added and the mixture was stirred at room temperature for 2 hours. The solution was diluted with water and extracted with ethyl acetate. The organic layer was washed with brine and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give 130 mg of 4-t-butylsulfonylaminopiperidine-l-carboxylic acid(4-butylphenyl)amide (1-120). Other Compounds (I) are synthesized by the similar methods. The structures and physical properties are shown below. ^% 1-2 1h-NMR (CDCI3) 6 ppm: 0.94 (t, 3H, J = 7.5 Hz), 1.34-1.44 (m, 2H), 1.40 (d, 6H, J = 6.6 Hz), 1.59-1.68 (m, 2H), 2.69 (t, 2H, J= 7.8 Hz), 3.24-3.35 (m, IH), 6.49 (s, IH), 7.23-7.32 (m, 4H), 7.6 (d, 2H, J = 8.7 Hz), 7.79 (d, 2H, J = 8.1 Hz), 7.85 (s, IH). 1-3 1h-NMR (CDCI3) 5 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.30-1.39 (m, 2H), 1.37 (d, 6H, J = 6.9 Hz), 1.57 (quint, 2H, J = 7.5 Hz), 1.96 (quint, 2H, J = 6.6 Hz), 2.49 (t, 2H, J = 6.6 Hz), 2.57 (t, 2H, J = 7.8 Hz), 3.16-3.26 (m, 3H), 4.62 (brs, IH), 7.12 (d, 2H, J= 8.1 Hz), 7.43 (d, 2H, J = 8.4 Hz), 7.64 (s, IH). 1-4 1h-NMR (CD3OD) 5 ppm: 0.92 (t, 3H, J = 6.9 Hz), 1.28-1.41 (m, 2H), 1.46 (d, 6H, J = 6.3 Hz), 1.53-1.63 (m, 2H), 2.58 (t, 2H, J = 7.8 Hz), 3.33-3.43 (m, IH), 6.27-6.29 (m, IH), 7.14- 7.16 (m, 3H), 7.50 (d, 2H, J = 8.4 Hz), 7.90 (s, IH). 1-5 1h-NMR (CDCI3) 5 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.28-1.41 (m, 2H), 1.46 (d, 6H, J = 6.9 Hz), 1.53-1.63 (m, 2H), 2.59 (t, 2H, J = 7.8 Hz), 3.35-3.44 (m, IH), 7.15 (d, 2H, J = 8.7 Hz), 7.38 (s, IH), 7.45 (d, 2H, J = 8.7 Hz), 7.57 (s, IH). 1-6 1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.29-1.39 (m, 2H), 1.37 (d, 6H, J = 6.9 Hz), 1.55 (quint, 2H, J = 7.5 Hz), 2.55 (t, 2H, J = 5.1 Hz), 3.18-3.27 (m, IH), 3.92 (d, 2H, J = 6.0 Hz), 5.51 (t, IH, J = 5.7 Hz), 7.10 (d, 2H, J = 8.4 Hz), 7.39 (d, 2H, J = 8.4 Hz), 8.23 (s, IH). 1-7 1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.28-1.38 (m, 2H), 1.37 (d, 6H, J = 6.9 Hz), 1.51-1.67 (m, 4H), 1.78-1.88 (m, 2H), 2.39 (t, 2H, J = 7.2 Hz), 2.57 (t, 2H, J = 7.5 Hz), 3.12-3.22 (m, 3H), 4.30-4.37 (m, IH), 7.12 (d, 2H, J = 8.4 Hz), 7.36-7.42 (m, 3H). 1-8 1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.21-1.47 (m, 4H), 1.35 (d, 6H, J = 6.6 Hz), 1.51-1.63 (m, 4H), 1.67-1.77 (m, 2H), 2.34 (t, 2H, J = 7.5 Hz), 2.55 (t, 2H, J = 7.8 Hz), 3.08-3.17 (m, 3H), 4.71 (t, 1H, J = 6.0 Hz), 7.09 (d, 2H, J = 8.1 Hz), 7.43 (d, 2H, J = 8.4 Hz), 7.74 (s, 1H). 1-9 1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.29-1.39 (m, 2H), 1.35 (d, 6H, J = 6.9 Hz), 1.50-1.60 (m, 2H), 2.54 (t, 2H, J = 7.8 Hz), 2.64 (t, 2H, J = 5.7 Hz), 3.14-3.23 (m, 1H), 3.41-3.47 (m, 2H), 5.29 (t, 1H, J = 6.3 Hz), 7.10 (d, 2H, J = 8.4 Hz), 7.39 (d, 2H, J = 8.4 Hz), 7.91 (s, 1H). MO 1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.22 (s, 9H), 1.30-1.37 (m, 2H), 1.51- 1.68 (m, 4H), 1.76-1.86 (m, 2H), 2.31-2.40 (m, 2H), 2.56 (t, 2H, J = 7.5 Hz), 3.15-3.26 (m, 3H), 7.11 (t, 2H, J = 8.7 Hz), 7.42 (d, 2H, J = 8.1 Hz), 7.54 (s, 1H). Ml mp : 128-129 °C 1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.29-1.39 (m, 2H), 1.39 (a, 9H), 1.51- 1.68 (m, 4H), 1.76-1.84 (m, 2H), 2.37 (t, 2H, J = 7.5 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.19-3.26 (m, 2H), 4.20 (t, 1H, J = 5.7 Hz), 7.11 (d, 2H, J = 8.1 Hz), 7.42 (d, 2H, J = 8.7 Hz), 7.46 (s, 1H). 1-12 1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.28-1.37 (m, 2H), 1.47-1.68 (m, 6H), 2.23 (t, 2H, J = 7.2 Hz), 2.56 (t, 2H, J = 7.5 Hz), 2.90-2.97 (m, 2H), 5.10 (brs, 1H), 7.11 (d, 2H, J = 8.4 Hz), 7.36 (d, 2H, J = 8.1 Hz), 7.50-7.68 (m, 3H), 7.93 (d, 1H, J = 8.1 Hz), 8.06 (d, 1H, J = 8.4 Hz), 8.24 (d, 1H, J = 7.5 Hz), 8.66 (d, 1H, J = 8.7 Hz). 1-13 1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.28-1.40 (m, 2H), 1.45-1.73 (m, 6H), 2.23 (t, 2H, J = 7.5 Hz), 2.56 (t, 2H, J = 7.8 Hz), 2.88 (s, 6H), 2.88-2.95 (m, 2H), 5.04 (brs, 1H), 7.10 (d, 2H, J = 8.1 Hz), 7.17 (d, 1H, J = 7.2 Hz), 7.37 (d, 2H, J = 8.4 Hz), 7.48-7.54 (m, 2H), 8.23 (d, 1H, J = 7.2 Hz), 8.30 (d, 1H, J = 8.7 Hz), 8.53 (d, 1H, J = 8.4 Hz). 1-14 1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.30-1.43 (m, 6H), 1.36 (d, 6H, J = 6.6 Hz), 1.51-1.62 (m, 4H), 1.67-1.78 (m, 2H), 2.34 (t, 2H, J = 7.5 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.09-3.20 (m, 3H), 4.34 (brs, 1H), 7.10 (d, 2H, J = 8.4 Hz), 7.41-7.44 (m, 3H). 1-15 1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.23 (s, 9H), 1.27-1.80 (m, 12H), 2.30- 2.38 (m, 2H), 2.56 (t, 2H, J= 7.5 Hz), 3.15 (brs, 2H), 7.11 (d, 2H, J = 7.8 Hz), 7.43 (d, 2H, J = 7.8 Hz), 7.59 (s, 1H). 1-16 1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.29-1.44 (m, 6H), 1.39 (s, 9H), 1.51- 1.61 (m, 4H), 1.68-1.78 (m, 2H), 2.35 (t, 2H, J = 7.5 Hz), 2.56 (t, 2H, J = 8.1 Hz), 3.15-3.21 (m, 2H), 4.14-4.23 (m, 1H), 7.11 (d, 2H, J = 7.8 Hz), 7.36-7.44 (m, 3H). 1-19 IH-NMR (CDCI3) 6 ppm: 0.92 (t, 3H, J = 7.5 Hz), 1.21 (s, 9H), 1.30-1.40 (m, 2H), 1.55- 1.72 (m, 6H), 2.64 (t, 2H, J = 7.8 Hz), 3.08-3.33 (m, 3H), 3.42-3.50 (m, 2H), 6.39 (s, 1H), 7.22 (d, 2H, J = 8.4 Hz), 7.69 (d, 2H, J = 8.1 Hz). 1-20 1h-NMR (CDCI3) 5 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.31-1.39 (m, 2H), 1.39 (s, 9H), 1.55- 1.72 (m, 6H), 2.64 (t, 2H, J = 7.8 Hz), 3.24 (quart, 2H, J = 6.6 Hz), 3.48 (quart, 2H, J = 6.6 Hz), 4.21 (t, 1H, J = 6.3 Hz), 6.29 (s, 1H), 7.22 (d, 2H, J = 7.8 Hz), 7.67 (d, 2H, J = 8.1 Hz). 1-21 1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.23 (s, 9H), 1.30-1.42 (m, 2H), 1.50- 2.02 (m, 10H), 2.30-2.42 (m, 1H), 2.57 (t, 2H, J = 8.1 Hz), 3.10 (brs, 1H), 3.57 (brs, 1H), 7.12 (d, 2H, J = 8.4 Hz), 7.41 (d, 2H, J = 7.8 Hz). 1-22 mp : 78-79 °C 1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.30-1.40 (m, 2H), 1.40 (s, 9H), 1.50- 1.65 (m, 4H), 1.70-1.98 (m, 8H), 2.30-2.40 (m, IH), 2.57 (t, 2H, J = 7.5 Hz), 3.58-3.70 (m, IH), 4.16 (d, IH, J = 9.3 Hz), 7.11-7.15 (m, 3H), 7.40 (d, 2H, J = 8.1 Hz). 1-23 1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.21 (s, 9H), 1.21-1.41 (m, 4H), 1.51- 1.64 (m, 4H), 1.86-2.01 (m, 4H), 2.12-2.25 (m, IH), 2.56 (t, 2H, J = 7.5 Hz), 2.87-2.96 (m, IH), 3.00-3.12 (m, IH), 3.23-3.34 (m, IH), 3.67-3.75 (m, IH), 7.11 (d, 2H, J = 8.1 Hz), 7.40 (d, 2H, J = 8.4 Hz). 1-24 1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.25-1.37 (m, 2H), 1.40 (s, 9H), 1.48- 1.65 (m, 6H), 1.90 (d, 2H, J = 11.7 Hz), 2.02 (d, 2H, J = 11.7 Hz), 2.12-2.24 (m, IH), 2.56 (t, 2H, J = 7.5 Hz), 3.04 (t, 2H, J = 6.3 Hz), 4.31 (t, IH, J = 5.7 Hz), 7.11 (d, 2H, J = 8.1 Hz), 7.42 (d,2H, J = 8.4 Hz). 1-25 mp : 232-233 °C 1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.23-1.40 (m, 4H), 1.40 (s, 9H), 1.51- 1.76 (m, 4H), 2.01-2.26 (m, 5H), 2.56 (t, 2H, J = 7.5 Hz), 3.22-3.38 (m, IH), 3.79 (d, IH, J = 9.3 Hz), 7.11 (d, 2H, J= 8.7 Hz), 7.17 (s, IH), 7.40 (d, 2H, J = 8.4 Hz). 1-26 1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.22 (s, 9H), 1.28-1.40 (m, 2H), 1.52- 1.62 (m, 2H), 1.85-1.96 (m, IH), 2.00-2.14 (m, IH), 2.38-2.53 (m, 2H), 2.56 (t, 2H, J = 7.5 Hz), 3.22-3.37 (m, 3H), 7.11 (d, 2H, J = 8.4 Hz), 7.45 (d, 2H, J = 8.4 Hz), 8.19 (s, IH). 1-27 1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.30-1.40 (m, 2H), 1.40 (s, 9H), 1.52- 1.61 (m, 2H), 1.95 (quint, 2H, J = 6.3 Hz), 2.50 (t, 2H, J = 6.9 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.31 (quart, 2H, J = 6.0 Hz), 4.30-4.36 (m, IH), 7.12 (d, 2H, J = 8.4 Hz), 7.43 (d, 2H, J = 8.4 Hz), 7.65 (s, IH). 1-28 1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J= 7.2 Hz), 1.21 (s, 9H), 1.30-1.62 (m, 8H), 2.08 (d, 4H, J = 11.1 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.04 (d, IH, J = 4.8 Hz), 3.20-3.30 (m, IH), 4.65- 4.76 (m, IH), 6.57 (s, IH), 7.10 (d, 2H, J = 8.7 Hz), 7.26 (d, 2H, J = 8.1Hz). 1-29 1h-NMR (CDCI3) 5ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.23-1.62 (m, 8H), 1.40 (s, 9H), 2.12 (d, 4H, J = 14.4 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.28-3.40 (m, IH), 3.90 (s, IH), 4.60-4.73 (m, IH), 6.57 (s, IH), 7.10 (d, 2H, J = 8.4 Hz), 7.25 (d, 2H, J = 8.4Hz). 1-30 1h-NMR (CDCI3) Sppm: 0.91 (t, 3H, J = 7.5 Hz), 1.26-1.39 (m, 2H), 1.51-1.64 (m, 4H), 1.72-1.81 (m, 2H), 2.34 (t, 2H, J = 6.9 Hz), 2.56 (t, 2H, J = 7.8 Hz), 2.95-3.01 (m, 2H), 4.84 (t, IH, J = 5.7 Hz), 6.99-7.12 (m, 6H), 7.19-7.24 (m, IH), 7.30 (s, IH), 7.38-7.43 (m, 4H), 7.79 (d, 2H, J = 8.7 Hz). 1-31 XH-NMR (CDCI3) 5 ppm: 0.92 (t, 3H, J = 7.5 Hz), 1.21 (s, 9H), 1.28-1.62 (m, 8H), 2.07- 2.14 (m, 4H), 2.64 (t, 2H, J = 7.8 Hz), 3.11 (d, IH, J = 5.1 Hz), 3.20 (brs, IH), 3.90-4.04 (m, IH), 6.06-6.14 (m, IH), 7.21 (t, 2H, J = 8.1 Hz), 7.67 (t, 2H, J = 8.4 Hz). 1-32 1h-NMR (CDCI3) 6 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.27-1.65 (m, 8H), 1.40 (s, 9H), 2.10- 2.23 (m, 4H), 2.65 (t, 2H, J = 7.5 Hz), 3.23-3.35 (m, IH), 3.49 (s, IH), 3.88-4.02 (m, IH), 5.84-5.92 (m, IH), 7.13 (t, 2H, J = 8.4 Hz), 7.65 (d, 2H, J = 8.1 Hz). 1-33 1h-NMR (CDCI3) 6 ppm: 0.94 (t, 3H, J = 7.2 Hz), 1.30-1.42 (m, 2H), 1.32 (s, 9H), 1.57- 1.66 (m, 2H), 2.67 (t, 2H, J = 7.8 Hz), 5.61 (s, IH), 6.93 (d, 2H, J = 8.7 Hz), 7.25 (d, 2H, J = 8.4 Hz), 7.49 (d, 2H, J = 9.0 Hz), 7.80 (d, 2H, J = 8.1 Hz), 8.22 (s, IH). 1-34 1h-NMR (CD3OD) 5 ppm: 0.95 (t, 3H, J = 7.5 Hz), 1.35 (s, 9H), 1.35-1.44 (m, 2H), 1.57- 1.69 (m, 2H), 2.69 (t, 2H, J = 7.5 Hz), 7.28-7.33 (m, 4H), 7.56 (d, 2H, J = 9.0 Hz), 7.83 (d, 2H, J = 8.4 Hz). 1-36 1h-NMR (CDCI3) 6 ppm: 0.92 (t, 3H, J = 7.5 Hz), 1.31-1.70 (m, 11H), 1.39 (s, 9H), 1.75- 1.85 (m, IH), 2.65 (t, 2H, J = 8.1 Hz), 3.13 (t, 2H, J = 6.6 Hz), 3.40 (t, 2H, J = 7.2 Hz), 4.10 (t, IH, J = 5.7 Hz), 6.21 (t, IH, J = 5.7 Hz), 7.23 (d, 2H, J = 8.1 Hz), 7.67 (d, 2H, J = 8.4 Hz). 1-37 1h-NMR (CDCI3) 6 ppm: 0.92 (t, 3H, J = 7.5 Hz), 0.95-1.10 (m, 2H), 1.31-1.40 (m, 2H), 1.39 (s, 9H), 1.55-1.63 (m, 4H), 1.80-1.92 (m, 4H), 2.65 (t, 2H, J = 7.8 Hz), 3.03 (t, 2H, J = 6.6 Hz), 3.31 (t, 2H, J = 6.6 Hz), 4.06 (t, IH, J = 6.0 Hz), 6.22 (t, IH, J = 6.0 Hz), 7.23 (d, 2H, J = 8.4 Hz), 7.67 (d, 2H, J = 8.1 Hz). 1-39 1h-NMR (CDCI3) 6 ppm: 1.13 (t, 3H, J = 7.2 Hz), 1.39 (s, 9H), 1.69-1.97 (m, 8H), 2.27- 2.38 (m, IH), 3.29-3.35 (m, 4H), 3.60-3.70 (m, IH), 4.52 (d, IH, J = 9.3 Hz), 6.64 (d, 2H, J = 8.4 Hz), 7.22 (s, IH), 7.31 (d, 2H, J = 9.0 Hz). 1-40 1h-NMR (CDCI3) 6 ppm: 1.38 (s, 9H), 1.68-1.96 (m, 8H), 2.30-2.40 (m, IH), 3.11 (t, 4H, J = 4.8 Hz), 3.60-3.72 (m, IH), 3.86 (t, 4H, J = 4.8 Hz), 4.51 (brs, IH), 6.89 (d, 2H, J = 9.0 Hz), 7.42 (d, 2H, J = 8.7 Hz). 1-41 mp : >278 °C (dec.) 1h-NMR (CDCI3) 5 ppm: 1.18-1.40 (m, 2H), 1.40 (s, 9H), 1.62-1.75 (m, 2H), 2.01-2.27 (m, 5H), 3.10-3.13 (m, 4H), 3.22-3.38 (m, IH), 3.72 (d, IH, J= 9.3 Hz), 3.85-3.88 (m, 4H), 6.87 (d, 2H, J = 9.0 Hz), 7.10 (s, IH), 7.40 (d, 2H, J = 9.0 Hz). 1-42 1h-NMR (CDCI3) 6ppm: 1.40 (s, 9H), 1.61-1.97 (m, 8H), 2.16 (s, 3H), 2.33-2.43 (m, IH), 3.60-3.70 (m, IH), 4.66 (brs, IH), 7.12 (d, IH, J = 8.7 Hz), 7.46-7.50 (m, IH), 7.62 (s, H), 7.75-7.78 (m, IH), 7.86-7.91 (m, 2H). 1-43 1h-NMR (CDCI3) 5 ppm: 1.40 (s, 9H), 1.62-2.00 (m, 8H), 1.87 (s, 3H), 2.36-2.47 (m, IH), 3.24 (s, 3H), 3.64-3.74 (m, IH), 4.87 (brs, IH), 7.13 (d, 2H, J = 9.0 Hz), 7.64 (d, 2H, J = 8.4 Hz), 7.81 (s, H). 1-44 mp : 235-236 °C 1h-NMR (CDCI3) 5 ppm: 1.13 (t, 6H, J = 6.9 Hz), 1.18-1.33 (m, 2H), 1.40 (s, 9H), 1.60- 1.77 (m, 2H), 2.00-2.26 (m, 5H), 3.28-3.35 (m, 4H), 3.73 (d, IH, J = 9.3 Hz), 6.60-6.70 (m, 2H), 7.03 (brs, IH), 7.31 (d, 2H, J = 7.8 Hz). 1-45 mp : >268 °C (dec.) 1h-NMR (CDCI3) 6 ppm: 1.20-1.34 (m, 2H), 1.40 (s, 9H), 1.56-1.76 (m, 8H), 2.00-2.26 (m, 5H), 3.06-3.14 (m, 4H), 3.24-3.36 (m, IH), 3.72 (d, IH, J = 9.3 Hz), 6.90 (d, 2H, J = 8.7 Hz), 7.09 (s, IH), 7.36 (d, 2H, J = 8.7 Hz). 1-46 mp : >272 °C (dec.) 1h-NMR (DMSO-d6) 6 ppm: 1.28 (s, 9H), 1.31-1.59 (m, 7H), 1.87-2.00 (m, 4H), 2.23-2.34 (m, IH), 3.00-3.16 (m, IH), 4.35-4.45 (m, 2H), 6.81 (d, IH, J = 9.0 Hz), 7.16 (t, IH, J = 7.2 Hz), 7.43 (t, IH, J = 8.4 Hz), 7.52-7.58 (m, 3H), 8.04 (d, IH, J = 7.8 Hz), 8.43 (s, IH). 1-47 1h-NMR (CDCI3) 5 ppm: 1.20-1.36 (m, 2H), 1.40 (s, 9H), 1.62-1.77 (m, 2H), 1.98-2.32 (m, 5H), 3.31-3.40 (m, IH), 3.62 (d, IH, J = 9.0 Hz), 7.08 (s, IH), 7.29 (d, 2H, J = 9.0 Hz), 7.61 (d, 2H, J = 9.0 Hz). 1-48 1h-NMR (CDCI3) 6ppm: 1.22-1.36 (m, 2H), 1.40 (s, 9H), 1.62-1.77 (m, 2H), 2.00-2.31 (m, 5H), 3.24-3.40 (m, IH), 3.62 (d, IH, J = 10.2 Hz), 7.01 (t, 2H, J = 8.7 Hz), 7.09 (s, IH), 7.42-7.50 (m, 2H). 1-49 mp:270°C (dec.) 2H-NMR (CDCI3) 5ppm: 1.20-1.36 (m, 2H), 1.40 (s, 9H), 1.61-1.77 (m, 2H), 1.95-2.30 (m, 9H), 3.17-3.38 (m, 5H), 3.67 (d, IH, J = 9.3 Hz), 6.50 (d, 2H, J = 9.0 Hz), 6.97 (s, IH), 7.30 (d, 2H, J = 9.0 Hz). 1-50 mp : 252-253 °C H-NMR (CDCI3) 5 ppm: 1.21-1.37 (m, 2H), 1.40 (s, 9H), 1.62-1.78 (m, 2H), 1.98-2.32 (m, 5H), 3.26-3.40 (m, IH), 3.68 (d, IH, J = 9.6 Hz), 6.94-7.02 (m, 4H), 7.08 (t, IH, J = 7.5 Hz), 7.13 (s, IH), 7.31 (t, 2H, J = 7.5 Hz), 7.46 (d, 2H, J = 9.0 Hz). 1-51 mp : 278-279 °C 1h-NMR (CDCI3) 6 ppm: 1.02 (d, 6H, J = 6.9 Hz), 1.35 (s, 9H), 1.39-1.71 (m, 6H), 1.90- 2.09 (m, 2H), 3.16-3.30 (m, IH), 3.46 (d, IH, J = 9.0 Hz), 4.92-5.01 (m, IH), 6.91-6.95 (m, 2H), 7.00-7.07 (m, 3H), 7.13-7.16 (m, 2H), 7.30-7.36 (m, 2H). 1-52 mp : 276-277 °C 1h-NMR (CDCI3) 5 ppm: 1.20-1.36 (m, 2H), 1.40 (s, 9H), 1.60-1.78 (m, 2H), 1.98-2.30 (m, 5H), 2.36 (s, 3H), 2.58 (t, 4H, J = 4.5 Hz), 3.17 (t, 4H, J = 4.5 Hz), 3.21-3.40 (m, IH), 3.64 (d, IH, J = 9.0 Hz), 6.88 (d, 2H, J = 9.0 Hz), 7.01 (s, IH), 7.37 (d, 2H, J = 9.0 Hz). 1-53 mp : >300 °C 1h-NMR (DMSO-d6) 5 ppm: 1.20-1.54 (m, 4H), 1.27 (s, 9H), 1.73-1.88 (m, 2H), 1.89-2.01 (m, 2H), 2.13-2.25 (m, IH), 2.98-3.12 (m, IH), 3.15-3.31 (m, 8H), 6.76-6.84 (m, 2H), 6.93 (d, 2H, J = 9.0 Hz), 6.99 (d, 2H, J = 8.1 Hz), 7.24 (d, 2H, J = 8.1 Hz), 7.46 (d, 2H, J = 9.0 Hz), 9.60 (s, IH). 1-54 mp : >215 °C (dec.) 1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.27-2.00 (m, 18H), 2.14-2.26 (m, IH), 2.53-2.84 (m, 4H), 2.86-3.30 (m, 2H), 3.46-3.54 (m, IH), 3.62-3.74 (m, 2H), 6.78 (d, IH, J = 8.7 Hz), 6.87 (d, 2H, J = 7.8 Hz), 7.42 (d, 2H, J = 8.7 Hz), 9.58 (s, IH). 1-55 mp : >290 °C (dec.) 1h-NMR (CDC13) 6 ppm: 1.23-1.40 (m, 2H), 1.40 (s, 9H), 1.60-1.76 (m, 2H), 2.02-2.27 (m, 5H), 3.20 (t, 4H, J = 5.4 Hz), 3.21-3.32 (m, IH), 3.67 (d, IH, J = 9.3 Hz), 3.98 (t, 4H, J = 4.8 Hz), 6.52 (t, IH, J = 4.8 Hz), 6.93 (d, 2H, J = 8.4 Hz), 7.06 (s, IH), 7.41 (d, 2H, J = 8.7 Hz), 8.33 (d, 2H, J = 4.8 Hz). 1-56 mp : >232 °C (dec.) 1h-NMR (DMSO-d6) 5 ppm: 1.27 (s, 9H), 1.27-1.48 (m, 4H), 1.80-1.99 (m, 4H), 2.14-2.25 (m, IH), 3.04-3.24 (m, 8H), 3.68 (s, 3H), 3.76 (s, 3H), 6.44-6.47 (m, IH), 6.66 (s, IH), 6.76- 6.84 (m, 2H), 6.92 (d, 2H, J = 8.4 Hz), 7.46 (d, 2H, J = 8.4 Hz), 9.61 (s, IH). 1-57 mp : 284-285 °C (dec.) 1h-NMR (CDCI3) 6 ppm: 1.27 (t, 3H, J = 7.2 Hz), 1.40 (a, 9H), 1.61-2.24 (m, 9H), 2.35- 2.49 (m, IH), 2.76 (t, 2H, J= 10.2 Hz), 3.04-3.15 (m, 2H), 3.20-3.36 (m, IH), 3.55-3.59 (m, 2H), 3.87 (d, IH, J = 9.6 Hz), 4.12-4.19 (m, 2H), 6.90 (d, 2H, J = 8.7 Hz), 2.79 (s, IH), 7.40 (d, 2H, J = 8.7 Hz). 1-58 mp : >299 °C (dec.) :H-NMR (CDCI3) 5 ppm: 1.26-1.33 (m, 2H), 1.40 (s, 9H), 1.56-2.42 (m, 19H), 2.73-2.81 (m, 4H), 3.16-3.26 (m, 4H), 3.64 (d, IH, J = 9.6 Hz), 6.87 (d, 2H, J = 8.7 Hz), 7.04 (s, IH), 7.37 (d, 2H, J = 9.0 Hz). 1-59 mp : >270 °C (dec.) 1h-NMR (CDCI3) Sppm: 1.26-1.47 (m, 2H), 1.47 (s, 9H), 1.60-1.80 (m, 4H), 2.01-2.32 (m, 5H), 3.28-3.40 (m, 3H), 3.62-3.74 (m, 3H), 5.74-5.96 (m, 2H), 6.92 (d, 2H, J = 8.7 Hz), 7.13 (s, IH), 7.39 (d, 2H, J = 9.0 Hz). 1-60 mp : 247-250 °C (dec.) 1h-NMR (CDCI3) 6 ppm: 1.20-1.37 (m, 2H), 1.40 (s, 9H), 1.60-1.78 (m, 2H), 1.98-2.33 (m, 5H), 2.93-3.03 (m, 2H), 3.22-3.40 (m, IH), 3.52 (t, 2H, J = 6.0 Hz), 3.62 (d, IH, J = 8.4 Hz), 4.36 (s, 2H), 6.93 (d, 2H, J = 8.7 Hz), 7.00 (s, IH), 7.11-7.22 (m, 4H),7.39 (d, 2H, J = 8.7 Hz). 1-61 mp : 280-281 °C 1h-NMR (CDCI3) 6 ppm: 1.21-1.38 (m, 2H), 1.41 (s, 9H), 1.64-1.80 (m, 2H), 2.02-2.33 (m, 5H), 3.24-3.40 (m, IH), 3.61 (d, IH, J = 9.0 Hz), 6.33 (t, 2H, J = 2.1 Hz), 7.04 (t, 2H, J = 2.1 Hz), 7.14 (s, IH), 7.34 (d, 2H, J = 9.0 Hz), 7.56 (d, 2H, J = 9.0 Hz). 1-62 mp : 260-262 °C 1h-NMR (CDCI3) 5 ppm: 1.22-1.39 (m, 2H), 1.41 (s, 9H), 1.64-1.82 (m, 2H), 2.02-2.35 (m, 5H), 3.24-3.40 (m, IH), 3.62 (d, IH, J = 9.6 Hz), 7.31 (d, 2H, J= 9.0 Hz), 7.51 (s, IH), 7.69 (d, 2H, J = 9.0 Hz). 1-63 mp : 248 °C 1h-NMR (CDCI3) Sppm: 1.20-1.38 (m, 2H), 1.40 (s, 9H), 1.61-1.78 (m, 2H), 1.98-2.32 (m, 5H), 3.22-3.45 (m, IH), 3.64 (d, IH, J = 9.3 Hz), 7.11 (s, IH), 7.37-7.46 (m, 4H). 1-64 mp : 272-275 °C (dec.) 1h-NMR (DMSO-d6) 6 ppm: 1.20-1.53 (m, 4H), 1.27 (s, 9H), 1.75-1.88 (m, 2H), 1.88-2.00 (m, 2H), 2.11-2.24 (m, IH), 2.96-3.12 (m, IH), 5.96 (s, 2H), 6.77 (d, IH, J = 8.7 Hz), 6.82 (d, IH, J = 8.4 Hz), 6.95 (dd, IH, J = 1.8, 8.4 Hz), 7.29 (d, IH, J = 1.8 Hz), 9.70 (s, IH). 1-65 mp : 293-296 °C (dec.) 1h-NMR (DMSO-d6) 6 ppm: 1.20-1.70 (m, 10H), 1.27 (s, 9H), 1.79-2.038 (m, 4H), 2.18- 2.33 (m, IH), 2.98-3.30 (m, 5H), 6.79 (d, IH, J = 9.0 Hz), 6.97 (d, 2H, J = 8.1 Hz), 7.43-7.57 (m, 4H), 7.62 (d, 2H, J= 8.1 Hz), 9.82 (s, IH). 1-66 mp : >300 °C 1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.27-1.53 (m, 4H), 1.86-1.99 (m, 4H), 2.22-2.34 (m, IH), 2.39 (s, 3H), 3.00-3.14 (m, IH), 6.25 (s, IH), 6.79 (d, IH, J = 9.0 Hz), 7.47-7.50 (m, IH), 7.69-7.76 (m, IH), 10.27 (s, IH). 1-67 mp : 248-249 °C 1h-NMR (DMSO-d6) 6 ppm: 1.20-1.54 (m, 4H), 1.27 (s, 9H), 1.77-1.90 (m, 2H), 1.90-2.02 (m, 2H), 2.02 (s, 3H), 2.17-2.32 (m, IH), 2.96-3.13 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.12- 7.30 (m, 3H), 7.89 (s, IH), 9.79 (s, IH), 9.88 (s, IH). 1-68 mp :>300 °C 1h-NMR (DMSO-d6) 5 ppm: 1.20-1.54 (m, 4H), 1.27 (s, 9H), 1.77-1.89 (m, 2H), 1.89-2.03 (m, 2H), 2.00 (s, 3H), 2.14-2.28 (m, IH), 2.95-3.13 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.40- 7.54 (m, 4H), 9.72 (s, IH), 9.83 (s, IH). 1-69 mp : 199-201 °C 1h-NMR (DMSO-d6) 6 ppm: 1.21-1.53 (m, 4H), 1.27 (s, 9H), 1.76-1.89 (m, 2H), 1.89-2.02 (m, 2H), 2.13-2.30 (m, 1H), 2.85 (s, 6H), 2.94-3.14 (m, 1H), 6.40 (dd, 1H, J = 2.4, 8.4 Hz), 6.78 (d, 1H, J = 8.7 Hz), 6.90 (d, 1H, J = 8.4 Hz), 7.05 (t, 2H, J = 8.4 Hz), 9.60 (s, 1H). 1-70 mp : 227-230 °C 1h-NMR (DMSO-d6) 6 ppm: 1.22-1.52 (m, 4H), 1.27 (s, 9H), 1.72-1.87 (m, 2H), 1.87-2.01 (m, 2H), 2.12-2.29 (m, 1H), 2.96-3.12 (m, 1H), 5.00 (s, 2H), 6.22 (d, 1H, J = 7.5 Hz), 6.66 (d, 1H, J = 7.5 Hz), 6.78 (d, 1H, J = 9.0 Hz), 6.86 (d, 1H, J = 7.5 Hz), 6.89-6.95 (m, 1H), 9.46 (s, 1H). 1-71 mp : 270-272 °C 1h-NMR (DMSO-dg) 6 ppm: 1.22-1.52 (m, 4H), 1.26 (s, 9H), 1.73-1.86 (m, 2H), 1.88-2.00 (m, 2H), 2.08-2.22 (m, 1H), 2.95-3.11 (m, 1H), 4.80 (s, 2H), 6.47 (d, 2H, J = 8.4 Hz), 6.77 (d, 1H, J = 8.4 Hz), 7.20 (d, 2H, J = 8.4 Hz), 9.35 (s, 1H). 1-72 mp : 262-263 °C 1h-NMR (CDC13) 6 ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.17-1.42 (m, 2H), 1.40 (s, 9H), 1.60- 1.78 (m, 2H), 1.98-2.43 (m, 7H), 3.20-3.43 (m, 3H), 3.67 (d, 1H, J = 9.6 Hz), 3.74-3.86 (m, 2H), 6.86 (d, 2H, J = 9.0 Hz), 7.04 (s, 1H), 7.38 (d, 2H, J = 9.0 Hz). 1-73 mp : 218-219 °C 1h-NMR (CD3OD) 6 ppm: 1.36 (s, 9H), 1.36-1.69 (m, 4H), 1.45 (s, 9H), 1.88-2.02 (m, 3H), 2.06-2.30 (m, 4H), 3.05-3.44 (m, 3H), 3.46-3.56 (m, 1H), 4.16-4.26 (m, 1H), 6.51 (d, 2H, J = 9.0 Hz), 7.30 (d, 2H, J = 8.7 Hz). 1-74 mp : 295-296 °C (dec.) 1h-NMR (CD3OD) 6 ppm: 1.36 (s, 9H), 1.36-1.67 (m, 4H), 1.92-2.13 (m, 4H), 2.26-2.40 (m, 2H), 2.62-2.75 (m, IH), 3.16-3.25 (m, IH), 3.58-3.98 (m, 4H), 4.16-4.25 (m, IH), 7.20-7.30 (m, 2H), 7.62 (d, 2H, J = 9.0 Hz). 1-75 mp : 250-251 °C 1h-NMR (DMSO-d6) 6 ppm: 1.23-1.55 (m, 4H), 1.27 (s, 9H), 1.78-1.90 (m, 2H), 1.90-2.02 (m, 2H), 2.15-2.28 (m, IH), 2.98-3.14 (m, IH), 3.06 (t, 2H, J = 8.4 Hz), 3.87 (t, 2H, J = 8.4 Hz), 6.67 (dd, IH, J= 1.5, 7.2 Hz), 6.80 (d, IH, J = 8.4 Hz), 6.94-7.05 (m, 2H), 7.12-7.19 (m, IH), 7.16 (d, 2H, J = 9.3 Hz), 7.57 (d, 2H, J = 9.3 Hz), 9.73 (s, IH). 1-76 mp : 265-266 °C 1h-NMR (DMSO-dg) 6 ppm: 1.23-1.58 (m, 4H), 1.28 (s, 9H), 1.83-2.04 (m, 4H), 2.20-2.36 (m, IH), 2.97-3.16 (m, IH), 6.67 (d, IH, J = 3.0 Hz), 6.82 (d, IH, J = 8.4 Hz), 7.07-7.22 (m, 2H), 7.47-7.53 (m, IH), 7.50 (d, 2H, J = 9.0 Hz), 7.58 (d, IH, J = 3.0 Hz), 7.64 (d, IH, J = 7.5 Hz), 7.79 (d, 2H, J = 9.0 Hz), 10.02 (s, IH). 1-77 mp :281°C 1-H-NMR (DMSO-dg) Sppm: 1.21-1.56 (m, 4H), 1.27 (s, 9H), 1.80-2.03 (m, 4H), 2.18-2.31 (m, IH), 2.97-3.14 (m, IH), 6.51 (dd, IH, J = 2.1, 2.7 Hz), 6.81 (d, IH, J = 9.0 Hz), 7.67-7.78 (m, 5H), 8.41 (d, IH, J = 2.1 Hz), 9.96 (s, IH). 1-78 mp : >300 °C (dec.) 1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.27-1.52 (m, 4H), 1.74-2.04 (m, 7H), 2.10-2.25 (m, 2H), 2.96-3.20 (m, 2H), 3.48-3.58 (m, IH), 3.75-3.84 (m, IH), 6.39 (d, 2H, J = 8.4 Hz), 6.79 (d, IH, J = 8.4 Hz), 7.02 (s, IH), 7.30 (s, IH), 7.36 (d, 2H, J = 8.1 Hz), 9.48 (s, IH). 1-79 mp : 248-250 °C (dec.) 1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.27-1.54 (m, 4H), 1.85-1.99 (m, 4H), 2.24-2.33 (m, IH), 3.00-3.14 (m, IH), 6.82 (d, IH, J = 8.7 Hz), 7.77 (d, 2H, J = 8.4 Hz), 8.07 (d, 2H, J = 8.4 Hz). 1-80 mp : >300 °C 1h-NMR (DMSO-dg) 6 ppm: 1.22-1.58 (m, 4H), 1.27 (s, 9H), 1.80-2.03 (m, 4H), 2.18-2.32 (m, IH), 2.98-3.14 (m, IH), 6.80 (d, IH, J = 8.7 Hz), 7.35-7.50 (m, 2H), 7.99 (s, IH), 8.11 (s, IH), 9.79 (s, IH), 12.94 (s, IH). 1-81 mp : 261-262 °C 1h-NMR (DMSO-dg) 6 ppm: 1.21-1.57 (m, 4H), 1.27 (s, 9H), 1.78-2.02 (m, 4H), 2.17-2.30 (m, IH), 2.96-3.16 (m, IH), 6.34 (s, IH), 6.80 (d, IH, J = 8.7 Hz), 7.14-7.32 (m, 3H), 7.85 (s, IH), 9.58 (s, IH), 10.95 (s, IH). 1-82 1h-NMR (CDC13) 6 ppm: 0.86 (s, 18H), 1.24-1.37 (m, 2H), 1.37 (s, 9H), 1.56-1.74 (m, 2H), 1.95-2.19 (m, 5H), 3.18-3.32 (m, IH), 3.44 (t, 4H, J = 6.3 Hz), 3.70 (t, 4H, J = 6.3 Hz), 4.39 (d, IH, J = 9.0 Hz), 6.59 (d, 2H, J = 9.0 Hz), 7.31 (d, 2H, J = 8.7 Hz), 7.43 (s, IH). 1-83 mp : 264-265 °C 1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.27-1.52 (m, 4H), 1.78-1.88 (m, 2H), 1.90-2.00 (m, 2H), 2.14-2.26 (m, IH), 2.96-3.14 (m, IH), 6.72-6.82 (m, 2H), 6.99 (t, 4H, J = 7.8 Hz), 7.18 (t, 2H, J = 7.5 Hz), 7.46 (d, 2H, J = 9.0 Hz), 8.00 (s, IH), 9.65 (s, IH). 1-84 mp : 257 °C (dec.) 1h-NMR (DMSO-dg) 5 ppm: 1.23-1.57 (m, 4H), 1.27 (s, 9H), 1.83-2.03 (m, 4H), 2.23-2.35 (m, IH), 2.98-3.15 (m, IH), 6.80 (d, IH, J = 8.1 Hz), 7.87 (d, 2H, J = 9.0 Hz), 8.34 (d, 2H, J = 9.0 Hz), 9.21 (s, IH), 10.20 (s, IH). 1-85 mp : 256-258 °C 1h-NME (DMSO-d6) 6 ppm: 1.22-1.53 (m, 4H), 1.26 (s, 9H), 1.79-2.01 (m, 4H), 2.25 (s, 3H), 2.28-2.42 (m, IH), 2.97-3.02 (m, IH), 6.71 (d, IH, J= 0.9 Hz), 6.80 (d, IH, J = 8.1 Hz), 11.91 (s, IH). 1-86 mp : 228-230 °C 1h-NMR (CD3OD) 6 ppm: 1.36 (s, 9H), 1.36-1.48 (m, 2H), 1.55-1.70 (m, 2H), 1.87-1.98 (m, 2H), 2.08-2.17 (m, 2H), 2.20-2.32 (m, IH), 3.15-3.27 (m, IH), 3.50 (t, 4H, J = 5.7 Hz), 3.69 (t, 4H, J = 5.7 Hz), 6.72 (d, 2H, J = 9.0 Hz), 7.29-7.33 (m, 2H). 1-87 mp : 183-184 °C 1h-NMR (DMSO-d6) 5 ppm: 1.27 (s, 9H), 1.27-1.48 (m, 4H), 1.73-1.89 (m, 4H), 1.90-2.00 (m, 2H), 2.16-2.28 (m, IH), 2.28 (t, 2H, J = 7.5 Hz), 2.51-2.54 (m, 2H), 2.97-3.13 (m, IH), 3.58 (s, 3H), 6.79 (d, IH, J = 8.7 Hz), 7.08 (d, 2H, J = 8.7 Hz), 7.49 (d, 2H, J = 8.4 Hz), 9.73 (s, IH). 1-88 mp : 217-218 °C 1h-NMR (CD3OD) Sppm: 1.36 (s, 9H), 1.36-1.46 (m, 2H), 1.55-1.69 (m, 2H), 1.83-2.00 (m, 4H), 2.07-2.18 (m, 2H), 2.26-2.36 (m, 3H), 2.61 (t, 2H, J = 7.5 Hz), 3.14-3.26 (m, IH), 7.13 (d, 2H, J = 8.1 Hz), 7.44 (d, 2H, J = 8.1 Hz). 1-89 1h-NMR (CDCI3) 6 ppm: 0.08 (d, 6H, J = 3.3 Hz), 0.88(s, 9H), 1.21-1.36 (m, 2H), 1.39 (s, 9H), 1.61-1.74 (m, 2H), 1.88-2.23 (m, 6H), 3.06-3.11 (m, IH), 3.24-3.74 (m, 4H), 3.92 (d, IH, J = 9.6 Hz), 4.48-4.56 (m, IH), 6.47 (d, 2H, J = 9.0 Hz), 7.17 (s, IH), 7.32 (d, 2H, J = 9.0 Hz). 1-90 mp : amorphous 1h-NMR (CD3OD) 5 ppm: 1.36 (s, 9H), 1.36-1.47 (m, 2R), 1.56-1.70 (m, 3H), 1.88-2.30 (m, 6H), 3.05-3.49 (m, 5H), 4.50 (brs, IH), 6.50 (d, 2H, J = 9.0 Hz), 7.29 (d, 2H, J = 9.0 Hz). 1-91 mp : 105-106 °C 1h-NMR (CDCI3) 5 ppm: 0.92(t, 3H, J = 7.3 Hz), 1.25-1.27(m, 2H), 1.36(d, 6H, J = 6.9 Hz), 1.51-1.59(m, 2H), 2.56(t, 2H, J = 7.8 Hz), 3.27(sept, IH, J = 6.9 Hz), 7.12(d, 2H, J = 8.6 Hz), 7.32(t, IH, J = 7.8 Hz), 7.45(brd, IH, J = 7.8 Hz), 7.53(d, 2H, J = 8.6 Hz), 7.58(d, IH, J = 7.8 Hz), 7.71-7.72(m, 2H), 8.27(s, IH). 1-92 mp : 163-164 °C 1h-NMR (CDCI3) 6 ppm: 0.93(t, 3H, J = 7.3 Hz), 1.32-1.39(m, 2H), 1.55-1.65(m, 2H), 1.87(s, 3H), 1.95(8, 3H), 2.60(t, 2H, J = 7.6 Hz), 7.07(d, 2H, J = 8.4 Hz), 7.18(d, 2H, J = 8.5 Hz), 7.54(d, 2H, J = 8.5 Hz), 7.91(brs, IH), 8.18(d, 2H, J = 8.4 Hz), 8.77(s, IH). 1-93 mp : 173 °C 1h-NMR (CDCI3) 5 ppm: 0.93(t, 3H, J = 7.3 Hz), 1.32-1.40(m, 2H), 1.39(d, 6H, J = 6.9 Hz), 1.55-1.62(m, 2H), 2.60(t, 2H, J = 7.8 Hz), 3.13(sept, IH, J = 6.9 Hz), 4.39(d, 2H, J = 6.3 Hz), 4.45(t, IH, J = 6.3 Hz), 7.18(d, 2H, J = 8.7 Hz), 7.46(d, 2H, J = 8.7 Hz), 7.54 (d, 2H, J = 8.7 Hz), 7.80(s, IH), 7.85(d, 2H, J = 8.7 Hz). 1-94 mp : 159-160 °C 1h-NMR (CDCI3) 6 ppm: 0.93(t, 3H, J = 7.3 Hz), 1.32-1.39(m, 2H), 1.54-1.80(m, 2H), 1.79(s, 3H), 1.80(s, 3H), 2.60t, 2H, J = 7.7 Hz), 3.18(s, 3H), 7.18(d, 2H, J = 8.5 Hz), 7.30(d, 2H, J = 8.8 Hz), 7.52(d, 2H, J = 8.5 Hz), 7.70(brs, IH), 7.84(d, 2H, J = 8.8 Hz), 8.77(s, IH). 1-95 mp : 177-178 °C 1h-NMR (CDCI3) 5 ppm: 0.94(t, 3H, J = 7.2Hz), 1.31-1.48(m, 8H), 1.54-1.66(m, 2H), 2.55(8, 3H), 2.62(t, 2H, J = 7.6Hz), 3.92(sept, IH, J = 6.6Hz), 7.20(d, 2H, J = 8.45Hz), 7.74(d, 2H, J = 8.5Hz), 9.01(brs, IH), 9.17(s, IH). 1-96 mp : 220-223 °C 1h-NMR (CDCI3) 6 ppm: 0.93(t, 3H, J = 7.3Hz), 1.28-1.42(m, 2H), 1.50(d, 6H, J = 6.8Hz), 1.54-1.65(m, 2H), 2.62(t, 2H, J= 7.6Hz), 4.08(sept, IH, J= 7.1Hz), 7.20(d, 2H, J = 8.5Hz), 7.48(d, 2H, J = 8.5Hz), 7.71(brs, IH), 8.51(brs, IH), 8.95(s, IH). 1-97 mp : 195-197 °C 1h-NMR (CDCI3) 6 ppm: 0.91(t, 3H, J = 7.6Hz), 0.94(t, 3H, J = 7.3Hz), 1.32-1.44(m, 6H), 1.54-1.64(m, 2H), 1.66-1.78(m, 2H), 2.62(t, 2H, J = 7.7Hz), 2.86(brs, 2H), 3.98(sept, IH, J = 7.1Hz), 7.19(d, 2H, J = 8.5Hz), 7.63(d, 2H, J = 8.4Hz), 8.72(brs, IH), 8.81(brs, IH). 1-98 mp : 216-218 °C 1h-NMR (CDCI3+CD3OD) 6 ppm: 0.93(t, 3H, J = 7.4Hz), 1.29-1.40(m, 2H), 1.43(d, 2H, J = 6.9Hz), 1.51-1.63(m, 2H), 2.60(t, 2H, J = 7.8Hz), 3.65(sept, IH, J = 6.9Hz), 7.18(d, 2H, J = 8.5Hz), 7.22(d, IH, J = 8.8Hz), 7.55(d, 2H, J = 8.5Hz), 8.18(dd, IH, J = 8.8, 2.4Hz), 8.63(d, IH, J = 2.4Hz). 1-99 mp : 201-202 °C 1h-NMR (CDCI3) 6ppm:0.93(t, 3H, J = 7.3Hz), 1.22-1.40(m, 2H), 1.49(d, 2H, J = 7.1Hz), 1.51-1.63(m, 2H), 2.59(t, 2H, J = 7.7Hz), 4.22(sept, IH, J= 7.1Hz), 7.16(d, 2H, J = 8.4Hz), 7.41(brs, IH), 7.52(d, 2H, J = 8.4Hz), 8.10(brs, IH), 8.13(d, IH, J = 2.2Hz), 8.61(brs, IH). I-100 mp : 160-162 °C 1h-NMR (CDCI3) 6ppm: 0.93(t, 3H, J = 7.3Hz), 1.22-1.42(m, 2H), 1.45(d, 2H, J = 6.9Hz), 1.51-1.63(m, 2H), 2.61(t, 2H, J = 7.8Hz), 3.37(sept, IH, J= 6.9Hz), 6.89(brs, IH), 7.19(d, 2H, J = 8.4Hz), 7.65(d, 2H, J = 8.4Hz), 7.80(dd, IH, J = 8.4, 2.4Hz), 8.27(d, IH, J = 8.4Hz), 8.45(d, IH, J= 2.4Hz), 9.75(brs, IH). I-101,1-214 mp: 192-194 °C 1h-NMR (CDC13) 6 ppm:0.93(t, 3H, J = 7.3Hz), 1.27-1.41(m, 2H), 1.35(s, 9H), 1.50- 1.66(m, 2H), 2.60(t, 2H, J = 7.6Hz), 5.58(brs, IH), 7.07(d, 2H, J = 8.5Hz), 7.17(d, 2H, J = 8.5Hz), 7.52(d, 2H, J = 8.5Hz), 7.71(brs, IH), 7.79(d, 2H, J = 8.5Hz). 1-102 mp : 216-217 °C 1h-NMR (CDCI3) 5 ppm:0.93(t, 3H, J = 7.3Hz), 1.26-1.42(m, 2H), 1.45(s, 9H), 1.70- 1.83(m, 2H), 2.60(t, 2H, J = 7.7Hz), 6.42(brs, IH), 7.18(d, 2H, J = 8.5Hz), 7.35(d, 2H, J = 8.5Hz), 7.51(d, 2H, J = 8.5Hz), 7.68(brs, IH), 7.82(d, 2H, J = 8.5Hz). 1-103 1h-NMR (CDC13) 5 ppm: 0.91(t, 3H, J = 7.3 Hz), 1.28-1.36(m, 2H), 1.32(d, 6H, J = 6.9 Hz), 1.49-1.59(m, 2H), 2.54(t, 2H, J = 7.7 Hz), 3.23(sept, IH, J = 6.9 Hz), 3.46(s, 3H), 6.76(brs, IH), 6.91(d, 2H, J = 8.2 Hz), 6.99(d, 2H, J = 8.8 Hz), 7.03(d, 2H, J = 8.2 Hz), 7.25(d, 2H, J = 8.8 Hz). 1-104 mp : 182-183 °C XH-NMR (CDCI3) 6 ppm:0.93(t, 3H, J = 7.3Hz), 1.28-1.40(m, 2H), 1.51-1.63(m, 2H), 1.64-1.88(m, 4H), 1.90-2.23(m, 4H), 2.60(t, 2H, J = 7.6Hz), 3.39(m, IH), 6.16(brs, IH), 7.07(d, 2H, J = 8.5Hz), 7.16(d, 2H, J = 8.5Hz), 7.52(d, 2H, J = 8.5Hz), 7.74(brs, IH), 7.77(d, 2H, J=8.5Hz). 1-105 mp : 190-191 °C 1h-NMR (CDCI3) 5 ppm:0.93(t, 3H, J = 7.3Hz), 1.28-1.41(m, 2H), 1.52-1.69(m, 4H), 1.75-1.90(m, 2H), 1.92-2.07(m, 4H), 2.58(t, 2H, J = 7.6Hz), 3.59(m, IH), 6.53(brs, IH), 7.18(d, 2H, J = 8.5Hz), 7.31(d, 2H, J = 8.5Hz), 7.52(d, 2H, J = 8.5Hz), 7.67(brs, IH), 7.84(d, 2H, J = 8.5Hz). 1-106 mp : 194-197 °C 1h-NMR (CDCI3) 6 ppm:0.93(t, 3H, J = 7.3Hz), 1.22-1.41(m, 2H), 1.53-1.65(111, 2H), 1.90(s, 6H), 2.60(t, 2H, J = 7.8Hz), 6.86(brs, IH), 7.18(d, 2H, J = 8.5Hz), 7.43(d, 2H, J = 8.5Hz), 7.5l(d, 2H, J = 8.5Hz), 7.71(brs, IH), 7.84(d, 2H, J = 8.5Hz). 1-107 mp : 211-212 °C 1h-NMR (CDCI3) 6 ppm:0.93(t, 3H, J = 7.3Hz), 1.24-1.40(m, 2H), 1.50-1.62(m, 2H), 2.60(t, 2H, J = 7.6Hz), 6.19(brs, IH), 7.17(d, 2H, J = 8.5Hz), 7.18(d, 2H, J = 8.5Hz), 7.51(d, 2H, J = 8.5Hz), 7.66(brs, IH), 7.86(d, 2H, J = 8.5Hz). 1-108 mp : 298-300 °C 1h-NMR (DMSO-d6) 6 ppm: 0.90(t, 3H, J = 7.3Hz), 1.22-1.39(m, 2H), 1.48-1.60(m, 2H), 2.54(t, 2H, J = 7.3Hz), 7.04(d, 2H, J = 8.8Hz), 7.12(d, 2H, J = 8.5Hz), 7.64(d, 2H, J = 8.5Hz), 7.69(d, 2H, J = 8.8Hz), 9.80(s, IH). 1-109 mp: 122-123 °C 1h-NMR (CDCI3) 5 ppm:0.90(t, 3H, J = 7.4Hz), 0.97(t, 3H, J = 7.7Hz), 1.26-1.38(m, 2H), 1.30(s, 6H), 1.50-1.66(m, 4H), 1.72-1.83(m, 4H), 2.34(t, 2H, J = 7.1Hz), 2.55(t, 2H, J = 7.6Hz), 3.19(q, IH, J = 6.0Hz), 4.60(brs, IH), 7.08(d, 2H, J = 8.5Hz), 7.42(d, 2H, J = 8.5Hz), 7.85(8, IH). 1-110 mp : 109-110 °C 1h-NMR (CDCI3) 6ppm:0.91(t, 3H, J = 7.4Hz), 1.10(d, 6H, J = 6.7Hz), 1.29-1.38(m, 2H), 1.55(8, 9H), 1.60-1.70(m, 2H), 1.78-1.89(m, 2H), 2.26(m, IH), 2.39(t, 2H, J = 7.0Hz), 2.57(t, 2H, J = 7.7Hz), 2.90(d, 2H, J = 6.6Hz), 3.16(brs, IH), 4.24(brs, IH), 7.12(d, 2H, J = 8.5Hz), 7.40(d,2H, J = 8.5Hz). Mil mp : 64-65 °C 1h-NMR (CDCI3) 6 ppm:0.91(t, 3H, J = 7.3Hz), 1.02(t, 3H, J = 7.5Hz), 1.35(d, 3H, J = 6.7Hz), 1.26-1.38(m, 2H), 1.48-1.69(m, 5H), 1.76-1.87(m, 2H), 2.04(m, IH), 2.38(t, 2H, J = 7.3Hz), 2.56(t, 2H, J = 7.6Hz), 2.91(m, IH), 3.16(brs, 2H), 4.42(brs, IH), 7.11(d, 2H, J = 8.5Hz), 7.42(d, 2H, J = 8.5Hz), 7.47(brs, IH). 1-112 mp : 79-80 °C 1h-NMR (CDCI3) 6 ppm:1.36(s, 9H), 1.52-1.62(m, 2H), 1.67-1.76(m, 2H), 2.22(t, 2H, J = 7.4Hz), 3.16(q, 2H, J = 6.3Hz), 3.78(s, 3H), 4.33(d, 2H, J = 5.4Hz), 4.62(brs, IH), 6.20(brs, IH), 6.86(d, 2H, J = 8.8Hz), 7.19(d, 2H, J = 8.8Hz). 1-113 mp : 125-126 °C 1h-NMR (CDCI3) 6 ppm:1.38(s, 9H), 1.62-1.70(m, 2H), 1.76-1.88(m, 2H), 2.46(t, 2H, J = 7.4Hz), 3.22(q, 2H, J = 6.1Hz), 4.22(t, IH, J = 6.1Hz), 7.24(dd, IH, J = 8.9, 2.3Hz), 7.36(d, IH, J= 2.3Hz), 7.65(brs, IH), 8.29(d, IH, J = 8.9Hz). 1-114 mp : 89-91 °C 1h-NMR (CDCI3) 6 ppm:0.92 (t, 3H, J = 7.0Hz), 1.06 (d, 6H, J = 7.0Hz), 1.36 (m ,1H), 1.50-1.72 (m ,5H), 1.94-2.06 (m, 2H), 2.26 (m, IH), 2.60 (t, 2H, J = 7.7Hz), 2.84 (t, 2H, J = 7.7Hz), 2.93 (d, 2H, J = 6.3Hz), 3.20 (t, 2H, J = 6.6Hz), 4.30 (brs, IH), 7.19 (d, 2H, J = 8.5Hz), 7.63 (d, 2H, J = 8.5Hz), 9.15(brs, IH). 1-115 mp : 94-95 °C 1h-NMR (CDCI3) 5 ppm:0.92 (t, 3H, J = 7.5Hz), 1.03 (t, 3H, J = 7.5Hz), 1.23-1.40 (m ,5H), 1.42-1.65 (m, 6H), 1.75 (m, IH), 2.02 (m, IH), 2.24 (t, 2H, J = 7.0Hz), 2.59 (t, 2H, J = 8.0Hz), 2.90 (m, IH), 3.14 (q, 2H, J = 6.6Hz), 4.20 (m, IH), 4.40 (d, 2H, J = 5.4Hz), 5.70 (brs, IH), 7.14 (d, 2H, J = 8.1Hz), 7.18(d, 2H, J = 8.1Hz). 1-116 mp : 89-91 °C 1h-NMR (CDC13) 6 ppm:0.97 (t, 3H, J = 7.3Hz), 1.02 (t, 3H, J = 7.5Hz), 1.35 (d, 3H, J = 7.0Hz), 1.40-1.90 (m ,9H), 2.04 (m ,1H), 2.37 (t, 2H, J= 7.0Hz), 2.90 (m, IH), 3.17 (q, 2H, J = 6.6Hz), 3.93 (t, 2H, J = 6.6Hz), 4.32 (m, IH), 6.84 (d, 2H, J = 9.0Hz), 7.31 (brs, IH), 7.40 (d, 2H, J = 9.0Hz). 1-117 mp: 110-111 °C 1h-NMR (CDCI3) 5 ppm:1.02 (t, 3H, J = 7.5Hz), 1.34 (d, 3H, J = 6.6Hz), 1.45-1.70 (m ,3H), 1.75-1.85 (m, 2H), 2.05 (m ,1H), 2.36 (t, 2H, J = 7.5Hz), 2.90 (m, IH), 3.16 (q, 2H, J = 6.6Hz), 3.78 (s, 3H), 4.50 (m, IH), 6.84 (d, 2H, J = 6.8Hz), 7.42 (d, 2H, J = 6.8Hz), 7.48 (brs, IH). 1-118 mp: 113-115 °C 1h-NMR (CDCI3) 6 ppm:0.92 (t, 3H, J = 7.0Hz), 1.20-1.34 (m ,1H), 1.37 (d, 6H, J = 7.0Hz), 1.48-1.70 (m, 3H), 2.43 (q, 2H, J = 6.6Hz), 2.58 (t, 2H, J = 7.7Hz), 3.10-3.31 (m, 3H), 4.75 (m, IH), 6.04 (d, IH, J = 15.0Hz), 6.77 (dt, IH, J = 7.7, 15.0Hz), 7.14 (d, 2H, J = 8.4Hz), 7.55 (d, 2H, J = 8.4Hz), 7.85 (brs, IH). 1-119 mp: 139-140 °C 1h-NMR (CDCI3) 6 ppm:1.19(s, 9H), 1.47(m, 2H), 1.61(m, 2H), 2.18(t, 2H, J = 7.6Hz), 3.03(q, 2H, J = 6.3Hz), 4.09(t, IH, J = 5.9Hz), 6.85(brd, IH, J = 8.0Hz), 7.00(t, IH, J = 8.0Hz), 7.16(brd, IH, J = 8.0), 7.48(brs, IH), 7.57(brs, IH). 1-120 mp: 183°C 1h-NMR (CDCI3) 6 ppm:0.91(t, 3H, J = 7.3Hz), 1.20-1.58(m, 6H), 1.40(s, 9H), 2.07(dd, IH, J = 12.9, 3.1Hz), 2.52(t, 2H, J = 7.7Hz), 2.95(dd, 2H, J = 11.5, 2.5Hz), 3.46(m, IH), 3.88-4.07(m, 3H), 6.47(s, IH), 7.08(d, 2H, J = 8.5Hz), 7.22(d, 2H, J = 8.5Hz). 1-121 mp: 163-166°C 1h-NMR (CDCI3) 5 ppm:0.91(t, 3H, J = 7.3Hz), 1.32-1.62(m, 6H), 1.45(s, 9H), 1.95- 2.07(m, 3H), 2.20(m, IH), 2.46(td, IH, J = 10.4, 3.7Hz), 2.37(t, 2H, J = 7.6Hz), 3.43(brd, 2H, J = 10.4Hz), 4.80(s, IH), 7.12(d, 2H, J= 8.4Hz), 7.14(s, IH), 7.39(d, 2H, J = 8.4Hz). 1-122 mp: 188-189 °C 1h-NMR (CDCI3) 6 ppm:0.91 (t, 3H, J = 7.5Hz), 1.25-1.41 (m ,2H), 1.42 (s, 9H), 1.50- 1.62 (m ,2H), 1.78-1.95 (m ,4H), 2.00-2.20 (m ,6H), 2.57 (t, 2H, J = 7.5Hz), 3.99 (brs, IH), 7.10 (brs, IH), 7.12 (d, 2H, J = 6.5Hz), 7.41 (d, 2H, J = 6.5Hz). 1-123 mp : 197-198 °C 1h-NMR (CDCI3) 5 ppm:0.9l (t, 3H, J = 7.5Hz), 1.24-1.40 (m ,2H), 1.39 (s, 9H), 1.50- 1.70 (m ,2H), 1.99 (brs ,12H), 2.56 (t, 2H, J = 7.5Hz), 3.47 (brs, IH), 7.10 (s, IH), 7.11 (d, 2H, J = 8.5Hz), 7.38 (d, 2H, J = 8.5Hz). 1-124 mp : 258-260 °C 1h-NMR (CDC13) 5 ppm: 1.20-1.40 (m, 2H), 1.41 (s, 9H), 1.62-1.81 (m, 2H), 2.03-2.35 (m, 5H), 2.37 (s, 3H), 2.71 (s, 3H), 3.32 (m, IH), 3..64 (d, IH, J = 8.4Hz), 7.08 (brs, IH), 7.24 (m, IH), 7.33 (m, 2H), 7.60 (d, IH, J = 8.1Hz), 7.77 (s, IH), 7.80 (d, IH, J = 8.4Hz), 8.14 (m, IH). 1-125 mp : 297-299 °C 1h-NMR (DMSO-d6) 5 ppm:1.27 (s, 9H), 1.28-1.56 (m, 4H), 1.80-2.01 (m, 4H), 2.47 (m, IH), 2.76 (brs, IH), 3.05 (m, 2H), 6.78 (d, IH, J = 9.0Hz), 7.23 (d, IH, J = 9.0Hz), 7.46 (dd, IH, J = 2.0, 9.0Hz), 8.03 (d, IH, J = 2.0Hz). 1-126 mp : 198-199 °C 1h-NMR (CDC13) 5ppm:1.18-1.39 (m, 2H), 1.40 (s, 9H), 1.60-1.79 (m, 2H), 1.98-2.35 (m, 5H), 3.30 (m, IH), 3.67 (d, IH, J = 9.6Hz), 5.89 (tt, IH, J = 3.0, 50.0Hz), 6.97 (d, IH, J = 7.8Hz), 7.21 (s, IH), 7.30-7.40 (m, 2H), 7.55 (s, IH) 1-127 mp : 262-264 °C 1h-NMR (CDCI3) 6 ppm: 1.20-1.39 (m, 2H), 1.41 (s, 9H), 1.60-1.80 (m, 2H), 2.00-2.36 (m, 5H), 2.57 (s, 3H), 3.33 (m, IH), 3..62 (d, IH, J = 8.7Hz), 7.28 (brs, IH), 7.62 (d, 2H, J = 8.7Hz), 7.94 (d, 2H; J = 8.7Hz). 1-128 mp : 252-254 °C 1h-NMR (CDCI3) 5ppm:1.18-1.39 (m, 2H), 1.40 (s, 9H), 1.58-1.79 (m, 2H), 1.99-2.30 (m, 5H), 2.46 (s, 3H), 3.32 (m, IH), 3..64 (m, IH), 7.11 (brs, IH), 7.23 (d, 2H, J = 9.0Hz), 7.44 (d, 2H, J = 9.0Hz). 1-129 mp : >300 °C 1h-NMR (CDCI3+CD3OD) 6ppm:1.30-1.45(m, 2H), 1.42(s, 9H), 1.70-1.88(m, 2H), 2.10- 2.37(m, 4H), 2.52(m, IH), 3.34(m, IH), 7.43-7.54(m, 3H), 7.82(d, IH, J = 6.7Hz), 7.88(d, IH, J = 8.5Hz), 7.98-8.07(m, 2H), 8.44(s, IH), 8.46(s, IH). 1-130 mp : 123-124 °C 1h-NMR (CDCI3) 6 ppm:1.18-1.34(m, 2H), 1.40(s, 9H), 1.62-1.75(m, 2H), 2.00-2.28(m, 5H), 3.31(m, IH), 3.6l(d, IH, J = 9.5Hz), 5.59(s, IH), 7.17(s, IH), 7.30-7.37(m, 6H), 7.41(d, IH, J = 8.5Hz), 7.84(d, IH, J = 2.1Hz). 1-131 mp : 202-204 °C 1h-NMR (CDCI3) 6 ppm:1.27-1.38(m, 2H), 1.38(s, 9H), 1.62-1.75(m, 2H), 1.97-2.04(m, 2H), 2.18-2.27(m, 3H), 3.26(m, IH), 3.81(s, 3H), 4.62(d, IH, J = 7.9Hz), 7.12(d, IH, J = 7.8Hz), 7.40(t, IH, J = 7.8Hz), 7.51(s, 3H), 7.61(d, IH, J = 7.8Hz), 7.71(s, IH), 8.21(brs, IH). 1-132 mp : 236-237 °C 1h-NMR (CDCI3) 6 ppm:1.23-1.43(m, 2H), 1.41(s, 9H), 1.66-1.80(m, 2H), 2.08-2.12(m, 2H), 2.23-2.31(m, 3H), 3.34(m, IH), 3.87(d, IH, J = 9.5Hz), 4.02(s, 3H), 7.30(td, IH, J = 7.3, 1.1Hz), 7.36(s, IH), 7.39(td, IH, J = 7.3, 1.5Hz), 7.53(brd, IH, J = 7.3Hz), 7.84(brd, IH, J = 7.3Hz), 8.05(s, IH), 8.73(s, IH). 1-133 mp : 198-200 °C 1h-NMR (CDCI3) 6ppm:0.93(t, 3H, J = 7.3Hz), 0.97(t, 3H, J= 6.7Hz), 1.18-1.8l(m, 7H), 1.39(s, 9H), 1.98-2.05(m, 2H), 2.2l-2.24(m, 3H), 3.29(m, IH), 4.00(dd, IH, J = 10.7, 6.7Hz), 4.09(dd, IH, J= 10.7, 6.1Hz), 4.27(d, IH, J = 9.8Hz), 6.37(d, IH, J= 15.9Hz), 7.47(d, 2H, J = 8.5Hz), 7.59(d, 2H, J = 8.5Hz), 7.62(d, IH, J = 15.9Hz), 7.83(brs, IH). 1-134 mp : 212-213 °C 1h-NMR (CDCI3) 6ppm:1.21-1.32(m, 2H), 1.39(s, 9H), 1.59-1.73(m, 2H), 1.99-2.04(m, 2H), 2.10-2.26(m, 3H), 3.26(m, IH), 3.72(d, IH, J = 9.6Hz), 6.74(m, IH), 7.02(d, 2H, J = 7.4Hz), 7.11(t, IH, J = 7.4Hz), 7.13-7.19(m, 2H), 7.22-7.26(m, 2H), 7.34(t, 2H, J = 7.4Hz). 1-135 mp : 294-296 °C 1h-NMR (DMSO-dg) 5 ppm:1.27 (s, 9H), 1.28-1.55 (m, 4H), 1.81-2.05 (m, 4H), 2.26 (m, IH), 2,98-3.20 (m, 2H), 6.78 (d, IH, J = 9.0Hz), 7.31 (t, IH, J = 7.5Hz), 7.54-7.72 (m, 5H), 7.94 (brs, IH). 1-136 mp : >300 °C 1h-NMR (DMSO-dg) 6ppm:1.28 (a, 9H), 1.29-1.59 (m, 4H), 1.81-2.02 (m, 4H), 2.27 (m, IH), 3.06 (m, IH), 6.81 (d, IH, J = 8.7Hz), 7.38 (t, IH, J = 7.2Hz), 7.48 (t, 2H, J = 7.2Hz), 7.62-7.81 (m, 10H), 9.93 (brs, IH). 1-137 mp : 291-292 °C J-H-NMR (CDCI3) 6 ppm:l.25-1.39 (m, 2H), 1.41 (a, 9H), 1.61-1.80 (m, 2H), 2.01-2.36 (m, 5H), 3.32 (m, IH), 3.63 (d, IH, J= 9.3Hz), 7.20 (brs, IH), 7.53-7.74 (m, 8H). 1-138 mp : 259-262 °C 1h-NMR (CD3OD) 6 ppm:1.40 (a, 9H), 1.40-1.80 (m, 4H), 2.00-2.30 (m, 4H), 2.45 (m, IH), 3.00 (a, 3H), 3.15-3.30 (m, 2H), 7.90 (d, IH, J = 8.4Hz), 8,12 (d, IH, J = 9.0Hz), 8.39 (d, IH, J = 9.0Hz), 8.72 (s, IH), 8.92 (d, IH, J = 8.4Hz), 10.4 (s, IH). 1-139 mp : 265-268 °C 1h-NMR (CDCI3) 6ppm:1.25-1.40(m, 2H), 1.40(s, 9H), 168-1.81(m, 2H), 2.05-2.10(m, 2H), 2.23-2.37(m, 3H), 3.32(m, IH), 4.27(d, IH, J = 9.1Hz), 7.53(t, IH, J= 7.9Hz), 7.63(td, IH, J = 7.9, 1.4Hz), 7.77(d, IH, J = 7.9Hz), 8.03(d, IH, J = 7.9Hz), 8.37(brs, IH), 8.85- 8.86(m, 2H). 1-140 mp : 258-260 °C 1h-NMR (CDCI3) 6 ppm:1.20-1.40 (m, 2H), 1.41 (s, 9H), 1.52-1.85 (m, 2H), 2.03-2.35 (m, 5H), 3.34 (m, IH), 3.75 (m, IH), 7.35-7.66 (m, 3H), 8.05 (d, IH, J = 9.0Hz), 8.11 (d, IH, J = 9.0Hz), 8.40 (brs, IH), 8.83 (s, IH). 1-141 mp : 205-206 °C 1h-NMR (CDCI3) 6ppm:1.20-1.37(m, 2H), 1.40(s, 9H), 1.43-1.62(m, 2H), 1.90-2.01(m, 2H), 2.02-2.23(m, 3H), 3.27(m, IH), 3.63(d, IH, J = 9.6Hz), 3.70(s, 3H), 6.64(d, IH, J = 8.8Hz), 7.28-7.41(m, 5H), 7.45(brs, IH), 8.26(d, IH, J = 8.8Hz). 1-142 mp : 277-280 °C 1h-NMR (CDCI3) 5ppm:0.23-0.34(m) 2H), 1.34(s, 9H), 1.34-1.55(m, 5H), 1.76-1.80(m, 2H), 2.97(m, IH), 3.31(d, IH, J = 9.6Hz), 7.18(s, IH), 7.50-7.59(m, 4H), 7.77(dd, IH, J = 7.4, 1.0Hz), 7.9l-7.98(m, 2H), 8.39(dd, IH, J = 7.4, 1.9Hz). 1-143 mp : 202-203 °C 1h-NMR (CDCI3) 5ppm:1.23-1.40(m, 2H), 1.40(s, 9H), 1.57-1.71(m, 2H), 2.05-2.10(m, 2H), 2.18-2.28(m, 3H), 3.31(m, IH), 3.9l(s, 3H), 3.93(s, 3H), 4.05(d, IH, J = 9.5Hz), 8.15(s, IH), 9.56(s, IH). 1-144 mp: 177-178 °C 1h-NMR (CDCI3) 6ppm:1.27-1.39(m, 2H), 1.40(s, 9H), 1.65-1.79(m, 2H), 2.04-2.07(m, 2H), 2.12-2.34(m, 3H), 3.22(m, IH), 3.93(d, IH, J = 9.1Hz), 6.90-7.03(m, 3H), 7.25(m, IH), 7.77(dd, IH, J = 4.9, 1.7Hz), 7.81(brs, IH), 8.72(dd, IH, J= 7.8, 1.5Hz). 1-145 mp : >300 °C 1h-NMR (DMSO-d6) 6 ppm:1.30(s, 9H), 1.44-1.70(m, 4H), 2.05-2.19(m, 4H), 2.73(m, IH), 3.18(m, IH), 6.86(d, IH, J = 8.8Hz), 7.62(t, 2H, J = 8.5Hz), 7.86(t, 2H, J = 8.5Hz), 7.89(d, 2H, J = 8.5Hz), 8.16(d, 2H, J = 8.5Hz). 1-146 mp : 240-242 °C H-NMR (DMSO-d6) Sppm:1.26-1.53(m, 4H), 1.27(8, 9H), 1.74-1.83(m, 2H), 1.90- 1.97(m, 2H), 2.26(m, IH), 3.04(m, IH), 6.59(brs, IH), 6.74-6.79(m, 3H), 7.74(s, IH), 10.32(s, IH), 12.80(s, IH). 1-147 mp: 167-169 °C 1h-NMR (CDC13) 5 ppm: 1.05-1.28 (m, 2H), 1.38 (s, 9H), 1.47-1.70 (m, 2H), 1.80-2.00 (m, 3H), 2.13-2.25 (m, 2H), 2.75 (t, 2H, J = 6.9Hz), 3.24 (m, IH), 3.49 (dt, 2H, J = 6.3, 6.9Hz), 3.58 (d, IH, J = 8.7Hz), 3.87 (s, 6H), 5.40 (brs, IH), 6.71 (m, 2H), 6.82 (d, IH, J = 8.7Hz). 1-148 mp: 171-172 °C 1H-NMR (CDCI3) 5 ppm:l. 16-1.38 (m, 2H), 1.39 (s, 9H), 1.50-1.79 (m, 4H), 1.85-2.02 (m, 3H), 2.15-2.30 (m, 2H), 2.35-2.56 (m, 6H), 3.25 (m, IH), 3.33 (q, 2H, J = 6.0Hz), 3.63 (d, IH, J = 9.0Hz), 3.72 (t, 4H, J = 4.6Hz), 6.77 (brs, IH). 1-149 1h-NMR (CDCI3) 5 ppm:1.20-1.36 (m, 2H), 1.28 (t, 3H, J = 7.2Hz), 1.39 (s, 9H), 1.45- 1.70 (m, 2H), 1.85-2.30 (m, 7H), 2.43 (s, 3H), 3.05-3.42 (m, 3H), 3.46-3.80 (m, 3H), 7.31 (d, IH, J = 7.2Hz), 7.40-7.52 (m, 3H), 8.18 (brs, IH). 