BACKGROUND OF THE INVENTION 0001 Neuropeptide Y is a 36 amino acid peptide that is widely distributed in the central and peripheral nervous systems. This peptide mediates a number of physiological effects through its various receptor subtypes. Studies in animals have shown that neuropeptide Y is a powerful stimulus of food intake, and it has been demonstrated that activation of neuropeptide Y Y5 receptors results in hyperphagia and decreased thermogenesis. 0002 Therefore compounds that antagonize neuropeptide Y at the Y5 receptor subtype represent an approach to the treatment of eating disorders such as obesity and hyperphagia. 0003 The current approach is aiming at medical intervention to induce weight loss or prevention of weight gain. This is achieved by interfering with appetite control, which is mediated by the Hypothalamus, an important brain region proven to control food intake. Herein, neuropeptide Y (NPY) has been proven to be one of the strongest central mediators of food intake in several animal species. Increased NPY levels result in profound food intake. Various receptors of neuropeptide Y (NPY) have been described to play a role in appetite control and weight gain. Interference with these receptors is likely to reduce appetite and consequently weight gain. Reduction and long-term maintenance of body weight can also have beneficial consequences on con associated risk factors such as arthritis, cardiovascular diseases, diabetes and renal failure.

SUMMARY OF THE INVENTION 0004 The invention provides compounds of formula I and pharmaceutically acceptable salts and esters thereof 2

0005 wherein 0006 R1 is aryl or heteroaryl; 0007 R2 is hydrogen, alkyl or cycloalkyl; 0008 R3 is hydrogen, alkyl or cycloalkyl; 0009 R4 is hydrogen, alkyl or cycloalkyl; 0010 R5 is alkyl, cycloalkyl, aryl, heteroaryl; 0011 R6 is hydrogen, alkyl or cycloalkyl; 0012 A is C(O); S(O)2; N(R6)C(O) or OC(O); 0013 n is 2 to 6; and 0014 m is zero to 2. 0015 The compounds of formula I and their pharmaceutically acceptable salts and esters are neuropeptide ligands, for example, neuropeptide receptor antagonists and in particular, they are selective neuropeptides Y Y5 receptor antagonists.

DETAILED DESCRIPTION OF THE INVENTION 0016 The present invention is concerned with novel thiazole derivatives useful as neuropeptide Y (NPY) receptor ligands, particularly neuropeptide Y (NPY) antagonists. 0017 The invention provides compounds of formula I and pharmaceutically acceptable salts and esters thereof 3

0018 wherein 0019 R1 is aryl or heteroaryl; 0020 R2 is hydrogen, alkyl or cycloalkyl; 0021 R3 is hydrogen, alkyl or cycloalkyl; 0022 R4 is hydrogen, alkyl or cycloalkyl; 0023 R5 is alkyl, cycloalkyl, aryl, heteroaryl; 0024 R6 is hydrogen, alkyl or cycloalkyl; 0025 A is C(O); S(O)2; N(R6)C(O) or OC(O); 0026 n is 2 to 6; and 0027 m is zero to 2. 0028 The compounds of formula I and their pharmaceutically acceptable salts and esters are neuropeptide ligands, for example, neuropeptide receptor antagonists and in particular, they are selective neuropeptides Y Y5 receptor antagonists. 0029 The compounds of formula I, their salts and esters can be used in the prophylaxis or treatment of arthritis, cardiovascular diseases, diabetes, renal failure and particularly eating disorders and obesity. 0030 Objects of the present invention are the compounds of formula I and their aforementioned salts and esters per se and their use as therapeutically active substances, a process for the manufacture of the said compounds, intermediates, pharmaceutical compositions, medicaments comprising the said compounds, their pharmaceutically acceptable salts and esters, the use of the said compounds, salts and esters for the prophylaxis and/or therapy of illnesses, especially in the treatment or prophylaxis of arthritis, cardiovascular diseases, diabetes, renal failure and particularly eating disorders such as hyperphagia and particularly obesity, and the use of the said compounds, salts and esters for the production of medicaments for the treatment or prophylaxis of arthritis, cardiovascular diseases, diabetes, renal failure and particularly eating disorders and obesity. 