Indian Patents. 222328:NOVEL CB 1 RECEPTOR INVERSE AGONISTS

Title of Invention	NOVEL CB 1 RECEPTOR INVERSE AGONISTS
Abstract	The present invention relates to compounds of formula (1) wherein R<SUB>1</SUB>, R<SUB>2</SUB>, R<SUB>3</SUB>, R<SUB>4</SUB>, R<SUB>5</SUB>, R<SUB>6</SUB> and R<SUB>7</SUB> are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CBI receptors.

Full Text	PYRROLYL-THIAZOLES AND THEIR USE AS CB 1 RECEPTOR INVERSE AGONISTS The present invention is concerned with novel pyrrolyl-thiazole derivatives, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in treating obesity and other disorders. In particular, the present invention relates to compounds of formula (I): wherein R1 is hydrogen, or lower alkyl; R2 is hydrogen, lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, lower alkoxycarbonylamino, -(CH2)m-R2a or -NHC(0)-R2a; or R and R together with the nitrogen atom to which they are attached form a 5- or 6-membered, saturated heterocyclic ring optionally containing one or two further heteroatom(s) independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl>.lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; R"a is cycloalkyl, optionally mono-, di-, tri- or tetra-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; cycloalkenyl, optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower allcyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower allcyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino, lower alkylamino; or phenyl, which may optionally be mono-,di-or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; R is lower alkyl, lower aikenyl, lower alkoxy-lower alkyl, di-phenyl-lower alkyl, or -(CH2)n-R3a; R3a is cycloalkyl fused to a phenyl ring; or cycloalkyl which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower0 alkyl or fluorinated lower alkoxy; cycloalkenyl, which may optionally be mono-, di-or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; R4 is lower alkyl, lower alkoxycarbonyl; cycloalkyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino, lower alkylamino; 'phenqxy-lower alkyl, wherein the phenyl moiety may optionally be mono-, di- or tri-substituted, independendy, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by, hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or two adjacent substituents of the said phenyl residue together are -O-(CH2)p-0- or -(CH2)rO-; R5 and R6 are each independently selected from hydrogen, lower alkyl, halogen or fluorinated methyl; R7 is hydrogen, lower alkyl or halogen; m is 0,1,2 or 3; nisO, 1,2, 3 or 4; p is 1, 2 or 3; and pharmaceuticaly acceptable salts thereof. Two different subtypes of cannabinoid receptors (CBi amd CB2) have been isolated and both belong to G protein coupled receptor superfamily. An alternative spliced form of CBi, CBiA has also been described, but it did not exhibit different properties in terms of ligand binding and receptor activation than CBi (D.Shire, C. Carrillon, M. Kaghad,.B. Calandra, M. Rinaldi-Carmona, G. Le Fur, D. Caput, P. Ferrara, J. Biol. Chem. 270 (8) (1995) 3726-31). The CBi receptor is mainly located in the brain, whereas the CB2 receptor is predominately distributed in the periphery and primarily localized in spleen and cells of > the immune system (S. Munro, K.L. Thomas, M. Abu-Shaar, Nature 365 (1993) 61-61). Therefore in order to avoid side effects a CBi-selective compound is desirable. A9-tetrahydrocannabinol (A9-THC) is the principal psychoactive compound in the Indian hemp (Y. Gaoni, R. Mechoulam, J. Am. Chem. Soc, 86 (1964) 1646), canabis savita (marijuanan), which is used in medicine since ages (R. Mechoulam (Ed.) in "Cannabinoids as therapeutic Agents", 1986, pp. 1-20, CRC Press). A9-THC is a non-selective CBi/2 receptor agonist and is available in the USA as dronabinol (marinol®) for the alleviation of cancer chemotherapy-induced emesis (CIE) and the reversal of body weight loss experienced by AIDS patients through appetite stimulation. In the UK Nabolinone (LY- 109514, Cesamet®), a synthetic analogue of A9-THC, is used for CIE (R. G.' Pertwee, Pharmaceut. Sci. 3 (11) (1997) 539-545, E. M. Williamson, F. J. Evans, Drugs 60 (6) (2000) 1303-1314). Anandamide (arachidonylethanolamide) was identified as the endogenous ligand (agonist) for the CBj receptor (R.G. Pertwee, Curr. Med. Chem., 6 (8) (1999) 635-664;W.A. Devane, L. Hanus, A. Breuer, R.G. Pertwee, L.A. Stevenson, G. Griffin, D. Gibson, A. Mandelbaum, A. Etinger, R. Mechoulam, Science 258 (1992) 1946-9). Anandamide and 2-arachidonoylglycerol (2-AG) modulate at the presynaptic nerve teminal negatively adenylate cyclase and voltage-sensitive Ca2+ channels and activates the inwardly rectifying K+ channel (V. Di Marzo, D. Melck, T. Bisogno, L. De Petrocellis, Trends in Neuroscience 21 (12) (1998) 521-8), thereby affecting neurotransmitter release and/or action, which decreases the release of neurotransmitter (A. C Porter, C.C. Efilder, Pharmacol. Ther., 90 (1) (2001) 45-60). Anandamide as A9-THC also increases feeding through CBi receptor-mediated mechanism. CB1 receptor selective antagonists block the increase in feeding associated with administration of anandamide (C.M. Williams, T.C, Kirkham, Psychopharmacology 143 (3) (1999) 315-317; C. C. Felder, E. M. Briley, J. Axelrod, J. T. Simpson, K. Mackie, W. A. Devane, Proc. Natl. Acad. Sci. U. S. A. 90 (16) (1993) 7656-60) and caused appetite suppression and weight loss (G. Colombo, R. Agabio, G. Diaz, C. Lobina, R. Reali, G. L. Gessa, Life Sci. 63 (8) (1998) L113-PL117). Leptin is the primary signal through which the hypothalamus senses nutritional state and modulates food intake and energy balance. Following temporary food restriction, CBI receptor knockout mice eat less than their wild-type littermates, and the CBI antagonist SR141716A reduces food intake in wild-type but not knockout mice. Furthermore, defective leptin signaling is associated with elevated hypothalamic, but not cerebellar, levels of endocannabinoids in obese db/db and ob/ob mice and Zucker rats. Acute leptin treatment of normal rats and ob/ob mice reduces anandamide and 2-arachidonoyl glycerol in the hypothalamus. These findings indicate that endocannabinoids in the hypothalamus may tonically activate CBl receptors to maintain food intake and form part of the neural circuitry regulated by leptin (V. Di Marzo, S. K. Goparaju, L. Wang, J. Liu, S. Bitkai, Z. Jarai, F. Fezza, G. I. Miura, R. D. Palmiter, T. Sugiura, G. Kunos, Nature 410 (6830) 822-825). SR-141716A, a CBl selective antagonist / inverse agonist is undergoing currently phase III clinical trials for the treatment of obesity. In a double blind placebo-controlled study, at the doses of 5,10 and 20 mg daily, SR 141716 significantly reduced body weight when compared to placebo (F. Barth, M, Rinaldi-Carmona, M. Arnone, H. Heshmati, G. Le Fur, "Cannabinoid antagonists: From research tools to potential new drugs" Abstracts of Papers, 222nd ACS National Meeting, Chicago, IL, United States, August 26-30,2001). Other compounds which have been proposed as CBl receptor antagonists respectively inverse agonists are aminoalkylindols (AAI; M. Pacheco, S. R. Childers, R. Arnold, F. Casiano, S. J. Ward, J. Pharmacol Exp. Ther. 257 (1) (1991) 170-183), like 6-bromo- (WIN54661; F. M. Casiano, R. Arnold, D. Haycock, J. Kuster, S. J. Ward, NIDA Res. Monogr. 105 (1991) 295-6) or 6-iodopravadoline (AM630, K. Hosohata, R. M. Quock, R.M; Hosohata, T. H. Burkey, A. Makriyannis, P. Consroe, W. R. Roeske, H. I. Yamamura, Life Sci. 61 (1997) 115 -118; R. Pertwee, G. Griffin, S. Fernando, X. Li, A. Hill, A. Makriyannis, Life Sci. 56 (23-24) (1995) 1949-55). Arylbenzo[b]thiophene and benzo[b]furan (LY320135, C. C. Felder, K. E. Joyce, E. M. Briley, M. Glass, K. P. Mackie, K. J. Fahey, G. J. Cullinan, D. C. Hunden, D. W. Johnson, M. O. Chaney, G. A. Koppel, M. Brownstein, J. Pharmacol. Exp. Ther. 284 (1) (1998) 291-7) disclosed in WO9602248, US5596106,3-alkyl-(5,5-diphenyl)imidazolidinediones (M. Kanyonyo, S. J. Govaerts, E. Hermans, J. H. Poupaert, D. M. Lambert, Bioorg. Med. Chem. Lett 9 (15) (1999) 2233 -2236.) as well as 3-alkyl-5-arylimidazolidinediones (F. Ooms, J. Wouters, O. Oscaro. T. Happaerts, G. Bouchard, P.-A. Carrupt, B. Testa, D. M. Lambert, J, Med. Chem. 45'(9) (2002) 1748-1756) are known to antagonize the CBi receptor respectively act as an inverse agonist on the hCBi receptor. WO0015609 (FR2783246-A1), WO0164634 (FR2805817-Al), WO0228346, WO0164632 (FR2805818-A1), WO0164633 (FR2805810-A1) disclosed substituted l-bis(aryl)methyl-azetidines derivatives as antagonists of CBj. In WO0170700 4,5-dihydro-lH-pyrazole derivatives are described as CBi antagonists. In several patents bridged and non-bridgedl,5-diphenyl-3-pyrazolecarboxamide derivatives are disclosed as CBi antagonists/inverse agonists (WO0132663, WO0046209, WO9719063, EP658546, EP656354, US5624941, EP576357, US3940418). It is an object of this invention to provide selective, directly acting CB1 receptor antagonists respectively inverse agonists. Such antagonists / inverse antagonists are useful in medical therapy, particularly in the treatment and/or prevention of diseases which are associated with the modulation of CB1 receptors. Unless otherwise indicated, the following definitions are set forth to illustrate and define the meaning and scope of the various terms used to describe the invention herein. In this specification the term "lower" is used to mean a group consisting of one to eight, preferably of one to four carbon atom(s). The term "halogen" refers to fluorine, chlorine, bromine and iodine, preferably to chlorine and fluorine. The term "alkyl", alone or in combination with other groups, refers to a branched or straight-chain monovalent saturated aliphatic hydrocarbon radical of one to twenty carbon atoms, preferably one to sixteen carbon atoms, more preferably one to ten carbon atoms. The term "lower alkyl", alone or in combination with other groups, refers to a branched or straight-chain monovalent alkyl radical of one to eight carbon atoms, preferably one to four carbon atoms. This term is further exemplified by radicals such as methyl, ethyl, n-propyl, isopropyl, n-butyl, s-butyl, isobutyl, t-butyl, n-pentyl, 3-methylbutyl, n-hexyl, 2-ethylbutyl and the like. The term "alkoxy" refers to the group R'-O-, wherein R' is alkyl. The term "lower alkoxy" refers to the group R'-O-, wherein R5 is lower alkyl. Examples of lower alkoxy groups are e.g. methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy and hexyloxy, with methoxy being especially preferred. The term "lower alkenyl" refers to a lower alkyl group containing one or more double bond(s) in the alkylene chain. This term is further exemplified by radicals such as vinyl, 1-propenyl, allyl, 1-butenyl, 2-butenyl and 3-butenyl, with allyl being preferred. The term "lower alkylarjiino" refers to the group R'-NH-, wherein R' is lower alkyl. The term "lower alkoxycarbonyl" refers to the group R'-O-C(O)-, wherein R' is lower alkyl. The term "lower alkoxycarbonylamino" refers to the group R>-0-C(0)NH-> wherein IV is lower alkyl. The term "halogenated lower alkyl" refers to a lower alkyl group wherein at least one of the hydrogens of the lower alkyl group is replaced by a halogen atom, preferably fluoro or chloro. Among the preferred halogenated lower alkyl groups are trifluoromethyl, difluoromethyl, fluoromethyl and chloromethyl, with trifluoromethyl being especially preferred. The term "fluorinated lower alkyl" refers to a lower alkyl group wherein at least one of the hydrogens of the lower alkyl group is replaced by fluoro. Among the preferred fluorinated lower alkyl groups are trifluoromethyl, difluoromethyl and fluoromethyl, with trifluoromethyl being especially preferred. The term "halogenated lower alkoxy" refers to a lower alkoxy group wherein at least one of the hydrogens of the lower alkoxy group is replaced by halogen, preferably by fluorine or chlorine. Among the preferred halogenated lower alkoxy groups are fluorinated lower alkoxy groups such as trifluoromethoxy, difluoromethoxy and fluoromethoxy, with trifluoromethoxy being especially preferred. The term "fluorinated lower alkoxy" refers to a lower alkoxy group wherein at least one of the hydrogens of the lower alkoxy group is replaced by fluoro. Among the preferred fluorinated lower alkoxy groups are trifluoromethoxy, difluoromethoxy and fluoromethoxy, with trifluoromethoxy being especially preferred. The term "di-phenyl-lower alkyl" refers to a lower alkyl group wherein two of the hydrogens of the lower alkyl group is replaced by phenyl. The phenyl moiety may optionally be mono-, di-, or tri-substituted, independently, by lower alkyl, lower alkoxy or halogen. The term "phenoxy-lower alkyl" refers to a lower alkyl group wherein one of the hydrogens of the lower alkyl group is replaced by phenoxy. The phenyl moiety of the phenoxy-lower alkyl residues may optionally be mono-, di-, or tri-substituted, independently, by lower alkyl, lower alkoxy or halogen. The term "cycloalkyl" refers to a monovalent carbocyclic radical of three to six, preferably three to five carbon atoms. This term is further exemplified by radicals such as cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl. The term "cycloalkenyl" refers to a monovalent carbocyclic radical of three to six, preferably three to five carbon atoms, which carbocyclic ring contains at least on double bond. This term is further exemplified by radicals such as cyclobutenyl, cyclopentenyl and cyclohexenyl, with cyclohexenyl being preferred. The term "pharmaceutical^ acceptable salts" embraces salts of the compounds of formula (I) with inorganic or organic acids such as hydrochloric acid, hydrobromic acid, nitric acid, sulphuric acid, phosphoric acid, citric acid, formic acid, maleic acid, acetic acid, fumaric acid, succinic acid, tartaric acid, methanesulphonic acid, salicylic acid, p-toluenesulphonic acid and the like, which are non toxic to living organisms. Preferred salts with acids are formates, maleates, citrates, hydrochlorides, hydrobromides and methanesulfonic acid salts, with hydrochlorides being especially preferred. In one embodiment, the present invention relates to a compound of formula (I) as defined above, wherein R1 is hydrogen or lower alkyl. Preferable lower alkyl residues R1 are methyl and ethyl, with methyl being especially preferred. Most preferably, R1 is hydrogen. In another embodiment, the present invention relates to a compound of formula (I) as defined above, wherein R2 is hydrogen, lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, lower alkoxycarbonylamino, -(CH2)m-R2a or -NHC(0)-R2Preferable lower alkyl residues R are branched or straight chain alkyl residues with one to eight, preferably three to five carbon atoms, such as n-propyl, n-butyl, s-butyl, isobutyl, n-pentyl and 2-ethylhexyl. Most preferred lower alkyl residues R2 are n-propyl, n-butyl, s-butyl, isobutyl and n-pentyl. Preferable lower alkenyl residues R are 1-butenyl and allyl, with allyl being especially preferred. Preferable lower alkoxy-lower alkyl residues R2,are methoxymethyl, methoxyethyl, methoxypropyl, ethoxymethyl, ethoxyethyl and ethoxypropyl, with methoxyethyl and methoxypropyl being especially preferred. Preferable lower alkoxycarbonylamino groups R2 are methoxycarbonylamino, ethoxycarbonylamino, propoxycarbonylamino and butoxycarbonylamino, with ethoxycarbonylamino being specially preferred. Preferable residues R" are lower alkyi as defined above, -(CH2)m-R2a ■r -NHC(0)~R2a, wherein R2a is as defined below and m is 0 or 1, preferably 0. Most referable residues R are lower alkyi as defined above or -(CH2)m-R a> wherein R is as lefined below and m is 0 or 1, preferably 0. In one embodiment, R2a is cycloalkyl, optionally mono-, di-, tri- or tetra-substituted, ndependently, by hydroxy, lower alkyi, lower alkoxy, fluorinated lower alkyi ox luorinated lower alkoxy; cycloalkenyl, optionally mono-, di- or tri-substituted, ■ndependently, by hydroxy, lower alkyi, lower alkoxy, fluorinated lower alkyi or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring . containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyi, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyi or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyi, lower alkoxy, halogen, amino, lower alkylamino; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower "alkyi, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyi, halogenated lower alkoxy or nitro. Preferable cycloalkyl residues R2a are cycloalkyl residues with three to six carbon atoms, such as cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, which may optionally be mono-, di-, tri- or tetra-substituted, preferably mono- or tetra-substituted, independently, by hydroxy, lower alkyi, lower alkoxy, fluorinated lower alkyi or fluorinated lower alkoxy, preferably by lower alkyi, such as methyl, and/or hydroxy. Most preferable cycloalkyl residues R a are cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and 2-hydroxycyclopentyl. Preferable cycloalkenyl residues R2a are cyclobutenyl, cyclopentenyl and cyclohexenyl, with cyclohexenyl, preferably cyclohex-l-enyl, being especially preferred. Preferable heterocyclic rings R2a are 5- or 6-memberd, with 5-membered being especially preferred, and contain one to three, preferably one or two, heteroatoms independently selected from nitrogen, oxygen and sulfur, preferably selected form nitrogen and oxygen, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyi, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyi or fluorinated lower alkoxy. Preferably, heterocyclic rings R a are unsubstituted. Most preferred heterocyclic rings R2a are piperidinyl, morpholino and tetrahydrofuranyl, with piperidinyl and morpholino being especially preferred. Preferable heteroaromatic rings R~a are 5- or 6-membered and contain one to three, preferably one or two, heteroatoms independently selected from nitrogen, oxygen and sulfur, preferably selected form nitrogen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino. Examples of heteroaromatic rings R a are pyridinyl, pyrimidinyl, thiazolyl and isoxazolyl, optionally substituted as defined above. Preferably, heteroaromatic rings R2a are unsubstituted or mono-substituted by lower alkyl, preferably methyl. Most preferable heteroaromatic rings R a are pyridinyl, pyrimidinyl, 4-methylthiazolyl or 5-methylisoxazolyl. Preferable phenyl residues R a are optionally mono-, di- or tri-substituted, preferably mono- or di-substituted, independently, by lower alkoxy, such as methoxy, halogen, such as chloro, halogenated lower alkyl, such as trifluoromethyl, halogenated lower alkoxy, such as trifluoromethoxy, or nitro. Most preferable phenyl residues R2a are unsubstituted phenyl, 4-trifluoromethyl-phenyl, 4-chloro-phenyl, 3,4-dichloro-phenyl, 3,4-dimethoxy-phenyl, 2-nitro-phenyl and4-trifluoromethoxy-phenyl. Preferably, m is 0,1 or 2, more preferably m is 0 or 1, most preferably m is 0. " In another embodiment, R and R together with the nitrogen atom to which they are attached form a 5- or 6-membered, saturated heterocyclic ring optionally containing one or two, preferably one, further heteroatom(s) independently selected from nitrogen, oxygen and sulfur, preferably oxygen, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy. Preferably, heterocyclic rings formed by R and R together with the nitrogen atom to which they are attached are unsubstituted, with unsubstituted pyrrolidinyl, piperidinyl and morpholino being especially preferred. In another embodiment, the present invention relates to a compound of formula (I) as defined above, wherein R is lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, di-phenyl-lower alkyl, or -(CH2)n-R3a. Preferable lower alkyl residues R are branched or straight chain alkyl residues with one to sk, preferably four carbon atoms, such as ethyl, n-propyl, isopropyl, n-butyl, s-butyl, isobutyl, n-pentyl and n-hexyl. Most preferred lower alkyl residues R3 are n-butyl and s-butyl. Preferable lower alkenyl residues R are 1-butenyl and allyl, with allyl being especially preferred. Preferable lower alkoxy-lower alkyl residues R3 are methoxymethyl, methoxyethyl, methoxypropyl, ethoxymethyl, ethoxyethyl and ethoxypropyl, with methoxyethyl and methoxypropyl being especially preferred. Preferable di-phenyl-lower alkyl is di-phenyl-methyl. Most preferably, R3 is a residue -(CH2)n-R3a, wherein R3a is as i defined below and n is 1 or 2, preferably 1. In one embodiment, R3a is cycloalkyl fused to a phenyl ring; or cycloalkyl which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; cycloalkenyl, which may . optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-y di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent h'eteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower ' alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro. Preferable cycloalkyl residues R3a are cycloalkyl residues with five or six carbon atoms, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy, or which may optionally be fused to a phenyl ring. Preferably, cycloalkyl residues R3a are unsubstituted, such as unsubstituted cyclopentyl or unsubstituted cyclohexyl, with unsubstituted cyclohexyl being preferred, or fused to a phenyl residue, such as indanyl. Preferable cycloalkenyl residues R2a are cyclobutenyl, cyclopentenyl and cyclohexenyl, with cyclohexenyl, preferably cyclohex-1-enyl, being especially preferred. Preferable heterocyclic rings R3a are 5- or 6-memberd and contain one to three, preferably one or two, heteroatoms independently selected from nitrogen, oxygen and sulfur, preferably selected form nitrogen and oxygen, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy. Examples of heterocyclic rings R3a are piperidinyl, morpholino and pyrrolidinyl, optionally substituted as defined above. Preferably, heterocyclic rings R a are unsubstituted or substituted by lower alkyl, such as methyl or ethyl, with ethyl being especially preferred. Most preferred heterocyclic rings R3a are piperidinyl, morpholino and 1-ethyl-pyrrolidinyl. Preferable heteroaromatic rings R3a are 5- or 6-membered and contain one to three, preferably one, heteroatom(s) independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino. Examples of heteroaromatic rings R3a are furyl, thienyl and pyridinyl, optionally substituted as defined above. Preferably, heteroaromatic rings R a are unsubstituted or mono-substituted by lower alkyl, preferably methyl. Most preferable heteroaromatic rings R3a are furyl, thienyl, 3-methylthienyl and pyridinyl. Preferable phenyl residues R a are optionally mono-, di- or tri-substituted, preferably mono- or di-substituted, most preferably mono-substituted, independently, by hydroxy, lower alkyl, such as methyl or isopropyl, lower alkoxy, such as methoxy, halogen, such as chloro, halogenated lower alkyl, such as trifluoromethyl, halogenated lower alkoxy, such as trifluoromethoxy, or rtitro. Most preferable phenyl residues R3a are unsubstituted phenyl, 2-methyl-phenyl, 4-methyl-phenyl, 3,4-dimethyl-phenyl, 3,5-dimethyl-phenyl, 4-isopropyl-phenyl, 4-chloro-phenyl, 3,4-dichloro-phenyl, 3,5-dichloro-phenyl, 3-methoxy-phenyl, 4-methoxy-phenyl, 3,4-dimethoxy-phenyl, 3,5-dimethoxy-phenyl, 2,4-dimethoxy-phenyl, 3,4,5-trimethoxy-phenyl, 3-trifluoromethoxy-phenyl, 4-trifluoromethoxy-phenyl, 3-trifluormethyl-4-chlorophenyl and 4-nitro-phenyl, with 4-methoxy-phenyl being especially preferred. Most preferable residue R3a is a phenyl residue as defined above. Preferably, n is 0,1, 2 or 3, more preferably n is 1 or 2, most preferably n is 1. In another embodiment, the present invention relates to a compound of formula (I) as defined above, wherein R4 is lower alkyl; lower alkoxycarbonyl; cycloalkyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independendy selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino, lower alkylamino; phenoxy-lower alkyl, wherein the phenyl moiety may optidnally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by, hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or two adjacent substituents of the said phenyl residue together are -0-(CH2)p-0- or -(CH2)2-0-. Preferable lower alkyl residues R4 are branched or straight chain alkyl residues with one to six, preferably one to three carbon atoms, such as methyl, ethyl, n-propyl, isopropyl, n-butyl, s-butyl, t-butyl, isobutyl and n-pentyL Most preferred lbwer alkyl residue R4 is methyl. Preferable lower allcoxycarbonylamino groups R4 are methoxycarbonylamino, ethoxycarbonylamino, propoxycarbonylamino and butoxycarbonylamino, with ethoxycarbonylamino being especially preferred. Preferable cycloalkyl residues R4 are cycloalkyl residues with three to six carbon atoms, such as cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, which may optionally be mono-, di-> tri- or tetra-substituted, preferably mono- or tetra-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy, preferably by lower alkyl, such as methyl, and/or hydroxy. Most preferable cycloalkyl residue R4 is unsubstituted cyclohexyl. Preferable heteroaromatic rings R4 are 5- or 6-membered and contain one to three, preferably one or two, heteroatoms independently selected from nitrogen, oxygen and sulfur, preferably selected form nitrogen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently/by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino. Examples of heteroaromatic rings R are pyridinyl, pyrazinyl and thiazolyl, optionally substituted as defined above. Preferably, heteroaromatic rings R4 are unsubstituted or mono-substituted by lower alkyl, such as methyl and ethyl, or by lower alkoxy, such as methoxy. Most preferable heteroaromatic rings R are 2-methoxy-pyridinyl, 2-methyl-pyridinyl, pyrazinyl and 2-methyl-thiazolyl. Preferable phenoxy-lower alkyl residues R4 are phenoxy-methyl and phenoxy ethyl, wherein the phenyl moiety may optionally be mono-substituted by lower alkoxy, such as methoxy. Most preferable phenoxy-lower alkyl residue R4 is 3-methoxy-phenoxy-methyl. Preferable phenyl residues R4 are mono-, di- or tri-substituted, preferably mono- or di-substituted, most preferably mono-substituted, independently, by hydroxy, lower alkyl, such as methyl, ethyl or t-butyl, lower alkoxy, such as methoxy, halogen, such as chloro or fluoro, halogenated lower alkyl, such as trifluoromethyl, halogenated lower alkoxy, such as trifluoromethoxy or nitro. Alternatively, two adjacent substituents of the said phenyl residue together maybe -0-(CH2)p-0- or -(CfkVO-, wherein p is 1, 2 or 3, preferably 1 or 2, most preferably 1. Preferable substituents of phenyl residues R4 are nitro and lower alkoxy, or two adjacent substituents being -O-CH2-O-. Most preferable substituted phenyl residues R4 are 2-methyl-phenyl, 4- methyl-phenyl, 4-ethyl-phenyl, 4-t-butyl-phenyl, 2-chloro-phenyl, 4-chloro-phenyl, 2,4-dichloro-phenyl, 2-fluoro-phenyl, 4-fluoro-phenyl, 2-methoxy-phenyl, 3-methoxy-phenyl, - 4-methoxy-phenyl, 3,4-dimethoxy-phenyl, 3,5-dimethoxy-phenyl, 4-hydroxy-phenyl, 4-trifluoromethyI-phenyl> 4-trifluoromethoxy-phenyl, 4-nitro-phenyl, benzo[ls3]dioxolyl ■and 2,3-dihydro-benzofuranyI, with 4-methoxyphenyl, 4-nitro-phenyI and benzo[l,3]dioxolyl being especially preferred. Preferable residues R4 are cycloalkyl residues and substituted phenyl residues as defined above. In another embodiment, the present invention relates to a compound of formula (I) as defined above, wherein R5 and R are each independently selected from hydrogen, lower alkyl, halogen or fluorinated methyl. Preferable lower alkyl residues R5 and R6 are methyl and ethyl, with methyl being especially preferred. Preferable halogen residues R5 and R6 are fluoro and chloro, with chloro being especially preferred. Preferable residue R5 is lower alkyl, such as methyl. Preferable residues R6 are hydrogen and lower alkyl, such as methyl. In another embodiment, the present invention relates to a compound of formula (I) as defined above, wherein R is hydrogen, lower alkyl or halogen. Preferable lower alkyl residues R7 are methyl and ethyl, with methyl being especially preferred. Preferable halogen residues R are fluoro and chloro, with chloro being especially preferred. Preferable residue R7 are hydrogen and lower alkyl, such as methyl. Preferred compounds of general formula (I) are the compounds of Examples 1 to 377, preferably 1 to 375 (see section Examples below) and pharmaceutically acceptable salts thereof. Especially preferred are the compounds selected from the group consisting of: l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-meAyl-lH-pyrrole-3-c arboxylic acid butylamide, l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH- pyrrole-3 -carboxylic acid butylamide, «■ ■ mc-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyI)-thiazoI-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid sec-butylamide, rac-1 -Cyclohexylmethyl-5- [2-(4-methoxy-phenpxymethyl)-thiazol-4-yl] -2-methyl-lH-pyrr ole-3-carboxylic acid sec-butylamide, . 1 -Cyclohexylmethyl-5- [2- (4-methoxy-phenyl)-thiazol-4-yl] -2-methyl- lH-pyrrole-3-c arboxylic acid isobutyl-amide, l-Furan-2-ylmethyl-5-[2-(4-methoxy~phenylM c arboxylic acid isobutyl-amide, l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazoI-4-yl]-2-methyl-lH-pyrrole-3 -carboxylic acid isobutyl-amide, l-Cyclohexylmethyl-5-[2-(4-methoxy-pheny^ 3-c arboxylic acid allylamide, l-Cyclohexylmethyl-5- [2-(4-methoxy-phenyl)-thiazol-4-yl] -2-methyl- lH-pyrroIe-3-c arboxylic acid cyclohexylmethyl-amide, l-Cyclohexylmethyl-2-methyl-5-(2-pyrazm^ lie acid cyclohexylmethyl-amide, l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yI]-2-methyl-lH-pyrrole-3 -carboxylic acid cyclohexylmethyl-amide, 5-[2-(4-Methoxy-phenoxymethyl)-lhiazol-4-yl]-l-(3-methoxy-propyl)-2-meti\yl-lH-py rrole-3-carboxylic acid cyclohexylmethyl-amide, 4-[ 1-[2-(3,4-Dimethoxy-phenyl)-ethyl]-4-(3-methoxy-propylcarbamoyl)-5-methyl-1H- pyrrol-2-yl]-thiazole-2-carboxylic acid ethyl ester, l-Cyclohexylmethyl-5-[2-(4-metlioxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid piperidin-1-ylamide, N'-{l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carbonyl}-hydrazinecarboxylic acid ethyl ester, r^c-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid sec-butylamide, {l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrol-3-yl}-piperidin-l-yl-methanone, l-Cyclohexylmethyl-5-[2"(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid phenylamide, l-Cydohexyimethyl-5-te^ 3-carboxylic acid pyrimidin-2-ylamide, mc-l-CydohexylmethyI-5-[2-(4-m^ pyrroleO-carboxyiicadd(5-hydroxjr-2,2,6-trimeth 5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-(3-trifluoromethoxy-^ lH-pyrrole-3-carboxylic acid butylamide, l-BenzyI-5-[2-(4-methoxy-ph^ . acid butylamide, {l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyI)-thiazol-4-yl]-2-methyl^ 3-yl}-pyrrolidin-1-yl-methanone, l-Cydohexylmethyl-5-[2-(^ pyrroIe-3-carboxyIic acid butylamide, l-Cydohexylmeth]d-5-[2-(3-metho^ 3-carboxylic acid butylamide, 5-(2-Benzo[l,3]dioxol-5-yI-thiazol-4-yl)-l-qrdohexyImethyI-2-m 3-carboxylic acid butylamide, l-Cyclohexylmethyl-5-[2-(4-fluoro-pte^ carboxylic acid butylamide, l-Cyclohexylmethyl-5-[2-(2-fluoro-phenyl)-thiazol-4-yI]-2-methyI-lH-pyrrole--3-carboxylic acid butylamide, l-Cyclohexylmethyl-2-methyl-5-[2-(4-trifluoromethoxy-phenyl)-thiazol-4-yl]"lH pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmetiyi-5-[2-(3,5-dimethoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrroIe-3-carboxylic acid butylamide, l-Cyclohexylmethyl-2-methyl-5-(2-m-tolyl-thiazol-4-yl)-lH-pyrrole-3--carboxylic acid butylamide, l-Cyclohexylmethyl-2-methyl-5^^ :arf>oxylic acid butylamide, l-Cyclohexylmetiiyl-5-[2-(4-ethyl-phenyl)-thiazol-4-yl]-2-methyl"lH-pyrrole-3-:arboxylic acid butylamide, 5-[2-(4-Chloro-phenyl)-thiazol-4-yl]-l-cyd^ carboxylic acid butylamide, 5-[2-(4-tert-Butyl-phenyl)-thiazol-4^ 3-carboxylic acid butylamide, l-Cyclohexylmethyl-542-(2,3-dihydro-benzofa^ lH-pyrrole-3-carboxylic acid butylamide, l-CyclohexyImethyl-2-methyl-5-(2-p-to^ acid butylamide, l-Cyclohexylmethyl-5-[2-(6-m pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-5-[2-(2>4-dicUoro-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-2-oiet^ carboxylic acid butylamide> l-Cyclohexylmethyl-5-[2-(4-methoxy-pheny^ 3-carboxylic acid pentylamide, l-Cyclohexylmethyl-5-[2-(4-methoxy--phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid propylamide, l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyI)"thiazol-4-yI]-2-methyl-lH-pyrrole-3-carboxylic acid cyclohexylamide, l-Cyclohexylmethyl-5-[2-(4-methoxy-pheny^ 3-carboxylic acid cyclopentylamide, l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid cyclopropylamide, l7Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrro^ 3-carboxylic acid cyclobutylamide, (traits) rac-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)"thiazoI-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid (2-hydroxy-cyclopentyl)-amide> l-(4-Chloro-benzyl)-5-[2-(4-methoxy-phe^ 3-carboxylic acid butylamide, l-(3,4-Dichloro-benzyl)-5-[2-(4-methoxy-phenyI)-thia2ol-4-yl]-2-meth)4-lH-pyrrole-3-carboxylic acid butylamide, .^-(3,4«Dimethyl-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2 pyrrole-3-carboxylic acid butylamide, l-(3,4-Dimethoxy-benzyl)-5-[2-(4-methoxy«phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-5-[2-(4-hydroxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3- . carboxylic acid butylamide, l-(4-IsopropyI-benzyl)-5-[2-(4-methoxy-phenyl)-tiiiazol-4-yl]-2-rnethyl«lH-pyrrole-3-carboxylic acid butylamide, 5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-pyridin-2-ylmethyl-lH-pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-5-(2-cyclohexyl-tiiiazol-4-yl)-2-methyl-lH-pyrrole-3-carboxylic acid butylamide, and pharmaceutically acceptable salts thereof. Most preferred compounds of general formula (I) are those selected from the group consisting of: l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid butylamide, rac-l-Cyclohexylmethyl-5-[2«(4-methoxy-phenyl)-thiazol-4-yI]-2-methyl-lH-pyrrole-3-carboxylic acid sec-butylamide, {l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-liuazol-4-yl]-2-methyl-lH-pyrrol-3-yl}-piperidin-l-yl-methanone, 5- (2-Benzo [ 1,3 ] dioxol-5-yl-thiazol-4-yl)-1 -cyclohexylmethyl-2-methyl- lH-pyrrole-3-carboxylic acid butylamide,-l-Cyclohexylmetiiyl-5-[2-(4-fluoro-phenyl)"thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide, 1-Cyclohexylmethyl-acid butylamide^ 1 -Cyclohexylmethyl-5- [2-(6-methoxy-pyridin-3-yl)-thiazol-4-yl] -2-methyl-lH-pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmediyl-2-m carboxylic acid butylamide, l-Cyclohexylmethyl-5-[2-(4-methoxy-phen^ 3-carboxylic acid pentylamide, l-Cyclohexylmethyl-5-[2-(4-methoxy-phen^ 3-carboxylic acid cyclohexylamide, 1 -Cyclohexylmethyl-5- [2- (4-methoxy-phenyl)-thiazol-4'-yll -2-methyl- iH-pyrrole-3-carboxylic acid cyclopentylamide, l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl^ 3-carboxylic acid cyclopropylamide, l-Cyclohexylmethyl-5-[2-(4-hydroxy-phenyl^^^ carboxylic acid butylamide, l-Cyclohexylmeliiyl-5-(2"Cyclohexyl-thiazol-4-yl)-2»metiiyl-lH-pyrrole-3-carboxylic acid butylamide, and pharmaceutical^ acceptable salts thereof. The present invention also relates to a process for the manufacture of compounds of formula (I) as defined above. The compounds of formula (I) can be manufactured by the methods given below, by the methods given in the Examples or by analogous methods. Appropriate reaction conditions for the individual reaction steps are known to the person skilled in the art. Starting materials are either commercially available or can be prepared by methods analogous to the methods given below or in the Examples or by methods known in the art. 'The compounds of formula (I) may be prepared using the general methods described-below: Compounds of formula (I), wherein R1 to R7 and m are as previously defined, can be prepared by reaction of enamines of formula A with alfa-bromoketones of formula B according to methods known in the art (Scheme 1), For example, the reaction can be performed in an inert solvent such as DMF in the presence of a hindered base such as 2,6-.di-tert-butylpyridine or 2,6-lutidine. Scheme 1: Compounds of formula I can be purified by methods known in the art such as precipitation from mixtures of solvents (e.g. acetonitrile and water) or by column chromatography using Si02 with eluents know in the art (e.g. n-heptane/Ethyl acetate, dichloromethane/methanol and dichloromethane/(.l% NH3 in MeOH)). Thiazole derivatives of formula B can be prepared from dibromodilcetones of formula C and thioamides of formula C by methods known in the art (Scheme 2). For example, the reaction can be performed by addition of thioamides of formula C to dibromo-diketones of formula D in an inert solvent such as DMF. Scheme 2: Enamines of formula A can be prepared from beta-ketoamides of formula E and amines of formula F by methods known in the art (Scheme 3). For example a beta-keto amide of formula E can be reacted with an amine of formula B in a suitable inert solvent (e.g. DMF) in the presence of a hindered base (e.g. 2,6-di-tert-butylpyridine) to yield enamine of formula A. Scheme 3 Beta-ketoamides of formula E are either known form the literature or can be purchased from commercial sources or else can be prepared by methods known in the art. For example, beta-ketoamides of formula E wherein R = methyl can be prepared by reaction of amines of formula G with diketene in an inert solvent such as dichloromethane (Scheme 4). Scheme 4 Compounds of formula D, F and G are either known from the literature or can be purchased from commercial sources or else can be synthesized by methods known in the art. The invention further relates to compounds of formula (I) as defined above, when manufactured according to a process as defined above. Some compounds of formula (I) may possess asymmetric centres and are therefore capable of existing in more than one stereoisomeric form. The invention thus also relates to compounds in substantially pure isomeric form at one or more asymmetric centres as well as mixtures, including racemic mixtures, thereof. Such isomers maybe prepared by asymmetric synthesis, for example using chiral intermediate, or mixtures may be resolved by conventional mehtods, eg., chromatography (chromatography with a chiral adsorbens or eluent), or use of a solving agent. It will be appreciated, that the compounds of general formula (I) in this invention maybe derivatised at functional groups to provide derivatives which are capable of conversion back to the parent compound in vivo. As described above, the compounds of formula (I) or pharmaceutical^ acceptable salts thereof can be used as medicaments for the treatment and/or prophylaxis of diseases which are associated with the modulation of the CBl receptors. The invention therefore also relates to pharmaceutical compositions comprising, a compound as defined above and a pharmaceutical!-/ acceptable carrier and/or adjuvant. Further, the invention relates to compounds as defined above for use as therapeutic active substances, particularly as therapeutic active substances for the treatment and/or prophylaxis of diseases which are associated with the modulation of CBl receptors. In another embodiment, the invention relates to a method for the treatment and/or prophylaxis of diseases which are associated with the modulation of CBl receptors, which method comprises administering a compound as defined above to a human being or i animal. The invention further relates to the use of compounds as defined above for the treatment and/or prophylaxis of diseases which are associated with the modulation of CBl receptors. In addition, the invention relates to the use of compounds as defined above for the preparation of medicaments for the treatment and/or prophylaxis of diseases which are associated with the modulation of CBl receptors. Such medicaments comprise a compound as defined above. In this context, the expression 'diseases associated with modulation of CBl receptors' means diseases which can be treated and/or prevented by modulation of CBl receptors. Such diseases encompass, but are not limited to, psychic disorders, especially anxiety, psychosis, schizophrenia, depression, abuse of psychotropes, for example for the abuse and/or dependence of a substances, including alcohole dependency and nicotine dependency, neuropathies, migraine, stress, epilepsy, dyskinesias, Parkinson!s disease, amnesia, cognitive disorders, senile dementia, Alzheimer's disease, eating disorders, obesity, diabetes type II or nori insulin dependent diabetes (NIDD), gastrointestinal diseases, vomiting, diarrhea, urinary disorders, cardiovascular disorders, infertility disorders, inflammations, infections, cancer, neuroinflammation, in particular in atherosclerosis, or the Guillain-Barre syndrome, viral encephalitis, cerebral vascular incidents and cranial trauma. In a preferable aspect, the expression 'diseases associated with modulation of CB1 receptors3 relates to eating disorders, obesity, diabetes type II or non insulin dependent diabetes (NIDD), neuroinflammation, diarrhea> abuse and/or dependence of a substances, including alcohole dependency and nicotine dependency. In a more preferable aspect, the said term related to eating disorders, obesity, diabetes type II or non insulin dependent diabetes (NIDD), abuse and/or dependence of a substances, including alcohole dependency and nicotine dependency, with obesity being especially preferred. It is a further preferred object to provide a method of treatment or prevention of Type II diabetes (non-insulin dependent diabetes meUitus (NIDDM) in a human which comprises administration of a therapeutically effective amount of a compound according to formula (I) in combination or association with a therapeutically effective amount of a lipase inhibitor, particularly, Wherein the lipase inhibitor is orlistat. Also an object of the invention is the method as described above for the simultaneous, separate or sequential administration of a compound according to formula (I) and a lipase inhibitor, particularly tetrahydr olipstatin. It is a further preferred object to provide a method for the treatment or prevention of obesity and obesity related disorders which comprises administration of a therapeutically effective amount of a compound according to formula (I) in combination or association with a therapeutically effective amount of other drugs for the treatment of obesity or eating disorders so that together they give effective relief. Suitable other drugs include but are not limited to anorectic agents, lipase inhibitors and selective serotonin reuptake inhibitors (SSRI). Combinations or associations of the above agents maybe encompassing separate, sequential or simultaneous administration. Preferable lipase inhibitor is tetrahydrolipstatin. Suitable anorectic agents of use in combination with a compound of the present invention include, but are not limited to, aminorex, amphechloral, amphetamine, benzphetamine, chlorphentermine, clobenzorex, cloforex, clominorex, clortermine, cyclexedrine, dexfenfluramine, dextroamphetamine, diethylpropion, diphemethoxidine, N-ethylamphetamine, fenbutrazate, fenfluramine, fenisorex, fenproporex, fludorex, fluminorex, furfurylmethylamphetamine, levamfetamine, levophacetoperane, mazindol, mefenorex, metamfepramone, methamphetamine, norpseudoephedrine, pentorex, phendimetrazine, phenmetrazine, phentermine, phenylpropanolamine, picilorex and • sibutramine, and pharmaceutical^ acceptable salts thereof. Most preferable anorectic agents are sibutramine and phentermine. Suitable selective serotonin reuptake inhibitors of use in combination with a compound of the present invention include: fluoxetine, fluvoxamine, paroxetine and sertraline, and pharmaceutically acceptable salts thereof. Demonstration of additional biological activities of the compounds of the present invention may be accomplished through in vitro, ex vivo, and in vivo assays that are well known in the art. For example, to demonstrate the efficacy of a pharmaceutical agent for the treatment of obesity-related disorders such as diabetes, Syndrome X, or atherosclerotic disease and related disorders such as hypertriglyceridemia and hypercholesteremia, the following assays maybe used., Method for Measuring Blood Glucose Levels db/db mice (obtained from Jackson Laboratories, Bar Harbor, ME) are bled (by either eye or tail vein) and grouped according to equivalent mean blood glucose levels. They are dosed orally (by gavage in a pharmaceutically acceptable vehicle) with the test compound once daily for 7 to 14 days. At this point, the animals are bled again by eye or tail vein and blood glucose levels are determined. Method for Measuring Triglyceride Levels hApoAI mice (obtained from Jackson Laboratories, Bar Harbor, ME) are bled (by either eye or tail vein) and grouped according to equivalent mean serum triglyceride levels. They are dosed orally (by gavage in a pharmaceutically acceptable vehicle) with the test compound once daily for 7 to 14 days. The animals are then bled again by eye or tail vein, •r and serum triglyceride levels are determined. Method for Measuring HDL-Cholesterol Levels To determine plasma HDL-cholesterol levels, hApoAI mice are bled and grouped with equivalent mean plasma HDL-cholesterol levels. The mice are orally dosed once daily with vehicle or test compound for 7 to 14 days, and then bled on the following day. Plasma is analyzed for HDL-cholesterol. In addition, to demonstrate CNS activities of the compounds of the present invention, the following in vivo assays maybe used. Method for Testing Task Learning and Spatial Memory The Morris Water Maze is routinely used to assess task learning and spatial memory (Jaspers et al., Neurosci. Lett 117:149-153,1990; Morris, J. NeuroscL Methods 11:47-60, 1984). In this assay, animals are placed in a water pool which is divided into quadrants. One platform is hidden in one of the quadrants. The animal is placed in the water pool and is expected to locate the hidden platform within a predetermined time. During a number of training trials, the animal learns the location of the platform and escape from the pool. The animal receives multiple trials in this task. Total distance traveled, number of trials to locate platform, latency to fin(d platform, and the swimming path is recorded for each animal. The animal's learning ability is measured by the length of time or number of trials required to find the hidden platform. Memory deficit or improvement is determined by the number of trials or the latency to find the platform at predetermined delay time after acquisition. Leaning and memory may be measured by the number of times that the animal crosses the quadrant where the platform was located during the acquisition phase. Method for Testing Drug Dependence Self-administration in animals is a predictor of a compound's abuse potential in humans. Modifications to this procedure may also be used to identify compounds that prevent or block the reinforcing properties of drugs that have abuse potential. A compound that extinguishes the self-administration of a drug may prevent that drug's abuse or its . dependence. (Ranaldi et al., Psychopharmacol. 