1-150 mp : 203-204 °C 1H-NMR (CDCI3) 6 ppm:1.15-1.37 (m, 2H), 1.39 (s, 9H), 1.42-1.70 (m, 2H), 1.85-2.29 (m, 5H), 2.76 (t, 2H, J = 6.0Hz), 3.26 (m, IH), 3.49 (q, 2H, J = 6.0Hz), 3.61 (m, IH), 4.03 (s, 2H), 5.88 (brs, IH), 7.15 (dd, IH, J = 7.0, 8.8Hz), 7.30-7.35 (m, 2H). 1-151 mp : 181-183 °C 1h-NMR (CDCI3) 6 ppm: 1.15-1.30 (m, 2H), 1.39 (s, 9H), 1.45-1.64 (m, 2H), 1.88-2.05 (m, 3H), 2.15-2.25 (m, 2H), 2.69 (t, 2H, J = 6.0Hz), 3.28 (m, IH), 3.47 (q, 2H, J = 6.0Hz), 3.58 (d, IH, J = 9.9Hz), 3.87 (s, 2H), 5.83 (brs, IH), 7.00 (m, IH), 7.20 (m, 2H). 1-152 mp : 222-224 °C 1h-NMR (CDCI3) 6ppm:1.16-1.37 (m, 2H), 1.39 (s, 9H), 1.49-1.70 (m, 2H), 1.90-2.25 (m, 5H), 3.26 (m, IH), 3.36 (t, 2H, J = 6.4Hz), 3.66 (dt, 3H, J = 6.0, 6.4Hz), 5.87 (t, IH, J = 6.0Hz), 7.58 (s, IH), 7.68 (dd, IH, J = 7.0, 8.5Hz), 7.83 (dd, IH, J = 7.0, 8.5Hz), 8.19 (t, 2H, J = 8.5Hz). 1-153 mp : 207-209 °C 1h-NMR (CDCI3) 6 ppm:1.05-1.25 (m, 2H), 1.38 (s, 9H), 1.40-2.03 (m, 10H), 2.05-2.25 (m, 2H), 2.58 (s, 3H), 2.76 (m, IH), 3.05-3.35 (m, 2H), 3.97 (d, IH, J = 9.5Hz), 4.94 (t, IH, J = 4.0Hz), 8.42 (d, IH, J = 5.5Hz), 8.97 (d, IH, J = 5.5Hz). 1-154 mp : 184-185 °C 1h-NMR (CDCI3) 6 ppm:1.05-1.25 (m, 2H), 1.37 (s, 9H), 1.50-1.69 (m, 2H), 1.85-2.05 (m, 3H), 2.10-2.21 (m, 2H), 3.24 (m, IH), 3.64 (m, IH), 4.87 (s, IH), 4.88 (s, IH), 5.67 (brs, IH), 7.42 (d, 2H, J = 5.5Hz), 7.52 (m, 2H), 7.78 (m, IH), 7.82 (m, IH), 7.95 (d, IH, J = 7.0Hz). 1-155 mp : 208-210 °C 1h-NMR (DMSO-d6) 6ppm:1.26 (s, 9H), 1.27-1.50 (m, 4H), 1.75-2.00 (m, 4H), 2.16 (m, IH), 2.81 (s, 3H), 3.02 (m, IH), 6.79 (d, IH, J = 8.5Hz), 10.00 (s, IH), 10.66 (s, IH). 1-156 mp : 256-257 °C 1h-NMR (CDCI3) 5 ppm:1.20-1.39 (m, 2H), 1.41 (s, 9H), 1.60-1.81 (m, 2H), 2.01-2.35 (m, 5H), 2.69 (t, 2H, J = 6.0Hz), 3.11 (t, 2H, J = 6.0Hz), 3.30 (m, IH), 3.61 (d, IH, J = 9.3Hz), 7.21 (d, IH, J = 8.0Hz), 7.31 (s, IH), 7.70 (d, IH, J = 8.0Hz), 7.99 (s, IH). 1-157 mp : 269-271 °C 1h-NMR (CDCI3) 5 ppm: 1.20-1.45 (m, 2H), 1.41 (s, 9H), 1.70-1.90 (m, 2H), 2.10-2.45 (m, 5H), 3.37 (m, IH), 3.68 (m, IH), 7.45 (dd, IH, J= 4.0, 8.0Hz), 7.53 (brs, IH), 7.72 (t, IH, J = 8.0Hz), 7.83 (d, IH, J = 8.0Hz), 8.02 (d, IH, J = 8.0Hz), 8.18 (d, IH, J = 8.0Hz), 8.93 (d, IH, J = 4.0Hz). 1-158 mp : 253-255 °C 1h-NMR (CDCI3) 5ppm:1.20-1.40 (m, 2H), 1.42 (s, 9H), 1.60-1.90 (m, 2H), 2.06-2.50 (m, 5H), 2.72 (s, 3H), 3.33 (m, IH), 3.78 (d, IH, J = 9.2Hz), 7.52 (t, IH, J = 7.0Hz), 7.62-7.80 (m, 2H), 7.94 (brs, IH), 8.05 (d, IH, J= 8.5Hz), 8.20 (s, IH). 1-159 mp : 253-255 °C 1h-NMR (CDCI3) 6 ppm: 1.20-1.39 (m, 2H), 1.40 (s, 9H), 1.60-1.80 (m, 2H), 1.98-2.30 (m, 5H), 2.71 (s, 3H), 3.31 (m, IH), 3.68 (d, IH, J = 9.0Hz), 7.41 (brs, IH), 7.61 (d, 2H, J = 9.0Hz), 7.70 (d, 2H, J = 9.0Hz). 1-160 mp: 211-212 °C XH-NMR (CDCI3) 6 ppm:1.20-1.32 (m, 2H), 1.39 (t, 3H, J = 7.0Hz), 1.40 (s, 9H), 1.55- 1.79 (m, 2H), 1.98-2.35 (m, 5H), 3.31 (m, IH), 3.65 (d, IH, J = 9.5Hz), 4.03 (q, 2H, J = 7.0Hz), 6.64 (d, IH, J = 8.0Hz), 6.92 (d, IH, J = 8.0Hz), 7.10 (s, IH), 7.19 (t, IH, J = 8.0Hz), 7.30 (brs, IH). 1-161 mp : 202-203 °C 1h-NMR (CDCI3) 5 ppm:0.96 (t, IH, J = 7.3Hz), 1.29-1.39 (m, 2H), 1.40 (s, 9H), 1.41- 1.58 (m, 2H), 1.60-1.80 (m, 4H), 1.98-2.31 (m, 5H), 3.31 (m, IH), 3.66 (d, IH, J = 8.5Hz), 3.96 (t, 2H, J = 6.4Hz), 6.64 (d, IH, J = 8.0Hz), 6.90 (d, IH, J = 8.0Hz), 7.11 (s, IH), 7.19 (t, IH, J = 8.0Hz), 7.31 (brs, 11 1-162 mp: 177-180 °C 1h-NMR (CDCI3) 5 ppm:l. 18-1.38 (m, 2H), 1.39 (s, 9H), 1.59-1.78 (m, 2H), 1.95-2.05 (m, 2H), 2.07-2.25 (m, 3H), 3.26 (m, IH), 3.46 (s, 3H), 4.17 (d, IH, J = 9.5Hz), 5.15 (s, 2H), 6.77 (d, IH, J = 8.0Hz), 7.10-7.23 (m, 2H), 7.34 (s, IH), 7.58 (s, IH). 1-163 mp: 175-178 °C 1h-NMR (DMSO-d6) 5 ppm: 1.27 (s, 9H), 1.28-1.50 (m, 4H), 1.78-2.00 (m, 4H), 2.22 (m, IH), 2.96-3.15 (m, 2H), 6.67 (m, IH), 6.79 (d, IH, J = 8.5Hz), 7.18 (m, 2H), 7.38 (s, IH), 9.81 (s, IH). 1-164 mp : 232-233 °C H-NMR (CDCI3) 6 ppm:0.97(t, 3H, J = 1.3Hz), 1.22-1.30(m, 2H), 1.40(s, 9H), 1.44- 1.51(m, 2H), 1.67-1.77(m, 4H), 2.02-2.24(m, 5H), 3.22(m, IH), 3.62(d, IH, J = 9.6Hz), 4.25(t, 2H, J= 6.8Hz), 6.71(d, IH, J = 8.4Hz), 7.01(brs, IH), 7.91(dd, IH, J = 8.4, 3.3Hz), 8.08(d, IH, J = 3.3Hz). 1-165 mp : 199-200 °C 1h-NMR (CDCI3) 6 ppm:0.96(t, 3H, J = 7.4Hz), 1.24-1.50(m, 4H), 1.40(s, 9H), 1.67- 1.76(m, 3H), 2.03-2.08(m, 2H), 2.24-2.35(m, 3H), 3.29(m, IH), 3.76(d, IH, J = 9.1Hz), 3.91(t, 2H, J = 6.6Hz), 6.41(dd, IH, J = 8.8, 2.5Hz), 6.55(d, IH, J = 2.5Hz), 6.82(d, IH, J = 8.8Hz), 7.43(8, IH), 8.95(s, IH). 1-166 mp : 215-218 °C 1h-NMR (CDCI3+CD3OD) 6 ppm:0.97(t, 3H, J = 7.4Hz), 1.24-1.40(m, 4H), 1.39(s, 9H), 1.42-1.50(m, 2H), 1.54-1.72(m, 2H), 1.76-1.82(m, 2H), 1.9l-2.00(m, 2H), 2.06-2.22(m, 3H), 3.24(m, IH), 4.00(t, 2H, J = 6.6Hz), 6.78(d, IH, J = 8.8Hz), 6.98(dd, IH, J = 8.8, 2.5Hz), 7.09(d, IH, J = 8.8Hz). 1-167 mp : 212-213 °C :H-NMR (CDCI3) 5 ppm:0.96(t, 3H, J = 7.5Hz), 1.26-1.34(m, 2H), 1.40(s, 9H), 1.45- 1.50(m, 2H), 1.68-1.77(m, 4H), 2.03-2.08(m, 2H), 2.17(m, IH), 2.26-2.29(m, 2H), 3.29(m, IH), 3.60(d, IH, J = 9.0Hz), 4.25(t, 2H, J = 6.8Hz), 6.71(d, IH, J = 8.4Hz), 7.01(brs, IH), 7.91(dd, IH, J = 8.4, 3.3Hz), 8.08(d, IH, J = 3.3Hz). 1-168 mp : 230-232 °C 1h-NMR (CDCI3) 6ppm:1.22-1.35(m, 2H), 1.40(s, 9H), 1.63-1.77(m, 2H), 2.03-2.08(m, 2H), 2.15-2.29(m, 3H), 3.31(m, IH), 3.63(d, IH, J = 9.3Hz), 6.89(d, IH, J = 9.4Hz), 7.10(brd, 2H, J = 7.4Hz), 7.12(brs, IH), 7.18(t, IH, J = 7.4Hz), 7.36(brt, 2H, J = 7.4Hz), 8.09-8.15(m, 2H). 1-169 mp: 159-160 °C J-H-NMR (CDCI3) 6 ppm:0.97(t, 3H, J = 7.3), 1.20-1.35(m, 2H), 1.40(s, 9H), 1.37-1.49(m, 2H), 1.61-1.78(m, 4H), 2.05-2.08(m, 2H), 2.23-2.26(m, 2H), 2.36(s, 3H), 2.97(brs, IH), 3.32(m, IH), 3.86(brs, IH), 4.30(t, 2H, J = 6.5Hz), 6.25(s, IH), 7.92(brs, IH). 1-170 mp : 180-181 °C XH-NMR (CDCI3) 6 ppm:0.88-0.89(m, 2H), 1.39(s, 9H), 1.42-1.60(m, 2H), 1.86-1.90(m, 2H), 2.04-2.09(m, 2H), 2.42(s, 3H), 2.91(m, IH), 3.20(m, IH), 3.63(d, IH, J = 9.2Hz), 6.38(s, IH), 7.15(m, 2H), 7.28(m, IH), 7.45(m, 2H), 7.84(brs, IH). 1-171 mp : 173-174 °C 1h-NMR (CDCI3) 6 ppm:0.98(t, 3H, J = 7.5Hz), 1.29-1.40(m, 2H), 1.40(s, 9H), 1.55(m, 2H), 1.62-1.83(m, 4H), 2.09-2.12(m, 2H), 2.24-2.32(m, 3H), 3.32(m, IH), 3.63(d, IH, J = 9.5Hz), 3.99(t, 2H, J = 6.4Hz), 7.22(dd, IH, J = 9.4, 2.7Hz), 7.66(d, IH, J = 2.7Hz), 8.63(d, IH, J = 9.4Hz), 10.17(8, IH). 1-172 mp : 238-242 °C 1h-NMR (CDCI3) 5 ppm;0.96(t, 3H, J = 7.3Hz), 1.23-1.52(m, 4H), 1.40(s, 9H), 1.61- 1.78(m, 4H), 2.05-2.28(m, 5H), 3.30(m, IH), 3.66(d, IH, J = 9.4Hz), 3.84(brs, 2H), 3.90(t, 2H, J = 6.4Hz), 6.32-6.35(m, 2H), 6.96(brs, IH), 6.97(d, IH, J = 9.4Hz). 1-173 mp : 165-166 °C 1h-NMR (CDCI3) 6ppm:1.23-1.26(m, 2H), 1.40(s, 9H), 1.67-1.72(m, 2H), 2.01-2.06(m, 2H), 2.11-2.28(m, 3H), 3.31(m, IH), 3.60(s, 2H), 3.69(s, 3H), 4.02(brs, IH), 7.01(d, IH, J = 8.0Hz), 7.25(t, IH, J = 8.0Hz), 7.43(d, IH, J = 8.0Hz), 7.49(brs, IH), 7.51(brs, IH). 1-174 mp : 264-265 °C 1h-NMR (CDCI3+CD3OD) 6ppm: 1.26-1.29(m, 2H), 1.39(s, 9H), 1.62-1.69(m, 2H), 1.96-2.00(m, 2H), 2.18-2.21(m, 3H), 3.25(m, IH), 3.58(s, 2H), 7.01(d, IH, J = 7.5Hz), 7.26(t, IH, J = 7.5Hz), 7.42(brs, IH), 7.50(d, IH, J = 7.5Hz). 1-175 mp : 90-94 °C ^-NMR (CDCI3) 6ppm:1.16-1.23(m, 2H), 1.37(s, 9H), 1.44-1.56(m, 2H), 1.73-1.85(m, 3H), 2.11-2.15(m, 2H), 3.57(t, 2H, J = 6.4Hz), 3.21(m, IH), 3.58(m, 2H), 3.84(d, IH, J = 9.3Hz), 5.56(brs, IH), 7.01(s, IH), 7.11(t, IH, J = 7.5Hz), 7.21(t, IH, J = 7.5Hz), 7.38(d, IH, J = 7.5Hz), 7.59(d, IH, J = 7.5Hz), 8.24(brs, IH). 1-176 mp : 116-118 °C 1h-NMR (CDCI3) 6ppm:1.18-1.38 (m, 2H), 1.40 (s, 9H), 1.60-1.79 (m, 2H), 1.95-2.30 (m, 5H), 3.30 (m, IH), 3.69 (m, IH), 3.80 (s, 3H), 4.64 (s, 2H), 6.67 (d, IH, J = 8.0Hz), 7.00 (d, IH, J = 8.5Hz), 7.15-7.24 (m, 2H), 7.32 (brs, IH). 1-177 mp : 219-220 °C 1h-NMR (DMSO-d6) 5 ppm: 1.27 (s, 9H), 1.28-1.50 (m, 4H), 1.75-2.01 (m, 4H), 2.18-) 2.30 (m, IH), 2.95-3.15 (m, 2H), 4.61 (s, 2H), 6.56 (m, IH), 6.80 (d, IH, J = 8.5Hz), 7.16 (m, 2H), 7.28 (brs, IH), 9.87 (brs, IH). 1-178 mp : 170-173 °C 1h-NMR (CDC13) 6 ppm:l.18-1.39 (m, 2H), 1.40 (s, 9H), 1.50-1.80 (m, 2H), 1.90-2.33 (m, 1 5H), 2.36 (s, 6H), 2.75 (t, 2H, J = 5.5 Hz), 3.30 (m, IH), 3.70 (m, IH), 4.08 (t, 2H, J = 5.5Hz), 6.68 (d, IH, J = 8.0Hz), 6.94 (d, IH, J = 7.5Hz), 7.15-7.23 (m, 2H), 7.33 (brs, IH). 1-179 mp : 191-193 °C 1h-NMR (CDCI3) 6 ppm:1.20-1.39 (m, 2H), 1.40 (s, 9H), 1.58-1.80 (m, 2H), 1.98-2.32 (m, 5H), 3.30 (m, IH), 3.70 (d, IH, J = 9.5 Hz), 4.77 (s, 2H), 6.73 (d, IH, J = 8.0Hz), 7.04 (d, IH, J = 8.0Hz), 7.20-7.31 (m, 2H), 7.48 (brs, IH). 1-180 mp : 174-176 °C 1h-NMR (CDCI3) 5 ppm:1.10-1.30 (m, 2H), 1.40 (s, 9H), 1.45-1.65 (m, 2H), 1.81-2.02 (m, 3H), 2.15-2.30 (m, 2H), 2.58 (t, 2H, J = 6.5Hz), 3.25 (m, IH), 3.37 (dt, 2H, J = 5.5, 6.5Hz), 3.60 (d, IH, J = 9.5Hz), 3.71 (s, 2H), 5.73 (brs, IH), 7.20-7.40 (m, 5H). 1-181 mp: 176-178 °C 1h-NMR (CDCI3) 6ppm:1.15-1.30 (m, 2H), 1.39 (s, 9H), 1.45-1.70 (m, 6H), 1.85-2.01 (m, 3H), 2.15-2.28 (m, 2H), 2.63 (t, 2H, J = 7.0Hz), 3.25 (dt, 2H, J = 6.0, 7.0Hz), 3.27 (m, IH), 3.63 (m, IH), 5.35 (brs, IH), 7.17 (m, 3H), 7.29 (m, 2H). 1-182 mp: 152-154 °C 1h-NMR (CDCI3) 6 ppm:1.15-1.30 (m, 2H), 1.39 (s, 9H), 1.45-1.65 (m, 2H), 1.85-2.05 (m, 3H), 2.09-2.25 (m, 2H), 3.25 (m, IH), 3.45 (dt, 2H, J = 5.0, 5.0Hz), 3.55 (t, 2H, J = 5.0Hz), 3.60 (m, IH), 4.51 (s, 2H), 5.81 (brs, IH), 7.29-7.40 (m, 5H). 1-183 mp : 208-211 °C 1h-NMR (CDCI3) 6ppm:1.20-1.31(m, 2H), 1.39(s, 9H), 1.62-1.68(m, 2H), 1.98-2.25(m, 5H), 3.30(m, IH), 3.57(d, IH, J = 9.2Hz), 4.59(d, 2H , J = 5.8Hz), 5.76(brs, IH), 7.37(dd, IH, J = 8.4, 2.0Hz), 7.46-7.52(m, 2H), 7.69(brs, IH), 7.78-7.83(m, 3H). 1-184 mp: 180-182 °C 1h-NMR (CDCI3) 6ppm:1.22-1.37(m, 2H), 1.40(s, 9H), 1.60-1.69(m, 2H), 2.05-2.09(m, 2H), 2.21-2.27(m, 3H), 3.45(m, IH), 3.64(d, IH, J = 9.6Hz), 4.77(d, 2H, J = 4.9Hz), 7.43(d, IH, J = 8.6Hz), 7.46(brs, IH), 7.61(t, IH, J=7.7Hz), 7.73(t, IH, J= 7.7Hz), 7.87(t, IH, J = 7.7Hz), 8.20(t, IH, J = 7.7Hz), 8.24(d, IH, J = 8.6Hz). 1-185 mp : 260-261 °C 1h-NMR (CDCI3) 5ppm:1.22-1.32(m, 2H), 1.39(s, 9H), 1.60-1.70(m, 2H), 1.97-2.01(m, 2H), 2.11(m, IH), 2.21-2.24(m, 2H), 3.30(m, IH), 3.61(d, IH, J = 9.3Hz),4.95(d, 2H, J = 6.0Hz), 5.85(brs, IH), 7.33(d, IH, J=4.8Hz), 7.62(dd, IH, J = 8.4, 6.9Hz), 7.75(dd, IH, J = 8.1, 6.9Hz), 8.00(d, IH, J = 8.1Hz), 8.20(d, IH, J = 8.4Hz), 8.42(d, IH, J = 4.8Hz). 1-186 mp : 231-233 °C 1h-NMR (CDCI3) 6ppm:1.23-1.40(m, 2H), 1.40(s, 9H), 1.62-1.76(m, 2H), 2.04-2.10(m, 2H), 2.22-2.32(m, 3H), 3.30(m, IH), 3.95(d, IH, J = 9.3Hz), 5.04(d, 2H, J = 4.1Hz), 7.61(d, IH, J = 5.8Hz), 7.63(brs, IH), 7.65(dd, IH, J = 8.2, 6.9Hz), 7.73(dd, IH, J = 8.5, 6.9Hz), 7.86(d, IH, J = 8.2Hz), 8.10(d, IH, J = 8.5Hz), 8.42(d, IH, J = 5.8Hz). 1-187 mp: 184-187 °C 1h-NMR (CDCI3) 6 ppm:0.97(t, 3H, J = 7.3 Hz), 1.18-1.30(m, 2H), 1.39(s, 9H), 1.42- 1.65(m, 4H), 1.70-1.80(m, 2H), 1.94-2.08(m, 3H), 2.18-2.26(m, 2H), 3.29(m, IH), 3.61(d, IH, J = 9.5Hz), 3.93(t, 2H, J = 6.4Hz), 4.39(d, 2H, J = 5.5Hz), 5.67(brs, IH), 6.79-6.83(m, 3H), 7.23(t, IH, J=7.6Hz). 1-188 mp : 224-226 °C 1h-NMR (CDCI3) 5ppm:.16-1.31(m, 2H), 1.38(s, 9H), 1.55-1.70(m, 2H), 1.92-2.07(m, 3H), 2.17-2.23(m, 2H), 3.21(m, IH), 3.81(s, 3H), 3.83(s, 6H), 4.06(d, IH, J = 9.8Hz), 4.34(d, 2H, J = 5.8Hz), 5.96(brs, IH), 6.47(s, 2H). 1-189 mp : 217-218 °C 1h-NMR (CDCI3) 6ppm:1.15-1.30(m, 2H), 1.37(s, 9H), 1.52-1.66(m, 2H), 1.90-2.06(m, 3H), 2.13-2.20(m, 2H), 2.93(s, 6H), 3.24(m, IH), 3.94(d, IH, J = 9.5Hz), 4.30(d, 2H, J = 5.5Hz), 5.73(brs, IH), 6.69(d, 2H, J = 8.9Hz), 7.12(d, 2H, J = 8.9Hz). 1-190 mp : amorphous solid 1h-NMR (CDCI3) 6ppm:1.17-1.32(m, 2H), 1.39(s, 9H), 1.54-1.72(m, 2H), 1.96-2.13(m, 3H), 2.18-2.27(m, 2H), 3.30(m, IH), 3.63(d, IH, J = 9.2Hz), 4.51(d, 2H, J = 5.8Hz), 5.82(brs, IH), 7.40(d, 2H, J = 8.5Hz), 8.02(d, 2H, J = 8.5Hz), 8.64(s, IH). 1-191 mp : 126-128 °C 1h-NMR (CDCI3) 6ppm:0.97(t, 3H, J = 7.4 Hz), 1.10-1.28(m, 2H), 1.36(s, 9H), 1.42- 1.86(m, 9H), 2.06-2.18(111, 2H), 3.22(m, IH), 3.95(t, 2H, J = 4.5Hz), 4.16(brs, IH), 4.85(s, 2H), 6.82-6.95(m, 3H), 7.26(t, IH, J = 7.8Hz), 8.54(brs, IH). 1-192 mp : 178-181 °C 1h-NMR (CDCI3) 5 ppm:0.96(t, 3H, J = 7.3 Hz), 1.18-1.52(m, 4H), 1.39(s, 9H), 1.58- 1.76(m, 4H), 1.92-2.00(m, 2H), 2.02-2.29(m, 3H), 3.28(m, IH), 3.78(d, IH, J = 9.5Hz), 3.89(t, 2H, J = 6.6Hz), 6.00(bra, IH), 6.78(s, 4H), 7.35(brs, IH). 1-193 mp : 187-188 °C 1h-NMR (CDCI3+CD3OD) 5ppm:1.2l-1.40(m, 2H), 1.38(s, 9H), 1.52-1.69(m, 2H), 1.90- 2.00(m, 2H), 2.02-2.20(m, 3H), 3.22(m, IH), 3.75(s, 3H), 6.79(s, 4H). 1-194 mp : 251-253 °C 1h-NMR (DMSO-d6) 6ppm:1.27(s, 9H), 1.24-1.50(m, 4H), 1.72-1.83(m, 2H), 1.91- 1.99(m, 2H), 2.16(m, IH), 3.02(m, IH), 3.82(s, 3H), 6.79(d, IH, J = 8.2Hz), 7.01(d, 2H, J = 8.8Hz), 7.85(d, 2H, J = 8.8Hz), 9.72(brs, IH), 8.64(brs, IH). 1-195 mp : 183-185 °C 1h-NMR (CDCI3) Sppm:1.22-1.37(m, 2H), 1.40(s, 9H), 1.58-1.75(m, 2H), 2.05-2.10(m, 2H), 2.20-2.30(m, 3H), 3.32(m, IH), 3.70(s, 2H), 3.73(s, 3H), 6.79(s, IH), 8.83(brs, IH). 1-196 mp : 185-187 °C 1h-NMR (CDCI3) 6 ppm:1.20-1.39 (m, 2H), 1.40 (s, 9H), 1.44 (t, 6H, J = 7.0 Hz), 1.60- 1.80 (m, 2H), 1.95-2.35 (m, 5H), 3.30 (m, IH), 3.62 (d, IH, J = 8.9 Hz), 4.06 (q, 2H, J = 7.0 Hz), 4.09 (q, 2H, J = 7.0 Hz), 6.08 (s, IH), 7.02 (s, IH), 7.36 (s, IH). 1-197 mp : 211-213 °C 1h-NMR (CDCI3) 5 ppm:1.20-1.40 (m, 2H), 1.41 (s, 9H), 1.60-1.80 (m, 2H), 2.00-2.36 (m, 5H), 2.61 (s, 3H), 3.32 (m, IH), 3.64 (d, IH, J = 9.2 Hz), 7.28 (s, IH), 7.43 (t, IH, J= 7.5 Hz), 7.69 (d, IH, J = 7.5 Hz), 7.85 (d, IH, J = 7.5 Hz), 8.02 (s, IH). 1-198 mp : 268-269 °C 1h-NMR (CDCI3) 6ppm:1.20-1.39 (m, 2H), 1.40 (s, 9H), 1.42-2.32 (m, 7H), 2.90-3.10 (m, 4H), 3.30 (m, IH), 3.68 (d, IH, J = 8.8 Hz), 6.59 (s, IH), 7.18 (d, IH, J = 8.7 Hz), 7.59 (d, IH, J = 8.7 Hz), 7.77 (brs, IH). 1-199 mp : 221-224 °C 1-200 mp : 237-240 °C 1-201 mp : 87-90 °C 1-202 mp : 222-223°C 1-203 mp : 255-257 °C 1-204 mp : 234-236 °C 1-205 mp : 208-210 °C 1-206 mp : 217-218 °C 1-207 mp : 275-279 °C 1-208 mp : 248-250 °C 1-209 mp : 256-258 °C 1-210 mp: 270-271 °C 1-211 mp : 219-220 °C 1-212 mp : 260-261 °C 1-213 mp : >300 °C 1-214 mp : 206-207 °C 1h-NMR (CDCI3) 6 ppm: 0.93(t, 3H, J = 7.4 Hz), 1.30-1.42(m, 2H), 1.49(d, 6H, J = 6.9 Hz), 1.53-1.65(m, 2H), 2.61(t, 2H, J = 7.7 Hz), 4.15(sept, IH, J = 6.9 Hz), 7.04(d, IH, J = 8.2 Hz), 7.20(d, 2H, J = 8.2 Hz), 7.51(d, 2H, J = 8.2 Hz), 7.89(d, IH, J = 8.8 Hz), 8.18(s, IH), 10.55(s, IH). 1-215 1h-NMR (CDCI3) 5 ppm:0.93(t, 3H, J = 7.3Hz), 1.30-1.41(m, 2H), 1.52-1.63(m, 2H), 1.95(8, 6H), 2.61(t, 2H, J = 7.8Hz), 6.99(brs, IH), 7.20(d, 2H, J = 8.5Hz), 7.65(d, 2H, J = 8.5Hz), 7.93(dd, IH, J = 8.5, 2.5Hz), 8.28(d, IH, J = 8.5Hz), 8.55(d, IH, J = 2.5Hz), 9.76(brs, IH). Ia-1 mp 221-224 °C 1h-NMR (CDC13) 6ppm: 1.19-1.38 (m, 2H), 1.40 (s, 9H), 1.62-1.77 (m, 2H), 2.00-2.31 (m, 5H), 3.18 (t, 4H, J = 4.8 Hz), 3.21-3.38 (m, IH), 3.85 (t, 4H, J = 4.8 Hz), 6.64-6.32 (m, 2H), 7.11 (s, IH), 7.20 (t, IH, J = 7.8 Hz), 7.45 (s, IH). Ia-3 mp 87-90 °C 1h-NMR (CDCI3) 5 ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.37 (d, 6H, J = 6.9 Hz), 1.59-1.70 (m, 2H), 1.76-1.88 (m, 2H), 2.32-2.42 (m, 4H), 3.11-3.23 (m, 3H), 3.39 (d, 2H, J = 10.8 Hz), 3.74-3.86 (m, 2H), 4.34 (t, IH, J = 9.0 Hz), 6.86 (d, 2H, J = 9.0 Hz), 7.30 (s, IH), 7.40 (d, 2H, J = 9.0 Hz). Ia-4 mp 233-234 °C 1h-NMR (CDCI3) 5 ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.40 (s, 9H), 1.26-1.37 (m, 2H), 1.62- 1.78 (m, 2H), 2.00-2.22 (m, 5H), 2.42 (t, 2H, J = 11.7 Hz), 3.20-3.40 (m, IH), 3.46 (d, 2H, J = 10.5 Hz), 3.67 (d, IH, J = 9.3 Hz), 3.72-3.84 (m, 2H), 6.62-6.76 (m, 2H), 7.10 (s, IH), 7.18 (t, IH, J = 7.8 Hz), 7.42 (s, IH). Ia-5 mp 125-126 °C 1H-NMR (CDCI3) 6 ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.40 (s, 9H), 1.59-1.70 (m, 2H), 1.77- 1.84 (m, 2H), 2.30-2.46 (m, 4H), 3.24 (q, 2H, J = 6.6 Hz), 3.38 (d, 2H, J = 11.7 Hz), 3.74- 3.88 (m, 2H), 4.08 (t, IH, J = 5.7 Hz), 6.87 (d, 2H, J = 8.7 Hz), 7.30 (s, IH), 7.41 (d, 2H, J = 8.7 Hz). Ia-6 mp 229-230 °C 1h-NMR (CDCI3) 5 ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.26-1.34 (m, 2H), 1.39 (d, 6H, J = 6.9 Hz), 1.61-1.77 (m, 2H), 1.98-1.26 (m, 5H), 2.32-2.46 (m, 2H), 3.15 (quintet, IH, J = 6.6 Hz), 3.22-3.35 (m, IH), 3.39 (d, 2H, J= 11.4 Hz), 3.74-3.92 (m, 2H), 3.88 (d, IH, J = 8.4 Hz), 6.96-6.71 (m, 2H), 7.05 (brs, IH), 7.39 (d, 2H, J = 9.3 Hz). Ia-7 mp 253-254 °C 1h-NMR (DMSO) 5 ppm: 1.24-1.60 (m, 4H), 1.27 (s, 9H), 1.77-2.07 (m, 4H), 2.16-2.34 (m, IH), 2.97-3.15 (m, IH), 6.78 (d, IH, J = 7.2 Hz), 7.01 (t, IH, J = 6.0 Hz), 7.27 (t, 2H, J = 6.6 Hz), 7.58 (d, 2H, J = 7.5 Hz), 9.78 (s, IH). Ia-8 mp 257-258 °C 1h-NMR (DMSO) 5 ppm: 1.22-1.54 (m, 4H), 1.27 (s, 9H), 1.77-1.88 (m, 2H), 1.88-2.00 (m, 2H), 2.16-2.34 (m, IH), 2.23 (s, 3H), 2.92-3.14 (m, IH), 6.77 (d, IH, J = 8.4 Hz), 7.07 (d, 2H, J = 8.4 Hz), 7.46 (d, 2H, J = 8.1 Hz), 9.68 (s, IH). Ia-9 mp 231-232 °C 1h-NMR (CDCI3) 6 ppm: 1.21 (t, 3H, J = 7.5 Hz), 1.22-1.38 (m, 2H), 1.40 (s, 9H), 1.62- 1.78 (m, 2H), 1.98-2.31 (m, 5H), 2.61 (q, 2H, J = 7.5 Hz), 3.24-3.38 (m, IH), 3.70 (d, IH, J = 9.9 Hz), 7.11 (s, IH), 7.14 (d, 2H, J = 8.7 Hz), 7.40 (d, 2H, J = 8.7 Hz). Ia-10 mp 233-234 °C 1h-NMR (CDCI3) 5 ppm: 0.96 (t, 3H, J = 7.2 Hz), 1.20-1.37 (m, 2H), 1.40 (s, 9H), 1.56- 1.78 (m, 4H), 1.98-2.32 (m, 5H), 2.54 (t, 2H, J= 7.2 Hz), 3.23-3.39 (m, IH), 3.66 (d, IH, J = 9.6 Hz), 7.08 (s, IH), 7.12 (d, 2H, J = 8.4 Hz), 7.39 (d, 2H, J = 8.4 Hz). Ia-11 mp 243-244 °C 1h-NMR (CDC13) 5 ppm: 1.22 (d, 6H, J = 6.9), 1.22-1.77 (m, 4H), 1.40 (s, 9H), 2.01-2.30 (m, 5H), 2.83-2.92 (m, IH), 3.24-3.40 (m, IH), 3.66-3.69 (m, IH), 7.09 (s, IH), 7.17 (d, 2H, J = 8.4 Hz), 7.41 (d, 2H, J = 8.1 Hz). Ia-12 mp 246-247 °C 1h-NMR (CDC13) 6 ppm: 0.80 (t, 3H, J = 7.5), 1.20 (d, 3H, J = 7.2), 1.26-1.77 (m, 6H), 1.40 (s, 9H), 2.01-2.27 (m, 5H), 2.51-2.60 (m, IH), 3.20-3.38 (m, IH), 3.64-3.69 (m, IH), 7.08 (s, IH), 7.12 (d, 2H, J = 8.4 Hz), 7.41 (d, 2H, J = 8.4 Hz). Ia-13 mp 278-279 °C 1h-NMR (CDC13) 6 ppm: 1.22-1.52 (m, 4H), 1.29 (s, 9H), 1.40 (s, 9H), 1.61-1.77 (m, 2H), 2.02-2.30 (m, 5H), 3.20-3.38 (m, IH), 3.66-3.69 (m, IH), 7.10 (s, IH), 7.33 (d, 2H, J = 9.0 Hz), 7.42 (d, 2H, J = 8.7 Hz). Ia-14 mp 263-264 °C 1h-NMR (DMSO) 6 ppm: 1.24-1.51 (m, 4H), 1.27 (s, 9H), 1.82-1.99 (m, 4H), 2.19-2.28 (m, IH), 2.98-3.12 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.33 (d, 2H, J = 8.7 Hz), 7.61 (d, 2H, J = 9.0 Hz), 9.94 (s, IH). Ia-15 mp 209-210 °C 1h-NMR (CDC13) 6 ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.40 (s, 9H), 1.70-1.98 (m, 8H), 2.19- 2.38 (m, 3H), 3.39 (d, 2H, J= 11.7 Hz), 3.58-3.92 (m, 3H), 4.12-4.26 (m, IH), 6.82-6.96 (m, 2H), 7.10 (br, IH), 7.41 (d, 2H, J = 8.1 Hz). Ia-16 mp 238-240 °C 1h-NMR (DMSO) 5 ppm: 1.22-1.52 (m, 4H), 1.27 (a, 9H), 1.81-1.84 (m, 2H), 1.93-1.97 (m, 2H), 2.16-2.23 (m, IH), 2.95-3.12 (m, IH), 3.70 (s, 3H), 6.77 (d, IH, J = 8.4 Hz), 6.85 (d, 2H, J = 9.0 Hz), 7.48 (d, 2H, J = 9.3 Hz), 9.64 (s, IH). Ia-17 mp 245-246 °C 1h-NMR (DMSO) Sppm: 1.22-1.52 (m, 4H), 1.27 (s, 9H), 1.83-1.87 (m, 2H), 1.94-1.99 (m, 2H), 2.20-2.28 (m, IH), 2.98-3.12 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.28 (d, 2H, J = 8.7 Hz), 7.69 (d, 2H, J = 9.0 Hz), 9.64 (s, IH). Ia-18 mp 240-241 °C H-NMR (CDC13) 6 ppm: 1.22-1.78 (m, 4H), 1.40 (s, 9H), 2.05-2.33 (m, 5H), 3.22-3.44 (m, IH), 3.64-3.67 (m, IH), 6.61 (s, IH), 6.69-6.77 (m, 2H). Ia-19 mp 240-241 °C XH-NMR (CDC13) 6 ppm: 1.24-1.77 (m, 4H), 1.40 (s, 9H), 2.05-2.30 (m, 5H), 3.22-3.38 (m, IH), 3.70-3.74 (m, IH), 7.00-7.15 (m, 3H), 7.36 (s, IH), 8.29-8.34 (m, IH). Ia-20 mp 239-240 °C 1h-NMR (CDC13) 6 ppm: 1.24-1.78 (m, 4H), 1.40 (s, 9H), 2.02-2.30 (m, 5H), 3.22-3.40 (m, IH), 3.63-3.66 (m, IH), 6.89-6.84 (m, IH), 7.10-7.17 (m, 2H), 7.22-7.34 (m, IH), 7.48-7.51 (m, IH). Ia-21 mp 259-260 °C 1h-NMR (CDCI3/DMSO) 6 ppm: 1,21 (d, 6H, J = 6.0 Hz), 1.22-1.44 (m, 2H), 1.40 (s, 9H), 1.60-1.78 (m, 2H), 1.87-2.03 (m, 2H), 2.08-2.29 (m, 3H), 2.39 (t, 2H, J = 10.2 Hz), 3.14-3.32 (m, IH), 3.19 (d, 2H, J = 11.4 Hz), 3.77-3.93 (m, 2H), 5.33 (d, IH, J = 9.0 Hz), 6.84 (dd, IH, JFH, HH = 8.1, 8.1 Hz), 7.20 (d, IH, J = 7.8 Hz), 7.49 (d, IH, JFH = 14.7 Hz), 8.86 (s, IH). Ia-22 mp 234-235 °C 1h-NMR (CDCI3) 5ppm: 1,20 (d, 6H, J = 5.7 Hz), 1.22-1.44 (m, 2H), 1.38 (s, 9H), 1.54- 1.76 (m, 2H), 1.94-2.32 (m, 5H), 2.27 (s, 3H), 2.39 (t, 2H, J= 10.8 Hz), 2.87 (d, 2H, J= 11.4 Hz), 3.20-3.40 (m, 1H), 3.76-3.92 (m, 2H), 3.91 (d, 1H, J = 9.3 Hz), 6.93 (d, 1H, J = 8.1 Hz), 7.21 (brs, 1H), 7.27 (bra, 1H), 7.36 (brs, 1H). Ia-23 mp 195-196 °C 1h-NMR (CDCI3) 6ppm: 1.20-1.44 (m, 4H), 1.41 (s, 9H), 1.59-1.76 (m, 2H), 2.03-2.14 (m, 2H), 2.15-2.33 (m, 3H), 3.20-3.40 (m, 1H), 3.64 (s, 1H, J = 9.0 Hz), 7.19-7.24 (m, 1H), 7.44 (brs, 1H), 7.52-7.63 (m, 2H), 8.17 (d, 1H, J = 8.7 Hz). Ia-24 mp 209-210 °C 2H-NMR (CDCI3) Sppm: 1.22-1.39 (m, 2H), 1.56 (s, 9H), 1.61-1.78 (m, 2H), 2.00-2.12 (m, 2H), 2.17-2.33 (m, 3H), 3.24-3.39 (m, 1H), 3.67 (d, 1H, J = 9.6 Hz), 6.90-7.01 (m, 1H), 7.21 (s, 1H), 7.95-8.06 (m, 1H). Ia-25 mp 278-281 °C 1h-NMR (DMSO-d6) 5 ppm: 1.10 (d, 6H, J = 6.3 Hz), 1.27 (s, 9H), 1.28-1.55 (m, 4H), 1.78-2.00 (m, 4H), 2.11-2.26 (m, 1H), 2.31 (t, 2H, J = 11.1 Hz), 3.00-3.10 (m, 1H), 3.08 (d, 1H, J = 10.8 Hz), 3.67-3.80 (m, 2H), 6.78 (d, 1H, J = 8.7 Hz), 7.08 (d, 1H, J = 9.0 Hz), 7.41 (dd, 1H, J = 2.4, 8.7 Hz), 7.78 (d, 1H, J = 8.7 Hz), 9.85 (s, 1H). Ia-26 mp 253-255 °C 1h-NMR (DMSO-d6) Sppm: 1.13 (d, 6H, J = 6.0 Hz), 1.27 (s, 9H), 1.28-1.52 (m, 4H), 1.78-2.00 (m, 4H), 2.21 (t, 2H, J = 11.1 Hz), 2.26-2.36 (m, 1H), 2.96-3.10 (m, 1H), 3.56 (d, 1H, J= 12.3 Hz), 3.60-3.72 (m, 2H), 6.66-6.84 (m, 4H), 7.47 (t, 1H, J = 9.3 Hz), 9.28 (s, 1H). Ia-27 mp 223-226 °C 1h-NMR (DMSO-d6) 6 ppm: 1.09 (d, 6H, J = 6.3 Hz), 1.27 (s, 9H), 1.28-1.54 (m, 4H), 1.77-2.01 (m, 4H), 2.32 (t, 2H, J = 11.1 Hz), 2.32-2.42 (m, 1H), 2.90 (d, 1H, J = 11.4 Hz), 2.96-3.12 (m, 1H), 3.76-3.92 (m, 2H), 6.78-6.98 (m, 3H), 7.68 (dd, 1H, J = 3.3, 8.7 Hz), 8.84 (s, 1H). Ia-28 mp 237-238 °C 1h-NMR (CDCI3) 8 ppm: 1.22-1.44 (m, 2H), 1,25 (d, 6H, J = 6.3 Hz), 1.40 (s, 9H), 1.61- 1.79 (m, 2H), 2.05-2.32 (m, 5H), 2.21 (s, 3H), 2.38 (t, 2H, J= 10.2 Hz), 3.22-3.42 (m, 1H), 3.40 (d, 2H, J = 11.1 Hz), 3.65 (d, 1H, J = 9.3 Hz), 3.72-3.90 (m, 2H), 6.70-6.78 (m, 2H), 6.81 (brs, 1H), 7.50 (d, 1H, J = 9.6 Hz). Ia-29 mp 208-209 °C 1h-NMR (CDCI3) 6 ppm: 1.22 (d, 6H, J = 6.0 Hz), 1.23-1.40 (m, 2H), 1.40 (s, 9H), 1.60- 1.78 (m, 2H), 2.00-2.16 (m, 2H), 2.14-2.33 (m, 3H), 2.45 (t, 2H, J = 11.1 Hz), 3.21 (d, 2H, J = 10.8 Hz), 3.24-3.38 (m, 1H), 3.63 (d, 1H, J = 9.3 Hz), 3.80-3.94 (m, 2H), 5.33 (d, 1H, J = 9.0 Hz), 6.66 (dd, 1H, JFH, HH = 6.6, 6.6 Hz), 7.16 (brs, 1H), 7.89 (dd, 1H, JFH, HH = 9.0, 9.0 Hz). Ia-30 mp 284-287 °C 1h-NMR (DMSO-d6) 6 ppm: 1.08 (d, 6H, J = 6.0 Hz), 1.26 (s, 9H), 1.28-1.53 (m, 4H), 1.82-2.22 (m, 4H), 2.25-2.39 (m, 1H), 2.78 (t, 2H, J = 10.5 Hz), 2.97-3.14 (m, 1H), 3.18 (d, 2H, J = 11.4 Hz), 3.65-3.76 (m, 2H), 6.79 (d, 1H, J = 8.7 Hz), 9.75 (s, 1H). Ia-31 mp 200-201 °C 1h-NMR (CDC13) 6 ppm: 1.22-1.40 (m, 2H), 1.40 (s, 9H), 1.62-1.76 (m, 2H), 2.04-2.32 (m, 5H), 3.22-3.40 (m, 1H), 3.62-3.66 (m, 1H), 7.22-7.24 (m, 1H), 7.38-7.38 (m, 1H), 7.60 (s, IH), 8.33-8.36 (m, IH). Ia-32 mp 260-261 °C 1h-NMR (CDCI3/DMSO) 6 ppm: 1.25-1.42 (m, 2H), 1.38 (s, 9H), 1.64 (q, 2H, J = 13.5 Hz), 1.95 (d, 2H, J= 12.3 Hz), 2.16 (d, 2H, J = 10.5 Hz), 2.18-2.32 (m, IH), 3.14-3.30 (m, IH), 5.53 (d, IH, J = 9.0 Hz), 7.31 (d, IH, J = 8.7 Hz), 7.46 (dd, IH, J = 2.4, 8.7 Hz), 7.90 (d, IH, J = 2.1 Hz), 9.35 (s, IH). Ia-33 mp 227 °C 1h-NMR (DMSO-d6) 5 ppm: 1.27 (s, 9H), 1.30-1.56 (m, 4H), 1.78-2.01 (m, 2H), 2.12-2.36 (m, 2H), 2.96-3.13 (m, IH), 3.70 (s, 3H), 3.71 (s, 3H), 6.77 (d, IH, J = 8.7 Hz), 6.85 (d, IH, J = 8.7 Hz), 7.06 (dd, IH, J = 2.4, 8.7 Hz), 7.33 (d, IH, J = 2.4 Hz), 9.65 (s, IH). Ia-35 mp 214-216 °C 1h-NMR (CDCI3) 6 ppm: 1.23-1.38 (m, 2H), 1.40 (s, 9H), 1.60-1.76 (m, 2H), 2.00-2.12 (m, 2H), 2.20-2.32 (m, 3H), 3.24-3.39 (m, IH), 3.68 (d, IH, J = 9.0 Hz), 6.77 (d, IH, J = 8.7 Hz), 7.00 (dd, IH, J = 2.4, 8.7 Hz), 7.77 (s, IH), 8.45 (d, IH, J = 2.4 Hz). Ia-36 mp 241-242 °C XH-NMR (CDCI3/DMSO) 6 ppm: 1.25-1.42 (m, 2H), 1.37 (a, 9H), 1.62 (q, 2H, J = 11.7 Hz), 1.93 (d, 2H, J = 12.0 Hz), 2.12 (d, 2H, J = 10.8 Hz), 2.16-2.30 (m, IH), 3.12-3.28 (m, IH), 3.84 (s, 3H), 6.07 (d, IH, J = 8.4 Hz), 6.89 (dd, IH, JFH, HH = 9.3, 9.3 Hz), 7.24 (d, IH, J = 8.7 Hz), 7.55 (d, IH, JFH = 13.5 Hz), 9.32 (s, IH). Ia-37 mp 248-249 °C 1h-NMR (CDC13) 6 ppm: 0.60-0.73 (m, IH), 0.91 (d, 6H, J = 6.6), 1.12-1.40 (m, 2H), 1.40 (s, 9H), 1.54-1.88 (m, 5H), 1.98-2.29 (m, 7H), 3.22-3.37 (m, IH), 3.51-3.54 (m, 2H), 3.72 (d, IH, J = 9.6), 6.88 (d, IH, J = 8.7), 7.06 (s, IH), 7.35 (d, IH, J = 9.0). Ia-38 mp 237-238 °C 1h-NMR (CDC13) 6 ppm: 1.01 (d, 6H, J = 6.6), 1.20-1.40 (m, 2H), 1.40 (s, 9H), 1.60-1.74 (m, 4H), 1.99-2.28 (m, 7H), 2.69-2.82 (m, 2H), 3.02-3.14 (m, 2H), 3.20-3.38 (m, IH), 3.80- 3.90 (m, IH), 6.83-6.86 (m, 2H), 7.14 (s, IH), 7.34 (d, IH, J = 8.4). Ia-39 mp 234-235 °C 2H-NMR (CDC13) 5 ppm: 1.20-1.36 (m, 2H), 1.40 (s, 9H), 1.60-1.77 (m, 2H), 1.90-2.32 (m, 5H), 3.21-3.39 (m, IH), 3.65 (d, IH, J = 9.6 Hz), 6.87 (d, IH, J = 8.7 Hz), 7.04 (s, IH), 7.37 (dd, IH, J = 2.7, 8.7 Hz), 7.56 (d, IH, J = 2.7 Hz). Ia-40 mp 257-258 °C H-NMR (DMSO-d6) 6 ppm: 1.14 (d, 6H, J = 6.0 Hz), 1.27 (s, 9H), 1.28-1.53 (m, 4H), 1.78-2.00 (m, 4H), 2.13-2.256 (m, IH), 2.30 (t, 2H, J = 11.7 Hz), 2.97-3.12 (m, IH), 3.53- 3.67 (m, 2H), 4.01 (d, IH, J = 12.3 Hz), 6.80 (dd, IH, J = 3.0, 9.0 Hz), 7.79 (d, IH, J = 9.0 Hz), 8.27 (s, IH), 9.66 (s, IH). Ia-41 mp 245-246 °C 1h-NMR (CDCI3/DMSO) 5 ppm: 1.25-1.42 (m, 2H), 1.37 (s, 9H), 1.62 (q, 2H, J = 12.6 Hz), 1.94 (d, 2H, J= 11.1 Hz), 2.13 (d, 2H, J= 11.1 Hz), 2.18-2.35 (m, IH), 3.11-3.29 (m, IH), 6.07 (d, IH, J = 8.1 Hz), 6.95-7.06 (m, IH), 7.14-7.27 (m, IH), 7.44 (d, IH, J = 7.2 Hz), 7.79 (s, IH), 9.48 (s, IH). Ia-43 mp 294-295 °C 1h-NMR (DMSO-d6) 5 ppm: 1.26 (s, 9H), 1.28-1.53 (m, 4H), 1.76-1.87 (m, 2H), 1.89-2.00 (m, 2H), 2.13-2.25 (m, IH), 2.96-3.10 (m, 5H), 3.52-3.60 (m, 4H), 6.78 (d, IH, J = 9.0 Hz), 6.88 (d, 2H, J = 9.0 Hz), 7.44 (d, 2H, J = 9.0 Hz), 9.59 (s, IH). Ia-44 mp 250-252 °C 1h-NMR (CDC13) 5 ppm: 1.13 (d, 6H, J = 6.3 Hz), 1.21-1.38 (m, 2H), 1.41 (s, 9H), 1.63- 1.80 (m, 2H), 1.93 (t, 2H, J = 10.8 Hz), 2.00-2.10 (m, 2H), 2.16-2.32 (m, 3H), 3.24-3.39 (m, IH), 3.54 (d, 2H, J = 10.2 Hz), 3.64-3.78 (m, 3H), 7.47 (s, IH), 7.69 (d, 2H, J = 9.0 Hz), 7.73 (d, 2H, J = 9.0 Hz). Ia-45 mp 193 °C 1h-NMR (DMSO-d6) 5 ppm: 1.10 (t, 6H, J = 7.2 Hz), 1.26 (s, 9H), 1.28-1.52 (m, 4H), 1.75-1.86 (m, 2H), 1.89-2.01 (m, 2H), 2.10-2.22 (m, IH), 2.96-3.10 (m, IH), 3.30-3.52 (m, 12H), 6.60 (d, 2H, J = 9.0 Hz), 6.80 (d, IH, J = 9.0 Hz), 7.33 (d, 2H, J = 9.0 Hz), 9.46 (s, IH). Ia-46 mp >300 °C 1h-NMR (DMSO-dg) 5 ppm: 1.28 (s, 9H), 1.28-1.58 (m, 4H), 1.83-2.04 (m, 4H), 2.23-2.36 (m, IH), 2.46 (s, 3H), 3.00-3.14 (m, IH), 6.79 (d, IH, J = 8.7 Hz), 7.34 (d, IH, J = 8.7 Hz), 7.78 (d, 2H, J = 8.7 Hz), 7.89 (d, IH, J = 8.4 Hz), 7.91 (s, IH), 8.00 (d, 2H, J = 8.7 Hz), 10.13 (s, IH). Ia-47 mp 236-237 °C 1h-NMR (CDCI3) 6 ppm: 0.97 (d, 6H, J = 6.6 Hz), 1.01 (d, 6H, J = 6.6 Hz), 1.20-1.37 (m, 2H), 1.40 (s, 9H), 1.60-1.84 (m, 3H), 1.97-2.31 (m, 5H), 2.50 (t, IH, J= 10.8 Hz), 2.78 (dt, IH, J = 3.3, 11.4 Hz), 3.25-3.38 (m, IH), 3.45 (d, IH, J= 11.4 Hz), 3.75 (dt, IH, J = 2.4, 11.4 Hz), 4.02 (dt, IH, J = 2.4, 11.4 Hz), 6.88 (d, 2H, J = 9.0 Hz), 7.05 (s, IH), 7.39 (d, 2H, J = 9.0 Hz). Ia-48 mp 228-229 °C XH-NMR (CDCI3) 6 ppm: 0.88 (t, 6H, J = 7.2 Hz), 1.19-1.45 (m, 4H), 1.40 (s, 9H), 1.45- 1.76 (m, 4H), 1.76-1.92 (m, IH), 1.96-2.30 (m, 5H), 2.66-3.20 (m, 3H), 3.20-3.40 (m, IH), 3.78 (d, IH, J = 9.3 Hz), 3.82 (s, IH), 6.62-6.98 (m, 2H), 7.09 (brs, IH), 7.37 (d, 2H, J = 7.8 Hz). Ia-49 mp 262-263 °C 1h-NMR (CDCI3/DMSO) 6 ppm: 1.21 (d, 6H, J = 5.7 Hz), 1.26-1.34 (m, 2H), 1.37 (d, 6H, J = 5.4 Hz), 1.52-1.76 (m, 2H), 1.85-2.03 (m, 2H), 2.03-2.30 (m, 3H), 2.30-2.53 (m, 2H), 3.02-3.33 (m, 4H), 3.75-3.98 (m, 2H), 5.70 (brs, IH), 6.73-6.98 (m, IH), 7.14-7.25 (m, IH), 7.52 (d, IH, JFH = 13.5 Hz), 8.86 (brs, IH). Ia-50 mp 232-233 °C 1h-NMR (CDCI3) 6 ppm: 1.21 (d, 6H, J = 6.3 Hz), 1.22-1.37 (m, 2H), 1.38 (d, 6H, J = 6.9 Hz), 1.68 (q, 2H, J = 12.6 Hz), 1.98-2.26 (m, 5H), 2.29 (s, 3H), 2.41 (t, 2H, J = 10.2 Hz), 2.88 (d, 2H, J = 11.1 Hz), 3.15 (septet, IH, J = 6.6 Hz), 3.21-3.37 (m, IH), 3.77-3.92 (m, 2H), 3.87 (d, IH, J = 7.8 Hz), 6.88-7.06 (m, 3H), 7.35 (s, IH). Ia-51 mp 211-212 °C 1h-NMR (CDC13) 5 ppm: 1.20-1.42 (m, 2H), 1.26 (d, 6H, J = 6.3 Hz), 1.38 (d, 6H, J = 6.9 Hz), 1.62-1.78 (m, 2H), 1.99-2.28 (m, 5H), 2.49 (dd, 2H, J= 10.5, 10.5 Hz), 3.17 (quint, IH, J = 6.9 Hz), 3.20-3.38 (m, IH), 3.66-3.99 (m, 2H), 3.90-4.01 (m, 3H), 6.62 (d, IH, J= 9.0 Hz), 7.06 (s, IH), 7.90 (dd, lH, J = 2.4, 9.0 Hz), 8.09 (d, IH, J = 2.4 Hz). Ia-52 mp 247-249 °C 1h-NMR (CDCI3) 6 ppm: 1.21-1.36 (m, 2H), 1.40 (s, 9H) 1.62-1.78 (m, 2H), 1.98-2.32 (m, 5H), 2.55 (t, 4H, J = 6.0 Hz), 3.23-3.38 (m, IH), 3.55 (t, 4H, J = 6.0 Hz), 3.72 (d, IH, J = 9.6 Hz), 6.94 (d, 2H, J = 9.0 Hz), 7.10 (s, IH), 7.42 (d, IH, J = 9.0 Hz). Ia-53 mp 234-235 °C 1h-NMR (CDC13) 6 ppm: 1.22-1.38 (m, 2H), 1.41 (s, 9H) 1.64-1.80 (m, 2H), 2.00-2.32 (m, 5H), 3.25-3.40 (m, IH), 3.73 (d, IH, J = 9.3 Hz), 7.43 (a, IH), 7.48 (t, 2H, J = 7.5 Hz), 7.55- 7.66 (m, 3H), 7.68-7.89 (m, 4H). Ia-54 mp 235-236 °C 1h-NMR (CDCI3) 5 ppm: 1.24-1.39 (m, 2H), 1.25 (d, 6H, J = 6.3 Hz), 1.39 (d, 6H, J = 6.9 Hz), 1.60-1.80 (m, 2H), 2.00-2.28 (m, 5H), 2.21 (s, 3H), 2.38 (t, 2H, J= 10.8 Hz), 3.15 (septet, IH, J = 6.3 Hz), 3.23-3.38 (m, IH), 3.40 (d, 2H, J = 11.7 Hz), 3.72-3.88 (m, 2H), 3.87 (d, IH, J = 9.3 Hz), 6.78-6.86 (m, 3H), 7.50 (d, IH, J = 9.6 Hz). Ia-55 mp 185-186 °C 1h-NMR (CDCI3) 6 ppm: 1.14 (d, 6H, J = 6.3 Hz), 1.22-1.38 (m, 2H), 1.41 (s, 9H), 1.62- 1.78 (m, 2H), 2.02 (t, 2H, J= 10.5 Hz), 2.02-2.10 (m, 2H), 2.16-2.31 (m, 3H), 3.24-3.39 (m, IH), 3.56 (d, 2H, J = 9.3 Hz), 3.63-3.80 (m, 3H), 7.46 (dd, IH, J= 1.5, 8.1 Hz), 7.51 (t, IH, J = 8.1 Hz), 7.63 (s, IH), 7.81 (t, IH, J = 1.8 Hz), 7.98 (dt, IH, J = 1.8, 8.1 Hz). Ia-56 mp 229-230 °C 1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.28-1.54 (m, 4H), 1.38 (s, 6H), 1.78-1.84 (m, 2H), 1.90-2.00 (m, 2H), 2.15-2.30 (m, IH), 2.97-3.13 (m, IH), 4.90 (s, IH), 6.79 (d, IH, J = 9.0 Hz), 7.34 (d, 2H, J = 8.7 Hz), 7.48 (d, 2H, J = 8.4 Hz), 9.72 (s, IH). Ia-57 mp 211-212 °C 1h-NMR (CDCI3/DMSO) 6 ppm: 1.24-1.40 (m, 2H), 1.38 (s, 9H), 1.57-1.74 (m, 2H), 1.91 (s, 3H), 1.92-2.01 (m, 2H), 2.12-2.24 (m, 2H), 2.51 (brs, IH), 3.18-3.33 (m, IH), 4.96 (d, IH, J = 9.3 Hz), 7.16-7.53 (m, 9H), 7.41 (s, IH). Ia-58 mp 298-299 °C 1h-NMR (DMSO-d6) Sppm: 1.24 (s, 9H), 1.27 (s, 9H), 1.28-1.54 (m, 4H), 1.75-2.02 (m, 4H), 2.14-2.28 (m, IH), 2.97-3.11 (m, IH), 6.78 (d, IH, J= 8.4 Hz), 7.18 (d, 2H, J = 9.0 Hz), 7.48 (d, 2H, J = 9.0 Hz), 9.46 (s, IH), 9.76 (s, IH). Ia-59 mp 253-254 °C XH-NMR (CDC13) Sppm: 1.22-1.40 (m, 2H), 1.41 (s, 9H), 1.65-1.81 (m, 2H), 2.04-2.16 (m, 2H), 2.22-2.36 (m, 2H), 3.24-3.41 (m, IH), 3.74 (d, IH, J = 9.6 Hz), 7.40-7.54 (m, 3H), 7.88-8.01 (m, 3H), 8.66 (d, IH, J = 1.5 Hz), 9.57 (d, IH, J = 1.2 Hz). Ia-60 mp 213-214 QC 1h-NMR (DMSO) Sppm: 1.32-1.50 (m, 2H), 1.35 (s, 9H), 1.52-1.70 (m, 2H), 1.88-2.00 (m, 2H), 2.04-2.16 (m, 2H), 2.22-2.38 (m, IH), 2.65 (s, 3H), 2.99-3.15 (m, IH), 6.46 (d, IH, J = 9.3 Hz), 7.28 (d, IH, J = 9.0 Hz), 7.81 (s, IH), 8.20 (s, IH), 8.47 (s, IH), 9.89 (s, IH). Ia-61 mp 274-275 °C 1h-NMR (DMSO) Sppm: 1.27 (s, IH), 1.28-1.58 (m, 4H), 1.84-2.08 (m, 4H), 2.22-2.40 (m, IH), 2.99-3.15 (m, IH), 3.01 (s, 3H), 6.81 (d, IH, J = 8.1 Hz), 7.78 (d, 2H, J = 7.8 Hz), 7.84 (d, 2H, J = 8.4 Hz), 8.18 (s, IH), 10.43 (s, IH). Ia-62 mp 235-236 °C 1h-NMR (CDCI3) 6 ppm: 1.22-1.39 (m, 2H), 1.41 (s, 3H), 1.66-1.80 (m, 2H), 2.01-2.12 (m, 2H), 2.14-2.22 (m, IH), 2.23-2.34 (m, 2H), 3.24-3.42 (m, IH), 3.69 (d, IH, J = 9.5 Hz), 6.44 (d, IH, J = 9.3 Hz), 7.27 (brs, IH), 7.28 (d, IH, J = 9.3 Hz), 7.37 (dd, IH, J = 2.4, 9.0 Hz), 7.68 (d, IH, J = 9.6 Hz), 8.04 (d, IH, J = 2.4 Hz). Ia-63 mp 277-279 °C 1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.28-1.54 (m, 4H), 1.77-2.02 (m, 4H), 2.15-2.29 (m, IH), 2.90 (s, 3H), 2.96-3.13 (m, IH), 6.79 (d, IH, J = 8.7 Hz), 7.12 (d, 2H, J = 9.0 Hz), 7.54 (d, 2H, J = 9.0 Hz), 9.50 (s, IH), 9.81 (s, IH). Ia-64 mp 259-260 °C 1h-NMR (DMSO-d6) 5 ppm: 1.26 (s, 9H), 1.26-1.50 (m, 4H), 1.74-1.99 (m, 4H), 2.10-2.25 (m, IH), 2.95-3.10 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 6.97 (d, 2H, J = 9.0 Hz), 7.42 (d, 2H, J = 9.0 Hz), 7.50-7.71 (m, 5H), 9.73 (s, IH), 10.05 (s, IH). Ia-65 mp 292-293 °C 1h-NMR (DMSO-de) 6 ppm: 1.27 (s, 9H), 1.28-1.54 (m, 4H), 1.62-1.72 (m, 2H), 1.77-1.87 (m, 2H), 1.91-2.10 (m, 4H), 2.13-2.25 (m, IH), 2.98-3.12 (m, IH),-3.41-3.52 (m, 2H), 5.09 (s, IH), 6.79 (d, IH, J = 9.0 Hz), 6.91 (d, 2H, J = 9.0 Hz), 7.37 (d, 2H, J = 9.0 Hz), 7.42 (d, 2H, J = 9.0 Hz), 7.51 (d, 2H, J = 9.0 Hz), 9.56 (s, IH). Ia-66 mp >300 °C 1h-NMR (DMSO-d6) 5 ppm: 1.27 (s, 9H), 1.28-1.58 (m, 4H), 1.85-2.02 (m, 4H), 2.40-2.52 (m, IH), 3.00-3.16 (m, IH), 6.81 (d, IH, J = 9.0 Hz), 7.50-7.58 (m, 3H), 7.90-7.97 (m, 2H), 12.58 (s, IH). Ia-67 mp 199-200 °C 1h-NMR (DMSO-d6) 6 ppm: 1.14 (d, 6H, J = 6.3 Hz), 1.28 (s, 9H), 1.31-1.48 (m, 4H), 1.76-1.88 (m, 2H), 2.17 (t, 2H, J= 11.1 Hz), 2.82 (t, 2H, J= 11.7 Hz), 3.46 (d, 2H, J= 11.4 Hz), 3.20-3.36 (m, IH), 3.62-3.74 (m, 2H), 4.02 (d, 2H, J = 12.9 Hz), 6.83 (d, 2H, J = 9.0 Hz), 6.89 (d, IH, J = 8.7 Hz), 7.28 (d, 2H, J = 9.0 Hz), 8.27 (s, IH). Ia-68 mp 237-239 °C 1h-NMR (CDCI3/DMSO) 5 ppm: 1.40 (s, 9H), 1.49-1.65 (m, 2H), 1.99-2.10 (m, 2H), 2.95 (t, 2H, J = 11.1 Hz), 3.36-3.52 (m, IH), 4.17 (d, IH, J = 12.9 Hz), 5.84 (d, IH, J = 8.7 Hz), 6.39 (d, IH, J = 9.6 Hz), 7.21 (d, IH, J = 9.3 Hz), 7.51 (dd, IH, J = 2.4, 9.3 Hz), 7.72 (d, IH, J = 9.9 Hz), 7.85 (d, IH, J = 2.7 Hz), 8.04 (s, IH). Ia-69 mp 259-260 °C 1h-NMR (DMSO) 5 ppm: 1.25-1.55 (m, 4H), 1.27 (s, 9H), 1.82-2.05 (m, 4H), 2.22-2.36 (m, IH), 2.98-3.17 (m, IH), 4.16 (s, 3H), 6.80 (d, IH, J = 8.4 Hz), 7.77-7.87 (m, 4H), 10.16 (s, IH). Ia-70 mp 259-260 °C 1h-NMR (DMSO) 6 ppm: 1.28 (s, 9H), 1.36-1.56 (m, 2H), 1.80-1.92 (m, 2H), 2.86-3.02 (m, 2H), 3.36-3.52 (m, IH), 4.04-4.20 (m, 2H), 6.92 (d, IH, J = 7.5 Hz), 7.38-7.58 (m, 3H), 8.00-8.14 (m, 2H), 8.90 (s, IH), 9.08 (s, IH), 9.63 (s, IH). Ia-71 mp 228-229 °C 1h-NMR (CDCI3/DMSO) 6 ppm: 1.27-1.42 (m, 2H), 1.38 (s, 9H), 1.57-1.75 (m, 2H), 1.90-2.02 (m, 2H), 2.12-2.34 (m, 3H), 3.14-3.32 (m, IH), 5.37 (d, IH, J = 9.3 Hz), 7.38-7.43 (m, 3H), 7.46 (d, 2H, J = 8.7 Hz), 7.51-7.60 (m, 2H), 7.68 (d, 2H, J = 9.0 Hz), 9.33 (s, IH). Ia-75 mp 169-170 °C 1h-NMR (CDCI3) 5 ppm: 0.58-0.72 (m, IH), 0.80 (d, 3H, J = 6.6 Hz), 0.94 (d, 3H, J = 6.0 Hz), 1.14-1.35 (m, 3H), 1.39 (s, 9H), 1.48-1.66 (m, 2H), 1.74-2.06 (m, 5H), 2.06-2.44 (m, 6H), 3.18-3.35 (m, IH), 3.64-3.74 (m, IH), 4.46-4.60 (m, IH), 6.98-7.38 (m, 5H). Ia-76 mp 236-237 °C :H-NMR (CDCI3/DMSO) Sppm: 1.27-1.42 (m, 2H), 1.38 (d, 6H, J = 6.6 Hz), 1.60-1.78 (m 2H), 1.94-2.06 (m, 2H), 2.12-2.30 (m, 3H), 3.06-3.34 (m, 2H), 5.10 (brs, IH), 6.41 (d, IH, J = 9.9 Hz), 7.25 (d, IH, J = 8.4 Hz), 7.48 (dd, IH, J = 2.4, 8.7 Hz), 7.68 (d, IH, J = 9.9 Hz), 8.12 (d, IH, J = 2.4 Hz), 8.88 (brs, IH). Ia-77 mp 117-118 °C 1h-NMR (CDCI3) 6 ppm: 1.38 (d, 6H, J = 6.9 Hz), 1.65 (quintet, 2H, J = 5.4 Hz), 1.75- 1.91 (m, 2H), 2.42 (t, 2H, J = 7.4 Hz), 3.10-3.24 (m, 3H), 4.77 (brs, IH), 6.41 (d, IH, J = 9.6 Hz), 7.18-7.26 (m, IH), 7.48 (dd, IH, J= 1.8, 8.7 Hz), 7.67 (d, IH, J = 9.9 Hz), 8.01 (s, IH), 8.23 (brs, IH). Ia-78 mp 138-139 °C 1h-NMR (CDCI3) 6 ppm: 1.41 (s, 9H), 1.64 (quintet, 2H, J = 6.6 Hz), 1.84 (quintet, 2H, J = 7.3 Hz), 2.42 (t, 2H, J = 7.5 Hz), 3.26 (q, 2H, J = 6.5 Hz), 4.59 (brs, IH), 6.41 (d, IH, J = 9.3 Hz), 7.23 (d, IH, J = 8.7 Hz), 7.49 (dd, IH, J = 2.4, 9.0 Hz), 7.67 (d, IH, J = 9.9 Hz), 8.03 (d, IH, J = 2.4 Hz), 8.28 (brs, IH). Ia-79 mp 289-290 °C 1h-NMR (DMSO) 6 ppm: 1.24-1.63 (m, 4H), 1.28 (s, 9H), 1.84-2.08 (m, 4H), 2.24-2.41 (m, IH), 3.00-3.16 (m, IH), 6.82 (d, IH, J = 8.1 Hz), 7.36-7.60 (m, 5H), 7.86-7.99 (m, 2H), 8.28 (s, IH), 10.50 (s, IH). Ia-80 mp 239-240 °C 1h-NMR (DMSO) 6 ppm: 1.22 (d, IH, J = 6.6 Hz), 1.23-1.40 (m, 2H), 1.40-1.59 (m, 2H), 1.83-2.04 (m, 4H), 2.23-2.39 (m, IH), 2.98-3.23 (m, 2H), 7.00 (d, IH, J = 7.8 Hz), 7.36-7.59 (m, 5H), 7.85-7.97 (m, 2H), 8.29 (s, IH), 10.50 (s, IH). Ia-81 mp 205-206 °C 1h-NMR (CDCI3/DMSO) 5 ppm: 1.40 (s, 9H), 1.66 (quintet, 2H, J = 7.0 Hz), 1.85 (quintet, 2H, J = 7.2 Hz), 2.45 (t, 2H, J = 7.5 Hz), 3.24 (t, 2H, J = 6.5 Hz), 5.17 (brs, IH), 7.36-7.54 (m, 5H), 7.85 (d, IH, J = 8.4 Hz), 8.07 (dd, IH, J = 1.8, 8.1 Hz), 8.23 (d, IH, J = 1.8 Hz), 9.61 (s, IH). Ia-82 mp 216-217 °C 1h-NMR (DMSO-d6) 6 ppm: 1.14 (d, 6H, J = 6.3 Hz), 1.22 (d, 6H, J = 6.9 Hz), 1.22-1.53 (m, 4H), 1.76-1.98 (m, 2H), 2.21 (t, 2H, J = 10.8 Hz), 2.22-2.36 (m, IH), 2.96-3.20 (m, 2H), 3.57 (d, 2H, J = 12.0 Hz), 3.60-3.74 (m, IH), 6.66-6.85 (m, 2H), 6.98 (d, IH, J = 7.8 Hz), 7.47 (d, IH, J = 8.7 Hz), 9.30 (s, IH). Ia-83 mp 118-119 °C 1h-NMR (DMSO-d6) 6 ppm: 1.41 (d, 6H, J = 6.3 Hz), 1.26 (s, 9H), 1.40-1.67 (m, 4H), 2.17-2.36 (m, 3H), 2.97-3.10 (m, 2H), 3.57 (d, 2H, J = 12.0 Hz), 3.61-3.74 (m, IH), 6.67-6.92 (m, 3H), 7.48 (t, IH, J = 9.0 Hz), 9.37 (s, IH). Ia-84 mp 265-267 °C H-NMR (DMSO-d6) 5 ppm: 1.21 (d, 6H, J = 6.6 Hz), 1.20-1.57 (m, 4H), 1.60-2.30 (m, 9H), 2.99-3.20 (m, 4H), 3.40-3.52 (m, 2H), 5.09 (s, IH), 6.91 (d, 2H, J = 8.7 Hz), 6.98 (d, IH, J = 7.5 Hz), 7.37 (d, 2H, J = 8.7 Hz), 7.42 (d, 2H, J = 8.7 Hz),.7.51 (d, 2H, J = 8.7 Hz), 9.56 (a, IH). Ia-85 mp 185-186 °C 1h-NMR (DMSO-d6) 5 ppm: 1.26 (s, 9H), 1.42-1.72 (m, 6H), 1.96-2.10 (m, 2H), 2.26 (t, 2H, J = 6.9 Hz), 2.96-3.12 (m, 4H), 3.41-3.52 (m, 2H), 5.09 (s, IH), 6.88 (d, IH, J = 8.7 Hz), 6.92 (d, 2H, J = 9.0 Hz), 7.37 (d, 2H, J = 8.7 Hz), 7.43 (d, 2H, J = 9.0 Hz), 7.52 (d, 2H, J = 8.7 Hz), 9.63 (s, IH). Ia-86 mp 162-164 °C 1h-NMR (DMSO-d6) 5 ppm: 1.21 (d, 6H, J = 6.6 Hz), 1.41-1.73 (m, 6H), 1.96-2.10 (m, 2H), 2.26 (t, 2H, J = 7.2 Hz), 2.91-3.20 (m, 5H), 3.42-3.52 (m, 2H), 5.09 (s, IH), 6.92 (d, 2H, J = 9.3 Hz), 6.99 (t, IH, J = 6.0 Hz), 7.37 (d, 2H, J = 8.7 Hz), 7.43 (d, 2H, J = 9.3 Hz), 7.52 (d, 2H, J = 8.7 Hz), 9.64 (s, IH). Ia-87 mp 245-247 °C H-NMR (DMSO-d6) 5 ppm: 1.22 (d, 6H, J = 6.6 Hz), 1.22-1.58 (m, 4H), 1.81-2.02 (m, 4H), 2.22-2.36 (m, IH), 3.00-3.20 (m, 2H), 3.01 (s, 3H), 6.99 (d, IH, J = 8.4 Hz), 7.75-7.88 (m, 2H), 8.19 (d, IH, J= 1.2 Hz), 10.43 (s, IH). Ia-88 mp 208-209 °C 1h-NMR (DMSO-d6) 6ppm: 1.22 (d, 6H, J = 6.9 Hz), 1.22-1.55 (m, 4H), 1.75-1.98 (m, 4H), 2.11-2.24 (m, IH), 2.98-3.20 (m, 2H), 5.96 (s, 2H), 6.82 (d, IH, J = 8.4 Hz), 6.91-7.03 (m, 2H), 7.30 (d, IH, J= 1.8 Hz), 9.72 (s, IH). Ia-89 mp 142-143 °C 1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.40-1.66 (m, 4H), 2.26 (t, 2H, J = 7.5 Hz), 3.02 (q, 2H, J = 6.6 Hz), 5.96 (s, 2H), 6.82 (d, IH, J = 8.4 Hz), 6.88 (t, IH, J = 8.4 Hz), 6.94 (dd, IH, J = 1.8, 8.4 Hz), 7.30 (d, IH, J = 1.8 Hz), 9.78 (s, IH). Ia-90 mp 100 °C 1h-NMR (DMSO-d6) 6 ppm: 1.20 (d, 6H, J = 6.9 Hz), 1.40-1.66 (m, 4H), 2.26 (t, 2H, J = 7.5 Hz), 2.89-2.99 (m, 2H), 3.13 (quint, IH, J = 6.6 Hz), 5.96 (s, 2H), 6.83 (d, IH, J = 8.1 Hz), 6.91-7.02 (m, 2H), 7.30 (d, IH, J= 1.8 Hz), 9.78 (s, IH). Ia-91 mp 189-190 °C 1h-NMR (DMSO-d6) 5 ppm: 1.26 (s, 9H), 1.43-1.71 (m, 4H), 2.40 (t, 2H, J = 7.5 Hz), 2.97-3.09 (m, 2H), 3.01 (s, 3H), 6.85-6.93 (m, IH), 7.76-7.88 (m, 2H), 8.20 (d, IH, J= 1.2 Hz), 10.49 (s, IH). la-104 mp 238-241 °C 1h-NMR (DMSO) 6 ppm: 1.27 (s. 9H), 1.3-1.5 (m. 4H), 1.8-2.0 (m, 4H), 2.50 (m, IH), 3.05 (m, IH), 6.55 (br s, IH), 6.79 (d, IH, J= 8.2), 7.15 (t, IH, J= 4.8), 8.64 (d, 2H, J= 4.8). Ia-105 mp 232-234 °C 1h-NMR (DMSO) 6 ppm: 1.26 (s, 9H), 1.2-1.5.(m, 4H), 1.8-2.0 (m, 4H), 2.55 (m, IH), 3.05 (m, IH), 6.77 (d, IH, J=8.7), 9.92 (s, 2H), 10.93 (s, IH). la-106 mp 226-228 °C 1h-NMR (DMSO) 6 ppm: 1.28 (s, 9H), 1.22-1.58 (m, 4H), 1.82-2.04 (m, 4H), 2.29 (m, IH), 3.07 (m, IH), 6.79 (d, IH, J = 8.7 Hz), 7.6 l(d-d, IH, J = 1.8 Hz, 8.7 Hz), 8.04 (d, IH, J = 8.7 Hz), 8.48 (d, IH, 2.1 Hz), 9.35 (s, IH), 10.05 (s, IH). Ia-107 mp 282-283 °C 1h-NMR (DMSO) 6 ppm: 1.22-1.57 (m, 4H), 1.27 (s, 9H), 1.80-2.04 (m, 4H), 2.27 (m, IH), 3.06 (m, IH), 6.81 (d, IH, J = 8.7 Hz), 7.32 (m, IH), 7.44 (t, 2H, J = 7.5 Hz), 7.57-7.72 (m, 6H), 9.91 (s, IH). la-108 mp 191-192°C 1h-NMR (DMSO) 6ppm: 1.24-1.58 (m, 4H), 1.28 (s, 9H), 1.86-2.04 (m, 4H), 2.70 (m, IH), 3.08 (m, IH), 6.83 (d, IH, J = 8.7 Hz), 7.63-7.79 (m, 2H), 8.31 (d, IH, J = 7.2 Hz). 