0031 In the present description the term alkyl, alone or in combination, signifies a straight-chain or branched-chain alkyl group with 1 to 8 carbon atoms, preferably a straight or branched-chain alkyl group with 1 to 6 carbon atoms and particularly preferred a straight or branched-chain alkyl group with 1 to 4 carbon atoms. Examples of straight-chain and branched C1-C8 alkyl groups are methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert.-butyl, the isomeric pentyls, the isomeric hexyls, the isomeric heptyls and the isomeric octyls, preferably methyl and ethyl, and most preferred methyl. 0032 The term cycloalkyl, alone or in combination, signifies a cycloalkyl ring with 3 to 8 carbon atoms and preferably a cycloalkyl ring with 3 to 6 carbon atoms. Examples of C3-C8 cycloalkyl are cyclopropyl, methyl-cyclopropyl, dimethylcyclopropyl, cyclobutyl, methyl-cyclobutyl, cyclopentyl, methyl-cyclopentyl, cyclohexyl, methyl-cyclohexyl, dimethyl-cyclohexyl, cycloheptyl and cyclooctyl, preferably cyclopropyl and cyclopentyl. 0033 The term alkoxy, alone or in combination, signifies a group of the formula alkyl-O in which the term alkyl has the previously given significance, such as methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec. butoxy and tert.butoxy, 2-hydroxyethoxy, 2-methoxyethoxy, preferably methoxy and ethoxy, and most preferred methoxy. 0034 The term aryl, alone or in combination, signifies a phenyl or naphthyl group, preferably a phenyl group which optionally carries one or more, preferably one to three substituents each independently selected from halogen, haloalkyl, amino, alkyl, alkoxy, aryloxy, alkylcarbonyl, cyano, carbamoyl, alkoxycarbamoyl, methylenedioxy, carboxy, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, hydroxy, nitro, and haloalkoxy. Preferred substituents of aryl, preferably phenyl, are independently selected from halogen, trifluoromethyl, alkyl, alkoxy and haloalkoxy. 0035 The term aralkyl, alone or in combination, signifies an alkyl or cycloalkyl group as previously defined, preferably an alkyl group in which one hydrogen atom has been replaced by an aryl group as previously defined. Preferred are benzyl, benzyl substituted with hydroxy, alkoxy or halogen, preferably fluorine. 0036 The term heteroaryl, alone or in combination, signifies an aromatic 5- or 6-membered ring comprising 1 to 3 atoms independently selected from nitrogen, oxygen or sulfur. Optionally, the heteroaryl ring can be substituted on one or more carbon atoms with at least one substituent selected from halogen, alkyl, alkoxy and cyano. Examples of heteroaryl rings include furyl, pyridyl, 1,2-, 1,3- and 1,4-diazinyl or pyrazinyl, thienyl, isoxazolyl, oxazolyl, thiazolyl and pyrrolyl. Preferred heteroaryl rings are pyridinyl, thiophenyl and pyrazinyl which are optionally substituted with alkyl. 0037 The term amino, alone or in combination, signifies a primary, secondary or tertiary amino group bonded via the nitrogen atom, with the secondary amino group carrying an alkyl or cycloalkyl substituent and the tertiary amino group carrying two similar or different alkyl or cycloalkyl substituents or the two nitrogen substituents together forming a ring, such as, for example, NH2, methylamino, ethylamino, dimethylamino, diethylamino, methyl-ethylamino, pyrrolidin-1-yl or piperidino etc., preferably amino, dimethylamino and diethylamino and particularly preferred primary amino. 0038 The term halogen, alone or in combination, signifies fluorine, chlorine, bromine or iodine and preferably fluorine, chlorine or bromine and particularly chlorine. 0039 The term haloalkyl, alone or in combination, signifies an alkyl group as previously defined, wherein one or several hydrogen atoms, preferably one to three hydrogen atoms have/has been replaced by halogen. Examples of haloalkyl groups are trifluoromethyl, pentafluoroethyl and trichloromethyl. Preferred examples are trifluoromethyl and difluoromethyl. Most preferred is trifluoromethyl. 0040 The term haloalkoxy, alone or in combination, signifies an alkoxy group as previously defined, wherein one or several hydrogen atoms, preferably one to three hydrogen atoms have/has been replaced by halogen. A preferred example is trifluoromethoxy. 0041 The term cyano, alone or in combination, signifies a CN group. 0042 The term nitro, alone or in combination, signifies a NO2 group. 0043 The term C(O) means a carbonyl group. 4