161:442-448, 2002; Campbell et al., Exp. Clin. Psychopharmacol. 8:312-25, 2000). In a self-administration test, animals are placed in the operant chambers containing both an active and inactive lever. Each response on the active lever produces an infusion of either the test compound or a drug known to be self-administered. Presses on the inactive lever have no effect, but are also recorded. Animals are. then trained to self-administer compound/drug over a set period of time by having drug access during each daily session. Illumination of the chamber house light signals the beginning of the session and the availability of the compound/drug. When the session ends, the house light is turned off. Initially, a drug infusion occurs with every press of the active lever. Once lever-pressing behavior has been established, the number of presses to produce a drug infusion is increased. After stable compound/drug self-administration is - obtained, the effect of a second compound on the drug-reinforced behavior may be evaluated. Administration of this second compound prior to the session can either potentiate, extinguish, or produce no change to the self-administrating behavior. The following tests were carried out in order to determine the activity of the compounds of formula (I). The affinity of the compounds of the invention for cannabinoid CBl receptors was determined using membrane preparations of human embryonic kidney (HEK) cells in which the human cannabis CBl receptor is transiently transfected using the Semliki Forest Virus system in conjunction with [3H]-CP-55,940 as radioligand. After incubation of a freshly prepared cell membrane preparation with the [3H]-ligand, with or without addition of compounds of the invention, separation of bound and free ligand was performed by filtration over glassfiber filters. Radioactivity on the filter was measured by liquid scintillation counting. The affinity of the compounds of the invention for cannabinoid CB2 receptors was determined using membrane preparations of human embryonic kidney (HEK) cells in which the human cannabis CB2 receptor is transiently transfected using the Semliki Forest virus system in conjunction with [3H]-CP-55,940 as radioligand. After incubation of a freshly prepared cell membrane preparation with the [3H]-ligand, with or without addition of compounds of the invention, separation of bound of bound and free ligand was performed by filtration over glassfiber filters. Radioactivity on the filter was measured by liquid scintillation counting. The cannabinoid CBl antagonistic activity of compounds of the invention was determined by functional studies using CHO cells in which human cannabinoid CBl receptors are stably expressed (see M. Rinaldi-Carmona et. al., J. Pharmacol, Exp. Ther. 278 (1996) 871). The stable expression of the human cannabinoid receptor in cell systems was first described in Nature 1990,346, 561-564 (CBl) and Nature 1993, 365,61-65 (CB2) respectively. Adenylyl cyclase was stimulated using forskolin and measured by quantifying the atnount of accumulated cyclic AMP. Concomitant activation of CBl receptors by CBl receptor agonists (e.g. CP-55,940 or (R)-WIN-55212-2) can attenuate the forskolin-induced accumulation of cAMP in a concentration dependent manner. This CBl receptor mediated response can be antagonised by CB1 receptor antagonists such as the compounds of the invention. The compounds of formula (I) show an excellent affinity for the CB1 receptor, determined with the experimental conditions described in Devane et.al. Mol. Pharmacol. 34 (1988) 605-613. The compounds of the present invention or the pharmaceutical^ acceptable salts or sovates are antagonists and selective for the CBl receptor with affinites below IC5o = 2 \xM. They exhibit at least, a 10 fold selectivity against the CB2 receptor. Effect of CBl receptor antagonist/inverse agonist on CP 55,940-induced Hypothermia in NMRI mice Animals Male NMRI mice were used in this study and were obtained from Research Consulting Company Ltd (RCC) of Fiillinsdorf (Switzerland). Mice, weighing 30-31g were used in this study. Ambient temperature is approximately 20-21°C and relative humidity 55-65%. A 12 hours light-dark cycle is maintained in the rooms with all tests being performed during the light phase. Access to tap water and food are ad libitum. L. Method All measurements were made between 12:00 am and 5:00 pm. Mice were brought in this environment and habituated for at least two hours before the start of the experiment. •They had always free access to food and water. For each dose, 8 mice were used. Rectal body, temperature measurements were recorded by mean of a rectal probe (RET2 of Physitemp) and digital thermometer (Digi-sense n°8528-20 of Cole Parmer, Chicago USA). The probe was inserted about 3.5 cm in each mouse. The body temperature was taken 15 min before administration of either Vehicle or CB1 receptor antagonist/inverse agonist. 30 or 90 min after i.p. or p.o. administration of this compound, respectively, rectal body temperature was recorded in order to evaluate any influence of the compound itself. The CB receptor agonist CP 55,940 (0.3 mg/kg) was immediately administered intravenously, then 20 min after i.v. administration of CP 55940, body temperature was again measured. The in vivo activity of compounds of formula (1) was assessed for their ability to regulate feeding behaviour by recording food consumption in food deprived animals. Rats were trained to have access to food for 2h per day and were food deprived for 22h. When they were trained under this schedule, the amount of food taken every day during these 2h food intake session was consistent day after day. To test the ability of compounds of formula (1) to decrease food intake, 8 animals were used in a cross-over study. Rats were individually housed in Plexiglas boxes with a grid on the floor and a paper was placed below the cage floor to collect any spillage. A food dispenser (becher) filled with a pre-weighed amount of food was presented to them for 2h. At the end of the food intake session, rats returned to their home cage. Each rat was weighed before the start of the experiment and the amount of food consumed during this 2h food intake session was recorded. Either various doses of test compound or vehicle was administered orally 60 min before the 2h food intake session. A positive control Rimonabant (SR141716) was included in the experiment. An Anova analysis with repeated measures was used followed by a posthoc test Student Neumann-Keuls. P Furthermore the utility of compounds of formula (1) in diseases or disorders maybe demonstrated in animal disease models that have been reported in the literature. The following are examples of such animal disease models: a) reduction of sweet food intake in marmosets (Behavioural Pharm, 1998, 9,179-181); b) reduction of sucrose and ethanol - intake in mice (Psychophafm. 1997, 132, 104-106); c) increased motor activity and place conditioning in rats (Psychopharm. 1998, 135, 324-332; Psychopharmacol 2000, 151: 25-30); d) spontaneous locomotor activity in mice (J. Pharm. Exp. Ther. 1996, 277, 586-594); e) reduction in opiate self-administration in mice (Sci. 1999,283,401-404); The compounds of. formula (I) and/or their pharmaceutical^ acceptable salts can be -used as medicaments, e.g. in the form of pharmaceutical preparations for enteral, parenteral or topical administration. They can be administered, for example, perorally, e.g. in the form of tablets, coated tablets, dragees, hard and soft gelatine capsules, solutions, emulsions or suspensions, rectally, e.g. in the form of suppositories, parenterally, e.g. in the form of injection solutions or infusion solutions, or topically, e.g. in the form of ointments, creams or oils. Oral administration is preferred. The production of the pharmaceutical preparations can be effected in a manner which will be familiar to any person skilled in the art by bringing the described compounds of formula (I) and/or their pharmaceutical^ acceptable salts, optionally in combination with other therapeutically valuable substances, into a galenical administration form together with suitable, non-toxic, inert, therapeutically compatible solid or liquid carrier materials and, if desired, usual pharmaceutical adjuvants. Suitable carrier materials are not only inorganic carrier materials, but also organic carrier materials. Thus, for example, lactose, corn starch or derivatives thereof, talc, stearic acid or its salts can be used as carrier materials for tablets, coated tablets, dragees and hard gelatine capsules. Suitable carrier materials for soft gelatine capsules are, for example, vegetable oils, waxes, fats and semi-solid and liquid polyols (depending on the nature of the active ingredient no carriers might, however, be required in the case of soft gelatine capsules). Suitable carrier materials for the production of solutions and syrups are, for example, water, polyols, sucrose, invert sugar and the like. Suitable carrier materials for injection solutions are, for example, water, alcohols, polyols, glycerol and vegetable oils. Suitable carrier materials for suppositories are, for example, natural or hardened oils, waxes, fats and semi-liquid or liquid polyols. Suitable carrier materials for topical preparations are glycerides, semi-synthetic and synthetic glycerides, hydrogenated oils, liquid waxes, liquid paraffins, liquid fatty alcohols, sterols, polyethylene glycols and cellulose derivatives. Usual stabilizers, preservatives, wetting and emulsifying agents, consistency-improving agents, flavour-improving agents, salts for varying the osmotic pressure, buffer • substances, solubilizers, colorants and masking agents and antioxidants come into consideration as pharmaceutical adjuvants. The dosage of the compounds of formula (I) can vary within wide limits depending on the disease to be controlled, the age and the individual condition of the patient and the mode of administration, and will, of course, be fitted to the individual requirements in each particular case. For adult patients a daily dosage of about 1 to 1000 mg, especially about 1 to 100 mg, comes into consideration. Depending on severity of the disease and the precise pharmacokinetic profile the compound could be administered with one or several daily dosage units, e.g. in 1 to 3 dosage units. The pharmaceutical preparations conveniently contain about 1-500 mg, preferably 1-100 mg, of a compound of formula (I). i The following Examples serve to illustrate the present invention in more detail. They are, however, not intended to limit its scope in any manner. Examples JViS = mass spectrometry; ISP = ion spray (positive ion), corresponds to ESI and ES+ (electrospray, positive ion); mp = melting point. Example 1 1-Cyclohexylmethyl-2-methyl-5-[2 carboxylic acid butylamide The title compound was obtained using butylamine as R R NH> aminomethylcyclohexane as R -(CH2)m-NH2 and 4-nitrophenyl thioamide as R C(S)NH2, as follows: 1. Synthesis of 2-bromo-l-[2-(4-nitro-phenyl)-thiazol-4-yl]-ethanone (Compound B) To a solution of 1.4 g of l,4-dibromo-2,3-butanedione in dimethylformamide (110 ml) at room temperature was added 1.4 ml of 2,6-di-tert-butylpyridine. Then a solution of 1.0 g of 4-nitro-phenyl-thiobenzamide in 20 ml of dimethylformamide was slowly added to the reaction mixture over 1 hour. The reaction mixture was then allowed to stir for an additional hour at room temperature before being concentrated in vacuo. The residue was then purified by chromatography over a short column (SiO?, 120g, CH2CI2100%). The isolated compound was triturated with isopropylether to yield 771 mg of the title compound as a yellow solid, mp = 186-187°C, MS (EI) 326(M). 2. Synthesis of l-Cyclohexylmethyl-2-methyl-5-[2-(4-nitro-phenyl)-thiazol-4-yl]-lH- pyrrole-3-carboxylic acid butylamide To a solution of 4.2 g of diketene in.dichloromethane (70 ml) cooled at 0°C was added over 1 hour a solution of 3,7 g of butylamine in 50 ml of dichloromethane. The reaction mixture was then stirred for one hour at 0°C and then let to stir at room temperature for another hour. The reaction mixture was then concentrated in vacuo and the crude residue was partitioned in batches which were directly used in the next step. To 180 mg of the previous crude material in 5 ml of dimethylformamide was added 0.15 ml of cyclohexylmethylamine together with 0.13 ml of trimethyl orthoformate and the reaction mixture was stirred for 24 hours at room temperature. After such time, 260 mg of 2-bromo-l-[2-(4-nitro-phenyl)-thiazol-4-yl]-ethanone was added together with 0.14 ml of 2,6-lutidine and the reaction mixture was stirred for another 24 hours at room temperature. After such time, 5 ml of a MeCN-H20 (1:1) solution is added to the reaction mixture, the precipitate is filtrated and washed with MeCN-H20 (1:1) and isopropylether to yield 264 mg of the title compound as a yellow solid, mp = 184-187 °C, MS (ISP) 481.3 (M+H)+. Examples 2-375 were synthesized in analogy to Example 1, using the indicated educts. Example 2 . l-Butyl-5- [2-(2-chloro-phenyl)-thiazol-4-yl] -2-methyl-lH-pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH> butylamine as R -(CH2)m-NH2 and 2-cHoro-phenyl thiobenzamide as R4C(S)NH2, MS(ES-h) 430. (M+H)+. " l-Butyl-5-[2-(4~methoxy-phenyl)-thiazol-4^ butylamide The title compound was obtained using butylamine as R R NH, butylamine as R -(CH2)m-NH2 and 4-methoxy-phenyl thiobenzamide as R4C(S)NH2> MS(ES+) 426 (M+H)+. Example 4 5-[2-(2-Chloro-phenyl)-tHazol-4-yl]-l-isobutyl butylamide The title compound was obtained using butylamine as R R"NH, isobutylamine as R -(CH2)nrNH2 and 2-chloro-phenyl thiobenzamide as R4C(S)NH2, MS(ES+) (M+H)+. Example 5 l-I$obutyl-5-[2-(4-methoxy-phenyl butylamide The title compound was obtained using butylamine as R R NH, isobutylamine as R -(CH2)m-NH2 and 4-methoxy-phenyl thiobenzamide as R4C(S)NH2, MS(ES+) 426 (M+H)+. Example 6 l-Isobutyl-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxyUcacid butylamide The title compound was obtained using butylamine as R R NH, isobutylamine as R -(CH2WNH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 398 (M+H)+. Example 7 5-[2-(2-CHoro-phenyl)-thiazol-4-yl]-l-cyclota carboxylic acid butylamide The title compound was obtained using butylamine as RlR2NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-chloro-phenyl thiobenzamide as R4C(S)NH2> MS(ES+) 470 (M+H)+. Example 8 l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-&^ carboxylic acid butylamide The title compound was obtained using butylamine as R1R2NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxy-phenyl thiobenzamide as R4C(S)NH2> MS(ES+) 466 (M+H)+. Example 9 1-Cyclohexylmethyl-5-[-2-(4^ pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES-f) 496 (M+H)+. Example 10 l-Cyclohexylmethyl-5-[2-(2-ethyl-pyridin-4-yl)-thiazol-4-yl]-2-methyl-lH-pyrrole- carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-ethyl-4-pyridinecarbothioamide as R4C(S)NH2) MS(ES+) 465 (M+H)+. Example 11 1-Cyclohe:xylmethyl-2-methyl acid butylamide The title compound was obtained using butylamine as R R~NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 438-(M+H)+. Example 12 5-[2^2-Chloro-phenyl)-thiazol-4-yl]-2-methyl-l-(tetrahydro-furan-2-ylmetbyl)-lH^ pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 2-chlorophenyl thioamide as R4C(S)NH2, MS(ES+) 458 (M+H)+. Example 13 5-[2-(4-Methoxy-phenyl)-ftiazol pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R1R2NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 4-methoxy-phenyl thioamide as R4C(S)NH2> MS(ES+) 454 (M+H)+. Example 14 5-[2-(4-Methoxy-phenoxymethyl)-thiazol-4-yl]-2-meliyl-l-(tetrahydro-furan"2-ylmethyl)-lH-pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 484 (M+H)+. Example 15 . 5-[2-(2-Ethyl-pyridin-4-yl)-thiazol-4^ pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as RlR2NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 2-ethyI-4-pyridine carbothioamide as R4C(S)NH2, MS(ES+) 453 (M+H)+. Example 16 2-Methyl-5-[2-(6-methyl-pyridin-3-yl)-tta lH-pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 6-methyl-pyridine-3-carbothiamide as R4C(S)NH2) MS(ES+) 439 (M+H)+. Example 17 - 2-Methyl-5-(2-pyrazin-2-yta carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, tetrahydrofurfiirylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothiamide as R4C(S)NH2, MS(ES+) 426 (M+Hf. Example 18 l-(2-Mellioxy-ethyl)-5-[2-(4-m carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 2-methoxyethylamine as R3-(CH2)m-NH2 and 4-methoxy-phenyl thioamide as R4C(S)NH2> MS(ES+) 428 (M+H)+. Example 19 l-(2-Methoxy-ethyl)-2-methy^ acid butylamide The title compound was obtained using butylamine as R R NH, 2-methoxyethylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 400 (M+H)+. Example 20 5-[2-(2-Chloro-phenyl)-thia2ol-4-yl]-l-furan-2-ylmethyl-2-methyl-lH-pyrrole-3- carboxylic acid butylamide The title compound was obtained using butylamine as R^NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 2-chlorophenyl thioamide as R4C(S)NH2, MS(ES+) 454 (M+H)+. Example 21 l-Furan-2-ylmethyl-5-[2-(4-me&thoxy carboxylic acid butylamide The title compound was obtained using butylamine as RlR2NH, 3-(aminomethyl)-thiophene as R3-(CH2)m-NH2 and 4-methoxy-phenyl thioamide as R4C(S)NH2, MS(ES+) 450 (M+H)+. Example 22 5-[2-(2-Ethyl-pyridin-4-yl)-tHazol~4-yl^ carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 3-furyl methylamine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothioamide as R4C(S)NH2, MS(ES+) 449 (M+H)+. Example 23 5-[2-(2-CUoro-phenyl)-thiazol-4-yl]-l-(4-methoxy-benzyl)-2-methyl-lH carboxylic acid butylamide The title compound was obtained using butylamine as R1R2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2-chlorophenyl thioamide as R4C(S)NH2, MS(ES+) 494 (M+H)+. Example 24 l-(4-Methoxy-benzyl)-5-[2-(4~methoxy-pheny^ carboxylic acid butylamide The title compound was obtained using butylamine as R1R2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 490 (M+H)+. Example 25 l-(4-Methoxy-benzyl)-5-{2-(4-methoxy-phenoxyme&^ pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R R2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 520 (M+H)+. Example 26 5-[2-(2-Ethyl-pyridin-4-yl)-liuazol-4-yl]-l«(4-methoxy-benzyl)-2-methyl-lH carboxylic acid butylamide 9 ■ The title compound was obtained using butylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)ra-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2) MS(ES+) 489 (M+H)+. Example 27 4-[4-ButylcWrbamoyl-l-(4-methoxy-te carboxylic acid ethyl ester The title compound was obtained using butylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2, MS(ES-h) 456 (M+H)+. Example 28 l-(4-Methoxy-benzyl)-2-methyl-5-[2-(6-methyl-pyridin-3-yl)-thiazol-4-yl]-lH-pyrrole- 3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 475 (M+H)+. Example 29 - l-(4-Methoxy-benzyl)-2-methyl-5-(2-pyrazin acid butylamide The title compound was obtained using butylamine as R1R2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothiamide as R4C(S)NH2, MS(ES+) 462 (M+H)+. Example 30 5-[ 2 - (4-Methoxy-phenyl)-thiazol-4^ carboxylic acid butylamide The title compound was obtained using butylamine as RXR2NH, methoxypropylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 442 (M+H)+. Example 31 5-[2-(4-Methbxy-phenoxymrthyl) pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, methoxypropylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethane thioamide as R4C(S)NH2, MS(ES+) 472 (M+H)+. Example 32 4- [4-Butylcarbamoyl-1 - (3 -methoxy-propyl)-5-methyl- lH-pyrrol-2-yl] -thiazole-2- carboxylic acid ethyl ester The title compound was obtained using butylamine as R1R2NH, methoxypropylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2> MS(ES+) 408 (M+H)+. Example 33 5-[2-(2-CUoro-phenyl)-thiazol-4^ carboxylic acid butyiamide The tide compound was obtained using butylamine as RR NH> 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 470 (M+H)+. Example 34 5- [2-(4-Methoxy-phenyl) -thiazol-4-yl] -2-methyl-1 -thiophen-2-ylmethyl- lH-pyrrole-3- carboxylic acid butyiamide The title compound was obtained using butylamine as R R NH, 3-(aminomethyl)thiophene as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 466 (M+H)+. Example 35 5-[2-(4-Methbxy-phenoxymethyl)-thfe^^ pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R^NH, 3-(aminomethyl)thiophene as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2> MS(ES+) 496 (M+H)+. Example 36 5-[2-(2-Ethyl-pyridin-4-y])-thiazol-4-yl]-2-^^ carboxylic acid butylamide The title compound was obtained using butylamine as R R NH> 3-(aminomethyl)thiophene as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 465 (M+H)+- Example 37 . l-[2-(3,4-Dimelhoxy-phenyl)-^ lH-pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH> homoveratrylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 533 (M+H)+. Example 38 mc-l-Butyl-5-[2-(2-cUoro-phenyl)-thiazol-4-yl]--2-methyl-lH-pyrrole-3-carboxylicacid ■»►* sec-butylamide The title compound was obtained using sec-butylamine as R R NH> butylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 430 (M+H)+. Example 39 rac-l-Butyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl- acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, butylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2) MS(ES+) 426 (M+H)+. Example 40 rac-l-Butyl-5-[2-(4-meliioxy-pheno}ty^ carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, butylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 456 (M+H)+. Example 41 rac-l-Butyl-5-[2-(2-ethyl-pyri& acid sec-butylamide The title compound was obtained using sec-butylamine as R R'NH, butylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2) MS(ES+) 425 (M+H)+. Example 42 rac-5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-isobutyl-2-methyl-lH-pyrrole-3-carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, isobutylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 430 (M+H)+. Example 43 . rac-l-Isobutyl-5-[2-(4-methoxy-phenyl)^ acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, isobutylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 426 (M+H)+. Example 44 rac-1 -lsobutyl-5- [ 2-(4-methoxy-phenoxymethyl) -thiazol-4-yl] -2-methyl- lH-pyrrole-3- carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, isobutylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 456 (M+H)+. Example 45 rac-5-[2-(2-chloro-phenyl)-thia2ol-4-yl]-l-cyclohexylmethyl-2-methyl-lH-pyrrole-3- carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES-h) 470 (M+H)+. Example 46 rac-l-Cydohexylmethyl-5-[2-(4-metiioxy-^^ carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, "" * ' ' exane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as 15 f)466'(M+H)+. Example 47 rac-1-Cyclohexylmethyl^ pyrrole-3-carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2> MS(ES+) 496 (M+H)+. Example 48 rac-l-Cyclohexylmethyl-5-[2-(2-ethyl-^^ carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 465 (M+H)+. Example 49 rac-1-Cyclohexylmeth^ carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R"NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2) MS(ES+) 438 (M+H)+. Example 50 rac-5-[2»(2-Chloro-phenyl)-thiazol-4-yl]-2-methyl-l-(tetrahydro-furan-2-ylmethyl)-lH- pyrrole-3-carboxylic acid sec-butylamide 1 o The title compound was obtained using sec-butylamine as R R NH, i tetrahydrofiirfurylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2> MS(ES+) 458 (M+H)+. Example 51 . rac-5-[2-(4-Methoxy-phe^ lH-pyrrole-3-carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as RlR2NH, tetrahydrofurfurylamine as R ~(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ES+) 454 (M+H)+. Example 52 rac-5-[2-(4-Methoxy-phenoxyme^ ylmethyl)-lH-pyrrole-3-carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2j MS(ES+) 484 (M+H)+. Example 53 rac-2-Methyl-5-(2-pyrazin-2-yl-th^ pyrrole-3-carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, tetrahydrofurfurylamine as R3-(CH2)nrNH2 and pyrazine-2-carbothioamide as R4C(S)NH2) MS(ES+) 426 (M+H)+. Example 54 rac-l-(2-Methoxy-ethyl)-5-[2-(4-methoxy-phen^ carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as RlR2NH> methoxyethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 428 (M+H)+. Example 55 rac-5-[2-(2-CHoro-phenyl)-thiazol-4^ carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, 3-furylmethylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 454 (M+H)+. Example 56 rac-l-Furan-2-ylmethyl-542-(4-methoxy-phenyl)-thiazol-4-yl]-2-metityl--lH-pyrrole-3- carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R^NH, 3-furylmethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES-t-) 450 (M+H)+. Example 57 . rac-5-[2-(2-Ethyl-pyridin-4-yl carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, 3-furylmethylamine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 449 (M+H)+. Example 58 rac-5-[2-(2-CMoro-phenyl)-thiazol-4-yl]-l-(4-m carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, 4-methoxybenzyl-amine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 494 (M+H)+. Example 59 . rac4-(4-Me&oxy-benzyl)-5-[2-(4-methoxy-phen^ 3-carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH> 4-methoxybenzyl-amine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 490 (M+H)+. Example 60 rac-l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenoxymetiiyl)-lWazol-4-yl]-2-methyl-lH- pyrrole-3-carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, 4-methoxybenzyl-amine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 520 (M-hH)+. :' Example 61 raC-5-[2-(2-Ethyl-pyridin-4-yl)-to pyrrole-3-carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, 4-methoxybenzyl-amine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 489-(M+H)+. Example 62 mc-l-(4-Melhoxy-benzyl)-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3- carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, 4-methoxybenzyl-amine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 462 (M+H)+. Example 63 . rac-5-[2-(4-Methoxy-phenyl)-thiazol-4-yl 3-carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, methoxyethylamine as R3-(GH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 442 (M+H)+. Example 64 rac-5-[2-(4-Methoxy-phenoxymethylH pyrrole-3-carboxylic acid sec-butylamide The title compound was obtained using sec-butylamine as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 472(M+H)+. Example 127 1 l-Butyl-5-[2-(4-methoxy-ph cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R R'NH, butylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ES+) 466 (M+H)+. Example 128 l-Butyl-5-[2-(4-methoxy-phenoxymethyl)-thiazol"4-yl]-2-methyl-lH-pyrrole-3- carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R.R NH, butylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 496 (M+H)+. Example 129 * l-Butyl-5- [2-(2-ethyl-pyridin-4-yl)-thiazol"4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R R NH, butylamine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 465 (M-t-H)+. Example 130 5-[2-(2-Chloro-phenyl)--thiazol-4-yl]-l-isobutyl-2-methyl-lH-pyrrole-3-carboxylicacid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R.R NH, isobutylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 470 (M+H)+. Example 131 ■ l-Isobutyl-5-[2-(4-methoxy-phe^^ cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as RlR2NH> isobutylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2) MS(ES+) 466 (M+H)+. Example 132 l-Isobutyl-5-[2«(4-methoxyrphenoxymethyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3- carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R?R2NH, isobutylamine as R3-(CH2)nrNH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 496 (M+H)+. Example 133 l-Isobutyl-2-methyl-5-(2-pyrazin-2«yl-thiazol-4-yl)-lH-pyrrole-3-carboxylicacid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R^NH, isobutylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+)438(M+H)+. Example 134 l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3- carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R. R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 506 (M+H)+. Example 135 l-Cyclohexylmethyl-5-[2-(2-ethyl-py^ carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as RR2NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 505 (M+H)+. Example 136 l-Cyclohexylmethyl-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R.R"NH, aminomethylcyclohexane as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 478 "(M+H)+. Example 137 5-[2-(2-Chloro-phenyl)-thiazoI-4-yl]-^^ pyrrole-3-carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R R"NH, tetrahydrofiirfiirylamine as R -(CH2)m-NH2 and 2-chloro-pheiiyl thioamide as R4C(S)NH2J MS(ES+) 498 (M+H)+. Example 138 5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-(tetrahydro-flxran-2-ylmethyl)-lH- pyrrole-3-carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R.R NH, tetrahydrofiirfiirylamine as R -(CH2)m"NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 494 (M+H)+. Example 139 5-[2~(4-Methoxy-phenbxymethyl)-thiazol-4^ ylmethyl)-lH-pyrrole-3-carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R R NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES-h) 524 (M+H)+. Example 140 5-[2-(2-Ethyl-pyridin-4-yl)-thiazol-4-yl]^^ pyrrole-3-carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R. R NH, tetrahydrofurfurylamine as R -(CH2)m~NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 493 (M+H)+. Example 141 4-[4-(Cyclohexylmethyl-carbamoyl)-5-meth^ pyrrol-2-yl]-thiazole-2-carboxylic acid ethyl ester The title compound was obtained using aminomethylcyclohexane as R R~NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and ethylthiooxamate, MS(ES+) 460 (M+H)+. Example 142 2-Methyl-5-[2-(6-methyl-pyridin-3-yl)-thiazol-4-yl]-l-(tetrahydro-furan-2-ylmethyl)- lH-pyrrole-3rcarboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as RR NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioanlide as R4C(S)NH2. xx479 Example 143 ■ 2-Methyl-5-(2-pyrazin-2-yl"^ carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R R NH, tetrahydrofurfiirylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 466 (M+H)+. Example 144 5-[2-(2-Chloro-phenyl)-thiazol-4-ylH^ carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R- R NH, methoxyethylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2> MS(ES+) 472 (M+H)+. Example 145 l-(2-Methoxy-ethyl)-5-[2^ «»■' carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ES+) 468 (M+H)+. Example 146 l-(2-Methoxy-ethyl)-5-[2-(4-methoxy-phenoxymeliyl)-thiazol-4-yl]-2-methyl-lH- pyrrole-3-carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R -(C^m-NH^ and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2> MS(ES+) 498 (M+H)+. Example 147 5-[2-(2-Ethyi-pyridm-^ carboxylic acid cyclohexylmethyl-arnide The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 467 (M+H)+. Example 148 4-[4-(Cyclohexylmethyl-carbamoyl)-l-(2-methoxy-ethyl)-5-methyl-lH-pyrrol-2-yl]- thiazole-2-carboxylic acid ethyl ester The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2., MS(ES+) 434 (M+H)+. Example 149 • l-(2-Methoxy-ethyl)-2-methyl-5-[2-(6-m^ carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R^NH, methoxyethylamine as R3-(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 453 (M+H)Example 150 l-(2-Methoxy-ethyl)-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxylic acid cyclohexylmethyl-amide t The title compound was obtained using aminomethylcyclohexane as R-R NH, methoxyethylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R C(S)NH2, MS(ES+) 440 (M+H)+. Example 151 l-(2-Cyclohex-l-enyl-^ pyrrole-3-carboxylic acid cyclohexylmethyl-amide The title compound was obtained using arninomethylcyclohexane as R R NH, 2-(l-cyclohexenyl)ethylamine as R -(CH2)nrNH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 517 (M+H)+. Example 152 l-Furan-2-ylmethyl-5-[2--(4-methoxy-phenyl)-tliiazol-4-yl]-2-methyHH-pyrrole-3- carboxylic acid cyclohexylmethyl-amide The title compound was obtained using arninomethylcyclohexane as R.R NH, 3-furylmethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ES+) 490 (M+H)+. Example 153 5-[2-(2-CMoro-phenyl)-t^ »■* carboxylic acid cyclohexylmethyl-amide i i The title compound was obtained using aminomethylcyclohexane as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2, MS(ES+) 534 (M+H)+. Example 154 l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3- carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2, MS(ES+) 530 (M+H) Example 155 " 5-[2-(2-Ethyl-pyridin-4-yl)-thiazol-4^ carboxylic acid cyclohexylmethyl-amide The tide compound was obtained using aminomethylcyclohexane as R!R2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridihe carbothiamide as R4C(S)NH2, MS(ES+) 529 (M+H)+. Example 156 5-[2-(2-Chloro-phenyl)-thiazol"4-yl]-l-(3-methoxy-propyl)-2-methyl~lH-pyrrole-3- carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2, MS(ESH-) 486 (M+H)+. ■r Example 157 • 5-[2-(4~Methoxy-phenyl):thiazol-4-yl]-l-(3-m carboxylic acid cyclohexylmethyl-amide " The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ES+) 482 (M+H)+. Example 158 5-[2-(4-Methoxy-phenoxymethyl)-thiazol-4-yl]-l-(3-methoxy-propyl)-2-methyl-lH- pyrrole-3-carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R.R NH, methoxyethylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 512 (M+H)+. .Example ypy ' 5-[2-(2-Ethyl-pyridin-4-y^ carboxylic acid cyclohexylmethyl-amide The tide compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 481 (M+H)+. Example 160 4-[4-(Cyclohexylmethyl-carbamoyl)-l-(3-methoxy-propyl)-5-methyl-lH-pyrrol-2"yl]- thiazole-2-carboxylic acid ethyl ester The title compound was obtained using aminomethylcyclohexane as R.R NH, methoxyethylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2., MS(ES+) 448 (M+H)+. Example 161 * l-(3-Methoxy-propyl)-2-methyl-5-(2-pyrazin-2-yM^ acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R3-(CH2)nrNH2 and pyrazine-2-carbothioamide as R4C(S)NH2,(-MS(ES+) 454 (M+H)+. Example 162 5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-thiophen-2-ylmethyl-lH-pyrrole-3- carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as R. R NH, 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 506 (M+H)+. Example 163 ' 5-[2-(2-Ethyl-pyridin-4-^ carboxylic acid cyclohexylmethyl-amide The title compound was obtained using aminomethylcyclohexane as RR2NH, 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES-f) 505 (M+H)+. Example 164 5-[2-(2-Chloro-phenyl)-thiazol-4^ pyrrole-3-carboxylic acid cyclohexylmethyl-amide / The title compound was obtained using aminomethylcyclohexane as R. R NH, homoveratrylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2, MS(ES+) 578 (M+H)+. Example 165 l-Butyl-5-[2-(4-methoxy-phenyl)-thiazol-^^ (tetrahydro-furan-2-ylmethyl)-amide * \ The title compound was obtained using tetrahydrofurfurylamine as R R NH, butylamine as R3-(CH2)m-NH2 and 4^methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 454 (M+H)+. Example 166 4-{l-Isobutyl-5-methyl-4-[(tetrahydro-furan-2-ylmethyl)-carbamoyl]-lH-pyrrol-2-yl^ thiazole-2-carboxylic acid ethyl ester The title compound was obtained using tetrahydrofurfurylamine as R R NH, isobutylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2, MS(ES+) 420. (M+H)+. Example 167 l-Isobutyl-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxylica (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R1R2NH, isobutylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 426 (M+H)+. Example 168 5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-cyclohexylmethyl-2-methyl-lH-pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 498 (M+H)+. Example 169 l-Cyclohexylmethyl-5-[2^ carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2) MS(ES+) 494 (M+H)+. Example 170 l^yclohexylmethyl-5-[2-(4rmethoxy-phenoxym pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl) -amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2) MS(ES+) 524 (M+H)+. Example 171 l-Cyclohexylmethyl-5-^ carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide i i The title compound was obtained using tetrahydrofiirfurylamine as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 493 (M+H)+. Example 172 l-Cyclohexylmethyl-2-methyl-5-(2-pyrazin~2^ acid (tetrahydro-furan-2-ylmethyl) -amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 466 (M+H)+. Example 173 5-[2-(2-Chloro-phenyl)-tliiazol-4-yl]^ pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES-t-) 486 (M+H)+. Example 174 2-Methyl-5-(2-pyrazin-2-yl-thiazol-4-yl^ carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The tide compound was obtained using tetrahydrofurfurylamine as R R NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2> MS(ES+) 454 (M+H)+. Example 175 5-[2-(2-EthyI-pyridin-4-yI)-thiazol-4-yl]-l-(2-m^ carboxylic acid (tetrahydro-furan-2-ylrnethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, methoxyethylamine as R -(CH2)m-NH2 and 2-ethyI-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 455 (M+H)+. Example 176 5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-furan-2-ylmethyl-2-methyl-lH-pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, 3-furylmethylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2> MS(ES+) 482 (M+H)+. Example 177 l-Furan-2-ylmethyl-5-[2-(4-m carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as RlR2NH, 3-furylmethylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2, MS(ES+) 478 (M+H)+. Example 178 5-[2-(2-Ethyl~pyridin-4-ylMhm^ carboxylic acid (tetrahydro-furan-2-ylmethyl) -amide The title compound was obtained using tetrahydrofurfurylamine as RlR2NH, 3-furylmethylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 477 (M+H)+. Example 179 - l-(4-Methoxy~benzyl)-^ (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofiirfurylamine as R R NH> 4-methoxybenzylamine as R3-(CH2)m-NH2 and thioacetamide as R4C(S)NH2, MS(ES-i-) 426 (M+H)+. Example 180 5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-(4-methoxy-benzyl)-2-methyl-lH"pyrrole-3- carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, 4-methoxybenzylamine as R -(CH2)nrNH2 and 2-chloro-phenyl thioamide as R C(S)NH2, MS(ES+) 522 (M+H)+. Example 181 1 -(4-Methoxy-benzyl)-5- [2- (4-methoxy-phenyl)-thiazol-4-yl] -2-methyl- lH-pyrrole-3- ~arboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2> MS(ES+) 518 (M+H)+, Example 182 l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 548 (M+H)+. 9 Example 183 4-{l-(4-Methoxy-benzyl)-5-methyl-4-[(tetrahydro-furan«2-ylmethyl)-carbam pyrrol-2-yl}-thiazole-2-carboxylic acid ethyl ester The title compound was obtained using tetrahydrofurfurylamine as R R NH, 4-methoxybenzyiamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2.