10.27 (s, IH). Ia-109 mp 283-285 °C 1h-NMR (DMSO) 5 ppm: 1.24-1.60 (m, 4H), 1.28 (s, 9H), 1.87-2.04 (m, 4H), 2.42 (m, IH), 3.09 (m, IH), 3.87 (s, 2H), 6.82 (d, IH, J = 8.7 Hz), 7.28-7.43 (m, 3H), 7.60 (d, 2H, J = 7.8 Hz), 7.68 (d, IH, J = 7.2 Hz), 7.89 (d, IH, J = 7.5 Hz), 9.48 (s, IH). Ia-110 mp 263-265 °C 1h-NMR (DMSO) 6 ppm: 1.24-1.54 (m, 4H), 1.27 (s, 9H), 1.76-1.87 (m, 2H), 1.89-2.01 (m, 2H), 2.17 (m, IH), 3.04 (m, IH), 4.01 (a, 4H), 6.01 (s, 2H), 6.44 (d, 2H, J = 8.7 Hz), 6.77 (d, IH, J = 8.7 Hz), 7.39 (d, 2H, J = 9,0 Hz), 9.44 (s, IH). Ia-111 mp 239-241 °C 1h-NMR (DMSO) 6 ppm: 1.24-1.54 (m, 4H), 1.27 (s, 9H), 1.62-1.76 (m, 4H), 1.80-2.02 (m, 4H), 2.30 (m, IH), 2.47-2.59 (m, 2H), 2.66-2.76 (m, 2H), 6.08 (m, IH), 6.79 (d, IH, J = 9.0 Hz), 6.88 (d, IH, J = 6.9 Hz), 7.02 (t, IH, J = 7.5 Hz), 7.13 (d, IH, J = 7.5 Hz), 8.98 (s, IH). Ia-124 mp 247-249 °C H-NMR (DMSO) 6 ppm: 1.15 (d, 6H, J = 6.3 Hz), 1.30 (s, 9H), 2.15-2.26 (m, 2H), 3.48- 3.57 (m, 2H), 3.63-3.76 (m, 2H), 6.92 (d, 2H, J = 8.7 Hz), 7.59 (d, 2H, J = 9.0 Hz), 7.38 (d, 2H, J = 9.0 Hz), 7.87 (d, 2H, J = 8.7 Hz), 9.92 (brs, IH), 9.98 (brs, IH). Ia-125 mp 228.-232 °C 1h-NMR (DMSO) 6 ppm: 1.30 (s, 9H), 1.95-2.08 (m, 2H), 2.77-2.89 (m, 4H), 7.17 (d, IH, J = 8.4 Hz), 7.39 (d, 2H, J = 9.0 Hz), 7.42-7.48 (m, IH), 7.64 (brs, IH), 7.87 (d, 2H, J = 9.0 Hz), 9.99 (brs, 2H). Ia-126 mp 244-246 °C 1h-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 7.42 (d, 2H, J = 8.4 Hz), 7.81 (d-d, IH, J = 2.1 Hz, 8.7 Hz), 7.93 (d, 2H, J = 9.0 Hz), 8.05 (d, IH, J = 9.0 Hz), 8.66 (d, IH, J = 2.1 Hz), 9.29 (s, IH), 10.05 (brs, IH), 10.39 (brs, IH). Ia-127 mp 238-239 °C 1h-NMR (DMSO) 5 ppm: 1.30 (s, 9H), 4.18-4.27 (m, 4H), 6.81 (d, IH, J = 8.4 Hz), 7.16 (d-d, IH, J = 2.7 Hz, 9.0 Hz), 7.34-7.42 (m, 3H), 7.85 (d, 2H, J = 8.4 Hz), 9.94 (brs, IH), 9.99 (brs, IH). Ia-128 mp 286-287 °C 1h-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 7.41 (d, 2H, J = 8.7 Hz), 7.71 (d, 2H, J = 8.4 Hz), 7.91 (d, 2H, J = 8.7 Hz), 7.99 (d, 2H, J = 8.7 Hz), 10.05 (brs, IH), 10.44 (brs, IH). Ia-129 mp 232-234 °C 1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.25 (IH, m), 3.07 (m, IH), 6.80 (d, IH, J=9.0), 7.37 (d, IH, J= 8.1), 7.53 (t, IH, J=8.1), 7.75 (t, IH, J= 8.1), 8.12 (s, IH), 10.16 (s, IH). Ia-130 mp 274-277 °C 1h-NMR (DMSO) 5 ppm: 1.27 (s, 9H), 1.23-1.58 (m, 4H), 1.81-2.03 (m, 4H), 2.28 (m, IH), 3.07 (m, IH), 6.80 (d, IH, J = 8.4 Hz), 7.36 (d-d, IH, J = 0.9 Hz, 5.7 Hz), 7.43 (d-d, IH, J = 2.1 Hz, 8.7 Hz), 7.60 (d, IH, J = 5.4 Hz), 7.78 (d, IH, J = 8.7 Hz), 8.40 (d, IH, 1.8 Hz), 9.97 (brs, IH). Ia-131 mp 259-260 °C XH-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 7.40 (d, IH, J = 4.8 Hz), 7.41 (d, 2H, J = 8.7 Hz), 7.66 (d, IH, J = 5.1 Hz), 7.67 (d-d, IH, J = 1.8 Hz, 8.7 Hz), 7.84 (d, IH, J = 9.0 Hz), 7.92 (d, 2H, J = 8.7 Hz), 8.50 (s, IH), 10,03 (brs, IH), 10,27 (brs IH). Ia-132 mp 265-266 °C H-NMR (DMSO) 6 ppm: 1.17 (d, 6H, J = 6.6 Hz), 1.31 (s, 9H), 4.10 (m, IH), 7.35-7.46 (m, 3H), 7.54 (d, IH, J = 7.5 Hz), 7.87-7.97 (m, 3H), 8.15 (brs, IH), 8.20 (d, IH, J = 7.5 Hz), 10.03 (brs, IH), 10.25 (brs, IH). Ia-133 mp 249-250 °C 1h-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 7.41 (d, 2H, J = 8.7 Hz), 7.45 (d, IH, J = 5.4 Hz), 7.67 (d-d, IH, J = 1.8 Hz, 8.7 Hz), 7.76 (d, IH, J = 5.4 Hz), 7.92 (d, 2H, J = 8.7 Hz), 7.95 (d, IH, J = 8.1 Hz), 8.39 (d, IH, J = 1.8 Hz), 10.02 (brs, IH), 10 23 (brs, IH). la-134 mp 305-306 °C 1h-NMR (DMSO) 6 ppm: 1.25 (m, 2H), 1.25 (s, 9H), 1.52 (m, 2H), 1.82 (m, 2H,), 1.94 (m, 2H), 2.13 (m, IH), 3.04 (m, IH), 6.00 (d, IH, J= 8.1), 6.74 (d, IH, J= 8.4), 7.3-7.5 (m, 6H), 7.85 (d, 2H, J=7.5), 8.31 (d, IH, J=8.4). Ia-135 mp 220-222 °C 1h-NMR (DMSO) 5 ppm: 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.37 (m, IH), 3.03 (m, IH), 6.80 (d, IH, J=8.7), 7.04 (m, IH), 7.29 (m, IH), 7.79 (m, IH), 9.60 (s, IH). Ia-136 mp 263-264 °C 1h-NMR (DMSO) 6 ppm: 1.27 ( s, 9H), 1.3-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.20(m, IH), 3.03 (m, IH), 6.80 (d, IH, J= 8.4), 6.87 ( m, IH), 7.31 (m, 2H), 10.21 (s, IH). la-137 mp 260-262 °C 1h-NMR (DMSO) 5 ppm: 1.27 ( s, 9H), 1.3-1.5 ( m, 4H), 1.8-2.0 (m, 4H), 2.30 (m, IH), 3.05 (m, IH), 6.80 (d, IH, J= 8.4), 7.13 (t, 2H, J= 8.1), 7.31 (m, IH), 9.52 (s, IH). la-138 mp 270-273 °C XH-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.12 (m, IH), 3.05 (m, IH), 6.79 (d, IH, J=9.0), 7.31 (m, 2H), 7.80 (m, IH), 10.05 (s, IH). Ia-139 mp 267-270 °C 1h-NMR (DMSO) 6 ppm: 1.30 (s, 9H), 4.05 (s, 4H), 6.04 (s, 2H), 6.51 (d, 2H, J = 8.7 Hz), 7.34 (d, 2H, J = 8.4 Hz), 7.54 (d, 2H, J = 8.4 Hz), 7.87 (d, 2H, J = 8.4 Hz), 9.82 (brs, IH), 9.97 (brs, IH). la-140 mp 227-229 °C 1h-NMR (DMSO) 6 ppm: 1.22 (d, 6H, J = 6.6 Hz), 1.20-1.57 (m 4H), 1.80-2.01 (m, 4H), 2.27 (m, IH), 2.95-3.22 (m, 2H), 6.99 (d,lH, J = 7.8 Hz), 7.65 (d, 2H, J = 8.7 Hz), 7.80 (d, 2H, J = 8.4 Hz), 10.18 (brs, IH). Ia-141 mp 205-207 °C 1h-NMR (DMSO) 8 ppm: 1.22 (d, 6H, J = 6.9 Hz), 1.20-1.55 (m, 4H), 1.75-2.05 (m, 6H), 2.21 (m, IH), 2.72-2.85 (m, 4H), 2.93-3.20 (m, 2H), 6.98 (d, IH, J = 8.1 Hz), 7.10 (d, IH, J = 8.1 Hz), 7.26 (d-d, IH, J = 2.1 Hz, 8.1 Hz), 7.51 (s, IH), 9.67 (brs, IH). Ia-142 mp 295-296 °C 1h-NMR (DMSO) 5 ppm: 1.15 (d, 6H, J=6.6), 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.27 (m, IH), 3.05 (m, IH), 4.07 (m, IH), 6.80 (d, IH, J=8.7), 7.64 (d, 2H, J=8.7), 7.79 (d, 2H, J=8.7), 8.06 (d, IH, J=7.5), 10.01 (s, IH). Ia-143 mp 146-147 °C 1h-NMR (DMSO) 5ppm: 1.26 (s, 9H), 1.5-1.7 (m, 4H), 2.36 (t, 2H, J=7.8), 3.03 (q, 2H; J=6.3), 6.89 (t, IH, J=6.3), 7.66 (d, 2H, J=8.4), 7.80 (d, 2H, J=8.4), 10.25 (s, IH). Ia-144 mp 138-140 °C 1h-NMR (DMSO) Sppm: 1.21 (d, 6H, J=6.0), 1.4-1.7 (m, 4H), 2.37 (t, 2H, J=7.5), 2.96 (q, 2H, J=6.3), 3.14 (m, IH), 6.99 (t, IH, J=5.4), 7.66 (d, 2H, J=7.8), 7.81 (d, 2H, J=7.8), 10.26 (s, IH). la-145 mp 134-136 °C 1h-NMR (DMSO) Sppm: 1.26 (s, 9H), 1.39 (m, 2H), 1.4-1.7 (m, 4H), 2.28 (t, 2H, J=7.2), 2.79 (m, 4H), 3.02 (q, 2H, J=7.2), 6.88 (t, IH, J=6.0), 7.10 (t, IH, J=6.0), 7.51 (s, IH), 9.73 (a, IH). Ia-146 mp 135-137 °C 1h-NMR (DMSO) 6 ppm: 1.20 (d. 6H, J=6.6), 1.4-1.7 (m, 4H), 1.99 (m, 2H), 2.28 (t, 2H, J=7.2), 2.79 (m, 4H), 2.94 (q, 2H, J=6.3), 3.13 (m, IH), 6.98 (t, IH, J=6.9), 7.10 (d, 2H, J=8.1), 7.26 (d, 2H, J=8.1), 7.51 (a, IH), 9.73 (s,lH). la-147 mp 206-207 °C 1h-NMR (DMSO) 6 ppm; 1.29 (s, 9H), 4.54 (d, 2H, J = 5.7 Hz), 7.35 (d, 2H, J = 9.0 Hz), 7.52 (d, 2H, J = 7.8 Hz), 7.69 (d, 2H, J = 8.1 Hz), 7.83 (d, 2H, J = 8.7Hz), 9.02 (t, IH, J = 5.7 Hz), 9.97 (brs, IH). Ia-148 mp 250-251 °C 1h-NMR (DMSO) 6 ppm: 1.30 (s, 9H), 7.18 (t, 2H, J = 9.3 Hz), 7.40 (d, 2H, J = 8.7 Hz), 7.76 (d-d, 2H, J = 5.1 Hz, 9.3 Hz), 7.88 (d, 2H, J = 9.0 Hz), 10.02 (brs, IH), 10.17 (brs, IH). Ia-149 mp 220-222 °C 1h-NMR (DMSO) 6 ppm: 1.30 (s, 9H), 3.74 (s, 3H), 6.92 (d, 2H, J = 9.0 Hz), 7.38 (d, 2H, J = 9.0 Hz), 7.64 (d, 2H, J = 9.0 Hz), 7.87 (d, 2H, J = 9.0 Hz), 9.99 (s, 2H). Ia-150 mp 264-266 °C 1h-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 1.66-1.76 (m, 4H), 2.57- 2.66 (m, 2H), 2,71-2.80 (m, 2H), 6.98 (m, IH), 7.06-7.16 (m, 2H), 7.38 (d, 2H, J = 9.0 Hz), 7.90 (d, 2H, J = 8.7 Hz), 9.60 (s, IH), 9.99 (s, IH). Ia-151 mp 235-236 °C H-NMR (DMSO) 6 ppm: 1.03-1.39 (m, 5H), 1.27 (s, 9H), 1.55-1.87 (m, 5H), 3.73 (m, IH), 7.31 (d, 2H, J = 8.7 Hz), 7.76 (d, 2H, J = 8.4 Hz), 8.01 (d, IH, J = 7.8 Hz), 9.90 (s, IH). Ia-152 mp 244-246 °C 1h-NMR (DMSO) 6 ppm: 0.50-0.72 (m, 4H), 1.27 (s, 9H), 2.81 (m, IH), 7.31 (d, 2H, J = 8.7 Hz), 7.73 (d, 2H, J = 8.7 Hz), 8.30 (d, IH, J = 4.2 Hz), 9.91 (brs, IH). Ia-153 mp >300 °C 1h-NMR (DMSO) 5 ppm: 1.06 (m, 6H), 1.27 (s, 9H), 1.2-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.25 (m, IH), 2.7 (m, IH), 3.05 (m, IH), 3.51 (m, 4H), 4.30 (m, IH), 6.80 (d, IH, J=8.4), 7.34 (d, 2H, J=8.4), 7.65 (d, 2H, J=8.4), 10.01 (s, IH). Ia-154 mp 247-249 °C 1h-NMR (DMSO) 6 ppm: 1.05 (m,6H), 1.27 (s, 9H), 1.2-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.23 (m, IH), 2.77 (m, IH), 3.05 (m, IH), 3.52 (m, 4H), 4.33 (m, IH), 6.80 (d, IH, J=9.0), 7.03 (d, IH, J=7.8), 7.35 (t, IH, J=7.8), 7.59 (d, IH, J=7.8), 7.68 (s, IH), 9.96 (s, IH). la-155 mp 258-259 °C 1h-NMR (DMSO) 5 ppm: 1.25(m, 2H), 1.50 (m,2H), 1.86 (m, 2H), 1.99 (m, 2H), 2.28 (m ,.1H), 2.93 (s, 3H), 3.10 (m, IH), 7.02 (d, IH, J=7.5), 7.65 (d, 2H, J=8.4), 7.80 (d, 2H, J=8.4). 10.20 (s, IH). Ia-156 mp 250-253 °C 1h-NMR (DMSO) 5 ppm: 1.28 (m, 2H), 1.50 (m, 2H), 1.82 (m, 2H), 2.00 (m, 4H), 2.22 (m, IH), 2.79 (m, 4H), 2.92 (s, 3H), 3.11 (m, IH), 7.01 (d, IH, J=(.l), 7.26 (d, IH, J=8.1), 7.51 (s, IH), 9.68 (s, IH). Ia-157 mp 259-262 °C 1h-NMR (DMSO) 6 ppm: 1.13 (d, 6H, J=6.0), 1.25 (m, 2H), 1.50 (m, 2H), 1.80 (m, 2H), 1.95 (m, 2H), 2.17 (m, 3H), 2.92 (s, 3H), 3.10 (m, IH), 3.70 (m,2H), 3.68 (m, 2H), 6.86 (d, 2H J=9.3), 7.00 (d, IH, J=7.2), 7.43 (d, 2H, J=9.3), 9.58 (s, IH). Ia-158 mp 298-300 °C 1h-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 7.30-7.50 (m, 5H), 7.63-7,71 (m, 4H), 7.87 (d, 2H, J = 8.7 Hz), 7.91 (d, 2H, J = 9.0 Hz), 10.03 (brs, IH), 10.22 (brs, IH). Ia-159 mp 278-281 °C 1h-NMR (DMSO) 5 ppm: 0.74-1.87 (m, 20H), 1.29 (s, 9H), 3.76 (m, IH), 7.32 (d, 2H, J = 8.4 Hz), 7.75 (d, 2H, J = 8.7 Hz), 7.75 (d, IH, J = 8.7 Hz), 7.90 (brs, IH). la-160 mp 227-228 °C 1h-NMR (DMSO) 5 ppm: 1.22-1.55 (m, 4H), 1.27 (s, 9H), 1.80-2.02 (m, 4H), 2.23 (m, IH), 3.06 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.45 (t, IH, J = 9.9 Hz), 7.82 (m, IH), 8.12 (d-d, IH, J = 2.4 Hz, 6.3 Hz), 10.17 (brs, IH). Ia-161 mp 259-260 °C 1h-NMR (DMSO) 5 ppm: 1.22-1.54 (m, 4H), 1.27 (s, 9H), 1.78-2.01 (m, 4H), 2.16 (s, 3H), 2.21 (m, IH), 3.05 (m, IH), 6.77 (d, IH, J = 8.4 Hz), 7.12-7.21 (m, 2H), 7.53 (m, IH), 9.90 (brs, IH). Ia-162 mp 222-226 °C 1h-NMR (DMSO) 6 ppm: 1.15 (d,6H,J = 6.3 Hz), 1.26 (d, 6H, J = 6.9 Hz), 2.16-2.26 (m, 2H), 3.31 (m, IH), 3.48-3.58 (m, 2H), 3.63-3.76 (m, 2H), 6.92 (d, 2H, J = 9.0 H), 7.32 (d, 2H, J = 8.7 Hz), 7.59 (d, 2H, 9.0 Hz), 7.89 (d, 2H, J = 9.0 Hz), 9.92 (s, IH), 10.13 (brs, IH). Ia-163 mp 197-200 °C 1h-NMR (DMSO) 6 ppm: 1.26 (d, 6H, J = 6.3 Hz), 1.95-2.09 (m, 2H), 2.77-2.90 (m, 4H), 3.32 (m, IH), 7.17 (d, IH, J = 8.1 Hz), 7.32 (d, 2H, J = 8.7 Hz), 7.45 (d-d, IH, J = 1.8 Hz, 8.1 Hz), 7.64 (brs, IH), 7.90 (d, 2H, J = 8.7 Hz), 9.99 (brs, IH), 10.13 (brs, IH). Ia-164 mp 145-247 °C 1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.3-2.0 (m, 16H), 2.19 (m, IH), 3.05 (m, IH), 4.74 (m, IH), 6.79 (d, IH, J=9.0), 6.80 (d, 2H, J=9.0), 7.47 (d, 2H, J=9.0), 9.63 (s, IH). Ia-165 mp >300 °C 1h-NMR (DMSO) 6 ppm: 1.03-2.02 (m, 18H), 1.27 (s, 9H), 2.26 (m, IH), 3.06 (m, IH), 3.73 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.63 (d, 2H, J = 9.0 Hz), 7.78 (d, 2H, J = 8.7 Hz), 8.02 (d, IH, J = 8.1Hz), 10.00 (brs, IH). Ia-166 mp 200-201 °C H-NMR (DMSO) 5 ppm: 1.03-2.02 (m, 18H), 1.27 (s, 9H), 2.25 (m, IH), 3.06 (m, IH), 3.73 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.33 (t, IH, J = 8.1 Hz), 7.46 (d, IH, J = 8.1 Hz), 7.76 (m, IH), 7.94 (m, IH), 8.14 (d, IH, J = 8.1 Hz), 9.92 (brs, IH). Ia-167 mp 282-285 °C 1h-NMR (DMSO) 5 ppm: 1.22-1.57 (m, 4H), 1.27 (s, 9H), 1.87-2.03 (m, 4H), 2.49 (m, IH), 3.07 (m, IH), 6.83 (d, IH, J = 8.7 Hz), 13.20 (brs, IH). la-168 mp 120-124 °C 1h-NMR (DMSO) 5ppm: 0.94-1.66 (m, 14H), 1.27 (s, 9H), 1.80-2.04 (m, 4H), 2.25 (mlH), 2.92 (m, IH), 3.06 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.42-7.53 (m, 2H), 7.63 (d, IH, J = 7.2 Hz), 7.73 (m, IH), 8.17 (m, IH), 10.11 (brs, IH). Ia-169 mp 256-257 °C 1h-NMR (DMSO) 6 ppm: 0.93-1.20 (m, 5H), 1.24-1.64 (m, 9H), 1.27 (s, 9H), 1.80-2.02 (m, 4H), 2.27 (m, IH), 2.87 (m, IH), 3.06 (m, IH), 6.79 (d, IH, J = 9.0 Hz), 7.48 (d, IH, J = 7.2 Hz), 7.68-7.79 (m, 4H), 10.17 (brs, IH). Ia-171 mp 242-244 °C 1h-NMR (DMSO) 6 ppm: 1.27 (m, 12H), 1.45 (m, 4H), 1.90 (m, 4H), 2.25 (m, IH), 3.07 (m, IH), 3.67 (m, 2H), 6.77(d, IH, J=8.7), 6.90 (d, IH, J=7.8), 7.31 (t, IH, J=7.5), 7.53 (d, IH, J=7.8), 7.59 (s,lH), 9.89 (s, IH). Ia-172 mp >310 °C 1h-NMR (DMSO) 6 ppm: 1.27 (m, 12H), 1.38 (m, 4H), 1.84 (m, 2H), 1.97 (m,; 2H), 2.25 (m, IH), 3.07 (m, IH), 3.66 (m, 2H), 6.81 (d, IH, J=8.7), 7.20 (d, 2H, J=6.7), 7.61 (d, 2H, J=8.7), 9.94 (s, IH). Ia-173 mp 279-281 °C 1h-NMR (DMSO) 6ppm: 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.83 (m, 6H), 1.93 (m, 2H), 2.21 (m, IH), 2.36 (m, 2H), 3.05 (m, IH), 3.54 (m, 2H), 6.79 (d, IH, J=8.7), 7.16 (d, 2H, J=9.0), 7.56 (d, 2H, J=9.0), 9.83 (s, IH). Ia-174 mp 258-262 °C H-NMR (DMSO) 5ppm: 0.29 (m, 2H), 0.53 (m,2H), 1.20 (m, IH), 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.7-2.0 (m, 4H), 2.20 (m, IH), 3.05 (m, IH), 3.75 (d, 2H, J=6.9), 6.79 (d, IH, J=9.0), 6.83 (d, 2H, J=9.0), 7.46 (d, 2H, J=9.0), 9.64 (s, IH). Ia-175 mp 246-248 °C 1h-NMR (DMSO) 6ppm: 1.27 (s, 9H), 1.3-2.0 (m, 18H), 2.19 (m, IH), 3.04 (m, IH), 4.23 (m, IH), 6.79 (d, IH, J=8.7), 6.84 (d, 2H, J=9.0), 7.45 (d, 2H, J=9.0), 9.64 (s, IH). Ia-176 mp 200-202 °C XH-NMR (DMSO) Sppm: 1.27 (s, 9H), 1.3-2.0 (m, 18H), 2.21 (m, IH), 3.05 (m, IH), 4.23 (m, IH), 6.57 (d, IH, J=6.9), 6.80 (d, IH, J=9.0), 7.0-7.2 (m, 2H), 7.28 (s, IH), 9.74 (s, IH). Ia-177 mp 266-268 °C 1h-NMR (DMSO) Sppm: 1.22-1.56 (m, 4H), 1.27 (s, 9H), 1.79-2.02 (m, 4H), 2.25 (m,lH), 3.05 (m, IH), 6.56 (m, IH), 6.77-6.84 (m, 2H), 7.58-7.71 (m, 5H), 9.92 (brs, IH). Ia-178 mp 223-224 °C 1h-NMR (DMSO) 5 ppm: 1.26-1.54 (m,4H), 1.27 (s, 9H), 1.81-2.02 (m,4H), 2.45 (m, IH), 3.06 (m, IH), 6.80 (d, IH, J = 8.7 Hz), 8.15 (d-d, IH, J = 2.4 Hz, 9.0 Hz), 8.27 (d, IH, J = 9.0 Hz), 8.70 (m, IH), 10.85 (brs, IH). Ia-179 mp 224-227 °C 1h-NMR (DMSO) 5ppm: 1.24-1.56 (m, 4H), 1.27 (s, 9H), 1.80-2.03 (m, 4H), 2.27 (m, IH), 3.06 (m, IH), 6.80 (d, IH, J = 8.7 Hz), 6.90 (d, IH, J = 1.8 Hz), 7.72-7.84 (m, 4H), 8.60 (d, IH, J = 1.8 Hz), 10.09 (brs, IH). Ia-180 mp 226-227 °C 1h-NMR (DMSO) 5 ppm: 0.92 (d, 6H, J = 6.6 Hz), 1.26-1.55 (m, 4H), 1.27 (s, 9H), 1.80- 2.03 (m, 4H), 2.27 (m, IH), 3.05 (m, IH), 3.20 (m, IH), 6.80 (d, IH, J = 8.7 Hz), 7.42 (d, IH, J = 7.2 Hz), 7.67-7.79 (m, 4H), 10.19 (brs, IH). Ia-181 mp 191-192 °C 1h-NMR (DMSO) 6 ppm: 0.95 (d, 6H, J = 6.6 Hz), 1.26-1.55 (m, 4H), 1.27 (s, 9H), 1.80- 2.03 (m, 4H), 2.25 (m, IH), 3.06 (m, IH), 3.23 (m, IH), 6.80 (d, IH, J = 8.4 Hz), 7.41-7.53 (m, 2H), 7.58 (d, IH, J = 7.2 Hz), 7.73 (m, IH), 8.18 (m, IH), 10.13 (brs, IH). Ia-182 mp 192-193 °C 1h-NMR (DMSO) 5 ppm: 0.30 (m, 2H), 0.55 (m, 2H), 1.2-1.5 (m, 5H), 1.27 (s, IH), 1.8- 2.0 (m, 4H), 2.20 (m, IH), 3.04 (m, IH), 3.75 (d, 2H, J=6.9), 6.58 (m, IH), 6.79 (d, IH, J=8.7), 7.0-7.2 (m, 2H), 7.31 (s, IH), 9.76 (s, IH). Ia-183 mp>310°C 1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.3-1.5 (m,4H), 1.82 (m, 2H), 1.97 (m, 2H), 2.04 (m, 2H), 2.39 (m, IH), 2.46 (t, 2H, J=7.8), 3.07 (m, IH), 3.79 (t, 2H, J=7.5), 6.79 (d, IH, J=8.7), 7.56 (m, 4H), 9.80 (s, IH). Ia-184 mp 281-283 °C 1h-NMR (DMSO) 6 ppm: 1.24-1.57 (m, 4H), 1.27 (s, 9H), 1.80-2.04 (m, 4H), 2.27 (m, IH), 3.06 (m, IH), 6.80 (d, IH, J= 9,0 Hz), 7.33 (s, IH), 7.75 (d, 2H, J = 9.3 Hz), 7.91 (d, 2H, J = 8.7 Hz), 8.16 (s, IH), 10.09 (brs, IH). Ia-185 mp 226-227 °C 1h-NMR (DMSO) 5 ppm: 1.24-1.58 (m, 10H), 1.27 (s, 9H), 1.81-2.02 (m, 4H), 2.28 (m, IH), 2.78-2.88 (m, 4H), 3.06 (m, IH), 6.80 (d, IH, J = 8.7 Hz), 7.64 (d, 2H, J = 8.7 Hz), 7.82 (d, 2H, J = 8.7 Hz), 10.25 (brs, IH). Ia-186 mp 148-150 °C XH-NMR (DMSO) 6 ppm: 1.25-1.60 (m, 10H), 1.27 (s, 9H), 1.82-2.03 (m, 4H), 2.24 (m, IH), 2.82-2.92 (m, 4H), 3.06 (m,lH), 6.79 (d, IH, J = 8.4 Hz), 7.36 (m, IH), 7.55 (t, IH, J = 7.8 Hz), 7.84 (m, IH), 8.06 (m, IH), 10.18 (brs, IH). Ia-187 mp >310 °C 1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.36 (s, 9H), 1.43 (m,4H), 1.85 (m, 2H), 1.93 (m, 2H), 2.27 (m, IH), 3.06 (m, IH), 6.80 (d, IH, J=8.7), 7.58 (s, IH), 7.62 (d, 2H), 7.75 (d, 2H, J=9.0), 10.00 (s, IH). Ia-188 mp 285-292 °C 1h-NMR (DMSO) 5 ppm: 0.85 (t, 3H, J=7.5), 1.11 (d, 3H, J=6.3), 1.26 (s, 9H), 1,3-1.6 (m, 6H), 1.85 (m, 2H), 1.95 (m, 2H), 2.27 (m, IH), 3.06 (m, IH), 3.90 (m, IH), 6.80 (d, IH, J=8.4), 7.64 (d, 2H, J=8.7), 7.79 (d, 2H, J=8.7), 7.99 (d, IH, J=8.1), 10.02 (s, IH). la-189 mp 278-281 °C 1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.2-2.0 (m, 17H), 2.03 (m, 2H), 3.03 (m, IH), 6.79 (d, IH, J=8.4), 7.1-7.3 (m, 3H), 7.94 (s, IH), 9.78 (m, 2H). Ia-190 mp >310 °C XH-NMR (DMSO) 6 ppm: 1.1-2.0 (m, 17H), 1.27 (s, 9H), 2.25 (m, 2H), 3.03 (m, IH), 6.79 (d, IH, J=8.7), 7.48 (m, 4H), 9.71 (m, 2H). Ia-191 mp 275-277 °C 1h-NMR (DMSO) 5ppm: 1.16 (d, 6H, J = 6.6 Hz), 1.31 (s, 9H), 4.09 (m, IH), 7.41 (d, 2H, J = 8.7 Hz), 7.84 (s, 4H), 7.90 (d, 2H, J = 9.0 Hz), 8.11 (d, IH, J = 7.5 Hz), 10.04 (brs, IH), 10.30 (brs, IH). Ia-192 mp 204-205 °C XH-NMR (DMSO) 6 ppm: 1.15 (d, 6H, J = 6.6 Hz), 1.20-1.56 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.78-2.00 (m, 4H), 2.25 (m, IH), 2.98-3.22 (m, 2H), 4.06 (m, IH), 6.99 (d, IH, J = 8.1 Hz), 7.34 (t, IH, J = 8.1 Hz), 7.46 (d, IH, J = 7.8 Hz), 7.75 (m IH), 7.96 (m, IH), 8.17 (d, IH, J = 8.7 Hz), 9.94 (brs, IH). Ia-193 mp 285-286 °C 1h-NMR (DMSO) 6 ppm: 1.15 (d, 6H, J = 6.6 Hz), 1.20-1.56 (m, 4H), 1.22 (d, 6H, J = 6.9 Hz), 1.79-2.00 (m, 4H), 2.26 (m, IH), 2.97-3.20 (m, 2H), 4.07 (m, IH), 6.99 (d, IH, J = 7.8 Hz), 7.64 (d, 2H, J = 8.7 Hz), 7.79 (d, 2H, J = 8.7 Hz), 8.06 (d, IH, J = 7.5 Hz), 10.02 (brs, IH). Ia-194 mp 248-250 °C 1h-NMR (DMSO) 6 ppm: 1.22-1.57 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.78-2.00 (m, 4H), 2.25 (m, IH), 2.98-3.22 (m, 2H), 6.56 (m, IH), 6.82 (d, IH, J = 3.3 Hz), 6.99 (d, IH, J = 7.8 Hz), 7.58- 7.71 (m, 5H), 9.92 (bra, IH). la-195 mp 271-275 °C 1h-NMR (DMSO) 6ppm: 1.27 (s, 9H), 1.28-1.56 (m, 4H), 1.80-2.02 (m, 4H), 2.25 (m, IH), 3.06 (m, IH), 6.80 (d, IH, J = 9.0 Hz), 7.57 (s, IH), 7.62-7.74 (m, 4H), 8.39 (s, IH), 9.99 (brs, IH). Ia-196 mp 226-228 °C 1h-NMR (CDCI3) 6 ppm: 0.30 (m, 2H), 1.23 (d, 6H, J=6.9), 1.2-2.0 (m, 4H), 2.20 (m, IH), 3.10 (m, 2H), 3.76 (d, 2H, J=6.9), 6.83 (d, 2H, J=8.7), 6.99 (d, IH, J=8.1), 7.46 (d, 2H, J=8.7), 9.65 (s, IH). Ia-197 mp 173-175 °C 1h-NMR (DMSO) 6 ppm:0.31 (m, 2H), 0.56 (m, 2H), 1.22 (d, 6H, J=6.6), 1.2-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.22 (m, IH), 3.10 (m, IH), 3.76 (d, IH, J=7.2), 6.58 (d, IH, J=8.1), 7.0-7.2 (m, 2H), 7.32 (s, IH), 9.78 (s, IH). Ia-198 mp 233-235 °C 1h-NMR (DMSO) 6 ppm: 1.25 (d, 6H, J=6.9), 1.2-2.0 (m, 16H), 2.19 (m, IH), 3.10 (m, 2H), 4.73 (m, IH), 6.80 (d, 2H, J=8.7), 6.98 (d, IH, J=7.8), 7..45 (d, 2H, J=8.7), 9.63 (s, IH). Ia-199 mp 185-186 °C 1h-NMR (DMSO) 5 ppm: 1.22 (d, 6H, J=6.9), 1.2-2.0 (m, 16H), 2.22 (m, IH), 3.10 (m, 2H), 4.73 (m, IH), 6.54 (m, IH), 7.0-7.2 (m, 2H), 7.3 (s, IH), 9.75 (s ,1H). Ia-200 mp 235-237 °C 1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.3-1.6 (m, 6H), 1.8-2.0 (m, 6H), 2.20 (m, IH), 3.05 (m, IH), 3.45 (m, 2H), 3.82 (m, 2H), 4.47 (m, IH), 6.79 (d, IH, J=9.0), 6.89 (d, 2H, J=9.0), 7.47 (d, 2H,J=9.0), 9.66 (s, IH). Ia-201 mp 300-301 °C 1h-NMR (DMSO) 5 ppm: 1.15 (d, 6H, J = 6.6 Hz), 1.26-1.56 (m, 4H), 1.27 (s, 9H), 1.82- 2.03 (m, 4H), 2.23 (s, 3H), 2.37 (m, IH), 3.06 (m, IH), 4.07 (m, IH), 6.81 (d, lH, J = 8.7 Hz), 7.52 (d, IH, J = 8.4 Hz), 7.62 (d, IH, J = 8.4 Hz), 7.68 (s, IH), 8.09 (d, IH, J = 7.5 Hz), 9.22 (brs, IH). Ia-202 mp 269-270 °C 1h-NMR (DMSO) 5 ppm: 1.25-1.26 (m, 4H), 1.27 (s, 9H), 1.80-2.03 (m, 4H), 2.25 (m, IH), 3.07 (m, IH), 6.80 (d, IH, J = 8.4 Hz), 7.11 (m, IH), 7.42 (d, IH, J = 3.6 Hz), 7.48 (m, IH), 7.58 (d, 2H, J = 8.7 Hz), 7.64 (d, 2H, J = 8.4 Hz), 9.92 (brs, IH). Ia-203 mp 271-273 °C 4i-NMR (DMSO) 5 ppm: 1.14-1.54 (m, 9H), 1.26 (s, 9H), 1.63-1.88 (m, 7H), 1.89-2.01 (m, 2H), 2.21 (m, IH), 2.42 (m, IH), 3.04 (m, IH), 6.79 (d, IH, J = 9.0 Hz), 7.11 (d, 2H, J = 8.4 Hz), 7.47 (d, 2H, J = 8.1 Hz), 9.70 (brs, lH). Ia-204 mp 250-251 °C 1h-NMR (DMSO) 6 ppm: 1.22-1.39 (m, 2H), 1.22 (d, 6H, J = 6.6 Hz), 1.40-1.57 (m 2H), 1.80-2.01 (m, 4H), 2.28 (m, lH), 2.98-3.21 (m, 2H), 7.00 (d, IH, J = 7.8 Hz), 7.34 (s, IH), 7.75 (d, 2H, J = 9.0 Hz), 7.91 (d, 2H, J = 8.7 Hz), 8.17 (s, lH), 10.10 (brs, IH). Ia-205 mp 239-240 °C XH-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.2-1.5 (m, 4H), 1.8-2.0 (m, 5H), 2.08 (m, 2H), 3.05 (m, IH), 3.80 (m, 4H), 4.95 (m, IH), 6.79 (d, IH, J=8.7), 6.83 (d, 2H, J=8.7), 7.48 (d, 2H, J=8.7), 9.66 (s, IH). Ia-206 mp 236-238 °C 1h-NMR (DMSO) 5 ppm: 1.27 (s, 9H), 1.2-1.7 (m, 8H), 1.8-2.0 (m, 6H), 2.18 (m, IH), 3.04 (m, IH), 3.3-3.6(m, 2H), 3.85 (m, 3H), 6.80 (d, IH, J=9.0), 6.84 (d, 2H, J=9.0), 7.47 (d, 2H, J=9.0), 9.65 (s, IH). Ia-207 mp 224-226 °C 1h-NMR (DMSO) 5 ppm: 1.27 (s, 9H), 1.2-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.24(m, IH), 2.39 (m, 2H), 3.06 (m, IH), 3.50 (t, 2H, J=7.5), 3.70 (t, 2H, J=6.3), 6.78 (d, IH, J=6.6), 6.83 (m, IH), 7.25 (m, IH), 7.27 (m, IH), 7.54 (s,lH), 9.61 (s, IH). Ia-208 mp 275-277 °C 1h-NMR (DMSO) 5 ppm: 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.22 (m, IH), 2.38 (m, 2H), 3.07 (m, IH), 3.47 (t, 2H, J=6.9), 3.69 (t, 2H, J=6.6), 6.80 (d, IH, J=8.7), 7.14 (d, 2H, J=8.4), 7.58 (d, 2H, J=8.4), 9.83 (s, IH). Ia-209 mp 214-215 °C 1h-NMR (DMSO) 6 ppm: 1.26-1.56 (m, 4H), 1.27 (s, 9H), 1.80-2.03 (m, 4H), 2.25 (m, IH), 3.06 (m, IH), 6.59 (m, IH), 6.81 (d, IH, J = 8.4 Hz), 6.86 (d, IH, J = 2.7 Hz), 7.28-7.40 (m, 2H), 7.47 (m, IH), 7.75 (s, IH), 8.01 (s, IH), 9.91 (brs, IH). Ia-210 mp 272-275 °C 1h-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 6.59 (m, IH), 6.87 (d, IH, J = 3.3 Hz), 7.41 (d, 2H, J = 8.7 Hz), 7.68 (d, 2H, J = 8.7 Hz), 7.72 (m, IH), 7.83 (d, 2H, J = 8.7 Hz), 7.90 (d, 2H, J = 8.7 Hz), 10.03 (brs, IH), 10.22 (brs, IH). Ia-211 mp 251-255 °C 1h-NMR (DMSO) 5 ppm: 1.31 (s, 9H), 7.36 (s, IH), 7.41 (d, 2H, J = 8.4 Hz), 7.91 (d, 2H, J = 8.4 Hz), 7.92-8.00 (m, 4H), 8.19 (s, IH), 10.06 (brs, IH), 10.38 (brs, IH). Ia-212 mp 241-244 °C 1h-NMR (DMSO) 6 ppm: 1.30 (s, 9H), 1.50-1.78 (m, 6H), 1.81-1.97 (m, 2H), 4.78 (m, IH), 6.87 (d, 2H, J = 9.0 Hz), 7.38 (d, 2H, J = 8.7 Hz), 7.61 (d, 2H, J = 9.0 Hz), 7.87 (d, 2H, J = 8.7 Hz), 9.97 (brs, IH), 9.99 (brs, IH). Ia-213 mp 283-286 °C H-NMR (DMSO) 5 ppm: 1.31 (s, 9H), 7.12 (d-d, IH, J = 3.6 Hz, 5.1 Hz), 7.41 (d, 2H, J = 9.0 Hz), 7.46 (m, IH), 7.50 (d-d, IH, J = 1.2 Hz, 5.1 Hz), 7.64 (d, 2H, J = 8.7 Hz), 7.82 (d, 2H, J = 8.7 Hz), 7.90 (d, 2H, J = 9.3 Hz), 10.03 (brs, IH), 10.22 (brs, IH). Ia-216 mp 224-225°C 1h-NMR (CDCI3) 6 ppm: 1.22 (d, 6H, J=6.9), 1.2-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.45 (m, IH), 3.12 (m, 2H), 6.99 (d, IH, J=8.1), 8.15 (m, IH), 8.27 (d, IH, J=9.0), 8.69 (s, IH), 10.86 (s, IH). Ia-219 mp 270-272 °C 1h-NMR (DMSO) 6 ppm: 1.28 (s, 9H), 1.34-1.51 (m, 2H), 1.80-1.92 (m, 2H), 2.83- 2.97 (m, 2H), 3.32 (m, IH), 3.99-4.12 (m 2H), 6.92 (d, IH, J = 8.7 Hz), 7.57 (d, 2H, J = 8.7 Hz), 7.68 (d, 2H, J = 9.0 Hz), 8.90 (brs, IH). Ia-220 mp 187-189 °C 1h-NMR (DMSO) 6 ppm: 1.28 (s, 9H), 1.31-1.51 (m, 2H), 1.78-1.90 (m, 2H), 2.78-2.93 (m, 2H), 3.30 (m, IH), 3.97-4.09 (m, 2H), 6.90 (d, IH, J = 8.7 Hz), 7.06 (t, 2H, J = 9.0 Hz), 7.44 (d-d, 2H, J = 4.8 Hz, 9.0 Hz), 8.53 (brs, IH). Ia-221 mp 260-262 °C :H-NMR (DMSO) 5 ppm: 1.12-1.50 (m, 7H), 1.28 (s, 9H), 1.63-1.90 (m, 7H), 2.40 (m, IH), 2.76-2.91 (m, 2H), 3.28 (m, IH), 3.96-4.09 (m, 2H), 6.90 (d, IH, J = 8.7 Hz), 7.06 (d, 2H, J = 8.4 Hz), 7.32 (d, 2H, J = 8.4 Hz), 8.40 (brs, IH). Ia-222 mp 265-267 °C 1h-NMR (DMSO) 6 ppm: 1.23 (d, 6H, J = 6.6 Hz), 1.31-1.48 (m, 2H), 1.77-1.90 (m, 2H), 2.84-2.98 (m, 2H), 3.16 (m, IH), 3.33 (m, IH), 3.96-4.10 (m, 2H), 7.11 (d, IH, J = 7.8 Hz), 7.57 (d, 2H, J = 8.7 Hz), 7.67 (d, 2H, J = 8.4 Hz), 8.90 (brs, IH). Ia-223 mp 183-186 °C 1h-NMR (DMSO) 6 ppm: 1.23 (d, 6H, J = 6.9 Hz), 1.28-1.47 (m, 2H), 1.76-1.88 (m, 2H), 2.80-3.16 (m, 2H), 3.16 (m, IH), 3.32 (m, IH), 3.94-4.07 (m, 2H), 7.00-7.14 (m, 3H), 7.44 (d-d, 2H, J = 4.8 Hz, 9.0 Hz), 8.53 (brs, IH). Ia-224 mp 232-234 °C 1h-NMR (DMSO) 6 ppm: 1.12-1.46 (m, 7H), 1.23 (d, 6H, J = 6.6 Hz), 1.63-1.87 (m, 7H), 2.40 (m, IH), 2.78-2.93 (m, 2H), 3.15 (m,lH), 3.31 (m,lH), 3.94-4.07 (m, 2H), 7.06 (d, 2H, J = 8.4 Hz), 7.09 (d, IH, J = 8.1 Hz), 7.32 (d, 2H, J = 8.4 Hz), 8.39 (brs, IH). Ia-225 mp 222-224 °C 1h-NMR (DMSO) 6 ppm: 1.28 (s, 9H), 1.30-1.61 (m, 4H), 1.77-1.98 (m, 4H), 2.66-2.90 (m, 2H), 3.28 (m, IH), 3.40-3.50 (m, 2H), 3.79-3.88 (m, 2H), 3.96-4.08 (m, 2H), 4.44 (m, IH), 6.85 (d, 2H, J = 9.0 Hz), 6.91 (d, IH, J = 9.0 Hz), 7.31 (d, 2H, J = 9.3 Hz), 8.34 (brs, IH). Ia-226 mp 194-195 °C 1h-NMR (CDCI3/DMSO) 5 ppm: 1.39 (d, 6H, J = 7.2 Hz), 1.66 (quintet, 2H, J = 6.8 Hz), 1.87 (quintet, 2H, J = 7.7 Hz), 2.47 (t, 2H, J = 7.5 Hz), 3.11-3.22 (m, IH), 3.21 (t, 2H, J = 6.2 Hz), 5.00 (brs, IH), 7.35-7.56 (m, 5H), 7.86 (d, IH, J = 8.4 Hz), 8.05 (dd, IH, J = 1.8, 8.1 Hz), 8.20 (d, IH, J = 1.8 Hz), 9.24 (s, IH). Ia-227 mp >300 °C 1h-NMR (DMSO) 6 ppm: 1.22 (d, 6H, J = 6.3 Hz), 1.20-1.40 (m, 4H), 1.74-2.10 (m, 4H), 2.20-2.40 (m, IH), 2.39 (s, 3H), 3.00-3.30 (m, 2H), 6.25 (s, IH), 6.99 (brs, IH), 7.43-7.57 (m, IH), 7.71 (d, IH, J = 8.1 Hz), 7.76 (s, IH), 10.27 (s, IH). Ia-228 mp 168-169 °C 1h-NMR (DMSO) 6 ppm: 1.26 (s, 9H), 1.49 (quintet, 2H, J = 7.5 Hz), 1.64 (quintet, 2H, J = 7.4 Hz), 2.38 (t, 2H, J = 7.2 Hz), 2.40 (s, 3H), 3.04 (q, 2H, J = 6.5 Hz), 6.25 (s, IH), 6.89 (t, IH, J = 6.0 Hz), 7.48 (dd, IH, J = 1.8, 8.4 Hz), 7.71 (d, IH, J = 8.4 Hz), 7.77 (d, IH, J = 1.8 Hz), 10.33 (s, IH). Ia-229 mp 174-175 °C 1h-NMR (DMSO) 5 ppm: 1.21 (d, 6H, J = 6.6 Hz), 1.42-1.56 (m, 2H), 1.56-1.70 (m, 2H), 2.33-2.42 (m, 2H), 2.40 (s, 3H), 2.90-3.02 (m, 2H), 3.14 (septet, IH, J = 6.5 Hz), 6.26 (s, IH), 6.99 (brs, IH), 7.48 (d, IH, J = 8.4 Hz), 7.71 (d, IH, J = 8.7 Hz), 7.77 (s, IH), 10.33 (s, IH). Ia-230 mp 194-195 °C 1h-NMR (DMSO) 5 ppm: 0.86 (d, 6H, J = 6.9 Hz), 1.25-1.65 (m, 4H), 1.27 (s, 9H), 1.81- 2.05 (m, 5H), 2.23-2.35 (m, IH), 2.99-3.15 (m, IH), 3.36 (d, 2H, J = 7.2 Hz), 6.80 (d, IH, J = 8.4 Hz), 7.80 (d, IH, J = 8.4 Hz), 7.87 (d, IH, J = 8.4 Hz), 8.19 (s, IH), 10.44 (s, IH). Ia-231 mp 221-222 °C 1h-NMR (DMSO) 6 ppm: 0.86 (d, 6H, J = 6.9 Hz), 1.22-1.40 (m, 2H), 1.23 (d, 6H, J = 6.9 Hz), 1.40-1.58 (m, 2H), 1.82-2.04 (m, 5H), 2.22-2.37 (m, IH), 3.00-3.16 (m, IH), 3.15 (septet, IH, J = 6.6 Hz), 3.36 (d, 2H, J = 7.5 Hz), 6.99 (d, IH, J = 7.5 Hz), 7.80 (d, IH, J = 8.4 Hz), 7.86 (d, IH, J = 8.4 Hz), 8.19 (s, IH), 10.45 (s, IH). Ia-232 mp 196-197 °C 1h-NMR (CDCI3) 6 ppm: 0.93 (d, 6H, J = 6.6 Hz), 1.42 (s, IH), 1.60-1.70 (m, 2H), 1.88 (quintet, 2H, J = 7.4 Hz), 2.02-2.20 (m, IH), 2.46 (t, 2H, J = 7.7 Hz), 3.29 (q, 2H, J = 6.1 Hz), 3.48 (d, 2H, J = 7.8 Hz), 4.26 (t, IH, J = 6.0 Hz), 7.76 (d, IH, J = 8.1 Hz), 7.90 (dd, IH, J = 1.8, 8.1 Hz), 8.07 (d, IH, J = 1.5 Hz), 8.39 (s, IH). Ia-233 p. 151-152 °C 1h-NMR (CDCI3) 5 ppm: 0.93 (d, 6H, J = 6.6 Hz), 1.40 (d, 6H, J = 6.6 Hz), 1.62-1.69 (m, 2H), 1.88 (quintet, 2H, J = 7.3 Hz), 2.03-2.16 (m, IH), 2.47 (t, 2H, J = 7.5 Hz), 3.21 (septet, IH, J = 6.8 Hz), 3.23 (q, 2H, J = 6.3 Hz), 3.48 (d, 2H, J = 7.5 Hz), 4.43 (t, IH, J = 6.0 Hz), 7.76 (d, IH, J = 8.4 Hz), 7.91 (dd, IH, J = 1.8, 8.4 Hz), 8.06 (d, IH, J = 1.8 Hz), 8.36 (s, IH). Ia-234 mp 219-220 °C 1h-NMR (DMSO-d6) 6 ppm: 1.28 (s, 9H), 1.30-1.50 (m, 2H), 1.74-1.88 (m, 2H), 2.83 (t, 2H, J= 11.1 Hz), 3.20-3.32 (m, IH), 3.94-4.07 (m, 2H), 5.94 (s, 2H), 6.77 (d, IH, J = 8.8 Hz), 6.82 (dd, IH, J = 1.8, 8.7 Hz), 6.89 (d, IH, J = 8.7 Hz), 7.11 (d, IH, J = 1.8 Hz), 8.38 (s, IH). Ia-235 mp 280-282 °C XH-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.26-1.57 (m, 4H), 1.86-2.03 (m, 4H), 2.38-2.50 (m, IH), 3.00-3.14 (m, IH), 6.81 (d, IH, J = 8.4 Hz), 7.29 (t, IH, J = 8.4 Hz), 7.43 (t, IH, J = 7.5 Hz), 7.73 (d, IH, J = 8.4 Hz), 7.96 (d, IH, J = 7.5 Hz), 12.27 (s, IH). Ia-237 mp 204-205 °C 1h-NMR (DMSO) 6 ppm: 1.23 (d, 6H, J = 6.6 Hz), 1.29-1.61 (m, 4H), 1.75-1.98 (m, 4H), 2.78-2.92 (m, 2H), 3.15 (m, IH), 3.29 (m, IH), 3.38-3.51 (m, 2H), 3.78-3.89 (m, 2H), 3.94- 4.06 (m, 2H), 4.44 (m, IH), 6.85 (d, 2H, J = 9.0 Hz), 7.10 (d, IH, J = 7.8 Hz), 7.31 (d, 2H, J = 9.3 Hz), 8.34 (brs, IH). Ia-238 mp 128-130 °C 1h-NMR (DMSO) 6 ppm: 1.26 (s, 9H), 1.41-1.53 (m, 2H), 1.55-1.68 (m, 2H), 2.44 (t, 2H, J = 7.2 Hz), 2.98-3.07 (m, 2H), 6.90 (t, IH, J = 6.0 Hz), 8.16 (d-d, IH, J = 2.1 Hz, 8.7 Hz), 8.29 (d, IH, J = 8.7 Hz), 8.70 (m, IH), 10.91 (brs, IH). Ia-239 mp 256-258 °C J-H-NMR (DMSO) 5 ppm: 1.26-1.53 (m, 4H), 1.26 (s, 9H), 1.76-2.00 (m, 4H), 2.23 (s, 3H), 2.39 (m, IH), 3.04 (m, IH), 6.80 (d, IH, J = 8.7 Hz), 7.57 (d-d, IH, J = 2.4 Hz, 8.4 Hz), 7.97 (d, IH, J = 8.4 Hz), 8.12 (m, IH), 10.26 (brs, IH). Ia-240 mp 288-290 °C 1h-NMR (DMSO) 6 ppm: 1.26-1.53 (m, 4H), 1.27 (s, 9H), 1.78-1.90 (m, 4H), 2.40 (m, IH), 3.04 (m, IH), 6.81 (d, IH, J = 8.7 Hz), 7.07 (m, IH), 7.75 (m, IH), 8.07 (d, IH, J = 8.4 Hz), 8.29 (m, IH), 10.36 (brs, IH). Ia-241 mp 249-250 °C XH-NMR (DMSO) 6 ppm: 1.28 (s, 9H), 1.34-1.50 (m, 2H), 1.79-1.90 (m, 2H), 2.74-2.98 (m, 2H), 3.32 (m, IH), 4.02-4.14 (m, 2H), 6.91 (d, IH, J = 8.4 Hz), 7.94 (d, IH, J = 9.0 Hz), 8.04 (d-d, IH, J = 2.1 Hz, 9.0 Hz), 8.60 (s, IH), 9.76 (brs, IH). Ia-242 mp 250-252 °C 2H-NMR (DMSO) 5 ppm: 1.24 (s, 9H), 1.27 (s, 9H), 1.24-1.54 (m, 4H), 1.76-1.88 (m, 2H), 1.90-2.01 (m, 2H), 2.21 (m, IH), 3.05 (m, IH), 6.79 (d, IH, J = 8.7 Hz), 6.88 (d, 2H, J = 9.0 Hz), 7.48 (d, 2H, J = 9.0 Hz), 9.72 (brs, IH). 136-0290 mp 250-252 °C H-NMR (DMSO) 6 ppm: 1.15 (d, 6H, J = 6.6 Hz), 1.28 (s, 9H), 1.35-1.52 (m, 2H), 1.78- 1.92 (m, 2H), 2.20 (s, 3H), 2.81-2.96 (m, 2H), 3.33 (m, IH), 3.96-4.16 (m, 3H), 6.92 (d, IH, J = 8.7 Hz), 7.27 (d, IH, J = 8.1 Hz), 7.60 (m, IH), 7.66 (m, IH), 8.06 (d, IH, J = 7.8 Hz), 8.14 (brs, IH). Ia-244 mp 211-213 °C 1h-NMR (DMSO) 6 ppm: 1.29 (s, 9H), 1.35-1.52 (m, 2H), 1.81-1.93 (m, 2H), 2.83-2.97 (m, 2H), 3.32 (m, IH), 4.03-4.14 (m, 2H), 6.93 (d, IH, J = 8.7 Hz), 7.55 (d-d, IH, J = 2.1 Hz, 9.0 Hz), 7.94 (d, IH, J = 9.0 Hz), 8.29 (d, IH, J = 1.8 Hz), 8.78 (brs, IH), 9.19 (s, IH). Ia-245 mp 196-197°C 1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.2-1.6 (m, 6H), 1.8-2.0 (m, 6H), 2.23 (m, IH), 3.05 (m, IH), 3.73 (m, 4h), 4.99 (s, IH), 6.79 (d, IH, J=8.7), 7.13 (d, IH, J=6.8), 7.22 (t, IH, J=6.8), 7.49 (d, IH, J=6.8), 7.72 (s, IH), 9.78 (s, IH). Ia-246 mp 242-244 °C 1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.2-1.5 (m, 4H), 1.65 (m, 4H), 1.8-2.0 (m, 4H), 2.23 (m, IH), 2.71 (m, IH), 3.06 (m, IH), 3.43 (m, 2H), 3.93 (m, 2H), 6.79 (d, IH, J=8.7), 6.91 (d, IH, J=8.7), 7.20 (t, IH, J=7.5), 7.40 (d, IH, J=7.5), 7.53 (s, IH), 9.76 (s, IH). Ia-247 mp 242-245°C 1h-NMR (DMSO) 5 ppm: 1.27 (s, 9H), 1.2-1.6 (m, 6H), 1.8-2.0 (m, 6H), 2.23 (m, IH), 3.05 (m, IH), 3.74 (m, 4H), 4.94 (brs, IH), 6.79 (d, lh, J=8.7), 7.38 (d, IH, J=8.7), 7.52 (d, IH, J=8.7), 9.76 (s, IH). Ia-248 mp 272-274 °C 1h-NMR (CDC13) 6 ppm: 1.27 (s, 9H), 1.2-1.5 (m, 4H), 1.62 (m, 4H), 1.8-2.0 (m, 4H), 2.22 (m, IH), 2.68 (m, IH), 3.05 (m, IH), 3.41 (m, 2H), 3.92 (m, 2H), 6.79 (d, IH, J=9.0), 7.15 (d, 2H, J=8.7), 7.50 (d, 2H, J=8.7), 9.73(s, IH). Ia-249 mp 174-176 °C Ia-250mp 255-257 °C Ia-252 mp 249-251 °C Ia-253 mp 120-121 °C Ia-254 mp 236-237 °C Ia-255 mp 172-174 °C Ia-256 mp 257-259 °C Ia-257 mp 179-180 °C Ia-258 mp 227-229 °C Ia-259mp 135-136 °C Experiment 1 Affinity for NPY Y5 receptor cDNA sequence encoding a human NPY Y5 receptor (W096/16542) was cloned in the expression vector pMEl8S (Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into a host CHO cells by using a Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to an instruction protocol to obtain the cells that stably express NPY Y5 receptor. The membranes prepared from the above CHO cells expressing NPY Y5 receptor, the compound of the present invention and 30,000 cpm [125x] peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25 °C for 2 hours, and then the mixture was filtered with a glassfilter GF/C treated with polyethyleneimine. After the glassfilter was washed with 50 mM Tris-HCl buffer (pH 7.4), the radioactivity on the filter was measured with a gamma counter. The non-specific binding was detected in the presence of 200 nM of peptide YY. The 50 % inhibitory concentration of the test compound against the specific peptide YY binding (IC50 value) was calculated (Inui, A. et al. Endocrinology 131, 2090 - 2096 (1992)). The results are shown in Tables 1 and 2. The compounds of the present invention inhibited the binding of peptide YY (NPY homologue) to NPY Y5 receptors. In other words, the compounds of the present invention showed affinity for the NPY Y5 receptor. Experiment 2 cAMP production inhibitory activity in CHO cells After CHO cells expressing human NPY Y5 receptor were incubated in the presence of 2.5 mM isobutylmethylxanthine (SIGMA) at 37 °C for 20 min, the compound of the present invention was added and incubated for 5 min. Then, 50 nM NPY and 10 uM forskolin (SIGMA) were added to the cells and incubated for 30 min. After the reaction was terminated by adding IN HCl, the amount of cAMP in the supernatant was measured with EIA kit (Amersham LIFE SCIENCE). The inhibitory activity of NPY against forskolin stimulated cAMP was regarded as 100 % and the 50 % inhibitory concentration (IC50 value) of the compound of the present invention against the NPY activity was calculated. The results are shown in Tables 1 to 4. Experiment 3 Using the membranes prepared from Yl-expression cells (human neuroblastoma, SK-N-MC) and the membranes prepared from Y2-expression cells (human neuroblastoma, SMS-KAN), the experiment was carried out in a similar way as Experiment 1 to determine the affinity for NPY Yl receptor and NPY Y2 receptor. Binding IC 50 values for NPY Yl and NPY Y2 receptors of 1-27,1-32,1-41,1-45,1-46, 1-47,1-48,1-49,1-59,1-61,1-63, 1-64,1-66,1-69,1-72,1-152,1-154,1-204,1-205,1-212, Ia-3, Ia-5, Ia-6, Ia-12, Ia-16, Ia-17, Ia-20, Ia-21, Ia-22, Ia-26, Ia-28, Ia-29, Ia-30, Ia-31, Ia-32, Ia-33, Ia-37, Ia-39, Ia-40, Ia-50, Ia-51, Ia-54, Ia-62, Ia-67, Ia-124, Ia-126, Ia-139, Ia-140, Ia-142, Ia-178, Ia-199 and Ia-200 were 100,000 nM or higher and each compound had a selectivity for NPY Y5 receptor. Formulation Example 1 Tablets Compound (1-1) 15 mg Starch 15 mg Lactose 15 mg Crystalline cellulose 19 mg Polyvinyl alcohol 3 mg Distilled water 30 ml Calcium stearate 3 mg After all of the above ingredients except for calcium stearate are uniformly mixed, the mixture is crushed and granulated, and dried to obtain a suitable size of granules. After calcium stearate is added to the granules, tablets are formed by compression molding. Formulation Example 2 Capsules Compound (1-2) 10 mg Magnesium stearate 10 mg Lactose 80 mg After the above ingredients are mixed to prepare powders or granules, the obtained are filled in capsules. Formulation Example 3 Granules Compound (1-3) 30 g Lactose 265 g Magnesium Stearate 5 g After the above ingredients are mixed uniformly and formed by compression molding, the obtained are crushed, granulated and sieved to prepare suitable volume of granules. Industrial Applicability As shown in the above Experiments, the compounds of the present invention have an NPY Y5 receptor antagonistic activity. Therefore, the compounds of the present invention are useful as an anti-obestic agent and anorectic agent. WE CLAIM: 1. A compound of formula I which is an NPY Y5 receptor antagonist wherein R1 is optionally substituted lower alkyl, optionally substituted cycloalkyl or optionally substituted aryl, R2 is hydrogen or lower alkyl, and R1 and R2 taken together may form lower alkylene, n is 1 or 2, X is optionally substituted lower alkylene, optionally substituted lower alkenylene, optionally substituted -CO-lowcr alkylene, optionally substituted -CO-lower alkenylene or wherein R3, R4, R5 and R6 are each independently hydrogen or lower alkyl, is optionally substituted cycloalkylene, optionally substituted cycloalkenylene, optionally substituted bicycloalkylene, optionally substituted arylene or optionally substituted heterocyclediyl and p and q are each independently 0 or wherein is piperidinediyl, piperazinediyl, pyridinediyl, pyrazinediyl, pyrrolidinediyl or pyrrolediyl and U is single bond, lower alkylene or lower alkenylene, Y is OCONR7, CONR7, CSNR7, NR7CO or NR7CS, R is hydrogen or lower alkyl, and Z is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted amino, optionally substituted lower alkoxy, optionally substituted carbocyclyl or optionally substituted heterocyclyl. 2. The compound as claimed in claim 1, wherein R2 is hydrogen or lower alkyl and Z is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted carbocyclyl, optionally substituted heterocyclyl or optionally substituted amino, provided that R1 is optionally substituted C3 to CKJ alkyl when Z is optionally substituted amino. 3. The compound as claimed in claim 1, wherein R1 is optionally substituted lower alkyl or optionally substituted cycloalkyl, X is optionally substituted lower alkylene, optionally substituted lower alkenylene or is the same as claimed in claim 1, and Z is optionally substituted lower alkyl, optionally substituted carbocyclyl or optionally substituted heterocyclyl. 4. The compound as claimed in any one of claims 1 to 3, wherein R is optionally substituted C3 to C10 alkyl. 5. The compound as claimed in any one of claims 1 to 4, which is an anti-obestic agent. 6. The compound as claimed in any one of claims 1 to 4, which is an anorectic agent. 7. The compound of the formula (I) as claimed in claim 1, wherein X is C2 to C6 alkylene or C3 to C6 alkenylene, R1 is optionally substituted C3 to C10 alkyl or optionally substituted C5 to C6 cycloalkyl and the other symbols are the same as claimed in claim 1, provided that Z is not lower alkylphenylamino, hydroxy(lower)alkylphenylamino and acylphenylamino when Y is NR CO, prodrug, pharmaceutical^ acceptable salt or solvate thereof. 8. The compound as claimed in claim 7, wherein Z is optionally substituted lower alkyl or optionally substituted phenyl, prodrug, pharmaceutically acceptable salt or solvate thereof. 9. The compound of the formula (I) as claimed in claim 1, wherein X is is optionally substituted cyclcoalkylene, optionally substituted cycloalkenylene, optionally substituted bicycloalkylene or optionally substituted piperidinylene, R1 is optionally substituted C3 to C10 alkyl or optionally substituted C5 to C6 cycloalkyl and the other symbols are the same as claimed in claim 1, prodrug, pharmaceutically acceptable salt or solvate thereof. 10. The compound as claimed in claim 9, wherein is optionally substituted cyclohexylene or optionally substituted piperidinylene and p and q are simultaneously 0, prodrug, pharmaceutically acceptable salt or solvate thereof. 11. The compound as claimed in claim 9 or 10, wherein Y is CONH, prodrug, pharmaceutically acceptable salt or solvate thereof. 12. The compound as claimed in any one of claims 9 to 11, wherein Z is optionally substituted lower alkyl, optionally substituted phenyl, optionally substituted pyridyl or optionally substituted benzopyranyl, prodrug, pharmaceutically acceptable salt or solvate thereof. 13. The compound of the formula (I): R1 is optionally substituted C3 to C10 alkyl or optionally substituted C5 to C6 cycloalkyl, Z is p-lower alkylphenyl and the other symbols are the same as claimed in claim 1, provided that Z is not p-n-butylphenyl when R1 is isopropyl, prodrug, pharmaceutical^ acceptable salt or solvate thereof. 14. The compound of the formula (I) as claimed in claim 1, is heteroarylene, R1 is optionally substituted C3 to C10 alkyl or optionally substituted C5 to C6 cycloalkyl and the other symbols are the same as claimed in claim 1. -747- 15. The compound as claimed in 14, wherein is thiophenediyl or furandiyl, prodrug, pharmaceutically acceptable salt or solvate thereof.