0044 The term S(O)2 means the following group: 5

0045 The term N(R6)C(O) means the following group: 6

0046 The term OC(O) means the following group: 7

0047 Examples of pharmaceutically acceptable salts of the compounds of formula I are salts with physiologically compatible mineral acids such hydrochloric acid, sulfuric acid or phosphoric acid; or with organic acids such as methanesulfonic acid, formic acid, acetic acid, trifluoroacetic acid, citric acid, fumaric acid, maleic acid, tartaric acid, succinic acid or salicylic acid. Preferred is oxalic acid. The compounds of formula I with free carboxy groups can also form salts with physiologically compatible bases. Examples of such salts are alkali metal, alkali earth metal, ammonium and alkylammonium salts such as the Na, K, Ca or tertramethylammonium salt. The compound of formula I can also be present in the form of zwitterions. 0048 The compounds of formula I can also be solvated, e.g. hydrated. The solvation can be effected in the course of the manufacturing process or can take place e.g. as a consequence of hygroscopic properties of an initially anhydrous compound of formula I (hydration). The term pharmaceutically acceptable salts also includes pharmaceutically acceptable solvates. 0049 The term pharmaceutically acceptable esters of the compounds of formula I means that compounds of general formula (I) may be derivatised at functional groups to provide derivatives which are capable of conversion back to the parent compounds in vivo. Examples of such compounds include physiologically acceptable and metabolically labile ester derivatives, such as methoxymethyl esters, methylthiomethyl esters and pivaloyloxymethyl esters. Additionally, any physiologically acceptable equivalents of the compounds of general formula (I), similar to the metabolically labile esters, which are capable of producing the parent compounds of general formula (I) in vivo, are within the scope of this invention. 0050 In more detail, for example, the COOH groups of compounds according to formula I can be esterified. The alkyl and aralkyl esters are examples of suitable esters. The methyl, ethyl, propyl, butyl and benzyl esters are preferred esters. The methyl and ethyl esters are especially preferred. Further examples of pharmaceutically usable esters are compounds of formula I, wherein the hydroxy groups can be esterified. Examples of such esters are formate, acetate, propionate, butyrate, isobutyrate, valerate, 2-methylbutyrate, isovalerate and N,N-dimethylaminoacetate. Preferred esters are acetate and N,N-dimethylaminoacetate. 0051 The term lipase inhibitor refers to compounds which are capable of inhibiting the action of lipases, for example gastric and pancreatic lipases. For example orlistat and lipstatin as described in U.S. Pat. No. 4,598,089 are potent inhibitor of lipases. Lipstatin is a natural product of microbial origin, and orlistat is the result of a hydrogenation of lipstatin. Other lipase inhibitors include a class of compound commonly referred to as panclicins. Panclicins are analogues of orlistat (Mutoh et al, 1994). The term lipase inhibitor refers also to polymer bound lipase inhibitors for example described in International Patent Application WO99/34786 (Geltex Pharmaceuticals Inc.). These polymers are characterized in that they have been substituted with one or more groups that inhibit lipases. The term lipase inhibitor also comprises pharmaceutically acceptable salts of these compounds. The term lipase inhibitor preferably refers to orlistat. 