> MS(ES+) 484 (M+H)+. Example 184 i l-(4-Methoxy-benzyl)-2-methyl-5-[2-(6-methyl-pyridin-3-yl)-thiazol-4-yl]-lH-pyrrole- 3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2> MS(ES+) 503 (M+H)+. Example 135 l-(4-Methoxy-benzyl)-2-met^ acid (tetrahydro-fiiran-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as RlR2NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R C(S)NH2, MS(ES+) 490 (M+H)+. Example 186 5-[2-(2-Ethyl-pyridin-4-yl)-thiazol-4-yl]-l-(3-methoxy-propyl)-2-methyl-lH-pyrrole-3- carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, methoxyethylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 469 (M+H)+. Example 187 ■ ' l-(3-Methoxy-propyl)-2-me^ 3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfarylamine as R R NH, methoxyethylamine as R -(CH2)m-NH2 and 6-methyl-pyridine~3-carbothioamide as R4C(S)NH2, MS(ES+) 455 (M+H)+. Example 188 \ l-(3-Methoxy-propyl)-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl) -amide The title compound was obtained using tetrahydrofurfurylamine as R R NH* methoxyethylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R C(S)NH2, MS(ES+) 442 (M+H)+. Example 189 5-[2-(2-Chloro-phenyl)-thiazol^ carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH> 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2j MS(ES+) 498 (M+H)+. Example 190 5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-thiophen-2-ylmethyl-lH-pyrrole-3- carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, 3-(aminomethyl)thiophene as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 494 (M+H)+. Example 191 5-[2-(2-Ethyl-pyridin-4-yl^ carboxylic acid (tetrahydro~furan-2-yimethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 2~ethyl-4-pyridine carbothiamide as R4C(S)NH2) MS(ES+) 493 (M+H)Example 192 l-[2-(3,4-Dimetho:^-phenyl)-^ lH-pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide The title compound was obtained using tetrahydrofurfurylamine as R R NH, homoveratrylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 561 "(M+H)+. Example 193 • l-Butyl-5-[2-(4-methoxy-phenyl)-thiaz^ (2-methoxy-ethyl)-amide The title compound was obtained using methoxyethyiamine as R!R2NH, butylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES-h) 428 (M+H)+. Example 194 5-[2-(2-Chloro-phenyl)-thiazoI-4-yI]-l-cycto^ carboxylic acid (2-methoxy-ethyl)-arnide The title compound was obtained using methoxyethyiamine as R^NH, aminomethylcyclohexane as R ~(CH2)m~NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2> MS(ES+) 472 (M-hH)+. Example 195 l-Cyclohexylmethyl-5-[2-(4-metho carboxylic acid (2-methoxy-ethyl)-amide The title compound was obtained using methoxyethylamine as R R NH, arninomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 468 (M+H)+. Example 196 l-Cyclohexylmethyl-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]--2-methyl-lH- pyrrole-3-carboxylic acid (2-methoxy-ethyl)-amide The title compound was obtained using methoxyethylamine as R R NH, arninomethylcyclohexane as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2> MS(ES+) 498 (M+H)+. Example 201 l-Furan-2-ylmethyl-5-[2^^ carboxylic acid (2-methoxy-ethyl)-amide The title compound was obtained using methoxyethylamine as R R NH, 3-furylmethylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2> MS(ES+) 452 (M+H)+. Example 202 5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-(4-methoxy-benzyl)"2-methyl-lH-pyrrole-3- carboxylic acid (2~methoxy-ethy])-amide The title compound was obtained using methoxyethylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2> MS(ES+) 496 (M+H) Example 203 l-(4-Methoxy4>enzyI)-5-[2-(4-methoxy-pta carboxylic acid (2-methoxy-ethyl)-amide The title compound was obtained using methoxyethylamine as RlRNH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2, MS(ES+) 492 (M+H)+. Example 204 l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-lH- pyrrole-3-carboxylic acid (2-methoxy-ethyl)-amide The title compound was obtained using methoxyethylamine as R^NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 522 (M+H)+. Example 205 5-[2-(2-Ethyl-pyridin-4-yl)-^ carboxylic acid (2-methoxy-ethyl)-amide The title compound was obtained using methoxyethylamine as R1R2NH> 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 491 (M+H)+. Example 206 4-[l-(4-Methoxy-benzyl)-4-(2-methoxy-ethylcarbamoyl)-5--methyl--lH-pyTrol-2-yl]- thiazole-2-carboxylic acid ethyl ester The title compound was obtained using methoxyethylamine as RlR2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2o MS(ES+) 458 (M+H) Example 209 l-f2-(3,4-Dimethoxy-pheny^ lH-pyrrole-3-carboxylic acid (2-methoxy-ethyl)-amide The title compound was obtained using methoxyethylamine as R R NH, homoveratrylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES-b) 535 (M+H)+. Example 210 l-Butyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylicacid (2-cyclohex-l-enyl-ethyl)-amide The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as R R NH, butylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 478 (M+H)+. Example 211 l-Cyclohexylmethyl-5-[2^ carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as RlR2NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 518 (M+H)+. Example 212 l-Cyclohexylmethyl-5-[2-(2-ethyl-pyridin-4-^^^ carboxylic acid (2-cyclohex-l-enyl~ethyl)-amide The tide compound was obtained using 2-cyclohex-l-enyl-ethylamine as RR2NH> aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 517 (M+H)+. Example 213 5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-(tetrahyd pyrrole-3-carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as R^NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 506 (M+H)+. Example 214 5-[2-(2-Ethyl-pyridin-4-yl)-thm^ pyrrole-3-carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as RlR2NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 505 (M+H)+. Example 21 5 2-Methyl-5-[2-(6-methyl-pyri^ lH-pyrrole-3-carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as R R"NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 491 (M+H)+. Example 216 l-(2-Methoxy-ethyl)-2-methyl-5-[2-(6-methyl-pyridin-3-yl)-thiazol--4-yl]-lH-pyrrole-3- carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 465 (M+H)+. Example 217 5-[2-(2-Ethyl-pyridin-4-yl)-to^ carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as RlR2NH> 3-furylmethylamine as R3-(CH2)nrNH2 and 2-ethyi-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 501 (M+H)+. Example 218 5-[2-(2-Ethyl-pyridin-4-yI)-thiazol-4-yl]-l-(4-methoxy-benzyl)-2-methyl-lH-pyrrole-3- carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as R R"NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 54-1 (M+H)+. Example 221 rac-l-Butyl-5-[2-(4-methoxy-phenyl)-thia2ol-4-yl]-2-methyl"lH-pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH, butylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 482 (M+H)+. Example 222 mc-l-Butyl-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-lH-pyrrQle-3- carboxylic acid (2-ethyl-hexyl)-amide 1 "5 ^ The title compound was obtained using 2-ethyl-hexylamine as R R NH, butylamine as R -(CH2)ra-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 512 (M+H)+. Example 223 rac-l-Butyl-5-[2-(2-ethyl-pyri acid (2-ethyl-hexyl)-amide The tide compound was obtained using 2-ethyl-hexylamine as R R NH> butylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 481 (M+H)+. Example 224 rac-4-[l-Butyl-4-(2-ethyl-hexylcarbamoyl)-5-methyl-lH-pyrrol-2-yl]-thiazole-2- carboxylic acid ethyl ester 1 9 ^ The title compound was obtained using 2-ethyl-hexylamine as R R NH, butylamine as R -(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2, MS(ES+) 448 (M+H)+. Example 229 ' mc-l-Isobutyl-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxylic acid (2- ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH, isobutylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 454 (M+H)+. Example 230 rac-5-[2-(4-Methoxy-phenoxymethyl)-thiazol-4-yl]-l-[2-(4-methoxy-phenyl)-ethyl]-2-methyl-lH-pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH, 2-(l-cyclohexenyl)ethylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2> MS(ES+) 590 (M+H)+. Example 231 rac-5-j2-(2-Ethyl-pyrid^ lH-pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH> 2-(l-cyclohexenyl)ethylamine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 559 (M+H)+. Example 232 rac-5-[2-(2-CUoro-phenyl)-tiiiazol-4-yl]-l-cyclohexylmethyl-2-methyl-lH-pyrrole-3- carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH> aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 526 (M+H)+. Example 233 rac-1 - Cyclohexylmeth^ carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R^NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 522 (M+H)+. Example 234 rac-l-Cyclohexylmethyl-5-[2-(2-ethyl-pyrid^ carboxylic acid (2-ethyl-hexyl)-amide l ^ The title compound was obtained using 2-ethyl-hexylamine as R R NH, aminomethylcyclohexane as R3-(CH2)nrNH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 521 (M+H)+. Example 235 ra.c-4- [ l-Cyclohexylmethyl-4-(2-ethyl-hexylcarbamoyl)-5-methyl- lH-pyrrol-2-yl] - thiazole-2-carboxylic acid ethyl ester The title compound was obtained using 2-ethyl-hexylamine as R R NH, aminomethylcyclohexane asR -(CH2)m-NH2 and ethylthiooxamate as R C(S)NH2-> MS(ES+) 488 (M+H)+. Example 236 rac-l-Cyclohexylmethyl-2-methyl-5-[2-(6-methyl-pyridin-3-yl)-thiazol-4-yl]-lH-pyrrole- 3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R]R2NH, aminomethylcyclohexane asR3-(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 507 (M+H)+. Example 237 rac-1-Cyclohexylmet^ rii> carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2) MS(ES+) 494 (M+H)+. i Example 238 rac-5-[2-(2-Chloro-phenyl)-thiazol^ pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2,MS(ES+) 514 (M+H)+. Example 239 rac-5-p-(4-Methoxy-phenyl)-thiazol-4-yl]-2-m^ lH-pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as RlR2NH> tetrahydrofurfurylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 510 (M+H)+. Example 240 rac-5-[2-(4-Methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-l-(tetrahydro-furan«2«-ylmethyl)-lH-pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R1R2NH, tetrahydrofiirfurylamine as.R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES-h) 540 (M+H) Example 243 rac-2-Methyl-5-[2-(6-me^ ylmethyl)-lH-pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyI-hexylamine as R R NH, tetrahydrofurfurylamine as R "(CH2)m~NH2 and 6-methyI-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 495 (M-hH)Example 244 rac-2-Methyl-5-(2~pyrazin-2-yl-tM pyrrole-3-carboxyiic acid (2-ethyl-hexyl)-amide i i The title compound was obtained using 2-ethyl-hexylamine as R R NH, tetrahydrofurfurylamine as.R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 482 (M+H)+. Example 245 rac- lT(2-Methoxy-ethyl)-5-[2-(4-meft carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH, methoxyethylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2, MS(ES+) 484 (M+H)+. Example 246 rac- l-(2-Methoxy-ethyl)-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-lH- pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The tide compound was obtained using 2-ethyl-hexylamine as R1R2NH, methoxyethylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2 MS(ES+) 514 (M+H)+. Example 247 rac-l-(2-Methoxy-ethyl)-2-m^ pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as RlR2NH, methoxyethylamine as R -(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 469 (M+H)+. Example 248 mc-l-(2-Methoxy-ethyl)-2-metliyl-5-(2-pyra2in-2-yl-thia2ol«4-yl)«lH-pyrrole-3- carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R1R2NH methoxyethylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R C(S)NH2, MS(ES+) 456 (M+H)+. Example 249 ' rac-l.-j;2-Cyclohex-l-enyl-ethyl)-5-[2-(2-ethyl-pyridin-4-yl)-thiazol-4-yl]-2-methyl-lH- pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH> 2-(l-cyclohexenyl)ethylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2) MS(ES+) 533 (M+H)+. Example 250 rac-542-(2-Chloro-phenyl)-thiazol-4-yl]-l-furan-2-ylmethyl-2-methyl-lH-pyrrole- carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R1R2NH, 3-fiirylmethylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2, MS(ES+)510(M+H)+. Example 253 rac-l-(4-Methoxy-benzyl)-2-methyl-5-(2-methyl-thiazol-4-yl)-lH acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as RlR2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and thioacetamide as R4C(S)NH2, MS(ES+) 454 (M+H)+. Example 254 rac-5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-(4-methoxy-benzyl)-2-methyl-lH-pyrrole-3- carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as RlR2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 550 (M+H)+. Example 255 mc-l-(4-Methoxy-benzyl)-5-^ 3-carboxylic acid (2-ethyl-hexyl) -amide The title compound was obtained using 2-ethyl-hexylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 546 (M+H)+. Example 256 rac-l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phe^^ pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES-h) 576 (M+H)+. Example 257 rac-5-[2-(2-Ethyl-pyridin-4^ pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R"NH, 4- t methoxybenzylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2,MS(ES+) 545 (M+H)+. Example 258 mc-l-(4-Methoxy-benzyl)-2-methyl-5-[2-(6-methyl-pyridin-3-yl)-thiazol-4-yl]-lH- pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH, 4-methoxybenzylamine as R r(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 531 (M+H)+. Example 259 rac-l-(4-Metho^-benzyl)-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3- carboxylic acid (2-ethyl-hexyl)-amide i o The title compound was obtained using 2-ethyl-hexylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R C(S)NH2> MS(ES+) 518 (M+H)+. Example 260 rac-l-(3-Methoxy-propyl)-2-methyl-5-(2-methyl-thiazol-4-yl)-lH-pyrrole-3-carboxylic acid (2~ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and thioacetamide as R4C(S)NH2, MS(ES+) 406 (M+H),+. Example 261 rac-5-j2-(4-Methoxy-phenyl)-^ 3-carboxylic acid (2-ethyl-hexyl)-amide i 2 The title compound was obtained using 2-ethyl-hexylamine as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 498 (M+H)+. Example 262 rac-5-[2-(4-Methoxy-phenoxymethyl)-thiazol-4-yl]-l-(3-methoxy-propyl)-2-methyl-lH- pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as R R NH, methoxyethylamine as R -(CH2)m~NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES-h) 528 (M+H)+. Example 263 rac-4-[4-(2-Ethyl-hexylcaA thiazole-2-carboxylic acid ethyl ester The title compound was obtained using 2-ethyl-hexylamine as RR"NH, methoxyethyl-amine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2, MS(ES+) 564 (M+H)+. Example 264 rac-l-(3-Methoxy-propyl)-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrok-3- carboxylic acid (2-ethyl-hexyl)-amide 1 5 The title compound was obtained using 2-ethyl-hexylamine as R R NH, methoxyethylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R C(S)NH2, MS(ES+) 470 (M+H)+. Example 267 rac-5-[2-(4-Methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-l-thioph pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide The title compound was obtained using 2-ethyl-hexylamine as RlR2NH, 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 552 (M+H)Example 268 rac-5-[2-(2-Ethyl-pyridin-4-yl)-^ pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide to The title compound was obtained using 2-ethyl-hexylamine as R R NH, 3-(aminomethyl)thiophene as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 521 (M+H)+. Example 273 l-Is9,butyl-2-methyl-5-(2-pyrazm methoxy-propyl)-amide The tide compound was obtained using methoxypropylamine as R R NH, isobutylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2> MS(ES+) 414 (M+H)+. Example 274 5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-cyclohexylmethyl-2-methyl-lH-pyrrok-3- carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R^NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 486 (M+H)+. Example 275 l-Cyclohexylmethyl-5-[2-(4-methoxy-pheny^ carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as RR2NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 482 (M+H)+. Example 276 l-Cyclohexylmethyl-5-[2-(4:methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide i ) The title compound was obtained using methoxypropylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 512 (M+H)+. Example 277 1-Cyplohexylmethyl^ carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R R NH, aminomethylcyclohexane as R3-(CH2)mNH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 481 (M+H)+. Example 278 l-Cyclohexylmethyl-2-methyl-5--(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as . R4C(S)NH2, MS(ES+) 454 (M+H)+. Example 279 5~[2-^4-Metho:xy-phenyl)-thiaz pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as RR NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 470 (M+H)+. Example 280 5-[2-(4-Methoxy-phenoxymethyl)^ ylmethyl)-lH-pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R R NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 500 (M+H)+. Example 281 H^Cydohex-l-enyl-^ pyrrole-3-carboxylic acid (3-methoxy~propyl)-amide The title compound was obtained using methoxypropylamine as R R NH, 2-(l-cyclohexenyl)ethylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 493 (M+H)+. Example 282 5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-furan-2-ylmethyl-2-methyl-lH-pyrrole-3- carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R R NH, 3-furylmethylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2, MS(ES+) 470 (M+H)+. l-Furan-2-ylmethyl-5-[2-(4-methoxy-ph^ carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R^NH, 3-furylmethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 466 (M+H)+. Example 284 1-Furan-2-ylmethyl-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-1H-pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as RlR2NH, 3-furylmethylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2) MS(ES-h) 496 (M+H)+. Example 285 l-(4-]^ethoxy-benzyl)-2-methy^ (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and thioacetamide as R4C(S)NH2, MS(ES+) 414 (M+H)+. Example 286 5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-(4-methoxy-benzyl)-2-methyl-lH«pyrrole-3- carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2> MS(ES) 510 (M+H)+. Example 287 l-(4-Metho;xy^ carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R1R2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2. 506 Example 288 l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-metiiyl-lH- pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2~(4-methoxyphenoxy)ethanethioamide as R4C(S)]SfH2) MS(ES+) 536 (M+H)+. Example 289 5^2-(\|2-Ethyl-pyridin-4-yl)-&^^ carboxylic acid (3-rnethoxy«propyl)-amide The title compound was obtained using methoxypropylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 289 (M+H)+. Example 290 4-[l-(4-Methoxy-benzyl)-4-(3-methoxy-propylcarbamoyi)-5"methyl-lH-pyrrol-2-yl]- thiazole-2-carboxylic acid ethyl ester The title compound was obtained using methoxypropylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2., MS(ES+) 472 (M+H)+. Example 293 5-[2;(2-CUoro-phenyl)-^ carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R R NH, 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2) MS(ES+) 486 (M+H)+. Example 294 5-[2-(4-Methoxy-phenyl)-thia2ol-4-yl]-2-me&^ carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R R NH, 3-(aminomethyl)thiophene as R -(CH2)nrNH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 482 (M+H)+. Example 295 ' 542-(2-Ethyl-pyridin-4-yl)-thiazol-4-yl]-2-methyl-l-thiophen-2-ylmethyl-lH-pyrrole-3- carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as R R NH, 3-(aminomethyl)thiophene as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 481 (M-fH)+. Example 296 1- [2-(3>4-Dimethoxy-phenyl)-ethyl] -5- [2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide The title compound was obtained using methoxypropylamine as RlR2NH, homoveratrylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2> MS(ES+) 580 (M+H)+. Example 297 4-[K[,2-(3,4-Dimethoxy-pte^ pyrrol-2-yl]-thiazole-2-carboxylic acid ethyl ester The title compound was obtained using methoxypropylamine as R R NH, . homoveratrylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2, MS(ES+) 516 (M+H)+. Example 298 l-Cyclohexylmethyl-5-[2-(4»methoxy-phenyl)-tWazol-4-yl]-2-methyl-lH-pyrrole-3- carboxylic acid morpholin-4-ylamide r The title compound was obtained using 1-amino-morpholine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 495.3 (M+H)+. Example 299 l-Cyclohexylmethyl-5-[2-(4-methoxy-phen^ carboxylic acid piperidin-1-ylamide The title compound was obtained using 1-amino-piperidine as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 493.4 (M+H)+. Example 300 l-(4-Chloro-phenyl)-5-[2-(4-methoxy-pheny^ carboxylic acid butylamide The tide compound was obtained using butylamine as R R NH, 4-chloroaniline as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ISP) 480.3 (M+H)+. Example 301 l-Cyclohexylmethyl-5-[2-(4-methoxy-pta carboxylic acid (3,4-dimethoxy-phenyl)-amide The title compound was obtained using 3,4-dimethoxy aniline as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ISP) 5463 (M+H)+. Example 302 l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3- carboxylic acid (2-nitro-phenyl)-amide The title compound was obtained using 2-nitroaniline as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ISP) 531.3 (M+H)+. Example 303 l-Cyclohexylmethyl-5-[2-(4-methoxy-pheny^ carboxylic acid (4-trifluoromethyl-phenyl)-amide The title compound was obtained using 4-trifluoromethylaniline as RJR2NH5 aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2? MS(ISP) 554.3 (M+H)+. Example 304 N'-{ l-Cyclohexylmethyl-5- [2-(4-methoxy-phenyl)-thiazol-4-yl] -2-methyl- lH-pyrrole-3- carbonylj-hydrazinecarboxylic acid ethyl ester. The title compound was obtained using ethyl carbazate as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 497.4 (M+H)+. Example 305 l-Cyclohexylmethyl-5-[2-(4-me carboxylic acid (pyridin-2-ylmethyl)-amide The title compound was obtained using 2-(aminomethyl)pyridine as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 501.3 (M+H)+. Example 306 l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3- carboxylic acid (4-chloro-phenyl)-amide The title compound was obtained using 4-chloro-aniline as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 520.3 (M+H)+. Example 313 l-(2-pyclohexyl-et^ carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 2-cyclohexyl-ethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ISP) 480.4 (M+H)+. Example 314 l-(3,5-Dimethyl-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3- carboxylic acid butylamide 1 0 The title compound was obtained using butylamine as R R NH, 3,5-dimethylbenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 488.3 (M+H)+. Example 319 ' 5-[2-(4-Methoxy-phenyl)-tta^ 3-carboxylic acid butylamide The title compound was obtained using butylarnine as R R NH, 4-(2-aminoethyl)morpholine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2) MS(ISP) 483.3 (M+H)+. Example 320 l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazoi-4-yl]-2-methyMH-pyrrole-3- carboxylic acid (4-methyl-thiazol-2-yl)-amide The title compound was obtained using 2-amino-4-methylthiazole as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 507.3 (M+H)+. Example 321 l-(3:Methoxy-benzyl)-5-[2-^ carboxylic acid butylamide The title compound was obtained using butylamine as R!R2NH, 3-methoxybenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 490.3 (M+H)+. Example 322 l-(3,5-Dichloro-benzyl)-5-[2-(4-methoxyTphenyl)-thiazol-4-yl]-2-methyl-lH-pyrxole-3- carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 3,5-dichloroaniline as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 528.2 (M+H)+, Example 323 Mndan-2-yl-5-[2-(4-methoxy-phenyl)-th^^ acid butylamide The title compound was obtained using butylamine as R^NH, 2-aminoindane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 486.4 (M+H)+. Example 324 l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3- carboxylic acid pyrimidin-2-ylamide The title compound was obtained using 2-aminopyrimidine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2) MS(ISP) 488.3 (M+H)+. Example 325 l-(3,4-Dihydroxy-benzyl)-5-[2-(4-m 3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 3,4-dihydroxybenzylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 492.3 (M+H)+. Example 326 5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-(3-piperidin-l-yl-propyl)-lH-pyrrole- 3-carboxylic acid butylamide The title compound was obtained using butylamine as R^NH, 3-piperidino-propylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 495.4 (M+HX+, Example 327 rac-l:Cyclohexylmethyl-5-[2-^^ carboxylic acid (5-hydroxy-2,2,6-trimethyl-cydohexylmethyl)-amide The title compound was obtained using aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 564.4 (M+H)+. Example 328 5-[2-(4-Metlioxy-phenyl)-thiazol-4-yl]»2-methyl-l-(3-trifluoromethoxy-benzyl)-lH- pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 3-(trifluoromethoxy)benzylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 544.4 (M+H)+. Example 329 5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-(4-trifluoromethoxy-benzyl)-lH- pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 4-(trifluoromethoxy)benzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 544.3 (M+H)+. Example 330 5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-me pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, (3-methyl-2- T JL thienyl)methylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2> MS(ISP,) 480.3 (M+H)+. Example 345 l-Cy;clohexylmethyl-2-methyl-5-(2-m-tolyl-thiazol-4-yl)-lH-pyrrole-3-carb butylamide The title compound was obtained using butylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 3-methylphenyl thioamide as R4C(S)NH2, MS(ISP) 450.3 (M+H)+. Example 346 l-Cyclohexylmethyl-2-methyl-5-(2'-me^ carboxylic acid butylamide The title compound was obtained using butylamine as R^NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-methyl-l,3-thiazole-4-carbothioamide as R4C(S)NH2, MS(ISP) 457.3 (M+H)+. Example 353 l-C^lohexylmethyl-5-[2-(2,4-dichloro-phenyl)-thiazol-4-yl] carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, aminomethylcyclohexane as R3-(CH2)nrNH2 and 2,4-dichlorophenyl thioamide as R4C(S)NH2, MS(ISP) 504.2 (M+H)+. Example 354 l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-metiLyl-lH-pyrrole-3^ carboxylic acid pentylamide The title compound was obtained using pentylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2,MS(ISP) 481.3 (M+H)+. Example 357 1-GyclohexylmethyU^ carboxylic acid cyclopentylamide The title compound was obtained using cyclopentylamine as RlR2NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2J MS(ISP) 478.3 (M+H)+. Example 358 l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3- carboxylic acid cyclopropylamide The title compound was obtained using cyclopropylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ISP) 450.3 (M+H)+. Example 359 1 - Cy clohexylmethyl-5-^ carboxylic acid cyclobutylamide The title compound was obtained using cyclobutylamine as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 464.3 (M+H)+. Example 360 (trans) rac-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2"methyl--lH-pyrrole-3-carboxylic acid (2-hydroxy-cyclopentyl)-amide The title compound was obtained using trans-2-aminocyclopentanol as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 494.3 (M+H)+. Example 361 l-(4;CMoro-benzyl)-5-[2-(4-^^ carboxylic acid butylamide The title compound was obtained using butylamine as R!R"NH, 4-chloroaniline as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 494.2 (M+H)+. Example 362 l-(3,4-DicUoro-benzyl)-5-[2-(4-methdxy-:phenyl)-thiazol-4-yl]--2-methyl-lH-pyrrole-3- carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 3,4-dichloroaniline as R -(CH2)nrNH2 and 4-methoxyphenyl thioamide as R4C(S)NH2) MS(ISP) 527.2 (M+H)+. Example 365 5-[2;(4-Methoxy-phenyl)-tH carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 2-methylbenzylamine as R3-(CH2)nrNH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ISP) 474.3 (M+H)+. Example 366- l-(3,4-Dimethoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-* 3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 3,4-dimethoxybenzyl-amine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 520.4 (M+H)+. Example 367 l-(3,4^Dimethyl-benz^ carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 2,4-dimethoxybenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 520.3 (M+H)+. Example 368 l-(3,5-Dimethoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole- 3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, 3,5-methoxybenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 520.3 (M+H)+. Example 377 rac-l-(5-Hydroxy-l>3,3-trimethyl-cycto^ yl]-2-methyMH-pyrrole-3-carboxylic acid butylamide The title compound was obtained using butylamine as R R NH, S-aminomethyl-S^S-trimethyl-cyclohexanol as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2. MS(ISP) 524.4 (&+H)+. Galenical Examples Example A Film coated tablets containing the following ingredients can be manufactured in a conventional manner: Ingredients Per tablet Kernel: Compound of formula (I) 10,0 mg 200.0 mg Macrocrystalline cellulose 23.5 mg 43.5 mg Lactose hydrous 60.0 mg 70.0 mg Povidone K30 12.5 mg 15.0 mg Sodium starch glycolate 12.5 mg 17.0 mg Magnesium stearate 1.5 mg 4.5 mg (Kernel Weight) 120.0 mg 350.0 mg Film Coat: Hydroxypropyl methyl cellulose 3.5 mg 7.0 mg;' Polyethylene glycol 6000 0.8 mg 1.6 mg Talc 1.3 mg 2.6 mg Iron oxyde (yellow) 0.8 mg 1.6 mg Titan dioxide 0.8 mg 1.6 mg The active ingredient is sieved and mixed with microcrystalline cellulose and the mixture is granulated with a solution of polyvinylpyrrolidone in water. The granulate is mixed with sodium starch glycolate and magesiurn stearate and compressed to yield kernels of 120 or 350 mg respectively. The kernels are lacquered with an aq. solution / suspension of the above mentioned film coat. Example B Capsules containing the following ingredients can be manufactured in a conventional manner: • Ingredients Per capsule Compound of formula (I) 25.0 mg Lactose 150.0 mg Maize starch 20.0 mg Talc 5.0 mg The components are sieved and mixed and filled into capsules of size 2. Example C Injection solutions can have the following composition: Compound of formula (I) 3.0 mg 'Pi Polyethylene glycol 400 150.0 mg Acetic acid q.s. ad pH 5.0 Water for injection solutions ad 1.0 ml The active ingredient is dissolved in a mixture of Polyethylene glycol 400 and water for injection (part). The pH is adjusted to 5.0 by addition of acetic acid. The volume is adjusted to 1.0 ml by addition of the residual amount of water. The solution is filtered, filled into vials using an appropriate overage and sterilized. Claims k Compounds of formula (I) wherein R1 is hydrogen, or lower alkyl; R is hydrogen, lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, lower alkoxycarbonylamino, -(CH2)m-R2a or -NHC(0)-R2a; or R and R together with the nitrogen atom to which they are attached form a 5- or 6-membered, saturated heterocyclic ring optionally containing one or two further heteroatom(s) independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; R2a is cycloalkyl, optionally mono-, di-, tri- or tetra-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; cycloalkenyl, optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino, lower alkylamino; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower allcylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; IT is lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, di-phenyl-lower alkyl, or -(CH2VR3a; R3a is cycloalkyl, which may'optiorially be fused to a phenyl ring; or cycloalkyl which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; cycloalkenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; R4 is lower alkyl, lower alkoxycarbonyl; cycloalkyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted,. independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino, lower alkylamino; phenoxy-lower alkyl, wherein the phenyl moiety may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by, hydroxy, lower alkyl, loWer.alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or two adjacent substituents of the said phenyl residue together are -O-(CH2)p-0- or -(CH2)2-0-; R5 and R6 are each independently selected from hydrogen, lower alkyl, halogen or fluorinated methyl; R is hydrogen, lower alkyl or halogen; m is 0, 1,2 or 3; nis0> 1,2,3 or"4; p is 1, 2 or 3; and pharmaceutical^ acceptable salts thereof. 2. Compounds according to claim 1, wherein R1 is hydrogen. 3. Compounds according to any of claims 1 or 2, wherein R2 is lower alkyl or a residue -(CH2)m-R2a or -NHq(0)-R2a. 4. Compounds according to claim 2, wherein R2a is a cycloalkyl residues with three to six carbon atoms, which may optionally be mono- or tetra-substituted, independently, by lower alkyl and/or hydroxy. 5. Compounds according to claim 2, wherein R2a is cyclohexenyi. 6. Compounds according to claim 2, wherein R2a is an unsubstituted 5-membered monovalent saturated heterocyclic ring containing one or two heteroatoms independently selected from nitrogen and oxygen. 7. Compounds according to claim 6, wherein R2a is piperidinyl, morpholino or tetrahydrofuranyl. 8. Compounds according to claim 2, wherein R2a is a 5- or 6-membered monovalent heterocyclic ring containing one or two heteroatoms independently selected from nitrogen and sulfur, said heteroaromatic ring bein optionally substituted by lower alkyl. 9. Compounds according to claim 8, wherein R2a is pyridinyl, pyrimidinyl, thiazolyl or isoxazolyl, optionally substituted by lower alkyl. 10. Compounds according to any of claims 1 to 9, wherein R a is a phenyl residue which is optionally mono- or di-substituted, independently, by lower alkoxy, halogen, halogenated lower alkyl, halogenated lower alkoxy or nitro. 11. Compounds according to any of claims 1 to 10, wherein m is 0 or 1. f 12. Compounds according to claim 1, wherein R1 and R2 together with the nitrogen atom to which they are attached form a 5- or 6-membered, saturated heterocyclic ring optionally containing an oxygen atom in the ring. 13. Compounds according to claim 12, wherein R andR together with the nitrogen atom to which they are attached are unsubstituted pyrrolidinyl, piperidinyl or morpholino. •a 14. Compounds according to any of claims 1 to 13, wherein R is a residue -(CH2)n-R3a- 15. Compounds according to claim 14, wherein R3a is cycloalkyl fused to a phenyl ring. 16. Compounds according to claim 14, wherein R a is an unsubstituted cycloalkyl residue with five or six carbon atoms. 17. Compounds according to claim 14, wherein R a is a 5- or 6-memberd heterocyclic ring containing one or two heteroatoms independently selected from nitrogen and oxygen, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by lower alkyj. 18. Compounds according to claim 14, wherein R a is a 5- or 6-membered heteroaromatic ring containing one heteroatom selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-substituted by lower alkyl. 1§. Compounds according to claim 14, wherein R3a is phenyl optionally mono- or di-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, halogenated lower alkyl, halogenated lower alkoxy or nitro. ,20. Compounds according to any of claims 14 to 19, wherein n is 1 or 2. 21. • Compounds according to any of claims 1 to 20, wherein R4 is unsubstituted cyclohexyl. 22. Compounds according to any of claims 1 to 20, wherein R4 is a 5- or 6- membered heteroaromatic ring containing one or two heteroatoms independently selected ' from nitrogen and sulfur, said heteroaromatic ring being optionally mono-substituted by lower alkyl. 23. Compounds according to any of claims 1 to 20, wherein R4 is phenyl mono- or di-substituted, independently, by'hydroxy, lower alkyl, lower alkoxy, halogen, halogenated lower alkyl, halogenated lower alkoxy or nitro. 24. Compounds according to any of claims 1 to 20, wherein two adjacent substituents of a phenyl residue R4 together are -0-(CH2) -O- or -(CH2)2-0-. 25. Compounds according to any of claims 1 to 24, selected from the group consisting of: l-Cyclohexylmethyl-5- [2-(4-methoxy-phenyl)-thiazol-4-yl] -2-methyl- lH-pyrrole-3-c arboxylic acid butylamide,, l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3 -carboxylic acid butylamide, rac-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid sec-butylamide, rac-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-IH-pyrr ole-3-carboxylic acid sec-butylamide, l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid isobutyl-amide, l-Furan-2-ylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid isobutyl-amide, l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2"methyl-lH-pyrrole,-3 -carboxylic acid isobutyl-amide, l-CycIohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid allylamide, '■ i.l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid cyclohexylmethyl-amide, l-Cyclohex)rlmethyl-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxy lie acid cyclohexylmethyl-amide, and pharmaceutical acceptable salts thereof. 26. A process for the manufacture of compounds of formula (I) as defined in any of claims 1 to 25, which process comprises reaction of an enamine of formula A: wherein R1 , R 2 R 3, R5and m are as defined claim 1; with an alfa-bromoketone of formula B: AC "J wherein R , R and R are as defined claim 1. 27. Compounds according to any of claims 1 to 25 when manufactured by a process according to claim 26. 28. Pharmaceutical compositions comprising a compound according to any of claims 1 to 25 and a pharmaceutically acceptable carrier and/or adjuvant. 29. Compounds according to any of claims 1 to 25 for use as therapeutic active substances. 30. Compounds according to any of claims 1 to 25 for use as therapeutic active substances for the treatment and/or prophylaxis of diseases which are associated with modulation of the CB1 receptor. 31. A method for the treatment and/or prophylaxis of diseases which are associated with the modulation of the CBl receptors which method comprises administering a compound according to any of claims 1 to 25 to a human being or animal. 32. The use of compounds according to any of claims 1 to 25 for the treatment and/or prophylaxis of diseases which are associated with the modulation of CBl receptors. 33. The use of compounds according to any of claims 1 to 25 for the preparation of medicaments for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors. or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower allcylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; IT is lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, di-phenyl-lower alkyl, or -(CH2VR3a; R3a is cycloalkyl, which may'optiorially be fused to a phenyl ring; or cycloalkyl which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; cycloalkenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; R4 is lower alkyl, lower alkoxycarbonyl; cycloalkyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted,. independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino, lower alkylamino; phenoxy-lower alkyl, wherein the phenyl moiety may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by, hydroxy, lower alkyl, loWer.alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or two adjacent substituents of the said phenyl residue together are -O-(CH2)p-0- or -(CH2)2-0-; Compounds according to any of claims 1 to 9, wherein R a is a phenyl residue which is optionally mono- or di-substituted, independently, by lower alkoxy, halogen, halogenated lower alkyl, halogenated lower alkoxy or nitro. 11. Compounds according to any of claims 1 to 10, wherein m is 0 or 1. f 12. Compounds according to claim 1, wherein R1 and R2 together with the nitrogen atom to which they are attached form a 5- or 6-membered, saturated heterocyclic ring optionally containing an oxygen atom in the ring. 13. Compounds according to claim 12, wherein R andR together with the nitrogen atom to which they are attached are unsubstituted pyrrolidinyl, piperidinyl or morpholino. •a 14. Compounds according to any of claims 1 to 13, wherein R is a residue -(CH2)n-R3a- 15. Compounds according to claim 14, wherein R3a is cycloalkyl fused to a phenyl ring. 16. Compounds according to claim 14, wherein R a is an unsubstituted cycloalkyl residue with five or six carbon atoms. 17. Compounds according to claim 14, wherein R a is a 5- or 6-memberd heterocyclic ring containing one or two heteroatoms independently selected from nitrogen and oxygen, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by lower alkyj. 18. Compounds according to claim 14, wherein R a is a 5- or 6-membered heteroaromatic ring containing one heteroatom selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-substituted by lower alkyl. 1§. Compounds according to claim 14, wherein R3a is phenyl optionally mono- or di-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, halogenated lower alkyl, halogenated lower alkoxy or nitro. ,20. Compounds according to any of claims 14 to 19, wherein n is 1 or 2. 21. • Compounds according to any of claims 1 to 20, wherein R4 is unsubstituted cyclohexyl. 22. Compounds according to any of claims 1 to 20, wherein R4 is a 5- or 6- membered heteroaromatic ring containing one or two heteroatoms independently selected ' from nitrogen and sulfur, said heteroaromatic ring being optionally mono-substituted by lower alkyl. 23. Compounds according to any of claims 1 to 20, wherein R4 is phenyl mono- or di-substituted, independently, by'hydroxy, lower alkyl, lower alkoxy, halogen, halogenated lower alkyl, halogenated lower alkoxy or nitro. 24. Compounds according to any of claims 1 to 20, wherein two adjacent substituents of a phenyl residue R4 together are -0-(CH2) -O- or -(CH2)2-0-. 25. Compounds according to any of claims 1 to 24, selected from the group consisting of: l-Cyclohexylmethyl-5- [2-(4-methoxy-phenyl)-thiazol-4-yl] -2-methyl- lH-pyrrole-3-c arboxylic acid butylamide,, l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3 -carboxylic acid butylamide, rac-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid sec-butylamide, rac-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-IH-pyrr ole-3-carboxylic acid sec-butylamide, l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid isobutyl-amide, l-Furan-2-ylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid isobutyl-amide, l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2"methyl-lH-pyrrole,-3 -carboxylic acid isobutyl-amide, l-CycIohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid allylamide, '■ i.l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid cyclohexylmethyl-amide, l-Cyclohex)rlmethyl-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxy lie acid cyclohexylmethyl-amide, l-(4-Metho;^-benzyl)-5-[2-(4-m^ pyrrole-3 -carboxylic acid cyclohexylmethyl-amide, '5'-[2-(4-Methoxy-phenoxymethyl)-thiazol^^ lH-py rrole-3-carboxylic acid cydohexylmethyl-amide, 4-[l-[2-(3)4-Dimethoxy-ph:enyl)-ethyl]-4-(3-methoxy-propylcarb 1H-pyrrol-2-yl]-thiazole-2-carboxylic acid ethyl ester, l-Cyclohexylmethyl-5-[2-(4-me^^ 3-carboxylic acid piperidin-1-ylamide, N'-{l-Cyclohexylmethyl«5-[2-(4-methoxy-phenyI)-thiazol-4-yI]-2-me^ pyrrole-3-carbonyi}-hydrazinecarboxylic acid ethyl ester, r«c-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid sec-butylamide, {l-Cyclohexylmethyl-5-'[2-(4-^ 3-yl}-piperidin-l-yl-methanone, l-CyclohexyImethyl-5-[2-(4-methoxy-phenyl)-thiazoI-4-yl]-2-methyl-lH-pyrroIe-3-carboxylic acid phenylamide, l-Cyclohexylmethyl-5-[2-(4-methoxy~pheny^ 3-carboxylic acid pyrimidin-2-ylamide, mc-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-niethyl-lH-pyrrole-3-carboxylicacid(5-hydroxy-2,2>6-trimethyl-cyclohexylmethyl)-amideJ 5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-^^ lH-pyrrole-3-carboxylic acid butylamide, l-Benzyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole--3-carboxylic acid butylamide, {l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyMH-pyrrol-3-yl}-pyrrolidin-l-yl-methanone, l-Cyclohexylmethyl-5-[2-(3,4-dimethoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyirole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-5-[2-(3-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole' 3-carboxylic acid butylamide, 5-(2-Benzo[l>3]dioxol-5-yl-thiaz^ 3-carboxylic acid butylamide, l-Cydohexylmethyl-5-[2-(4-fluo^^ carboxylic acid butylamide, l-Cydohexylmethyl-5-[2-(2-fluoro^ carboxylic acid butylamide, l-Cyclohexylmethyl-2-methyl-5-[2-(4-trifluoromethoxy-phenyl)-thiazol-4-yl]-lH pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-5-[2-(3,5-dimethoxy-phenyl)-thiazol-4"yl]-2-methyl-lH*-pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-2-methyl-5-(2-m-tolyl-thiazol--4-yl)-lH-pyrrole-3-carboxylic acid butylamide, l-Cydohexylmethyl-2-methyl-5-(2'-met^ carboxylic acid butylamide, l-Cyclohexylmethyl-5-[2-(4-ethyl-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide, 5-[2-(4-Chloro-phenyl)-thiazol-4-yl]-l-cyclohexylmethyl-2-methyl-lH-pyrrole-3-carboxylic acid butylamide, 5-[2-(4-tert-Butyl-phenyl)-thiazol-4-yl]-l-cyclohexylmethyl-2-methyl-lH-pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-542-(2,3-dihydro-benzofo lH-pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-2-methyl-5-(2"p-tolyl-thiazol-4-yl)-lH-pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-5-[2-(6-methoxy-pyridin-3-yl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-5-[2-(2,4-dichloro-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-2-methyl-5-[2-(4-nitro-phenyl)-thiazol-4-yl]-lH-pyrrole-3-carboxylic acid butylamide, 1-Cyclohexylmethy^ 3-carboxylic acid pentylamide, l-Cyclohexylmethyl-5-[2-(4-methoxy-pheny^ 3-carboxylic acid propylamide, l-Cydohexylmethyl-542-(4-methoxy-phenyl)^ 3-carboxylic acid cyclohexylamide, l-Cyclohexylmethyl-5-[2-(4~methoxy-phenylH 3-carboxylic acid cyclopentylamide, l-Cyclohexylmethyl-5-[2-(4-methoxy^ 3-carboxylic acid cyclopropylamide, l~Cyclohexylmethyl-5-[2-(4-methox^^ 3-carboxylic acid cyclobutylamide, {trans) rac-l-Cyclohexylmethyl-5-[2-(^ lH-pyrrole-3-carboxylic acid (2-hydroxy-cyclopentyl)-amide, l-(4-Chloro-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide, l-(3,4-Dichloro-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]"2-methyl-lH-pyrrole-3-carboxylic acid butylamide, l~(3,4-Dimethyl4)enzyl)-542-(4-metho^ pyrrole-3-carboxylic acid butylamide, l-(3,4-Dimethoxy-benzyl)-5-[2-(4-me&^ pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-5-[2-(4-hydroxy-phenyl)-thiazol-4-yl]-2-methyl-lH--pyrrole-3-carboxylic acid butylamide, l-(4-Isopropyl-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide, 5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l--pyridin-2--ylmethyl-lH-pyrrole-3-carboxylic acid butylamide, l-Cyclohexylmethyl-5-(2-cyclohexyl-thiazol-4-yl)-2--methyl-lH-pyrrole-3-carboxylic acid butylamide, and pharmaceutical acceptable salts thereof. 26. A process for the manufacture of compounds of formula (I) as defined in any of claims 1 to 25, which process comprises reaction of an enamine of formula A: wherein R , R > R , R and m are as defined claim 1; with an alfa-bromoketone of formula B: AC "J wherein R , R and R are as defined claim 1. 27. Compounds according to any of claims 1 to 25 when manufactured by a process according to claim 26. 28. Pharmaceutical compositions comprising a compound according to any of claims 1 to 25 and a pharmaceutical^ acceptable carrier and/or adjuvant. 29. Compounds according to any of claims 1 to 25 for use as therapeutic active substances. 30. Compounds according to any of claims 1 to 25 for use as therapeutic active substances for the treatment and/or prophylaxis of diseases which are associated with modulation of the CB1 receptor. 31. A method for the treatment and/or prophylaxis of diseases which are associated with the modulation of the CBl receptors which method comprises administering a compound according to any of claims 1 to 25 to a human being or animal. 32. The use of compounds according to any of claims 1 to 25 for the treatment and/or prophylaxis of diseases which aTe associated with the modulation of CBl receptors. 33. The use of compounds according to any of claims 1 to 25 for the preparation of medicaments for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.