Full Text

The present invention relates to a novel quinazoline derivative.
Background Art
Neuropeptide Y (hereinafter referred to as NPY) is a peptide which consists of 36 amino acid residues and was isolated from porcine brain in 1982. NPY is widely distributed in the central nervous system and peripheral tissues of humans and animals.
It has been reported that NPY possesses a stimulating activity of food intake, an anti-seizure activity, a learning-promoting activity, an anti-anxiety activity, an anti-stress activity etc. in central nervous system, and it may be pivotally involved in the central nervous system diseases such as depression, Alzheimer's disease and Parkinson's disease. NPY is thought to be associated with the cardiovascular diseases, since it induces a contraction of smooth muscles such as blood vessels or cardiac muscles in the peripheral tissues. Furthermore, NPY is also known to be involved in the metabolic diseases such as obesity, diabetes, and hormone abnormalities (Trends in Pharmacological Sciences, Vol. 15, and 153 (1994)). Therefore, an NPY receptor antagonist is expected as a medicine for preventing or treating various diseases involved in the NPY receptor.
Subtypes of Yl, Y2, Y3, Y4, Y5 and Y6 have now been identified as the NPY receptor (Trends in Pharmacological Sciences, Vol. 18, and 372 (1997)). It has been suggested that the Y5 receptor is at least involved it the feeding behaviour and its antagonist is expected as an anti-obestic agent (Peptides, Vol. 18, and 445 (1997)).

Quinazoline compounds having similar structures to those of the compounds of the present invention and exhibiting an NPY receptor antagonistic activity are described in WO97/20820, WO97/20821, WO97/20823 and the like. In addition, it is described that urea derivatives having a sulfonamide group and amide derivatives having a sulfonyl group in W099/64349 and benzyl sulfonamide derivatives in EP1010691-A, have an NPY antagonistic activity.
Compounds having similar structures to those of the compounds of the present invention are described in JP59-16871 -A and W097/15567. Their activities are quite different from that of the present invention and these documents do not suggest the present invention.
Disclosure of Invention
The object of the present invention is to provide a superior pharmaceutical composition for use as an NPY Y5 receptor antagonist and novel compounds having the activity.
Best Mode for Carrying out the Invention

2

In the present specification, the term "halogen" includes fluorine, chlorine, bromine and iodine. Fluorine or chlorine is preferable.
The term "protective group" in "optionally protected hydroxy" and "optionally protected hydroxy(lower)alkyl" includes all of hydroxy protecting groups usually used. For example, acyl such as acetyl, trichloroacetyl and benzoyl, lower alkoxycarbonyl such as t-butoxycarbonyl, lower alkylsulfonyl such as methane sulfonyl, lower alkoxy(lower)alkyl such as methoxymethyl, trialkylsilyl such as t-butyldimethylsilyl are included.
The term "lower alkyl" includes Cl to CIO straight or branched alkyl. The examples of "lower alkyl" are methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, isopentyl, neopentyl, hexyl, isohexyl, n-heptyl, isoheptyl, n-octyl, isooctyl, n-nonyl and n-decyl.
"Lower alkyl" represented by BA is preferably C3 to ClO alkyl, more preferably C3 to C6 alkyl and most preferably isopropyl or t-butyl.
"Lower alkyl" in other cases is preferably Cl to C6 alkyl and more preferably Cl to C4 alkyl.
The examples of substituents of "optionally substituted lower alkyl" represented by Z are, (1) halogen; (2) cyano;
(3) the following groups (i) to (xvi), which are optionally substituted with one or more
substituents selected from "a substituents group f$" defined below,
(i) hydroxy, (ii) lower alkoxy, (iii) mercapto, (iv) lower alkylthio, (v) acyl, (vi) acyloxy, (vii) carboxy, (viii) lower alkoxycarbonyl, (ix) imino, (x) carbamoyl, (xi) thiocarbamoyl, (xii) lower alkylcarbamoyl, (xiii) lower alkylthiocarbamoyl, (xiv) amino, (xv) lower alkylamino or (xvi) heterocyclylcarbonyl; or
(4) a group of the formula:

wherein RlO and R2 are each independently hydrogen or lower alkyl and when this
group has two or more of R2 and/or two or more of R-2, each R2O and/or each RH may
be different,
W is single bond, 0, S or NR12,
Rl2 is hydrogen, lower alkyl or phenyl,
is cycloalkyl, bicycloalkyl, cycloalkenyl, aryl or heterocyclyl, each of which is optionally substituted with one or more of substituents selected from "a substituents group a" defined below and s is an integer of 0 to 4.
In the present specification, "a substituents group a" is a group constituting of (1) halogen; (2) oxo; (3) cyano; (4) nitro; (5) imino optionally substituted with lower alkyl or hydroxy;
(6) the following groups (i) to (xxi), which are optionally substituted with one or more of
groups selected from the substituents group p,
(i) hydroxy, (ii) lower alkyl, (iii) lower alkenyl, (iv) lower alkoxy, (v) carboxy, (vi) lower alkoxycarbonyl, (vii) acyl, (viii) acyloxy, (ix) imino, (x) mercapto, (xi) lower alkylthio, (xii) carbamoyl, (xiii) lower alkylcarbamoyl, (xiv) cycloalkylcarbamoyl, (xv) thiocarbamoyl, (xvi) lower alkylthiocarbamoyl, (xvii) lower alkylsulfinyl, (xviii) lower alkylsulfonyl, (xix) sulfamoyl, (xx) lower alkylsulfamoyl and (xxi) cycloalkylsulfamoyl;
(7) the following groups (i) to (v), which are optionally substituted with the substituents
group (3, lower alkyl, lower alkoxy(lower)alkyl, optionally protected hydroxy(lower)alkyl,
halogeno(lower)alkyl, lower alkylsulfonyl and/or arylsulfonyl,
(i) cycloalkyl, (ii) cycloalkenyl, (iii)cycloalkyloxy, (iv) amino and (v) alkylenedioxy;

and
(8) the following groups (i) to (xii), which are optionally substituted with the substituents
group 0, lower alkyl, halogeno(lower)alkyl and/or oxo,
(i) phenyl, (ii) naphthyl, (iii) phenoxy, (iv) phenyl(lower)alkoxy, (v) phenylthio, (vi) phenyl(lower)alkylthio, (vii) phenylazo, (viii) heterocyclyl, (ix) heterocyclyloxy, (x) heterocyclylthio, (xi) heterocyclylcarbonyl and (xii) heterocyclylsulfonyl. The preferable examples of the substituents group a as substituents for B ring are halogen; nitro; hydroxy;
optionally substituted lower alkyl wherein the substituents is halogen, cyano, phenyl, carboxy and/or lower alkoxycarbonyl; lower alkenyl; lower alkoxycarbonyl(lower)alkenyl;
optionally substituted lower alkoxy wherein the substituents is halogen, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, lower alkylamino and/or cyano; acyl; hydroxyimino; lower alkylthio; lower alkylsulfinyl; sulfamoyl; optionally substituted amino wherein the substituents is lower alkyl, optionally protected hydroxy(lower)alkyl, phenyl and/or acyl;
alkylenedioxy; cyanophenyl; heterocyclylphenyl; biphenylyl; phenoxy; phenylazo optionally substituted with lower alkyl; or
optionally substituted heterocyclyl wherein the substituents is optionally protected hydroxy, mercapto, halogen, lower alkyl, cycloalkyl, lower alkoxycarbonyl, amino, lower alkoxycarbonyl amino, carbamoyl, oxo, phenyl, lower alkoxyphenyl or heterocyclyl. More preferable examples are halogen; lower alkyl optionally substituted with halogen; or lower alkoxy optionally substituted with halogen.
"A substituents group p" is a group consisting of halogen, optionally protected hydroxy, mercapto, lower alkoxy, lower alkenyl, amino, lower alkylamino, lower alkoxycarbonylamino, lower alkylthio, acyl, carboxy, lower alkoxycarbonyl, carbamoyl,

cyano, cycloalkyl, phenyl, phenoxy, lower alkylphenyl, lower alkoxyphenyl, halogenophenyl, naphthyl and heterocyclyl.
Examples of the substituents for "optionally substituted lower alkyl" represented by any other than Z (e.g., R1) are one or more substituents selected from the substituents group p. The lower alkyl may be substituted with these substituents at any possible positions.
The lower alkyl part in "lower alkoxy", "lower alkoxycarbonyl", "lower alkoxycarbonyl(lower)alkyl", "lower alkylphenyl", "lower alkoxyphenyl", "lower alkylcarbamoyl", "lower alkylthiocarbamoyl", "lower alkylamino", "halogeno(lower)alkyl", "hydroxy(lower)alkyl", "phenyl(lower)alkoxy", "lower alkylthio", "phenyl(lower)alkylthio", "lower alkoxycarbonylamino", "lower alkoxycarbonyl(lower)alkenyl", "lower alkylsulfinyl", "lower alkylsulfonyl", "aryl(lower)alkoxycarbonyl", "lower alkylbenzoyl" and "lower alkoxybenzoyl" is the same as defined in the above "lower alkyl".
Examples of substituents for "optionally substituted lower alkoxy" are one or more substituents selected from the substituents group p. Preferable examples are phenyl, lower alkylphenyl, lower alkoxyphenyl, naphthyl and heterocyclyl.
The term "cycloalkyl" includes C3 to C8 cyclic alkyl and preferably C5 to C6 cyclic alkyl. Examples are cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl.
Examples of substituents for "optionally substituted cycloalkyl" are one or more substituents selected from the substituents group a and the cycloalkyl may be substituted with these substituents at any possible positions.
The term "bicycloalkyl" includes a group which is formed by excluding one hydrogen from a C5 to C8 aliphatic cycle containing two rings which possess two or more of atoms in common. Examples are bicyclo[2.1.0]pentyl, bicyclo[2.2.1]heptyl, bicyclo[2.2.2]octyl and bicyclo[3.2.1]octyl.
The term "lower alkenyl" includes C2 to CIO, preferably C2 to C8 and more

preferably C3 to C6 straight or branched alkenyl having one or more double bonds at any possible positions. Examples are vinyl, propenyl, isopropenyl, butenyl, isobutenyl, prenyl, butadienyl, pentenyl, isopentenyl, pentadienyl, hexenyl, isohexenyl, hexadienyl, heptenyl, octenyl, nonenyl and decenyl.
The "lower alkenyl" part in "lower alkoxycarbonyl(lower)alkenyl" is the same as the above "lower alkenyl".
Examples of the substituents for "optionally substituted lower alkenyl" are halogen, lower alkoxy, lower alkenyl, amino, lower alkylamino, lower alkoxycarbonylamino, lower alkylthio, acyl, carboxy, lower alkoxycarbonyl, carbamoyl, cyano, cycloalkyl, phenyl, lower alkylphenyl, lower alkoxyphenyl, naphthyl and/or heterocyclyl.
The term "acyl" includes (1) Cl to CIO, preferably Cl to C6 and more preferably Cl to C4 straight or branched alkylcarbonyl or alkenylcarbonyl, (2) C4 to C9 and preferably C4 to C7 cycloalkylcarbonyl and (3) C7 to Cll arylcarbonyl. Examples are formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, pivaloyl, hexanoyl, acryloyl, propioloyl, methacryloyl, crotonoyl, cyclopropylcarbonyl, cyclohexylcarbonyl, cyclooctylcarbonyl and benzoyl.
The "acyl" part in "acyloxy" is the same as the above.
The term "cycloalkenyl" includes a group having at least one double bond at any possible positions in the above cycloalkyl. Examples are cyclopropenyl, cyclobutenyl, cyclopentenyl, cyclohexenyl and cyclohexadienyl.
Examples of substituents for "optionally substituted cycloalkenyl" are one or more substituents selected from the substituents group p.
Examples of substituents for "optionally substituted amino" are the substituents group p, optionally substituted benzoyl and/or optionally substituted heterocyclylcarbonyl wherein the substituents is hydroxy, lower alkyl, lower alkoxy and/or lower alkylthio.
The term "aryl" includes a monocyclic of polycyclic aromatic carbocyclyl group and

examples are phenyl, naphthyl, anthryl and phenanthryl. "Aryl" includes aryl fused with other a non-aromatic carbocyclyl group, for example, indanyl, indenyl, biphenylyl, acenaphthyl, tetrahydronaphthyl and fluorenyl. Phenyl is preferable.
The aryl part in "aryl lower alkoxycarbonyl" is the same as the above. The term "optionally substituted aryl" and "optionally substituted phenyl" represented by Z include the above "aryl" and "phenyl" respectively, which may be substituted with the substLtuents group a or lower alkyl which may be substituted with one or more group selected from the substituents group a.
Examples of the substituents for "optionally substituted aryl" and "optionally substituted phenyl" represented by any other than Z are one or more groups selected from the substituents group |3.
The term "carbocyclyl" includes the above "cycloalkyl", "cycloalkenyl", "bicycloalkyl" and "aryl".
The term "non-aromatic carbocyclyl" includes the above "cycloalkyl", "cycloalkenyl" and "bicycloalkyl".
The term "optionally substituted carbocyclyl" includes the above "optionally substituted cycloalkyl", "optionally substituted cycloalkenyl", "optionally substituted bicycloalkyl" and "optionally substituted aryl".
The term "heterocyclyl" includes a heterocyclic group containing at least one heteroatom arbitrarily selected from 0, S and N. For example, 5- or 6-membered heteroaryl such as pyrrolyl, imidazolyl, pyrazolyl, pyridyl, pyridazinyl, pyrimidinyl, oxazolyl, oxadiazolyl, isothiazolyl, thiazolyl, thiadiazolyl, furyl and thienyl; fused heterocyclyl consisting of two rings such as indolyl, isoindolyl, indazolyl, indolizinyl, indolinyl, isoindolinyl, quinolyl, isoquinolyl, cinnolinyl, phthalazinyl, quinazolinyl, naphthyridinyl, quinoxalinyl, purinyl, pteridinyl, benzopyranyl, benzimidazolyl, benzisoxazolyl, benzoxazolyl benbzoxadiazolyl, benzisothiazolyl, benzothiazolyl, benzothiadiazolyl, benzofuryl, isobenzofuryl, benzothienyl, benzotriazolyl,

imidazopyridyl, triazoropyridyl, imidazothiazolyl, pyrazinopyridazinyl, quinazolinyl, quinolyl, isoquinolyl, naphthyridinyl, dihydropyridyl, tetrahydroquinolyl and tetrahydrobenzothienyl; fused heterocyclyl consisting of three rings such as carbazolyl, acridinyl, xanthenyl, phenothiazinyl, phenoxathiinyl, phenoxazinyl and dibenzofuryl; and non-aromatic heterocyclyl such as dioxanyl, thiiranyl, oxiranyl, oxathiolanyl, azetidinyl, thianyl, pyrrolidinyl, pyrrolinyl, imidazolidinyl, imidazolinyl, pyrazolidinyl, pyrazolinyl, piperidyl, piperazinyl, morpholinyl, morpholino, thiomorpholinyl, thiomorpholino, dihydropyridyl, tetrahydrofuryl, tetrahydropyranyl, tetrahydrothiazolyl and tetrahydroisothiazolyl.
"Fused heterocyclyl" fused with a ring other than a heterocycle (e.g., benzothiazolyl), may connect at any possible position.
Substituents for "optionally substituted heterocyclyl" are the same as those for the above "optionally substituted aryl".
Heterocyclyl parts in "heterocyclylcarbonyl", "heterocyclyloxy", "heterocyclylthio" and "heterocyclyl substituted phenyl" are the same as the above "heterocyclyl".
The term "lower alkylene" includes a bivalent group comprising 1 to 6 of methylene, preferably 2 to 6 of methylene and more preferably 3 to 6 of methylene. For example, methylene, ethylene, trimethylene, tetramethylene, pentamethylene and hexamethylene are included. Tetramethylene is preferable.
"Rl and R2 taken together may form lower alkylene" includes the case

Lower alkylene part in "lower alkylenedioxy" is the same as the above "lower alkylene". Methylenedioxy or ethylenedioxy is preferable.
The term "lower alkenylene" includes a bivalent group comprising 2 to 6 of

methylene, preferably 3 to 6 of methylene and more preferably 4 to 5 of methylene and including at least one double bond.
The term "cycloalkylene" includes a bivalent group which is formed by excluding one hydrogen from the above "cycloalkyl". A preferable example of cycloalkylene represented by X is 1, 4-cyclohexanediyl.
The term "cycloalkenylene" includes a group containing at least one double bonds in the above cycloalkylene.
The term "bicycloalkylene" includes a group which is formed by excluding one hydrogen from the above "bicycloalkyl". Examples are bicyclo[2. 1. OJpentylene, bicyclo[2. 2. l]heptylene, bicyclo[2. 2. 2]octylene, and bicyclo[3. 2. ljoctylene.
The term "heterocyclediyl" includes a bivalent group which is formed by excluding one hydrogen from the above "heterocyclyl". Piperidinediyl, piperazinediyl, pyridinediyl, pyrimidinediyl, pyrazinediyl, pyrrolidinediyl or pyrrolediyl is preferable and piperidindiyl is more preferable.
The term "arylene" includes a bivalent group which is formed by excluding one hydrogen from the above "aryl". Phenylene is preferable.
The term "heteroarylene" includes aromatic groups in the above "heterocyclediyl". Examples are pyrrolediyl, imidazolediyl, pyrazolediyl, pyridinediyl, pyridazinediyl, pyrimidinediyl, pyrazinediyl, triazolediyl, triazinediyl, isoxazolediyl, oxazolediyl, oxadiazolediyl, isothiazolediyl, thiazolediyl, thiadiazolediyl, furandiyl and thiophenediyl.
One or more groups selected from the substituents group p are examples of substituents for "optionally substituted lower alkylene", "optionally substituted lower alkenylene", "optionally substituted cycloalkylene", "optionally substituted cyclohexylene", "optionally substituted bicycloalkylene", "optionally substituted cycloalkenylene", "optionally substituted phenylene", "optionally substituted heterocyclediyl" and "optionally substituted piperidinylene". Halogen, hydroxy, lower alkyl, halogeno(lower)alkyl, lower alkoxy, amino, lower alkylamino, acyl, carboxy or

The compounds of the present invention include any formable and pharmaceutical2 acceptable salts thereof. Examples of "the pharmaceutical2 acceptable salt" are salts with mineral acids such as hydrochloric acid, sulfuric acid, nitric acid and phosphoric acid; salts with organic acids such as para-toluenesulfonic acid, methane sulfonic acid, oxalic acid and citric acid; salts with organic bases such as ammonium, trimethylammonium and triethylammonium; salts with alkaline metals such as sodium and potassium; and salts with alkaline earth metals such as calcium and magnesium.
The compounds of the present invention include solvates thereof. Hydrate is preferable and arbitrary numbers of water molecules may coordinate to the compound of the present invention.
The compounds of the present invention include prodrugs thereof. Prodrug includes derivatives of the compounds of the present invention which have a chemically or metabolically decomposable group and can be converted into pharmaceutical2 active compounds of the present invention in vivo by solvolysis or under the physiological conditions. The methods for selecting and producing suitable prodrugs are described in Design of Prodrugs, Elsevier, Amsterdam 1985.
When a compound (I) of the present invention has carboxy, examples of prodrugs are an ester derivative and an amide derivative, which can be produced by reacting a compound (I) having carboxy with a suitable alcohol or a suitable amine, respectively.

When a compound (I) of the present invention has hydroxy, an example of prodrugs is an acyloxy derivative, which can be synthesized by reacting a compound (I) having hydroxy with a suitable acyl halide or a suitable acid anhydride.
When a compound (I) of the present invention has amino, an example of prodrugs is an amide derivative, which can be synthesized by reacting a compound (I) having amino with a suitable acid halide or a suitable mixed acid anhydride.
When the compound (I) of the present invention has an asymmetric carbon atom, it includes racemates, all of enantiomers and all of stereoisomers such as diastereomer, epimer and enantiomer thereof.
When the compound (I) of the present invention having one or more double bonds forms an E isomer or Z isomer, the compound (I) includes both isomers. When X is cycloalkylene, the compound (I) includes both of cis isomer and trans isomer.
For example, the compound (I) of the present invention can be synthesized by the following methods.

wherein Hal is halogen, Q is an amino protecting group and the other symbols are the same as the above. Step A
Compound 1 is reacted with Amino Compound 2 having the desired substituent Z and R7 in a suitable solvent at 0 °C to 50 °C for several minutes to several hours. As

solvents, tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile, water, a mixture thereof etc. can be used. An activator such as thionyl chloride, acid halide, acid anhydride and activated ester can be used, if necessary. StepB
Compound 3 is deprotected by the usual method and reacted with Sulfonyl Halide 4 having the desired substituent R2 in a suitable solvent at 0 °C to 50 °C for several minutes to several hours to give Compound (I-A) wherein n is 2. Tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile, water and the mixture thereof etc. can be used as a solvent. StepC
Compound (I-B) wherein n is 1 can be synthesized by reacting Compound 3 with Sulfinyl Halide 5 having substituent R2-. The conditions for the reaction are the same as those of the above Step B. StepD
Compound (I-B) obtained in Step C is oxidized by the usual method to give Compound (I-A) wherein n is 2. m-Chloroperbenzoic acid, peracetic acid, hydrogen peroxide, trifluoroperacetic acid, sodium periodate, sodium hypochlorite, potassium permanganate etc. can be used as an oxidizer and the reaction may be carried out at 0 °C to 50 °C. Examples of solvents are tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile, water, methanol, ethanol, isopropanol and mixture thereof.
In case X is heterocyclediyl containing at least one N atom and the N atom connects to CONR2-Z in the compound (I), the following reaction may be employed to obtain

wherein R is lower alkyl or aryl and L is a leaving group. StepC
Compound 5 is reacted with Compound 6 in a similar manner to the above Step C to give Compound 7. StepE
Thus obtained Compound 7 is treated with a base in a suitable solvent to give Compound 8. For example, barium hydroxide, sodium hydroxide, potassium hydroxide, hydrazine or lithium propanethiolate=can be used as a base. As a solvent, tetrahydrofuran, dimethylformamide, dioxane, acetone, acetonitrile, methanol, ethanol, propanol, water, the mixture thereof or the like can be used. The reaction can be carried out at 0 °C to 100 °C for several minutes to several tens hours. StepF
Compound 8 is reacted with Compound 9 having a leaving group and a desired substituent in a suitable solvent in the presence or absence of a base at 0 °C to 100 °C for several minutes to several days to give Compound (I-B1). Examples of the leaving group are phenoxy, chloro and trichloromethyl. Examples of the base are triethylamine, pyridine, diisopropylethylamine, sodium hydroxide, potassium carbonate and sodium hydrogencarbonate. Examples of the solvent are tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile,

methanol, ethanol and the mixture thereof. StepD
Compound (I-B') is reacted in a similar manner to the above Step D to give Compound (I-A').

wherein each of the symbols is the same as the above. Step G and Step B
Compound 10 is reacted with Compound 11 under the same reaction condition as that in Step B. Thus obtained Compound 12 is reacted in a similar manner to the above Step B to give Compound (I-C) wherein n=2. Step C and Step D
To synthesize Compound (I-D), Compound 12 obtained in Step G may be reacted in similar manners to the above Step C and Step D.
(Compound wherein Y=OCONR7)

wherein each of symbols is the same as the above. StepH
Compound 13 is reacted with Isocianate Compound 14 having a substituent Z in a suitable solvent in the presence or absence of a suitable catalyst at 0 °C to 100 °C for several minutes to several days to give Compound 15. Examples of the solvent are tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile and the mixture thereof. Step C and Step D
Thus obtained Compound 15 is reacted in similar manners to Step C and Step D to give Compound (I-E) of the present invention.
(Compound wherein Y=CSNR7 or NR7CS)
Compound (I) wherein Y is CSNR7 or NR7CS can be synthesized by reacting Compound (I) wherein Y is CONR7 or NR7CO synthesized in any one of the above methods with the Lawesson's reagent or phosphorus pentasulfide in a suitable solvent at 30 °C to 100 °C for several minutes to several hours. Examples of the solvent are tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile and the mixture thereof.

Amino groups may be protected with a suitable protecting group in the usual manner at a suitable step. For example, phthalimide, lower alkoxycarbonyl, lower alkenyloxycarbonyl, halogenoalkoxycarbonyl, aryl(lower)alkoxycarbonyl, trialkylsilyl, lower alkylsulfonyl, halogeno(lower)alkylsulfonyl, arylsulfonyl, lower alkylcarbonyl and arylcarbonyl can be used as the protecting group.
After protection of the amino group, the compound is subjected to the above-mentioned reactions and the obtained compound is deprotected by treatment of an acid or a base in a suitable solvent at a suitable stage. Examples of a solvent is tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile and the mixture thereof. Examples of a base are hydrazine, pyridine, sodium hydroxide and potassium hydroxide and examples of an acid are hydrochloric acid, trifluoroacetic acid and hydrofluoric acid.
All of the compounds of the present invention have an NPY Y5 antagonistic activity and the following compounds are specifically preferable.
In the formula (I), a compound wherein SA is optionally substituted lower alkyl or optionally substituted cycloalkyl (hereinafter referred to as "R1 is Rl-1"),
a compound wherein R1 is C3 to CIO alkyl or C5 to C6 cycloalkyl, each of which is optionally substituted with halogen (hereinafter referred to as "R1 is Rl-2"), a compound wherein R1 is C3 to CIO alkyl optionally substituted with halogen (hereinafter referred to as "R* is Rl-3"),
a compound wherein R1 is isopropyl or t-butyl (hereinafter referred to as "R1 is Rl-4"), a compound wherein R2 is hydrogen or Cl to C3 alkyl (hereinafter referred to as "R2 is R2-1"), a compound wherein R2 is hydrogen (hereinafter referred to as" R2 is R2-2"),

a compound wherein X is optionally substituted lower alkylene, optionally substituted

wherein is optionally substituted cycloalkylene, optionally substituted phenylene,
optionally substituted piperidinylene, optionally substituted thiophenediyl or optionally
substituted furandiyl (hereinafter referred to as "X is X-3"),
a compound wherein X is (i) C2 to C6 alkylene or (ii) cycloalkylene or phenylene, each of
which is optionally substituted with halogen, hydroxy, lower alkyl or
halogeno(lower)alkyl (hereinafter referred to as "X is X-4"),
a compound wherein X is C2 to C6 alkylene or to C5 to C6 cycloalkylene (hereinafter
referred to as "X is X-5"),
a compound wherein X is C3 to C6 alkylene or 1,4-cyclohexylene (hereinafter referred to
as "X is X-6"),
a compound wherein Y is CONR7, CSNE7, NR7CO or NR7CS and R7is hydrogen or Cl to C3 alkyl (hereinafter referred to as "Y is Y-l"),
a compound wherein Y is CONH, CSNH or NHCO (hereinafter referred to as "Y is Y-2"), a compound wherein Y is CONH (hereinafter referred to as "Y is Y-3"),

a compound wherein Z is optionally substituted lower alkyl, optionally substituted carbocyclyl or optionally substituted heterocyclyl (hereinafter referred to as "Z is Z-1"),
a compound wherein Z is -(CR8 R2r-W-CCRiORi2s-V
wherein R8, R2, RlO and R*1 are each independently hydrogen or lower alkyl and
when Z has two or more of R8, two or more of R°, two or more of R*0 and /or two or
more of R11, each of R8, R2, RlO an(j R11 may be different, Wis single bond, 0, S or
NR12, Rl2
is hydrogen, lower alkyl or phenyl, V is hydrogen, optionally substituted
cycloalkyl, optionally substituted bicycloalkyl, optionally substituted aryl or
optionally substituted heterocyclyl, r is an integer of 1 to 4 and s is an integer of 0 to 4
(hereinafter referred to as "Z is Z-2"),
a compound wherein Z is -(CH2)r-W-(CH2)s-V
wherein W is single bond, 0, S or NR12 R12 JS hydrogen or lower alkyl, V is optionally substituted aryl or optionally substituted heterocyclyl wherein the substituents is halogen, hydroxy, lower alkyl, halogeno(lower)alkyl, lower alkoxy, lower alkenyl, amino, lower alkylamino, acyl, carboxy, lower alkoxycarbonyl, phenyl or monocyclic heteroaryl, r is an integer of 1 to 4 and s is an integer of 0 to 4
(hereinafter referred to as "Z is Z-3),
a compound wherein Z is -(CH2)r-W-(CH2)s-V
wherein W is single bond, O, S, NH or NMe, V is optionally substituted phenyl or optionally substituted heteroaryl wherein the substituents is halogen, lower alkyl, halogeno(lower)alkyl, lower alkoxy, amino or lower alkylamino, r is an integer of 1 to 3 and s is an integer of 0 or 1
(hereinafter referred to as "Z is Z-4"),

a compound wherein Z is optionally substituted carbocyclyl,
wherein the substituent is halogen; hydroxy;
optionally substituted lower alkyl wherein the substituents is halogen, hydroxy,
carboxy, lower alkoxycarbonyl, cyano and /or phenyl;
lower alkenyl optionally substituted with lower alkoxycarbonyl;
optionally substituted lower alkoxy wherein the substituents is halogen, hydroxy,
lower alkoxy, carboxy, lower alkoxycarbonyl, lower alkylamino, cycloalkyl, cyano and
/or heterocyclyl;
cycloalkyl; cycloalkyloxy; acyl; lower alkylthio; carbamoyl; lower alkylcarbamoyl;
cycloalkylcarbamoyl; hydroxy imino;
optionally substituted amino wherein the substituents is lower alkyl, optionally protected hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, acyl, lower alkylsulfonyl, arylsulfonyl and/or phenyl;
phenyl optionally substituted with halogen, cyano, phenyl and /or heterocyclyl; lower alkylsulfinyl; lower alkylsulfamoyl; cycloalkylsulfamoyl; nitro; cyano; alkylenedioxy; phenylazo optionally substituted with lower alkyl; phenoxy; oxo;
optionally substituted heterocyclyl wherein the substituents is optionally protected hydroxy, mercapto, halogen, lower alkyl, cycloalkyl, lower alkoxycarbonyl, acyl, amino, lower alkoxycarbonylamino, carbamoyl, oxo, phenyl, lower alkoxyphenyl, halogenophenyl, heterocyclyl and /or oxo;
heterocyclylsulfonyl optionally substituted with lower alkyl; heterocyclyloxy; heterocyclylcarbonyl optionally substituted with lower alkyl (hereinafter referred to as "Z is Z-5),
a compound wherein Z is optionally substituted phenyl

wherein the substituents is halogen; hydroxy; lower alkyl optionally substituted with halogen, hydroxy, lower alkoxycarbonyl, cyano and /or phenyl; lower alkoxycarbonyl(lower)alkenyl; lower alkoxy optionally substituted with halogen, lower alkoxy, lower alkoxycarbonyl, cycloalkyl and /or heterocyclyl; cycloalkyl; cycloalkyloxy; acyl; lower alkylthio; carbamoyl; lower alkycarbamoyl; amino optionally substituted with lower alkyl, hydroxy(lower)alkyl, acyl, lower alkylsulfonyl and /or phenyl; phenyl optionally substituted with halogen, cyano, phenyl and /or heterocyclyl;
lower alkyl sulfamoyl; cycloalkylsulfamoyl; nitro; alkylenedioxy; phenylazo optionally substituted with lower alkyl; phenoxy; oxo;
heterocyclyl optionally substituted with hydroxy, halogen, lower alkyl, lower alkoxycarbonyl, amino, carbamoyl, phenyl, halogenophenyl, heterocyclyl and /or oxo; heterocyclyloxy; and/or heterocyclylsulfonyl optionally substituted with lower alkyl (hereinafter referred to as" Z is Z-6"),
a compound wherein Z is optionally substituted phenyl
wherein the substituents is halogen; lower alkyl optionally substituted with halogen,
hydroxy, lower alkoxycarbonyl and/or phenyl; lower alkoxy optionally substituted with
halogen and/or cycloalkyl; cycloalkyl; cycloalkyloxy; acyl; lower alkylthio; lower
alkylcarbamoyl; amino optionally substituted with lower alkyl, hydroxy(lower)alkyl,
acyl and/or phenyl; phenyl optionally substituted with piperidyl; cycloalkylsulfamoyl;
alkylenedioxy; phenoxy;
morpholinyl or morpholino, each of which is optionally substituted with lower alkyl;
piperidyl optionally substituted with hydroxy, lower alkyl, lower alkoxycarbonyl,
phenyl, halogenophenyl and/or oxo; pyrrolidinyl optionally substituted with hydroxy,
carbamoyl and/or oxo;
piperazinyl optionally substituted with phenyl or pyrimidinyl; dihydropyridyl;

pyrrolyl; pyrrolinyl; imidazolyl optionally substituted with halogen and/or lower alkyl; pyrazolyl; thienyl; thiadiazolyl; furyl; oxazolyl; isoxazolyl; tetrazolyl optionally substituted with lower alkyl and/or phenyl; indolinyl; indolyl; tetrahydroquinolyl; benzothiazolyl optionally substituted with lower alkyl; tetrahydroisothiazolyl optionally substituted with oxo; benzopyranyl optionally substituted with oxo; tetrahydropyranyloxy; tetrahydrofuryloxy; morpholinosulfonyl optionally substituted with lower alkyl; and/or piperidylsulfonyl optionally substituted with lower alkyl (hereinafter referred to as "Z is Z-7"),
a compound wherein Z is optionally substituted phenyl
wherein the substituents is halogen, lower alkyl, halogeno(lower)alkyl, lower alkoxy, cycloalkyloxy, lower alkylcarbamoyl, phenyl, lower alkyl morpholino and/or tetrahydropyranyloxy
(hereinafter referred to as "Z is Z-8"),
a compound wherein Z is optionally substituted heterocyclyl
wherein the substituents is halogen, hydroxy, lower alkyl, halogeno(lower)alkyl, lower alkoxy, mercapto, lower alkylthio, acyl, carboxy, lower alkoxycarbonyl, amino, lower alkylamino, phenyl, naphthyl, phenylthio optionally substituted with halogen, phenoxy optionally substituted with halogen, oxo, and/or heterocyclyl optionally substituted with lower alkyl
(hereinafter referred to as "Z is Z-9"),
a compound wherein Z is thienyl, pyrazolyl, thiazolyl, thiadiazolyl, pyridyl, pyrimidinyl, pyrazinyl, triazinyl, indolyl, isoindolyl, indolinyl, isoindolinyl, indazolyl, benzopyranyl, benzoxazolyl, benzothienyl, benzothiazolyl, benzothiazolinyl, benzothiadiazolyl, quinolyl, isoquinolyl, dihydrobenzofuryl, carbazolyl, acridinyl or dibenzofuryl, each of which is

optionally substituted with substituents selected from the group of lower alkyl; halogeno(lower)alkyl; lower alkoxy; lower alkoxycarbonyl; acyl; lower alkoxycarbonyl(lower)alkyl; mercapto; phenyl, naphthyl, phenylthio or phenoxy, each of which is optionally substituted with halogen; furyl; nitro; oxo; and morpholino optionally substituted with lower alkyl) (hereinafter referred to as "Z is Z-10"),
a compound wherein Z is thienyl, thiazolyl, thiadiazolyl, pyridyl, pyrazinyl, indolyl, isoindolinyl, benzopyranyl, quinolyl, carbazolyl, dibenzofuryl, benzopyranyl, benzothienyl or benzothiazolyl, each of which is optionally substituted with one or more substituents selected from the group of lower alkyl, halogeno(lower)alkyl, lower alkoxy, lower alkoxycarbonyl, acyl, phenyl, naphthyl, phenylthio, lower alkyl morpholino and oxo) (hereinafter referred to as "Z is Z-ll),
a compound wherein R1 is Rl-2, R2 is R2-2, n is 2 and a combination of X, Y and Z, i.e., (X,
Y, Z), is any one of the followings.
(X, Y, Z) = (X-3, Y-2, Z-l), (X-3, Y-2, Z-2), (X-3, Y-2, Z-3), (X-3, Y-2, Z-4), (X-3, Y-2, Z-5),
(X-3, Y-2, Z-6), (X-3, Y-2, Z-7), (X-3, Y-2, Z-8), (X-3, Y-2, Z-9), (X-3, Y-2, Z-10), (X-3, Y-2,
Z-ll),
(X-3, Y-3, Z-l), (X-3, Y-3, Z-2), (X-3, Y-3, Z-3), (X-3, Y-3, Z-4), (X-3, Y-3, Z-5), (X-3, Y-3, Z-
6), (X-3, Y-3, Z-7), (X-3, Y-3, Z-8), (X-3, Y-3, Z-9), (X-3, Y-3, Z-10), (X-3, Y-3, Z-ll),
(X-4, Y-2, Z-l), (X-4, Y-2, Z-2), (X-4, Y-2, Z-3), (X-4, Y-2, Z-4), (X-4, Y-2, Z-5), (X-4, Y-2, Z-
6), (X-4, Y-2, Z-7), (X-4, Y-2, Z-8), (X-4, Y-2, Z-9), (X-4, Y-2, Z-10), (X-4, Y-2, Z-ll),
(X-4, Y-3, Z-l), (X-4, Y-3, Z-2), (X-4, Y-3, Z-3), (X-4, Y-3, Z-4), (X-4, Y-3, Z-5), (X-4, Y-3, Z-
6), (X-4, Y-3, Z-7), (X-4, Y-3, Z-8), (X-4, Y-3, Z-9), (X-4, Y-3, Z-10), (X-4, Y-3, Z-ll),
(X-5, Y-2, Z-l), (X-5, Y-2, Z-2), (X-5, Y-2, Z-3), (X-5, Y-2, Z-4), (X-5, Y-2, Z-5), (X-5, Y-2, Z-
6), (X-5, Y-2, Z-7), (X-5, Y-2, Z-8), (X-5, Y-2, Z-9), (X-5, Y-2, Z-10), (X-5, Y-2, Z-ll),
(X-5, Y-3, Z-l), (X-5, Y-3, Z-2), (X-5, Y-3, Z-3), (X-5, Y-3, Z-4), (X-5, Y-3, Z-5), (X-5, Y-3, Z-

6), (X-5, Y-3, Z-7), (X-5, Y-3, Z-8), (X-5, Y-3, Z-9), (X-5, Y-3, Z-10) or (X-5, Y-3, Z-ll), the pharmaceutically acceptable salt, solvate or prodrug thereof.
The NPY Y5 receptor antagonist of the present invention is effective for all of the diseases in which NPY Y5 is involved and it is especially useful for preventing and/or treating obesity and suppressing food intake. Moreover, the antagonist is effective for preventing and/or treating the diseases in which obesity acts as a risk factor, for example, diabetes, hypertension, hyperlipemia, atherosclerosis and acute coronary syndrome.
In addition, the NPY Y5 receptor antagonist of the present invention has a low affinity for NPY Yl and Y2 receptors, and has a high selectivity for NPYY5 receptor. NPY causes a sustained vasoconstrictive action in the periphery and this action is mainly via Yl receptor. Since Y5 receptor is not involved in this action at all, the NPY Y5 receptor antagonist has a low risk of inducing side effects based on the peripheral vasoconstriction, and is expected to be suitably used as a safe medicine.
The NPY Y5 receptor antagonist shows an anti-obestic effect by suppressing food intake. Therefore, it is one of the features that this antagonist does not induce side effects, e.g., an indigestion caused by an anti-obestic agent which inhibits digestion and absorption, and a central side effect such as anti-depression caused by a serotonin transporter inhibitor showing an anti-obesity effect.
A compound of the present invention can be administered orally or parenterally as an anti-obestic agent or anorectic agent. In the case of oral administration, it may be in any usual form such as tablets, granules, powders, capsules, pills, solutions, syrups, buccal tablets and sublingual tablets. When the compound is parenterally administered, any usual form is preferable, for example, injections (e.g., intravenous, intramuscular), suppositories, endermic agents and vapors. Oral administration is particularly preferable because the compounds of the present invention show a high oral

absorbability.
A pharmaceutical composition may be manufactured by mixing an effective amount of a compound of the present invention with various pharmaceutical additives suitable for the administration form, such as excipients, binders, moistening agents, disintegrators, lubricants and diluents. When the composition is of an injection, an active ingredient together with a suitable carrier can be sterilized to give a pharmaceutical composition.
Examples of the excipients include lactose, saccharose, glucose, starch, calcium carbonate and crystalline cellulose. Examples of the binders include methylcellulose, carboxymethylcellulose, hydroxypropylcellulose, gelatin and polyvinylpyrrolidone. Examples of the disintegrators include carboxymethylcellulose, sodium carboxymethylcellulose, starch, sodium alginate, agar and sodium lauryl sulfate. Examples of the lubricants include talc, magnesium stearate and macrogol. Cacao oil, macrogol, methylcellulose etc. may be used as base materials of suppositories. When the composition is manufactured as solutions, emulsified injections or suspended injections, dissolving accelerators, suspending agents, emulsifiers, stabilizers, preservatives, isotonic agents and the like may be added. For oral administration, sweetening agents, flavors and the like may be added.
Although the dosage of a compound of the present invention as an anti-obestic agent or anorectic agent should be determined in consideration of the patient's age and body weight, the type and degree of diseases, the administration route etc., a usual oral dosage for an adult is 0.05 to 100 mg/kg/day and preferable is 0.1 to 10 mg/kg/day. For parenteral administration, although the dosage highly varies with administration routes, a usual dosage is 0.005 to 10 mg/kg/day, preferably, 0.01 to 1 mg/kg/day. The dosage may be administered in one to several divisions per day.
The present invention is further explained by the following Examples and

Experiments, which are not intended to limit the scope of the present invention.
Examples
Example 1 Synthesis of Compound (1-7)
Step 1
Sodium carbonate (995 mg, 9.38 mmol) was dissolved in 30 ml of water and starting material amino acid (1.0 g, 8.53 mmol) and N-carbethoxyphthalimide (2.49 g, 11.4 mmol) were added thereto. The mixture was stirred at room temperature overnight. The pH of the mixture was adjusted to 1 by adding cone, hydrochloric acid. Precipitated crystals were washed with water and dried to give the desired compound (1.72 g, 82 % yield).
iH-NMR (CD3OD) 6 ppm: 1.59-1.77 (m, 4H), 2.34 (t, 2H, J = 6.3 Hz), 3.69 (t, 2H, J = 6.6 Hz), 7.78-7.87 (m, 4H).