0052 Orlistat is a known compound useful for the control or prevention of obesity and hyperlipidemia. See, U.S. Pat. No. 4,598,089, issued Jul. 1, 1986, which also discloses processes for making orlistat and U.S. Pat. No. 6,004,996, which discloses appropriate pharmaceutical compositions. Further suitable pharmaceutical compositions are described for example in International Patent Applications WO 00/09122 and WO 00/09123. Additional processes for the preparation of orlistat are disclosed in European Patent Applications Publication Nos. 185,359, 189,577, 443,449, and 524,495. 0053 Orlistat is preferably orally administered from 60 to 720 mg per day in divided doses two to three times per day. Preferred is wherein from 180 to 360 mg, most preferably 360 mg per day of a lipase inhibitor is administered to a subject, preferably in divided doses two or, particularly, three times per day. The subject is preferably an obese or overweight human, i.e. a human with a body mass index of 25 or greater. Generally, it is preferred that the lipase inhibitor be administered within about one or two hours of ingestion of a meal containing fat. Generally, for administering a lipase inhibitor as defined above it is preferred that treatment be administered to a human who has a strong family history of obesity and has obtained a body mass index of 25 or greater. 0054 Orlistat can be administered to humans in conventional oral compositions, such as, tablets, coated tablets, hard and soft gelatin capsules, emulsions or suspensions. Examples of carriers which can be used for tablets, coated tablets, dragees and hard gelatin capsules are lactose, other sugars and sugar alcohols like sorbitol, mannitol, maltodextrin, or other fillers; surfactants like sodium lauryle sulfate, Brij 96, or Tween 80; disintegrants like sodium starch glycolate, maize starch or derivatives thereof; polymers like povidone, crospovidone; talc; stearic acid or its salts and the like. Suitable carriers for soft gelatin capsules are, for example, vegetable oils, waxes, fats, semi-solid and liquid polyols and the like. Moreover, the pharmaceutical preparations can contain preserving agents, solubilizers, stabilizing agents, wetting agents, emulsifying agents, sweetening agents, coloring agents, flavoring agents, salts for varying the osmotic pressure, buffers, coating agents and antioxidants. They can also contain still other therapeutically valuable substances. The formulations may conveniently be presented in unit dosage form and may be prepared by any methods known in the pharmaceutical art. Preferably, orlistat is administered according to the formulation shown in the Examples and in U.S. Pat. No. 6,004,996, respectively. 0055 The compounds of formula I can contain several asymmetric centers and can be present in the form of optically pure enantiomers, mixtures of enantiomers such as, for example, racemates, optically pure diastereoisomers, mixtures of diastereoisomers, diastereoisomeric racemates or mixtures of diastereoisomeric racemates. 0056 In the nomenclature used in the present application the ring atoms of the thiazole ring are numbered as follows: 8

0057 wherein R1 to R5, m, n and A are defined as before. In a preferred embodiment of the present invention R2 is attached to the 5-position and the substituent C(O)R1 is attached to the 4-position of the thiazole ring. Particularly preferred are the compounds of formula I, wherein the substituent C(O)R1 is attached to the 5-position and R2 is attached to the 4-position of the thiazole ring. 0058 Preferred are compounds of formula I, wherein R2 is hydrogen or alkyl. Particularly preferred are compounds of formula I, wherein R2 is hydrogen or methyl. Most preferred are compounds according to formula I, wherein R2 is hydrogen. 0059 A further preferred object of the present invention are compounds of formula I, wherein R3 is hydrogen or alkyl. Particularly preferred are those compounds of formula I, wherein R3 is hydrogen. 