Full Text

PYRROLYL-THIAZOLES AND THEIR USE AS CB 1 RECEPTOR INVERSE AGONISTS
The present invention is concerned with novel pyrrolyl-thiazole derivatives, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in treating obesity and other disorders.
In particular, the present invention relates to compounds of formula (I):
wherein
R1 is hydrogen, or lower alkyl;
R2 is hydrogen, lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, lower alkoxycarbonylamino, -(CH2)m-R2a or -NHC(0)-R2a;
or R and R together with the nitrogen atom to which they are attached form a 5- or 6-membered, saturated heterocyclic ring optionally containing one or two further heteroatom(s) independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl>.lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy;
R"a is cycloalkyl, optionally mono-, di-, tri- or tetra-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy;

cycloalkenyl, optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower allcyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower allcyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino, lower alkylamino; or phenyl, which may optionally be mono-,di-or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro;
R is lower alkyl, lower aikenyl, lower alkoxy-lower alkyl, di-phenyl-lower alkyl, or -(CH2)n-R3a;
R3a is cycloalkyl fused to a phenyl ring; or cycloalkyl which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower0 alkyl or fluorinated lower alkoxy; cycloalkenyl, which may optionally be mono-, di-or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono*, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro;
R4 is lower alkyl, lower alkoxycarbonyl; cycloalkyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen

and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino, lower alkylamino; 'phenqxy-lower alkyl, wherein the phenyl moiety may optionally be mono-, di- or tri-substituted, independendy, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by, hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or two adjacent substituents of the said phenyl residue together are -O-(CH2)p-0- or -(CH2)rO-;
R5 and R6 are each independently selected from hydrogen, lower alkyl, halogen or fluorinated methyl;
R7 is hydrogen, lower alkyl or halogen;
m is 0,1,2 or 3;
nisO, 1,2, 3 or 4;
p is 1, 2 or 3;
and pharmaceuticaly acceptable salts thereof.
Two different subtypes of cannabinoid receptors (CBi amd CB2) have been isolated and both belong to G protein coupled receptor superfamily. An alternative spliced form of CBi, CBiA has also been described, but it did not exhibit different properties in terms of ligand binding and receptor activation than CBi (D.Shire, C. Carrillon, M. Kaghad,.B. Calandra, M. Rinaldi-Carmona, G. Le Fur, D. Caput, P. Ferrara, J. Biol. Chem. 270 (8) (1995) 3726-31). The CBi receptor is mainly located in the brain, whereas the CB2 receptor is predominately distributed in the periphery and primarily localized in spleen and cells of > the immune system (S. Munro, K.L. Thomas, M. Abu-Shaar, Nature 365 (1993) 61-61). Therefore in order to avoid side effects a CBi-selective compound is desirable.
A9-tetrahydrocannabinol (A9-THC) is the principal psychoactive compound in the Indian hemp (Y. Gaoni, R. Mechoulam, J. Am. Chem. Soc, 86 (1964) 1646), canabis savita (marijuanan), which is used in medicine since ages (R. Mechoulam (Ed.) in "Cannabinoids