The compound obtained in Step 1 (1.0 g, 4.0 mmol) was dissolved in 5 ml of dichloromethane at room temperature. Oxalyl chloride (0.459 ml, 5.2 mmol) and trace amounts of DMF were added to the mixture under ice-cooling and the mixture was reacted under ice-cooling and at room temperature, each for 30 min. After the solvent was removed under reduced pressure, 5 ml of dichloromethane was added. Under ice-

cooling, 4-butylaniline (664 mg, 4.4 mmol) and triethylamine (0.564 ml, 4.4 mmol) were added thereto and the mixture was reacted for 30 min. at room temperature. The reactant was poured into water and extracted with chloroform. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give the desired compound (1.49 g, 97 % yield).
!H-NMR (CDC13) 5 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.27-1.39 (m, 2H), 1.51-1.62 (m, 2H), 1.72-1.84 (m, 4H), 2.40-2.46 (m, 2H), 2.56 (t, 2H, J = 7.5 Hz), 3.76 (t, 1H, J = 5.7 Hz), 7.12 (d, 2H, J = 7.8 Hz), 7.33 (s, 1H), 7.42 (d, 2H, J = 8.1 Hz), 7.71-7.73 (m, 2H), 7.83-7.86 (m, 2H).

After the compound obtained in Step 2 (1.49 g, 3.9 mmol) was dissolved in 30 ml of ethanol, hydrazine monohydrate (0.591 mg, 11.8 mmol) was added and the mixture was reacted at 50 °C for 3 hours. The solvent was removed, 1 mol/1 aqueous NaOH was added and the solution was extracted with ethyl acetate. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure to give the desired compound (808 mg, 83 % yield) !H-NMR (CD3OD) 6 ppm: 0.93 (t, 3H, J = 7.2 Hz), 1.28-1.40 (m, 2H), 1.50-1.62 (m, 4H), 1.67-1.77 (m, 2H), 2.37 (t, 2H, J = 7.5 Hz), 2.56 (t, 2H, J = 7.8 Hz), 2.68 (t, 2H, J = 7.2 Hz), 7.11 (d, 2H, J = 8.1 Hz), 7.42 (d, 2H, J = 8.4 Hz).
Step 4

The compound obtained in Step 3 (808 mg, 3.25 mmol) was suspended in 5 ml of dichloromethane under ice-cooling and isopropylsulfonyl chloride (696 mg, 4.9 mmol) and triethylamine (494 mg, 4.9 mmol) were added. After the mixture was reacted under ice-cooling for an hour, the reactant was poured into water and extracted with chloroform. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give the desired compound quantitatively. !H-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.27-1.40 (m, 2H), 1.36 (d, 6H, J = 6.6 Hz), 1.51-1.69 (m, 4H), 1.77-1.86 (m, 2H), 2.38 (t, 2H, J = 7.2 Hz), 2.56 (t, 2H, J = 7.5 Hz), 3.12-3.21 (m, 3H), 4.38 (t, 1H, J = 5.7 Hz), 7.11 (d, 2H, J = 8.4 Hz), 7.36-7.41 (m, 3H).
Example 2 Synthesis of Compound (I-10)

The desired compound was synthesized in a similar manner to Step 4 in Example 1 except that tert-butylsulfinyl chloride (689 mg, 4.9 mmol) and triethylamine (494 mg, 4.9 mmol) were added to the compound obtained in Step 3 in Example 1. !H-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.22 (s, 9H), 1.30-1.37 (m, 2H), 1.51- . 1.68 (m, 4H), 1.76-1.86 (m, 2H), 2.31-2.40 (m, 2H), 2.56 (t, 2H, J = 7.5 Hz), 3.15-3.26 (m, 3H), 7.11 (t, 2H, J = 8.7 Hz), 7.42 (d, 2H, J = 8.1 Hz), 7.54 (s, 1H).

Example 3 Synthesis of Compound (I-11)

The compound obtained in Example 2 (352 mg, 1.0 mmol) was dissolved in 5 ml of dichloromethane under ice-cooling and mCPBA (259 mg, 1.5 mmol) was added to the
5 solution. The solution was reacted at room temperature for an hour and the insoluble material was filtered off. The filtrate was washed with 1 mol/1 NaOH, Na2S2C>5 and water, successively, and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give the desired compound (338 mg, 92 % yield).
) iH-NMR (CDC13) Sppm: 0.91 (t, 3H, J = 7.5 Hz), 1.29-1.39 (m, 2H), 1.39 (s, 9H), 1.51-1.68 (m, 4H), 1.76-1.84 (m, 2H), 2.37 (t, 2H, J = 7.5 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.19-3.26 (m, 2H), 4.20 (t, 1H, J = 5.7 Hz), 7.11 (t, 2H, J = 8.1 Hz), 7.42 (d, 2H, J = 8.7 Hz), 7.46 (s, 1H).
Example 4 Synthesis of Compound (1-72) Step 1
Starting material amino acid (a mixture of cis isomer and trans isomer) (1.0 g, 8.53 mmol) was dissolved in 7.5 ml of methanol. Thionyl chloride (1.0 ml, 13.7 mmol) was added to the mixture under ice-cooling and the mixture was stirred at room temperature overnight. After the mixture was concentrated under reduced pressure, diethylether was added and precipitated crystals were obtained by filtration. The crystals were

washed with diethylether and dried to give the desired compound (1.25 g, 93 % yield). l-H-NMR (CDCI3) Sppm: 1.50-2.60 (m, 9H), 3.08-3.36 (m, 1H), 3.67 (s, 3H, C02Me of cis isomer), 3.71 (s, 3H, C02Me of trans isomer), 8.15-8.55 (m, 3H). Step 2

The desired sulfonamide (a mixture of cis isomer and trans isomer) was synthesized from starting material methyl ester in similar manners to Step 3 in Example 1 and Example 2. cis isomer
iH-NMR (CDCI3) 6 ppm: 1.39 (s, 9H), 1.52-1.99 (m, 8H), 2.43-2.53 (m, 1H), 3.42-3.55 (m, 1H), 3.69 (s, 3H), 3.85 (d, 1H, J = 9.0 Hz). Step 3

Starting material sulfonamide (19.4 g, 70.0 mmol, a mixture of cis isomer and trans isomer) was dissolved in 30 ml of methanol. To the mixture, 28 % sodium methoxide (284 ml, 140.0 mmol) was added and refluxed with stirring under ice-cooling. After the solvent was removed, the residue was diluted with chloroform, and 1 mol/1 HC1 was added with stirring under ice-cooling until pH of an aqueous layer reached 3. The aqueous layer was extracted with chloroform and the organic layer was washed with water and dried over magnesium sulfate anhydride. The obtained crude crystals were recrystallized from hexane-ethyl acetate to give the desired sulfonamide (trans isomer,

7.75 g, 40 % yield).
trans isomer
!H-NMR (CD3OD) 5ppm: 1.16-1.32 (m, 2H), 1.39 (s, 9H), 1.44-1.52 (m, 2H), 1.98-2.09
(m, 2H), 2.14-2.29 (m, 3H), 3.18-3.37 (m, 1H), 3.63 (d, 1H, J = 9.0 Hz), 3.67 (s, 3H).
Step 4

Starting material methyl ester (4.77 g, 17.2 mmol) was dissolved in 95 ml of methanol and 1 mol/1 NaOH (43 ml, 43.0 mmol) was added with stirring under ice-cooling. The mixture was stirred at room temperature overnight and concentrated under reduced pressure. After 1 mol/1 HC1 was added with stirring until pH of the mixture reached 3 under ice-cooling, the precipitated crystals were collected by filtration, washed with water and dried. The obtained crude crystals were recrystallized from hexane-ethylacetate to give the desired carboxylic acid (4.20 g, 93 % yield). !H-NMR (CDCI3) 5ppm: 1.18-1.35 (m, 2H), 1.39 (s, 9H), 1.46-1.63 (m, 2H), 2.01-2.14 (m, 2H), 2.14-2.32 (m, 3H), 3.18-3.35 (m, 1H), 3.80 (d, 1H, J = 9.6 Hz). Step 5

A starting material carboxylic acid (5.86 g, 22.3 mmol) was dissolved in 88 ml of dichloromethane at room temperature. To the mixture, oxalyl chloride (2.34 ml, 26.7 mmol) and catalytic amount of DMF were added under ice-cooling and stirred at room temperature for an hour. After the solvent was removed under reduced pressure, dichloromethane (115 ml), substituted aniline (5.05 g, 24.5 mmol) and triethylamine

(4.65 ml, 33.4 mmol) were added. The mixture was stirred at room temperature for 2.5 hours, the ice-cooling water was poured thereto, and the mixture was extracted with chloroform. An organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and ethyl acetate and hexane were added to the residue. The precipitated crystals were collected with filtration to give the desired amide (7.00 g, 70 % yield).
!H-NMR (CDC13) 5ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.17-1.42 (m, 2H), 1.40 (s, 9H), 1.60-1.78 (m, 2H), 1.98-2.43 (m, 7H), 3.20-3.43 (m, 3H), 3.67 (d, 1H, J = 9.6 Hz), 3.74-3.86 (m, 2H), 6.86 (d, 2H, J = 9.0 Hz), 7.04 (s, 1H), 7.38 (d, 2H, J = 9.0 Hz).
Example 5 Synthesis of Compound (1-2) Step 1

After starting material diamine (461 mg, 2.5 mmol) was suspended in dichloromethane under ice-cooling, an acid chloride (500 mg, 2.5 mmol) and triethylamine (773 mg, 7.5 mmol) were added and the mixture was reacted for 30 min. Water and dichloromethane were added to the reactant and insoluble materials were filtered off. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure to give the desired compound as a residue (100 mg, 15 % yield).
iH-NMR (CDCI3) 6 ppm: 0.93 (t, 3H, J = 7.2 Hz), 1.30-1.42 (m, 2H), 1.57-1.67 (m, 2H), 2.66 (t, 2H, J = 7.8 Hz), 3.50 (brs, 1H), 6.57 (s, 1H), 6.68 (d, 2H, J = 8.7 Hz), 7.26 (d, 2H, J = 8.4 Hz), 7.39 (d, 2H, J = 8.7 Hz), 7.68 (s, 1H), 7.75 (d, 2H, J = 8.1 Hz). Step 2

t
The desired compound was synthesized in a similar manner to Step 4 in Example 1. !H-NMR (CDCI3) 5 ppm: 0.94 (t, 3H, J = 7.5 Hz), 1.34-1.44 (m, 2H), 1.40 (d, 6H, J = 6.6 Hz), 1.59-1.68 (m, 2H), 2.69 (t, 2H, J = 7.8 Hz), 3.24-3.35 (m, 1H), 6.49 (s, 1H), 7.23-7.32 (m, 4H), 7.6 (d, 2H, J = 8.7 Hz), 7.79 (d, 2H, J = 8.1 Hz), 7.85 (s, 1H).
Example 6 Synthesis of Compound (1-31) Step 1

A starting material diamine (8.37 g, 73.3 mmol) was dissolved in 30 ml of dioxane at room temperature and a solution of B0C2O (2 g, 9.2 mmol) in dioxane (30 ml) was added. The mixture was reacted at room temperature for 3 days and the solvent was removed. Water was added to the residue and the mixture was extracted with chloroform. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure to give the desired compound as a residue (1.8 g, 92 % yield based on B0C2O)
!H-NME (CDCI3) 6 ppm: 1.07-1.26 (m, 6H), 1.44 (s, 9H), 1.84-2.00 (m, 4H), 2.58-2.67 (m, 1H), 3.37 (brs, 1H), 4.43 (brs, 1H). Step 2

The desired compound was synthesized in a similar manner to Step 1 in Example 5. !H-NMR (CDCI3) 5 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.26-1.42 (m, 6H), 1.45 (s, 9H), 1.54-1.68 (m, 2H), 1.99-2.12 (m, 4H), 2.64 (t, 2H, J = 7.8 Hz), 3.43 (brs, 1H), 3.90-4.00 (m, 1H), 4.48 (d, 1H, J = 5.7 Hz), 5.95 (d, 1H, J = 8.4 Hz), 7.21 (d, 2H, J = 8.4 Hz), 7.65 (d, 2H, J = 8.4 Hz). Step 3

A starting material Boc compound (2.08 g, 5.55 mmol) was dissolved in 20 ml of ethyl acetate under ice-cooling and 20 ml of 4mol/l HCl/AcOEt was added. The mixture was reacted at room temperature for an hour and the solvent was removed under reduced pressure to give the desired compound as a residue (1.7 g, 98 % yield). iH-NMR (CD3OD) 6 ppm: 0.93 (t, 3H, J = 7.2 Hz), 1.29-1.41 (m, 2H), 1.50-1.66 (m, 6H), 2.02-2.18 (m, 4H), 2.66 (t, 2H, J = 7.8 Hz), 3.13 (brs, 1H), 3.82-3.94 (m, 1H), 7.26 (d, 2H, J = 8.7 Hz), 7.72 (d, 2H, J = 8.4Hz). Step 4

The desired compound was synthesized in a similar manner to Step 4 in Example 1.

!H-NMR (CDCI3) 6 ppm: 0.92 (t, 3H, J = 7.5 Hz), 1.21 (s, 9H), 1.28-1.62 (m, 8H), 2.07-2.14 (m, 4H), 2.64 (t, 2H, J= 7.8 Hz), 3.11 (d, 1H, J= 5.1 Hz), 3.20 (brs, 1H), 3.90-4.04 (m, 1H), 6.06-6.14 (m, 1H), 7.21 (t, 2H, J = 8.1 Hz), 7.67 (t, 2H, J = 8.4 Hz).
5 Example 7 Synthesis of Compound (1-32)

The desired compound was synthesized from the compound obtained in Example 6 in a similar manner to Example 3.
!H-NMR (CDCI3) 5 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.27-1.65 (m, 8H), 1.40 (s, 9H), 2.10-1 2.23 (m, 4H), 2.65 (t, 2H, J = 7.5 Hz), 3.23-3.35 (m, 1H), 3.49 (s, 1H), 3.88-4.02 (m, 1H), 5.84-5.92 (m, 1H), 7.13 (t, 2H, J = 8.4 Hz), 7.65 (d, 2H, J = 8.1 Hz).
Example 8 Synthesis of Compound (1-5) Step 1

The desired compound was synthesized in a similar manner to Step 2 in Example 1. !H-NMR (CDCI3) 6 ppm: 0.94 (t, 3H, J = 7.5 Hz), 1.30-1.42 (m, 2H), 1.50-1.65 (m, 2H), 2.61 (t, 2H, J = 7.8 Hz), 7.20 (d, 2H, J = 7.2 Hz), 7.48-7.51 (m, 3H), 7.72 (s, 1H), 7.88-7.90 (m, 1H). Step 2

To a mixture of a starting material nitro compound (593 mg, 1.95 mmol) and tin (358 mg, 3.0 mmol), 30 ml of 6 mol/1 HC1 and 6 ml of THF were added and reacted at 50 °C for 3 hours. After cooling, the solvent was removed and the residue was neutralized 10 % with NaOH and extracted with chloroform. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give the desired compound (110 mg, 21 % yield). !H-NMR (CDC13) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.26-1.39 (m, 2H), 1.49-1.59 (m, 2H), 2.50 (t, 2H, J = 7.8 Hz), 4.37 (s, 1H), 6.65 (d, 2H, J = 8.4 Hz), 6.97 (d, 2H, J = 8.4 Hz), 7.14 (d, 1H, J = 8.4 Hz), 7.43 (d, 1H, J = 8.7 Hz). Step 3

The desired compound was synthesized in a similar manner to Step 4 in Example 1. 1 J-H-NMR (CDCI3) 6 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.28-1.41 (m, 2H), 1.46 (d, 6H, J = 6.9 Hz), 1.53-1.63 (m, 2H), 2.59 (t, 2H, J = 7.8 Hz), 3.35-3.44 (m, 1H), 7.15 (d, 2H, J = 8.7 Hz), 7.38 (s, 1H), 7.45 (d, 2H, J = 8.7 Hz), 7.57 (s, 1H).
Example 9 Synthesis of Compound (1-4) Step 1

The desired compound was synthesized in a similar manner to Step 4 in Example 1. iH-NMR (CDCI3) 5 ppm: 1.44 (d, 6H, J = 6.9 Hz), 3.33-3.43 (m, 1H), 3.88 (s, 9H), 6.24-6.26 (m, 1H), 7.11-7.14 (m, 2H). Step 2
The desired compound was synthesized in a similar manner to Step 4 in Example 4. !H-NMR (CDCI3) 6 ppm: 1.44 (d, 6H, J = 6.3 Hz), 3.33-3.45 (m, 1H), 6.25-6.28 (m, 1H), 7.27-7.28 (m, 1H), 7.51 (s, 1H). Step 3

The desired compound was synthesized in a similar manner to Step 2 in Example 1. !H-NMR (CD3OD) 6 ppm: 0.92 (t, 3H, J = 6.9 Hz), 1.28-1.41 (m, 2H), 1.46 (d, 6H, J = 6.3 Hz), 1.53-1.63 (m, 2H), 2.58 (t, 2H, J = 7.8 Hz), 3.33-3.43 (m, 1H), 6.27-6.29 (m, 1H), 7.14-7.16 (m, 3H), 7.50 (d, 2H, J = 8.4 Hz), 7.90 (s, 1H).
Example 10 Synthesis of Compound (1-28) Step 1

The desired compound was synthesized in a similar manner to Step 1 in Example 1. iH-NMR (CDCI3) 5ppm: 1.37-1.52 (m, 3H), 1.74-1.79 (m, 2H), 2.07-2.13 (m, 2H), 2.28-2.42 (m, 2H), 3.72-3.81 (m, 1H), 4.09-4.20 (m, 1H), 7.68-7.73 (m, 2H), 7.81-7.85 (m, 2H). Step 2

4-butylphenyl isocyanate (2.85 g, 16.3 mmol) was dissolved in 30 ml of THF, and a starting material alcohol (1.0 g, 4.08 mmol) and bis(tributyltin)oxide (972 mg, 1.63 mmol) were added. After the mixture was stirred overnight, the solvent was removed, water was added and the solution was extracted with chloroform. The organic layer was washed with water and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give the desired compound (332 mg, 19 % yield). !H-NMR (CDCI3) 5ppm: 0.92 (t, 3H, J = 6.9 Hz), 1.30-1.40 (m, 2H), 1.48-1.62 (m, 4H), 1.79-1.83 (m, 2H), 2.21-2.25 (m, 2H), 2.37-2.50 (m, 2H), 2.57 (t, 2H, J = 7.8 Hz), 4.11-4.22 (m, 1H), 4.77-4.87 (m, 1H), 6.49 (s, 1H), 7.11 (d, 2H, J = 8.7 Hz), 7.28 (d, 2H, J = 8.7 Hz), 7.69-7.73 (m, 2H), 7.80-7.84 (m, 2H). Step 3

The desired compound was synthesized in similar manners to Step 3 in Example 1 and Example 2.
iH-NMR (CDC13) Sppm: 0.91 (t, 3H, J = 7.2 Hz), 1.21 (s, 9H), 1.30-1.62 (m, 8H), 2.08 (d, 4H, J = 11.1 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.04 (d, 1H, J = 4.8 Hz), 3.20-3.30 (m, 1H), 4.65-4.76 (m, 1H), 6.57 (s, 1H), 7.10 (d, 2H, J = 8.7 Hz), 7.26 (d, 2H, J = 8.1Hz).

The desired compound was synthesized in a similar manner to Example 3. iH-NMR (CDCI3) Sppm: 0.91 (t, 3H, J = 7.2 Hz), 1.23-1.62 (m, 8H), 1.40 (s, 9H), 2.12 (d, 4H, J = 14.4 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.28-3.40 (m, 1H), 3.90 (s, 1H), 4.60-4.73 (m, 1H), 6.57 (s, 1H), 7.10 (d, 2H, J = 8.4 Hz), 7.25 (d, 2H, J = 8.4Hz).
Example 12 Synthesis of Compound (1-114)

Lawesson's reagent [2,4-bis(4-methoxyphenyl)-l,3-dithia-2,4-diphosphetane-2,4-

disulfide] (132 mg) was added to a solution of 100 mg of Compound (I-110) synthesized in a similar manner to Example 1 in toluene (2.7 ml) and the mixture was stirred at 80 °C for 3 hours. The reactant was concentrated under reduced pressure and the residue was purified by silica gel chromatography (ethyl acetate: n-hexane=l:l) to give pale yellow crystals (82.3 mg, 79 %). The crystals were recrystallized from methylene chloride-diisopropyl ether to give the desired compound as colorless needles (50.5 mg, 48 %).
Example 13 Synthesis of Compound (1-120) Step 1

Ethyl 4-amino-l-piperidinecarboxylate (300 mg) and triethylamine (258 mg) were dissolved in 5 ml of dichloromethane. To the mixture, 2 ml of solution of t-butylsulfinyl chloride (222 mg) in dichloromethane was added and the mixture was stirred at room temperature for 4 hours. The solution was partitioned into an aqueous solution of potassium hydrogen sulfate and ethyl acetate. The organic layer was washed with brine and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give 378 mg of 4-t-butylsulfiny amino-1-ethoxycarbonyl piperidine. Step 2

In a mixture of 5 ml of 2-propanol and 5 ml of water, 378 mg of 4-t-butylsulfinylamino-1-ethoxycarbonyl piperidine was suspended and 1.77 g of barium

hydroxide was added. The mixture was refluxed with stirring and heating for 4 hours. The mixture was diluted with methanol and the insoluble material was filtered off. The solvent was removed under reduced pressure to give 4-t-butylsulfinylaminopiperidine. Without purification, the obtained material was dissolved in 5 ml of THF, and 984 mg of N-phenoxycarbonyl-4-butyl aniline and 236 mg of diisopropyl ethylamine were added, followed by stirring at room temperature overnight. An aqueous solution of potassium hydrogen sulfate was added to the mixture and the mixture was extracted with ethyl acetate. The organic layer was washed with brine and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give 291 mg of 4-t-butylsulfinylaminopiperidine-1-carboxlic acid(4-t-butylphenyl)amide. !H-NMR (CDC13) 5 ppm:0.89(t, 3H, J = 7.3Hz), 1.19(8, 9H), 1.25-1.38(m, 4H), 1.40-1.60(m, 4H), 1.89-2.03(m, 3H), 2.52(t, 2H, J = 7.7Hz), 2.89-3.04(m, 2H), 3.14(d, 1H, J = 5.2 Hz), 3.37(m, 1H), 3.96(m, 2H), 6.67(s, 1H), 7.05(d, 2H, J = 8.5Hz), 7.22(d, 2H, J = 8.5Hz). Step 3

In a mixture of 2 ml of methanol and 2 ml of methylene chloride, 291 mg of 4-t-butylsulfinyl aminopiperidine-1-carboxlic acid(4-t-butylphenyl)amide was dissolved. To the mixture, 570 mg of 80%-MMPP (magnesium monoperoxyphthalate hexahydrate) was added and the mixture was stirred at room temperature for 2 hours. The solution was diluted with water and extracted with ethyl acetate. The organic layer was washed with brine and dried over magnesium sulfate anhydride. The solvent was removed under reduced pressure and the residue was purified by silica gel chromatography to give 130 mg of 4-t-butylsulfonylaminopiperidine-l-carboxylic acid(4-butylphenyl)amide (1-120).

Other Compounds (I) are synthesized by the similar methods. The structures and physical properties are shown below.

^%

1-2
1h-NMR (CDCI3) 6 ppm: 0.94 (t, 3H, J = 7.5 Hz), 1.34-1.44 (m, 2H), 1.40 (d, 6H, J = 6.6
Hz), 1.59-1.68 (m, 2H), 2.69 (t, 2H, J= 7.8 Hz), 3.24-3.35 (m, IH), 6.49 (s, IH), 7.23-7.32
(m, 4H), 7.6 (d, 2H, J = 8.7 Hz), 7.79 (d, 2H, J = 8.1 Hz), 7.85 (s, IH).
1-3
1h-NMR (CDCI3) 5 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.30-1.39 (m, 2H), 1.37 (d, 6H, J = 6.9
Hz), 1.57 (quint, 2H, J = 7.5 Hz), 1.96 (quint, 2H, J = 6.6 Hz), 2.49 (t, 2H, J = 6.6 Hz), 2.57
(t, 2H, J = 7.8 Hz), 3.16-3.26 (m, 3H), 4.62 (brs, IH), 7.12 (d, 2H, J= 8.1 Hz), 7.43 (d, 2H, J
= 8.4 Hz), 7.64 (s, IH).
1-4
1h-NMR (CD3OD) 5 ppm: 0.92 (t, 3H, J = 6.9 Hz), 1.28-1.41 (m, 2H), 1.46 (d, 6H, J = 6.3
Hz), 1.53-1.63 (m, 2H), 2.58 (t, 2H, J = 7.8 Hz), 3.33-3.43 (m, IH), 6.27-6.29 (m, IH), 7.14-
7.16 (m, 3H), 7.50 (d, 2H, J = 8.4 Hz), 7.90 (s, IH).
1-5
1h-NMR (CDCI3) 5 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.28-1.41 (m, 2H), 1.46 (d, 6H, J = 6.9
Hz), 1.53-1.63 (m, 2H), 2.59 (t, 2H, J = 7.8 Hz), 3.35-3.44 (m, IH), 7.15 (d, 2H, J = 8.7 Hz),
7.38 (s, IH), 7.45 (d, 2H, J = 8.7 Hz), 7.57 (s, IH).
1-6
1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.29-1.39 (m, 2H), 1.37 (d, 6H, J = 6.9
Hz), 1.55 (quint, 2H, J = 7.5 Hz), 2.55 (t, 2H, J = 5.1 Hz), 3.18-3.27 (m, IH), 3.92 (d, 2H, J
= 6.0 Hz), 5.51 (t, IH, J = 5.7 Hz), 7.10 (d, 2H, J = 8.4 Hz), 7.39 (d, 2H, J = 8.4 Hz), 8.23 (s,
IH).
1-7
1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.28-1.38 (m, 2H), 1.37 (d, 6H, J = 6.9
Hz), 1.51-1.67 (m, 4H), 1.78-1.88 (m, 2H), 2.39 (t, 2H, J = 7.2 Hz), 2.57 (t, 2H, J = 7.5 Hz),
3.12-3.22 (m, 3H), 4.30-4.37 (m, IH), 7.12 (d, 2H, J = 8.4 Hz), 7.36-7.42 (m, 3H).
1-8

1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.21-1.47 (m, 4H), 1.35 (d, 6H, J = 6.6
Hz), 1.51-1.63 (m, 4H), 1.67-1.77 (m, 2H), 2.34 (t, 2H, J = 7.5 Hz), 2.55 (t, 2H, J = 7.8 Hz),
3.08-3.17 (m, 3H), 4.71 (t, 1H, J = 6.0 Hz), 7.09 (d, 2H, J = 8.1 Hz), 7.43 (d, 2H, J = 8.4 Hz),
7.74 (s, 1H).
1-9
1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.29-1.39 (m, 2H), 1.35 (d, 6H, J = 6.9
Hz), 1.50-1.60 (m, 2H), 2.54 (t, 2H, J = 7.8 Hz), 2.64 (t, 2H, J = 5.7 Hz), 3.14-3.23 (m, 1H),
3.41-3.47 (m, 2H), 5.29 (t, 1H, J = 6.3 Hz), 7.10 (d, 2H, J = 8.4 Hz), 7.39 (d, 2H, J = 8.4 Hz),
7.91 (s, 1H).
MO
1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.22 (s, 9H), 1.30-1.37 (m, 2H), 1.51-
1.68 (m, 4H), 1.76-1.86 (m, 2H), 2.31-2.40 (m, 2H), 2.56 (t, 2H, J = 7.5 Hz), 3.15-3.26 (m,
3H), 7.11 (t, 2H, J = 8.7 Hz), 7.42 (d, 2H, J = 8.1 Hz), 7.54 (s, 1H).
Ml
mp : 128-129 °C
1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.29-1.39 (m, 2H), 1.39 (a, 9H), 1.51-
1.68 (m, 4H), 1.76-1.84 (m, 2H), 2.37 (t, 2H, J = 7.5 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.19-3.26
(m, 2H), 4.20 (t, 1H, J = 5.7 Hz), 7.11 (d, 2H, J = 8.1 Hz), 7.42 (d, 2H, J = 8.7 Hz), 7.46 (s,
1H).
1-12
1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.28-1.37 (m, 2H), 1.47-1.68 (m, 6H),
2.23 (t, 2H, J = 7.2 Hz), 2.56 (t, 2H, J = 7.5 Hz), 2.90-2.97 (m, 2H), 5.10 (brs, 1H), 7.11 (d,
2H, J = 8.4 Hz), 7.36 (d, 2H, J = 8.1 Hz), 7.50-7.68 (m, 3H), 7.93 (d, 1H, J = 8.1 Hz), 8.06 (d,
1H, J = 8.4 Hz), 8.24 (d, 1H, J = 7.5 Hz), 8.66 (d, 1H, J = 8.7 Hz).
1-13
1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.28-1.40 (m, 2H), 1.45-1.73 (m, 6H),
2.23 (t, 2H, J = 7.5 Hz), 2.56 (t, 2H, J = 7.8 Hz), 2.88 (s, 6H), 2.88-2.95 (m, 2H), 5.04 (brs,

1H), 7.10 (d, 2H, J = 8.1 Hz), 7.17 (d, 1H, J = 7.2 Hz), 7.37 (d, 2H, J = 8.4 Hz), 7.48-7.54 (m,
2H), 8.23 (d, 1H, J = 7.2 Hz), 8.30 (d, 1H, J = 8.7 Hz), 8.53 (d, 1H, J = 8.4 Hz).
1-14
1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.30-1.43 (m, 6H), 1.36 (d, 6H, J = 6.6
Hz), 1.51-1.62 (m, 4H), 1.67-1.78 (m, 2H), 2.34 (t, 2H, J = 7.5 Hz), 2.56 (t, 2H, J = 7.8 Hz),
3.09-3.20 (m, 3H), 4.34 (brs, 1H), 7.10 (d, 2H, J = 8.4 Hz), 7.41-7.44 (m, 3H).
1-15
1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.23 (s, 9H), 1.27-1.80 (m, 12H), 2.30-
2.38 (m, 2H), 2.56 (t, 2H, J= 7.5 Hz), 3.15 (brs, 2H), 7.11 (d, 2H, J = 7.8 Hz), 7.43 (d, 2H, J
= 7.8 Hz), 7.59 (s, 1H).
1-16
1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.29-1.44 (m, 6H), 1.39 (s, 9H), 1.51-
1.61 (m, 4H), 1.68-1.78 (m, 2H), 2.35 (t, 2H, J = 7.5 Hz), 2.56 (t, 2H, J = 8.1 Hz), 3.15-3.21
(m, 2H), 4.14-4.23 (m, 1H), 7.11 (d, 2H, J = 7.8 Hz), 7.36-7.44 (m, 3H).
1-19
IH-NMR (CDCI3) 6 ppm: 0.92 (t, 3H, J = 7.5 Hz), 1.21 (s, 9H), 1.30-1.40 (m, 2H), 1.55-
1.72 (m, 6H), 2.64 (t, 2H, J = 7.8 Hz), 3.08-3.33 (m, 3H), 3.42-3.50 (m, 2H), 6.39 (s, 1H),
7.22 (d, 2H, J = 8.4 Hz), 7.69 (d, 2H, J = 8.1 Hz).
1-20
1h-NMR (CDCI3) 5 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.31-1.39 (m, 2H), 1.39 (s, 9H), 1.55-
1.72 (m, 6H), 2.64 (t, 2H, J = 7.8 Hz), 3.24 (quart, 2H, J = 6.6 Hz), 3.48 (quart, 2H, J = 6.6
Hz), 4.21 (t, 1H, J = 6.3 Hz), 6.29 (s, 1H), 7.22 (d, 2H, J = 7.8 Hz), 7.67 (d, 2H, J = 8.1 Hz).
1-21
1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.23 (s, 9H), 1.30-1.42 (m, 2H), 1.50-
2.02 (m, 10H), 2.30-2.42 (m, 1H), 2.57 (t, 2H, J = 8.1 Hz), 3.10 (brs, 1H), 3.57 (brs, 1H),
7.12 (d, 2H, J = 8.4 Hz), 7.41 (d, 2H, J = 7.8 Hz).
1-22

mp : 78-79 °C
1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.30-1.40 (m, 2H), 1.40 (s, 9H), 1.50-
1.65 (m, 4H), 1.70-1.98 (m, 8H), 2.30-2.40 (m, IH), 2.57 (t, 2H, J = 7.5 Hz), 3.58-3.70 (m,
IH), 4.16 (d, IH, J = 9.3 Hz), 7.11-7.15 (m, 3H), 7.40 (d, 2H, J = 8.1 Hz).
1-23
1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.21 (s, 9H), 1.21-1.41 (m, 4H), 1.51-
1.64 (m, 4H), 1.86-2.01 (m, 4H), 2.12-2.25 (m, IH), 2.56 (t, 2H, J = 7.5 Hz), 2.87-2.96 (m,
IH), 3.00-3.12 (m, IH), 3.23-3.34 (m, IH), 3.67-3.75 (m, IH), 7.11 (d, 2H, J = 8.1 Hz), 7.40
(d, 2H, J = 8.4 Hz).
1-24
1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.25-1.37 (m, 2H), 1.40 (s, 9H), 1.48-
1.65 (m, 6H), 1.90 (d, 2H, J = 11.7 Hz), 2.02 (d, 2H, J = 11.7 Hz), 2.12-2.24 (m, IH), 2.56 (t,
2H, J = 7.5 Hz), 3.04 (t, 2H, J = 6.3 Hz), 4.31 (t, IH, J = 5.7 Hz), 7.11 (d, 2H, J = 8.1 Hz),
7.42 (d,2H, J = 8.4 Hz).
1-25
mp : 232-233 °C
1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.5 Hz), 1.23-1.40 (m, 4H), 1.40 (s, 9H), 1.51-
1.76 (m, 4H), 2.01-2.26 (m, 5H), 2.56 (t, 2H, J = 7.5 Hz), 3.22-3.38 (m, IH), 3.79 (d, IH, J =
9.3 Hz), 7.11 (d, 2H, J= 8.7 Hz), 7.17 (s, IH), 7.40 (d, 2H, J = 8.4 Hz).
1-26
1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.22 (s, 9H), 1.28-1.40 (m, 2H), 1.52-
1.62 (m, 2H), 1.85-1.96 (m, IH), 2.00-2.14 (m, IH), 2.38-2.53 (m, 2H), 2.56 (t, 2H, J = 7.5
Hz), 3.22-3.37 (m, 3H), 7.11 (d, 2H, J = 8.4 Hz), 7.45 (d, 2H, J = 8.4 Hz), 8.19 (s, IH).
1-27
1h-NMR (CDCI3) 6 ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.30-1.40 (m, 2H), 1.40 (s, 9H), 1.52-
1.61 (m, 2H), 1.95 (quint, 2H, J = 6.3 Hz), 2.50 (t, 2H, J = 6.9 Hz), 2.56 (t, 2H, J = 7.8 Hz),
3.31 (quart, 2H, J = 6.0 Hz), 4.30-4.36 (m, IH), 7.12 (d, 2H, J = 8.4 Hz), 7.43 (d, 2H, J = 8.4

Hz), 7.65 (s, IH).
1-28
1h-NMR (CDCI3) 5 ppm: 0.91 (t, 3H, J= 7.2 Hz), 1.21 (s, 9H), 1.30-1.62 (m, 8H), 2.08 (d,
4H, J = 11.1 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.04 (d, IH, J = 4.8 Hz), 3.20-3.30 (m, IH), 4.65-
4.76 (m, IH), 6.57 (s, IH), 7.10 (d, 2H, J = 8.7 Hz), 7.26 (d, 2H, J = 8.1Hz).
1-29
1h-NMR (CDCI3) 5ppm: 0.91 (t, 3H, J = 7.2 Hz), 1.23-1.62 (m, 8H), 1.40 (s, 9H), 2.12 (d,
4H, J = 14.4 Hz), 2.56 (t, 2H, J = 7.8 Hz), 3.28-3.40 (m, IH), 3.90 (s, IH), 4.60-4.73 (m, IH),
6.57 (s, IH), 7.10 (d, 2H, J = 8.4 Hz), 7.25 (d, 2H, J = 8.4Hz).
1-30
1h-NMR (CDCI3) Sppm: 0.91 (t, 3H, J = 7.5 Hz), 1.26-1.39 (m, 2H), 1.51-1.64 (m, 4H),
1.72-1.81 (m, 2H), 2.34 (t, 2H, J = 6.9 Hz), 2.56 (t, 2H, J = 7.8 Hz), 2.95-3.01 (m, 2H), 4.84
(t, IH, J = 5.7 Hz), 6.99-7.12 (m, 6H), 7.19-7.24 (m, IH), 7.30 (s, IH), 7.38-7.43 (m, 4H),
7.79 (d, 2H, J = 8.7 Hz).
1-31
XH-NMR (CDCI3) 5 ppm: 0.92 (t, 3H, J = 7.5 Hz), 1.21 (s, 9H), 1.28-1.62 (m, 8H), 2.07-
2.14 (m, 4H), 2.64 (t, 2H, J = 7.8 Hz), 3.11 (d, IH, J = 5.1 Hz), 3.20 (brs, IH), 3.90-4.04 (m,
IH), 6.06-6.14 (m, IH), 7.21 (t, 2H, J = 8.1 Hz), 7.67 (t, 2H, J = 8.4 Hz).
1-32
1h-NMR (CDCI3) 6 ppm: 0.92 (t, 3H, J = 7.2 Hz), 1.27-1.65 (m, 8H), 1.40 (s, 9H), 2.10-
2.23 (m, 4H), 2.65 (t, 2H, J = 7.5 Hz), 3.23-3.35 (m, IH), 3.49 (s, IH), 3.88-4.02 (m, IH),
5.84-5.92 (m, IH), 7.13 (t, 2H, J = 8.4 Hz), 7.65 (d, 2H, J = 8.1 Hz).
1-33
1h-NMR (CDCI3) 6 ppm: 0.94 (t, 3H, J = 7.2 Hz), 1.30-1.42 (m, 2H), 1.32 (s, 9H), 1.57-
1.66 (m, 2H), 2.67 (t, 2H, J = 7.8 Hz), 5.61 (s, IH), 6.93 (d, 2H, J = 8.7 Hz), 7.25 (d, 2H, J =
8.4 Hz), 7.49 (d, 2H, J = 9.0 Hz), 7.80 (d, 2H, J = 8.1 Hz), 8.22 (s, IH).
1-34

1h-NMR (CD3OD) 5 ppm: 0.95 (t, 3H, J = 7.5 Hz), 1.35 (s, 9H), 1.35-1.44 (m, 2H), 1.57-
1.69 (m, 2H), 2.69 (t, 2H, J = 7.5 Hz), 7.28-7.33 (m, 4H), 7.56 (d, 2H, J = 9.0 Hz), 7.83 (d,
2H, J = 8.4 Hz).
1-36
1h-NMR (CDCI3) 6 ppm: 0.92 (t, 3H, J = 7.5 Hz), 1.31-1.70 (m, 11H), 1.39 (s, 9H), 1.75-
1.85 (m, IH), 2.65 (t, 2H, J = 8.1 Hz), 3.13 (t, 2H, J = 6.6 Hz), 3.40 (t, 2H, J = 7.2 Hz), 4.10
(t, IH, J = 5.7 Hz), 6.21 (t, IH, J = 5.7 Hz), 7.23 (d, 2H, J = 8.1 Hz), 7.67 (d, 2H, J = 8.4
Hz).
1-37
1h-NMR (CDCI3) 6 ppm: 0.92 (t, 3H, J = 7.5 Hz), 0.95-1.10 (m, 2H), 1.31-1.40 (m, 2H),
1.39 (s, 9H), 1.55-1.63 (m, 4H), 1.80-1.92 (m, 4H), 2.65 (t, 2H, J = 7.8 Hz), 3.03 (t, 2H, J =
6.6 Hz), 3.31 (t, 2H, J = 6.6 Hz), 4.06 (t, IH, J = 6.0 Hz), 6.22 (t, IH, J = 6.0 Hz), 7.23 (d,
2H, J = 8.4 Hz), 7.67 (d, 2H, J = 8.1 Hz).
1-39
1h-NMR (CDCI3) 6 ppm: 1.13 (t, 3H, J = 7.2 Hz), 1.39 (s, 9H), 1.69-1.97 (m, 8H), 2.27-
2.38 (m, IH), 3.29-3.35 (m, 4H), 3.60-3.70 (m, IH), 4.52 (d, IH, J = 9.3 Hz), 6.64 (d, 2H, J =
8.4 Hz), 7.22 (s, IH), 7.31 (d, 2H, J = 9.0 Hz).
1-40
1h-NMR (CDCI3) 6 ppm: 1.38 (s, 9H), 1.68-1.96 (m, 8H), 2.30-2.40 (m, IH), 3.11 (t, 4H, J
= 4.8 Hz), 3.60-3.72 (m, IH), 3.86 (t, 4H, J = 4.8 Hz), 4.51 (brs, IH), 6.89 (d, 2H, J = 9.0
Hz), 7.42 (d, 2H, J = 8.7 Hz).
1-41
mp : >278 °C (dec.)
1h-NMR (CDCI3) 5 ppm: 1.18-1.40 (m, 2H), 1.40 (s, 9H), 1.62-1.75 (m, 2H), 2.01-2.27 (m,
5H), 3.10-3.13 (m, 4H), 3.22-3.38 (m, IH), 3.72 (d, IH, J= 9.3 Hz), 3.85-3.88 (m, 4H), 6.87
(d, 2H, J = 9.0 Hz), 7.10 (s, IH), 7.40 (d, 2H, J = 9.0 Hz).
1-42

1h-NMR (CDCI3) 6ppm: 1.40 (s, 9H), 1.61-1.97 (m, 8H), 2.16 (s, 3H), 2.33-2.43 (m, IH),
3.60-3.70 (m, IH), 4.66 (brs, IH), 7.12 (d, IH, J = 8.7 Hz), 7.46-7.50 (m, IH), 7.62 (s, H),
7.75-7.78 (m, IH), 7.86-7.91 (m, 2H).
1-43
1h-NMR (CDCI3) 5 ppm: 1.40 (s, 9H), 1.62-2.00 (m, 8H), 1.87 (s, 3H), 2.36-2.47 (m, IH),
3.24 (s, 3H), 3.64-3.74 (m, IH), 4.87 (brs, IH), 7.13 (d, 2H, J = 9.0 Hz), 7.64 (d, 2H, J = 8.4
Hz), 7.81 (s, H).
1-44
mp : 235-236 °C
1h-NMR (CDCI3) 5 ppm: 1.13 (t, 6H, J = 6.9 Hz), 1.18-1.33 (m, 2H), 1.40 (s, 9H), 1.60-
1.77 (m, 2H), 2.00-2.26 (m, 5H), 3.28-3.35 (m, 4H), 3.73 (d, IH, J = 9.3 Hz), 6.60-6.70 (m,
2H), 7.03 (brs, IH), 7.31 (d, 2H, J = 7.8 Hz).
1-45
mp : >268 °C (dec.)
1h-NMR (CDCI3) 6 ppm: 1.20-1.34 (m, 2H), 1.40 (s, 9H), 1.56-1.76 (m, 8H), 2.00-2.26 (m,
5H), 3.06-3.14 (m, 4H), 3.24-3.36 (m, IH), 3.72 (d, IH, J = 9.3 Hz), 6.90 (d, 2H, J = 8.7 Hz),
7.09 (s, IH), 7.36 (d, 2H, J = 8.7 Hz).
1-46
mp : >272 °C (dec.)
1h-NMR (DMSO-d6) 6 ppm: 1.28 (s, 9H), 1.31-1.59 (m, 7H), 1.87-2.00 (m, 4H), 2.23-2.34
(m, IH), 3.00-3.16 (m, IH), 4.35-4.45 (m, 2H), 6.81 (d, IH, J = 9.0 Hz), 7.16 (t, IH, J = 7.2
Hz), 7.43 (t, IH, J = 8.4 Hz), 7.52-7.58 (m, 3H), 8.04 (d, IH, J = 7.8 Hz), 8.43 (s, IH).
1-47
1h-NMR (CDCI3) 5 ppm: 1.20-1.36 (m, 2H), 1.40 (s, 9H), 1.62-1.77 (m, 2H), 1.98-2.32 (m,
5H), 3.31-3.40 (m, IH), 3.62 (d, IH, J = 9.0 Hz), 7.08 (s, IH), 7.29 (d, 2H, J = 9.0 Hz), 7.61
(d, 2H, J = 9.0 Hz).
1-48

1h-NMR (CDCI3) 6ppm: 1.22-1.36 (m, 2H), 1.40 (s, 9H), 1.62-1.77 (m, 2H), 2.00-2.31 (m,
5H), 3.24-3.40 (m, IH), 3.62 (d, IH, J = 10.2 Hz), 7.01 (t, 2H, J = 8.7 Hz), 7.09 (s, IH),
7.42-7.50 (m, 2H).
1-49
mp:270°C (dec.)
2H-NMR (CDCI3) 5ppm: 1.20-1.36 (m, 2H), 1.40 (s, 9H), 1.61-1.77 (m, 2H), 1.95-2.30 (m,
9H), 3.17-3.38 (m, 5H), 3.67 (d, IH, J = 9.3 Hz), 6.50 (d, 2H, J = 9.0 Hz), 6.97 (s, IH), 7.30
(d, 2H, J = 9.0 Hz).
1-50
mp : 252-253 °C
*H-NMR (CDCI3) 5 ppm: 1.21-1.37 (m, 2H), 1.40 (s, 9H), 1.62-1.78 (m, 2H), 1.98-2.32 (m,
5H), 3.26-3.40 (m, IH), 3.68 (d, IH, J = 9.6 Hz), 6.94-7.02 (m, 4H), 7.08 (t, IH, J = 7.5 Hz),
7.13 (s, IH), 7.31 (t, 2H, J = 7.5 Hz), 7.46 (d, 2H, J = 9.0 Hz).
1-51
mp : 278-279 °C
1h-NMR (CDCI3) 6 ppm: 1.02 (d, 6H, J = 6.9 Hz), 1.35 (s, 9H), 1.39-1.71 (m, 6H), 1.90-
2.09 (m, 2H), 3.16-3.30 (m, IH), 3.46 (d, IH, J = 9.0 Hz), 4.92-5.01 (m, IH), 6.91-6.95 (m,
2H), 7.00-7.07 (m, 3H), 7.13-7.16 (m, 2H), 7.30-7.36 (m, 2H).
1-52
mp : 276-277 °C
1h-NMR (CDCI3) 5 ppm: 1.20-1.36 (m, 2H), 1.40 (s, 9H), 1.60-1.78 (m, 2H), 1.98-2.30 (m,
5H), 2.36 (s, 3H), 2.58 (t, 4H, J = 4.5 Hz), 3.17 (t, 4H, J = 4.5 Hz), 3.21-3.40 (m, IH), 3.64
(d, IH, J = 9.0 Hz), 6.88 (d, 2H, J = 9.0 Hz), 7.01 (s, IH), 7.37 (d, 2H, J = 9.0 Hz).
1-53
mp : >300 °C
1h-NMR (DMSO-d6) 5 ppm: 1.20-1.54 (m, 4H), 1.27 (s, 9H), 1.73-1.88 (m, 2H), 1.89-2.01
(m, 2H), 2.13-2.25 (m, IH), 2.98-3.12 (m, IH), 3.15-3.31 (m, 8H), 6.76-6.84 (m, 2H), 6.93 (d,

2H, J = 9.0 Hz), 6.99 (d, 2H, J = 8.1 Hz), 7.24 (d, 2H, J = 8.1 Hz), 7.46 (d, 2H, J = 9.0 Hz),
9.60 (s, IH).
1-54
mp : >215 °C (dec.)
1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.27-2.00 (m, 18H), 2.14-2.26 (m, IH), 2.53-2.84
(m, 4H), 2.86-3.30 (m, 2H), 3.46-3.54 (m, IH), 3.62-3.74 (m, 2H), 6.78 (d, IH, J = 8.7 Hz),
6.87 (d, 2H, J = 7.8 Hz), 7.42 (d, 2H, J = 8.7 Hz), 9.58 (s, IH).
1-55
mp : >290 °C (dec.)
1h-NMR (CDC13) 6 ppm: 1.23-1.40 (m, 2H), 1.40 (s, 9H), 1.60-1.76 (m, 2H), 2.02-2.27 (m,
5H), 3.20 (t, 4H, J = 5.4 Hz), 3.21-3.32 (m, IH), 3.67 (d, IH, J = 9.3 Hz), 3.98 (t, 4H, J = 4.8
Hz), 6.52 (t, IH, J = 4.8 Hz), 6.93 (d, 2H, J = 8.4 Hz), 7.06 (s, IH), 7.41 (d, 2H, J = 8.7 Hz),
8.33 (d, 2H, J = 4.8 Hz).
1-56
mp : >232 °C (dec.)
1h-NMR (DMSO-d6) 5 ppm: 1.27 (s, 9H), 1.27-1.48 (m, 4H), 1.80-1.99 (m, 4H), 2.14-2.25
(m, IH), 3.04-3.24 (m, 8H), 3.68 (s, 3H), 3.76 (s, 3H), 6.44-6.47 (m, IH), 6.66 (s, IH), 6.76-
6.84 (m, 2H), 6.92 (d, 2H, J = 8.4 Hz), 7.46 (d, 2H, J = 8.4 Hz), 9.61 (s, IH).
1-57
mp : 284-285 °C (dec.)
1h-NMR (CDCI3) 6 ppm: 1.27 (t, 3H, J = 7.2 Hz), 1.40 (a, 9H), 1.61-2.24 (m, 9H), 2.35-
2.49 (m, IH), 2.76 (t, 2H, J= 10.2 Hz), 3.04-3.15 (m, 2H), 3.20-3.36 (m, IH), 3.55-3.59 (m,
2H), 3.87 (d, IH, J = 9.6 Hz), 4.12-4.19 (m, 2H), 6.90 (d, 2H, J = 8.7 Hz), 2.79 (s, IH), 7.40
(d, 2H, J = 8.7 Hz).
1-58
mp : >299 °C (dec.)
:H-NMR (CDCI3) 5 ppm: 1.26-1.33 (m, 2H), 1.40 (s, 9H), 1.56-2.42 (m, 19H), 2.73-2.81

(m, 4H), 3.16-3.26 (m, 4H), 3.64 (d, IH, J = 9.6 Hz), 6.87 (d, 2H, J = 8.7 Hz), 7.04 (s, IH),
7.37 (d, 2H, J = 9.0 Hz).
1-59
mp : >270 °C (dec.)
1h-NMR (CDCI3) Sppm: 1.26-1.47 (m, 2H), 1.47 (s, 9H), 1.60-1.80 (m, 4H), 2.01-2.32 (m,
5H), 3.28-3.40 (m, 3H), 3.62-3.74 (m, 3H), 5.74-5.96 (m, 2H), 6.92 (d, 2H, J = 8.7 Hz), 7.13
(s, IH), 7.39 (d, 2H, J = 9.0 Hz).
1-60
mp : 247-250 °C (dec.)
1h-NMR (CDCI3) 6 ppm: 1.20-1.37 (m, 2H), 1.40 (s, 9H), 1.60-1.78 (m, 2H), 1.98-2.33 (m,
5H), 2.93-3.03 (m, 2H), 3.22-3.40 (m, IH), 3.52 (t, 2H, J = 6.0 Hz), 3.62 (d, IH, J = 8.4 Hz),
4.36 (s, 2H), 6.93 (d, 2H, J = 8.7 Hz), 7.00 (s, IH), 7.11-7.22 (m, 4H),7.39 (d, 2H, J = 8.7
Hz).
1-61
mp : 280-281 °C
1h-NMR (CDCI3) 6 ppm: 1.21-1.38 (m, 2H), 1.41 (s, 9H), 1.64-1.80 (m, 2H), 2.02-2.33 (m,
5H), 3.24-3.40 (m, IH), 3.61 (d, IH, J = 9.0 Hz), 6.33 (t, 2H, J = 2.1 Hz), 7.04 (t, 2H, J = 2.1
Hz), 7.14 (s, IH), 7.34 (d, 2H, J = 9.0 Hz), 7.56 (d, 2H, J = 9.0 Hz).
1-62
mp : 260-262 °C
1h-NMR (CDCI3) 5 ppm: 1.22-1.39 (m, 2H), 1.41 (s, 9H), 1.64-1.82 (m, 2H), 2.02-2.35 (m,
5H), 3.24-3.40 (m, IH), 3.62 (d, IH, J = 9.6 Hz), 7.31 (d, 2H, J= 9.0 Hz), 7.51 (s, IH), 7.69
(d, 2H, J = 9.0 Hz).
1-63
mp : 248 °C
1h-NMR (CDCI3) Sppm: 1.20-1.38 (m, 2H), 1.40 (s, 9H), 1.61-1.78 (m, 2H), 1.98-2.32 (m,
5H), 3.22-3.45 (m, IH), 3.64 (d, IH, J = 9.3 Hz), 7.11 (s, IH), 7.37-7.46 (m, 4H).