0060 Also a preferred object of the present invention are compounds of formula I, wherein R4 is hydrogen or alkyl. Particularly preferred are compounds according to formula I, wherein R4 is hydrogen. 0061 Another preferred object of the present invention are compounds of formula I, wherein R5 is alkyl, cycloalkyl, phenyl, phenyl substituted with one to three substituents independently selected from halogen, alkyl, alkoxy and haloalkyl, or R5 is thiophenyl or thiophenyl substituted with alkyl, or R5 is pyridinyl or pyridinyl substituted with alkyl or R is pyrazinyl or pyrazinyl substituted with alkyl. Particularly preferred are compounds according to formula I, wherein R5 is n-butyl, tert. butyl, cyclohexyl, thiophenyl, phenyl or phenyl substituted with one to three substituents independently selected from methyl, ethyl, methoxy, fluoro, chloro and trifluoromethyl. Further particularly preferred are compounds according to formula I, wherein R5 is thiophenyl or phenyl optionally substituted with one to three substituents independently selected from alkyl, alkoxy, halogen and haloalkyl. 0062 Preferred are compounds according to formula I, wherein R5 is thiophenyl or phenyl both optionally substituted with one to three substituents independently selected from alkyl, alkoxy, halogen, haloalkyl, haloalkoxy and nitro. 0063 A further preferred object of the present invention are compounds according to formula I, wherein R6 is hydrogen. 0064 Also preferred are compounds of formula I, wherein R1 is pyridinyl or pyridinyl substituted with alkyl, or R1 is thiophenyl or thiophenyl substituted with alkyl or R1 is phenyl or phenyl substituted with one to three substituents independently selected from alkyl, halogen, haloalkyl or R1 is pyrazinyl or pyrazinyl substituted with alkyl. Particularly preferred are compound according to formula I, wherein R1 is pyridinyl, phenyl or phenyl substituted with one to three substituents independently selected from alkyl, alkoxy, halogen and haloalkyl. Very preferred are compounds of formula I, wherein R1 is pyridinyl or phenyl substituted with one to three substituents independently selected from alkyl, alkoxy, halogen and haloalkyl. 0065 A further particularly preferred object of the present invention are compounds according to formula I, wherein A is S(O)2. 0066 Another preferred embodiment of the present invention are compounds of formula I, wherein A is C(O). 0067 Further preferred are compounds of formula I, wherein A is N(R6)C(O). 0068 Also preferred are compounds of formula I, wherein A is OC(O). 0069 Likewise preferred are compounds of formula I, wherein n is 3 to 5. Particularly preferred are compounds of formula I, wherein n is 3. Further particularly preferred are compounds of formula I, wherein n is 5. 0070 Preferred compounds of formula I are those, wherein m is zero or 1. Particularly preferred are those compounds of formula I, wherein m is zero. A further very preferred embodiment of this invention are compounds of formula I, wherein A is S(O)2 and m is zero. 0071 Examples of preferred compounds of formula I are: 0072 1. 2-Fluoro-N-3-5-(pyridine-2-carbonyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0073 2. 2-Methoxy-5-methyl-N-3-5-(pyridine-2-carbonyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0074 3. 2-Methoxy-5-methyl-N-3-5-(pyridine-3-carbonyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0075 4. 2-Methoxy-5-methyl-N-3-5-(pyridine-4-carbonyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0076 5. 2-Fluoro-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0077 6. 4-Methoxy-N-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-benzenesulfonamide 0078 7. Thiophene-2-sulfonic acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0079 8. 2-Methoxy-5-methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0080 9. 4-Fluoro-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0081 10. 2-Methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0082 11. 3-Fluoro-N-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-benzenesulfonamide 0083 12. 