as therapeutic Agents", 1986, pp. 1-20, CRC Press). A9-THC is a non-selective CBi/2
receptor agonist and is available in the USA as dronabinol (marinol®) for the alleviation of cancer chemotherapy-induced emesis (CIE) and the reversal of body weight loss experienced by AIDS patients through appetite stimulation. In the UK Nabolinone (LY-
109514, Cesamet®), a synthetic analogue of A9-THC, is used for CIE (R. G.' Pertwee, Pharmaceut. Sci. 3 (11) (1997) 539-545, E. M. Williamson, F. J. Evans, Drugs 60 (6) (2000) 1303-1314).
Anandamide (arachidonylethanolamide) was identified as the endogenous ligand (agonist) for the CBj receptor (R.G. Pertwee, Curr. Med. Chem., 6 (8) (1999) 635-664;W.A. Devane, L. Hanus, A. Breuer, R.G. Pertwee, L.A. Stevenson, G. Griffin, D. Gibson, A. Mandelbaum, A. Etinger, R. Mechoulam, Science 258 (1992) 1946-9). Anandamide and 2-arachidonoylglycerol (2-AG) modulate at the presynaptic nerve teminal negatively adenylate cyclase and voltage-sensitive Ca2+ channels and activates the inwardly rectifying K+ channel (V. Di Marzo, D. Melck, T. Bisogno, L. De Petrocellis, Trends in Neuroscience 21 (12) (1998) 521-8), thereby affecting neurotransmitter release and/or action, which decreases the release of neurotransmitter (A. C Porter, C.C. Efilder, Pharmacol. Ther., 90 (1) (2001) 45-60).
Anandamide as A9-THC also increases feeding through CBi receptor-mediated mechanism. CB1 receptor selective antagonists block the increase in feeding associated with administration of anandamide (C.M. Williams, T.C, Kirkham, Psychopharmacology 143 (3) (1999) 315-317; C. C. Felder, E. M. Briley, J. Axelrod, J. T. Simpson, K. Mackie, W. A. Devane, Proc. Natl. Acad. Sci. U. S. A. 90 (16) (1993) 7656-60) and caused appetite suppression and weight loss (G. Colombo, R. Agabio, G. Diaz, C. Lobina, R. Reali, G. L. Gessa, Life Sci. 63 (8) (1998) L113-PL117).
Leptin is the primary signal through which the hypothalamus senses nutritional state and modulates food intake and energy balance. Following temporary food restriction, CBI receptor knockout mice eat less than their wild-type littermates, and the CBI antagonist SR141716A reduces food intake in wild-type but not knockout mice. Furthermore, defective leptin signaling is associated with elevated hypothalamic, but not cerebellar, levels of endocannabinoids in obese db/db and ob/ob mice and Zucker rats. Acute leptin treatment of normal rats and ob/ob mice reduces anandamide and 2-arachidonoyl glycerol in the hypothalamus. These findings indicate that endocannabinoids in the hypothalamus

may tonically activate CBl receptors to maintain food intake and form part of the neural circuitry regulated by leptin (V. Di Marzo, S. K. Goparaju, L. Wang, J. Liu, S. Bitkai, Z. Jarai, F. Fezza, G. I. Miura, R. D. Palmiter, T. Sugiura, G. Kunos, Nature 410 (6830) 822-825).
SR-141716A, a CBl selective antagonist / inverse agonist is undergoing currently phase III clinical trials for the treatment of obesity. In a double blind placebo-controlled study, at the doses of 5,10 and 20 mg daily, SR 141716 significantly reduced body weight when compared to placebo (F. Barth, M, Rinaldi-Carmona, M. Arnone, H. Heshmati, G. Le Fur, "Cannabinoid antagonists: From research tools to potential new drugs" Abstracts of Papers, 222nd ACS National Meeting, Chicago, IL, United States, August 26-30,2001).
Other compounds which have been proposed as CBl receptor antagonists respectively inverse agonists are aminoalkylindols (AAI; M. Pacheco, S. R. Childers, R. Arnold, F. Casiano, S. J. Ward, J. Pharmacol Exp. Ther. 257 (1) (1991) 170-183), like 6-bromo- (WIN54661; F. M. Casiano, R. Arnold, D. Haycock, J. Kuster, S. J. Ward, NIDA Res. Monogr. 105 (1991) 295-6) or 6-iodopravadoline (AM630, K. Hosohata, R. M. Quock, R.M; Hosohata, T. H. Burkey, A. Makriyannis, P. Consroe, W. R. Roeske, H. I. Yamamura, Life Sci. 61 (1997) 115 -118; R. Pertwee, G. Griffin, S. Fernando, X. Li, A. Hill, A. Makriyannis, Life Sci. 56 (23-24) (1995) 1949-55). Arylbenzo[b]thiophene and benzo[b]furan (LY320135, C. C. Felder, K. E. Joyce, E. M. Briley, M. Glass, K. P. Mackie, K. J. Fahey, G. J. Cullinan, D. C. Hunden, D. W. Johnson, M. O. Chaney, G. A. Koppel, M. Brownstein, J. Pharmacol. Exp. Ther. 284 (1) (1998) 291-7) disclosed in WO9602248, US5596106,3-alkyl-(5,5-diphenyl)imidazolidinediones (M. Kanyonyo, S. J. Govaerts, E. Hermans, J. H. Poupaert, D. M. Lambert, Bioorg. Med. Chem. Lett 9 (15) (1999) 2233 -2236.) as well as 3-alkyl-5-arylimidazolidinediones (F. Ooms, J. Wouters, O. Oscaro. T. Happaerts, G. Bouchard, P.-A. Carrupt, B. Testa, D. M. Lambert, J, Med. Chem. 45'(9) (2002) 1748-1756) are known to antagonize the CBi receptor respectively act as an inverse agonist on the hCBi receptor. WO0015609 (FR2783246-A1), WO0164634 (FR2805817-Al), WO0228346, WO0164632 (FR2805818-A1), WO0164633 (FR2805810-A1) disclosed substituted l-bis(aryl)methyl-azetidines derivatives as antagonists of CBj. In WO0170700 4,5-dihydro-lH-pyrazole derivatives are described as CBi antagonists. In several patents bridged and non-bridgedl,5-diphenyl-3-pyrazolecarboxamide derivatives are disclosed as CBi antagonists/inverse agonists (WO0132663, WO0046209, WO9719063, EP658546, EP656354, US5624941, EP576357, US3940418).

It is an object of this invention to provide selective, directly acting CB1 receptor antagonists respectively inverse agonists. Such antagonists / inverse antagonists are useful in medical therapy, particularly in the treatment and/or prevention of diseases which are associated with the modulation of CB1 receptors.
Unless otherwise indicated, the following definitions are set forth to illustrate and define the meaning and scope of the various terms used to describe the invention herein.
In this specification the term "lower" is used to mean a group consisting of one to eight, preferably of one to four carbon atom(s).
The term "halogen" refers to fluorine, chlorine, bromine and iodine, preferably to chlorine and fluorine.
The term "alkyl", alone or in combination with other groups, refers to a branched or straight-chain monovalent saturated aliphatic hydrocarbon radical of one to twenty carbon atoms, preferably one to sixteen carbon atoms, more preferably one to ten carbon atoms.
The term "lower alkyl", alone or in combination with other groups, refers to a branched or straight-chain monovalent alkyl radical of one to eight carbon atoms, preferably one to four carbon atoms. This term is further exemplified by radicals such as methyl, ethyl, n-propyl, isopropyl, n-butyl, s-butyl, isobutyl, t-butyl, n-pentyl, 3-methylbutyl, n-hexyl, 2-ethylbutyl and the like.
The term "alkoxy" refers to the group R'-O-, wherein R' is alkyl. The term "lower alkoxy" refers to the group R'-O-, wherein R5 is lower alkyl. Examples of lower alkoxy groups are e.g. methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy and hexyloxy, with methoxy being especially preferred.
The term "lower alkenyl" refers to a lower alkyl group containing one or more double bond(s) in the alkylene chain. This term is further exemplified by radicals such as vinyl, 1-propenyl, allyl, 1-butenyl, 2-butenyl and 3-butenyl, with allyl being preferred.
The term "lower alkylarjiino" refers to the group R'-NH-, wherein R' is lower alkyl.

The term "lower alkoxycarbonyl" refers to the group R'-O-C(O)-, wherein R' is lower alkyl.
The term "lower alkoxycarbonylamino" refers to the group R>-0-C(0)NH-> wherein IV is lower alkyl.
The term "halogenated lower alkyl" refers to a lower alkyl group wherein at least one of the hydrogens of the lower alkyl group is replaced by a halogen atom, preferably fluoro or chloro. Among the preferred halogenated lower alkyl groups are trifluoromethyl, difluoromethyl, fluoromethyl and chloromethyl, with trifluoromethyl being especially preferred. The term "fluorinated lower alkyl" refers to a lower alkyl group wherein at least one of the hydrogens of the lower alkyl group is replaced by fluoro. Among the preferred fluorinated lower alkyl groups are trifluoromethyl, difluoromethyl and fluoromethyl, with trifluoromethyl being especially preferred.
The term "halogenated lower alkoxy" refers to a lower alkoxy group wherein at least one of the hydrogens of the lower alkoxy group is replaced by halogen, preferably by fluorine or chlorine. Among the preferred halogenated lower alkoxy groups are fluorinated lower alkoxy groups such as trifluoromethoxy, difluoromethoxy and fluoromethoxy, with trifluoromethoxy being especially preferred. The term "fluorinated lower alkoxy" refers to a lower alkoxy group wherein at least one of the hydrogens of the lower alkoxy group is replaced by fluoro. Among the preferred fluorinated lower alkoxy groups are trifluoromethoxy, difluoromethoxy and fluoromethoxy, with trifluoromethoxy being especially preferred.
The term "di-phenyl-lower alkyl" refers to a lower alkyl group wherein two of the hydrogens of the lower alkyl group is replaced by phenyl. The phenyl moiety may optionally be mono-, di-, or tri-substituted, independently, by lower alkyl, lower alkoxy or halogen.
The term "phenoxy-lower alkyl" refers to a lower alkyl group wherein one of the hydrogens of the lower alkyl group is replaced by phenoxy. The phenyl moiety of the phenoxy-lower alkyl residues may optionally be mono-, di-, or tri-substituted, independently, by lower alkyl, lower alkoxy or halogen.

The term "cycloalkyl" refers to a monovalent carbocyclic radical of three to six, preferably three to five carbon atoms. This term is further exemplified by radicals such as cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl.
The term "cycloalkenyl" refers to a monovalent carbocyclic radical of three to six, preferably three to five carbon atoms, which carbocyclic ring contains at least on double bond. This term is further exemplified by radicals such as cyclobutenyl, cyclopentenyl and cyclohexenyl, with cyclohexenyl being preferred.
The term "pharmaceutical^ acceptable salts" embraces salts of the compounds of formula (I) with inorganic or organic acids such as hydrochloric acid, hydrobromic acid, nitric acid, sulphuric acid, phosphoric acid, citric acid, formic acid, maleic acid, acetic acid, fumaric acid, succinic acid, tartaric acid, methanesulphonic acid, salicylic acid, p-toluenesulphonic acid and the like, which are non toxic to living organisms. Preferred salts with acids are formates, maleates, citrates, hydrochlorides, hydrobromides and methanesulfonic acid salts, with hydrochlorides being especially preferred.
In one embodiment, the present invention relates to a compound of formula (I) as defined above, wherein R1 is hydrogen or lower alkyl.
Preferable lower alkyl residues R1 are methyl and ethyl, with methyl being especially preferred. Most preferably, R1 is hydrogen.
In another embodiment, the present invention relates to a compound of formula (I) as defined above, wherein R2 is hydrogen, lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, lower alkoxycarbonylamino, -(CH2)m-R2a or -NHC(0)-R2Preferable lower alkyl residues R are branched or straight chain alkyl residues with one to eight, preferably three to five carbon atoms, such as n-propyl, n-butyl, s-butyl, isobutyl, n-pentyl and 2-ethylhexyl. Most preferred lower alkyl residues R2 are n-propyl, n-butyl, s-butyl, isobutyl and n-pentyl. Preferable lower alkenyl residues R are 1-butenyl and allyl, with allyl being especially preferred. Preferable lower alkoxy-lower alkyl residues R2,are methoxymethyl, methoxyethyl, methoxypropyl, ethoxymethyl, ethoxyethyl and ethoxypropyl, with methoxyethyl and methoxypropyl being especially preferred. Preferable lower alkoxycarbonylamino groups R2 are methoxycarbonylamino, ethoxycarbonylamino, propoxycarbonylamino and butoxycarbonylamino, with ethoxycarbonylamino being

specially preferred. Preferable residues R" are lower alkyi as defined above, -(CH2)m-R2a ■r -NHC(0)~R2a, wherein R2a is as defined below and m is 0 or 1, preferably 0. Most referable residues R are lower alkyi as defined above or -(CH2)m-R a> wherein R is as lefined below and m is 0 or 1, preferably 0.
In one embodiment, R2a is cycloalkyl, optionally mono-, di-, tri- or tetra-substituted, ndependently, by hydroxy, lower alkyi, lower alkoxy, fluorinated lower alkyi ox luorinated lower alkoxy; cycloalkenyl, optionally mono-, di- or tri-substituted, ■ndependently, by hydroxy, lower alkyi, lower alkoxy, fluorinated lower alkyi or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring . containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyi, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyi or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyi, lower alkoxy, halogen, amino, lower alkylamino; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower "alkyi, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyi, halogenated lower alkoxy or nitro.
Preferable cycloalkyl residues R2a are cycloalkyl residues with three to six carbon atoms, such as cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, which may optionally be mono-, di-, tri- or tetra-substituted, preferably mono- or tetra-substituted, independently, by hydroxy, lower alkyi, lower alkoxy, fluorinated lower alkyi or fluorinated lower alkoxy, preferably by lower alkyi, such as methyl, and/or hydroxy. Most preferable cycloalkyl residues R a are cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and 2-hydroxycyclopentyl. Preferable cycloalkenyl residues R2a are cyclobutenyl, cyclopentenyl and cyclohexenyl, with cyclohexenyl, preferably cyclohex-l-enyl, being especially preferred. Preferable heterocyclic rings R2a are 5- or 6-memberd, with 5-membered being especially preferred, and contain one to three, preferably one or two, heteroatoms independently selected from nitrogen, oxygen and sulfur, preferably selected form nitrogen and oxygen, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyi, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyi or fluorinated lower alkoxy. Preferably, heterocyclic rings R a are unsubstituted. Most preferred heterocyclic rings R2a are piperidinyl, morpholino and

tetrahydrofuranyl, with piperidinyl and morpholino being especially preferred. Preferable heteroaromatic rings R~a are 5- or 6-membered and contain one to three, preferably one or two, heteroatoms independently selected from nitrogen, oxygen and sulfur, preferably selected form nitrogen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino. Examples of heteroaromatic rings R a are pyridinyl, pyrimidinyl, thiazolyl and isoxazolyl, optionally substituted as defined above. Preferably, heteroaromatic rings R2a are unsubstituted or mono-substituted by lower alkyl, preferably methyl. Most preferable heteroaromatic rings R a are pyridinyl, pyrimidinyl, 4-methylthiazolyl or 5-methylisoxazolyl. Preferable phenyl residues R a are optionally mono-, di- or tri-substituted, preferably mono- or di-substituted, independently, by lower alkoxy, such as methoxy, halogen, such as chloro, halogenated lower alkyl, such as trifluoromethyl, halogenated lower alkoxy, such as trifluoromethoxy, or nitro. Most preferable phenyl residues R2a are unsubstituted phenyl, 4-trifluoromethyl-phenyl, 4-chloro-phenyl, 3,4-dichloro-phenyl, 3,4-dimethoxy-phenyl, 2-nitro-phenyl and4-trifluoromethoxy-phenyl.
Preferably, m is 0,1 or 2, more preferably m is 0 or 1, most preferably m is 0. "
In another embodiment, R and R together with the nitrogen atom to which they are attached form a 5- or 6-membered, saturated heterocyclic ring optionally containing one or two, preferably one, further heteroatom(s) independently selected from nitrogen, oxygen and sulfur, preferably oxygen, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy. Preferably, heterocyclic rings formed by R and R together with the nitrogen atom to which they are attached are unsubstituted, with unsubstituted pyrrolidinyl, piperidinyl and morpholino being especially preferred.
In another embodiment, the present invention relates to a compound of formula (I) as defined above, wherein R is lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, di-phenyl-lower alkyl, or -(CH2)n-R3a.
Preferable lower alkyl residues R are branched or straight chain alkyl residues with one to sk, preferably four carbon atoms, such as ethyl, n-propyl, isopropyl, n-butyl, s-butyl, isobutyl, n-pentyl and n-hexyl. Most preferred lower alkyl residues R3 are n-butyl and s-butyl. Preferable lower alkenyl residues R are 1-butenyl and allyl, with allyl being

especially preferred. Preferable lower alkoxy-lower alkyl residues R3 are methoxymethyl, methoxyethyl, methoxypropyl, ethoxymethyl, ethoxyethyl and ethoxypropyl, with methoxyethyl and methoxypropyl being especially preferred. Preferable di-phenyl-lower alkyl is di-phenyl-methyl. Most preferably, R3 is a residue -(CH2)n-R3a, wherein R3a is as i defined below and n is 1 or 2, preferably 1.
In one embodiment, R3a is cycloalkyl fused to a phenyl ring; or cycloalkyl which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; cycloalkenyl, which may . optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-y di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent h'eteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower ' alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro.
Preferable cycloalkyl residues R3a are cycloalkyl residues with five or six carbon atoms, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy, or which may optionally be fused to a phenyl ring. Preferably, cycloalkyl residues R3a are unsubstituted, such as unsubstituted cyclopentyl or unsubstituted cyclohexyl, with unsubstituted cyclohexyl being preferred, or fused to a phenyl residue, such as indanyl. Preferable cycloalkenyl residues R2a are cyclobutenyl, cyclopentenyl and cyclohexenyl, with cyclohexenyl, preferably cyclohex-1-enyl, being especially preferred. Preferable heterocyclic rings R3a are 5- or 6-memberd and contain one to three, preferably one or two, heteroatoms independently selected from nitrogen, oxygen and sulfur, preferably selected form nitrogen and oxygen, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy. Examples of heterocyclic rings R3a are piperidinyl, morpholino and pyrrolidinyl, optionally substituted as defined

above. Preferably, heterocyclic rings R a are unsubstituted or substituted by lower alkyl, such as methyl or ethyl, with ethyl being especially preferred. Most preferred heterocyclic rings R3a are piperidinyl, morpholino and 1-ethyl-pyrrolidinyl. Preferable heteroaromatic rings R3a are 5- or 6-membered and contain one to three, preferably one, heteroatom(s) independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino. Examples of heteroaromatic rings R3a are furyl, thienyl and pyridinyl, optionally substituted as defined above. Preferably, heteroaromatic rings R a are unsubstituted or mono-substituted by lower alkyl, preferably methyl. Most preferable heteroaromatic rings R3a are furyl, thienyl, 3-methylthienyl and pyridinyl. Preferable phenyl residues R a are optionally mono-, di- or tri-substituted, preferably mono- or di-substituted, most preferably mono-substituted, independently, by hydroxy, lower alkyl, such as methyl or isopropyl, lower alkoxy, such as methoxy, halogen, such as chloro, halogenated lower alkyl, such as trifluoromethyl, halogenated lower alkoxy, such as trifluoromethoxy, or rtitro. Most preferable phenyl residues R3a are unsubstituted phenyl, 2-methyl-phenyl, 4-methyl-phenyl, 3,4-dimethyl-phenyl, 3,5-dimethyl-phenyl, 4-isopropyl-phenyl, 4-chloro-phenyl, 3,4-dichloro-phenyl, 3,5-dichloro-phenyl, 3-methoxy-phenyl, 4-methoxy-phenyl, 3,4-dimethoxy-phenyl, 3,5-dimethoxy-phenyl, 2,4-dimethoxy-phenyl, 3,4,5-trimethoxy-phenyl, 3-trifluoromethoxy-phenyl, 4-trifluoromethoxy-phenyl, 3-trifluormethyl-4-chlorophenyl and 4-nitro-phenyl, with 4-methoxy-phenyl being especially preferred. Most preferable residue R3a is a phenyl residue as defined above.
Preferably, n is 0,1, 2 or 3, more preferably n is 1 or 2, most preferably n is 1.
In another embodiment, the present invention relates to a compound of formula (I) as defined above, wherein R4 is lower alkyl; lower alkoxycarbonyl; cycloalkyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independendy selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino, lower alkylamino; phenoxy-lower alkyl, wherein the phenyl moiety may optidnally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by, hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl,

halogenated lower alkoxy or nitro; or two adjacent substituents of the said phenyl residue together are -0-(CH2)p-0- or -(CH2)2-0-.
Preferable lower alkyl residues R4 are branched or straight chain alkyl residues with one to six, preferably one to three carbon atoms, such as methyl, ethyl, n-propyl, isopropyl, n-butyl, s-butyl, t-butyl, isobutyl and n-pentyL Most preferred lbwer alkyl residue R4 is methyl. Preferable lower allcoxycarbonylamino groups R4 are methoxycarbonylamino, ethoxycarbonylamino, propoxycarbonylamino and butoxycarbonylamino, with ethoxycarbonylamino being especially preferred. Preferable cycloalkyl residues R4 are cycloalkyl residues with three to six carbon atoms, such as cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, which may optionally be mono-, di-> tri- or tetra-substituted, preferably mono- or tetra-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy, preferably by lower alkyl, such as methyl, and/or hydroxy. Most preferable cycloalkyl residue R4 is unsubstituted cyclohexyl. Preferable heteroaromatic rings R4 are 5- or 6-membered and contain one to three, preferably one or two, heteroatoms independently selected from nitrogen, oxygen and sulfur, preferably selected form nitrogen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently/by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino. Examples of heteroaromatic rings R are pyridinyl, pyrazinyl and thiazolyl, optionally substituted as defined above. Preferably, heteroaromatic rings R4 are unsubstituted or mono-substituted by lower alkyl, such as methyl and ethyl, or by lower alkoxy, such as methoxy. Most preferable heteroaromatic rings R are 2-methoxy-pyridinyl, 2-methyl-pyridinyl, pyrazinyl and 2-methyl-thiazolyl. Preferable phenoxy-lower alkyl residues R4 are phenoxy-methyl and phenoxy ethyl, wherein the phenyl moiety may optionally be mono-substituted by lower alkoxy, such as methoxy. Most preferable phenoxy-lower alkyl residue R4 is 3-methoxy-phenoxy-methyl. Preferable phenyl residues R4 are mono-, di- or tri-substituted, preferably mono- or di-substituted, most preferably mono-substituted, independently, by hydroxy, lower alkyl, such as methyl, ethyl or t-butyl, lower alkoxy, such as methoxy, halogen, such as chloro or fluoro, halogenated lower alkyl, such as trifluoromethyl, halogenated lower alkoxy, such as trifluoromethoxy or nitro. Alternatively, two adjacent substituents of the said phenyl residue together maybe -0-(CH2)p-0- or -(CfkVO-, wherein p is 1, 2 or 3, preferably 1 or 2, most preferably 1. Preferable substituents of phenyl residues R4 are nitro and lower alkoxy, or two adjacent substituents being -O-CH2-O-. Most preferable substituted phenyl residues R4 are 2-methyl-phenyl, 4-

methyl-phenyl, 4-ethyl-phenyl, 4-t-butyl-phenyl, 2-chloro-phenyl, 4-chloro-phenyl, 2,4-dichloro-phenyl, 2-fluoro-phenyl, 4-fluoro-phenyl, 2-methoxy-phenyl, 3-methoxy-phenyl, - 4-methoxy-phenyl, 3,4-dimethoxy-phenyl, 3,5-dimethoxy-phenyl, 4-hydroxy-phenyl, 4-trifluoromethyI-phenyl> 4-trifluoromethoxy-phenyl, 4-nitro-phenyl, benzo[ls3]dioxolyl ■and 2,3-dihydro-benzofuranyI, with 4-methoxyphenyl, 4-nitro-phenyI and benzo[l,3]dioxolyl being especially preferred. Preferable residues R4 are cycloalkyl residues and substituted phenyl residues as defined above.
In another embodiment, the present invention relates to a compound of formula (I) as defined above, wherein R5 and R are each independently selected from hydrogen, lower alkyl, halogen or fluorinated methyl.
Preferable lower alkyl residues R5 and R6 are methyl and ethyl, with methyl being especially preferred. Preferable halogen residues R5 and R6 are fluoro and chloro, with chloro being especially preferred. Preferable residue R5 is lower alkyl, such as methyl. Preferable residues R6 are hydrogen and lower alkyl, such as methyl.
In another embodiment, the present invention relates to a compound of formula (I) as defined above, wherein R is hydrogen, lower alkyl or halogen.
Preferable lower alkyl residues R7 are methyl and ethyl, with methyl being especially preferred. Preferable halogen residues R are fluoro and chloro, with chloro being especially preferred. Preferable residue R7 are hydrogen and lower alkyl, such as methyl.
Preferred compounds of general formula (I) are the compounds of Examples 1 to 377, preferably 1 to 375 (see section Examples below) and pharmaceutically acceptable salts thereof.
Especially preferred are the compounds selected from the group consisting of:
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-meAyl-lH-pyrrole-3-c arboxylic acid butylamide,
l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-
pyrrole-3 -carboxylic acid butylamide,
«■ ■
mc-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyI)-thiazoI-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid sec-butylamide,

rac-1 -Cyclohexylmethyl-5- [2-(4-methoxy-phenpxymethyl)-thiazol-4-yl] -2-methyl-lH-pyrr ole-3-carboxylic acid sec-butylamide,
. 1 -Cyclohexylmethyl-5- [2- (4-methoxy-phenyl)-thiazol-4-yl] -2-methyl- lH-pyrrole-3-c arboxylic acid isobutyl-amide,
l-Furan-2-ylmethyl-5-[2-(4-methoxy~phenylM c arboxylic acid isobutyl-amide,
l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazoI-4-yl]-2-methyl-lH-pyrrole-3 -carboxylic acid isobutyl-amide,
l-Cyclohexylmethyl-5-[2-(4-methoxy-pheny^ 3-c arboxylic acid allylamide,
l-Cyclohexylmethyl-5- [2-(4-methoxy-phenyl)-thiazol-4-yl] -2-methyl- lH-pyrroIe-3-c arboxylic acid cyclohexylmethyl-amide,
l-Cyclohexylmethyl-2-methyl-5-(2-pyrazm^ lie acid cyclohexylmethyl-amide,
l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yI]-2-methyl-lH-pyrrole-3 -carboxylic acid cyclohexylmethyl-amide,
5-[2-(4-Methoxy-phenoxymethyl)-lhiazol-4-yl]-l-(3-methoxy-propyl)-2-meti\yl-lH-py rrole-3-carboxylic acid cyclohexylmethyl-amide,
4-[ 1-[2-(3,4-Dimethoxy-phenyl)-ethyl]-4-(3-methoxy-propylcarbamoyl)-5-methyl-1H- pyrrol-2-yl]-thiazole-2-carboxylic acid ethyl ester,
l-Cyclohexylmethyl-5-[2-(4-metlioxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid piperidin-1-ylamide,
N'-{l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carbonyl}-hydrazinecarboxylic acid ethyl ester,
r^c-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid sec-butylamide,
{l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrol-3-yl}-piperidin-l-yl-methanone,
l-Cyclohexylmethyl-5-[2"(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid phenylamide,

l-Cydohexyimethyl-5-te^ 3-carboxylic acid pyrimidin-2-ylamide,
mc-l-CydohexylmethyI-5-[2-(4-m^ pyrroleO-carboxyiicadd(5-hydroxjr-2,2,6-trimeth
5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-(3-trifluoromethoxy-^ lH-pyrrole-3-carboxylic acid butylamide,
l-BenzyI-5-[2-(4-methoxy-ph^ .
acid butylamide,
{l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyI)-thiazol-4-yl]-2-methyl^ 3-yl}-pyrrolidin-1-yl-methanone,
l-Cydohexylmethyl-5-[2-(^ pyrroIe-3-carboxyIic acid butylamide,
l-Cydohexylmeth]d-5-[2-(3-metho^ 3-carboxylic acid butylamide,
5-(2-Benzo[l,3]dioxol-5-yI-thiazol-4-yl)-l-qrdohexyImethyI-2-m 3-carboxylic acid butylamide,
l-Cyclohexylmethyl-5-[2-(4-fluoro-pte^ carboxylic acid butylamide,
l-Cyclohexylmethyl-5-[2-(2-fluoro-phenyl)-thiazol-4-yI]-2-methyI-lH-pyrrole--3-carboxylic acid butylamide,
l-Cyclohexylmethyl-2-methyl-5-[2-(4-trifluoromethoxy-phenyl)-thiazol-4-yl]"lH pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmetiyi-5-[2-(3,5-dimethoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrroIe-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-2-methyl-5-(2-m-tolyl-thiazol-4-yl)-lH-pyrrole-3--carboxylic acid butylamide,
l-Cyclohexylmethyl-2-methyl-5^^ :arf>oxylic acid butylamide,
l-Cyclohexylmetiiyl-5-[2-(4-ethyl-phenyl)-thiazol-4-yl]-2-methyl"lH-pyrrole-3-:arboxylic acid butylamide,

5-[2-(4-Chloro-phenyl)-thiazol-4-yl]-l-cyd^ carboxylic acid butylamide,
5-[2-(4-tert-Butyl-phenyl)-thiazol-4^ 3-carboxylic acid butylamide,
l-Cyclohexylmethyl-542-(2,3-dihydro-benzofa^ lH-pyrrole-3-carboxylic acid butylamide,
l-CyclohexyImethyl-2-methyl-5-(2-p-to^ acid butylamide,
l-Cyclohexylmethyl-5-[2-(6-m pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-5-[2-(2>4-dicUoro-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-2-oiet^ carboxylic acid butylamide>
l-Cyclohexylmethyl-5-[2-(4-methoxy-pheny^ 3-carboxylic acid pentylamide,
l-Cyclohexylmethyl-5-[2-(4-methoxy--phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid propylamide,
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyI)"thiazol-4-yI]-2-methyl-lH-pyrrole-3-carboxylic acid cyclohexylamide,
l-Cyclohexylmethyl-5-[2-(4-methoxy-pheny^ 3-carboxylic acid cyclopentylamide,
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid cyclopropylamide,
l7Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrro^ 3-carboxylic acid cyclobutylamide,
(traits) rac-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)"thiazoI-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid (2-hydroxy-cyclopentyl)-amide>
l-(4-Chloro-benzyl)-5-[2-(4-methoxy-phe^ 3-carboxylic acid butylamide,

l-(3,4-Dichloro-benzyl)-5-[2-(4-methoxy-phenyI)-thia2ol-4-yl]-2-meth)4-lH-pyrrole-3-carboxylic acid butylamide,
.^-(3,4«Dimethyl-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2 pyrrole-3-carboxylic acid butylamide,
l-(3,4-Dimethoxy-benzyl)-5-[2-(4-methoxy«phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-5-[2-(4-hydroxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3- . carboxylic acid butylamide,
l-(4-IsopropyI-benzyl)-5-[2-(4-methoxy-phenyl)-tiiiazol-4-yl]-2-rnethyl«lH-pyrrole-3-carboxylic acid butylamide,
5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-pyridin-2-ylmethyl-lH-pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-5-(2-cyclohexyl-tiiiazol-4-yl)-2-methyl-lH-pyrrole-3-carboxylic acid butylamide,
and pharmaceutically acceptable salts thereof.
Most preferred compounds of general formula (I) are those selected from the group consisting of:
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid butylamide,
rac-l-Cyclohexylmethyl-5-[2«(4-methoxy-phenyl)-thiazol-4-yI]-2-methyl-lH-pyrrole-3-carboxylic acid sec-butylamide,
{l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-liuazol-4-yl]-2-methyl-lH-pyrrol-3-yl}-piperidin-l-yl-methanone,
5- (2-Benzo [ 1,3 ] dioxol-5-yl-thiazol-4-yl)-1 -cyclohexylmethyl-2-methyl- lH-pyrrole-3-carboxylic acid butylamide,-l-Cyclohexylmetiiyl-5-[2-(4-fluoro-phenyl)"thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide,

1-Cyclohexylmethyl-acid butylamide^
1 -Cyclohexylmethyl-5- [2-(6-methoxy-pyridin-3-yl)-thiazol-4-yl] -2-methyl-lH-pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmediyl-2-m carboxylic acid butylamide,
l-Cyclohexylmethyl-5-[2-(4-methoxy-phen^ 3-carboxylic acid pentylamide,
l-Cyclohexylmethyl-5-[2-(4-methoxy-phen^ 3-carboxylic acid cyclohexylamide,
1 -Cyclohexylmethyl-5- [2- (4-methoxy-phenyl)-thiazol-4'-yll -2-methyl- iH-pyrrole-3-carboxylic acid cyclopentylamide,
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl^ 3-carboxylic acid cyclopropylamide,
l-Cyclohexylmethyl-5-[2-(4-hydroxy-phenyl^^^ carboxylic acid butylamide,
l-Cyclohexylmeliiyl-5-(2"Cyclohexyl-thiazol-4-yl)-2»metiiyl-lH-pyrrole-3-carboxylic acid butylamide,
and pharmaceutical^ acceptable salts thereof.
The present invention also relates to a process for the manufacture of compounds of formula (I) as defined above. The compounds of formula (I) can be manufactured by the methods given below, by the methods given in the Examples or by analogous methods. Appropriate reaction conditions for the individual reaction steps are known to the person skilled in the art. Starting materials are either commercially available or can be prepared by methods analogous to the methods given below or in the Examples or by methods known in the art.
'The compounds of formula (I) may be prepared using the general methods described-below:

Compounds of formula (I), wherein R1 to R7 and m are as previously defined, can be prepared by reaction of enamines of formula A with alfa-bromoketones of formula B according to methods known in the art (Scheme 1), For example, the reaction can be performed in an inert solvent such as DMF in the presence of a hindered base such as 2,6-.di-tert-butylpyridine or 2,6-lutidine.
Scheme 1:

Compounds of formula I can be purified by methods known in the art such as precipitation from mixtures of solvents (e.g. acetonitrile and water) or by column chromatography using Si02 with eluents know in the art (e.g. n-heptane/Ethyl acetate, dichloromethane/methanol and dichloromethane/(.l% NH3 in MeOH)).
Thiazole derivatives of formula B can be prepared from dibromodilcetones of formula C and thioamides of formula C by methods known in the art (Scheme 2). For example, the reaction can be performed by addition of thioamides of formula C to dibromo-diketones of formula D in an inert solvent such as DMF.
Scheme 2:

Enamines of formula A can be prepared from beta-ketoamides of formula E and amines of formula F by methods known in the art (Scheme 3). For example a beta-keto amide of formula E can be reacted with an amine of formula B in a suitable inert solvent (e.g. DMF) in the presence of a hindered base (e.g. 2,6-di-tert-butylpyridine) to yield enamine of formula A.
Scheme 3

Beta-ketoamides of formula E are either known form the literature or can be purchased from commercial sources or else can be prepared by methods known in the art. For example, beta-ketoamides of formula E wherein R = methyl can be prepared by reaction of amines of formula G with diketene in an inert solvent such as dichloromethane (Scheme 4).
Scheme 4

Compounds of formula D, F and G are either known from the literature or can be purchased from commercial sources or else can be synthesized by methods known in the art.
The invention further relates to compounds of formula (I) as defined above, when manufactured according to a process as defined above.
Some compounds of formula (I) may possess asymmetric centres and are therefore capable of existing in more than one stereoisomeric form. The invention thus also relates to compounds in substantially pure isomeric form at one or more asymmetric centres as well as mixtures, including racemic mixtures, thereof. Such isomers maybe prepared by asymmetric synthesis, for example using chiral intermediate, or mixtures may be resolved by conventional mehtods, eg., chromatography (chromatography with a chiral adsorbens or eluent), or use of a solving agent.
It will be appreciated, that the compounds of general formula (I) in this invention maybe derivatised at functional groups to provide derivatives which are capable of conversion back to the parent compound in vivo.