1-64
mp : 272-275 °C (dec.)
1h-NMR (DMSO-d6) 6 ppm: 1.20-1.53 (m, 4H), 1.27 (s, 9H), 1.75-1.88 (m, 2H), 1.88-2.00
(m, 2H), 2.11-2.24 (m, IH), 2.96-3.12 (m, IH), 5.96 (s, 2H), 6.77 (d, IH, J = 8.7 Hz), 6.82 (d,
IH, J = 8.4 Hz), 6.95 (dd, IH, J = 1.8, 8.4 Hz), 7.29 (d, IH, J = 1.8 Hz), 9.70 (s, IH).
1-65
mp : 293-296 °C (dec.)
1h-NMR (DMSO-d6) 6 ppm: 1.20-1.70 (m, 10H), 1.27 (s, 9H), 1.79-2.038 (m, 4H), 2.18-
2.33 (m, IH), 2.98-3.30 (m, 5H), 6.79 (d, IH, J = 9.0 Hz), 6.97 (d, 2H, J = 8.1 Hz), 7.43-7.57
(m, 4H), 7.62 (d, 2H, J= 8.1 Hz), 9.82 (s, IH).
1-66
mp : >300 °C
1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.27-1.53 (m, 4H), 1.86-1.99 (m, 4H), 2.22-2.34
(m, IH), 2.39 (s, 3H), 3.00-3.14 (m, IH), 6.25 (s, IH), 6.79 (d, IH, J = 9.0 Hz), 7.47-7.50 (m,
IH), 7.69-7.76 (m, IH), 10.27 (s, IH).
1-67
mp : 248-249 °C
1h-NMR (DMSO-d6) 6 ppm: 1.20-1.54 (m, 4H), 1.27 (s, 9H), 1.77-1.90 (m, 2H), 1.90-2.02
(m, 2H), 2.02 (s, 3H), 2.17-2.32 (m, IH), 2.96-3.13 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.12-
7.30 (m, 3H), 7.89 (s, IH), 9.79 (s, IH), 9.88 (s, IH).
1-68
mp :>300 °C
1h-NMR (DMSO-d6) 5 ppm: 1.20-1.54 (m, 4H), 1.27 (s, 9H), 1.77-1.89 (m, 2H), 1.89-2.03
(m, 2H), 2.00 (s, 3H), 2.14-2.28 (m, IH), 2.95-3.13 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.40-
7.54 (m, 4H), 9.72 (s, IH), 9.83 (s, IH).
1-69
mp : 199-201 °C

1h-NMR (DMSO-d6) 6 ppm: 1.21-1.53 (m, 4H), 1.27 (s, 9H), 1.76-1.89 (m, 2H), 1.89-2.02
(m, 2H), 2.13-2.30 (m, 1H), 2.85 (s, 6H), 2.94-3.14 (m, 1H), 6.40 (dd, 1H, J = 2.4, 8.4 Hz),
6.78 (d, 1H, J = 8.7 Hz), 6.90 (d, 1H, J = 8.4 Hz), 7.05 (t, 2H, J = 8.4 Hz), 9.60 (s, 1H).
1-70
mp : 227-230 °C
1h-NMR (DMSO-d6) 6 ppm: 1.22-1.52 (m, 4H), 1.27 (s, 9H), 1.72-1.87 (m, 2H), 1.87-2.01
(m, 2H), 2.12-2.29 (m, 1H), 2.96-3.12 (m, 1H), 5.00 (s, 2H), 6.22 (d, 1H, J = 7.5 Hz), 6.66 (d,
1H, J = 7.5 Hz), 6.78 (d, 1H, J = 9.0 Hz), 6.86 (d, 1H, J = 7.5 Hz), 6.89-6.95 (m, 1H), 9.46 (s,
1H).
1-71
mp : 270-272 °C
1h-NMR (DMSO-dg) 6 ppm: 1.22-1.52 (m, 4H), 1.26 (s, 9H), 1.73-1.86 (m, 2H), 1.88-2.00 (m, 2H), 2.08-2.22 (m, 1H), 2.95-3.11 (m, 1H), 4.80 (s, 2H), 6.47 (d, 2H, J = 8.4 Hz), 6.77 (d, 1H, J = 8.4 Hz), 7.20 (d, 2H, J = 8.4 Hz), 9.35 (s, 1H).
1-72
mp : 262-263 °C
1h-NMR (CDC13) 6 ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.17-1.42 (m, 2H), 1.40 (s, 9H), 1.60-
1.78 (m, 2H), 1.98-2.43 (m, 7H), 3.20-3.43 (m, 3H), 3.67 (d, 1H, J = 9.6 Hz), 3.74-3.86 (m,
2H), 6.86 (d, 2H, J = 9.0 Hz), 7.04 (s, 1H), 7.38 (d, 2H, J = 9.0 Hz).
1-73
mp : 218-219 °C
1h-NMR (CD3OD) 6 ppm: 1.36 (s, 9H), 1.36-1.69 (m, 4H), 1.45 (s, 9H), 1.88-2.02 (m, 3H),
2.06-2.30 (m, 4H), 3.05-3.44 (m, 3H), 3.46-3.56 (m, 1H), 4.16-4.26 (m, 1H), 6.51 (d, 2H, J =
9.0 Hz), 7.30 (d, 2H, J = 8.7 Hz).
1-74
mp : 295-296 °C (dec.)
1h-NMR (CD3OD) 6 ppm: 1.36 (s, 9H), 1.36-1.67 (m, 4H), 1.92-2.13 (m, 4H), 2.26-2.40 (m,

2H), 2.62-2.75 (m, IH), 3.16-3.25 (m, IH), 3.58-3.98 (m, 4H), 4.16-4.25 (m, IH), 7.20-7.30
(m, 2H), 7.62 (d, 2H, J = 9.0 Hz).
1-75
mp : 250-251 °C
1h-NMR (DMSO-d6) 6 ppm: 1.23-1.55 (m, 4H), 1.27 (s, 9H), 1.78-1.90 (m, 2H), 1.90-2.02
(m, 2H), 2.15-2.28 (m, IH), 2.98-3.14 (m, IH), 3.06 (t, 2H, J = 8.4 Hz), 3.87 (t, 2H, J = 8.4
Hz), 6.67 (dd, IH, J= 1.5, 7.2 Hz), 6.80 (d, IH, J = 8.4 Hz), 6.94-7.05 (m, 2H), 7.12-7.19 (m,
IH), 7.16 (d, 2H, J = 9.3 Hz), 7.57 (d, 2H, J = 9.3 Hz), 9.73 (s, IH).
1-76
mp : 265-266 °C
1h-NMR (DMSO-dg) 6 ppm: 1.23-1.58 (m, 4H), 1.28 (s, 9H), 1.83-2.04 (m, 4H), 2.20-2.36
(m, IH), 2.97-3.16 (m, IH), 6.67 (d, IH, J = 3.0 Hz), 6.82 (d, IH, J = 8.4 Hz), 7.07-7.22 (m,
2H), 7.47-7.53 (m, IH), 7.50 (d, 2H, J = 9.0 Hz), 7.58 (d, IH, J = 3.0 Hz), 7.64 (d, IH, J =
7.5 Hz), 7.79 (d, 2H, J = 9.0 Hz), 10.02 (s, IH).
1-77
mp :281°C
1-H-NMR (DMSO-dg) Sppm: 1.21-1.56 (m, 4H), 1.27 (s, 9H), 1.80-2.03 (m, 4H), 2.18-2.31
(m, IH), 2.97-3.14 (m, IH), 6.51 (dd, IH, J = 2.1, 2.7 Hz), 6.81 (d, IH, J = 9.0 Hz), 7.67-7.78
(m, 5H), 8.41 (d, IH, J = 2.1 Hz), 9.96 (s, IH).
1-78
mp : >300 °C (dec.)
1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.27-1.52 (m, 4H), 1.74-2.04 (m, 7H), 2.10-2.25
(m, 2H), 2.96-3.20 (m, 2H), 3.48-3.58 (m, IH), 3.75-3.84 (m, IH), 6.39 (d, 2H, J = 8.4 Hz),
6.79 (d, IH, J = 8.4 Hz), 7.02 (s, IH), 7.30 (s, IH), 7.36 (d, 2H, J = 8.1 Hz), 9.48 (s, IH).
1-79
mp : 248-250 °C (dec.)
1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.27-1.54 (m, 4H), 1.85-1.99 (m, 4H), 2.24-2.33

(m, IH), 3.00-3.14 (m, IH), 6.82 (d, IH, J = 8.7 Hz), 7.77 (d, 2H, J = 8.4 Hz), 8.07 (d, 2H, J
= 8.4 Hz).
1-80
mp : >300 °C
1h-NMR (DMSO-dg) 6 ppm: 1.22-1.58 (m, 4H), 1.27 (s, 9H), 1.80-2.03 (m, 4H), 2.18-2.32
(m, IH), 2.98-3.14 (m, IH), 6.80 (d, IH, J = 8.7 Hz), 7.35-7.50 (m, 2H), 7.99 (s, IH), 8.11 (s,
IH), 9.79 (s, IH), 12.94 (s, IH).
1-81
mp : 261-262 °C
1h-NMR (DMSO-dg) 6 ppm: 1.21-1.57 (m, 4H), 1.27 (s, 9H), 1.78-2.02 (m, 4H), 2.17-2.30
(m, IH), 2.96-3.16 (m, IH), 6.34 (s, IH), 6.80 (d, IH, J = 8.7 Hz), 7.14-7.32 (m, 3H), 7.85 (s,
IH), 9.58 (s, IH), 10.95 (s, IH).
1-82
1h-NMR (CDC13) 6 ppm: 0.86 (s, 18H), 1.24-1.37 (m, 2H), 1.37 (s, 9H), 1.56-1.74 (m, 2H),
1.95-2.19 (m, 5H), 3.18-3.32 (m, IH), 3.44 (t, 4H, J = 6.3 Hz), 3.70 (t, 4H, J = 6.3 Hz), 4.39
(d, IH, J = 9.0 Hz), 6.59 (d, 2H, J = 9.0 Hz), 7.31 (d, 2H, J = 8.7 Hz), 7.43 (s, IH).
1-83
mp : 264-265 °C
1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.27-1.52 (m, 4H), 1.78-1.88 (m, 2H), 1.90-2.00
(m, 2H), 2.14-2.26 (m, IH), 2.96-3.14 (m, IH), 6.72-6.82 (m, 2H), 6.99 (t, 4H, J = 7.8 Hz),
7.18 (t, 2H, J = 7.5 Hz), 7.46 (d, 2H, J = 9.0 Hz), 8.00 (s, IH), 9.65 (s, IH).
1-84
mp : 257 °C (dec.)
1h-NMR (DMSO-dg) 5 ppm: 1.23-1.57 (m, 4H), 1.27 (s, 9H), 1.83-2.03 (m, 4H), 2.23-2.35
(m, IH), 2.98-3.15 (m, IH), 6.80 (d, IH, J = 8.1 Hz), 7.87 (d, 2H, J = 9.0 Hz), 8.34 (d, 2H, J
= 9.0 Hz), 9.21 (s, IH), 10.20 (s, IH).
1-85

mp : 256-258 °C
1h-NME (DMSO-d6) 6 ppm: 1.22-1.53 (m, 4H), 1.26 (s, 9H), 1.79-2.01 (m, 4H), 2.25 (s,
3H), 2.28-2.42 (m, IH), 2.97-3.02 (m, IH), 6.71 (d, IH, J= 0.9 Hz), 6.80 (d, IH, J = 8.1 Hz),
11.91 (s, IH).
1-86
mp : 228-230 °C
1h-NMR (CD3OD) 6 ppm: 1.36 (s, 9H), 1.36-1.48 (m, 2H), 1.55-1.70 (m, 2H), 1.87-1.98 (m,
2H), 2.08-2.17 (m, 2H), 2.20-2.32 (m, IH), 3.15-3.27 (m, IH), 3.50 (t, 4H, J = 5.7 Hz), 3.69
(t, 4H, J = 5.7 Hz), 6.72 (d, 2H, J = 9.0 Hz), 7.29-7.33 (m, 2H).
1-87
mp : 183-184 °C
1h-NMR (DMSO-d6) 5 ppm: 1.27 (s, 9H), 1.27-1.48 (m, 4H), 1.73-1.89 (m, 4H), 1.90-2.00
(m, 2H), 2.16-2.28 (m, IH), 2.28 (t, 2H, J = 7.5 Hz), 2.51-2.54 (m, 2H), 2.97-3.13 (m, IH),
3.58 (s, 3H), 6.79 (d, IH, J = 8.7 Hz), 7.08 (d, 2H, J = 8.7 Hz), 7.49 (d, 2H, J = 8.4 Hz), 9.73
(s, IH).
1-88
mp : 217-218 °C
1h-NMR (CD3OD) Sppm: 1.36 (s, 9H), 1.36-1.46 (m, 2H), 1.55-1.69 (m, 2H), 1.83-2.00 (m,
4H), 2.07-2.18 (m, 2H), 2.26-2.36 (m, 3H), 2.61 (t, 2H, J = 7.5 Hz), 3.14-3.26 (m, IH), 7.13
(d, 2H, J = 8.1 Hz), 7.44 (d, 2H, J = 8.1 Hz).
1-89
1h-NMR (CDCI3) 6 ppm: 0.08 (d, 6H, J = 3.3 Hz), 0.88(s, 9H), 1.21-1.36 (m, 2H), 1.39 (s,
9H), 1.61-1.74 (m, 2H), 1.88-2.23 (m, 6H), 3.06-3.11 (m, IH), 3.24-3.74 (m, 4H), 3.92 (d, IH,
J = 9.6 Hz), 4.48-4.56 (m, IH), 6.47 (d, 2H, J = 9.0 Hz), 7.17 (s, IH), 7.32 (d, 2H, J = 9.0
Hz).
1-90
mp : amorphous

1h-NMR (CD3OD) 5 ppm: 1.36 (s, 9H), 1.36-1.47 (m, 2R), 1.56-1.70 (m, 3H), 1.88-2.30 (m,
6H), 3.05-3.49 (m, 5H), 4.50 (brs, IH), 6.50 (d, 2H, J = 9.0 Hz), 7.29 (d, 2H, J = 9.0 Hz).
1-91
mp : 105-106 °C
1h-NMR (CDCI3) 5 ppm: 0.92(t, 3H, J = 7.3 Hz), 1.25-1.27(m, 2H), 1.36(d, 6H, J = 6.9
Hz), 1.51-1.59(m, 2H), 2.56(t, 2H, J = 7.8 Hz), 3.27(sept, IH, J = 6.9 Hz), 7.12(d, 2H, J =
8.6 Hz), 7.32(t, IH, J = 7.8 Hz), 7.45(brd, IH, J = 7.8 Hz), 7.53(d, 2H, J = 8.6 Hz), 7.58(d,
IH, J = 7.8 Hz), 7.71-7.72(m, 2H), 8.27(s, IH).
1-92
mp : 163-164 °C
1h-NMR (CDCI3) 6 ppm: 0.93(t, 3H, J = 7.3 Hz), 1.32-1.39(m, 2H), 1.55-1.65(m, 2H),
1.87(s, 3H), 1.95(8, 3H), 2.60(t, 2H, J = 7.6 Hz), 7.07(d, 2H, J = 8.4 Hz), 7.18(d, 2H, J = 8.5
Hz), 7.54(d, 2H, J = 8.5 Hz), 7.91(brs, IH), 8.18(d, 2H, J = 8.4 Hz), 8.77(s, IH).
1-93
mp : 173 °C
1h-NMR (CDCI3) 5 ppm: 0.93(t, 3H, J = 7.3 Hz), 1.32-1.40(m, 2H), 1.39(d, 6H, J = 6.9
Hz), 1.55-1.62(m, 2H), 2.60(t, 2H, J = 7.8 Hz), 3.13(sept, IH, J = 6.9 Hz), 4.39(d, 2H, J =
6.3 Hz), 4.45(t, IH, J = 6.3 Hz), 7.18(d, 2H, J = 8.7 Hz), 7.46(d, 2H, J = 8.7 Hz), 7.54 (d, 2H,
J = 8.7 Hz), 7.80(s, IH), 7.85(d, 2H, J = 8.7 Hz).
1-94
mp : 159-160 °C
1h-NMR (CDCI3) 6 ppm: 0.93(t, 3H, J = 7.3 Hz), 1.32-1.39(m, 2H), 1.54-1.80(m, 2H),
1.79(s, 3H), 1.80(s, 3H), 2.60t, 2H, J = 7.7 Hz), 3.18(s, 3H), 7.18(d, 2H, J = 8.5 Hz), 7.30(d,
2H, J = 8.8 Hz), 7.52(d, 2H, J = 8.5 Hz), 7.70(brs, IH), 7.84(d, 2H, J = 8.8 Hz), 8.77(s, IH).
1-95
mp : 177-178 °C
1h-NMR (CDCI3) 5 ppm: 0.94(t, 3H, J = 7.2Hz), 1.31-1.48(m, 8H), 1.54-1.66(m, 2H),

2.55(8, 3H), 2.62(t, 2H, J = 7.6Hz), 3.92(sept, IH, J = 6.6Hz), 7.20(d, 2H, J = 8.45Hz),
7.74(d, 2H, J = 8.5Hz), 9.01(brs, IH), 9.17(s, IH).
1-96
mp : 220-223 °C
1h-NMR (CDCI3) 6 ppm: 0.93(t, 3H, J = 7.3Hz), 1.28-1.42(m, 2H), 1.50(d, 6H, J = 6.8Hz), 1.54-1.65(m, 2H), 2.62(t, 2H, J= 7.6Hz), 4.08(sept, IH, J= 7.1Hz), 7.20(d, 2H, J = 8.5Hz), 7.48(d, 2H, J = 8.5Hz), 7.71(brs, IH), 8.51(brs, IH), 8.95(s, IH). 1-97
mp : 195-197 °C
1h-NMR (CDCI3) 6 ppm: 0.91(t, 3H, J = 7.6Hz), 0.94(t, 3H, J = 7.3Hz), 1.32-1.44(m, 6H), 1.54-1.64(m, 2H), 1.66-1.78(m, 2H), 2.62(t, 2H, J = 7.7Hz), 2.86(brs, 2H), 3.98(sept, IH, J = 7.1Hz), 7.19(d, 2H, J = 8.5Hz), 7.63(d, 2H, J = 8.4Hz), 8.72(brs, IH), 8.81(brs, IH). 1-98
mp : 216-218 °C
1h-NMR (CDCI3+CD3OD) 6 ppm: 0.93(t, 3H, J = 7.4Hz), 1.29-1.40(m, 2H), 1.43(d, 2H, J = 6.9Hz), 1.51-1.63(m, 2H), 2.60(t, 2H, J = 7.8Hz), 3.65(sept, IH, J = 6.9Hz), 7.18(d, 2H, J = 8.5Hz), 7.22(d, IH, J = 8.8Hz), 7.55(d, 2H, J = 8.5Hz), 8.18(dd, IH, J = 8.8, 2.4Hz), 8.63(d, IH, J = 2.4Hz). 1-99
mp : 201-202 °C
1h-NMR (CDCI3) 6ppm:0.93(t, 3H, J = 7.3Hz), 1.22-1.40(m, 2H), 1.49(d, 2H, J = 7.1Hz), 1.51-1.63(m, 2H), 2.59(t, 2H, J = 7.7Hz), 4.22(sept, IH, J= 7.1Hz), 7.16(d, 2H, J = 8.4Hz), 7.41(brs, IH), 7.52(d, 2H, J = 8.4Hz), 8.10(brs, IH), 8.13(d, IH, J = 2.2Hz), 8.61(brs, IH). I-100
mp : 160-162 °C
1h-NMR (CDCI3) 6ppm: 0.93(t, 3H, J = 7.3Hz), 1.22-1.42(m, 2H), 1.45(d, 2H, J = 6.9Hz), 1.51-1.63(m, 2H), 2.61(t, 2H, J = 7.8Hz), 3.37(sept, IH, J= 6.9Hz), 6.89(brs, IH), 7.19(d,

2H, J = 8.4Hz), 7.65(d, 2H, J = 8.4Hz), 7.80(dd, IH, J = 8.4, 2.4Hz), 8.27(d, IH, J = 8.4Hz),
8.45(d, IH, J= 2.4Hz), 9.75(brs, IH).
I-101,1-214
mp: 192-194 °C
1h-NMR (CDC13) 6 ppm:0.93(t, 3H, J = 7.3Hz), 1.27-1.41(m, 2H), 1.35(s, 9H), 1.50-
1.66(m, 2H), 2.60(t, 2H, J = 7.6Hz), 5.58(brs, IH), 7.07(d, 2H, J = 8.5Hz), 7.17(d, 2H, J =
8.5Hz), 7.52(d, 2H, J = 8.5Hz), 7.71(brs, IH), 7.79(d, 2H, J = 8.5Hz).
1-102
mp : 216-217 °C
1h-NMR (CDCI3) 5 ppm:0.93(t, 3H, J = 7.3Hz), 1.26-1.42(m, 2H), 1.45(s, 9H), 1.70-
1.83(m, 2H), 2.60(t, 2H, J = 7.7Hz), 6.42(brs, IH), 7.18(d, 2H, J = 8.5Hz), 7.35(d, 2H, J =
8.5Hz), 7.51(d, 2H, J = 8.5Hz), 7.68(brs, IH), 7.82(d, 2H, J = 8.5Hz).
1-103
1h-NMR (CDC13) 5 ppm: 0.91(t, 3H, J = 7.3 Hz), 1.28-1.36(m, 2H), 1.32(d, 6H, J = 6.9
Hz), 1.49-1.59(m, 2H), 2.54(t, 2H, J = 7.7 Hz), 3.23(sept, IH, J = 6.9 Hz), 3.46(s, 3H),
6.76(brs, IH), 6.91(d, 2H, J = 8.2 Hz), 6.99(d, 2H, J = 8.8 Hz), 7.03(d, 2H, J = 8.2 Hz),
7.25(d, 2H, J = 8.8 Hz).
1-104
mp : 182-183 °C
XH-NMR (CDCI3) 6 ppm:0.93(t, 3H, J = 7.3Hz), 1.28-1.40(m, 2H), 1.51-1.63(m, 2H),
1.64-1.88(m, 4H), 1.90-2.23(m, 4H), 2.60(t, 2H, J = 7.6Hz), 3.39(m, IH), 6.16(brs, IH),
7.07(d, 2H, J = 8.5Hz), 7.16(d, 2H, J = 8.5Hz), 7.52(d, 2H, J = 8.5Hz), 7.74(brs, IH), 7.77(d,
2H, J=8.5Hz).
1-105
mp : 190-191 °C
1h-NMR (CDCI3) 5 ppm:0.93(t, 3H, J = 7.3Hz), 1.28-1.41(m, 2H), 1.52-1.69(m, 4H),
1.75-1.90(m, 2H), 1.92-2.07(m, 4H), 2.58(t, 2H, J = 7.6Hz), 3.59(m, IH), 6.53(brs, IH),

7.18(d, 2H, J = 8.5Hz), 7.31(d, 2H, J = 8.5Hz), 7.52(d, 2H, J = 8.5Hz), 7.67(brs, IH), 7.84(d,
2H, J = 8.5Hz).
1-106
mp : 194-197 °C
1h-NMR (CDCI3) 6 ppm:0.93(t, 3H, J = 7.3Hz), 1.22-1.41(m, 2H), 1.53-1.65(111, 2H),
1.90(s, 6H), 2.60(t, 2H, J = 7.8Hz), 6.86(brs, IH), 7.18(d, 2H, J = 8.5Hz), 7.43(d, 2H, J =
8.5Hz), 7.5l(d, 2H, J = 8.5Hz), 7.71(brs, IH), 7.84(d, 2H, J = 8.5Hz).
1-107
mp : 211-212 °C
1h-NMR (CDCI3) 6 ppm:0.93(t, 3H, J = 7.3Hz), 1.24-1.40(m, 2H), 1.50-1.62(m, 2H),
2.60(t, 2H, J = 7.6Hz), 6.19(brs, IH), 7.17(d, 2H, J = 8.5Hz), 7.18(d, 2H, J = 8.5Hz), 7.51(d,
2H, J = 8.5Hz), 7.66(brs, IH), 7.86(d, 2H, J = 8.5Hz).
1-108
mp : 298-300 °C
1h-NMR (DMSO-d6) 6 ppm: 0.90(t, 3H, J = 7.3Hz), 1.22-1.39(m, 2H), 1.48-1.60(m, 2H),
2.54(t, 2H, J = 7.3Hz), 7.04(d, 2H, J = 8.8Hz), 7.12(d, 2H, J = 8.5Hz), 7.64(d, 2H, J =
8.5Hz), 7.69(d, 2H, J = 8.8Hz), 9.80(s, IH).
1-109
mp: 122-123 °C
1h-NMR (CDCI3) 5 ppm:0.90(t, 3H, J = 7.4Hz), 0.97(t, 3H, J = 7.7Hz), 1.26-1.38(m, 2H),
1.30(s, 6H), 1.50-1.66(m, 4H), 1.72-1.83(m, 4H), 2.34(t, 2H, J = 7.1Hz), 2.55(t, 2H, J =
7.6Hz), 3.19(q, IH, J = 6.0Hz), 4.60(brs, IH), 7.08(d, 2H, J = 8.5Hz), 7.42(d, 2H, J = 8.5Hz),
7.85(8, IH).
1-110
mp : 109-110 °C
1h-NMR (CDCI3) 6ppm:0.91(t, 3H, J = 7.4Hz), 1.10(d, 6H, J = 6.7Hz), 1.29-1.38(m, 2H),
1.55(8, 9H), 1.60-1.70(m, 2H), 1.78-1.89(m, 2H), 2.26(m, IH), 2.39(t, 2H, J = 7.0Hz), 2.57(t,

2H, J = 7.7Hz), 2.90(d, 2H, J = 6.6Hz), 3.16(brs, IH), 4.24(brs, IH), 7.12(d, 2H, J = 8.5Hz),
7.40(d,2H, J = 8.5Hz).
Mil
mp : 64-65 °C
1h-NMR (CDCI3) 6 ppm:0.91(t, 3H, J = 7.3Hz), 1.02(t, 3H, J = 7.5Hz), 1.35(d, 3H, J =
6.7Hz), 1.26-1.38(m, 2H), 1.48-1.69(m, 5H), 1.76-1.87(m, 2H), 2.04(m, IH), 2.38(t, 2H, J =
7.3Hz), 2.56(t, 2H, J = 7.6Hz), 2.91(m, IH), 3.16(brs, 2H), 4.42(brs, IH), 7.11(d, 2H, J =
8.5Hz), 7.42(d, 2H, J = 8.5Hz), 7.47(brs, IH).
1-112
mp : 79-80 °C
1h-NMR (CDCI3) 6 ppm:1.36(s, 9H), 1.52-1.62(m, 2H), 1.67-1.76(m, 2H), 2.22(t, 2H, J =
7.4Hz), 3.16(q, 2H, J = 6.3Hz), 3.78(s, 3H), 4.33(d, 2H, J = 5.4Hz), 4.62(brs, IH), 6.20(brs,
IH), 6.86(d, 2H, J = 8.8Hz), 7.19(d, 2H, J = 8.8Hz).
1-113
mp : 125-126 °C
1h-NMR (CDCI3) 6 ppm:1.38(s, 9H), 1.62-1.70(m, 2H), 1.76-1.88(m, 2H), 2.46(t, 2H, J =
7.4Hz), 3.22(q, 2H, J = 6.1Hz), 4.22(t, IH, J = 6.1Hz), 7.24(dd, IH, J = 8.9, 2.3Hz), 7.36(d,
IH, J= 2.3Hz), 7.65(brs, IH), 8.29(d, IH, J = 8.9Hz).
1-114
mp : 89-91 °C
1h-NMR (CDCI3) 6 ppm:0.92 (t, 3H, J = 7.0Hz), 1.06 (d, 6H, J = 7.0Hz), 1.36 (m ,1H),
1.50-1.72 (m ,5H), 1.94-2.06 (m, 2H), 2.26 (m, IH), 2.60 (t, 2H, J = 7.7Hz), 2.84 (t, 2H, J =
7.7Hz), 2.93 (d, 2H, J = 6.3Hz), 3.20 (t, 2H, J = 6.6Hz), 4.30 (brs, IH), 7.19 (d, 2H, J =
8.5Hz), 7.63 (d, 2H, J = 8.5Hz), 9.15(brs, IH).
1-115
mp : 94-95 °C
1h-NMR (CDCI3) 5 ppm:0.92 (t, 3H, J = 7.5Hz), 1.03 (t, 3H, J = 7.5Hz), 1.23-1.40

(m ,5H), 1.42-1.65 (m, 6H), 1.75 (m, IH), 2.02 (m, IH), 2.24 (t, 2H, J = 7.0Hz), 2.59 (t, 2H,
J = 8.0Hz), 2.90 (m, IH), 3.14 (q, 2H, J = 6.6Hz), 4.20 (m, IH), 4.40 (d, 2H, J = 5.4Hz), 5.70
(brs, IH), 7.14 (d, 2H, J = 8.1Hz), 7.18(d, 2H, J = 8.1Hz).
1-116
mp : 89-91 °C
1h-NMR (CDC13) 6 ppm:0.97 (t, 3H, J = 7.3Hz), 1.02 (t, 3H, J = 7.5Hz), 1.35 (d, 3H, J =
7.0Hz), 1.40-1.90 (m ,9H), 2.04 (m ,1H), 2.37 (t, 2H, J= 7.0Hz), 2.90 (m, IH), 3.17 (q, 2H, J
= 6.6Hz), 3.93 (t, 2H, J = 6.6Hz), 4.32 (m, IH), 6.84 (d, 2H, J = 9.0Hz), 7.31 (brs, IH), 7.40
(d, 2H, J = 9.0Hz).
1-117
mp: 110-111 °C
1h-NMR (CDCI3) 5 ppm:1.02 (t, 3H, J = 7.5Hz), 1.34 (d, 3H, J = 6.6Hz), 1.45-1.70
(m ,3H), 1.75-1.85 (m, 2H), 2.05 (m ,1H), 2.36 (t, 2H, J = 7.5Hz), 2.90 (m, IH), 3.16 (q, 2H,
J = 6.6Hz), 3.78 (s, 3H), 4.50 (m, IH), 6.84 (d, 2H, J = 6.8Hz), 7.42 (d, 2H, J = 6.8Hz), 7.48
(brs, IH).
1-118
mp: 113-115 °C
1h-NMR (CDCI3) 6 ppm:0.92 (t, 3H, J = 7.0Hz), 1.20-1.34 (m ,1H), 1.37 (d, 6H, J =
7.0Hz), 1.48-1.70 (m, 3H), 2.43 (q, 2H, J = 6.6Hz), 2.58 (t, 2H, J = 7.7Hz), 3.10-3.31 (m,
3H), 4.75 (m, IH), 6.04 (d, IH, J = 15.0Hz), 6.77 (dt, IH, J = 7.7, 15.0Hz), 7.14 (d, 2H, J =
8.4Hz), 7.55 (d, 2H, J = 8.4Hz), 7.85 (brs, IH).
1-119
mp: 139-140 °C
1h-NMR (CDCI3) 6 ppm:1.19(s, 9H), 1.47(m, 2H), 1.61(m, 2H), 2.18(t, 2H, J = 7.6Hz),
3.03(q, 2H, J = 6.3Hz), 4.09(t, IH, J = 5.9Hz), 6.85(brd, IH, J = 8.0Hz), 7.00(t, IH, J =
8.0Hz), 7.16(brd, IH, J = 8.0), 7.48(brs, IH), 7.57(brs, IH).
1-120

mp: 183°C
1h-NMR (CDCI3) 6 ppm:0.91(t, 3H, J = 7.3Hz), 1.20-1.58(m, 6H), 1.40(s, 9H), 2.07(dd,
IH, J = 12.9, 3.1Hz), 2.52(t, 2H, J = 7.7Hz), 2.95(dd, 2H, J = 11.5, 2.5Hz), 3.46(m, IH),
3.88-4.07(m, 3H), 6.47(s, IH), 7.08(d, 2H, J = 8.5Hz), 7.22(d, 2H, J = 8.5Hz).
1-121
mp: 163-166°C
1h-NMR (CDCI3) 5 ppm:0.91(t, 3H, J = 7.3Hz), 1.32-1.62(m, 6H), 1.45(s, 9H), 1.95-
2.07(m, 3H), 2.20(m, IH), 2.46(td, IH, J = 10.4, 3.7Hz), 2.37(t, 2H, J = 7.6Hz), 3.43(brd,
2H, J = 10.4Hz), 4.80(s, IH), 7.12(d, 2H, J= 8.4Hz), 7.14(s, IH), 7.39(d, 2H, J = 8.4Hz).
1-122
mp: 188-189 °C
1h-NMR (CDCI3) 6 ppm:0.91 (t, 3H, J = 7.5Hz), 1.25-1.41 (m ,2H), 1.42 (s, 9H), 1.50-
1.62 (m ,2H), 1.78-1.95 (m ,4H), 2.00-2.20 (m ,6H), 2.57 (t, 2H, J = 7.5Hz), 3.99 (brs, IH),
7.10 (brs, IH), 7.12 (d, 2H, J = 6.5Hz), 7.41 (d, 2H, J = 6.5Hz).
1-123
mp : 197-198 °C
1h-NMR (CDCI3) 5 ppm:0.9l (t, 3H, J = 7.5Hz), 1.24-1.40 (m ,2H), 1.39 (s, 9H), 1.50-
1.70 (m ,2H), 1.99 (brs ,12H), 2.56 (t, 2H, J = 7.5Hz), 3.47 (brs, IH), 7.10 (s, IH), 7.11 (d,
2H, J = 8.5Hz), 7.38 (d, 2H, J = 8.5Hz).
1-124
mp : 258-260 °C
1h-NMR (CDC13) 5 ppm: 1.20-1.40 (m, 2H), 1.41 (s, 9H), 1.62-1.81 (m, 2H), 2.03-2.35 (m,
5H), 2.37 (s, 3H), 2.71 (s, 3H), 3.32 (m, IH), 3..64 (d, IH, J = 8.4Hz), 7.08 (brs, IH), 7.24
(m, IH), 7.33 (m, 2H), 7.60 (d, IH, J = 8.1Hz), 7.77 (s, IH), 7.80 (d, IH, J = 8.4Hz), 8.14 (m,
IH).
1-125
mp : 297-299 °C

1h-NMR (DMSO-d6) 5 ppm:1.27 (s, 9H), 1.28-1.56 (m, 4H), 1.80-2.01 (m, 4H), 2.47 (m,
IH), 2.76 (brs, IH), 3.05 (m, 2H), 6.78 (d, IH, J = 9.0Hz), 7.23 (d, IH, J = 9.0Hz), 7.46 (dd,
IH, J = 2.0, 9.0Hz), 8.03 (d, IH, J = 2.0Hz).
1-126
mp : 198-199 °C
1h-NMR (CDC13) 5ppm:1.18-1.39 (m, 2H), 1.40 (s, 9H), 1.60-1.79 (m, 2H), 1.98-2.35 (m,
5H), 3.30 (m, IH), 3.67 (d, IH, J = 9.6Hz), 5.89 (tt, IH, J = 3.0, 50.0Hz), 6.97 (d, IH, J =
7.8Hz), 7.21 (s, IH), 7.30-7.40 (m, 2H), 7.55 (s, IH)
1-127
mp : 262-264 °C
1h-NMR (CDCI3) 6 ppm: 1.20-1.39 (m, 2H), 1.41 (s, 9H), 1.60-1.80 (m, 2H), 2.00-2.36 (m,
5H), 2.57 (s, 3H), 3.33 (m, IH), 3..62 (d, IH, J = 8.7Hz), 7.28 (brs, IH), 7.62 (d, 2H, J =
8.7Hz), 7.94 (d, 2H; J = 8.7Hz).
1-128
mp : 252-254 °C
1h-NMR (CDCI3) 5ppm:1.18-1.39 (m, 2H), 1.40 (s, 9H), 1.58-1.79 (m, 2H), 1.99-2.30 (m,
5H), 2.46 (s, 3H), 3.32 (m, IH), 3..64 (m, IH), 7.11 (brs, IH), 7.23 (d, 2H, J = 9.0Hz), 7.44
(d, 2H, J = 9.0Hz).
1-129
mp : >300 °C
1h-NMR (CDCI3+CD3OD) 6ppm:1.30-1.45(m, 2H), 1.42(s, 9H), 1.70-1.88(m, 2H), 2.10-
2.37(m, 4H), 2.52(m, IH), 3.34(m, IH), 7.43-7.54(m, 3H), 7.82(d, IH, J = 6.7Hz), 7.88(d,
IH, J = 8.5Hz), 7.98-8.07(m, 2H), 8.44(s, IH), 8.46(s, IH).
1-130
mp : 123-124 °C
1h-NMR (CDCI3) 6 ppm:1.18-1.34(m, 2H), 1.40(s, 9H), 1.62-1.75(m, 2H), 2.00-2.28(m,
5H), 3.31(m, IH), 3.6l(d, IH, J = 9.5Hz), 5.59(s, IH), 7.17(s, IH), 7.30-7.37(m, 6H), 7.41(d,

IH, J = 8.5Hz), 7.84(d, IH, J = 2.1Hz).
1-131
mp : 202-204 °C
1h-NMR (CDCI3) 6 ppm:1.27-1.38(m, 2H), 1.38(s, 9H), 1.62-1.75(m, 2H), 1.97-2.04(m,
2H), 2.18-2.27(m, 3H), 3.26(m, IH), 3.81(s, 3H), 4.62(d, IH, J = 7.9Hz), 7.12(d, IH, J =
7.8Hz), 7.40(t, IH, J = 7.8Hz), 7.51(s, 3H), 7.61(d, IH, J = 7.8Hz), 7.71(s, IH), 8.21(brs,
IH).
1-132
mp : 236-237 °C
1h-NMR (CDCI3) 6 ppm:1.23-1.43(m, 2H), 1.41(s, 9H), 1.66-1.80(m, 2H), 2.08-2.12(m,
2H), 2.23-2.31(m, 3H), 3.34(m, IH), 3.87(d, IH, J = 9.5Hz), 4.02(s, 3H), 7.30(td, IH, J = 7.3,
1.1Hz), 7.36(s, IH), 7.39(td, IH, J = 7.3, 1.5Hz), 7.53(brd, IH, J = 7.3Hz), 7.84(brd, IH, J =
7.3Hz), 8.05(s, IH), 8.73(s, IH).
1-133
mp : 198-200 °C
1h-NMR (CDCI3) 6ppm:0.93(t, 3H, J = 7.3Hz), 0.97(t, 3H, J= 6.7Hz), 1.18-1.8l(m, 7H),
1.39(s, 9H), 1.98-2.05(m, 2H), 2.2l-2.24(m, 3H), 3.29(m, IH), 4.00(dd, IH, J = 10.7, 6.7Hz),
4.09(dd, IH, J= 10.7, 6.1Hz), 4.27(d, IH, J = 9.8Hz), 6.37(d, IH, J= 15.9Hz), 7.47(d, 2H, J
= 8.5Hz), 7.59(d, 2H, J = 8.5Hz), 7.62(d, IH, J = 15.9Hz), 7.83(brs, IH).
1-134
mp : 212-213 °C
1h-NMR (CDCI3) 6ppm:1.21-1.32(m, 2H), 1.39(s, 9H), 1.59-1.73(m, 2H), 1.99-2.04(m,
2H), 2.10-2.26(m, 3H), 3.26(m, IH), 3.72(d, IH, J = 9.6Hz), 6.74(m, IH), 7.02(d, 2H, J =
7.4Hz), 7.11(t, IH, J = 7.4Hz), 7.13-7.19(m, 2H), 7.22-7.26(m, 2H), 7.34(t, 2H, J = 7.4Hz).
1-135
mp : 294-296 °C
1h-NMR (DMSO-dg) 5 ppm:1.27 (s, 9H), 1.28-1.55 (m, 4H), 1.81-2.05 (m, 4H), 2.26 (m,

IH), 2,98-3.20 (m, 2H), 6.78 (d, IH, J = 9.0Hz), 7.31 (t, IH, J = 7.5Hz), 7.54-7.72 (m, 5H),
7.94 (brs, IH).
1-136
mp : >300 °C
1h-NMR (DMSO-dg) 6ppm:1.28 (a, 9H), 1.29-1.59 (m, 4H), 1.81-2.02 (m, 4H), 2.27 (m,
IH), 3.06 (m, IH), 6.81 (d, IH, J = 8.7Hz), 7.38 (t, IH, J = 7.2Hz), 7.48 (t, 2H, J = 7.2Hz),
7.62-7.81 (m, 10H), 9.93 (brs, IH).
1-137
mp : 291-292 °C
J-H-NMR (CDCI3) 6 ppm:l.25-1.39 (m, 2H), 1.41 (a, 9H), 1.61-1.80 (m, 2H), 2.01-2.36 (m,
5H), 3.32 (m, IH), 3.63 (d, IH, J= 9.3Hz), 7.20 (brs, IH), 7.53-7.74 (m, 8H).
1-138
mp : 259-262 °C
1h-NMR (CD3OD) 6 ppm:1.40 (a, 9H), 1.40-1.80 (m, 4H), 2.00-2.30 (m, 4H), 2.45 (m,
IH), 3.00 (a, 3H), 3.15-3.30 (m, 2H), 7.90 (d, IH, J = 8.4Hz), 8,12 (d, IH, J = 9.0Hz), 8.39 (d,
IH, J = 9.0Hz), 8.72 (s, IH), 8.92 (d, IH, J = 8.4Hz), 10.4 (s, IH).
1-139
mp : 265-268 °C
1h-NMR (CDCI3) 6ppm:1.25-1.40(m, 2H), 1.40(s, 9H), 168-1.81(m, 2H), 2.05-2.10(m,
2H), 2.23-2.37(m, 3H), 3.32(m, IH), 4.27(d, IH, J = 9.1Hz), 7.53(t, IH, J= 7.9Hz), 7.63(td,
IH, J = 7.9, 1.4Hz), 7.77(d, IH, J = 7.9Hz), 8.03(d, IH, J = 7.9Hz), 8.37(brs, IH), 8.85-
8.86(m, 2H).
1-140
mp : 258-260 °C
1h-NMR (CDCI3) 6 ppm:1.20-1.40 (m, 2H), 1.41 (s, 9H), 1.52-1.85 (m, 2H), 2.03-2.35 (m,
5H), 3.34 (m, IH), 3.75 (m, IH), 7.35-7.66 (m, 3H), 8.05 (d, IH, J = 9.0Hz), 8.11 (d, IH, J =
9.0Hz), 8.40 (brs, IH), 8.83 (s, IH).

1-141
mp : 205-206 °C
1h-NMR (CDCI3) 6ppm:1.20-1.37(m, 2H), 1.40(s, 9H), 1.43-1.62(m, 2H), 1.90-2.01(m, 2H), 2.02-2.23(m, 3H), 3.27(m, IH), 3.63(d, IH, J = 9.6Hz), 3.70(s, 3H), 6.64(d, IH, J = 8.8Hz), 7.28-7.41(m, 5H), 7.45(brs, IH), 8.26(d, IH, J = 8.8Hz). 1-142
mp : 277-280 °C
1h-NMR (CDCI3) 5ppm:0.23-0.34(m) 2H), 1.34(s, 9H), 1.34-1.55(m, 5H), 1.76-1.80(m, 2H), 2.97(m, IH), 3.31(d, IH, J = 9.6Hz), 7.18(s, IH), 7.50-7.59(m, 4H), 7.77(dd, IH, J = 7.4, 1.0Hz), 7.9l-7.98(m, 2H), 8.39(dd, IH, J = 7.4, 1.9Hz). 1-143
mp : 202-203 °C
1h-NMR (CDCI3) 5ppm:1.23-1.40(m, 2H), 1.40(s, 9H), 1.57-1.71(m, 2H), 2.05-2.10(m, 2H), 2.18-2.28(m, 3H), 3.31(m, IH), 3.9l(s, 3H), 3.93(s, 3H), 4.05(d, IH, J = 9.5Hz), 8.15(s, IH), 9.56(s, IH). 1-144
mp: 177-178 °C
1h-NMR (CDCI3) 6ppm:1.27-1.39(m, 2H), 1.40(s, 9H), 1.65-1.79(m, 2H), 2.04-2.07(m, 2H), 2.12-2.34(m, 3H), 3.22(m, IH), 3.93(d, IH, J = 9.1Hz), 6.90-7.03(m, 3H), 7.25(m, IH), 7.77(dd, IH, J = 4.9, 1.7Hz), 7.81(brs, IH), 8.72(dd, IH, J= 7.8, 1.5Hz). 1-145
mp : >300 °C
1h-NMR (DMSO-d6) 6 ppm:1.30(s, 9H), 1.44-1.70(m, 4H), 2.05-2.19(m, 4H), 2.73(m, IH), 3.18(m, IH), 6.86(d, IH, J = 8.8Hz), 7.62(t, 2H, J = 8.5Hz), 7.86(t, 2H, J = 8.5Hz), 7.89(d, 2H, J = 8.5Hz), 8.16(d, 2H, J = 8.5Hz). 1-146 mp : 240-242 °C

*H-NMR (DMSO-d6) Sppm:1.26-1.53(m, 4H), 1.27(8, 9H), 1.74-1.83(m, 2H), 1.90-
1.97(m, 2H), 2.26(m, IH), 3.04(m, IH), 6.59(brs, IH), 6.74-6.79(m, 3H), 7.74(s, IH),
10.32(s, IH), 12.80(s, IH).
1-147
mp: 167-169 °C
1h-NMR (CDC13) 5 ppm: 1.05-1.28 (m, 2H), 1.38 (s, 9H), 1.47-1.70 (m, 2H), 1.80-2.00 (m,
3H), 2.13-2.25 (m, 2H), 2.75 (t, 2H, J = 6.9Hz), 3.24 (m, IH), 3.49 (dt, 2H, J = 6.3, 6.9Hz),
3.58 (d, IH, J = 8.7Hz), 3.87 (s, 6H), 5.40 (brs, IH), 6.71 (m, 2H), 6.82 (d, IH, J = 8.7Hz).
1-148
mp: 171-172 °C
1H-NMR (CDCI3) 5 ppm:l. 16-1.38 (m, 2H), 1.39 (s, 9H), 1.50-1.79 (m, 4H), 1.85-2.02 (m,
3H), 2.15-2.30 (m, 2H), 2.35-2.56 (m, 6H), 3.25 (m, IH), 3.33 (q, 2H, J = 6.0Hz), 3.63 (d, IH,
J = 9.0Hz), 3.72 (t, 4H, J = 4.6Hz), 6.77 (brs, IH).
1-149
1h-NMR (CDCI3) 5 ppm:1.20-1.36 (m, 2H), 1.28 (t, 3H, J = 7.2Hz), 1.39 (s, 9H), 1.45-
1.70 (m, 2H), 1.85-2.30 (m, 7H), 2.43 (s, 3H), 3.05-3.42 (m, 3H), 3.46-3.80 (m, 3H), 7.31 (d,
IH, J = 7.2Hz), 7.40-7.52 (m, 3H), 8.18 (brs, IH).
1-150
mp : 203-204 °C
1H-NMR (CDCI3) 6 ppm:1.15-1.37 (m, 2H), 1.39 (s, 9H), 1.42-1.70 (m, 2H), 1.85-2.29 (m,
5H), 2.76 (t, 2H, J = 6.0Hz), 3.26 (m, IH), 3.49 (q, 2H, J = 6.0Hz), 3.61 (m, IH), 4.03 (s,
2H), 5.88 (brs, IH), 7.15 (dd, IH, J = 7.0, 8.8Hz), 7.30-7.35 (m, 2H).
1-151
mp : 181-183 °C
1h-NMR (CDCI3) 6 ppm: 1.15-1.30 (m, 2H), 1.39 (s, 9H), 1.45-1.64 (m, 2H), 1.88-2.05 (m,
3H), 2.15-2.25 (m, 2H), 2.69 (t, 2H, J = 6.0Hz), 3.28 (m, IH), 3.47 (q, 2H, J = 6.0Hz), 3.58
(d, IH, J = 9.9Hz), 3.87 (s, 2H), 5.83 (brs, IH), 7.00 (m, IH), 7.20 (m, 2H).

1-152
mp : 222-224 °C
1h-NMR (CDCI3) 6ppm:1.16-1.37 (m, 2H), 1.39 (s, 9H), 1.49-1.70 (m, 2H), 1.90-2.25 (m, 5H), 3.26 (m, IH), 3.36 (t, 2H, J = 6.4Hz), 3.66 (dt, 3H, J = 6.0, 6.4Hz), 5.87 (t, IH, J = 6.0Hz), 7.58 (s, IH), 7.68 (dd, IH, J = 7.0, 8.5Hz), 7.83 (dd, IH, J = 7.0, 8.5Hz), 8.19 (t, 2H, J = 8.5Hz). 1-153
mp : 207-209 °C
1h-NMR (CDCI3) 6 ppm:1.05-1.25 (m, 2H), 1.38 (s, 9H), 1.40-2.03 (m, 10H), 2.05-2.25 (m, 2H), 2.58 (s, 3H), 2.76 (m, IH), 3.05-3.35 (m, 2H), 3.97 (d, IH, J = 9.5Hz), 4.94 (t, IH, J = 4.0Hz), 8.42 (d, IH, J = 5.5Hz), 8.97 (d, IH, J = 5.5Hz). 1-154
mp : 184-185 °C
1h-NMR (CDCI3) 6 ppm:1.05-1.25 (m, 2H), 1.37 (s, 9H), 1.50-1.69 (m, 2H), 1.85-2.05 (m, 3H), 2.10-2.21 (m, 2H), 3.24 (m, IH), 3.64 (m, IH), 4.87 (s, IH), 4.88 (s, IH), 5.67 (brs, IH), 7.42 (d, 2H, J = 5.5Hz), 7.52 (m, 2H), 7.78 (m, IH), 7.82 (m, IH), 7.95 (d, IH, J = 7.0Hz). 1-155
mp : 208-210 °C
1h-NMR (DMSO-d6) 6ppm:1.26 (s, 9H), 1.27-1.50 (m, 4H), 1.75-2.00 (m, 4H), 2.16 (m, IH), 2.81 (s, 3H), 3.02 (m, IH), 6.79 (d, IH, J = 8.5Hz), 10.00 (s, IH), 10.66 (s, IH). 1-156
mp : 256-257 °C
1h-NMR (CDCI3) 5 ppm:1.20-1.39 (m, 2H), 1.41 (s, 9H), 1.60-1.81 (m, 2H), 2.01-2.35 (m, 5H), 2.69 (t, 2H, J = 6.0Hz), 3.11 (t, 2H, J = 6.0Hz), 3.30 (m, IH), 3.61 (d, IH, J = 9.3Hz), 7.21 (d, IH, J = 8.0Hz), 7.31 (s, IH), 7.70 (d, IH, J = 8.0Hz), 7.99 (s, IH). 1-157

mp : 269-271 °C
1h-NMR (CDCI3) 5 ppm: 1.20-1.45 (m, 2H), 1.41 (s, 9H), 1.70-1.90 (m, 2H), 2.10-2.45 (m,
5H), 3.37 (m, IH), 3.68 (m, IH), 7.45 (dd, IH, J= 4.0, 8.0Hz), 7.53 (brs, IH), 7.72 (t, IH, J
= 8.0Hz), 7.83 (d, IH, J = 8.0Hz), 8.02 (d, IH, J = 8.0Hz), 8.18 (d, IH, J = 8.0Hz), 8.93 (d,
IH, J = 4.0Hz).
1-158
mp : 253-255 °C
1h-NMR (CDCI3) 5ppm:1.20-1.40 (m, 2H), 1.42 (s, 9H), 1.60-1.90 (m, 2H), 2.06-2.50 (m,
5H), 2.72 (s, 3H), 3.33 (m, IH), 3.78 (d, IH, J = 9.2Hz), 7.52 (t, IH, J = 7.0Hz), 7.62-7.80
(m, 2H), 7.94 (brs, IH), 8.05 (d, IH, J= 8.5Hz), 8.20 (s, IH).
1-159
mp : 253-255 °C
1h-NMR (CDCI3) 6 ppm: 1.20-1.39 (m, 2H), 1.40 (s, 9H), 1.60-1.80 (m, 2H), 1.98-2.30 (m,
5H), 2.71 (s, 3H), 3.31 (m, IH), 3.68 (d, IH, J = 9.0Hz), 7.41 (brs, IH), 7.61 (d, 2H, J =
9.0Hz), 7.70 (d, 2H, J = 9.0Hz).
1-160
mp: 211-212 °C
XH-NMR (CDCI3) 6 ppm:1.20-1.32 (m, 2H), 1.39 (t, 3H, J = 7.0Hz), 1.40 (s, 9H), 1.55-
1.79 (m, 2H), 1.98-2.35 (m, 5H), 3.31 (m, IH), 3.65 (d, IH, J = 9.5Hz), 4.03 (q, 2H, J =
7.0Hz), 6.64 (d, IH, J = 8.0Hz), 6.92 (d, IH, J = 8.0Hz), 7.10 (s, IH), 7.19 (t, IH, J = 8.0Hz),
7.30 (brs, IH).
1-161
mp : 202-203 °C
1h-NMR (CDCI3) 5 ppm:0.96 (t, IH, J = 7.3Hz), 1.29-1.39 (m, 2H), 1.40 (s, 9H), 1.41-
1.58 (m, 2H), 1.60-1.80 (m, 4H), 1.98-2.31 (m, 5H), 3.31 (m, IH), 3.66 (d, IH, J = 8.5Hz),
3.96 (t, 2H, J = 6.4Hz), 6.64 (d, IH, J = 8.0Hz), 6.90 (d, IH, J = 8.0Hz), 7.11 (s, IH), 7.19
(t, IH, J = 8.0Hz), 7.31 (brs, 11

1-162
mp: 177-180 °C
1h-NMR (CDCI3) 5 ppm:l. 18-1.38 (m, 2H), 1.39 (s, 9H), 1.59-1.78 (m, 2H), 1.95-2.05 (m,
2H), 2.07-2.25 (m, 3H), 3.26 (m, IH), 3.46 (s, 3H), 4.17 (d, IH, J = 9.5Hz), 5.15 (s, 2H), 6.77
(d, IH, J = 8.0Hz), 7.10-7.23 (m, 2H), 7.34 (s, IH), 7.58 (s, IH).
1-163
mp: 175-178 °C
1h-NMR (DMSO-d6) 5 ppm: 1.27 (s, 9H), 1.28-1.50 (m, 4H), 1.78-2.00 (m, 4H), 2.22 (m,
IH), 2.96-3.15 (m, 2H), 6.67 (m, IH), 6.79 (d, IH, J = 8.5Hz), 7.18 (m, 2H), 7.38 (s, IH),
9.81 (s, IH).
1-164
mp : 232-233 °C
*H-NMR (CDCI3) 6 ppm:0.97(t, 3H, J = 1.3Hz), 1.22-1.30(m, 2H), 1.40(s, 9H), 1.44-
1.51(m, 2H), 1.67-1.77(m, 4H), 2.02-2.24(m, 5H), 3.22(m, IH), 3.62(d, IH, J = 9.6Hz),
4.25(t, 2H, J= 6.8Hz), 6.71(d, IH, J = 8.4Hz), 7.01(brs, IH), 7.91(dd, IH, J = 8.4, 3.3Hz),
8.08(d, IH, J = 3.3Hz).
1-165
mp : 199-200 °C
1h-NMR (CDCI3) 6 ppm:0.96(t, 3H, J = 7.4Hz), 1.24-1.50(m, 4H), 1.40(s, 9H), 1.67-
1.76(m, 3H), 2.03-2.08(m, 2H), 2.24-2.35(m, 3H), 3.29(m, IH), 3.76(d, IH, J = 9.1Hz),
3.91(t, 2H, J = 6.6Hz), 6.41(dd, IH, J = 8.8, 2.5Hz), 6.55(d, IH, J = 2.5Hz), 6.82(d, IH, J =
8.8Hz), 7.43(8, IH), 8.95(s, IH).
1-166
mp : 215-218 °C
1h-NMR (CDCI3+CD3OD) 6 ppm:0.97(t, 3H, J = 7.4Hz), 1.24-1.40(m, 4H), 1.39(s, 9H),
1.42-1.50(m, 2H), 1.54-1.72(m, 2H), 1.76-1.82(m, 2H), 1.9l-2.00(m, 2H), 2.06-2.22(m, 3H),
3.24(m, IH), 4.00(t, 2H, J = 6.6Hz), 6.78(d, IH, J = 8.8Hz), 6.98(dd, IH, J = 8.8, 2.5Hz),

7.09(d, IH, J = 8.8Hz).
1-167
mp : 212-213 °C
:H-NMR (CDCI3) 5 ppm:0.96(t, 3H, J = 7.5Hz), 1.26-1.34(m, 2H), 1.40(s, 9H), 1.45-
1.50(m, 2H), 1.68-1.77(m, 4H), 2.03-2.08(m, 2H), 2.17(m, IH), 2.26-2.29(m, 2H), 3.29(m,
IH), 3.60(d, IH, J = 9.0Hz), 4.25(t, 2H, J = 6.8Hz), 6.71(d, IH, J = 8.4Hz), 7.01(brs, IH),
7.91(dd, IH, J = 8.4, 3.3Hz), 8.08(d, IH, J = 3.3Hz).
1-168
mp : 230-232 °C
1h-NMR (CDCI3) 6ppm:1.22-1.35(m, 2H), 1.40(s, 9H), 1.63-1.77(m, 2H), 2.03-2.08(m,
2H), 2.15-2.29(m, 3H), 3.31(m, IH), 3.63(d, IH, J = 9.3Hz), 6.89(d, IH, J = 9.4Hz),
7.10(brd, 2H, J = 7.4Hz), 7.12(brs, IH), 7.18(t, IH, J = 7.4Hz), 7.36(brt, 2H, J = 7.4Hz),
8.09-8.15(m, 2H).
1-169
mp: 159-160 °C
J-H-NMR (CDCI3) 6 ppm:0.97(t, 3H, J = 7.3), 1.20-1.35(m, 2H), 1.40(s, 9H), 1.37-1.49(m,
2H), 1.61-1.78(m, 4H), 2.05-2.08(m, 2H), 2.23-2.26(m, 2H), 2.36(s, 3H), 2.97(brs, IH),
3.32(m, IH), 3.86(brs, IH), 4.30(t, 2H, J = 6.5Hz), 6.25(s, IH), 7.92(brs, IH).
1-170
mp : 180-181 °C
XH-NMR (CDCI3) 6 ppm:0.88-0.89(m, 2H), 1.39(s, 9H), 1.42-1.60(m, 2H), 1.86-1.90(m,
2H), 2.04-2.09(m, 2H), 2.42(s, 3H), 2.91(m, IH), 3.20(m, IH), 3.63(d, IH, J = 9.2Hz), 6.38(s,
IH), 7.15(m, 2H), 7.28(m, IH), 7.45(m, 2H), 7.84(brs, IH).
1-171
mp : 173-174 °C
1h-NMR (CDCI3) 6 ppm:0.98(t, 3H, J = 7.5Hz), 1.29-1.40(m, 2H), 1.40(s, 9H), 1.55(m,
2H), 1.62-1.83(m, 4H), 2.09-2.12(m, 2H), 2.24-2.32(m, 3H), 3.32(m, IH), 3.63(d, IH, J =

9.5Hz), 3.99(t, 2H, J = 6.4Hz), 7.22(dd, IH, J = 9.4, 2.7Hz), 7.66(d, IH, J = 2.7Hz), 8.63(d,
IH, J = 9.4Hz), 10.17(8, IH).
1-172
mp : 238-242 °C
1h-NMR (CDCI3) 5 ppm;0.96(t, 3H, J = 7.3Hz), 1.23-1.52(m, 4H), 1.40(s, 9H), 1.61-
1.78(m, 4H), 2.05-2.28(m, 5H), 3.30(m, IH), 3.66(d, IH, J = 9.4Hz), 3.84(brs, 2H), 3.90(t,
2H, J = 6.4Hz), 6.32-6.35(m, 2H), 6.96(brs, IH), 6.97(d, IH, J = 9.4Hz).
1-173
mp : 165-166 °C
1h-NMR (CDCI3) 6ppm:1.23-1.26(m, 2H), 1.40(s, 9H), 1.67-1.72(m, 2H), 2.01-2.06(m,
2H), 2.11-2.28(m, 3H), 3.31(m, IH), 3.60(s, 2H), 3.69(s, 3H), 4.02(brs, IH), 7.01(d, IH, J =
8.0Hz), 7.25(t, IH, J = 8.0Hz), 7.43(d, IH, J = 8.0Hz), 7.49(brs, IH), 7.51(brs, IH).
1-174
mp : 264-265 °C
1h-NMR (CDCI3+CD3OD) 6ppm: 1.26-1.29(m, 2H), 1.39(s, 9H), 1.62-1.69(m, 2H),
1.96-2.00(m, 2H), 2.18-2.21(m, 3H), 3.25(m, IH), 3.58(s, 2H), 7.01(d, IH, J = 7.5Hz), 7.26(t,
IH, J = 7.5Hz), 7.42(brs, IH), 7.50(d, IH, J = 7.5Hz).
1-175
mp : 90-94 °C
^-NMR (CDCI3) 6ppm:1.16-1.23(m, 2H), 1.37(s, 9H), 1.44-1.56(m, 2H), 1.73-1.85(m,
3H), 2.11-2.15(m, 2H), 3.57(t, 2H, J = 6.4Hz), 3.21(m, IH), 3.58(m, 2H), 3.84(d, IH, J =
9.3Hz), 5.56(brs, IH), 7.01(s, IH), 7.11(t, IH, J = 7.5Hz), 7.21(t, IH, J = 7.5Hz), 7.38(d, IH,
J = 7.5Hz), 7.59(d, IH, J = 7.5Hz), 8.24(brs, IH).
1-176
mp : 116-118 °C
1h-NMR (CDCI3) 6ppm:1.18-1.38 (m, 2H), 1.40 (s, 9H), 1.60-1.79 (m, 2H), 1.95-2.30 (m,
5H), 3.30 (m, IH), 3.69 (m, IH), 3.80 (s, 3H), 4.64 (s, 2H), 6.67 (d, IH, J = 8.0Hz), 7.00 (d,

IH, J = 8.5Hz), 7.15-7.24 (m, 2H), 7.32 (brs, IH).
1-177
mp : 219-220 °C
1h-NMR (DMSO-d6) 5 ppm: 1.27 (s, 9H), 1.28-1.50 (m, 4H), 1.75-2.01 (m, 4H), 2.18-) 2.30 (m, IH), 2.95-3.15 (m, 2H), 4.61 (s, 2H), 6.56 (m, IH), 6.80 (d, IH, J = 8.5Hz), 7.16 (m,
2H), 7.28 (brs, IH), 9.87 (brs, IH). 1-178
mp : 170-173 °C
1h-NMR (CDC13) 6 ppm:l.18-1.39 (m, 2H), 1.40 (s, 9H), 1.50-1.80 (m, 2H), 1.90-2.33 (m, 1 5H), 2.36 (s, 6H), 2.75 (t, 2H, J = 5.5 Hz), 3.30 (m, IH), 3.70 (m, IH), 4.08 (t, 2H, J = 5.5Hz), 6.68 (d, IH, J = 8.0Hz), 6.94 (d, IH, J = 7.5Hz), 7.15-7.23 (m, 2H), 7.33 (brs, IH). 1-179
mp : 191-193 °C
1h-NMR (CDCI3) 6 ppm:1.20-1.39 (m, 2H), 1.40 (s, 9H), 1.58-1.80 (m, 2H), 1.98-2.32 (m, 5H), 3.30 (m, IH), 3.70 (d, IH, J = 9.5 Hz), 4.77 (s, 2H), 6.73 (d, IH, J = 8.0Hz), 7.04 (d, IH, J = 8.0Hz), 7.20-7.31 (m, 2H), 7.48 (brs, IH). 1-180
mp : 174-176 °C
1h-NMR (CDCI3) 5 ppm:1.10-1.30 (m, 2H), 1.40 (s, 9H), 1.45-1.65 (m, 2H), 1.81-2.02 (m, 3H), 2.15-2.30 (m, 2H), 2.58 (t, 2H, J = 6.5Hz), 3.25 (m, IH), 3.37 (dt, 2H, J = 5.5, 6.5Hz), 3.60 (d, IH, J = 9.5Hz), 3.71 (s, 2H), 5.73 (brs, IH), 7.20-7.40 (m, 5H). 1-181
mp: 176-178 °C
1h-NMR (CDCI3) 6ppm:1.15-1.30 (m, 2H), 1.39 (s, 9H), 1.45-1.70 (m, 6H), 1.85-2.01 (m, 3H), 2.15-2.28 (m, 2H), 2.63 (t, 2H, J = 7.0Hz), 3.25 (dt, 2H, J = 6.0, 7.0Hz), 3.27 (m, IH), 3.63 (m, IH), 5.35 (brs, IH), 7.17 (m, 3H), 7.29 (m, 2H). 1-182

mp: 152-154 °C
1h-NMR (CDCI3) 6 ppm:1.15-1.30 (m, 2H), 1.39 (s, 9H), 1.45-1.65 (m, 2H), 1.85-2.05 (m,
3H), 2.09-2.25 (m, 2H), 3.25 (m, IH), 3.45 (dt, 2H, J = 5.0, 5.0Hz), 3.55 (t, 2H, J = 5.0Hz),
3.60 (m, IH), 4.51 (s, 2H), 5.81 (brs, IH), 7.29-7.40 (m, 5H).
1-183
mp : 208-211 °C
1h-NMR (CDCI3) 6ppm:1.20-1.31(m, 2H), 1.39(s, 9H), 1.62-1.68(m, 2H), 1.98-2.25(m,
5H), 3.30(m, IH), 3.57(d, IH, J = 9.2Hz), 4.59(d, 2H , J = 5.8Hz), 5.76(brs, IH), 7.37(dd,
IH, J = 8.4, 2.0Hz), 7.46-7.52(m, 2H), 7.69(brs, IH), 7.78-7.83(m, 3H).
1-184
mp: 180-182 °C
1h-NMR (CDCI3) 6ppm:1.22-1.37(m, 2H), 1.40(s, 9H), 1.60-1.69(m, 2H), 2.05-2.09(m, 2H), 2.21-2.27(m, 3H), 3.45(m, IH), 3.64(d, IH, J = 9.6Hz), 4.77(d, 2H, J = 4.9Hz), 7.43(d,
IH, J = 8.6Hz), 7.46(brs, IH), 7.61(t, IH, J=7.7Hz), 7.73(t, IH, J= 7.7Hz), 7.87(t, IH, J =
7.7Hz), 8.20(t, IH, J = 7.7Hz), 8.24(d, IH, J = 8.6Hz).
1-185
mp : 260-261 °C
1h-NMR (CDCI3) 5ppm:1.22-1.32(m, 2H), 1.39(s, 9H), 1.60-1.70(m, 2H), 1.97-2.01(m,
2H), 2.11(m, IH), 2.21-2.24(m, 2H), 3.30(m, IH), 3.61(d, IH, J = 9.3Hz),4.95(d, 2H, J =
6.0Hz), 5.85(brs, IH), 7.33(d, IH, J=4.8Hz), 7.62(dd, IH, J = 8.4, 6.9Hz), 7.75(dd, IH, J =
8.1, 6.9Hz), 8.00(d, IH, J = 8.1Hz), 8.20(d, IH, J = 8.4Hz), 8.42(d, IH, J = 4.8Hz).
1-186
mp : 231-233 °C
1h-NMR (CDCI3) 6ppm:1.23-1.40(m, 2H), 1.40(s, 9H), 1.62-1.76(m, 2H), 2.04-2.10(m,
2H), 2.22-2.32(m, 3H), 3.30(m, IH), 3.95(d, IH, J = 9.3Hz), 5.04(d, 2H, J = 4.1Hz), 7.61(d,
IH, J = 5.8Hz), 7.63(brs, IH), 7.65(dd, IH, J = 8.2, 6.9Hz), 7.73(dd, IH, J = 8.5, 6.9Hz),
7.86(d, IH, J = 8.2Hz), 8.10(d, IH, J = 8.5Hz), 8.42(d, IH, J = 5.8Hz).