2-Chloro-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-5-trifluoromethyl-benzenesulfonamide 0084 13. N-3-5-(2-Methyl-benzoyl) -thiazol-2-ylamino-propyl-benzenesulfonamide 0085 14. 3-Methoxy-N-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-benzenesulfonamide 0086 15. N-3-5-(2-Chloro-benzoyl) -thiazol-2-ylamino-propyl-2-fluoro-benzenesulfonamide 0087 16. N-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-4-methoxy-benzenesulfonamide 0088 17. Thiophene-2-sulfonic acid 3-5-(2-chloro-benzoyl)-thiazol-2-ylamino-propyl-amide 0089 18. N-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-2-methoxy-5-methyl-benzenesulfonamide 0090 19. N-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-4-fluoro-benzenesulfonamide 0091 20. N-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-2-methyl-benzenesulfonamide 0092 21. N-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-3-fluoro-benzenesulfonamide 0093 22. 2-Chloro-N-3-5-(2-chloro-benzoyl)-thiazol-2-ylamino-propyl-5-trifluoromethyl-benzenesulfonamide 0094 23. N-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0095 24. N-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-3-methoxy-benzenesulfonamide 0096 25. 3-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester 0097 26. 3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester 0098 27. 3-5-(2-Ethyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester 0099 28. 3-5-(2-Trifluoromethyl-benzoyl) -thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester 0100 29. Cyclohexanecarboxylic acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0101 30. Cyclohexanecarboxylic acid 3-5-(2-ethyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0102 31. Pentanoic acid 3-(5-benzoyl-thiazol-2-ylamino)-propyl-amide 0103 32. Pentanoic acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0104 33. Pentanoic acid 3-5-(2-ethyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0105 34. Pentanoic acid 3-5-(2-fluoro-benzoyl)-thiazol-2-ylamino-propyl-amide 0106 35. Pentanoic acid 3-5-(2-chloro-benzoyl)-thiazol-2-ylamino-propyl-amide 0107 36. N-3-(5-Benzoyl-thiazol-2-ylamino)-propyl-2-(4-chloro-phenyl)-acetamide 0108 37. 2-(4-Chloro-phenyl)-N-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-acetamide 0109 38. 2-(4-Chloro-phenyl)-N-3-5-(2-ethyl-benzoyl)-thiazol-2-ylamino-propyl-acetamide 0110 39. Thiophene-2-carboxylic acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0111 40. Thiophene-2-carboxylic acid 3-5-(2-ethyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0112 41. Thiophene-2-carboxylic acid 3-5-(2-fluoro-benzoyl)-thiazol-2-ylamino-propyl-amide 0113 42. Thiophene-2-carboxylic acid 3-5-(2-chloro-benzoyl)-thiazol-2-ylamino-propyl-amide 0114 43. N-3-5-(2-Ethyl-benzoyl)-thiazol-2-ylamino-propyl-2-fluoro-benzamide 0115 44. N-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-2-fluoro-benzamide 0116 45. 3-Fluoro-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0117 46. N-3-5-(2-Ethyl-benzoyl)-thiazol-2-ylamino-propyl-3-fluoro-benzamide 0118 47. 3-Fluoro-N-3-5-(2-fluoro-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0119 48. N-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-3-fluoro-benzamide 0120 49. 4-Fluoro-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0121 50. N-3-5-(2-Ethyl-benzoyl)-thiazol-2-ylamino-propyl-4-fluoro-benzamide 0122 51. N-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-4-fluoro-benzamide 0123 52. N-3-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0124 53. N-3-5-(2-Ethyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0125 54. N-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0126 55. N-3-5-(2-Ethyl-benzoyl)-thiazol-2-ylamino-propyl-4-methoxy-benzamide 0127 56. N-3-(5-Benzoyl-thiazol-2-ylamino)-propyl-2-methoxy-benzamide 0128 57. N-3-5-(2-Ethyl-benzoyl) -thiazol-2-ylamino-propyl-2-methoxy-benzamide 0129 58. 4-Chloro-N-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-benzamide 0130 59. 