As described above, the compounds of formula (I) or pharmaceutical^ acceptable salts thereof can be used as medicaments for the treatment and/or prophylaxis of diseases which are associated with the modulation of the CBl receptors.
The invention therefore also relates to pharmaceutical compositions comprising, a compound as defined above and a pharmaceutical!-/ acceptable carrier and/or adjuvant.
Further, the invention relates to compounds as defined above for use as therapeutic active substances, particularly as therapeutic active substances for the treatment and/or prophylaxis of diseases which are associated with the modulation of CBl receptors.
In another embodiment, the invention relates to a method for the treatment and/or
prophylaxis of diseases which are associated with the modulation of CBl receptors, which
method comprises administering a compound as defined above to a human being or
i animal.
The invention further relates to the use of compounds as defined above for the treatment and/or prophylaxis of diseases which are associated with the modulation of CBl receptors.
In addition, the invention relates to the use of compounds as defined above for the preparation of medicaments for the treatment and/or prophylaxis of diseases which are associated with the modulation of CBl receptors. Such medicaments comprise a compound as defined above.
In this context, the expression 'diseases associated with modulation of CBl receptors' means diseases which can be treated and/or prevented by modulation of CBl receptors. Such diseases encompass, but are not limited to, psychic disorders, especially anxiety, psychosis, schizophrenia, depression, abuse of psychotropes, for example for the abuse and/or dependence of a substances, including alcohole dependency and nicotine dependency, neuropathies, migraine, stress, epilepsy, dyskinesias, Parkinson!s disease, amnesia, cognitive disorders, senile dementia, Alzheimer's disease, eating disorders, obesity, diabetes type II or nori insulin dependent diabetes (NIDD), gastrointestinal diseases, vomiting, diarrhea, urinary disorders, cardiovascular disorders, infertility disorders, inflammations, infections, cancer, neuroinflammation, in particular in

atherosclerosis, or the Guillain-Barre syndrome, viral encephalitis, cerebral vascular incidents and cranial trauma.
In a preferable aspect, the expression 'diseases associated with modulation of CB1 receptors3 relates to eating disorders, obesity, diabetes type II or non insulin dependent diabetes (NIDD), neuroinflammation, diarrhea> abuse and/or dependence of a substances, including alcohole dependency and nicotine dependency. In a more preferable aspect, the said term related to eating disorders, obesity, diabetes type II or non insulin dependent diabetes (NIDD), abuse and/or dependence of a substances, including alcohole dependency and nicotine dependency, with obesity being especially preferred.
It is a further preferred object to provide a method of treatment or prevention of Type II diabetes (non-insulin dependent diabetes meUitus (NIDDM) in a human which comprises administration of a therapeutically effective amount of a compound according to formula (I) in combination or association with a therapeutically effective amount of a lipase inhibitor, particularly, Wherein the lipase inhibitor is orlistat. Also an object of the invention is the method as described above for the simultaneous, separate or sequential administration of a compound according to formula (I) and a lipase inhibitor, particularly tetrahydr olipstatin.
It is a further preferred object to provide a method for the treatment or prevention of obesity and obesity related disorders which comprises administration of a therapeutically effective amount of a compound according to formula (I) in combination or association with a therapeutically effective amount of other drugs for the treatment of obesity or eating disorders so that together they give effective relief. Suitable other drugs include but are not limited to anorectic agents, lipase inhibitors and selective serotonin reuptake inhibitors (SSRI). Combinations or associations of the above agents maybe encompassing separate, sequential or simultaneous administration.
Preferable lipase inhibitor is tetrahydrolipstatin.
Suitable anorectic agents of use in combination with a compound of the present invention include, but are not limited to, aminorex, amphechloral, amphetamine, benzphetamine, chlorphentermine, clobenzorex, cloforex, clominorex, clortermine, cyclexedrine, dexfenfluramine, dextroamphetamine, diethylpropion, diphemethoxidine, N-ethylamphetamine, fenbutrazate, fenfluramine, fenisorex, fenproporex, fludorex, fluminorex, furfurylmethylamphetamine, levamfetamine, levophacetoperane, mazindol,

mefenorex, metamfepramone, methamphetamine, norpseudoephedrine, pentorex, phendimetrazine, phenmetrazine, phentermine, phenylpropanolamine, picilorex and • sibutramine, and pharmaceutical^ acceptable salts thereof.
Most preferable anorectic agents are sibutramine and phentermine.
Suitable selective serotonin reuptake inhibitors of use in combination with a compound of the present invention include: fluoxetine, fluvoxamine, paroxetine and sertraline, and pharmaceutically acceptable salts thereof.
Demonstration of additional biological activities of the compounds of the present invention may be accomplished through in vitro, ex vivo, and in vivo assays that are well known in the art. For example, to demonstrate the efficacy of a pharmaceutical agent for the treatment of obesity-related disorders such as diabetes, Syndrome X, or atherosclerotic disease and related disorders such as hypertriglyceridemia and hypercholesteremia, the following assays maybe used.,
Method for Measuring Blood Glucose Levels
db/db mice (obtained from Jackson Laboratories, Bar Harbor, ME) are bled (by either eye or tail vein) and grouped according to equivalent mean blood glucose levels. They are dosed orally (by gavage in a pharmaceutically acceptable vehicle) with the test compound once daily for 7 to 14 days. At this point, the animals are bled again by eye or tail vein and blood glucose levels are determined.
Method for Measuring Triglyceride Levels
hApoAI mice (obtained from Jackson Laboratories, Bar Harbor, ME) are bled (by either eye or tail vein) and grouped according to equivalent mean serum triglyceride levels. They are dosed orally (by gavage in a pharmaceutically acceptable vehicle) with the test compound once daily for 7 to 14 days. The animals are then bled again by eye or tail vein,
•r
and serum triglyceride levels are determined.
Method for Measuring HDL-Cholesterol Levels
To determine plasma HDL-cholesterol levels, hApoAI mice are bled and grouped with equivalent mean plasma HDL-cholesterol levels. The mice are orally dosed once daily

with vehicle or test compound for 7 to 14 days, and then bled on the following day. Plasma is analyzed for HDL-cholesterol.
In addition, to demonstrate CNS activities of the compounds of the present invention, the following in vivo assays maybe used.
Method for Testing Task Learning and Spatial Memory
The Morris Water Maze is routinely used to assess task learning and spatial memory (Jaspers et al., Neurosci. Lett 117:149-153,1990; Morris, J. NeuroscL Methods 11:47-60, 1984). In this assay, animals are placed in a water pool which is divided into quadrants. One platform is hidden in one of the quadrants. The animal is placed in the water pool and is expected to locate the hidden platform within a predetermined time. During a number of training trials, the animal learns the location of the platform and escape from the pool. The animal receives multiple trials in this task. Total distance traveled, number of trials to locate platform, latency to fin(d platform, and the swimming path is recorded for each animal. The animal's learning ability is measured by the length of time or number of trials required to find the hidden platform. Memory deficit or improvement is determined by the number of trials or the latency to find the platform at predetermined delay time after acquisition. Leaning and memory may be measured by the number of times that the animal crosses the quadrant where the platform was located during the acquisition phase.
Method for Testing Drug Dependence
Self-administration in animals is a predictor of a compound's abuse potential in humans. Modifications to this procedure may also be used to identify compounds that prevent or block the reinforcing properties of drugs that have abuse potential. A compound that extinguishes the self-administration of a drug may prevent that drug's abuse or its . dependence. (Ranaldi et al., Psychopharmacol. 161:442-448, 2002; Campbell et al., Exp. Clin. Psychopharmacol. 8:312-25, 2000). In a self-administration test, animals are placed in the operant chambers containing both an active and inactive lever. Each response on the active lever produces an infusion of either the test compound or a drug known to be self-administered. Presses on the inactive lever have no effect, but are also recorded. Animals are. then trained to self-administer compound/drug over a set period of time by having drug access during each daily session. Illumination of the chamber house light signals the beginning of the session and the availability of the compound/drug. When the session ends, the house light is turned off. Initially, a drug infusion occurs with every press of the

active lever. Once lever-pressing behavior has been established, the number of presses to produce a drug infusion is increased. After stable compound/drug self-administration is - obtained, the effect of a second compound on the drug-reinforced behavior may be evaluated. Administration of this second compound prior to the session can either potentiate, extinguish, or produce no change to the self-administrating behavior.
The following tests were carried out in order to determine the activity of the compounds of formula (I).
The affinity of the compounds of the invention for cannabinoid CBl receptors was determined using membrane preparations of human embryonic kidney (HEK) cells in which the human cannabis CBl receptor is transiently transfected using the Semliki Forest Virus system in conjunction with [3H]-CP-55,940 as radioligand. After incubation of a freshly prepared cell membrane preparation with the [3H]-ligand, with or without addition of compounds of the invention, separation of bound and free ligand was performed by filtration over glassfiber filters. Radioactivity on the filter was measured by liquid scintillation counting.
The affinity of the compounds of the invention for cannabinoid CB2 receptors was determined using membrane preparations of human embryonic kidney (HEK) cells in which the human cannabis CB2 receptor is transiently transfected using the Semliki Forest virus system in conjunction with [3H]-CP-55,940 as radioligand. After incubation of a freshly prepared cell membrane preparation with the [3H]-ligand, with or without addition of compounds of the invention, separation of bound of bound and free ligand was performed by filtration over glassfiber filters. Radioactivity on the filter was measured by liquid scintillation counting.
The cannabinoid CBl antagonistic activity of compounds of the invention was determined by functional studies using CHO cells in which human cannabinoid CBl receptors are stably expressed (see M. Rinaldi-Carmona et. al., J. Pharmacol, Exp. Ther. 278 (1996) 871). The stable expression of the human cannabinoid receptor in cell systems was first described in Nature 1990,346, 561-564 (CBl) and Nature 1993, 365,61-65 (CB2) respectively. Adenylyl cyclase was stimulated using forskolin and measured by quantifying the atnount of accumulated cyclic AMP. Concomitant activation of CBl receptors by CBl receptor agonists (e.g. CP-55,940 or (R)-WIN-55212-2) can attenuate the forskolin-induced accumulation of cAMP in a concentration dependent manner. This CBl receptor

mediated response can be antagonised by CB1 receptor antagonists such as the compounds of the invention.
The compounds of formula (I) show an excellent affinity for the CB1 receptor, determined with the experimental conditions described in Devane et.al. Mol. Pharmacol. 34 (1988) 605-613. The compounds of the present invention or the pharmaceutical^ acceptable salts or sovates are antagonists and selective for the CBl receptor with affinites
below IC5o = 2 \xM. They exhibit at least, a 10 fold selectivity against the CB2 receptor.

Effect of CBl receptor antagonist/inverse agonist on CP 55,940-induced Hypothermia in NMRI mice
Animals
Male NMRI mice were used in this study and were obtained from Research Consulting Company Ltd (RCC) of Fiillinsdorf (Switzerland). Mice, weighing 30-31g were used in this study. Ambient temperature is approximately 20-21°C and relative humidity 55-65%. A 12 hours light-dark cycle is maintained in the rooms with all tests being performed during the light phase. Access to tap water and food are ad libitum.
L.

Method
All measurements were made between 12:00 am and 5:00 pm. Mice were brought in this environment and habituated for at least two hours before the start of the experiment. •They had always free access to food and water. For each dose, 8 mice were used. Rectal body, temperature measurements were recorded by mean of a rectal probe (RET2 of Physitemp) and digital thermometer (Digi-sense n°8528-20 of Cole Parmer, Chicago USA). The probe was inserted about 3.5 cm in each mouse.
The body temperature was taken 15 min before administration of either Vehicle or CB1 receptor antagonist/inverse agonist. 30 or 90 min after i.p. or p.o. administration of this compound, respectively, rectal body temperature was recorded in order to evaluate any influence of the compound itself. The CB receptor agonist CP 55,940 (0.3 mg/kg) was immediately administered intravenously, then 20 min after i.v. administration of CP 55940, body temperature was again measured.
The in vivo activity of compounds of formula (1) was assessed for their ability to regulate feeding behaviour by recording food consumption in food deprived animals.
Rats were trained to have access to food for 2h per day and were food deprived for 22h. When they were trained under this schedule, the amount of food taken every day during these 2h food intake session was consistent day after day.
To test the ability of compounds of formula (1) to decrease food intake, 8 animals were used in a cross-over study. Rats were individually housed in Plexiglas boxes with a grid on the floor and a paper was placed below the cage floor to collect any spillage. A food dispenser (becher) filled with a pre-weighed amount of food was presented to them for 2h. At the end of the food intake session, rats returned to their home cage. Each rat was weighed before the start of the experiment and the amount of food consumed during this 2h food intake session was recorded. Either various doses of test compound or vehicle was administered orally 60 min before the 2h food intake session. A positive control Rimonabant (SR141716) was included in the experiment. An Anova analysis with repeated measures was used followed by a posthoc test Student Neumann-Keuls. * P Furthermore the utility of compounds of formula (1) in diseases or disorders maybe demonstrated in animal disease models that have been reported in the literature. The

following are examples of such animal disease models: a) reduction of sweet food intake in marmosets (Behavioural Pharm, 1998, 9,179-181); b) reduction of sucrose and ethanol - intake in mice (Psychophafm. 1997, 132, 104-106); c) increased motor activity and place conditioning in rats (Psychopharm. 1998, 135, 324-332; Psychopharmacol 2000, 151: 25-30); d) spontaneous locomotor activity in mice (J. Pharm. Exp. Ther. 1996, 277, 586-594); e) reduction in opiate self-administration in mice (Sci. 1999,283,401-404);
The compounds of. formula (I) and/or their pharmaceutical^ acceptable salts can be -used as medicaments, e.g. in the form of pharmaceutical preparations for enteral, parenteral or topical administration. They can be administered, for example, perorally, e.g. in the form of tablets, coated tablets, dragees, hard and soft gelatine capsules, solutions, emulsions or suspensions, rectally, e.g. in the form of suppositories, parenterally, e.g. in the form of injection solutions or infusion solutions, or topically, e.g. in the form of ointments, creams or oils. Oral administration is preferred.
The production of the pharmaceutical preparations can be effected in a manner which will be familiar to any person skilled in the art by bringing the described compounds of formula (I) and/or their pharmaceutical^ acceptable salts, optionally in combination with other therapeutically valuable substances, into a galenical administration form together with suitable, non-toxic, inert, therapeutically compatible solid or liquid carrier materials and, if desired, usual pharmaceutical adjuvants.
Suitable carrier materials are not only inorganic carrier materials, but also organic carrier materials. Thus, for example, lactose, corn starch or derivatives thereof, talc, stearic acid or its salts can be used as carrier materials for tablets, coated tablets, dragees and hard gelatine capsules. Suitable carrier materials for soft gelatine capsules are, for example, vegetable oils, waxes, fats and semi-solid and liquid polyols (depending on the nature of the active ingredient no carriers might, however, be required in the case of soft gelatine capsules). Suitable carrier materials for the production of solutions and syrups are, for example, water, polyols, sucrose, invert sugar and the like. Suitable carrier materials for injection solutions are, for example, water, alcohols, polyols, glycerol and vegetable oils. Suitable carrier materials for suppositories are, for example, natural or hardened oils, waxes, fats and semi-liquid or liquid polyols. Suitable carrier materials for topical preparations are glycerides, semi-synthetic and synthetic glycerides, hydrogenated oils, liquid waxes, liquid paraffins, liquid fatty alcohols, sterols, polyethylene glycols and cellulose derivatives.

Usual stabilizers, preservatives, wetting and emulsifying agents, consistency-improving agents, flavour-improving agents, salts for varying the osmotic pressure, buffer • substances, solubilizers, colorants and masking agents and antioxidants come into consideration as pharmaceutical adjuvants.
The dosage of the compounds of formula (I) can vary within wide limits depending on the disease to be controlled, the age and the individual condition of the patient and the mode of administration, and will, of course, be fitted to the individual requirements in each particular case. For adult patients a daily dosage of about 1 to 1000 mg, especially about 1 to 100 mg, comes into consideration. Depending on severity of the disease and the precise pharmacokinetic profile the compound could be administered with one or several daily dosage units, e.g. in 1 to 3 dosage units.
The pharmaceutical preparations conveniently contain about 1-500 mg, preferably 1-100 mg, of a compound of formula (I).
i The following Examples serve to illustrate the present invention in more detail. They are, however, not intended to limit its scope in any manner.

Examples
JViS = mass spectrometry; ISP = ion spray (positive ion), corresponds to ESI and ES+ (electrospray, positive ion); mp = melting point.
Example 1
1-Cyclohexylmethyl-2-methyl-5-[2
carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH> aminomethylcyclohexane as R -(CH2)m-NH2 and 4-nitrophenyl thioamide as R C(S)NH2, as follows:
1. Synthesis of 2-bromo-l-[2-(4-nitro-phenyl)-thiazol-4-yl]-ethanone (Compound B)
To a solution of 1.4 g of l,4-dibromo-2,3-butanedione in dimethylformamide (110 ml) at room temperature was added 1.4 ml of 2,6-di-tert-butylpyridine. Then a solution of 1.0 g of 4-nitro-phenyl-thiobenzamide in 20 ml of dimethylformamide was slowly added to the reaction mixture over 1 hour. The reaction mixture was then allowed to stir for an additional hour at room temperature before being concentrated in vacuo. The residue was then purified by chromatography over a short column (SiO?, 120g, CH2CI2100%). The isolated compound was triturated with isopropylether to yield 771 mg of the title compound as a yellow solid, mp = 186-187°C, MS (EI) 326(M).
2. Synthesis of l-Cyclohexylmethyl-2-methyl-5-[2-(4-nitro-phenyl)-thiazol-4-yl]-lH-
pyrrole-3-carboxylic acid butylamide
To a solution of 4.2 g of diketene in.dichloromethane (70 ml) cooled at 0°C was added over 1 hour a solution of 3,7 g of butylamine in 50 ml of dichloromethane. The reaction mixture was then stirred for one hour at 0°C and then let to stir at room temperature for

another hour. The reaction mixture was then concentrated in vacuo and the crude residue was partitioned in batches which were directly used in the next step.
To 180 mg of the previous crude material in 5 ml of dimethylformamide was added 0.15 ml of cyclohexylmethylamine together with 0.13 ml of trimethyl orthoformate and the reaction mixture was stirred for 24 hours at room temperature. After such time, 260 mg of 2-bromo-l-[2-(4-nitro-phenyl)-thiazol-4-yl]-ethanone was added together with 0.14 ml of 2,6-lutidine and the reaction mixture was stirred for another 24 hours at room temperature. After such time, 5 ml of a MeCN-H20 (1:1) solution is added to the reaction mixture, the precipitate is filtrated and washed with MeCN-H20 (1:1) and isopropylether to yield 264 mg of the title compound as a yellow solid, mp = 184-187 °C, MS (ISP) 481.3 (M+H)+.
Examples 2-375 were synthesized in analogy to Example 1, using the indicated educts.
Example 2 .
l-Butyl-5- [2-(2-chloro-phenyl)-thiazol-4-yl] -2-methyl-lH-pyrrole-3-carboxylic acid
butylamide

The title compound was obtained using butylamine as R R NH> butylamine as R -(CH2)m-NH2 and 2-cHoro-phenyl thiobenzamide as R4C(S)NH2, MS(ES-h) 430. (M+H)+. "

l-Butyl-5-[2-(4~methoxy-phenyl)-thiazol-4^
butylamide

The title compound was obtained using butylamine as R R NH, butylamine as R -(CH2)m-NH2 and 4-methoxy-phenyl thiobenzamide as R4C(S)NH2> MS(ES+) 426 (M+H)+.
Example 4
5-[2-(2-Chloro-phenyl)-tHazol-4-yl]-l-isobutyl
butylamide

The title compound was obtained using butylamine as R R"NH, isobutylamine as R -(CH2)nrNH2 and 2-chloro-phenyl thiobenzamide as R4C(S)NH2, MS(ES+) (M+H)+.

Example 5
l-I$obutyl-5-[2-(4-methoxy-phenyl
butylamide

The title compound was obtained using butylamine as R R NH, isobutylamine as R -(CH2)m-NH2 and 4-methoxy-phenyl thiobenzamide as R4C(S)NH2, MS(ES+) 426 (M+H)+.
Example 6
l-Isobutyl-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxyUcacid
butylamide

The title compound was obtained using butylamine as R R NH, isobutylamine as R -(CH2WNH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 398 (M+H)+.

Example 7
5-[2-(2-CHoro-phenyl)-thiazol-4-yl]-l-cyclota
carboxylic acid butylamide

The title compound was obtained using butylamine as RlR2NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-chloro-phenyl thiobenzamide as R4C(S)NH2> MS(ES+) 470 (M+H)+.
Example 8
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-&^
carboxylic acid butylamide

The title compound was obtained using butylamine as R1R2NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxy-phenyl thiobenzamide as R4C(S)NH2> MS(ES+) 466 (M+H)+.

Example 9
1-Cyclohexylmethyl-5-[-2-(4^
pyrrole-3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES-f) 496 (M+H)+.
Example 10
l-Cyclohexylmethyl-5-[2-(2-ethyl-pyridin-4-yl)-thiazol-4-yl]-2-methyl-lH-pyrrole-
carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-ethyl-4-pyridinecarbothioamide as R4C(S)NH2) MS(ES+) 465 (M+H)+.

Example 11
1-Cyclohe:xylmethyl-2-methyl
acid butylamide

The title compound was obtained using butylamine as R R~NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 438-(M+H)+.
Example 12
5-[2^2-Chloro-phenyl)-thiazol-4-yl]-2-methyl-l-(tetrahydro-furan-2-ylmetbyl)-lH^
pyrrole-3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 2-chlorophenyl thioamide as R4C(S)NH2, MS(ES+) 458 (M+H)+.

Example 13
5-[2-(4-Methoxy-phenyl)-ftiazol
pyrrole-3-carboxylic acid butylamide

The title compound was obtained using butylamine as R1R2NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 4-methoxy-phenyl thioamide as R4C(S)NH2> MS(ES+) 454 (M+H)+.
Example 14
5-[2-(4-Methoxy-phenoxymethyl)-thiazol-4-yl]-2-meliyl-l-(tetrahydro-furan"2-ylmethyl)-lH-pyrrole-3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 484 (M+H)+.

Example 15
. 5-[2-(2-Ethyl-pyridin-4-yl)-thiazol-4^
pyrrole-3-carboxylic acid butylamide

The title compound was obtained using butylamine as RlR2NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 2-ethyI-4-pyridine carbothioamide as R4C(S)NH2, MS(ES+) 453 (M+H)+.
Example 16
2-Methyl-5-[2-(6-methyl-pyridin-3-yl)-tta
lH-pyrrole-3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 6-methyl-pyridine-3-carbothiamide as R4C(S)NH2) MS(ES+) 439 (M+H)+.

Example 17
- 2-Methyl-5-(2-pyrazin-2-yta
carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, tetrahydrofurfiirylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothiamide as R4C(S)NH2, MS(ES+) 426 (M+Hf.
Example 18
l-(2-Mellioxy-ethyl)-5-[2-(4-m
carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, 2-methoxyethylamine as R3-(CH2)m-NH2 and 4-methoxy-phenyl thioamide as R4C(S)NH2> MS(ES+) 428 (M+H)+.

Example 19
l-(2-Methoxy-ethyl)-2-methy^
acid butylamide

The title compound was obtained using butylamine as R R NH, 2-methoxyethylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 400 (M+H)+.
Example 20
5-[2-(2-Chloro-phenyl)-thia2ol-4-yl]-l-furan-2-ylmethyl-2-methyl-lH-pyrrole-3-
carboxylic acid butylamide

The title compound was obtained using butylamine as R^NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 2-chlorophenyl thioamide as R4C(S)NH2, MS(ES+) 454 (M+H)+.

Example 21
l-Furan-2-ylmethyl-5-[2-(4-me&thoxy
carboxylic acid butylamide

The title compound was obtained using butylamine as RlR2NH, 3-(aminomethyl)-thiophene as R3-(CH2)m-NH2 and 4-methoxy-phenyl thioamide as R4C(S)NH2, MS(ES+) 450 (M+H)+.
Example 22
5-[2-(2-Ethyl-pyridin-4-yl)-tHazol~4-yl^
carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, 3-furyl methylamine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothioamide as R4C(S)NH2, MS(ES+) 449 (M+H)+.

Example 23
5-[2-(2-CUoro-phenyl)-thiazol-4-yl]-l-(4-methoxy-benzyl)-2-methyl-lH
carboxylic acid butylamide

The title compound was obtained using butylamine as R1R2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2-chlorophenyl thioamide as R4C(S)NH2, MS(ES+) 494 (M+H)+.
Example 24
l-(4-Methoxy-benzyl)-5-[2-(4~methoxy-pheny^
carboxylic acid butylamide

The title compound was obtained using butylamine as R1R2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 490 (M+H)+.

Example 25
l-(4-Methoxy-benzyl)-5-{2-(4-methoxy-phenoxyme&^
pyrrole-3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 520 (M+H)+.
Example 26
5-[2-(2-Ethyl-pyridin-4-yl)-liuazol-4-yl]-l«(4-methoxy-benzyl)-2-methyl-lH
carboxylic acid butylamide
9 ■
The title compound was obtained using butylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)ra-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2) MS(ES+) 489 (M+H)+.

Example 27
4-[4-ButylcWrbamoyl-l-(4-methoxy-te
carboxylic acid ethyl ester

The title compound was obtained using butylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2, MS(ES-h) 456 (M+H)+.
Example 28
l-(4-Methoxy-benzyl)-2-methyl-5-[2-(6-methyl-pyridin-3-yl)-thiazol-4-yl]-lH-pyrrole-
3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 475 (M+H)+.

Example 29
- l-(4-Methoxy-benzyl)-2-methyl-5-(2-pyrazin
acid butylamide

The title compound was obtained using butylamine as R1R2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothiamide as R4C(S)NH2, MS(ES+) 462 (M+H)+.
Example 30
5-[ 2 - (4-Methoxy-phenyl)-thiazol-4^
carboxylic acid butylamide

The title compound was obtained using butylamine as RXR2NH, methoxypropylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 442 (M+H)+.

Example 31
5-[2-(4-Methbxy-phenoxymrthyl)
pyrrole-3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, methoxypropylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethane thioamide as R4C(S)NH2, MS(ES+) 472 (M+H)+.
Example 32
4- [4-Butylcarbamoyl-1 - (3 -methoxy-propyl)-5-methyl- lH-pyrrol-2-yl] -thiazole-2-
carboxylic acid ethyl ester

The title compound was obtained using butylamine as R1R2NH, methoxypropylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2> MS(ES+) 408 (M+H)+.

Example 33
5-[2-(2-CUoro-phenyl)-thiazol-4^
carboxylic acid butyiamide

The tide compound was obtained using butylamine as RR NH> 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 470 (M+H)+.
Example 34
5- [2-(4-Methoxy-phenyl) -thiazol-4-yl] -2-methyl-1 -thiophen-2-ylmethyl- lH-pyrrole-3-
carboxylic acid butyiamide

The title compound was obtained using butylamine as R R NH, 3-(aminomethyl)thiophene as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 466 (M+H)+.

Example 35
5-[2-(4-Methbxy-phenoxymethyl)-thfe^^
pyrrole-3-carboxylic acid butylamide

The title compound was obtained using butylamine as R^NH, 3-(aminomethyl)thiophene as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2> MS(ES+) 496 (M+H)+.
Example 36
5-[2-(2-Ethyl-pyridin-4-y])-thiazol-4-yl]-2-^^
carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH> 3-(aminomethyl)thiophene as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 465 (M+H)+-

Example 37
. l-[2-(3,4-Dimelhoxy-phenyl)-^
lH-pyrrole-3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH> homoveratrylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 533 (M+H)+.
Example 38
mc-l-Butyl-5-[2-(2-cUoro-phenyl)-thiazol-4-yl]--2-methyl-lH-pyrrole-3-carboxylicacid
■»►*
sec-butylamide

The title compound was obtained using sec-butylamine as R R NH> butylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 430 (M+H)+.

Example 39
rac-l-Butyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-
acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, butylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2) MS(ES+) 426 (M+H)+.
Example 40
rac-l-Butyl-5-[2-(4-meliioxy-pheno}ty^
carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, butylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 456 (M+H)+.

Example 41
rac-l-Butyl-5-[2-(2-ethyl-pyri&
acid sec-butylamide

The title compound was obtained using sec-butylamine as R R'NH, butylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2) MS(ES+) 425 (M+H)+.
Example 42
rac-5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-isobutyl-2-methyl-lH-pyrrole-3-carboxylic
acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, isobutylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 430 (M+H)+.

Example 43
. rac-l-Isobutyl-5-[2-(4-methoxy-phenyl)^
acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, isobutylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 426 (M+H)+.
Example 44
rac-1 -lsobutyl-5- [ 2-(4-methoxy-phenoxymethyl) -thiazol-4-yl] -2-methyl- lH-pyrrole-3-
carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, isobutylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 456 (M+H)+.

Example 45
rac-5-[2-(2-chloro-phenyl)-thia2ol-4-yl]-l-cyclohexylmethyl-2-methyl-lH-pyrrole-3-
carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES-h) 470 (M+H)+.
Example 46
rac-l-Cydohexylmethyl-5-[2-(4-metiioxy-^^
carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH,
"" * ' ' exane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as
15 f)466'(M+H)+.

Example 47
rac-1-Cyclohexylmethyl^
pyrrole-3-carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2> MS(ES+) 496 (M+H)+.
Example 48
rac-l-Cyclohexylmethyl-5-[2-(2-ethyl-^^
carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 465 (M+H)+.

Example 49
rac-1-Cyclohexylmeth^
carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R"NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2) MS(ES+) 438 (M+H)+.
Example 50
rac-5-[2»(2-Chloro-phenyl)-thiazol-4-yl]-2-methyl-l-(tetrahydro-furan-2-ylmethyl)-lH-
pyrrole-3-carboxylic acid sec-butylamide

1 o
The title compound was obtained using sec-butylamine as R R NH, i tetrahydrofiirfurylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2> MS(ES+) 458 (M+H)+.

Example 51
. rac-5-[2-(4-Methoxy-phe^
lH-pyrrole-3-carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as RlR2NH, tetrahydrofurfurylamine as R ~(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ES+) 454 (M+H)+.
Example 52
rac-5-[2-(4-Methoxy-phenoxyme^
ylmethyl)-lH-pyrrole-3-carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2j MS(ES+) 484 (M+H)+.

Example 53
rac-2-Methyl-5-(2-pyrazin-2-yl-th^
pyrrole-3-carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, tetrahydrofurfurylamine as R3-(CH2)nrNH2 and pyrazine-2-carbothioamide as R4C(S)NH2) MS(ES+) 426 (M+H)+.
Example 54
rac-l-(2-Methoxy-ethyl)-5-[2-(4-methoxy-phen^
carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as RlR2NH> methoxyethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 428 (M+H)+.