1-187
mp: 184-187 °C
1h-NMR (CDCI3) 6 ppm:0.97(t, 3H, J = 7.3 Hz), 1.18-1.30(m, 2H), 1.39(s, 9H), 1.42-
1.65(m, 4H), 1.70-1.80(m, 2H), 1.94-2.08(m, 3H), 2.18-2.26(m, 2H), 3.29(m, IH), 3.61(d,
IH, J = 9.5Hz), 3.93(t, 2H, J = 6.4Hz), 4.39(d, 2H, J = 5.5Hz), 5.67(brs, IH), 6.79-6.83(m,
3H), 7.23(t, IH, J=7.6Hz).
1-188
mp : 224-226 °C
1h-NMR (CDCI3) 5ppm:.16-1.31(m, 2H), 1.38(s, 9H), 1.55-1.70(m, 2H), 1.92-2.07(m,
3H), 2.17-2.23(m, 2H), 3.21(m, IH), 3.81(s, 3H), 3.83(s, 6H), 4.06(d, IH, J = 9.8Hz), 4.34(d,
2H, J = 5.8Hz), 5.96(brs, IH), 6.47(s, 2H).
1-189
mp : 217-218 °C
1h-NMR (CDCI3) 6ppm:1.15-1.30(m, 2H), 1.37(s, 9H), 1.52-1.66(m, 2H), 1.90-2.06(m,
3H), 2.13-2.20(m, 2H), 2.93(s, 6H), 3.24(m, IH), 3.94(d, IH, J = 9.5Hz), 4.30(d, 2H, J =
5.5Hz), 5.73(brs, IH), 6.69(d, 2H, J = 8.9Hz), 7.12(d, 2H, J = 8.9Hz).
1-190
mp : amorphous solid
1h-NMR (CDCI3) 6ppm:1.17-1.32(m, 2H), 1.39(s, 9H), 1.54-1.72(m, 2H), 1.96-2.13(m,
3H), 2.18-2.27(m, 2H), 3.30(m, IH), 3.63(d, IH, J = 9.2Hz), 4.51(d, 2H, J = 5.8Hz), 5.82(brs,
IH), 7.40(d, 2H, J = 8.5Hz), 8.02(d, 2H, J = 8.5Hz), 8.64(s, IH).
1-191
mp : 126-128 °C
1h-NMR (CDCI3) 6ppm:0.97(t, 3H, J = 7.4 Hz), 1.10-1.28(m, 2H), 1.36(s, 9H), 1.42-
1.86(m, 9H), 2.06-2.18(111, 2H), 3.22(m, IH), 3.95(t, 2H, J = 4.5Hz), 4.16(brs, IH), 4.85(s,
2H), 6.82-6.95(m, 3H), 7.26(t, IH, J = 7.8Hz), 8.54(brs, IH).
1-192

mp : 178-181 °C
1h-NMR (CDCI3) 5 ppm:0.96(t, 3H, J = 7.3 Hz), 1.18-1.52(m, 4H), 1.39(s, 9H), 1.58-
1.76(m, 4H), 1.92-2.00(m, 2H), 2.02-2.29(m, 3H), 3.28(m, IH), 3.78(d, IH, J = 9.5Hz),
3.89(t, 2H, J = 6.6Hz), 6.00(bra, IH), 6.78(s, 4H), 7.35(brs, IH).
1-193
mp : 187-188 °C
1h-NMR (CDCI3+CD3OD) 5ppm:1.2l-1.40(m, 2H), 1.38(s, 9H), 1.52-1.69(m, 2H), 1.90-
2.00(m, 2H), 2.02-2.20(m, 3H), 3.22(m, IH), 3.75(s, 3H), 6.79(s, 4H).
1-194
mp : 251-253 °C
1h-NMR (DMSO-d6) 6ppm:1.27(s, 9H), 1.24-1.50(m, 4H), 1.72-1.83(m, 2H), 1.91-
1.99(m, 2H), 2.16(m, IH), 3.02(m, IH), 3.82(s, 3H), 6.79(d, IH, J = 8.2Hz), 7.01(d, 2H, J =
8.8Hz), 7.85(d, 2H, J = 8.8Hz), 9.72(brs, IH), 8.64(brs, IH).
1-195
mp : 183-185 °C
1h-NMR (CDCI3) Sppm:1.22-1.37(m, 2H), 1.40(s, 9H), 1.58-1.75(m, 2H), 2.05-2.10(m,
2H), 2.20-2.30(m, 3H), 3.32(m, IH), 3.70(s, 2H), 3.73(s, 3H), 6.79(s, IH), 8.83(brs, IH).
1-196
mp : 185-187 °C
1h-NMR (CDCI3) 6 ppm:1.20-1.39 (m, 2H), 1.40 (s, 9H), 1.44 (t, 6H, J = 7.0 Hz), 1.60-
1.80 (m, 2H), 1.95-2.35 (m, 5H), 3.30 (m, IH), 3.62 (d, IH, J = 8.9 Hz), 4.06 (q, 2H, J = 7.0
Hz), 4.09 (q, 2H, J = 7.0 Hz), 6.08 (s, IH), 7.02 (s, IH), 7.36 (s, IH).
1-197
mp : 211-213 °C
1h-NMR (CDCI3) 5 ppm:1.20-1.40 (m, 2H), 1.41 (s, 9H), 1.60-1.80 (m, 2H), 2.00-2.36 (m,
5H), 2.61 (s, 3H), 3.32 (m, IH), 3.64 (d, IH, J = 9.2 Hz), 7.28 (s, IH), 7.43 (t, IH, J= 7.5
Hz), 7.69 (d, IH, J = 7.5 Hz), 7.85 (d, IH, J = 7.5 Hz), 8.02 (s, IH).

1-198
mp : 268-269 °C
1h-NMR (CDCI3) 6ppm:1.20-1.39 (m, 2H), 1.40 (s, 9H), 1.42-2.32 (m, 7H), 2.90-3.10 (m,
4H), 3.30 (m, IH), 3.68 (d, IH, J = 8.8 Hz), 6.59 (s, IH), 7.18 (d, IH, J = 8.7 Hz), 7.59 (d,
IH, J = 8.7 Hz), 7.77 (brs, IH).
1-199 mp : 221-224 °C
1-200 mp : 237-240 °C
1-201 mp : 87-90 °C
1-202 mp : 222-223°C
1-203 mp : 255-257 °C
1-204 mp : 234-236 °C
1-205 mp : 208-210 °C
1-206 mp : 217-218 °C
1-207 mp : 275-279 °C
1-208 mp : 248-250 °C
1-209 mp : 256-258 °C
1-210 mp: 270-271 °C
1-211 mp : 219-220 °C
1-212 mp : 260-261 °C
1-213 mp : >300 °C
1-214 mp : 206-207 °C
1h-NMR (CDCI3) 6 ppm: 0.93(t, 3H, J = 7.4 Hz), 1.30-1.42(m, 2H), 1.49(d, 6H, J = 6.9
Hz), 1.53-1.65(m, 2H), 2.61(t, 2H, J = 7.7 Hz), 4.15(sept, IH, J = 6.9 Hz), 7.04(d, IH, J =
8.2 Hz), 7.20(d, 2H, J = 8.2 Hz), 7.51(d, 2H, J = 8.2 Hz), 7.89(d, IH, J = 8.8 Hz), 8.18(s, IH),
10.55(s, IH).
1-215
1h-NMR (CDCI3) 5 ppm:0.93(t, 3H, J = 7.3Hz), 1.30-1.41(m, 2H), 1.52-1.63(m, 2H),

1.95(8, 6H), 2.61(t, 2H, J = 7.8Hz), 6.99(brs, IH), 7.20(d, 2H, J = 8.5Hz), 7.65(d, 2H, J =
8.5Hz), 7.93(dd, IH, J = 8.5, 2.5Hz), 8.28(d, IH, J = 8.5Hz), 8.55(d, IH, J = 2.5Hz),
9.76(brs, IH).
Ia-1
mp 221-224 °C
1h-NMR (CDC13) 6ppm: 1.19-1.38 (m, 2H), 1.40 (s, 9H), 1.62-1.77 (m, 2H), 2.00-2.31 (m,
5H), 3.18 (t, 4H, J = 4.8 Hz), 3.21-3.38 (m, IH), 3.85 (t, 4H, J = 4.8 Hz), 6.64-6.32 (m, 2H),
7.11 (s, IH), 7.20 (t, IH, J = 7.8 Hz), 7.45 (s, IH).
Ia-3
mp 87-90 °C
1h-NMR (CDCI3) 5 ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.37 (d, 6H, J = 6.9 Hz), 1.59-1.70 (m,
2H), 1.76-1.88 (m, 2H), 2.32-2.42 (m, 4H), 3.11-3.23 (m, 3H), 3.39 (d, 2H, J = 10.8 Hz),
3.74-3.86 (m, 2H), 4.34 (t, IH, J = 9.0 Hz), 6.86 (d, 2H, J = 9.0 Hz), 7.30 (s, IH), 7.40 (d, 2H,
J = 9.0 Hz).
Ia-4
mp 233-234 °C
1h-NMR (CDCI3) 5 ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.40 (s, 9H), 1.26-1.37 (m, 2H), 1.62-
1.78 (m, 2H), 2.00-2.22 (m, 5H), 2.42 (t, 2H, J = 11.7 Hz), 3.20-3.40 (m, IH), 3.46 (d, 2H, J
= 10.5 Hz), 3.67 (d, IH, J = 9.3 Hz), 3.72-3.84 (m, 2H), 6.62-6.76 (m, 2H), 7.10 (s, IH), 7.18
(t, IH, J = 7.8 Hz), 7.42 (s, IH).
Ia-5
mp 125-126 °C
1H-NMR (CDCI3) 6 ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.40 (s, 9H), 1.59-1.70 (m, 2H), 1.77-
1.84 (m, 2H), 2.30-2.46 (m, 4H), 3.24 (q, 2H, J = 6.6 Hz), 3.38 (d, 2H, J = 11.7 Hz), 3.74-
3.88 (m, 2H), 4.08 (t, IH, J = 5.7 Hz), 6.87 (d, 2H, J = 8.7 Hz), 7.30 (s, IH), 7.41 (d, 2H, J =
8.7 Hz).
Ia-6

mp 229-230 °C
1h-NMR (CDCI3) 5 ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.26-1.34 (m, 2H), 1.39 (d, 6H, J = 6.9
Hz), 1.61-1.77 (m, 2H), 1.98-1.26 (m, 5H), 2.32-2.46 (m, 2H), 3.15 (quintet, IH, J = 6.6 Hz),
3.22-3.35 (m, IH), 3.39 (d, 2H, J= 11.4 Hz), 3.74-3.92 (m, 2H), 3.88 (d, IH, J = 8.4 Hz),
6.96-6.71 (m, 2H), 7.05 (brs, IH), 7.39 (d, 2H, J = 9.3 Hz).
Ia-7
mp 253-254 °C
1h-NMR (DMSO) 5 ppm: 1.24-1.60 (m, 4H), 1.27 (s, 9H), 1.77-2.07 (m, 4H), 2.16-2.34 (m,
IH), 2.97-3.15 (m, IH), 6.78 (d, IH, J = 7.2 Hz), 7.01 (t, IH, J = 6.0 Hz), 7.27 (t, 2H, J = 6.6
Hz), 7.58 (d, 2H, J = 7.5 Hz), 9.78 (s, IH).
Ia-8
mp 257-258 °C
1h-NMR (DMSO) 5 ppm: 1.22-1.54 (m, 4H), 1.27 (s, 9H), 1.77-1.88 (m, 2H), 1.88-2.00 (m,
2H), 2.16-2.34 (m, IH), 2.23 (s, 3H), 2.92-3.14 (m, IH), 6.77 (d, IH, J = 8.4 Hz), 7.07 (d, 2H,
J = 8.4 Hz), 7.46 (d, 2H, J = 8.1 Hz), 9.68 (s, IH).
Ia-9
mp 231-232 °C
1h-NMR (CDCI3) 6 ppm: 1.21 (t, 3H, J = 7.5 Hz), 1.22-1.38 (m, 2H), 1.40 (s, 9H), 1.62-
1.78 (m, 2H), 1.98-2.31 (m, 5H), 2.61 (q, 2H, J = 7.5 Hz), 3.24-3.38 (m, IH), 3.70 (d, IH, J =
9.9 Hz), 7.11 (s, IH), 7.14 (d, 2H, J = 8.7 Hz), 7.40 (d, 2H, J = 8.7 Hz).
Ia-10
mp 233-234 °C
1h-NMR (CDCI3) 5 ppm: 0.96 (t, 3H, J = 7.2 Hz), 1.20-1.37 (m, 2H), 1.40 (s, 9H), 1.56-
1.78 (m, 4H), 1.98-2.32 (m, 5H), 2.54 (t, 2H, J= 7.2 Hz), 3.23-3.39 (m, IH), 3.66 (d, IH, J =
9.6 Hz), 7.08 (s, IH), 7.12 (d, 2H, J = 8.4 Hz), 7.39 (d, 2H, J = 8.4 Hz).
Ia-11
mp 243-244 °C

1h-NMR (CDC13) 5 ppm: 1.22 (d, 6H, J = 6.9), 1.22-1.77 (m, 4H), 1.40 (s, 9H), 2.01-2.30
(m, 5H), 2.83-2.92 (m, IH), 3.24-3.40 (m, IH), 3.66-3.69 (m, IH), 7.09 (s, IH), 7.17 (d, 2H,
J = 8.4 Hz), 7.41 (d, 2H, J = 8.1 Hz).
Ia-12
mp 246-247 °C
1h-NMR (CDC13) 6 ppm: 0.80 (t, 3H, J = 7.5), 1.20 (d, 3H, J = 7.2), 1.26-1.77 (m, 6H),
1.40 (s, 9H), 2.01-2.27 (m, 5H), 2.51-2.60 (m, IH), 3.20-3.38 (m, IH), 3.64-3.69 (m, IH),
7.08 (s, IH), 7.12 (d, 2H, J = 8.4 Hz), 7.41 (d, 2H, J = 8.4 Hz).
Ia-13
mp 278-279 °C
1h-NMR (CDC13) 6 ppm: 1.22-1.52 (m, 4H), 1.29 (s, 9H), 1.40 (s, 9H), 1.61-1.77 (m, 2H),
2.02-2.30 (m, 5H), 3.20-3.38 (m, IH), 3.66-3.69 (m, IH), 7.10 (s, IH), 7.33 (d, 2H, J = 9.0
Hz), 7.42 (d, 2H, J = 8.7 Hz).
Ia-14
mp 263-264 °C
1h-NMR (DMSO) 6 ppm: 1.24-1.51 (m, 4H), 1.27 (s, 9H), 1.82-1.99 (m, 4H), 2.19-2.28 (m,
IH), 2.98-3.12 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.33 (d, 2H, J = 8.7 Hz), 7.61 (d, 2H, J =
9.0 Hz), 9.94 (s, IH).
Ia-15
mp 209-210 °C
1h-NMR (CDC13) 6 ppm: 1.25 (d, 6H, J = 6.3 Hz), 1.40 (s, 9H), 1.70-1.98 (m, 8H), 2.19-
2.38 (m, 3H), 3.39 (d, 2H, J= 11.7 Hz), 3.58-3.92 (m, 3H), 4.12-4.26 (m, IH), 6.82-6.96 (m,
2H), 7.10 (br, IH), 7.41 (d, 2H, J = 8.1 Hz).
Ia-16
mp 238-240 °C
1h-NMR (DMSO) 5 ppm: 1.22-1.52 (m, 4H), 1.27 (a, 9H), 1.81-1.84 (m, 2H), 1.93-1.97 (m,
2H), 2.16-2.23 (m, IH), 2.95-3.12 (m, IH), 3.70 (s, 3H), 6.77 (d, IH, J = 8.4 Hz), 6.85 (d, 2H,

J = 9.0 Hz), 7.48 (d, 2H, J = 9.3 Hz), 9.64 (s, IH).
Ia-17
mp 245-246 °C
1h-NMR (DMSO) Sppm: 1.22-1.52 (m, 4H), 1.27 (s, 9H), 1.83-1.87 (m, 2H), 1.94-1.99 (m,
2H), 2.20-2.28 (m, IH), 2.98-3.12 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.28 (d, 2H, J = 8.7 Hz),
7.69 (d, 2H, J = 9.0 Hz), 9.64 (s, IH).
Ia-18
mp 240-241 °C
*H-NMR (CDC13) 6 ppm: 1.22-1.78 (m, 4H), 1.40 (s, 9H), 2.05-2.33 (m, 5H), 3.22-3.44 (m,
IH), 3.64-3.67 (m, IH), 6.61 (s, IH), 6.69-6.77 (m, 2H).
Ia-19
mp 240-241 °C
XH-NMR (CDC13) 6 ppm: 1.24-1.77 (m, 4H), 1.40 (s, 9H), 2.05-2.30 (m, 5H), 3.22-3.38 (m,
IH), 3.70-3.74 (m, IH), 7.00-7.15 (m, 3H), 7.36 (s, IH), 8.29-8.34 (m, IH).
Ia-20
mp 239-240 °C
1h-NMR (CDC13) 6 ppm: 1.24-1.78 (m, 4H), 1.40 (s, 9H), 2.02-2.30 (m, 5H), 3.22-3.40 (m,
IH), 3.63-3.66 (m, IH), 6.89-6.84 (m, IH), 7.10-7.17 (m, 2H), 7.22-7.34 (m, IH), 7.48-7.51
(m, IH).
Ia-21
mp 259-260 °C
1h-NMR (CDCI3/DMSO) 6 ppm: 1,21 (d, 6H, J = 6.0 Hz), 1.22-1.44 (m, 2H), 1.40 (s, 9H),
1.60-1.78 (m, 2H), 1.87-2.03 (m, 2H), 2.08-2.29 (m, 3H), 2.39 (t, 2H, J = 10.2 Hz), 3.14-3.32
(m, IH), 3.19 (d, 2H, J = 11.4 Hz), 3.77-3.93 (m, 2H), 5.33 (d, IH, J = 9.0 Hz), 6.84 (dd, IH,
JFH, HH = 8.1, 8.1 Hz), 7.20 (d, IH, J = 7.8 Hz), 7.49 (d, IH, JFH = 14.7 Hz), 8.86 (s, IH).
Ia-22
mp 234-235 °C

1h-NMR (CDCI3) 5ppm: 1,20 (d, 6H, J = 5.7 Hz), 1.22-1.44 (m, 2H), 1.38 (s, 9H), 1.54-
1.76 (m, 2H), 1.94-2.32 (m, 5H), 2.27 (s, 3H), 2.39 (t, 2H, J= 10.8 Hz), 2.87 (d, 2H, J= 11.4
Hz), 3.20-3.40 (m, 1H), 3.76-3.92 (m, 2H), 3.91 (d, 1H, J = 9.3 Hz), 6.93 (d, 1H, J = 8.1 Hz),
7.21 (brs, 1H), 7.27 (bra, 1H), 7.36 (brs, 1H).
Ia-23
mp 195-196 °C
1h-NMR (CDCI3) 6ppm: 1.20-1.44 (m, 4H), 1.41 (s, 9H), 1.59-1.76 (m, 2H), 2.03-2.14 (m,
2H), 2.15-2.33 (m, 3H), 3.20-3.40 (m, 1H), 3.64 (s, 1H, J = 9.0 Hz), 7.19-7.24 (m, 1H), 7.44
(brs, 1H), 7.52-7.63 (m, 2H), 8.17 (d, 1H, J = 8.7 Hz).
Ia-24
mp 209-210 °C
2H-NMR (CDCI3) Sppm: 1.22-1.39 (m, 2H), 1.56 (s, 9H), 1.61-1.78 (m, 2H), 2.00-2.12 (m,
2H), 2.17-2.33 (m, 3H), 3.24-3.39 (m, 1H), 3.67 (d, 1H, J = 9.6 Hz), 6.90-7.01 (m, 1H), 7.21
(s, 1H), 7.95-8.06 (m, 1H).
Ia-25
mp 278-281 °C
1h-NMR (DMSO-d6) 5 ppm: 1.10 (d, 6H, J = 6.3 Hz), 1.27 (s, 9H), 1.28-1.55 (m, 4H),
1.78-2.00 (m, 4H), 2.11-2.26 (m, 1H), 2.31 (t, 2H, J = 11.1 Hz), 3.00-3.10 (m, 1H), 3.08 (d,
1H, J = 10.8 Hz), 3.67-3.80 (m, 2H), 6.78 (d, 1H, J = 8.7 Hz), 7.08 (d, 1H, J = 9.0 Hz), 7.41
(dd, 1H, J = 2.4, 8.7 Hz), 7.78 (d, 1H, J = 8.7 Hz), 9.85 (s, 1H).
Ia-26
mp 253-255 °C
1h-NMR (DMSO-d6) Sppm: 1.13 (d, 6H, J = 6.0 Hz), 1.27 (s, 9H), 1.28-1.52 (m, 4H),
1.78-2.00 (m, 4H), 2.21 (t, 2H, J = 11.1 Hz), 2.26-2.36 (m, 1H), 2.96-3.10 (m, 1H), 3.56 (d,
1H, J= 12.3 Hz), 3.60-3.72 (m, 2H), 6.66-6.84 (m, 4H), 7.47 (t, 1H, J = 9.3 Hz), 9.28 (s,
1H).
Ia-27
mp 223-226 °C
1h-NMR (DMSO-d6) 6 ppm: 1.09 (d, 6H, J = 6.3 Hz), 1.27 (s, 9H), 1.28-1.54 (m, 4H),
1.77-2.01 (m, 4H), 2.32 (t, 2H, J = 11.1 Hz), 2.32-2.42 (m, 1H), 2.90 (d, 1H, J = 11.4 Hz),
2.96-3.12 (m, 1H), 3.76-3.92 (m, 2H), 6.78-6.98 (m, 3H), 7.68 (dd, 1H, J = 3.3, 8.7 Hz), 8.84
(s, 1H).
Ia-28
mp 237-238 °C
1h-NMR (CDCI3) 8 ppm: 1.22-1.44 (m, 2H), 1,25 (d, 6H, J = 6.3 Hz), 1.40 (s, 9H), 1.61-
1.79 (m, 2H), 2.05-2.32 (m, 5H), 2.21 (s, 3H), 2.38 (t, 2H, J= 10.2 Hz), 3.22-3.42 (m, 1H),
3.40 (d, 2H, J = 11.1 Hz), 3.65 (d, 1H, J = 9.3 Hz), 3.72-3.90 (m, 2H), 6.70-6.78 (m, 2H),
6.81 (brs, 1H), 7.50 (d, 1H, J = 9.6 Hz).
Ia-29
mp 208-209 °C
1h-NMR (CDCI3) 6 ppm: 1.22 (d, 6H, J = 6.0 Hz), 1.23-1.40 (m, 2H), 1.40 (s, 9H), 1.60-
1.78 (m, 2H), 2.00-2.16 (m, 2H), 2.14-2.33 (m, 3H), 2.45 (t, 2H, J = 11.1 Hz), 3.21 (d, 2H, J
= 10.8 Hz), 3.24-3.38 (m, 1H), 3.63 (d, 1H, J = 9.3 Hz), 3.80-3.94 (m, 2H), 5.33 (d, 1H, J =
9.0 Hz), 6.66 (dd, 1H, JFH, HH = 6.6, 6.6 Hz), 7.16 (brs, 1H), 7.89 (dd, 1H, JFH, HH = 9.0,
9.0 Hz).
Ia-30
mp 284-287 °C
1h-NMR (DMSO-d6) 6 ppm: 1.08 (d, 6H, J = 6.0 Hz), 1.26 (s, 9H), 1.28-1.53 (m, 4H),
1.82-2.22 (m, 4H), 2.25-2.39 (m, 1H), 2.78 (t, 2H, J = 10.5 Hz), 2.97-3.14 (m, 1H), 3.18 (d,
2H, J = 11.4 Hz), 3.65-3.76 (m, 2H), 6.79 (d, 1H, J = 8.7 Hz), 9.75 (s, 1H).
Ia-31
mp 200-201 °C
1h-NMR (CDC13) 6 ppm: 1.22-1.40 (m, 2H), 1.40 (s, 9H), 1.62-1.76 (m, 2H), 2.04-2.32 (m,
5H), 3.22-3.40 (m, 1H), 3.62-3.66 (m, 1H), 7.22-7.24 (m, 1H), 7.38-7.38 (m, 1H), 7.60 (s,

IH), 8.33-8.36 (m, IH).
Ia-32
mp 260-261 °C
1h-NMR (CDCI3/DMSO) 6 ppm: 1.25-1.42 (m, 2H), 1.38 (s, 9H), 1.64 (q, 2H, J = 13.5
Hz), 1.95 (d, 2H, J= 12.3 Hz), 2.16 (d, 2H, J = 10.5 Hz), 2.18-2.32 (m, IH), 3.14-3.30 (m,
IH), 5.53 (d, IH, J = 9.0 Hz), 7.31 (d, IH, J = 8.7 Hz), 7.46 (dd, IH, J = 2.4, 8.7 Hz), 7.90 (d,
IH, J = 2.1 Hz), 9.35 (s, IH).
Ia-33
mp 227 °C
1h-NMR (DMSO-d6) 5 ppm: 1.27 (s, 9H), 1.30-1.56 (m, 4H), 1.78-2.01 (m, 2H), 2.12-2.36
(m, 2H), 2.96-3.13 (m, IH), 3.70 (s, 3H), 3.71 (s, 3H), 6.77 (d, IH, J = 8.7 Hz), 6.85 (d, IH, J
= 8.7 Hz), 7.06 (dd, IH, J = 2.4, 8.7 Hz), 7.33 (d, IH, J = 2.4 Hz), 9.65 (s, IH).
Ia-35
mp 214-216 °C
1h-NMR (CDCI3) 6 ppm: 1.23-1.38 (m, 2H), 1.40 (s, 9H), 1.60-1.76 (m, 2H), 2.00-2.12 (m,
2H), 2.20-2.32 (m, 3H), 3.24-3.39 (m, IH), 3.68 (d, IH, J = 9.0 Hz), 6.77 (d, IH, J = 8.7 Hz),
7.00 (dd, IH, J = 2.4, 8.7 Hz), 7.77 (s, IH), 8.45 (d, IH, J = 2.4 Hz).
Ia-36
mp 241-242 °C
XH-NMR (CDCI3/DMSO) 6 ppm: 1.25-1.42 (m, 2H), 1.37 (a, 9H), 1.62 (q, 2H, J = 11.7
Hz), 1.93 (d, 2H, J = 12.0 Hz), 2.12 (d, 2H, J = 10.8 Hz), 2.16-2.30 (m, IH), 3.12-3.28 (m,
IH), 3.84 (s, 3H), 6.07 (d, IH, J = 8.4 Hz), 6.89 (dd, IH, JFH, HH = 9.3, 9.3 Hz), 7.24 (d,
IH, J = 8.7 Hz), 7.55 (d, IH, JFH = 13.5 Hz), 9.32 (s, IH).
Ia-37
mp 248-249 °C
1h-NMR (CDC13) 6 ppm: 0.60-0.73 (m, IH), 0.91 (d, 6H, J = 6.6), 1.12-1.40 (m, 2H), 1.40
(s, 9H), 1.54-1.88 (m, 5H), 1.98-2.29 (m, 7H), 3.22-3.37 (m, IH), 3.51-3.54 (m, 2H), 3.72 (d,

IH, J = 9.6), 6.88 (d, IH, J = 8.7), 7.06 (s, IH), 7.35 (d, IH, J = 9.0).
Ia-38
mp 237-238 °C
1h-NMR (CDC13) 6 ppm: 1.01 (d, 6H, J = 6.6), 1.20-1.40 (m, 2H), 1.40 (s, 9H), 1.60-1.74
(m, 4H), 1.99-2.28 (m, 7H), 2.69-2.82 (m, 2H), 3.02-3.14 (m, 2H), 3.20-3.38 (m, IH), 3.80-
3.90 (m, IH), 6.83-6.86 (m, 2H), 7.14 (s, IH), 7.34 (d, IH, J = 8.4).
Ia-39
mp 234-235 °C
2H-NMR (CDC13) 5 ppm: 1.20-1.36 (m, 2H), 1.40 (s, 9H), 1.60-1.77 (m, 2H), 1.90-2.32 (m,
5H), 3.21-3.39 (m, IH), 3.65 (d, IH, J = 9.6 Hz), 6.87 (d, IH, J = 8.7 Hz), 7.04 (s, IH), 7.37
(dd, IH, J = 2.7, 8.7 Hz), 7.56 (d, IH, J = 2.7 Hz).
Ia-40
mp 257-258 °C
*H-NMR (DMSO-d6) 6 ppm: 1.14 (d, 6H, J = 6.0 Hz), 1.27 (s, 9H), 1.28-1.53 (m, 4H),
1.78-2.00 (m, 4H), 2.13-2.256 (m, IH), 2.30 (t, 2H, J = 11.7 Hz), 2.97-3.12 (m, IH), 3.53-
3.67 (m, 2H), 4.01 (d, IH, J = 12.3 Hz), 6.80 (dd, IH, J = 3.0, 9.0 Hz), 7.79 (d, IH, J = 9.0
Hz), 8.27 (s, IH), 9.66 (s, IH).
Ia-41
mp 245-246 °C
1h-NMR (CDCI3/DMSO) 5 ppm: 1.25-1.42 (m, 2H), 1.37 (s, 9H), 1.62 (q, 2H, J = 12.6
Hz), 1.94 (d, 2H, J= 11.1 Hz), 2.13 (d, 2H, J= 11.1 Hz), 2.18-2.35 (m, IH), 3.11-3.29 (m,
IH), 6.07 (d, IH, J = 8.1 Hz), 6.95-7.06 (m, IH), 7.14-7.27 (m, IH), 7.44 (d, IH, J = 7.2 Hz),
7.79 (s, IH), 9.48 (s, IH).
Ia-43
mp 294-295 °C
1h-NMR (DMSO-d6) 5 ppm: 1.26 (s, 9H), 1.28-1.53 (m, 4H), 1.76-1.87 (m, 2H), 1.89-2.00
(m, 2H), 2.13-2.25 (m, IH), 2.96-3.10 (m, 5H), 3.52-3.60 (m, 4H), 6.78 (d, IH, J = 9.0 Hz),

6.88 (d, 2H, J = 9.0 Hz), 7.44 (d, 2H, J = 9.0 Hz), 9.59 (s, IH).
Ia-44
mp 250-252 °C
1h-NMR (CDC13) 5 ppm: 1.13 (d, 6H, J = 6.3 Hz), 1.21-1.38 (m, 2H), 1.41 (s, 9H), 1.63-
1.80 (m, 2H), 1.93 (t, 2H, J = 10.8 Hz), 2.00-2.10 (m, 2H), 2.16-2.32 (m, 3H), 3.24-3.39 (m,
IH), 3.54 (d, 2H, J = 10.2 Hz), 3.64-3.78 (m, 3H), 7.47 (s, IH), 7.69 (d, 2H, J = 9.0 Hz), 7.73
(d, 2H, J = 9.0 Hz).
Ia-45
mp 193 °C
1h-NMR (DMSO-d6) 5 ppm: 1.10 (t, 6H, J = 7.2 Hz), 1.26 (s, 9H), 1.28-1.52 (m, 4H),
1.75-1.86 (m, 2H), 1.89-2.01 (m, 2H), 2.10-2.22 (m, IH), 2.96-3.10 (m, IH), 3.30-3.52 (m,
12H), 6.60 (d, 2H, J = 9.0 Hz), 6.80 (d, IH, J = 9.0 Hz), 7.33 (d, 2H, J = 9.0 Hz), 9.46 (s,
IH).
Ia-46
mp >300 °C
1h-NMR (DMSO-dg) 5 ppm: 1.28 (s, 9H), 1.28-1.58 (m, 4H), 1.83-2.04 (m, 4H), 2.23-2.36
(m, IH), 2.46 (s, 3H), 3.00-3.14 (m, IH), 6.79 (d, IH, J = 8.7 Hz), 7.34 (d, IH, J = 8.7 Hz),
7.78 (d, 2H, J = 8.7 Hz), 7.89 (d, IH, J = 8.4 Hz), 7.91 (s, IH), 8.00 (d, 2H, J = 8.7 Hz),
10.13 (s, IH).
Ia-47
mp 236-237 °C
1h-NMR (CDCI3) 6 ppm: 0.97 (d, 6H, J = 6.6 Hz), 1.01 (d, 6H, J = 6.6 Hz), 1.20-1.37 (m,
2H), 1.40 (s, 9H), 1.60-1.84 (m, 3H), 1.97-2.31 (m, 5H), 2.50 (t, IH, J= 10.8 Hz), 2.78 (dt,
IH, J = 3.3, 11.4 Hz), 3.25-3.38 (m, IH), 3.45 (d, IH, J= 11.4 Hz), 3.75 (dt, IH, J = 2.4,
11.4 Hz), 4.02 (dt, IH, J = 2.4, 11.4 Hz), 6.88 (d, 2H, J = 9.0 Hz), 7.05 (s, IH), 7.39 (d, 2H, J
= 9.0 Hz).
Ia-48

mp 228-229 °C
XH-NMR (CDCI3) 6 ppm: 0.88 (t, 6H, J = 7.2 Hz), 1.19-1.45 (m, 4H), 1.40 (s, 9H), 1.45-
1.76 (m, 4H), 1.76-1.92 (m, IH), 1.96-2.30 (m, 5H), 2.66-3.20 (m, 3H), 3.20-3.40 (m, IH),
3.78 (d, IH, J = 9.3 Hz), 3.82 (s, IH), 6.62-6.98 (m, 2H), 7.09 (brs, IH), 7.37 (d, 2H, J = 7.8
Hz).
Ia-49
mp 262-263 °C
1h-NMR (CDCI3/DMSO) 6 ppm: 1.21 (d, 6H, J = 5.7 Hz), 1.26-1.34 (m, 2H), 1.37 (d, 6H,
J = 5.4 Hz), 1.52-1.76 (m, 2H), 1.85-2.03 (m, 2H), 2.03-2.30 (m, 3H), 2.30-2.53 (m, 2H),
3.02-3.33 (m, 4H), 3.75-3.98 (m, 2H), 5.70 (brs, IH), 6.73-6.98 (m, IH), 7.14-7.25 (m, IH),
7.52 (d, IH, JFH = 13.5 Hz), 8.86 (brs, IH).
Ia-50
mp 232-233 °C
1h-NMR (CDCI3) 6 ppm: 1.21 (d, 6H, J = 6.3 Hz), 1.22-1.37 (m, 2H), 1.38 (d, 6H, J = 6.9
Hz), 1.68 (q, 2H, J = 12.6 Hz), 1.98-2.26 (m, 5H), 2.29 (s, 3H), 2.41 (t, 2H, J = 10.2 Hz),
2.88 (d, 2H, J = 11.1 Hz), 3.15 (septet, IH, J = 6.6 Hz), 3.21-3.37 (m, IH), 3.77-3.92 (m,
2H), 3.87 (d, IH, J = 7.8 Hz), 6.88-7.06 (m, 3H), 7.35 (s, IH).
Ia-51
mp 211-212 °C
1h-NMR (CDC13) 5 ppm: 1.20-1.42 (m, 2H), 1.26 (d, 6H, J = 6.3 Hz), 1.38 (d, 6H, J = 6.9
Hz), 1.62-1.78 (m, 2H), 1.99-2.28 (m, 5H), 2.49 (dd, 2H, J= 10.5, 10.5 Hz), 3.17 (quint, IH,
J = 6.9 Hz), 3.20-3.38 (m, IH), 3.66-3.99 (m, 2H), 3.90-4.01 (m, 3H), 6.62 (d, IH, J= 9.0
Hz), 7.06 (s, IH), 7.90 (dd, lH, J = 2.4, 9.0 Hz), 8.09 (d, IH, J = 2.4 Hz).
Ia-52
mp 247-249 °C
1h-NMR (CDCI3) 6 ppm: 1.21-1.36 (m, 2H), 1.40 (s, 9H) 1.62-1.78 (m, 2H), 1.98-2.32 (m,
5H), 2.55 (t, 4H, J = 6.0 Hz), 3.23-3.38 (m, IH), 3.55 (t, 4H, J = 6.0 Hz), 3.72 (d, IH, J = 9.6

Hz), 6.94 (d, 2H, J = 9.0 Hz), 7.10 (s, IH), 7.42 (d, IH, J = 9.0 Hz).
Ia-53
mp 234-235 °C
1h-NMR (CDC13) 6 ppm: 1.22-1.38 (m, 2H), 1.41 (s, 9H) 1.64-1.80 (m, 2H), 2.00-2.32 (m,
5H), 3.25-3.40 (m, IH), 3.73 (d, IH, J = 9.3 Hz), 7.43 (a, IH), 7.48 (t, 2H, J = 7.5 Hz), 7.55-
7.66 (m, 3H), 7.68-7.89 (m, 4H).
Ia-54
mp 235-236 °C
1h-NMR (CDCI3) 5 ppm: 1.24-1.39 (m, 2H), 1.25 (d, 6H, J = 6.3 Hz), 1.39 (d, 6H, J = 6.9
Hz), 1.60-1.80 (m, 2H), 2.00-2.28 (m, 5H), 2.21 (s, 3H), 2.38 (t, 2H, J= 10.8 Hz), 3.15
(septet, IH, J = 6.3 Hz), 3.23-3.38 (m, IH), 3.40 (d, 2H, J = 11.7 Hz), 3.72-3.88 (m, 2H),
3.87 (d, IH, J = 9.3 Hz), 6.78-6.86 (m, 3H), 7.50 (d, IH, J = 9.6 Hz).
Ia-55
mp 185-186 °C
1h-NMR (CDCI3) 6 ppm: 1.14 (d, 6H, J = 6.3 Hz), 1.22-1.38 (m, 2H), 1.41 (s, 9H), 1.62-
1.78 (m, 2H), 2.02 (t, 2H, J= 10.5 Hz), 2.02-2.10 (m, 2H), 2.16-2.31 (m, 3H), 3.24-3.39 (m,
IH), 3.56 (d, 2H, J = 9.3 Hz), 3.63-3.80 (m, 3H), 7.46 (dd, IH, J= 1.5, 8.1 Hz), 7.51 (t, IH, J
= 8.1 Hz), 7.63 (s, IH), 7.81 (t, IH, J = 1.8 Hz), 7.98 (dt, IH, J = 1.8, 8.1 Hz).
Ia-56
mp 229-230 °C
1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.28-1.54 (m, 4H), 1.38 (s, 6H), 1.78-1.84 (m, 2H),
1.90-2.00 (m, 2H), 2.15-2.30 (m, IH), 2.97-3.13 (m, IH), 4.90 (s, IH), 6.79 (d, IH, J = 9.0
Hz), 7.34 (d, 2H, J = 8.7 Hz), 7.48 (d, 2H, J = 8.4 Hz), 9.72 (s, IH).
Ia-57
mp 211-212 °C
1h-NMR (CDCI3/DMSO) 6 ppm: 1.24-1.40 (m, 2H), 1.38 (s, 9H), 1.57-1.74 (m, 2H), 1.91
(s, 3H), 1.92-2.01 (m, 2H), 2.12-2.24 (m, 2H), 2.51 (brs, IH), 3.18-3.33 (m, IH), 4.96 (d, IH,

J = 9.3 Hz), 7.16-7.53 (m, 9H), 7.41 (s, IH).
Ia-58
mp 298-299 °C
1h-NMR (DMSO-d6) Sppm: 1.24 (s, 9H), 1.27 (s, 9H), 1.28-1.54 (m, 4H), 1.75-2.02 (m,
4H), 2.14-2.28 (m, IH), 2.97-3.11 (m, IH), 6.78 (d, IH, J= 8.4 Hz), 7.18 (d, 2H, J = 9.0 Hz),
7.48 (d, 2H, J = 9.0 Hz), 9.46 (s, IH), 9.76 (s, IH).
Ia-59
mp 253-254 °C
XH-NMR (CDC13) Sppm: 1.22-1.40 (m, 2H), 1.41 (s, 9H), 1.65-1.81 (m, 2H), 2.04-2.16 (m,
2H), 2.22-2.36 (m, 2H), 3.24-3.41 (m, IH), 3.74 (d, IH, J = 9.6 Hz), 7.40-7.54 (m, 3H),
7.88-8.01 (m, 3H), 8.66 (d, IH, J = 1.5 Hz), 9.57 (d, IH, J = 1.2 Hz).
Ia-60
mp 213-214 QC
1h-NMR (DMSO) Sppm: 1.32-1.50 (m, 2H), 1.35 (s, 9H), 1.52-1.70 (m, 2H), 1.88-2.00 (m,
2H), 2.04-2.16 (m, 2H), 2.22-2.38 (m, IH), 2.65 (s, 3H), 2.99-3.15 (m, IH), 6.46 (d, IH, J =
9.3 Hz), 7.28 (d, IH, J = 9.0 Hz), 7.81 (s, IH), 8.20 (s, IH), 8.47 (s, IH), 9.89 (s, IH).
Ia-61
mp 274-275 °C
1h-NMR (DMSO) Sppm: 1.27 (s, IH), 1.28-1.58 (m, 4H), 1.84-2.08 (m, 4H), 2.22-2.40 (m,
IH), 2.99-3.15 (m, IH), 3.01 (s, 3H), 6.81 (d, IH, J = 8.1 Hz), 7.78 (d, 2H, J = 7.8 Hz), 7.84
(d, 2H, J = 8.4 Hz), 8.18 (s, IH), 10.43 (s, IH).
Ia-62
mp 235-236 °C
1h-NMR (CDCI3) 6 ppm: 1.22-1.39 (m, 2H), 1.41 (s, 3H), 1.66-1.80 (m, 2H), 2.01-2.12 (m,
2H), 2.14-2.22 (m, IH), 2.23-2.34 (m, 2H), 3.24-3.42 (m, IH), 3.69 (d, IH, J = 9.5 Hz), 6.44
(d, IH, J = 9.3 Hz), 7.27 (brs, IH), 7.28 (d, IH, J = 9.3 Hz), 7.37 (dd, IH, J = 2.4, 9.0 Hz),
7.68 (d, IH, J = 9.6 Hz), 8.04 (d, IH, J = 2.4 Hz).

Ia-63
mp 277-279 °C
1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.28-1.54 (m, 4H), 1.77-2.02 (m, 4H), 2.15-2.29
(m, IH), 2.90 (s, 3H), 2.96-3.13 (m, IH), 6.79 (d, IH, J = 8.7 Hz), 7.12 (d, 2H, J = 9.0 Hz),
7.54 (d, 2H, J = 9.0 Hz), 9.50 (s, IH), 9.81 (s, IH).
Ia-64
mp 259-260 °C
1h-NMR (DMSO-d6) 5 ppm: 1.26 (s, 9H), 1.26-1.50 (m, 4H), 1.74-1.99 (m, 4H), 2.10-2.25
(m, IH), 2.95-3.10 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 6.97 (d, 2H, J = 9.0 Hz), 7.42 (d, 2H, J
= 9.0 Hz), 7.50-7.71 (m, 5H), 9.73 (s, IH), 10.05 (s, IH).
Ia-65
mp 292-293 °C
1h-NMR (DMSO-de) 6 ppm: 1.27 (s, 9H), 1.28-1.54 (m, 4H), 1.62-1.72 (m, 2H), 1.77-1.87 (m, 2H), 1.91-2.10 (m, 4H), 2.13-2.25 (m, IH), 2.98-3.12 (m, IH),-3.41-3.52 (m, 2H), 5.09 (s,
IH), 6.79 (d, IH, J = 9.0 Hz), 6.91 (d, 2H, J = 9.0 Hz), 7.37 (d, 2H, J = 9.0 Hz), 7.42 (d, 2H,
J = 9.0 Hz), 7.51 (d, 2H, J = 9.0 Hz), 9.56 (s, IH).
Ia-66
mp >300 °C
1h-NMR (DMSO-d6) 5 ppm: 1.27 (s, 9H), 1.28-1.58 (m, 4H), 1.85-2.02 (m, 4H), 2.40-2.52
(m, IH), 3.00-3.16 (m, IH), 6.81 (d, IH, J = 9.0 Hz), 7.50-7.58 (m, 3H), 7.90-7.97 (m, 2H),
12.58 (s, IH).
Ia-67
mp 199-200 °C
1h-NMR (DMSO-d6) 6 ppm: 1.14 (d, 6H, J = 6.3 Hz), 1.28 (s, 9H), 1.31-1.48 (m, 4H),
1.76-1.88 (m, 2H), 2.17 (t, 2H, J= 11.1 Hz), 2.82 (t, 2H, J= 11.7 Hz), 3.46 (d, 2H, J= 11.4
Hz), 3.20-3.36 (m, IH), 3.62-3.74 (m, 2H), 4.02 (d, 2H, J = 12.9 Hz), 6.83 (d, 2H, J = 9.0 Hz),
6.89 (d, IH, J = 8.7 Hz), 7.28 (d, 2H, J = 9.0 Hz), 8.27 (s, IH).

Ia-68
mp 237-239 °C
1h-NMR (CDCI3/DMSO) 5 ppm: 1.40 (s, 9H), 1.49-1.65 (m, 2H), 1.99-2.10 (m, 2H), 2.95
(t, 2H, J = 11.1 Hz), 3.36-3.52 (m, IH), 4.17 (d, IH, J = 12.9 Hz), 5.84 (d, IH, J = 8.7 Hz),
6.39 (d, IH, J = 9.6 Hz), 7.21 (d, IH, J = 9.3 Hz), 7.51 (dd, IH, J = 2.4, 9.3 Hz), 7.72 (d, IH,
J = 9.9 Hz), 7.85 (d, IH, J = 2.7 Hz), 8.04 (s, IH).
Ia-69
mp 259-260 °C
1h-NMR (DMSO) 5 ppm: 1.25-1.55 (m, 4H), 1.27 (s, 9H), 1.82-2.05 (m, 4H), 2.22-2.36 (m,
IH), 2.98-3.17 (m, IH), 4.16 (s, 3H), 6.80 (d, IH, J = 8.4 Hz), 7.77-7.87 (m, 4H), 10.16 (s,
IH).
Ia-70
mp 259-260 °C
1h-NMR (DMSO) 6 ppm: 1.28 (s, 9H), 1.36-1.56 (m, 2H), 1.80-1.92 (m, 2H), 2.86-3.02 (m,
2H), 3.36-3.52 (m, IH), 4.04-4.20 (m, 2H), 6.92 (d, IH, J = 7.5 Hz), 7.38-7.58 (m, 3H),
8.00-8.14 (m, 2H), 8.90 (s, IH), 9.08 (s, IH), 9.63 (s, IH).
Ia-71
mp 228-229 °C
1h-NMR (CDCI3/DMSO) 6 ppm: 1.27-1.42 (m, 2H), 1.38 (s, 9H), 1.57-1.75 (m, 2H),
1.90-2.02 (m, 2H), 2.12-2.34 (m, 3H), 3.14-3.32 (m, IH), 5.37 (d, IH, J = 9.3 Hz), 7.38-7.43
(m, 3H), 7.46 (d, 2H, J = 8.7 Hz), 7.51-7.60 (m, 2H), 7.68 (d, 2H, J = 9.0 Hz), 9.33 (s, IH).
Ia-75
mp 169-170 °C
1h-NMR (CDCI3) 5 ppm: 0.58-0.72 (m, IH), 0.80 (d, 3H, J = 6.6 Hz), 0.94 (d, 3H, J = 6.0
Hz), 1.14-1.35 (m, 3H), 1.39 (s, 9H), 1.48-1.66 (m, 2H), 1.74-2.06 (m, 5H), 2.06-2.44 (m,
6H), 3.18-3.35 (m, IH), 3.64-3.74 (m, IH), 4.46-4.60 (m, IH), 6.98-7.38 (m, 5H).
Ia-76

mp 236-237 °C
:H-NMR (CDCI3/DMSO) Sppm: 1.27-1.42 (m, 2H), 1.38 (d, 6H, J = 6.6 Hz), 1.60-1.78 (m
2H), 1.94-2.06 (m, 2H), 2.12-2.30 (m, 3H), 3.06-3.34 (m, 2H), 5.10 (brs, IH), 6.41 (d, IH, J
= 9.9 Hz), 7.25 (d, IH, J = 8.4 Hz), 7.48 (dd, IH, J = 2.4, 8.7 Hz), 7.68 (d, IH, J = 9.9 Hz),
8.12 (d, IH, J = 2.4 Hz), 8.88 (brs, IH).
Ia-77
mp 117-118 °C
1h-NMR (CDCI3) 6 ppm: 1.38 (d, 6H, J = 6.9 Hz), 1.65 (quintet, 2H, J = 5.4 Hz), 1.75-
1.91 (m, 2H), 2.42 (t, 2H, J = 7.4 Hz), 3.10-3.24 (m, 3H), 4.77 (brs, IH), 6.41 (d, IH, J = 9.6
Hz), 7.18-7.26 (m, IH), 7.48 (dd, IH, J= 1.8, 8.7 Hz), 7.67 (d, IH, J = 9.9 Hz), 8.01 (s, IH),
8.23 (brs, IH).
Ia-78
mp 138-139 °C
1h-NMR (CDCI3) 6 ppm: 1.41 (s, 9H), 1.64 (quintet, 2H, J = 6.6 Hz), 1.84 (quintet, 2H, J
= 7.3 Hz), 2.42 (t, 2H, J = 7.5 Hz), 3.26 (q, 2H, J = 6.5 Hz), 4.59 (brs, IH), 6.41 (d, IH, J =
9.3 Hz), 7.23 (d, IH, J = 8.7 Hz), 7.49 (dd, IH, J = 2.4, 9.0 Hz), 7.67 (d, IH, J = 9.9 Hz),
8.03 (d, IH, J = 2.4 Hz), 8.28 (brs, IH).
Ia-79
mp 289-290 °C
1h-NMR (DMSO) 6 ppm: 1.24-1.63 (m, 4H), 1.28 (s, 9H), 1.84-2.08 (m, 4H), 2.24-2.41 (m,
IH), 3.00-3.16 (m, IH), 6.82 (d, IH, J = 8.1 Hz), 7.36-7.60 (m, 5H), 7.86-7.99 (m, 2H), 8.28
(s, IH), 10.50 (s, IH).
Ia-80
mp 239-240 °C
1h-NMR (DMSO) 6 ppm: 1.22 (d, IH, J = 6.6 Hz), 1.23-1.40 (m, 2H), 1.40-1.59 (m, 2H),
1.83-2.04 (m, 4H), 2.23-2.39 (m, IH), 2.98-3.23 (m, 2H), 7.00 (d, IH, J = 7.8 Hz), 7.36-7.59
(m, 5H), 7.85-7.97 (m, 2H), 8.29 (s, IH), 10.50 (s, IH).

Ia-81
mp 205-206 °C
1h-NMR (CDCI3/DMSO) 5 ppm: 1.40 (s, 9H), 1.66 (quintet, 2H, J = 7.0 Hz), 1.85
(quintet, 2H, J = 7.2 Hz), 2.45 (t, 2H, J = 7.5 Hz), 3.24 (t, 2H, J = 6.5 Hz), 5.17 (brs, IH),
7.36-7.54 (m, 5H), 7.85 (d, IH, J = 8.4 Hz), 8.07 (dd, IH, J = 1.8, 8.1 Hz), 8.23 (d, IH, J =
1.8 Hz), 9.61 (s, IH).
Ia-82
mp 216-217 °C
1h-NMR (DMSO-d6) 6 ppm: 1.14 (d, 6H, J = 6.3 Hz), 1.22 (d, 6H, J = 6.9 Hz), 1.22-1.53
(m, 4H), 1.76-1.98 (m, 2H), 2.21 (t, 2H, J = 10.8 Hz), 2.22-2.36 (m, IH), 2.96-3.20 (m, 2H),
3.57 (d, 2H, J = 12.0 Hz), 3.60-3.74 (m, IH), 6.66-6.85 (m, 2H), 6.98 (d, IH, J = 7.8 Hz),
7.47 (d, IH, J = 8.7 Hz), 9.30 (s, IH).
Ia-83
mp 118-119 °C
1h-NMR (DMSO-d6) 6 ppm: 1.41 (d, 6H, J = 6.3 Hz), 1.26 (s, 9H), 1.40-1.67 (m, 4H),
2.17-2.36 (m, 3H), 2.97-3.10 (m, 2H), 3.57 (d, 2H, J = 12.0 Hz), 3.61-3.74 (m, IH), 6.67-6.92
(m, 3H), 7.48 (t, IH, J = 9.0 Hz), 9.37 (s, IH).
Ia-84
mp 265-267 °C
*H-NMR (DMSO-d6) 5 ppm: 1.21 (d, 6H, J = 6.6 Hz), 1.20-1.57 (m, 4H), 1.60-2.30 (m,
9H), 2.99-3.20 (m, 4H), 3.40-3.52 (m, 2H), 5.09 (s, IH), 6.91 (d, 2H, J = 8.7 Hz), 6.98 (d, IH,
J = 7.5 Hz), 7.37 (d, 2H, J = 8.7 Hz), 7.42 (d, 2H, J = 8.7 Hz),.7.51 (d, 2H, J = 8.7 Hz), 9.56
(a, IH).
Ia-85
mp 185-186 °C
1h-NMR (DMSO-d6) 5 ppm: 1.26 (s, 9H), 1.42-1.72 (m, 6H), 1.96-2.10 (m, 2H), 2.26 (t,
2H, J = 6.9 Hz), 2.96-3.12 (m, 4H), 3.41-3.52 (m, 2H), 5.09 (s, IH), 6.88 (d, IH, J = 8.7 Hz),

6.92 (d, 2H, J = 9.0 Hz), 7.37 (d, 2H, J = 8.7 Hz), 7.43 (d, 2H, J = 9.0 Hz), 7.52 (d, 2H, J =
8.7 Hz), 9.63 (s, IH).
Ia-86
mp 162-164 °C
1h-NMR (DMSO-d6) 5 ppm: 1.21 (d, 6H, J = 6.6 Hz), 1.41-1.73 (m, 6H), 1.96-2.10 (m,
2H), 2.26 (t, 2H, J = 7.2 Hz), 2.91-3.20 (m, 5H), 3.42-3.52 (m, 2H), 5.09 (s, IH), 6.92 (d, 2H,
J = 9.3 Hz), 6.99 (t, IH, J = 6.0 Hz), 7.37 (d, 2H, J = 8.7 Hz), 7.43 (d, 2H, J = 9.3 Hz), 7.52
(d, 2H, J = 8.7 Hz), 9.64 (s, IH).
Ia-87
mp 245-247 °C
*H-NMR (DMSO-d6) 5 ppm: 1.22 (d, 6H, J = 6.6 Hz), 1.22-1.58 (m, 4H), 1.81-2.02 (m,
4H), 2.22-2.36 (m, IH), 3.00-3.20 (m, 2H), 3.01 (s, 3H), 6.99 (d, IH, J = 8.4 Hz), 7.75-7.88
(m, 2H), 8.19 (d, IH, J= 1.2 Hz), 10.43 (s, IH).
Ia-88
mp 208-209 °C
1h-NMR (DMSO-d6) 6ppm: 1.22 (d, 6H, J = 6.9 Hz), 1.22-1.55 (m, 4H), 1.75-1.98 (m,
4H), 2.11-2.24 (m, IH), 2.98-3.20 (m, 2H), 5.96 (s, 2H), 6.82 (d, IH, J = 8.4 Hz), 6.91-7.03
(m, 2H), 7.30 (d, IH, J= 1.8 Hz), 9.72 (s, IH).
Ia-89
mp 142-143 °C
1h-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.40-1.66 (m, 4H), 2.26 (t, 2H, J = 7.5 Hz), 3.02
(q, 2H, J = 6.6 Hz), 5.96 (s, 2H), 6.82 (d, IH, J = 8.4 Hz), 6.88 (t, IH, J = 8.4 Hz), 6.94 (dd,
IH, J = 1.8, 8.4 Hz), 7.30 (d, IH, J = 1.8 Hz), 9.78 (s, IH).
Ia-90
mp 100 °C
1h-NMR (DMSO-d6) 6 ppm: 1.20 (d, 6H, J = 6.9 Hz), 1.40-1.66 (m, 4H), 2.26 (t, 2H, J =
7.5 Hz), 2.89-2.99 (m, 2H), 3.13 (quint, IH, J = 6.6 Hz), 5.96 (s, 2H), 6.83 (d, IH, J = 8.1

Hz), 6.91-7.02 (m, 2H), 7.30 (d, IH, J= 1.8 Hz), 9.78 (s, IH).
Ia-91
mp 189-190 °C
1h-NMR (DMSO-d6) 5 ppm: 1.26 (s, 9H), 1.43-1.71 (m, 4H), 2.40 (t, 2H, J = 7.5 Hz),
2.97-3.09 (m, 2H), 3.01 (s, 3H), 6.85-6.93 (m, IH), 7.76-7.88 (m, 2H), 8.20 (d, IH, J= 1.2
Hz), 10.49 (s, IH).
la-104
mp 238-241 °C
1h-NMR (DMSO) 6 ppm: 1.27 (s. 9H), 1.3-1.5 (m. 4H), 1.8-2.0 (m, 4H), 2.50 (m, IH),
3.05 (m, IH), 6.55 (br s, IH), 6.79 (d, IH, J= 8.2), 7.15 (t, IH, J= 4.8), 8.64 (d, 2H, J= 4.8).
Ia-105
mp 232-234 °C
1h-NMR (DMSO) 6 ppm: 1.26 (s, 9H), 1.2-1.5.(m, 4H), 1.8-2.0 (m, 4H), 2.55 (m, IH),
3.05 (m, IH), 6.77 (d, IH, J=8.7), 9.92 (s, 2H), 10.93 (s, IH).
la-106
mp 226-228 °C
1h-NMR (DMSO) 6 ppm: 1.28 (s, 9H), 1.22-1.58 (m, 4H), 1.82-2.04 (m, 4H), 2.29 (m, IH),
3.07 (m, IH), 6.79 (d, IH, J = 8.7 Hz), 7.6 l(d-d, IH, J = 1.8 Hz, 8.7 Hz), 8.04 (d, IH, J =
8.7 Hz), 8.48 (d, IH, 2.1 Hz), 9.35 (s, IH), 10.05 (s, IH).
Ia-107
mp 282-283 °C
1h-NMR (DMSO) 6 ppm: 1.22-1.57 (m, 4H), 1.27 (s, 9H), 1.80-2.04 (m, 4H), 2.27 (m, IH),
3.06 (m, IH), 6.81 (d, IH, J = 8.7 Hz), 7.32 (m, IH), 7.44 (t, 2H, J = 7.5 Hz), 7.57-7.72 (m,
6H), 9.91 (s, IH).
la-108
mp 191-192°C
1h-NMR (DMSO) 6ppm: 1.24-1.58 (m, 4H), 1.28 (s, 9H), 1.86-2.04 (m, 4H), 2.70 (m, IH),

3.08 (m, IH), 6.83 (d, IH, J = 8.7 Hz), 7.63-7.79 (m, 2H), 8.31 (d, IH, J = 7.2 Hz). 10.27 (s,
IH).
Ia-109
mp 283-285 °C
1h-NMR (DMSO) 5 ppm: 1.24-1.60 (m, 4H), 1.28 (s, 9H), 1.87-2.04 (m, 4H), 2.42 (m, IH),
3.09 (m, IH), 3.87 (s, 2H), 6.82 (d, IH, J = 8.7 Hz), 7.28-7.43 (m, 3H), 7.60 (d, 2H, J = 7.8
Hz), 7.68 (d, IH, J = 7.2 Hz), 7.89 (d, IH, J = 7.5 Hz), 9.48 (s, IH).
Ia-110
mp 263-265 °C
1h-NMR (DMSO) 6 ppm: 1.24-1.54 (m, 4H), 1.27 (s, 9H), 1.76-1.87 (m, 2H), 1.89-2.01 (m,
2H), 2.17 (m, IH), 3.04 (m, IH), 4.01 (a, 4H), 6.01 (s, 2H), 6.44 (d, 2H, J = 8.7 Hz), 6.77 (d,
IH, J = 8.7 Hz), 7.39 (d, 2H, J = 9,0 Hz), 9.44 (s, IH).
Ia-111
mp 239-241 °C
1h-NMR (DMSO) 6 ppm: 1.24-1.54 (m, 4H), 1.27 (s, 9H), 1.62-1.76 (m, 4H), 1.80-2.02
(m, 4H), 2.30 (m, IH), 2.47-2.59 (m, 2H), 2.66-2.76 (m, 2H), 6.08 (m, IH), 6.79 (d, IH, J =
9.0 Hz), 6.88 (d, IH, J = 6.9 Hz), 7.02 (t, IH, J = 7.5 Hz), 7.13 (d, IH, J = 7.5 Hz), 8.98 (s,
IH).
Ia-124
mp 247-249 °C
*H-NMR (DMSO) 6 ppm: 1.15 (d, 6H, J = 6.3 Hz), 1.30 (s, 9H), 2.15-2.26 (m, 2H), 3.48-
3.57 (m, 2H), 3.63-3.76 (m, 2H), 6.92 (d, 2H, J = 8.7 Hz), 7.59 (d, 2H, J = 9.0 Hz), 7.38 (d,
2H, J = 9.0 Hz), 7.87 (d, 2H, J = 8.7 Hz), 9.92 (brs, IH), 9.98 (brs, IH).
Ia-125
mp 228.-232 °C
1h-NMR (DMSO) 6 ppm: 1.30 (s, 9H), 1.95-2.08 (m, 2H), 2.77-2.89 (m, 4H), 7.17 (d, IH,
J = 8.4 Hz), 7.39 (d, 2H, J = 9.0 Hz), 7.42-7.48 (m, IH), 7.64 (brs, IH), 7.87 (d, 2H, J = 9.0

Hz), 9.99 (brs, 2H).
Ia-126
mp 244-246 °C
1h-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 7.42 (d, 2H, J = 8.4 Hz), 7.81 (d-d, IH, J = 2.1 Hz,
8.7 Hz), 7.93 (d, 2H, J = 9.0 Hz), 8.05 (d, IH, J = 9.0 Hz), 8.66 (d, IH, J = 2.1 Hz), 9.29 (s,
IH), 10.05 (brs, IH), 10.39 (brs, IH).
Ia-127
mp 238-239 °C
1h-NMR (DMSO) 5 ppm: 1.30 (s, 9H), 4.18-4.27 (m, 4H), 6.81 (d, IH, J = 8.4 Hz), 7.16
(d-d, IH, J = 2.7 Hz, 9.0 Hz), 7.34-7.42 (m, 3H), 7.85 (d, 2H, J = 8.4 Hz), 9.94 (brs, IH),
9.99 (brs, IH).
Ia-128
mp 286-287 °C
1h-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 7.41 (d, 2H, J = 8.7 Hz), 7.71 (d, 2H, J = 8.4 Hz),
7.91 (d, 2H, J = 8.7 Hz), 7.99 (d, 2H, J = 8.7 Hz), 10.05 (brs, IH), 10.44 (brs, IH).
Ia-129
mp 232-234 °C
1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.25 (IH, m),
3.07 (m, IH), 6.80 (d, IH, J=9.0), 7.37 (d, IH, J= 8.1), 7.53 (t, IH, J=8.1), 7.75 (t, IH, J=
8.1), 8.12 (s, IH), 10.16 (s, IH).
Ia-130
mp 274-277 °C
1h-NMR (DMSO) 5 ppm: 1.27 (s, 9H), 1.23-1.58 (m, 4H), 1.81-2.03 (m, 4H), 2.28 (m, IH),
3.07 (m, IH), 6.80 (d, IH, J = 8.4 Hz), 7.36 (d-d, IH, J = 0.9 Hz, 5.7 Hz), 7.43 (d-d, IH, J =
2.1 Hz, 8.7 Hz), 7.60 (d, IH, J = 5.4 Hz), 7.78 (d, IH, J = 8.7 Hz), 8.40 (d, IH, 1.8 Hz), 9.97
(brs, IH).
Ia-131

mp 259-260 °C
XH-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 7.40 (d, IH, J = 4.8 Hz), 7.41 (d, 2H, J = 8.7 Hz),
7.66 (d, IH, J = 5.1 Hz), 7.67 (d-d, IH, J = 1.8 Hz, 8.7 Hz), 7.84 (d, IH, J = 9.0 Hz), 7.92 (d,
2H, J = 8.7 Hz), 8.50 (s, IH), 10,03 (brs, IH), 10,27 (brs IH).
Ia-132
mp 265-266 °C
*H-NMR (DMSO) 6 ppm: 1.17 (d, 6H, J = 6.6 Hz), 1.31 (s, 9H), 4.10 (m, IH), 7.35-7.46
(m, 3H), 7.54 (d, IH, J = 7.5 Hz), 7.87-7.97 (m, 3H), 8.15 (brs, IH), 8.20 (d, IH, J = 7.5 Hz),
10.03 (brs, IH), 10.25 (brs, IH).
Ia-133
mp 249-250 °C
1h-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 7.41 (d, 2H, J = 8.7 Hz), 7.45 (d, IH, J = 5.4 Hz),
7.67 (d-d, IH, J = 1.8 Hz, 8.7 Hz), 7.76 (d, IH, J = 5.4 Hz), 7.92 (d, 2H, J = 8.7 Hz), 7.95 (d,
IH, J = 8.1 Hz), 8.39 (d, IH, J = 1.8 Hz), 10.02 (brs, IH), 10 23 (brs, IH).
la-134
mp 305-306 °C
1h-NMR (DMSO) 6 ppm: 1.25 (m, 2H), 1.25 (s, 9H), 1.52 (m, 2H), 1.82 (m, 2H,), 1.94 (m,
2H), 2.13 (m, IH), 3.04 (m, IH), 6.00 (d, IH, J= 8.1), 6.74 (d, IH, J= 8.4), 7.3-7.5 (m, 6H),
7.85 (d, 2H, J=7.5), 8.31 (d, IH, J=8.4).
Ia-135
mp 220-222 °C
1h-NMR (DMSO) 5 ppm: 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.37 (m, IH),
3.03 (m, IH), 6.80 (d, IH, J=8.7), 7.04 (m, IH), 7.29 (m, IH), 7.79 (m, IH), 9.60 (s, IH).
Ia-136
mp 263-264 °C
1h-NMR (DMSO) 6 ppm: 1.27 ( s, 9H), 1.3-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.20(m, IH),
3.03 (m, IH), 6.80 (d, IH, J= 8.4), 6.87 ( m, IH), 7.31 (m, 2H), 10.21 (s, IH).