4-Chloro-N-3-5-(2-ethyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0131 60. Cyclohexanecarboxylic acid 3-5-(2-trifluoromethyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0132 61. Cyclohexanecarboxylic acid 3-5-(4-methyl-pyridine-3-carbonyl)-thiazol-2-ylamino-propyl-amide 0133 62. Pentanoic acid 3-5-(2-trifluoromethyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0134 63. Pentanoic acid 3-5-(4-methyl-pyridine-3-carbonyl)-thiazol-2-ylamino-propyl-amide 0135 64. Pentanoic acid 3-5-(2-methyl-pyridine-3-carbonyl)-thiazol-2-ylamino-propyl-amide 0136 65. Pentanoic acid 3-5-(3-methyl-thiophene-2-carbonyl)-thiazol-2-ylamino-propyl-amide 0137 66. 2-(4-Chloro-phenyl)-N-3-5-(2-trifluoromethyl-benzoyl)-thiazol-2-ylamino-propyl-acetamide 0138 67. 2-(4-Chloro-phenyl)-N-3-5-(3-methyl-pyridine-2-carbonyl)-thiazol-2-ylamino-propyl-acetamide 0139 68. 2-(4-Chloro-phenyl)-N-3-5-(3-methyl-pyrazine-2-carbonyl)-thiazol-2-ylamino-propyl-acetamide 0140 69. Thiophene-2-carboxylic acid 3-5-(2-trifluoromethyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0141 70. Thiophene-2-carboxylic acid 3-5-(3-methyl-pyridine-2-carbonyl)-thiazol-2-ylamino-propyl-amide 0142 71. 2-Fluoro-N-3-5-(2-trifluoromethyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0143 72. 2-Fluoro-N-3-5-(3-methyl-pyrazine-2-carbonyl)-thiazol-2-ylamino-propyl-benzamide 0144 73. 3-Fluoro-N-3-5-(2-trifluoromethyl-benzoyl) -thiazol-2-ylamino-propyl-benzamide 0145 74. 3-Fluoro-N-3-5-(4-methyl-pyridine-3-carbonyl)-thiazol-2-ylamino-propyl-benzamide 0146 75. 3-Fluoro-N-3-5-(3-methyl-pyridine-2-carbonyl)-thiazol-2-ylamino-propyl-benzamide 0147 76. 3-Fluoro-N-3-5-(3-methyl-pyrazine-2-carbonyl)-thiazol-2-ylamino-propyl-benzamide 0148 77. 4-Fluoro-N-3-5-(2-trifluoromethyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0149 78. 4-Fluoro-N-3-5-(4-methyl-pyridine-3-carbonyl)-thiazol-2-ylamino-propyl-benzamide 0150 79. 4-Fluoro-N-3-5-(3-methyl-pyridine-2-carbonyl)-thiazol-2-ylamino-propyl-benzamide 0151 80. 4-Fluoro-N-3-5-(3-methyl-thiophene-2-carbonyl)-thiazol-2-ylamino-propyl-benzamide 0152 81. N-3-5-(2-Trifluoromethyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0153 82. N-3-5-(4-Methyl-pyridine-3-carbonyl)-thiazol-2-ylamino-propyl-benzamide 0154 83. 4-Methoxy-N-3-5-(2-trifluoromethyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0155 84. 4-Methoxy-N-3-5-(4-methyl-pyridine-3-carbonyl)-thiazol-2-ylamino-propyl-benzamide 0156 85. 2-Methoxy-N-3-5-(2-trifluoromethyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0157 86. 4-Chloro-N-3-5-(2-trifluoromethyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0158 87. 4-Chloro-N-3-5-(4-methyl-pyridine-3-carbonyl) -thiazol-2-ylamino-propyl-benzamide 0159 88. 4-Chloro-N-3-5-(2-methyl-pyridine-3-carbonyl) -thiazol-2-ylamino-propyl-benzamide 0160 89. 1-3-(5-Benzoyl-thiazol-2-ylamino)-propyl-3-cyclohexyl-urea 0161 90. 1-Cyclohexyl-3-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-urea 0162 91. 1-Cyclohexyl-3-3-5-(2-ethyl-benzoyl)-thiazol-2-ylamino-propyl-urea 0163 92. 1-3-5-(2-Chloro-benzoyl) -thiazol-2-ylamino-propyl-3-cyclohexyl-urea 0164 93. 1-3-(5-Benzoyl-thiazol-2-ylamino)-propyl-3-butyl-urea 0165 94. 1-Butyl-3-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-urea 0166 95. 1-Butyl-3-3-5-(2-ethyl-benzoyl)-thiazol-2-ylamino-propyl-urea 0167 96. 1-Butyl-3-3-5-(2-fluoro-benzoyl)-thiazol-2-ylamino-propyl-urea 0168 97. 1-Butyl-3-3-5-(2-chloro-benzoyl)-thiazol-2-ylamino-propyl-urea 0169 98. 1-(2-Methoxy-phenyl)-3-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-urea 0170 99. 1-3-5-(2-Ethyl-benzoyl)-thiazol-2-ylamino-propyl-3-(2-methoxy-phenyl) -urea 0171 100. 1-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-3-(2-methoxy-phenyl)-urea 0172 101. 1-(2-Fluoro-phenyl)-3-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-urea 0173 102. 1-3-5-(2-Ethyl-benzoyl)-thiazol-2-ylamino-propyl-3-(2-fluoro-phenyl)-urea 0174 103. 1-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-3-(2-fluoro-phenyl)-urea 0175 104. 1-(3-Fluoro-phenyl)-3-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-urea 0176 105. 1-3-5-(2-Ethyl-benzoyl)-thiazol-2-ylamino-propyl-3-(3-fluoro-phenyl)-urea 0177 106. 