Example 55
rac-5-[2-(2-CHoro-phenyl)-thiazol-4^
carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, 3-furylmethylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 454 (M+H)+.
Example 56
rac-l-Furan-2-ylmethyl-542-(4-methoxy-phenyl)-thiazol-4-yl]-2-metityl--lH-pyrrole-3-
carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R^NH, 3-furylmethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES-t-) 450 (M+H)+.

Example 57
. rac-5-[2-(2-Ethyl-pyridin-4-yl
carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, 3-furylmethylamine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 449 (M+H)+.
Example 58
rac-5-[2-(2-CMoro-phenyl)-thiazol-4-yl]-l-(4-m
carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, 4-methoxybenzyl-amine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 494 (M+H)+.

Example 59
. rac4-(4-Me&oxy-benzyl)-5-[2-(4-methoxy-phen^
3-carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH> 4-methoxybenzyl-amine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 490 (M+H)+.
Example 60
rac-l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenoxymetiiyl)-lWazol-4-yl]-2-methyl-lH-
pyrrole-3-carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, 4-methoxybenzyl-amine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 520 (M-hH)+. :'

Example 61
raC-5-[2-(2-Ethyl-pyridin-4-yl)-to
pyrrole-3-carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, 4-methoxybenzyl-amine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 489-(M+H)+.
Example 62
mc-l-(4-Melhoxy-benzyl)-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-
carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, 4-methoxybenzyl-amine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 462 (M+H)+.

Example 63
. rac-5-[2-(4-Methoxy-phenyl)-thiazol-4-yl
3-carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, methoxyethylamine as R3-(GH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 442 (M+H)+.
Example 64
rac-5-[2-(4-Methoxy-phenoxymethylH
pyrrole-3-carboxylic acid sec-butylamide

The title compound was obtained using sec-butylamine as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 472(M+H)+.

Example 127
1 l-Butyl-5-[2-(4-methoxy-ph
cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R R'NH, butylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ES+) 466 (M+H)+.
Example 128
l-Butyl-5-[2-(4-methoxy-phenoxymethyl)-thiazol"4-yl]-2-methyl-lH-pyrrole-3-
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R.R NH, butylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 496 (M+H)+.

Example 129
* l-Butyl-5- [2-(2-ethyl-pyridin-4-yl)-thiazol"4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid
cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R R NH, butylamine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 465 (M-t-H)+.
Example 130
5-[2-(2-Chloro-phenyl)--thiazol-4-yl]-l-isobutyl-2-methyl-lH-pyrrole-3-carboxylicacid
cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R.R NH, isobutylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 470 (M+H)+.

Example 131
■ l-Isobutyl-5-[2-(4-methoxy-phe^^
cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as RlR2NH> isobutylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2) MS(ES+) 466 (M+H)+.
Example 132
l-Isobutyl-5-[2«(4-methoxyrphenoxymethyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R?R2NH, isobutylamine as R3-(CH2)nrNH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 496 (M+H)+.

Example 133
l-Isobutyl-2-methyl-5-(2-pyrazin-2«yl-thiazol-4-yl)-lH-pyrrole-3-carboxylicacid
cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R^NH, isobutylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+)438(M+H)+.
Example 134
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R. R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as
R4C(S)NH2, MS(ES+) 506 (M+H)+.

Example 135
l-Cyclohexylmethyl-5-[2-(2-ethyl-py^
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R*R2NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 505 (M+H)+.
Example 136
l-Cyclohexylmethyl-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxylic
acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R.R"NH, aminomethylcyclohexane as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as
R4C(S)NH2, MS(ES+) 478 "(M+H)+.

Example 137
5-[2-(2-Chloro-phenyl)-thiazoI-4-yl]-^^
pyrrole-3-carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R R"NH, tetrahydrofiirfiirylamine as R -(CH2)m-NH2 and 2-chloro-pheiiyl thioamide as R4C(S)NH2J MS(ES+) 498 (M+H)+.
Example 138
5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-(tetrahydro-flxran-2-ylmethyl)-lH-
pyrrole-3-carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R.R NH, tetrahydrofiirfiirylamine as R -(CH2)m"NH2 and 4-methoxyphenyl thioamide as
R4C(S)NH2, MS(ES+) 494 (M+H)+.

Example 139
5-[2~(4-Methoxy-phenbxymethyl)-thiazol-4^
ylmethyl)-lH-pyrrole-3-carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R R NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide
as R4C(S)NH2, MS(ES-h) 524 (M+H)+.
Example 140
5-[2-(2-Ethyl-pyridin-4-yl)-thiazol-4-yl]^^
pyrrole-3-carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R. R NH, tetrahydrofurfurylamine as R -(CH2)m~NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 493 (M+H)+.

Example 141
4-[4-(Cyclohexylmethyl-carbamoyl)-5-meth^
pyrrol-2-yl]-thiazole-2-carboxylic acid ethyl ester

The title compound was obtained using aminomethylcyclohexane as R R~NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and ethylthiooxamate, MS(ES+) 460 (M+H)+.
Example 142
2-Methyl-5-[2-(6-methyl-pyridin-3-yl)-thiazol-4-yl]-l-(tetrahydro-furan-2-ylmethyl)-
lH-pyrrole-3rcarboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as RR NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioanlide as R4C(S)NH2. xx479

Example 143
■ 2-Methyl-5-(2-pyrazin-2-yl"^
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R R NH, tetrahydrofurfiirylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as
R4C(S)NH2, MS(ES+) 466 (M+H)+.
Example 144
5-[2-(2-Chloro-phenyl)-thiazol-4-ylH^
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R- R NH, methoxyethylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2> MS(ES+) 472 (M+H)+.

Example 145
l-(2-Methoxy-ethyl)-5-[2^
«»■'
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ES+) 468 (M+H)+.
Example 146
l-(2-Methoxy-ethyl)-5-[2-(4-methoxy-phenoxymeliyl)-thiazol-4-yl]-2-methyl-lH-
pyrrole-3-carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R -(C^m-NH^ and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2> MS(ES+) 498 (M+H)+.

Example 147
5-[2-(2-Ethyi-pyridm-^
carboxylic acid cyclohexylmethyl-arnide

The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 467 (M+H)+.
Example 148
4-[4-(Cyclohexylmethyl-carbamoyl)-l-(2-methoxy-ethyl)-5-methyl-lH-pyrrol-2-yl]-
thiazole-2-carboxylic acid ethyl ester

The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2., MS(ES+) 434 (M+H)+.

Example 149
• l-(2-Methoxy-ethyl)-2-methyl-5-[2-(6-m^
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R^NH, methoxyethylamine as R3-(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 453 (M+H)Example 150
l-(2-Methoxy-ethyl)-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxylic
acid cyclohexylmethyl-amide
t
The title compound was obtained using aminomethylcyclohexane as R-R NH, methoxyethylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R C(S)NH2, MS(ES+) 440 (M+H)+.

Example 151
l-(2-Cyclohex-l-enyl-^
pyrrole-3-carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using arninomethylcyclohexane as R R NH, 2-(l-cyclohexenyl)ethylamine as R -(CH2)nrNH2 and 2-ethyl-4-pyridine carbothiamide as
R4C(S)NH2> MS(ES+) 517 (M+H)+.
Example 152
l-Furan-2-ylmethyl-5-[2--(4-methoxy-phenyl)-tliiazol-4-yl]-2-methyHH-pyrrole-3-
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using arninomethylcyclohexane as R.R NH, 3-furylmethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ES+) 490 (M+H)+.

Example 153
5-[2-(2-CMoro-phenyl)-t^ *»■*
carboxylic acid cyclohexylmethyl-amide

i i
The title compound was obtained using aminomethylcyclohexane as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2, MS(ES+) 534 (M+H)+.
Example 154
l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2, MS(ES+) 530 (M+H)
Example 155
" 5-[2-(2-Ethyl-pyridin-4-yl)-thiazol-4^
carboxylic acid cyclohexylmethyl-amide

The tide compound was obtained using aminomethylcyclohexane as R!R2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridihe carbothiamide as R4C(S)NH2, MS(ES+) 529 (M+H)+.
Example 156
5-[2-(2-Chloro-phenyl)-thiazol"4-yl]-l-(3-methoxy-propyl)-2-methyl~lH-pyrrole-3-
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2, MS(ESH-) 486 (M+H)+.
■r

Example 157
• 5-[2-(4~Methoxy-phenyl):thiazol-4-yl]-l-(3-m
carboxylic acid cyclohexylmethyl-amide

" The title compound was obtained using aminomethylcyclohexane as R R NH,
methoxyethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ES+) 482 (M+H)+.
Example 158
5-[2-(4-Methoxy-phenoxymethyl)-thiazol-4-yl]-l-(3-methoxy-propyl)-2-methyl-lH-
pyrrole-3-carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R.R NH, methoxyethylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 512 (M+H)+.

.Example ypy
' 5-[2-(2-Ethyl-pyridin-4-y^
carboxylic acid cyclohexylmethyl-amide

The tide compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 481 (M+H)+.
Example 160
4-[4-(Cyclohexylmethyl-carbamoyl)-l-(3-methoxy-propyl)-5-methyl-lH-pyrrol-2"yl]-
thiazole-2-carboxylic acid ethyl ester

The title compound was obtained using aminomethylcyclohexane as R.R NH, methoxyethylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2., MS(ES+) 448 (M+H)+.

Example 161
* l-(3-Methoxy-propyl)-2-m*ethyl-5-(2-pyrazin-2-yM^
acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R R NH, methoxyethylamine as R3-(CH2)nrNH2 and pyrazine-2-carbothioamide as R4C(S)NH2,(-MS(ES+) 454 (M+H)+.
Example 162
5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-thiophen-2-ylmethyl-lH-pyrrole-3-
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R. R NH, 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as
R4C(S)NH2, MS(ES+) 506 (M+H)+.

Example 163
' 5-[2-(2-Ethyl-pyridin-4-^
carboxylic acid cyclohexylmethyl-amide

The title compound was obtained using aminomethylcyclohexane as R*R2NH, 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES-f) 505 (M+H)+.
Example 164
5-[2-(2-Chloro-phenyl)-thiazol-4^
pyrrole-3-carboxylic acid cyclohexylmethyl-amide

/
The title compound was obtained using aminomethylcyclohexane as R. R NH, homoveratrylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2, MS(ES+) 578 (M+H)+.

Example 165
l-Butyl-5-[2-(4-methoxy-phenyl)-thiazol-^^
(tetrahydro-furan-2-ylmethyl)-amide

* *\ The title compound was obtained using tetrahydrofurfurylamine as R R NH, butylamine
as R3-(CH2)m-NH2 and 4^methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 454
(M+H)+.
Example 166
4-{l-Isobutyl-5-methyl-4-[(tetrahydro-furan-2-ylmethyl)-carbamoyl]-lH-pyrrol-2-yl^
thiazole-2-carboxylic acid ethyl ester

The title compound was obtained using tetrahydrofurfurylamine as R R NH, isobutylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2, MS(ES+) 420. (M+H)+.

Example 167
l-Isobutyl-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxylica
(tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R1R2NH, isobutylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 426 (M+H)+.
Example 168
5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-cyclohexylmethyl-2-methyl-lH-pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 498 (M+H)+.

Example 169
l-Cyclohexylmethyl-5-[2^
carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2) MS(ES+) 494 (M+H)+.
Example 170
l^yclohexylmethyl-5-[2-(4rmethoxy-phenoxym
pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl) -amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2) MS(ES+) 524 (M+H)+.

Example 171
l-Cyclohexylmethyl-5-^
carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

i i
The title compound was obtained using tetrahydrofiirfurylamine as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 493 (M+H)+.
Example 172
l-Cyclohexylmethyl-2-methyl-5-(2-pyrazin~2^
acid (tetrahydro-furan-2-ylmethyl) -amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 466 (M+H)+.

Example 173
5-[2-(2-Chloro-phenyl)-tliiazol-4-yl]^
pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES-t-) 486 (M+H)+.
Example 174
2-Methyl-5-(2-pyrazin-2-yl-thiazol-4-yl^
carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The tide compound was obtained using tetrahydrofurfurylamine as R R NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2> MS(ES+) 454 (M+H)+.

Example 175
5-[2-(2-EthyI-pyridin-4-yI)-thiazol-4-yl]-l-(2-m^
carboxylic acid (tetrahydro-furan-2-ylrnethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, methoxyethylamine as R -(CH2)m-NH2 and 2-ethyI-4-pyridine carbothiamide as
R4C(S)NH2, MS(ES+) 455 (M+H)+.
Example 176
5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-furan-2-ylmethyl-2-methyl-lH-pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, 3-furylmethylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2> MS(ES+) 482 (M+H)+.

Example 177
l-Furan-2-ylmethyl-5-[2-(4-m
carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as RlR2NH, 3-furylmethylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2, MS(ES+) 478 (M+H)+.
Example 178
5-[2-(2-Ethyl~pyridin-4-ylMhm^
carboxylic acid (tetrahydro-furan-2-ylmethyl) -amide

The title compound was obtained using tetrahydrofurfurylamine as RlR2NH, 3-furylmethylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as
R4C(S)NH2> MS(ES+) 477 (M+H)+.

Example 179 -
l-(4-Methoxy~benzyl)-^
(tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofiirfurylamine as R R NH> 4-methoxybenzylamine as R3-(CH2)m-NH2 and thioacetamide as R4C(S)NH2, MS(ES-i-) 426 (M+H)+.
Example 180
5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-(4-methoxy-benzyl)-2-methyl-lH"pyrrole-3-
carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, 4-methoxybenzylamine as R -(CH2)nrNH2 and 2-chloro-phenyl thioamide as R C(S)NH2, MS(ES+) 522 (M+H)+.

Example 181
1 -(4-Methoxy-benzyl)-5- [2- (4-methoxy-phenyl)-thiazol-4-yl] -2-methyl- lH-pyrrole-3-
~arboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2> MS(ES+) 518 (M+H)+,
Example 182
l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 548 (M+H)+.
9

Example 183
4-{l-(4-Methoxy-benzyl)-5-methyl-4-[(tetrahydro-furan«2-ylmethyl)-carbam
pyrrol-2-yl}-thiazole-2-carboxylic acid ethyl ester

The title compound was obtained using tetrahydrofurfurylamine as R R NH, 4-methoxybenzyiamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2.> MS(ES+) 484 (M+H)+.
Example 184
i l-(4-Methoxy-benzyl)-2-methyl-5-[2-*(6-methyl-pyridin-3-yl)-thiazol-4-yl]-lH-pyrrole-
3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2> MS(ES+) 503 (M+H)+.

Example 135
l-(4-Methoxy-benzyl)-2-met^
acid (tetrahydro-fiiran-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as RlR2NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R C(S)NH2, MS(ES+) 490 (M+H)+.
Example 186
5-[2-(2-Ethyl-pyridin-4-yl)-thiazol-4-yl]-l-(3-methoxy-propyl)-2-methyl-lH-pyrrole-3-
carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, methoxyethylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 469 (M+H)+.

Example 187 ■
' l-(3-Methoxy-propyl)-2-me^
3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfarylamine as R R NH, methoxyethylamine as R -(CH2)m-NH2 and 6-methyl-pyridine~3-carbothioamide as
R4C(S)NH2, MS(ES+) 455 (M+H)+.
Example 188
\ l-(3-Methoxy-propyl)-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxylic
acid (tetrahydro-furan-2-ylmethyl) -amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH* methoxyethylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R C(S)NH2, MS(ES+) 442 (M+H)+.

Example 189
5-[2-(2-Chloro-phenyl)-thiazol^
carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH> 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2j MS(ES+) 498 (M+H)+.
Example 190
5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-thiophen-2-ylmethyl-lH-pyrrole-3-
carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, 3-(aminomethyl)thiophene as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as
R4C(S)NH2, MS(ES+) 494 (M+H)+.

Example 191
5-[2-(2-Ethyl-pyridin-4-yl^
carboxylic acid (tetrahydro~furan-2-yimethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 2~ethyl-4-pyridine carbothiamide as R4C(S)NH2) MS(ES+) 493 (M+H)Example 192
l-[2-(3,4-Dimetho:^-phenyl)-^
lH-pyrrole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide

The title compound was obtained using tetrahydrofurfurylamine as R R NH, homoveratrylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 561 "(M+H)+.

Example 193
• l-Butyl-5-[2-(4-methoxy-phenyl)-thiaz^
(2-methoxy-ethyl)-amide

The title compound was obtained using methoxyethyiamine as R!R2NH, butylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES-h) 428 (M+H)+.
Example 194
5-[2-(2-Chloro-phenyl)-thiazoI-4-yI]-l-cycto^
carboxylic acid (2-methoxy-ethyl)-arnide

The title compound was obtained using methoxyethyiamine as R^NH, aminomethylcyclohexane as R ~(CH2)m~NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2> MS(ES+) 472 (M-hH)+.

Example 195
l-Cyclohexylmethyl-5-[2-(4-metho
carboxylic acid (2-methoxy-ethyl)-amide

The title compound was obtained using methoxyethylamine as R R NH, arninomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 468 (M+H)+.
Example 196
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]--2-methyl-lH-
pyrrole-3-carboxylic acid (2-methoxy-ethyl)-amide

The title compound was obtained using methoxyethylamine as R R NH, arninomethylcyclohexane as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2> MS(ES+) 498 (M+H)+.

Example 201
l-Furan-2-ylmethyl-5-[2^^
carboxylic acid (2-methoxy-ethyl)-amide

The title compound was obtained using methoxyethylamine as R R NH, 3-furylmethylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2> MS(ES+) 452 (M+H)+.
Example 202
5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-(4-methoxy-benzyl)"2-methyl-lH-pyrrole-3-
carboxylic acid (2~methoxy-ethy])-amide

The title compound was obtained using methoxyethylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2> MS(ES+) 496 (M+H)
Example 203
l-(4-Methoxy4>enzyI)-5-[2-(4-methoxy-pta
carboxylic acid (2-methoxy-ethyl)-amide

The title compound was obtained using methoxyethylamine as RlR*NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2, MS(ES+) 492 (M+H)+.
Example 204
l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-lH-
pyrrole-3-carboxylic acid (2-methoxy-ethyl)-amide

The title compound was obtained using methoxyethylamine as R^NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 522 (M+H)+.

Example 205
5-[2-(2-Ethyl-pyridin-4-yl)-^
carboxylic acid (2-methoxy-ethyl)-amide

The title compound was obtained using methoxyethylamine as R1R2NH> 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 491 (M+H)+.
Example 206
4-[l-(4-Methoxy-benzyl)-4-(2-methoxy-ethylcarbamoyl)-5--methyl--lH-pyTrol-2-yl]-
thiazole-2-carboxylic acid ethyl ester

The title compound was obtained using methoxyethylamine as RlR2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2o MS(ES+) 458 (M+H)

Example 209
l-f2-(3,4-Dimethoxy-pheny^
lH-pyrrole-3-carboxylic acid (2-methoxy-ethyl)-amide

The title compound was obtained using methoxyethylamine as R R NH, homoveratrylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as
R4C(S)NH2, MS(ES-b) 535 (M+H)+.
Example 210
l-Butyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylicacid
(2-cyclohex-l-enyl-ethyl)-amide

The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as R R NH, butylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 478 (M+H)+.

Example 211
l-Cyclohexylmethyl-5-[2^
carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide

The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as RlR2NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 518 (M+H)+.
Example 212
l-Cyclohexylmethyl-5-[2-(2-ethyl-pyridin-4-^^^
carboxylic acid (2-cyclohex-l-enyl~ethyl)-amide

The tide compound was obtained using 2-cyclohex-l-enyl-ethylamine as R*R2NH> aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as
R4C(S)NH2, MS(ES+) 517 (M+H)+.

Example 213
5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-(tetrahyd
pyrrole-3-carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide

The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as R^NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 506 (M+H)+.
Example 214
5-[2-(2-Ethyl-pyridin-4-yl)-thm^
pyrrole-3-carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide

The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as RlR2NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as
R4C(S)NH2> MS(ES+) 505 (M+H)+.

Example 21 5
2-Methyl-5-[2-(6-methyl-pyri^
lH-pyrrole-3-carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide

The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as R R"NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 491 (M+H)+.
Example 216
l-(2-Methoxy-ethyl)-2-methyl-5-[2-(6-methyl-pyridin-3-yl)-thiazol--4-yl]-lH-pyrrole-3-
carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide

The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 465 (M+H)+.

Example 217
5-[2-(2-Ethyl-pyridin-4-yl)-to^
carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide

The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as RlR2NH> 3-furylmethylamine as R3-(CH2)nrNH2 and 2-ethyi-4-pyridine carbothiamide as
R4C(S)NH2, MS(ES+) 501 (M+H)+.
Example 218
5-[2-(2-Ethyl-pyridin-4-yI)-thiazol-4-yl]-l-(4-methoxy-benzyl)-2-methyl-lH-pyrrole-3-
carboxylic acid (2-cyclohex-l-enyl-ethyl)-amide

The title compound was obtained using 2-cyclohex-l-enyl-ethylamine as R R"NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as
R4C(S)NH2, MS(ES+) 54-1 (M+H)+.

Example 221
rac-l-Butyl-5-[2-(4-methoxy-phenyl)-thia2ol-4-yl]-2-methyl"lH-pyrrole-3-carboxylic
acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH, butylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 482 (M+H)+.
Example 222
mc-l-Butyl-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-lH-pyrrQle-3-
carboxylic acid (2-ethyl-hexyl)-amide

1 "5 ^
The title compound was obtained using 2-ethyl-hexylamine as R R NH, butylamine as R -(CH2)ra-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 512 (M+H)+.

Example 223
rac-l-Butyl-5-[2-(2-ethyl-pyri
acid (2-ethyl-hexyl)-amide

The tide compound was obtained using 2-ethyl-hexylamine as R R NH> butylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2> MS(ES+) 481 (M+H)+.
Example 224
rac-4-[l-Butyl-4-(2-ethyl-hexylcarbamoyl)-5-methyl-lH-pyrrol-2-yl]-thiazole-2-
carboxylic acid ethyl ester

1 9 ^
The title compound was obtained using 2-ethyl-hexylamine as R R NH, butylamine as R -(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2, MS(ES+) 448
(M+H)+.

Example 229
' mc-l-Isobutyl-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxylic acid (2-
ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH, isobutylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 454 (M+H)+.
Example 230
rac-5-[2-(4-Methoxy-phenoxymethyl)-thiazol-4-yl]-l-[2-(4-methoxy-phenyl)-ethyl]-2-methyl-lH-pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH, 2-(l-cyclohexenyl)ethylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2> MS(ES+) 590 (M+H)+.

Example 231
rac-5-j2-(2-Ethyl-pyrid^
lH-pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH> 2-(l-cyclohexenyl)ethylamine as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 559 (M+H)+.
Example 232
rac-5-[2-(2-CUoro-phenyl)-tiiiazol-4-yl]-l-cyclohexylmethyl-2-methyl-lH-pyrrole-3-
carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH> aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as
R4C(S)NH2, MS(ES+) 526 (M+H)+.

Example 233
rac-1 - Cyclohexylmeth^
carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R^NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 522 (M+H)+.
Example 234
rac-l-Cyclohexylmethyl-5-[2-(2-ethyl-pyrid^
carboxylic acid (2-ethyl-hexyl)-amide

l ^
The title compound was obtained using 2-ethyl-hexylamine as R R NH, aminomethylcyclohexane as R3-(CH2)nrNH2 and 2-ethyl-4-pyridine carbothiamide as
R4C(S)NH2, MS(ES+) 521 (M+H)+.

Example 235
ra.c-4- [ l-Cyclohexylmethyl-4-(2-ethyl-hexylcarbamoyl)-5-methyl- lH-pyrrol-2-yl] -
thiazole-2-carboxylic acid ethyl ester

The title compound was obtained using 2-ethyl-hexylamine as R R NH, aminomethylcyclohexane asR -(CH2)m-NH2 and ethylthiooxamate as R C(S)NH2-> MS(ES+) 488 (M+H)+.
Example 236
rac-l-Cyclohexylmethyl-2-methyl-5-[2-(6-methyl-pyridin-3-yl)-thiazol-4-yl]-lH-pyrrole-
3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R]R2NH, aminomethylcyclohexane asR3-(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 507 (M+H)+.

Example 237
rac-1-Cyclohexylmet^
rii>
carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as
R4C(S)NH2) MS(ES+) 494 (M+H)+.
i Example 238
rac-5-[2-(2-Chloro-phenyl)-thiazol^ pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2,MS(ES+) 514 (M+H)+.

Example 239
rac-5-p-(4-Methoxy-phenyl)-thiazol-4-yl]-2-m^
lH-pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as RlR2NH> tetrahydrofurfurylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 510 (M+H)+.
Example 240
rac-5-[2-(4-Methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-l-(tetrahydro-furan«2«-ylmethyl)-lH-pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R1R2NH, tetrahydrofiirfurylamine as.R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES-h) 540 (M+H)

Example 243
rac-2-Methyl-5-[2-(6-me^
ylmethyl)-lH-pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyI-hexylamine as R R NH, tetrahydrofurfurylamine as R "*(CH2)m~NH2 and 6-methyI-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 495 (M-hH)Example 244
rac-2-Methyl-5-(2~pyrazin-2-yl-tM
pyrrole-3-carboxyiic acid (2-ethyl-hexyl)-amide

i i
The title compound was obtained using 2-ethyl-hexylamine as R R NH, tetrahydrofurfurylamine as.R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2, MS(ES+) 482 (M+H)+.

Example 245
rac- lT(2-Methoxy-ethyl)-5-[2-(4-meft
carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH, methoxyethylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2, MS(ES+) 484 (M+H)+.
Example 246
rac- l-(2-Methoxy-ethyl)-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-lH-
pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The tide compound was obtained using 2-ethyl-hexylamine as R1R2NH, methoxyethylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2 MS(ES+) 514 (M+H)+.

Example 247
rac-l-(2-Methoxy-ethyl)-2-m^
pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as RlR2NH, methoxyethylamine as R -(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 469 (M+H)+.
Example 248
mc-l-(2-Methoxy-ethyl)-2-metliyl-5-(2-pyra2in-2-yl-thia2ol«4-yl)«lH-pyrrole-3-
carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R1R2NH methoxyethylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R C(S)NH2, MS(ES+) 456 (M+H)+.

Example 249
' rac-l.-j;2-Cyclohex-l-enyl-ethyl)-5-[2-(2-ethyl-pyridin-4-yl)-thiazol-4-yl]-2-methyl-lH-
pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH> 2-(l-cyclohexenyl)ethylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as
R4C(S)NH2) MS(ES+) 533 (M+H)+.
Example 250
rac-542-(2-Chloro-phenyl)-thiazol-4-yl]-l-furan-2-ylmethyl-2-methyl-lH-pyrrole-
carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R1R2NH, 3-fiirylmethylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2,
MS(ES+)510(M+H)+.

Example 253
rac-l-(4-Methoxy-benzyl)-2-methyl-5-(2-methyl-thiazol-4-yl)-lH
acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as RlR2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and thioacetamide as R4C(S)NH2, MS(ES+) 454 (M+H)+.
Example 254
rac-5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-(4-methoxy-benzyl)-2-methyl-lH-pyrrole-3-
carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as RlR2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 550 (M+H)+.

Example 255
mc-l-(4-Methoxy-benzyl)-5-^
3-carboxylic acid (2-ethyl-hexyl) -amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 546 (M+H)+.
Example 256
rac-l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phe^^
pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as
R4C(S)NH2, MS(ES-h) 576 (M+H)+.

Example 257
rac-5-[2-(2-Ethyl-pyridin-4^
pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R"NH, 4- t
methoxybenzylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as
R4C(S)NH2,MS(ES+) 545 (M+H)+.
Example 258
mc-l-(4-Methoxy-benzyl)-2-methyl-5-[2-(6-methyl-pyridin-3-yl)-thiazol-4-yl]-lH-
pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH, 4-methoxybenzylamine as R r(CH2)m-NH2 and 6-methyl-pyridine-3-carbothioamide as R4C(S)NH2, MS(ES+) 531 (M+H)+.

Example 259
rac-l-(4-Metho^-benzyl)-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-
carboxylic acid (2-ethyl-hexyl)-amide

i o
The title compound was obtained using 2-ethyl-hexylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R C(S)NH2> MS(ES+) 518 (M+H)+.
Example 260
rac-l-(3-Methoxy-propyl)-2-methyl-5-(2-methyl-thiazol-4-yl)-lH-pyrrole-3-carboxylic
acid (2~ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and thioacetamide as R4C(S)NH2, MS(ES+) 406 (M+H),+.

Example 261
rac-5-j2-(4-Methoxy-phenyl)-^
3-carboxylic acid (2-ethyl-hexyl)-amide

i 2
The title compound was obtained using 2-ethyl-hexylamine as R R NH, methoxyethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 498 (M+H)+.
Example 262
rac-5-[2-(4-Methoxy-phenoxymethyl)-thiazol-4-yl]-l-(3-methoxy-propyl)-2-methyl-lH-
pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as R R NH, methoxyethylamine as R -(CH2)m~NH2 and 2-(4-methoxyphenoxy)ethanethioamide as
R4C(S)NH2, MS(ES-h) 528 (M+H)+.

Example 263
rac-4-[4-(2-Ethyl-hexylcaA
thiazole-2-carboxylic acid ethyl ester

The title compound was obtained using 2-ethyl-hexylamine as RR"NH, methoxyethyl-amine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2, MS(ES+) 564 (M+H)+.
Example 264
rac-l-(3-Methoxy-propyl)-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrok-3-
carboxylic acid (2-ethyl-hexyl)-amide

1 *5
The title compound was obtained using 2-ethyl-hexylamine as R R NH, methoxyethylamine as R -(CH2)m-NH2 and pyrazine-2-carbothioamide as R C(S)NH2, MS(ES+) 470 (M+H)+.

Example 267
rac-5-[2-(4-Methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-l-thioph
pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

The title compound was obtained using 2-ethyl-hexylamine as RlR2NH, 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 552 (M+H)Example 268
rac-5-[2-(2-Ethyl-pyridin-4-yl)-^
pyrrole-3-carboxylic acid (2-ethyl-hexyl)-amide

to
The title compound was obtained using 2-ethyl-hexylamine as R R NH, 3-(aminomethyl)thiophene as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as
R4C(S)NH2, MS(ES+) 521 (M+H)+.

Example 273
l-Is9,butyl-2-methyl-5-(2-pyrazm
methoxy-propyl)-amide

The tide compound was obtained using methoxypropylamine as R R NH, isobutylamine as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as R4C(S)NH2> MS(ES+) 414 (M+H)+.
Example 274
5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-cyclohexylmethyl-2-methyl-lH-pyrrok-3-
carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R^NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R4C(S)NH2, MS(ES+) 486 (M+H)+.

Example 275
l-Cyclohexylmethyl-5-[2-(4-methoxy-pheny^
carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R*R2NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as
R4C(S)NH2, MS(ES+) 482 (M+H)+.
Example 276
l-Cyclohexylmethyl-5-[2-(4:methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide

i *) The title compound was obtained using methoxypropylamine as R R NH,
aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide
as R4C(S)NH2, MS(ES+) 512 (M+H)+.

Example 277
1-Cyplohexylmethyl^
carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m*NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 481 (M+H)+.
Example 278
l-Cyclohexylmethyl-2-methyl-5--(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxylic
acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and pyrazine-2-carbothioamide as
. R4C(S)NH2, MS(ES+) 454 (M+H)+.

Example 279
5~[2-^4-Metho:xy-phenyl)-thiaz
pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as RR NH, tetrahydrofurfurylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 470 (M+H)+.
Example 280
5-[2-(4-Methoxy-phenoxymethyl)^
ylmethyl)-lH-pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R R NH, tetrahydrofurfurylamine as R -(CH2)m-NH2 and2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2, MS(ES+) 500 (M+H)+.

Example 281
H^Cydohex-l-enyl-^
pyrrole-3-carboxylic acid (3-methoxy~propyl)-amide

The title compound was obtained using methoxypropylamine as R R NH, 2-(l-cyclohexenyl)ethylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as
R4C(S)NH2, MS(ES+) 493 (M+H)+.
Example 282
5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-furan-2-ylmethyl-2-methyl-lH-pyrrole-3-
carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R R NH, 3-furylmethylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2,
MS(ES+) 470 (M+H)+.

l-Furan-2-ylmethyl-5-[2-(4-methoxy-ph^
carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R^NH, 3-furylmethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 466 (M+H)+.
Example 284
1-Furan-2-ylmethyl-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-1H-pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as RlR2NH, 3-furylmethylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2) MS(ES-h) 496 (M+H)+.

Example 285
l-(4-]^ethoxy-benzyl)-2-methy^
(3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and thioacetamide as R4C(S)NH2, MS(ES+) 414 (M+H)+.
Example 286
5-[2-(2-Chloro-phenyl)-thiazol-4-yl]-l-(4-methoxy-benzyl)-2-methyl-lH«pyrrole-3-
carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as R C(S)NH2> MS(ES*) 510 (M+H)+.