la-137
mp 260-262 °C
1h-NMR (DMSO) 5 ppm: 1.27 ( s, 9H), 1.3-1.5 ( m, 4H), 1.8-2.0 (m, 4H), 2.30 (m, IH),
3.05 (m, IH), 6.80 (d, IH, J= 8.4), 7.13 (t, 2H, J= 8.1), 7.31 (m, IH), 9.52 (s, IH).
la-138
mp 270-273 °C
XH-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.12 (m, IH),
3.05 (m, IH), 6.79 (d, IH, J=9.0), 7.31 (m, 2H), 7.80 (m, IH), 10.05 (s, IH).
Ia-139
mp 267-270 °C
1h-NMR (DMSO) 6 ppm: 1.30 (s, 9H), 4.05 (s, 4H), 6.04 (s, 2H), 6.51 (d, 2H, J = 8.7 Hz),
7.34 (d, 2H, J = 8.4 Hz), 7.54 (d, 2H, J = 8.4 Hz), 7.87 (d, 2H, J = 8.4 Hz), 9.82 (brs, IH),
9.97 (brs, IH).
la-140
mp 227-229 °C
1h-NMR (DMSO) 6 ppm: 1.22 (d, 6H, J = 6.6 Hz), 1.20-1.57 (m 4H), 1.80-2.01 (m, 4H),
2.27 (m, IH), 2.95-3.22 (m, 2H), 6.99 (d,lH, J = 7.8 Hz), 7.65 (d, 2H, J = 8.7 Hz), 7.80 (d,
2H, J = 8.4 Hz), 10.18 (brs, IH).
Ia-141
mp 205-207 °C
1h-NMR (DMSO) 8 ppm: 1.22 (d, 6H, J = 6.9 Hz), 1.20-1.55 (m, 4H), 1.75-2.05 (m, 6H),
2.21 (m, IH), 2.72-2.85 (m, 4H), 2.93-3.20 (m, 2H), 6.98 (d, IH, J = 8.1 Hz), 7.10 (d, IH, J =
8.1 Hz), 7.26 (d-d, IH, J = 2.1 Hz, 8.1 Hz), 7.51 (s, IH), 9.67 (brs, IH).
Ia-142
mp 295-296 °C
1h-NMR (DMSO) 5 ppm: 1.15 (d, 6H, J=6.6), 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.8-2.0 (m,
4H), 2.27 (m, IH), 3.05 (m, IH), 4.07 (m, IH), 6.80 (d, IH, J=8.7), 7.64 (d, 2H, J=8.7), 7.79

(d, 2H, J=8.7), 8.06 (d, IH, J=7.5), 10.01 (s, IH).
Ia-143
mp 146-147 °C
1h-NMR (DMSO) 5ppm: 1.26 (s, 9H), 1.5-1.7 (m, 4H), 2.36 (t, 2H, J=7.8), 3.03 (q, 2H;
J=6.3), 6.89 (t, IH, J=6.3), 7.66 (d, 2H, J=8.4), 7.80 (d, 2H, J=8.4), 10.25 (s, IH).
Ia-144
mp 138-140 °C
1h-NMR (DMSO) Sppm: 1.21 (d, 6H, J=6.0), 1.4-1.7 (m, 4H), 2.37 (t, 2H, J=7.5), 2.96 (q,
2H, J=6.3), 3.14 (m, IH), 6.99 (t, IH, J=5.4), 7.66 (d, 2H, J=7.8), 7.81 (d, 2H, J=7.8), 10.26
(s, IH).
la-145
mp 134-136 °C
1h-NMR (DMSO) Sppm: 1.26 (s, 9H), 1.39 (m, 2H), 1.4-1.7 (m, 4H), 2.28 (t, 2H, J=7.2),
2.79 (m, 4H), 3.02 (q, 2H, J=7.2), 6.88 (t, IH, J=6.0), 7.10 (t, IH, J=6.0), 7.51 (s, IH), 9.73
(a, IH).
Ia-146
mp 135-137 °C
1h-NMR (DMSO) 6 ppm: 1.20 (d. 6H, J=6.6), 1.4-1.7 (m, 4H), 1.99 (m, 2H), 2.28 (t, 2H,
J=7.2), 2.79 (m, 4H), 2.94 (q, 2H, J=6.3), 3.13 (m, IH), 6.98 (t, IH, J=6.9), 7.10 (d, 2H,
J=8.1), 7.26 (d, 2H, J=8.1), 7.51 (a, IH), 9.73 (s,lH).
la-147
mp 206-207 °C
1h-NMR (DMSO) 6 ppm; 1.29 (s, 9H), 4.54 (d, 2H, J = 5.7 Hz), 7.35 (d, 2H, J = 9.0 Hz),
7.52 (d, 2H, J = 7.8 Hz), 7.69 (d, 2H, J = 8.1 Hz), 7.83 (d, 2H, J = 8.7Hz), 9.02 (t, IH, J =
5.7 Hz), 9.97 (brs, IH).
Ia-148
mp 250-251 °C

1h-NMR (DMSO) 6 ppm: 1.30 (s, 9H), 7.18 (t, 2H, J = 9.3 Hz), 7.40 (d, 2H, J = 8.7 Hz),
7.76 (d-d, 2H, J = 5.1 Hz, 9.3 Hz), 7.88 (d, 2H, J = 9.0 Hz), 10.02 (brs, IH), 10.17 (brs, IH).
Ia-149
mp 220-222 °C
1h-NMR (DMSO) 6 ppm: 1.30 (s, 9H), 3.74 (s, 3H), 6.92 (d, 2H, J = 9.0 Hz), 7.38 (d, 2H,
J = 9.0 Hz), 7.64 (d, 2H, J = 9.0 Hz), 7.87 (d, 2H, J = 9.0 Hz), 9.99 (s, 2H).
Ia-150
mp 264-266 °C
1h-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 1.66-1.76 (m, 4H), 2.57- 2.66 (m, 2H), 2,71-2.80
(m, 2H), 6.98 (m, IH), 7.06-7.16 (m, 2H), 7.38 (d, 2H, J = 9.0 Hz), 7.90 (d, 2H, J = 8.7 Hz),
9.60 (s, IH), 9.99 (s, IH).
Ia-151
mp 235-236 °C
*H-NMR (DMSO) 6 ppm: 1.03-1.39 (m, 5H), 1.27 (s, 9H), 1.55-1.87 (m, 5H), 3.73 (m, IH),
7.31 (d, 2H, J = 8.7 Hz), 7.76 (d, 2H, J = 8.4 Hz), 8.01 (d, IH, J = 7.8 Hz), 9.90 (s, IH).
Ia-152
mp 244-246 °C
1h-NMR (DMSO) 6 ppm: 0.50-0.72 (m, 4H), 1.27 (s, 9H), 2.81 (m, IH), 7.31 (d, 2H, J =
8.7 Hz), 7.73 (d, 2H, J = 8.7 Hz), 8.30 (d, IH, J = 4.2 Hz), 9.91 (brs, IH).
Ia-153
mp >300 °C
1h-NMR (DMSO) 5 ppm: 1.06 (m, 6H), 1.27 (s, 9H), 1.2-1.5 (m, 4H), 1.8-2.0 (m, 4H),
2.25 (m, IH), 2.7 (m, IH), 3.05 (m, IH), 3.51 (m, 4H), 4.30 (m, IH), 6.80 (d, IH, J=8.4),
7.34 (d, 2H, J=8.4), 7.65 (d, 2H, J=8.4), 10.01 (s, IH).
Ia-154
mp 247-249 °C
1h-NMR (DMSO) 6 ppm: 1.05 (m,6H), 1.27 (s, 9H), 1.2-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.23

(m, IH), 2.77 (m, IH), 3.05 (m, IH), 3.52 (m, 4H), 4.33 (m, IH), 6.80 (d, IH, J=9.0), 7.03 (d,
IH, J=7.8), 7.35 (t, IH, J=7.8), 7.59 (d, IH, J=7.8), 7.68 (s, IH), 9.96 (s, IH).
la-155
mp 258-259 °C
1h-NMR (DMSO) 5 ppm: 1.25(m, 2H), 1.50 (m,2H), 1.86 (m, 2H), 1.99 (m, 2H), 2.28
(m ,.1H), 2.93 (s, 3H), 3.10 (m, IH), 7.02 (d, IH, J=7.5), 7.65 (d, 2H, J=8.4), 7.80 (d, 2H,
J=8.4). 10.20 (s, IH).
Ia-156
mp 250-253 °C
1h-NMR (DMSO) 5 ppm: 1.28 (m, 2H), 1.50 (m, 2H), 1.82 (m, 2H), 2.00 (m, 4H), 2.22 (m,
IH), 2.79 (m, 4H), 2.92 (s, 3H), 3.11 (m, IH), 7.01 (d, IH, J=(.l), 7.26 (d, IH, J=8.1), 7.51 (s,
IH), 9.68 (s, IH).
Ia-157
mp 259-262 °C
1h-NMR (DMSO) 6 ppm: 1.13 (d, 6H, J=6.0), 1.25 (m, 2H), 1.50 (m, 2H), 1.80 (m, 2H),
1.95 (m, 2H), 2.17 (m, 3H), 2.92 (s, 3H), 3.10 (m, IH), 3.70 (m,2H), 3.68 (m, 2H), 6.86 (d,
2H J=9.3), 7.00 (d, IH, J=7.2), 7.43 (d, 2H, J=9.3), 9.58 (s, IH).
Ia-158
mp 298-300 °C
1h-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 7.30-7.50 (m, 5H), 7.63-7,71 (m, 4H), 7.87 (d, 2H,
J = 8.7 Hz), 7.91 (d, 2H, J = 9.0 Hz), 10.03 (brs, IH), 10.22 (brs, IH).
Ia-159
mp 278-281 °C
1h-NMR (DMSO) 5 ppm: 0.74-1.87 (m, 20H), 1.29 (s, 9H), 3.76 (m, IH), 7.32 (d, 2H, J =
8.4 Hz), 7.75 (d, 2H, J = 8.7 Hz), 7.75 (d, IH, J = 8.7 Hz), 7.90 (brs, IH).
la-160
mp 227-228 °C

1h-NMR (DMSO) 5 ppm: 1.22-1.55 (m, 4H), 1.27 (s, 9H), 1.80-2.02 (m, 4H), 2.23 (m, IH),
3.06 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.45 (t, IH, J = 9.9 Hz), 7.82 (m, IH), 8.12 (d-d, IH,
J = 2.4 Hz, 6.3 Hz), 10.17 (brs, IH).
Ia-161
mp 259-260 °C
1h-NMR (DMSO) 5 ppm: 1.22-1.54 (m, 4H), 1.27 (s, 9H), 1.78-2.01 (m, 4H), 2.16 (s, 3H),
2.21 (m, IH), 3.05 (m, IH), 6.77 (d, IH, J = 8.4 Hz), 7.12-7.21 (m, 2H), 7.53 (m, IH), 9.90
(brs, IH).
Ia-162
mp 222-226 °C
1h-NMR (DMSO) 6 ppm: 1.15 (d,6H,J = 6.3 Hz), 1.26 (d, 6H, J = 6.9 Hz), 2.16-2.26 (m,
2H), 3.31 (m, IH), 3.48-3.58 (m, 2H), 3.63-3.76 (m, 2H), 6.92 (d, 2H, J = 9.0 H), 7.32 (d, 2H,
J = 8.7 Hz), 7.59 (d, 2H, 9.0 Hz), 7.89 (d, 2H, J = 9.0 Hz), 9.92 (s, IH), 10.13 (brs, IH).
Ia-163
mp 197-200 °C
1h-NMR (DMSO) 6 ppm: 1.26 (d, 6H, J = 6.3 Hz), 1.95-2.09 (m, 2H), 2.77-2.90 (m, 4H),
3.32 (m, IH), 7.17 (d, IH, J = 8.1 Hz), 7.32 (d, 2H, J = 8.7 Hz), 7.45 (d-d, IH, J = 1.8 Hz,
8.1 Hz), 7.64 (brs, IH), 7.90 (d, 2H, J = 8.7 Hz), 9.99 (brs, IH), 10.13 (brs, IH).
Ia-164
mp 145-247 °C
1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.3-2.0 (m, 16H), 2.19 (m, IH), 3.05 (m, IH), 4.74
(m, IH), 6.79 (d, IH, J=9.0), 6.80 (d, 2H, J=9.0), 7.47 (d, 2H, J=9.0), 9.63 (s, IH).
Ia-165
mp >300 °C
1h-NMR (DMSO) 6 ppm: 1.03-2.02 (m, 18H), 1.27 (s, 9H), 2.26 (m, IH), 3.06 (m, IH),
3.73 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.63 (d, 2H, J = 9.0 Hz), 7.78 (d, 2H, J = 8.7 Hz), 8.02
(d, IH, J = 8.1Hz), 10.00 (brs, IH).

Ia-166
mp 200-201 °C
*H-NMR (DMSO) 5 ppm: 1.03-2.02 (m, 18H), 1.27 (s, 9H), 2.25 (m, IH), 3.06 (m, IH),
3.73 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.33 (t, IH, J = 8.1 Hz), 7.46 (d, IH, J = 8.1 Hz), 7.76
(m, IH), 7.94 (m, IH), 8.14 (d, IH, J = 8.1 Hz), 9.92 (brs, IH).
Ia-167
mp 282-285 °C
1h-NMR (DMSO) 5 ppm: 1.22-1.57 (m, 4H), 1.27 (s, 9H), 1.87-2.03 (m, 4H), 2.49 (m, IH),
3.07 (m, IH), 6.83 (d, IH, J = 8.7 Hz), 13.20 (brs, IH).
la-168
mp 120-124 °C
1h-NMR (DMSO) 5ppm: 0.94-1.66 (m, 14H), 1.27 (s, 9H), 1.80-2.04 (m, 4H), 2.25 (mlH),
2.92 (m, IH), 3.06 (m, IH), 6.78 (d, IH, J = 8.7 Hz), 7.42-7.53 (m, 2H), 7.63 (d, IH, J = 7.2
Hz), 7.73 (m, IH), 8.17 (m, IH), 10.11 (brs, IH).
Ia-169
mp 256-257 °C
1h-NMR (DMSO) 6 ppm: 0.93-1.20 (m, 5H), 1.24-1.64 (m, 9H), 1.27 (s, 9H), 1.80-2.02 (m,
4H), 2.27 (m, IH), 2.87 (m, IH), 3.06 (m, IH), 6.79 (d, IH, J = 9.0 Hz), 7.48 (d, IH, J = 7.2
Hz), 7.68-7.79 (m, 4H), 10.17 (brs, IH).
Ia-171
mp 242-244 °C
1h-NMR (DMSO) 6 ppm: 1.27 (m, 12H), 1.45 (m, 4H), 1.90 (m, 4H), 2.25 (m, IH), 3.07
(m, IH), 3.67 (m, 2H), 6.77(d, IH, J=8.7), 6.90 (d, IH, J=7.8), 7.31 (t, IH, J=7.5), 7.53 (d,
IH, J=7.8), 7.59 (s,lH), 9.89 (s, IH).
Ia-172
mp >310 °C
1h-NMR (DMSO) 6 ppm: 1.27 (m, 12H), 1.38 (m, 4H), 1.84 (m, 2H), 1.97 (m,; 2H), 2.25

(m, IH), 3.07 (m, IH), 3.66 (m, 2H), 6.81 (d, IH, J=8.7), 7.20 (d, 2H, J=6.7), 7.61 (d, 2H,
J=8.7), 9.94 (s, IH).
Ia-173
mp 279-281 °C
1h-NMR (DMSO) 6ppm: 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.83 (m, 6H), 1.93 (m, 2H), 2.21
(m, IH), 2.36 (m, 2H), 3.05 (m, IH), 3.54 (m, 2H), 6.79 (d, IH, J=8.7), 7.16 (d, 2H, J=9.0),
7.56 (d, 2H, J=9.0), 9.83 (s, IH).
Ia-174
mp 258-262 °C
*H-NMR (DMSO) 5ppm: 0.29 (m, 2H), 0.53 (m,2H), 1.20 (m, IH), 1.27 (s, 9H), 1.3-1.5
(m, 4H), 1.7-2.0 (m, 4H), 2.20 (m, IH), 3.05 (m, IH), 3.75 (d, 2H, J=6.9), 6.79 (d, IH, J=9.0),
6.83 (d, 2H, J=9.0), 7.46 (d, 2H, J=9.0), 9.64 (s, IH).
Ia-175
mp 246-248 °C
1h-NMR (DMSO) 6ppm: 1.27 (s, 9H), 1.3-2.0 (m, 18H), 2.19 (m, IH), 3.04 (m, IH), 4.23
(m, IH), 6.79 (d, IH, J=8.7), 6.84 (d, 2H, J=9.0), 7.45 (d, 2H, J=9.0), 9.64 (s, IH).
Ia-176
mp 200-202 °C
XH-NMR (DMSO) Sppm: 1.27 (s, 9H), 1.3-2.0 (m, 18H), 2.21 (m, IH), 3.05 (m, IH), 4.23
(m, IH), 6.57 (d, IH, J=6.9), 6.80 (d, IH, J=9.0), 7.0-7.2 (m, 2H), 7.28 (s, IH), 9.74 (s, IH).
Ia-177
mp 266-268 °C
1h-NMR (DMSO) Sppm: 1.22-1.56 (m, 4H), 1.27 (s, 9H), 1.79-2.02 (m, 4H), 2.25 (m,lH),
3.05 (m, IH), 6.56 (m, IH), 6.77-6.84 (m, 2H), 7.58-7.71 (m, 5H), 9.92 (brs, IH).
Ia-178
mp 223-224 °C
1h-NMR (DMSO) 5 ppm: 1.26-1.54 (m,4H), 1.27 (s, 9H), 1.81-2.02 (m,4H), 2.45 (m, IH),

3.06 (m, IH), 6.80 (d, IH, J = 8.7 Hz), 8.15 (d-d, IH, J = 2.4 Hz, 9.0 Hz), 8.27 (d, IH, J =
9.0 Hz), 8.70 (m, IH), 10.85 (brs, IH).
Ia-179
mp 224-227 °C
1h-NMR (DMSO) 5ppm: 1.24-1.56 (m, 4H), 1.27 (s, 9H), 1.80-2.03 (m, 4H), 2.27 (m, IH),
3.06 (m, IH), 6.80 (d, IH, J = 8.7 Hz), 6.90 (d, IH, J = 1.8 Hz), 7.72-7.84 (m, 4H), 8.60 (d,
IH, J = 1.8 Hz), 10.09 (brs, IH).
Ia-180
mp 226-227 °C
1h-NMR (DMSO) 5 ppm: 0.92 (d, 6H, J = 6.6 Hz), 1.26-1.55 (m, 4H), 1.27 (s, 9H), 1.80-
2.03 (m, 4H), 2.27 (m, IH), 3.05 (m, IH), 3.20 (m, IH), 6.80 (d, IH, J = 8.7 Hz), 7.42 (d, IH,
J = 7.2 Hz), 7.67-7.79 (m, 4H), 10.19 (brs, IH).
Ia-181
mp 191-192 °C
1h-NMR (DMSO) 6 ppm: 0.95 (d, 6H, J = 6.6 Hz), 1.26-1.55 (m, 4H), 1.27 (s, 9H), 1.80-
2.03 (m, 4H), 2.25 (m, IH), 3.06 (m, IH), 3.23 (m, IH), 6.80 (d, IH, J = 8.4 Hz), 7.41-7.53
(m, 2H), 7.58 (d, IH, J = 7.2 Hz), 7.73 (m, IH), 8.18 (m, IH), 10.13 (brs, IH).
Ia-182
mp 192-193 °C
1h-NMR (DMSO) 5 ppm: 0.30 (m, 2H), 0.55 (m, 2H), 1.2-1.5 (m, 5H), 1.27 (s, IH), 1.8-
2.0 (m, 4H), 2.20 (m, IH), 3.04 (m, IH), 3.75 (d, 2H, J=6.9), 6.58 (m, IH), 6.79 (d, IH,
J=8.7), 7.0-7.2 (m, 2H), 7.31 (s, IH), 9.76 (s, IH).
Ia-183
mp>310°C
1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.3-1.5 (m,4H), 1.82 (m, 2H), 1.97 (m, 2H), 2.04
(m, 2H), 2.39 (m, IH), 2.46 (t, 2H, J=7.8), 3.07 (m, IH), 3.79 (t, 2H, J=7.5), 6.79 (d, IH,
J=8.7), 7.56 (m, 4H), 9.80 (s, IH).

Ia-184
mp 281-283 °C
1h-NMR (DMSO) 6 ppm: 1.24-1.57 (m, 4H), 1.27 (s, 9H), 1.80-2.04 (m, 4H), 2.27 (m, IH),
3.06 (m, IH), 6.80 (d, IH, J= 9,0 Hz), 7.33 (s, IH), 7.75 (d, 2H, J = 9.3 Hz), 7.91 (d, 2H, J =
8.7 Hz), 8.16 (s, IH), 10.09 (brs, IH).
Ia-185
mp 226-227 °C
1h-NMR (DMSO) 5 ppm: 1.24-1.58 (m, 10H), 1.27 (s, 9H), 1.81-2.02 (m, 4H), 2.28 (m,
IH), 2.78-2.88 (m, 4H), 3.06 (m, IH), 6.80 (d, IH, J = 8.7 Hz), 7.64 (d, 2H, J = 8.7 Hz), 7.82
(d, 2H, J = 8.7 Hz), 10.25 (brs, IH).
Ia-186
mp 148-150 °C
XH-NMR (DMSO) 6 ppm: 1.25-1.60 (m, 10H), 1.27 (s, 9H), 1.82-2.03 (m, 4H), 2.24 (m,
IH), 2.82-2.92 (m, 4H), 3.06 (m,lH), 6.79 (d, IH, J = 8.4 Hz), 7.36 (m, IH), 7.55 (t, IH, J =
7.8 Hz), 7.84 (m, IH), 8.06 (m, IH), 10.18 (brs, IH).
Ia-187
mp >310 °C
1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.36 (s, 9H), 1.43 (m,4H), 1.85 (m, 2H), 1.93 (m,
2H), 2.27 (m, IH), 3.06 (m, IH), 6.80 (d, IH, J=8.7), 7.58 (s, IH), 7.62 (d, 2H), 7.75 (d, 2H,
J=9.0), 10.00 (s, IH).
Ia-188
mp 285-292 °C
1h-NMR (DMSO) 5 ppm: 0.85 (t, 3H, J=7.5), 1.11 (d, 3H, J=6.3), 1.26 (s, 9H), 1,3-1.6 (m,
6H), 1.85 (m, 2H), 1.95 (m, 2H), 2.27 (m, IH), 3.06 (m, IH), 3.90 (m, IH), 6.80 (d, IH,
J=8.4), 7.64 (d, 2H, J=8.7), 7.79 (d, 2H, J=8.7), 7.99 (d, IH, J=8.1), 10.02 (s, IH).
la-189
mp 278-281 °C

1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.2-2.0 (m, 17H), 2.03 (m, 2H), 3.03 (m, IH), 6.79
(d, IH, J=8.4), 7.1-7.3 (m, 3H), 7.94 (s, IH), 9.78 (m, 2H).
Ia-190
mp >310 °C
XH-NMR (DMSO) 6 ppm: 1.1-2.0 (m, 17H), 1.27 (s, 9H), 2.25 (m, 2H), 3.03 (m, IH), 6.79
(d, IH, J=8.7), 7.48 (m, 4H), 9.71 (m, 2H).
Ia-191
mp 275-277 °C
1h-NMR (DMSO) 5ppm: 1.16 (d, 6H, J = 6.6 Hz), 1.31 (s, 9H), 4.09 (m, IH), 7.41 (d, 2H,
J = 8.7 Hz), 7.84 (s, 4H), 7.90 (d, 2H, J = 9.0 Hz), 8.11 (d, IH, J = 7.5 Hz), 10.04 (brs, IH),
10.30 (brs, IH).
Ia-192
mp 204-205 °C
XH-NMR (DMSO) 6 ppm: 1.15 (d, 6H, J = 6.6 Hz), 1.20-1.56 (m, 4H), 1.22 (d, 6H, J = 6.6
Hz), 1.78-2.00 (m, 4H), 2.25 (m, IH), 2.98-3.22 (m, 2H), 4.06 (m, IH), 6.99 (d, IH, J = 8.1
Hz), 7.34 (t, IH, J = 8.1 Hz), 7.46 (d, IH, J = 7.8 Hz), 7.75 (m IH), 7.96 (m, IH), 8.17 (d, IH,
J = 8.7 Hz), 9.94 (brs, IH).
Ia-193
mp 285-286 °C
1h-NMR (DMSO) 6 ppm: 1.15 (d, 6H, J = 6.6 Hz), 1.20-1.56 (m, 4H), 1.22 (d, 6H, J = 6.9
Hz), 1.79-2.00 (m, 4H), 2.26 (m, IH), 2.97-3.20 (m, 2H), 4.07 (m, IH), 6.99 (d, IH, J = 7.8
Hz), 7.64 (d, 2H, J = 8.7 Hz), 7.79 (d, 2H, J = 8.7 Hz), 8.06 (d, IH, J = 7.5 Hz), 10.02 (brs,
IH).
Ia-194
mp 248-250 °C
1h-NMR (DMSO) 6 ppm: 1.22-1.57 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.78-2.00 (m, 4H),
2.25 (m, IH), 2.98-3.22 (m, 2H), 6.56 (m, IH), 6.82 (d, IH, J = 3.3 Hz), 6.99 (d, IH, J = 7.8

Hz), 7.58- 7.71 (m, 5H), 9.92 (bra, IH).
la-195
mp 271-275 °C
1h-NMR (DMSO) 6ppm: 1.27 (s, 9H), 1.28-1.56 (m, 4H), 1.80-2.02 (m, 4H), 2.25 (m, IH),
3.06 (m, IH), 6.80 (d, IH, J = 9.0 Hz), 7.57 (s, IH), 7.62-7.74 (m, 4H), 8.39 (s, IH), 9.99 (brs,
IH).
Ia-196
mp 226-228 °C
1h-NMR (CDCI3) 6 ppm: 0.30 (m, 2H), 1.23 (d, 6H, J=6.9), 1.2-2.0 (m, 4H), 2.20 (m, IH),
3.10 (m, 2H), 3.76 (d, 2H, J=6.9), 6.83 (d, 2H, J=8.7), 6.99 (d, IH, J=8.1), 7.46 (d, 2H,
J=8.7), 9.65 (s, IH).
Ia-197
mp 173-175 °C
1h-NMR (DMSO) 6 ppm:0.31 (m, 2H), 0.56 (m, 2H), 1.22 (d, 6H, J=6.6), 1.2-1.5 (m, 4H),
1.8-2.0 (m, 4H), 2.22 (m, IH), 3.10 (m, IH), 3.76 (d, IH, J=7.2), 6.58 (d, IH, J=8.1), 7.0-7.2
(m, 2H), 7.32 (s, IH), 9.78 (s, IH).
Ia-198
mp 233-235 °C
1h-NMR (DMSO) 6 ppm: 1.25 (d, 6H, J=6.9), 1.2-2.0 (m, 16H), 2.19 (m, IH), 3.10 (m,
2H), 4.73 (m, IH), 6.80 (d, 2H, J=8.7), 6.98 (d, IH, J=7.8), 7..45 (d, 2H, J=8.7), 9.63 (s, IH).
Ia-199
mp 185-186 °C
1h-NMR (DMSO) 5 ppm: 1.22 (d, 6H, J=6.9), 1.2-2.0 (m, 16H), 2.22 (m, IH), 3.10 (m,
2H), 4.73 (m, IH), 6.54 (m, IH), 7.0-7.2 (m, 2H), 7.3 (s, IH), 9.75 (s ,1H).
Ia-200
mp 235-237 °C
1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.3-1.6 (m, 6H), 1.8-2.0 (m, 6H), 2.20 (m, IH),

3.05 (m, IH), 3.45 (m, 2H), 3.82 (m, 2H), 4.47 (m, IH), 6.79 (d, IH, J=9.0), 6.89 (d, 2H,
J=9.0), 7.47 (d, 2H,J=9.0), 9.66 (s, IH).
Ia-201
mp 300-301 °C
1h-NMR (DMSO) 5 ppm: 1.15 (d, 6H, J = 6.6 Hz), 1.26-1.56 (m, 4H), 1.27 (s, 9H), 1.82-
2.03 (m, 4H), 2.23 (s, 3H), 2.37 (m, IH), 3.06 (m, IH), 4.07 (m, IH), 6.81 (d, lH, J = 8.7 Hz),
7.52 (d, IH, J = 8.4 Hz), 7.62 (d, IH, J = 8.4 Hz), 7.68 (s, IH), 8.09 (d, IH, J = 7.5 Hz), 9.22
(brs, IH).
Ia-202
mp 269-270 °C
1h-NMR (DMSO) 5 ppm: 1.25-1.26 (m, 4H), 1.27 (s, 9H), 1.80-2.03 (m, 4H), 2.25 (m, IH),
3.07 (m, IH), 6.80 (d, IH, J = 8.4 Hz), 7.11 (m, IH), 7.42 (d, IH, J = 3.6 Hz), 7.48 (m, IH),
7.58 (d, 2H, J = 8.7 Hz), 7.64 (d, 2H, J = 8.4 Hz), 9.92 (brs, IH).
Ia-203
mp 271-273 °C
4i-NMR (DMSO) 5 ppm: 1.14-1.54 (m, 9H), 1.26 (s, 9H), 1.63-1.88 (m, 7H), 1.89-2.01 (m,
2H), 2.21 (m, IH), 2.42 (m, IH), 3.04 (m, IH), 6.79 (d, IH, J = 9.0 Hz), 7.11 (d, 2H, J = 8.4
Hz), 7.47 (d, 2H, J = 8.1 Hz), 9.70 (brs, lH).
Ia-204
mp 250-251 °C
1h-NMR (DMSO) 6 ppm: 1.22-1.39 (m, 2H), 1.22 (d, 6H, J = 6.6 Hz), 1.40-1.57 (m 2H),
1.80-2.01 (m, 4H), 2.28 (m, lH), 2.98-3.21 (m, 2H), 7.00 (d, IH, J = 7.8 Hz), 7.34 (s, IH),
7.75 (d, 2H, J = 9.0 Hz), 7.91 (d, 2H, J = 8.7 Hz), 8.17 (s, lH), 10.10 (brs, IH).
Ia-205
mp 239-240 °C
XH-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.2-1.5 (m, 4H), 1.8-2.0 (m, 5H), 2.08 (m, 2H),
3.05 (m, IH), 3.80 (m, 4H), 4.95 (m, IH), 6.79 (d, IH, J=8.7), 6.83 (d, 2H, J=8.7), 7.48 (d,

2H, J=8.7), 9.66 (s, IH).
Ia-206
mp 236-238 °C
1h-NMR (DMSO) 5 ppm: 1.27 (s, 9H), 1.2-1.7 (m, 8H), 1.8-2.0 (m, 6H), 2.18 (m, IH), 3.04
(m, IH), 3.3-3.6(m, 2H), 3.85 (m, 3H), 6.80 (d, IH, J=9.0), 6.84 (d, 2H, J=9.0), 7.47 (d, 2H,
J=9.0), 9.65 (s, IH).
Ia-207
mp 224-226 °C
1h-NMR (DMSO) 5 ppm: 1.27 (s, 9H), 1.2-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.24(m, IH), 2.39
(m, 2H), 3.06 (m, IH), 3.50 (t, 2H, J=7.5), 3.70 (t, 2H, J=6.3), 6.78 (d, IH, J=6.6), 6.83 (m,
IH), 7.25 (m, IH), 7.27 (m, IH), 7.54 (s,lH), 9.61 (s, IH).
Ia-208
mp 275-277 °C
1h-NMR (DMSO) 5 ppm: 1.27 (s, 9H), 1.3-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.22 (m, IH),
2.38 (m, 2H), 3.07 (m, IH), 3.47 (t, 2H, J=6.9), 3.69 (t, 2H, J=6.6), 6.80 (d, IH, J=8.7), 7.14
(d, 2H, J=8.4), 7.58 (d, 2H, J=8.4), 9.83 (s, IH).
Ia-209
mp 214-215 °C
1h-NMR (DMSO) 6 ppm: 1.26-1.56 (m, 4H), 1.27 (s, 9H), 1.80-2.03 (m, 4H), 2.25 (m, IH),
3.06 (m, IH), 6.59 (m, IH), 6.81 (d, IH, J = 8.4 Hz), 6.86 (d, IH, J = 2.7 Hz), 7.28-7.40 (m,
2H), 7.47 (m, IH), 7.75 (s, IH), 8.01 (s, IH), 9.91 (brs, IH).
Ia-210
mp 272-275 °C
1h-NMR (DMSO) 6 ppm: 1.31 (s, 9H), 6.59 (m, IH), 6.87 (d, IH, J = 3.3 Hz), 7.41 (d, 2H,
J = 8.7 Hz), 7.68 (d, 2H, J = 8.7 Hz), 7.72 (m, IH), 7.83 (d, 2H, J = 8.7 Hz), 7.90 (d, 2H, J =
8.7 Hz), 10.03 (brs, IH), 10.22 (brs, IH).
Ia-211

mp 251-255 °C
1h-NMR (DMSO) 5 ppm: 1.31 (s, 9H), 7.36 (s, IH), 7.41 (d, 2H, J = 8.4 Hz), 7.91 (d, 2H,
J = 8.4 Hz), 7.92-8.00 (m, 4H), 8.19 (s, IH), 10.06 (brs, IH), 10.38 (brs, IH).
Ia-212
mp 241-244 °C
1h-NMR (DMSO) 6 ppm: 1.30 (s, 9H), 1.50-1.78 (m, 6H), 1.81-1.97 (m, 2H), 4.78 (m, IH),
6.87 (d, 2H, J = 9.0 Hz), 7.38 (d, 2H, J = 8.7 Hz), 7.61 (d, 2H, J = 9.0 Hz), 7.87 (d, 2H, J =
8.7 Hz), 9.97 (brs, IH), 9.99 (brs, IH).
Ia-213
mp 283-286 °C
*H-NMR (DMSO) 5 ppm: 1.31 (s, 9H), 7.12 (d-d, IH, J = 3.6 Hz, 5.1 Hz), 7.41 (d, 2H, J =
9.0 Hz), 7.46 (m, IH), 7.50 (d-d, IH, J = 1.2 Hz, 5.1 Hz), 7.64 (d, 2H, J = 8.7 Hz), 7.82 (d,
2H, J = 8.7 Hz), 7.90 (d, 2H, J = 9.3 Hz), 10.03 (brs, IH), 10.22 (brs, IH).
Ia-216
mp 224-225°C
1h-NMR (CDCI3) 6 ppm: 1.22 (d, 6H, J=6.9), 1.2-1.5 (m, 4H), 1.8-2.0 (m, 4H), 2.45 (m,
IH), 3.12 (m, 2H), 6.99 (d, IH, J=8.1), 8.15 (m, IH), 8.27 (d, IH, J=9.0), 8.69 (s, IH), 10.86
(s, IH).
Ia-219
mp 270-272 °C
1h-NMR (DMSO) 6 ppm: 1.28 (s, 9H), 1.34-1.51 (m, 2H), 1.80-1.92 (m, 2H), 2.83- 2.97
(m, 2H), 3.32 (m, IH), 3.99-4.12 (m 2H), 6.92 (d, IH, J = 8.7 Hz), 7.57 (d, 2H, J = 8.7 Hz),
7.68 (d, 2H, J = 9.0 Hz), 8.90 (brs, IH).
Ia-220
mp 187-189 °C
1h-NMR (DMSO) 6 ppm: 1.28 (s, 9H), 1.31-1.51 (m, 2H), 1.78-1.90 (m, 2H), 2.78-2.93 (m,
2H), 3.30 (m, IH), 3.97-4.09 (m, 2H), 6.90 (d, IH, J = 8.7 Hz), 7.06 (t, 2H, J = 9.0 Hz), 7.44

(d-d, 2H, J = 4.8 Hz, 9.0 Hz), 8.53 (brs, IH).
Ia-221
mp 260-262 °C
:H-NMR (DMSO) 5 ppm: 1.12-1.50 (m, 7H), 1.28 (s, 9H), 1.63-1.90 (m, 7H), 2.40 (m, IH),
2.76-2.91 (m, 2H), 3.28 (m, IH), 3.96-4.09 (m, 2H), 6.90 (d, IH, J = 8.7 Hz), 7.06 (d, 2H, J =
8.4 Hz), 7.32 (d, 2H, J = 8.4 Hz), 8.40 (brs, IH).
Ia-222
mp 265-267 °C
1h-NMR (DMSO) 6 ppm: 1.23 (d, 6H, J = 6.6 Hz), 1.31-1.48 (m, 2H), 1.77-1.90 (m, 2H),
2.84-2.98 (m, 2H), 3.16 (m, IH), 3.33 (m, IH), 3.96-4.10 (m, 2H), 7.11 (d, IH, J = 7.8 Hz),
7.57 (d, 2H, J = 8.7 Hz), 7.67 (d, 2H, J = 8.4 Hz), 8.90 (brs, IH).
Ia-223
mp 183-186 °C
1h-NMR (DMSO) 6 ppm: 1.23 (d, 6H, J = 6.9 Hz), 1.28-1.47 (m, 2H), 1.76-1.88 (m, 2H),
2.80-3.16 (m, 2H), 3.16 (m, IH), 3.32 (m, IH), 3.94-4.07 (m, 2H), 7.00-7.14 (m, 3H), 7.44
(d-d, 2H, J = 4.8 Hz, 9.0 Hz), 8.53 (brs, IH).
Ia-224
mp 232-234 °C
1h-NMR (DMSO) 6 ppm: 1.12-1.46 (m, 7H), 1.23 (d, 6H, J = 6.6 Hz), 1.63-1.87 (m, 7H),
2.40 (m, IH), 2.78-2.93 (m, 2H), 3.15 (m,lH), 3.31 (m,lH), 3.94-4.07 (m, 2H), 7.06 (d, 2H, J
= 8.4 Hz), 7.09 (d, IH, J = 8.1 Hz), 7.32 (d, 2H, J = 8.4 Hz), 8.39 (brs, IH).
Ia-225
mp 222-224 °C
1h-NMR (DMSO) 6 ppm: 1.28 (s, 9H), 1.30-1.61 (m, 4H), 1.77-1.98 (m, 4H), 2.66-2.90 (m,
2H), 3.28 (m, IH), 3.40-3.50 (m, 2H), 3.79-3.88 (m, 2H), 3.96-4.08 (m, 2H), 4.44 (m, IH),
6.85 (d, 2H, J = 9.0 Hz), 6.91 (d, IH, J = 9.0 Hz), 7.31 (d, 2H, J = 9.3 Hz), 8.34 (brs, IH).
Ia-226

mp 194-195 °C
1h-NMR (CDCI3/DMSO) 5 ppm: 1.39 (d, 6H, J = 7.2 Hz), 1.66 (quintet, 2H, J = 6.8 Hz),
1.87 (quintet, 2H, J = 7.7 Hz), 2.47 (t, 2H, J = 7.5 Hz), 3.11-3.22 (m, IH), 3.21 (t, 2H, J =
6.2 Hz), 5.00 (brs, IH), 7.35-7.56 (m, 5H), 7.86 (d, IH, J = 8.4 Hz), 8.05 (dd, IH, J = 1.8, 8.1
Hz), 8.20 (d, IH, J = 1.8 Hz), 9.24 (s, IH).
Ia-227
mp >300 °C
1h-NMR (DMSO) 6 ppm: 1.22 (d, 6H, J = 6.3 Hz), 1.20-1.40 (m, 4H), 1.74-2.10 (m, 4H),
2.20-2.40 (m, IH), 2.39 (s, 3H), 3.00-3.30 (m, 2H), 6.25 (s, IH), 6.99 (brs, IH), 7.43-7.57 (m,
IH), 7.71 (d, IH, J = 8.1 Hz), 7.76 (s, IH), 10.27 (s, IH).
Ia-228
mp 168-169 °C
1h-NMR (DMSO) 6 ppm: 1.26 (s, 9H), 1.49 (quintet, 2H, J = 7.5 Hz), 1.64 (quintet, 2H, J
= 7.4 Hz), 2.38 (t, 2H, J = 7.2 Hz), 2.40 (s, 3H), 3.04 (q, 2H, J = 6.5 Hz), 6.25 (s, IH), 6.89 (t,
IH, J = 6.0 Hz), 7.48 (dd, IH, J = 1.8, 8.4 Hz), 7.71 (d, IH, J = 8.4 Hz), 7.77 (d, IH, J = 1.8
Hz), 10.33 (s, IH).
Ia-229
mp 174-175 °C
1h-NMR (DMSO) 5 ppm: 1.21 (d, 6H, J = 6.6 Hz), 1.42-1.56 (m, 2H), 1.56-1.70 (m, 2H),
2.33-2.42 (m, 2H), 2.40 (s, 3H), 2.90-3.02 (m, 2H), 3.14 (septet, IH, J = 6.5 Hz), 6.26 (s, IH),
6.99 (brs, IH), 7.48 (d, IH, J = 8.4 Hz), 7.71 (d, IH, J = 8.7 Hz), 7.77 (s, IH), 10.33 (s, IH).
Ia-230
mp 194-195 °C
1h-NMR (DMSO) 5 ppm: 0.86 (d, 6H, J = 6.9 Hz), 1.25-1.65 (m, 4H), 1.27 (s, 9H), 1.81-
2.05 (m, 5H), 2.23-2.35 (m, IH), 2.99-3.15 (m, IH), 3.36 (d, 2H, J = 7.2 Hz), 6.80 (d, IH, J =
8.4 Hz), 7.80 (d, IH, J = 8.4 Hz), 7.87 (d, IH, J = 8.4 Hz), 8.19 (s, IH), 10.44 (s, IH).
Ia-231

mp 221-222 °C
1h-NMR (DMSO) 6 ppm: 0.86 (d, 6H, J = 6.9 Hz), 1.22-1.40 (m, 2H), 1.23 (d, 6H, J = 6.9 Hz), 1.40-1.58 (m, 2H), 1.82-2.04 (m, 5H), 2.22-2.37 (m, IH), 3.00-3.16 (m, IH), 3.15 (septet, IH, J = 6.6 Hz), 3.36 (d, 2H, J = 7.5 Hz), 6.99 (d, IH, J = 7.5 Hz), 7.80 (d, IH, J =
8.4 Hz), 7.86 (d, IH, J = 8.4 Hz), 8.19 (s, IH), 10.45 (s, IH).
Ia-232
mp 196-197 °C
1h-NMR (CDCI3) 6 ppm: 0.93 (d, 6H, J = 6.6 Hz), 1.42 (s, IH), 1.60-1.70 (m, 2H), 1.88
(quintet, 2H, J = 7.4 Hz), 2.02-2.20 (m, IH), 2.46 (t, 2H, J = 7.7 Hz), 3.29 (q, 2H, J = 6.1
Hz), 3.48 (d, 2H, J = 7.8 Hz), 4.26 (t, IH, J = 6.0 Hz), 7.76 (d, IH, J = 8.1 Hz), 7.90 (dd, IH,
J = 1.8, 8.1 Hz), 8.07 (d, IH, J = 1.5 Hz), 8.39 (s, IH).
Ia-233
p. 151-152 °C
1h-NMR (CDCI3) 5 ppm: 0.93 (d, 6H, J = 6.6 Hz), 1.40 (d, 6H, J = 6.6 Hz), 1.62-1.69 (m,
2H), 1.88 (quintet, 2H, J = 7.3 Hz), 2.03-2.16 (m, IH), 2.47 (t, 2H, J = 7.5 Hz), 3.21 (septet,
IH, J = 6.8 Hz), 3.23 (q, 2H, J = 6.3 Hz), 3.48 (d, 2H, J = 7.5 Hz), 4.43 (t, IH, J = 6.0 Hz),
7.76 (d, IH, J = 8.4 Hz), 7.91 (dd, IH, J = 1.8, 8.4 Hz), 8.06 (d, IH, J = 1.8 Hz), 8.36 (s, IH).
Ia-234
mp 219-220 °C
1h-NMR (DMSO-d6) 6 ppm: 1.28 (s, 9H), 1.30-1.50 (m, 2H), 1.74-1.88 (m, 2H), 2.83 (t,
2H, J= 11.1 Hz), 3.20-3.32 (m, IH), 3.94-4.07 (m, 2H), 5.94 (s, 2H), 6.77 (d, IH, J = 8.8 Hz),
6.82 (dd, IH, J = 1.8, 8.7 Hz), 6.89 (d, IH, J = 8.7 Hz), 7.11 (d, IH, J = 1.8 Hz), 8.38 (s, IH).
Ia-235
mp 280-282 °C
XH-NMR (DMSO-d6) 6 ppm: 1.27 (s, 9H), 1.26-1.57 (m, 4H), 1.86-2.03 (m, 4H), 2.38-2.50
(m, IH), 3.00-3.14 (m, IH), 6.81 (d, IH, J = 8.4 Hz), 7.29 (t, IH, J = 8.4 Hz), 7.43 (t, IH, J =
7.5 Hz), 7.73 (d, IH, J = 8.4 Hz), 7.96 (d, IH, J = 7.5 Hz), 12.27 (s, IH).

Ia-237
mp 204-205 °C
1h-NMR (DMSO) 6 ppm: 1.23 (d, 6H, J = 6.6 Hz), 1.29-1.61 (m, 4H), 1.75-1.98 (m, 4H),
2.78-2.92 (m, 2H), 3.15 (m, IH), 3.29 (m, IH), 3.38-3.51 (m, 2H), 3.78-3.89 (m, 2H), 3.94-
4.06 (m, 2H), 4.44 (m, IH), 6.85 (d, 2H, J = 9.0 Hz), 7.10 (d, IH, J = 7.8 Hz), 7.31 (d, 2H, J
= 9.3 Hz), 8.34 (brs, IH).
Ia-238
mp 128-130 °C
1h-NMR (DMSO) 6 ppm: 1.26 (s, 9H), 1.41-1.53 (m, 2H), 1.55-1.68 (m, 2H), 2.44 (t, 2H,
J = 7.2 Hz), 2.98-3.07 (m, 2H), 6.90 (t, IH, J = 6.0 Hz), 8.16 (d-d, IH, J = 2.1 Hz, 8.7 Hz),
8.29 (d, IH, J = 8.7 Hz), 8.70 (m, IH), 10.91 (brs, IH).
Ia-239
mp 256-258 °C
J-H-NMR (DMSO) 5 ppm: 1.26-1.53 (m, 4H), 1.26 (s, 9H), 1.76-2.00 (m, 4H), 2.23 (s, 3H),
2.39 (m, IH), 3.04 (m, IH), 6.80 (d, IH, J = 8.7 Hz), 7.57 (d-d, IH, J = 2.4 Hz, 8.4 Hz), 7.97
(d, IH, J = 8.4 Hz), 8.12 (m, IH), 10.26 (brs, IH).
Ia-240
mp 288-290 °C
1h-NMR (DMSO) 6 ppm: 1.26-1.53 (m, 4H), 1.27 (s, 9H), 1.78-1.90 (m, 4H), 2.40 (m, IH),
3.04 (m, IH), 6.81 (d, IH, J = 8.7 Hz), 7.07 (m, IH), 7.75 (m, IH), 8.07 (d, IH, J = 8.4 Hz),
8.29 (m, IH), 10.36 (brs, IH).
Ia-241
mp 249-250 °C
XH-NMR (DMSO) 6 ppm: 1.28 (s, 9H), 1.34-1.50 (m, 2H), 1.79-1.90 (m, 2H), 2.74-2.98 (m,
2H), 3.32 (m, IH), 4.02-4.14 (m, 2H), 6.91 (d, IH, J = 8.4 Hz), 7.94 (d, IH, J = 9.0 Hz), 8.04
(d-d, IH, J = 2.1 Hz, 9.0 Hz), 8.60 (s, IH), 9.76 (brs, IH).
Ia-242

mp 250-252 °C
2H-NMR (DMSO) 5 ppm: 1.24 (s, 9H), 1.27 (s, 9H), 1.24-1.54 (m, 4H), 1.76-1.88 (m, 2H),
1.90-2.01 (m, 2H), 2.21 (m, IH), 3.05 (m, IH), 6.79 (d, IH, J = 8.7 Hz), 6.88 (d, 2H, J = 9.0
Hz), 7.48 (d, 2H, J = 9.0 Hz), 9.72 (brs, IH).
136-0290
mp 250-252 °C
*H-NMR (DMSO) 6 ppm: 1.15 (d, 6H, J = 6.6 Hz), 1.28 (s, 9H), 1.35-1.52 (m, 2H), 1.78-
1.92 (m, 2H), 2.20 (s, 3H), 2.81-2.96 (m, 2H), 3.33 (m, IH), 3.96-4.16 (m, 3H), 6.92 (d, IH, J
= 8.7 Hz), 7.27 (d, IH, J = 8.1 Hz), 7.60 (m, IH), 7.66 (m, IH), 8.06 (d, IH, J = 7.8 Hz), 8.14
(brs, IH).
Ia-244
mp 211-213 °C
1h-NMR (DMSO) 6 ppm: 1.29 (s, 9H), 1.35-1.52 (m, 2H), 1.81-1.93 (m, 2H), 2.83-2.97 (m,
2H), 3.32 (m, IH), 4.03-4.14 (m, 2H), 6.93 (d, IH, J = 8.7 Hz), 7.55 (d-d, IH, J = 2.1 Hz, 9.0
Hz), 7.94 (d, IH, J = 9.0 Hz), 8.29 (d, IH, J = 1.8 Hz), 8.78 (brs, IH), 9.19 (s, IH).
Ia-245
mp 196-197°C
1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.2-1.6 (m, 6H), 1.8-2.0 (m, 6H), 2.23 (m, IH),
3.05 (m, IH), 3.73 (m, 4h), 4.99 (s, IH), 6.79 (d, IH, J=8.7), 7.13 (d, IH, J=6.8), 7.22 (t, IH,
J=6.8), 7.49 (d, IH, J=6.8), 7.72 (s, IH), 9.78 (s, IH).
Ia-246
mp 242-244 °C
1h-NMR (DMSO) 6 ppm: 1.27 (s, 9H), 1.2-1.5 (m, 4H), 1.65 (m, 4H), 1.8-2.0 (m, 4H),
2.23 (m, IH), 2.71 (m, IH), 3.06 (m, IH), 3.43 (m, 2H), 3.93 (m, 2H), 6.79 (d, IH, J=8.7),
6.91 (d, IH, J=8.7), 7.20 (t, IH, J=7.5), 7.40 (d, IH, J=7.5), 7.53 (s, IH), 9.76 (s, IH).
Ia-247
mp 242-245°C

1h-NMR (DMSO) 5 ppm: 1.27 (s, 9H), 1.2-1.6 (m, 6H), 1.8-2.0 (m, 6H), 2.23 (m, IH),
3.05 (m, IH), 3.74 (m, 4H), 4.94 (brs, IH), 6.79 (d, lh, J=8.7), 7.38 (d, IH, J=8.7), 7.52 (d,
IH, J=8.7), 9.76 (s, IH).
Ia-248
mp 272-274 °C
1h-NMR (CDC13) 6 ppm: 1.27 (s, 9H), 1.2-1.5 (m, 4H), 1.62 (m, 4H), 1.8-2.0 (m, 4H),
2.22 (m, IH), 2.68 (m, IH), 3.05 (m, IH), 3.41 (m, 2H), 3.92 (m, 2H), 6.79 (d, IH, J=9.0),
7.15 (d, 2H, J=8.7), 7.50 (d, 2H, J=8.7), 9.73(s, IH).
Ia-249 mp 174-176 °C
Ia-250mp 255-257 °C
Ia-252 mp 249-251 °C
Ia-253 mp 120-121 °C
Ia-254 mp 236-237 °C
Ia-255 mp 172-174 °C
Ia-256 mp 257-259 °C
Ia-257 mp 179-180 °C
Ia-258 mp 227-229 °C
Ia-259mp 135-136 °C
Experiment 1 Affinity for NPY Y5 receptor
cDNA sequence encoding a human NPY Y5 receptor (W096/16542) was cloned in the expression vector pMEl8S (Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into a host CHO cells by using a Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to an instruction protocol to obtain the cells that stably express NPY Y5 receptor.
The membranes prepared from the above CHO cells expressing NPY Y5 receptor, the compound of the present invention and 30,000 cpm [125x] peptide YY (60 pM of final

concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25 °C for 2 hours, and then the mixture was filtered with a glassfilter GF/C treated with polyethyleneimine. After the glassfilter was washed with 50 mM Tris-HCl buffer (pH 7.4), the radioactivity on the filter was measured with a gamma counter. The non-specific binding was detected in the presence of 200 nM of peptide YY. The 50 % inhibitory concentration of the test compound against the specific peptide YY binding (IC50 value) was calculated (Inui, A. et al. Endocrinology 131, 2090 - 2096 (1992)). The results are shown in Tables 1 and 2. The compounds of the present invention inhibited the binding of peptide YY (NPY homologue) to NPY Y5 receptors. In other words, the compounds of the present invention showed affinity for the NPY Y5 receptor.
Experiment 2 cAMP production inhibitory activity in CHO cells
After CHO cells expressing human NPY Y5 receptor were incubated in the presence of 2.5 mM isobutylmethylxanthine (SIGMA) at 37 °C for 20 min, the compound of the present invention was added and incubated for 5 min. Then, 50 nM NPY and 10 uM forskolin (SIGMA) were added to the cells and incubated for 30 min. After the reaction was terminated by adding IN HCl, the amount of cAMP in the supernatant was measured with EIA kit (Amersham LIFE SCIENCE). The inhibitory activity of NPY against forskolin stimulated cAMP was regarded as 100 % and the 50 % inhibitory concentration (IC50 value) of the compound of the present invention against the NPY activity was calculated. The results are shown in Tables 1 to 4.

Experiment 3
Using the membranes prepared from Yl-expression cells (human neuroblastoma, SK-N-MC) and the membranes prepared from Y2-expression cells (human neuroblastoma, SMS-KAN), the experiment was carried out in a similar way as Experiment 1 to determine the affinity for NPY Yl receptor and NPY Y2 receptor.
Binding IC 50 values for NPY Yl and NPY Y2 receptors of 1-27,1-32,1-41,1-45,1-46, 1-47,1-48,1-49,1-59,1-61,1-63, 1-64,1-66,1-69,1-72,1-152,1-154,1-204,1-205,1-212, Ia-3, Ia-5, Ia-6, Ia-12, Ia-16, Ia-17, Ia-20, Ia-21, Ia-22, Ia-26, Ia-28, Ia-29, Ia-30, Ia-31, Ia-32, Ia-33, Ia-37, Ia-39, Ia-40, Ia-50, Ia-51, Ia-54, Ia-62, Ia-67, Ia-124, Ia-126, Ia-139, Ia-140, Ia-142, Ia-178, Ia-199 and Ia-200 were 100,000 nM or higher and each compound had a selectivity for NPY Y5 receptor.
Formulation Example 1 Tablets
Compound (1-1) 15 mg
Starch 15 mg
Lactose 15 mg
Crystalline cellulose 19 mg
Polyvinyl alcohol 3 mg
Distilled water 30 ml
Calcium stearate 3 mg
After all of the above ingredients except for calcium stearate are uniformly mixed, the mixture is crushed and granulated, and dried to obtain a suitable size of granules. After calcium stearate is added to the granules, tablets are formed by compression molding.
Formulation Example 2 Capsules
Compound (1-2) 10 mg

Magnesium stearate 10 mg
Lactose 80 mg
After the above ingredients are mixed to prepare powders or granules, the obtained are filled in capsules.
Formulation Example 3 Granules
Compound (1-3) 30 g
Lactose 265 g
Magnesium Stearate 5 g
After the above ingredients are mixed uniformly and formed by compression molding, the obtained are crushed, granulated and sieved to prepare suitable volume of granules.
Industrial Applicability
As shown in the above Experiments, the compounds of the present invention have an NPY Y5 receptor antagonistic activity. Therefore, the compounds of the present invention are useful as an anti-obestic agent and anorectic agent.

WE CLAIM:
1. A compound of formula I which is an NPY Y5 receptor antagonist

wherein R1 is optionally substituted lower alkyl, optionally substituted
cycloalkyl or optionally substituted aryl,
R2 is hydrogen or lower alkyl, and R1 and R2 taken together may form lower
alkylene, n is 1 or 2,
X is optionally substituted lower alkylene,
optionally substituted lower alkenylene,
optionally substituted -CO-lowcr alkylene,
optionally substituted -CO-lower alkenylene or

wherein R3, R4, R5 and R6 are each independently hydrogen or lower alkyl,

is optionally substituted cycloalkylene, optionally substituted cycloalkenylene, optionally substituted bicycloalkylene, optionally substituted arylene or optionally substituted heterocyclediyl and p and q are each independently 0 or

wherein

is piperidinediyl, piperazinediyl, pyridinediyl, pyrazinediyl, pyrrolidinediyl or
pyrrolediyl and U is single bond, lower alkylene or lower alkenylene,
Y is OCONR7, CONR7, CSNR7, NR7CO or NR7CS,
R is hydrogen or lower alkyl, and
Z is optionally substituted lower alkyl, optionally substituted lower alkenyl,
optionally substituted amino, optionally substituted lower alkoxy, optionally
substituted carbocyclyl or optionally substituted heterocyclyl.
2. The compound as claimed in claim 1, wherein R2 is hydrogen or lower alkyl and Z is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted carbocyclyl, optionally substituted heterocyclyl or optionally substituted amino, provided that R1 is optionally substituted C3 to CKJ alkyl when Z is optionally substituted amino.
3. The compound as claimed in claim 1, wherein R1 is optionally substituted lower alkyl or optionally substituted cycloalkyl, X is optionally substituted lower alkylene, optionally substituted lower alkenylene or

is the same as claimed in claim 1, and
Z is optionally substituted lower alkyl, optionally substituted carbocyclyl or
optionally substituted heterocyclyl.

4. The compound as claimed in any one of claims 1 to 3, wherein R is optionally substituted C3 to C10 alkyl.
5. The compound as claimed in any one of claims 1 to 4, which is an anti-obestic agent.
6. The compound as claimed in any one of claims 1 to 4, which is an anorectic agent.
7. The compound of the formula (I) as claimed in claim 1,

wherein X is C2 to C6 alkylene or C3 to C6 alkenylene, R1 is optionally substituted C3 to C10 alkyl or optionally substituted C5 to C6 cycloalkyl and the other symbols are the same as claimed in claim 1, provided that Z is not lower alkylphenylamino, hydroxy(lower)alkylphenylamino and acylphenylamino when Y is NR CO, prodrug, pharmaceutical^ acceptable salt or solvate thereof.
8. The compound as claimed in claim 7, wherein Z is optionally substituted lower alkyl or optionally substituted phenyl, prodrug, pharmaceutically acceptable salt or solvate thereof.
9. The compound of the formula (I) as claimed in claim 1,

wherein X is

is optionally substituted cyclcoalkylene, optionally substituted cycloalkenylene, optionally substituted bicycloalkylene or optionally substituted piperidinylene, R1 is optionally substituted C3 to C10 alkyl or optionally substituted C5 to C6 cycloalkyl and the other symbols are the same as claimed in claim 1, prodrug, pharmaceutically acceptable salt or solvate thereof.
10. The compound as claimed in claim 9, wherein

is optionally substituted cyclohexylene or optionally substituted piperidinylene and p and q are simultaneously 0, prodrug, pharmaceutically acceptable salt or solvate thereof.
11. The compound as claimed in claim 9 or 10, wherein Y is CONH, prodrug, pharmaceutically acceptable salt or solvate thereof.
12. The compound as claimed in any one of claims 9 to 11, wherein Z is optionally substituted lower alkyl, optionally substituted phenyl, optionally substituted pyridyl or optionally substituted benzopyranyl, prodrug, pharmaceutically acceptable salt or solvate thereof.

13. The compound of the formula (I):

R1 is optionally substituted C3 to C10 alkyl or optionally substituted C5 to C6
cycloalkyl,
Z is p-lower alkylphenyl and the other symbols are the same as claimed in
claim 1, provided that Z is not p-n-butylphenyl when R1 is isopropyl, prodrug,
pharmaceutical^ acceptable salt or solvate thereof.
14. The compound of the formula (I) as claimed in claim 1,

is heteroarylene, R1 is optionally substituted C3 to C10 alkyl or optionally substituted C5 to C6 cycloalkyl and the other symbols are the same as claimed in claim 1.
-747-

15. The compound as claimed in 14, wherein

is thiophenediyl or furandiyl, prodrug, pharmaceutically acceptable salt or solvate thereof.

Documents:

in-pct-2002-0781-che abstract duplicate.pdf

in-pct-2002-0781-che abstract.pdf

in-pct-2002-0781-che claims duplicate.pdf

in-pct-2002-0781-che claims.pdf

in-pct-2002-0781-che correspondence others.pdf

in-pct-2002-0781-che correspondence po.pdf

in-pct-2002-0781-che description (complete) duplicate-1.pdf

in-pct-2002-0781-che description (complete) duplicate-2.tif

in-pct-2002-0781-che description (complete) duplicate-3.pdf

in-pct-2002-0781-che description (complete) duplicate-4.pdf

in-pct-2002-0781-che description (complete) duplicate.pdf

in-pct-2002-0781-che description (complete)-1.pdf

in-pct-2002-0781-che description (complete)-2.pdf

in-pct-2002-0781-che description (complete)-3.pdf

in-pct-2002-0781-che description (complete)-4.pdf

in-pct-2002-0781-che description (complete).pdf

in-pct-2002-0781-che form-1.pdf

in-pct-2002-0781-che form-19.pdf

in-pct-2002-0781-che form-26.pdf

in-pct-2002-0781-che form-3.pdf

in-pct-2002-0781-che pct.pdf

in-pct-2002-0781-che petition.pdf

« Previous Patent

Next Patent »

Patent Number

222562

Indian Patent Application Number

IN/PCT/2002/781/CHE

PG Journal Number

47/2008

Publication Date

21-Nov-2008

Grant Date

14-Aug-2008

Date of Filing

24-May-2002

Name of Patentee

SHIONOGI & CO., LTD

Applicant Address

1-8, DOSHOMACHI 3-CHOME, CHUO-KU, OSAKA-SHI, OSAKA 541-0045

Inventors:

#	Inventor's Name	Inventor's Address
1	YASUYUKI KAWANISHI	Shionogi & Co., Ltd. 12-4, Sagisu 5-chome, Fukushima-ku Osaka-shi, Osaka 553-0002 (JP).
2	HIDEYUKI TAKENAKA	Shionogi & Co., Ltd. 12-4, Sagisu 5-chome, Fukushima-ku Osaka-shi, Osaka 553-0002 (JP).
3	TETSUO OKADA	Shionogi & Co., Ltd. 12-4, Sagisu 5-chome, Fukushima-ku Osaka-shi, Osaka 553-0002 (JP).
4	KOHJI HANASAKI	Shionogi & Co., Ltd. 12-4, Sagisu 5-chome, Fukushima-ku Osaka-shi, Osaka 553-0002 (JP).

PCT International Classification Number

C07D 239/94

PCT International Application Number

PCT/JP00/08197

PCT International Filing date

2000-11-21

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1	11-336469	1999-11-26	Japan
2	11-353786	1999-12-14	Japan