Example 287
l-(4-Metho;xy^
carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R1R2NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2. 506
Example 288
l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-metiiyl-lH-
pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and 2~(4-methoxyphenoxy)ethanethioamide as
R4C(S)]SfH2) MS(ES+) 536 (M+H)+.

Example 289
5^2-(|2-Ethyl-pyridin-4-yl)-&^^
carboxylic acid (3-rnethoxy«propyl)-amide

The title compound was obtained using methoxypropylamine as R R NH, 4-methoxybenzylamine as R -(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as R4C(S)NH2, MS(ES+) 289 (M+H)+.
Example 290
4-[l-(4-Methoxy-benzyl)-4-(3-methoxy-propylcarbamoyi)-5"methyl-lH-pyrrol-2-yl]-
thiazole-2-carboxylic acid ethyl ester

The title compound was obtained using methoxypropylamine as R R NH, 4-methoxybenzylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2., MS(ES+) 472 (M+H)+.

Example 293
5-[2;(2-CUoro-phenyl)-^
carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R R NH, 3-(aminomethyl)thiophene as R -(CH2)m-NH2 and 2-chloro-phenyl thioamide as
R4C(S)NH2) MS(ES+) 486 (M+H)+.
Example 294
5-[2-(4-Methoxy-phenyl)-thia2ol-4-yl]-2-me&^
carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R R NH, 3-(aminomethyl)thiophene as R -(CH2)nrNH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ES+) 482 (M+H)+.

Example 295
' 542-(2-Ethyl-pyridin-4-yl)-thiazol-4-yl]-2-methyl-l-thiophen-2-ylmethyl-lH-pyrrole-3-
carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as R R NH, 3-(aminomethyl)thiophene as R3-(CH2)m-NH2 and 2-ethyl-4-pyridine carbothiamide as
R4C(S)NH2> MS(ES+) 481 (M-fH)+.
Example 296
1- [2-(3>4-Dimethoxy-phenyl)-ethyl] -5- [2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid (3-methoxy-propyl)-amide

The title compound was obtained using methoxypropylamine as RlR2NH, homoveratrylamine as R -(CH2)m-NH2 and 2-(4-methoxyphenoxy)ethanethioamide as R4C(S)NH2> MS(ES+) 580 (M+H)+.

Example 297
4-[K[,2-(3,4-Dimethoxy-pte^
pyrrol-2-yl]-thiazole-2-carboxylic acid ethyl ester

The title compound was obtained using methoxypropylamine as R R NH, .
homoveratrylamine as R3-(CH2)m-NH2 and ethylthiooxamate as R4C(S)NH2, MS(ES+) 516 (M+H)+.
Example 298
l-Cyclohexylmethyl-5-[2-(4»methoxy-phenyl)-tWazol-4-yl]-2-methyl-lH-pyrrole-3-
carboxylic acid morpholin-4-ylamide

r
The title compound was obtained using 1-amino-morpholine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as
R4C(S)NH2, MS(ISP) 495.3 (M+H)+.

Example 299
l-Cyclohexylmethyl-5-[2-(4-methoxy-phen^
carboxylic acid piperidin-1-ylamide

The title compound was obtained using 1-amino-piperidine as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as
R4C(S)NH2, MS(ISP) 493.4 (M+H)+.
Example 300
l-(4-Chloro-phenyl)-5-[2-(4-methoxy-pheny^
carboxylic acid butylamide

The tide compound was obtained using butylamine as R R NH, 4-chloroaniline as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ISP) 480.3 (M+H)+.

Example 301
l-Cyclohexylmethyl-5-[2-(4-methoxy-pta
carboxylic acid (3,4-dimethoxy-phenyl)-amide

The title compound was obtained using 3,4-dimethoxy aniline as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ISP) 5463 (M+H)+.
Example 302
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-
carboxylic acid (2-nitro-phenyl)-amide

The title compound was obtained using 2-nitroaniline as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ISP) 531.3 (M+H)+.

Example 303
l-Cyclohexylmethyl-5-[2-(4-methoxy-pheny^
carboxylic acid (4-trifluoromethyl-phenyl)-amide

The title compound was obtained using 4-trifluoromethylaniline as RJR2NH5 aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as
R4C(S)NH2? MS(ISP) 554.3 (M+H)+.
Example 304
N'-{ l-Cyclohexylmethyl-5- [2-(4-methoxy-phenyl)-thiazol-4-yl] -2-methyl- lH-pyrrole-3-
carbonylj-hydrazinecarboxylic acid ethyl ester.

The title compound was obtained using ethyl carbazate as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as
R4C(S)NH2, MS(ISP) 497.4 (M+H)+.

Example 305
l-Cyclohexylmethyl-5-[2-(4-me
carboxylic acid (pyridin-2-ylmethyl)-amide

The title compound was obtained using 2-(aminomethyl)pyridine as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 501.3 (M+H)+.
Example 306
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-
carboxylic acid (4-chloro-phenyl)-amide

The title compound was obtained using 4-chloro-aniline as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 520.3 (M+H)+.

Example 313
l-(2-pyclohexyl-et^
carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, 2-cyclohexyl-ethylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ISP) 480.4 (M+H)+.
Example 314
l-(3,5-Dimethyl-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-
carboxylic acid butylamide

1 0
The title compound was obtained using butylamine as R R NH, 3,5-dimethylbenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 488.3 (M+H)+.

Example 319
' 5-[2-(4-Methoxy-phenyl)-tta^
3-carboxylic acid butylamide

The title compound was obtained using butylarnine as R R NH, 4-(2-aminoethyl)morpholine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2) MS(ISP) 483.3 (M+H)+.
Example 320
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazoi-4-yl]-2-methyMH-pyrrole-3-
carboxylic acid (4-methyl-thiazol-2-yl)-amide

The title compound was obtained using 2-amino-4-methylthiazole as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 507.3 (M+H)+.

Example 321
l-(3:Methoxy-benzyl)-5-[2-^
carboxylic acid butylamide

The title compound was obtained using butylamine as R!R2NH, 3-methoxybenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 490.3 (M+H)+.
Example 322
l-(3,5-Dichloro-benzyl)-5-[2-(4-methoxyTphenyl)-thiazol-4-yl]-2-methyl-lH-pyrxole-3-
carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, 3,5-dichloroaniline as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 528.2 (M+H)+,

Example 323
Mndan-2-yl-5-[2-(4-methoxy-phenyl)-th^^
acid butylamide

The title compound was obtained using butylamine as R^NH, 2-aminoindane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 486.4 (M+H)+.
Example 324
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-
carboxylic acid pyrimidin-2-ylamide

The title compound was obtained using 2-aminopyrimidine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2) MS(ISP) 488.3 (M+H)+.

Example 325
l-(3,4-Dihydroxy-benzyl)-5-[2-(4-m
3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, 3,4-dihydroxybenzylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 492.3 (M+H)+.
Example 326
5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-(3-piperidin-l-yl-propyl)-lH-pyrrole-
3-carboxylic acid butylamide

The title compound was obtained using butylamine as R^NH, 3-piperidino-propylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 495.4 (M+HX+,

Example 327
rac-l:Cyclohexylmethyl-5-[2-^^
carboxylic acid (5-hydroxy-2,2,6-trimethyl-cydohexylmethyl)-amide

The title compound was obtained using aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 564.4 (M+H)+.
Example 328
5-[2-(4-Metlioxy-phenyl)-thiazol-4-yl]»2-methyl-l-(3-trifluoromethoxy-benzyl)-lH-
pyrrole-3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, 3-(trifluoromethoxy)benzylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 544.4 (M+H)+.

Example 329
5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l-(4-trifluoromethoxy-benzyl)-lH-
pyrrole-3-carboxylic acid butylamide
The title compound was obtained using butylamine as R R NH, 4-(trifluoromethoxy)benzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 544.3 (M+H)+.
Example 330
5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-me
pyrrole-3-carboxylic acid butylamide
The title compound was obtained using butylamine as R R NH, (3-methyl-2-
T JL
thienyl)methylamine as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R C(S)NH2> MS(ISP,) 480.3 (M+H)+.

Example 345
l-Cy;clohexylmethyl-2-methyl-5-(2-m-tolyl-thiazol-4-yl)-lH-pyrrole-3-carb
butylamide

The title compound was obtained using butylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 3-methylphenyl thioamide as R4C(S)NH2, MS(ISP) 450.3 (M+H)+.
Example 346
l-Cyclohexylmethyl-2-methyl-5-(2'-me^
carboxylic acid butylamide

The title compound was obtained using butylamine as R^NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 2-methyl-l,3-thiazole-4-carbothioamide as R4C(S)NH2, MS(ISP) 457.3 (M+H)+.

Example 353
l-C^lohexylmethyl-5-[2-(2,4-dichloro-phenyl)-thiazol-4-yl]
carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, aminomethylcyclohexane as R3-(CH2)nrNH2 and 2,4-dichlorophenyl thioamide as R4C(S)NH2, MS(ISP) 504.2
(M+H)+.
Example 354
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-metiLyl-lH-pyrrole-3^
carboxylic acid pentylamide

The title compound was obtained using pentylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2,MS(ISP) 481.3 (M+H)+.

Example 357
1-GyclohexylmethyU^
carboxylic acid cyclopentylamide

The title compound was obtained using cyclopentylamine as RlR2NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as
R4C(S)NH2J MS(ISP) 478.3 (M+H)+.
Example 358
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-
carboxylic acid cyclopropylamide

The title compound was obtained using cyclopropylamine as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ISP) 450.3 (M+H)+.

Example 359
1 - Cy clohexylmethyl-5-^
carboxylic acid cyclobutylamide

The title compound was obtained using cyclobutylamine as R R NH, aminomethylcyclohexane as R -(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 464.3 (M+H)+.
Example 360
(trans) rac-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2"methyl--lH-pyrrole-3-carboxylic acid (2-hydroxy-cyclopentyl)-amide

The title compound was obtained using trans-2-aminocyclopentanol as R R NH, aminomethylcyclohexane as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 494.3 (M+H)+.

Example 361
l-(4;CMoro-benzyl)-5-[2-(4-^^
carboxylic acid butylamide

The title compound was obtained using butylamine as R!R"NH, 4-chloroaniline as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 494.2 (M+H)+.
Example 362
l-(3,4-DicUoro-benzyl)-5-[2-(4-methdxy-:phenyl)-thiazol-4-yl]--2-methyl-lH-pyrrole-3-
carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, 3,4-dichloroaniline as R -(CH2)nrNH2 and 4-methoxyphenyl thioamide as R4C(S)NH2) MS(ISP) 527.2 (M+H)+.

Example 365
5-[2;(4-Methoxy-phenyl)-tH
carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, 2-methylbenzylamine as R3-(CH2)nrNH2 and 4-methoxyphenyl thioamide as R4C(S)NH2> MS(ISP) 474.3 (M+H)+.
Example 366-
l-(3,4-Dimethoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-*
3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, 3,4-dimethoxybenzyl-amine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 520.4 (M+H)+.

Example 367
l-(3,4^Dimethyl-benz^
carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, 2,4-dimethoxybenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 520.3 (M+H)+.
Example 368
l-(3,5-Dimethoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-
3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, 3,5-methoxybenzylamine as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2, MS(ISP) 520.3 (M+H)+.

Example 377
rac-l-(5-Hydroxy-l>3,3-trimethyl-cycto^
yl]-2-methyMH-pyrrole-3-carboxylic acid butylamide

The title compound was obtained using butylamine as R R NH, S-aminomethyl-S^S-trimethyl-cyclohexanol as R3-(CH2)m-NH2 and 4-methoxyphenyl thioamide as R4C(S)NH2. MS(ISP) 524.4 (&+H)+.

Galenical Examples
Example A
Film coated tablets containing the following ingredients can be manufactured in a conventional manner:
Ingredients Per tablet
Kernel:
Compound of formula (I) 10,0 mg 200.0 mg
Macrocrystalline cellulose 23.5 mg 43.5 mg
Lactose hydrous 60.0 mg 70.0 mg
Povidone K30 12.5 mg 15.0 mg
Sodium starch glycolate 12.5 mg 17.0 mg
Magnesium stearate 1.5 mg 4.5 mg
(Kernel Weight) 120.0 mg 350.0 mg
Film Coat:
Hydroxypropyl methyl cellulose 3.5 mg 7.0 mg;'
Polyethylene glycol 6000 0.8 mg 1.6 mg
Talc 1.3 mg 2.6 mg
Iron oxyde (yellow) 0.8 mg 1.6 mg
Titan dioxide 0.8 mg 1.6 mg
The active ingredient is sieved and mixed with microcrystalline cellulose and the mixture is granulated with a solution of polyvinylpyrrolidone in water. The granulate is mixed with sodium starch glycolate and magesiurn stearate and compressed to yield kernels of 120 or 350 mg respectively. The kernels are lacquered with an aq. solution / suspension of the above mentioned film coat.

Example B
Capsules containing the following ingredients can be manufactured in a conventional manner:
• Ingredients Per capsule
Compound of formula (I) 25.0 mg
Lactose 150.0 mg
Maize starch 20.0 mg
Talc 5.0 mg
The components are sieved and mixed and filled into capsules of size 2.
Example C
Injection solutions can have the following composition:
Compound of formula (I) 3.0 mg
'Pi
Polyethylene glycol 400 150.0 mg
Acetic acid q.s. ad pH 5.0
Water for injection solutions ad 1.0 ml
The active ingredient is dissolved in a mixture of Polyethylene glycol 400 and water for injection (part). The pH is adjusted to 5.0 by addition of acetic acid. The volume is adjusted to 1.0 ml by addition of the residual amount of water. The solution is filtered, filled into vials using an appropriate overage and sterilized.

Claims k Compounds of formula (I)

wherein
R1 is hydrogen, or lower alkyl;
R is hydrogen, lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, lower alkoxycarbonylamino, -(CH2)m-R2a or -NHC(0)-R2a;
or R and R together with the nitrogen atom to which they are attached form a 5- or 6-membered, saturated heterocyclic ring optionally containing one or two further heteroatom(s) independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy;
R2a is cycloalkyl, optionally mono-, di-, tri- or tetra-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; cycloalkenyl, optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino, lower alkylamino; or phenyl, which may optionally be mono-, di-

or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower allcylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro;
IT is lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, di-phenyl-lower alkyl, or -(CH2VR3a;
R3a is cycloalkyl, which may'optiorially be fused to a phenyl ring; or cycloalkyl which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; cycloalkenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro;
R4 is lower alkyl, lower alkoxycarbonyl; cycloalkyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted,. independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino, lower alkylamino; phenoxy-lower alkyl, wherein the phenyl moiety may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by, hydroxy, lower alkyl, loWer.alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or two adjacent substituents of the said phenyl residue together are -O-(CH2)p-0- or -(CH2)2-0-;

R5 and R6 are each independently selected from hydrogen, lower alkyl, halogen or fluorinated methyl;
R is hydrogen, lower alkyl or halogen;
m is 0, 1,2 or 3;
nis0> 1,2,3 or"4;
p is 1, 2 or 3;
and pharmaceutical^ acceptable salts thereof.
2. Compounds according to claim 1, wherein R1 is hydrogen.
3. Compounds according to any of claims 1 or 2, wherein R2 is lower alkyl or a residue -(CH2)m-R2a or -NHq(0)-R2a.
4. Compounds according to claim 2, wherein R2a is a cycloalkyl residues with three to six carbon atoms, which may optionally be mono- or tetra-substituted, independently, by lower alkyl and/or hydroxy.
5. Compounds according to claim 2, wherein R2a is cyclohexenyi.
6. Compounds according to claim 2, wherein R2a is an unsubstituted 5-membered monovalent saturated heterocyclic ring containing one or two heteroatoms independently selected from nitrogen and oxygen.
7. Compounds according to claim 6, wherein R2a is piperidinyl, morpholino or tetrahydrofuranyl.
8. Compounds according to claim 2, wherein R2a is a 5- or 6-membered monovalent heterocyclic ring containing one or two heteroatoms independently selected from nitrogen and sulfur, said heteroaromatic ring bein optionally substituted by lower alkyl.
9. Compounds according to claim 8, wherein R2a is pyridinyl, pyrimidinyl, thiazolyl or isoxazolyl, optionally substituted by lower alkyl.

10. Compounds according to any of claims 1 to 9, wherein R a is a phenyl residue which is optionally mono- or di-substituted, independently, by lower alkoxy, halogen, halogenated lower alkyl, halogenated lower alkoxy or nitro.
11. Compounds according to any of claims 1 to 10, wherein m is 0 or 1.
f
12. Compounds according to claim 1, wherein R1 and R2 together with the nitrogen atom to which they are attached form a 5- or 6-membered, saturated heterocyclic ring optionally containing an oxygen atom in the ring.
13. Compounds according to claim 12, wherein R andR together with the nitrogen atom to which they are attached are unsubstituted pyrrolidinyl, piperidinyl or morpholino.
•a
14. Compounds according to any of claims 1 to 13, wherein R is a residue
-(CH2)n-R3a-
15. Compounds according to claim 14, wherein R3a is cycloalkyl fused to a phenyl ring.
16. Compounds according to claim 14, wherein R a is an unsubstituted cycloalkyl residue with five or six carbon atoms.
17. Compounds according to claim 14, wherein R a is a 5- or 6-memberd heterocyclic ring containing one or two heteroatoms independently selected from nitrogen and oxygen, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by lower alkyj.
18. Compounds according to claim 14, wherein R a is a 5- or 6-membered heteroaromatic ring containing one heteroatom selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-substituted by lower alkyl.
1§. Compounds according to claim 14, wherein R3a is phenyl optionally mono- or di-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, halogenated lower alkyl, halogenated lower alkoxy or nitro.
,20. Compounds according to any of claims 14 to 19, wherein n is 1 or 2.
21. • Compounds according to any of claims 1 to 20, wherein R4 is unsubstituted cyclohexyl.

22. Compounds according to any of claims 1 to 20, wherein R4 is a 5- or 6-
membered heteroaromatic ring containing one or two heteroatoms independently selected
' from nitrogen and sulfur, said heteroaromatic ring being optionally mono-substituted by lower alkyl.
23. Compounds according to any of claims 1 to 20, wherein R4 is phenyl mono- or di-substituted, independently, by'hydroxy, lower alkyl, lower alkoxy, halogen, halogenated lower alkyl, halogenated lower alkoxy or nitro.
24. Compounds according to any of claims 1 to 20, wherein two adjacent substituents of a phenyl residue R4 together are -0-(CH2) -O- or -(CH2)2-0-.
25. Compounds according to any of claims 1 to 24, selected from the group consisting of:
l-Cyclohexylmethyl-5- [2-(4-methoxy-phenyl)-thiazol-4-yl] -2-methyl- lH-pyrrole-3-c arboxylic acid butylamide,,
l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3 -carboxylic acid butylamide,
rac-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid sec-butylamide,
rac-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-IH-pyrr ole-3-carboxylic acid sec-butylamide,
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid isobutyl-amide,
l-Furan-2-ylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid isobutyl-amide,
l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2"methyl-lH-pyrrole,-3 -carboxylic acid isobutyl-amide,
l-CycIohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid allylamide,
'■ i.l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid cyclohexylmethyl-amide,
l-Cyclohex)rlmethyl-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxy lie acid cyclohexylmethyl-amide,

and pharmaceutical acceptable salts thereof.
26. A process for the manufacture of compounds of formula (I) as defined in any of
claims 1 to 25, which process comprises reaction of an enamine of formula A:

wherein R1 , R 2 R 3, R5and m are as defined claim 1; with an alfa-bromoketone of formula B:

AC "J
wherein R , R and R are as defined claim 1.
27. Compounds according to any of claims 1 to 25 when manufactured by a process according to claim 26.
28. Pharmaceutical compositions comprising a compound according to any of claims 1 to 25 and a pharmaceutically acceptable carrier and/or adjuvant.
29. Compounds according to any of claims 1 to 25 for use as therapeutic active substances.
30. Compounds according to any of claims 1 to 25 for use as therapeutic active substances for the treatment and/or prophylaxis of diseases which are associated with modulation of the CB1 receptor.
31. A method for the treatment and/or prophylaxis of diseases which are associated with the modulation of the CBl receptors which method comprises administering a compound according to any of claims 1 to 25 to a human being or animal.
32. The use of compounds according to any of claims 1 to 25 for the treatment and/or prophylaxis of diseases which are associated with the modulation of CBl receptors.

33. The use of compounds according to any of claims 1 to 25 for the preparation of medicaments for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.

or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower allcylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro;
IT is lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, di-phenyl-lower alkyl, or -(CH2VR3a;
R3a is cycloalkyl, which may'optiorially be fused to a phenyl ring; or cycloalkyl which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; cycloalkenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent saturated heterocyclic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, amino, lower alkylamino, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino or lower alkylamino; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro;
R4 is lower alkyl, lower alkoxycarbonyl; cycloalkyl, which may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, fluorinated lower alkyl or fluorinated lower alkoxy; a 5-or 6-membered monovalent heteroaromatic ring containing one to three heteroatoms independently selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-, di- or tri-substituted,. independently, by hydroxy, lower alkyl, lower alkoxy, halogen, amino, lower alkylamino; phenoxy-lower alkyl, wherein the phenyl moiety may optionally be mono-, di- or tri-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or phenyl, which may optionally be mono-, di- or tri-substituted, independently, by, hydroxy, lower alkyl, loWer.alkoxy, halogen, lower alkylamino, halogenated lower alkyl, halogenated lower alkoxy or nitro; or two adjacent substituents of the said phenyl residue together are -O-(CH2)p-0- or -(CH2)2-0-;

Compounds according to any of claims 1 to 9, wherein R a is a phenyl residue which is optionally mono- or di-substituted, independently, by lower alkoxy, halogen, halogenated lower alkyl, halogenated lower alkoxy or nitro.
11. Compounds according to any of claims 1 to 10, wherein m is 0 or 1.
f
12. Compounds according to claim 1, wherein R1 and R2 together with the nitrogen atom to which they are attached form a 5- or 6-membered, saturated heterocyclic ring optionally containing an oxygen atom in the ring.
13. Compounds according to claim 12, wherein R andR together with the nitrogen atom to which they are attached are unsubstituted pyrrolidinyl, piperidinyl or morpholino.
•a
14. Compounds according to any of claims 1 to 13, wherein R is a residue
-(CH2)n-R3a-
15. Compounds according to claim 14, wherein R3a is cycloalkyl fused to a phenyl ring.
16. Compounds according to claim 14, wherein R a is an unsubstituted cycloalkyl residue with five or six carbon atoms.
17. Compounds according to claim 14, wherein R a is a 5- or 6-memberd heterocyclic ring containing one or two heteroatoms independently selected from nitrogen and oxygen, said heterocyclic ring being optionally mono-, di- or tri-substituted, independently, by lower alkyj.
18. Compounds according to claim 14, wherein R a is a 5- or 6-membered heteroaromatic ring containing one heteroatom selected from nitrogen, oxygen and sulfur, said heteroaromatic ring being optionally mono-substituted by lower alkyl.
1§. Compounds according to claim 14, wherein R3a is phenyl optionally mono- or di-substituted, independently, by hydroxy, lower alkyl, lower alkoxy, halogen, halogenated lower alkyl, halogenated lower alkoxy or nitro.
,20. Compounds according to any of claims 14 to 19, wherein n is 1 or 2.
21. • Compounds according to any of claims 1 to 20, wherein R4 is unsubstituted cyclohexyl.

22. Compounds according to any of claims 1 to 20, wherein R4 is a 5- or 6-
membered heteroaromatic ring containing one or two heteroatoms independently selected
' from nitrogen and sulfur, said heteroaromatic ring being optionally mono-substituted by lower alkyl.
23. Compounds according to any of claims 1 to 20, wherein R4 is phenyl mono- or di-substituted, independently, by'hydroxy, lower alkyl, lower alkoxy, halogen, halogenated lower alkyl, halogenated lower alkoxy or nitro.
24. Compounds according to any of claims 1 to 20, wherein two adjacent substituents of a phenyl residue R4 together are -0-(CH2) -O- or -(CH2)2-0-.
25. Compounds according to any of claims 1 to 24, selected from the group consisting of:
l-Cyclohexylmethyl-5- [2-(4-methoxy-phenyl)-thiazol-4-yl] -2-methyl- lH-pyrrole-3-c arboxylic acid butylamide,,
l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3 -carboxylic acid butylamide,
rac-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid sec-butylamide,
rac-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenoxymethyl)-thiazol-4-yl]-2-methyl-IH-pyrr ole-3-carboxylic acid sec-butylamide,
l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid isobutyl-amide,
l-Furan-2-ylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid isobutyl-amide,
l-(4-Methoxy-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2"methyl-lH-pyrrole,-3 -carboxylic acid isobutyl-amide,
l-CycIohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid allylamide,
'■ i.l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-c arboxylic acid cyclohexylmethyl-amide,
l-Cyclohex)rlmethyl-2-methyl-5-(2-pyrazin-2-yl-thiazol-4-yl)-lH-pyrrole-3-carboxy lie acid cyclohexylmethyl-amide,

l-(4-Metho;^-benzyl)-5-[2-(4-m^ pyrrole-3 -carboxylic acid cyclohexylmethyl-amide,
'5'-[2-(4-Methoxy-phenoxymethyl)-thiazol^^ lH-py rrole-3-carboxylic acid cydohexylmethyl-amide,
4-[l-[2-(3)4-Dimethoxy-ph:enyl)-ethyl]-4-(3-methoxy-propylcarb 1H-pyrrol-2-yl]-thiazole-2-carboxylic acid ethyl ester,
l-Cyclohexylmethyl-5-[2-(4-me^^ 3-carboxylic acid piperidin-1-ylamide,
N'-{l-Cyclohexylmethyl«5-[2-(4-methoxy-phenyI)-thiazol-4-yI]-2-me^ pyrrole-3-carbonyi}-hydrazinecarboxylic acid ethyl ester,
r«c-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid sec-butylamide,
{l-Cyclohexylmethyl-5-'[2-(4-^ 3-yl}-piperidin-l-yl-methanone,
l-CyclohexyImethyl-5-[2-(4-methoxy-phenyl)-thiazoI-4-yl]-2-methyl-lH-pyrroIe-3-carboxylic acid phenylamide,
l-Cyclohexylmethyl-5-[2-(4-methoxy~pheny^ 3-carboxylic acid pyrimidin-2-ylamide,
mc-l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-niethyl-lH-pyrrole-3-carboxylicacid(5-hydroxy-2,2>6-trimethyl-cyclohexylmethyl)-amideJ
5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-^^ lH-pyrrole-3-carboxylic acid butylamide,
l-Benzyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole--3-carboxylic acid butylamide,
{l-Cyclohexylmethyl-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyMH-pyrrol-3-yl}-pyrrolidin-l-yl-methanone,
l-Cyclohexylmethyl-5-[2-(3,4-dimethoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyirole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-5-[2-(3-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole' 3-carboxylic acid butylamide,

5-(2-Benzo[l>3]dioxol-5-yl-thiaz^ 3-carboxylic acid butylamide,
l-Cydohexylmethyl-5-[2-(4-fluo^^ carboxylic acid butylamide,
l-Cydohexylmethyl-5-[2-(2-fluoro^
carboxylic acid butylamide,
l-Cyclohexylmethyl-2-methyl-5-[2-(4-trifluoromethoxy-phenyl)-thiazol-4-yl]-lH pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-5-[2-(3,5-dimethoxy-phenyl)-thiazol-4"yl]-2-methyl-lH*-pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-2-methyl-5-(2-m-tolyl-thiazol--4-yl)-lH-pyrrole-3-carboxylic acid butylamide,
l-Cydohexylmethyl-2-methyl-5-(2'-met^ carboxylic acid butylamide,
l-Cyclohexylmethyl-5-[2-(4-ethyl-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide,
5-[2-(4-Chloro-phenyl)-thiazol-4-yl]-l-cyclohexylmethyl-2-methyl-lH-pyrrole-3-carboxylic acid butylamide,
5-[2-(4-tert-Butyl-phenyl)-thiazol-4-yl]-l-cyclohexylmethyl-2-methyl-lH-pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-542-(2,3-dihydro-benzofo lH-pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-2-methyl-5-(2"p-tolyl-thiazol-4-yl)-lH-pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-5-[2-(6-methoxy-pyridin-3-yl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-5-[2-(2,4-dichloro-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-2-methyl-5-[2-(4-nitro-phenyl)-thiazol-4-yl]-lH-pyrrole-3-carboxylic acid butylamide,

1-Cyclohexylmethy^ 3-carboxylic acid pentylamide,
l-Cyclohexylmethyl-5-[2-(4-methoxy-pheny^ 3-carboxylic acid propylamide,
l-Cydohexylmethyl-542-(4-methoxy-phenyl)^ 3-carboxylic acid cyclohexylamide,
l-Cyclohexylmethyl-5-[2-(4~methoxy-phenylH 3-carboxylic acid cyclopentylamide,
l-Cyclohexylmethyl-5-[2-(4-methoxy^ 3-carboxylic acid cyclopropylamide,
l~Cyclohexylmethyl-5-[2-(4-methox^^ 3-carboxylic acid cyclobutylamide,
{trans) rac-l-Cyclohexylmethyl-5-[2-(^ lH-pyrrole-3-carboxylic acid (2-hydroxy-cyclopentyl)-amide,
l-(4-Chloro-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide,
l-(3,4-Dichloro-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]"2-methyl-lH-pyrrole-3-carboxylic acid butylamide,
l~(3,4-Dimethyl4)enzyl)-542-(4-metho^ pyrrole-3-carboxylic acid butylamide,
l-(3,4-Dimethoxy-benzyl)-5-[2-(4-me&^ pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-5-[2-(4-hydroxy-phenyl)-thiazol-4-yl]-2-methyl-lH--pyrrole-3-carboxylic acid butylamide,
l-(4-Isopropyl-benzyl)-5-[2-(4-methoxy-phenyl)-thiazol-4-yl]-2-methyl-lH-pyrrole-3-carboxylic acid butylamide,
5-[2-(4-Methoxy-phenyl)-thiazol-4-yl]-2-methyl-l--pyridin-2--ylmethyl-lH-pyrrole-3-carboxylic acid butylamide,
l-Cyclohexylmethyl-5-(2-cyclohexyl-thiazol-4-yl)-2--methyl-lH-pyrrole-3-carboxylic acid butylamide,

and pharmaceutical acceptable salts thereof.
26. A process for the manufacture of compounds of formula (I) as defined in any of
claims 1 to 25, which process comprises reaction of an enamine of formula A:

wherein R , R > R , R and m are as defined claim 1; with an alfa-bromoketone of formula B:

AC "J
wherein R , R and R are as defined claim 1.
27. Compounds according to any of claims 1 to 25 when manufactured by a process according to claim 26.
28. Pharmaceutical compositions comprising a compound according to any of claims 1 to 25 and a pharmaceutical^ acceptable carrier and/or adjuvant.
29. Compounds according to any of claims 1 to 25 for use as therapeutic active substances.
30. Compounds according to any of claims 1 to 25 for use as therapeutic active substances for the treatment and/or prophylaxis of diseases which are associated with modulation of the CB1 receptor.
31. A method for the treatment and/or prophylaxis of diseases which are associated with the modulation of the CBl receptors which method comprises administering a compound according to any of claims 1 to 25 to a human being or animal.
32. The use of compounds according to any of claims 1 to 25 for the treatment and/or prophylaxis of diseases which aTe associated with the modulation of CBl receptors.

33. The use of compounds according to any of claims 1 to 25 for the preparation of medicaments for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.

Documents:

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1466-chenp-2005 description (complete)-duplicate-1.pdf

1466-chenp-2005 description (complete)-duplicate-2.pdf

1466-chenp-2005 description (complete)-duplicate-3.pdf

1466-chenp-2005 description (complete)-duplicate.pdf

1466-chenp-2005-abstract.pdf

1466-chenp-2005-claims.pdf

1466-chenp-2005-correspondnece-others.pdf

1466-chenp-2005-correspondnece-po.pdf

1466-chenp-2005-description(complete).pdf

1466-chenp-2005-form 1.pdf

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1466-chenp-2005-form 5.pdf

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Patent Number

222328

Indian Patent Application Number

1466/CHENP/2005

PG Journal Number

47/2008

Publication Date

21-Nov-2008

Grant Date

05-Aug-2008

Date of Filing

30-Jun-2005

Name of Patentee

F. HOFFMANN-LA ROCHE AG

Applicant Address

124 GRENZACHERSTRASSE, CH-4070 BASEL,

Inventors:

#	Inventor's Name	Inventor's Address
1	GUBA, WOLFGANG	FRANKENSTRASSE 7, D-79379 MUELLHEIM,
2	HAAP, WOLFGANG	FRIDOLIN-ENGEL-STRASSE 51, D-79540 LOERRACH,
3	MARTY, HANS, PETER	MARKIRCHERSTRASSE 25, CH-4055 BASEL,
4	NARQUIZIAN, ROBERT	4 RUE DE MONTREUX, F-68300 ST.LOUIS,

PCT International Classification Number

C07D 417/04

PCT International Application Number

PCT/EP03/14721

PCT International Filing date

2003-12-22

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1	03000002.0	2003-01-02	EUROPEAN UNION