1-(4-Fluoro-phenyl)-3-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-urea 0178 107. 1-3-5-(2-Ethyl-benzoyl)-thiazol-2-ylamino-propyl-3-(4-fluoro-phenyl)-urea 0179 108. 1-3-(5-Benzoyl-thiazol-2-ylamino)-propyl-3-(2-chloro-benzyl)-urea 0180 109. 1-(2-Chloro-benzyl)-3-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-urea 0181 110. 1-(2-Chloro-benzyl)-3-3-5-(2-ethyl-benzoyl)-thiazol-2-ylamino-propyl-urea 0182 111. 1-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-3-(2-chloro-benzyl)-urea 0183 112. 1-3-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-3-phenyl-urea 0184 113. 1-3-5-(2-Ethyl-benzoyl)-thiazol-2-ylamino-propyl-3-phenyl-urea 0185 114. 1-3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-3-phenyl-urea 0186 115. 1-Butyl-3-3-5-(4-methyl-pyridine-3-carbonyl)-thiazol-2-ylamino-propyl-urea 0187 116. 1-3-5-(4-Methyl-pyridine-3-carbonyl) -thiazol-2-ylamino-propyl-3-phenyl-urea 0188 117. 1-Cyclohexyl-3-3-5-(3-methyl-pyrazine-2-carbonyl)-thiazol-2-ylamino-propyl-urea 0189 118. 1-Cyclohexyl-3-3-5-(3-methyl-thiophene-2-carbonyl) -thiazol-2-ylamino-propyl-urea 0190 119. 4-Fluoro-N-3-5-(4-methyl-pyridine-3-carbonyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0191 120. 4-Fluoro-N-3-5-(3-methyl-thiophene-2-carbonyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0192 121. 2-Methoxy-5-methyl-N-3-5-(4-methyl-pyridine-3-carbonyl) -thiazol-2-ylamino-propyl-benzenesulfonamide 0193 122. 2-Methoxy-5-methyl-N-3-5-(3-methyl-pyrazine-2-carbonyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0194 123. 2-Methoxy-5-methyl-N-3-5-(3-methyl-thiophene-2-carbonyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0195 124. 1-(4-Methoxy-phenyl)-3-3-5-(4-methyl-pyridine-3-carbonyl) -thiazol-2-ylamino-propyl-urea 0196 125. 3-4-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester 0197 126. N-3-4-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0198 127. 2-Fluoro-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0199 128. 3,5-Dimethoxy-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzamide 0200 129. Pentanoic acid 3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0201 130. 1-3-4-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-3-thiophen-2-yl-urea 0202 131. 1-(2-Fluoro-phenyl)-3-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-urea 0203 132. 2-Methyl-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0204 133. 4-Fluoro-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0205 134. 3-Methoxy-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0206 135. 4-Methoxy-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0207 136. N-3-4-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0208 137. 2-Chloro-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-5-trifluoromethyl-benzenesulfonamide 0209 138. Thiophene-2-sulfonic acid 3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0210 139. 3-Fluoro-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0211 140. 2-Methoxy-5-methyl-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0212 141. 2,5-Dimethoxy-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0213 142. 2-Fluoro-N-5-5-(pyridine-2-carbonyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0214 143. 4-Methoxy-N-5-5-(pyridine-2-carbonyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0215 144. Thiophene-2-sulfonic acid 5-5-(pyridine-2-carbonyl)-thiazol-2-ylamino-pentyl-amide 0216 145. 2-Methoxy-5-methyl-N-5-5-(pyridine-2-carbonyl) -thiazol-2-ylamino-pentyl-benzenesulfonamide 0217 146. 4-Fluoro-N-5-5-(pyridine-2-carbonyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0218 147. 2-Methyl-N-5-5-(pyridine-2-carbonyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0219 148. 3-Fluoro-N-5-5-(pyridine-2-carbonyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0220 149. 2-Chloro-N-5-5- (pyridine-2-carbonyl)-thiazol-2-ylamino-pentyl-5-trifluoromethyl-benzenesulfonamide 0221 150. N-5-5-(Pyridine-2-carbonyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0222 151. 3-Methoxy-N-5-5-(pyridine-2-carbonyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0223 152. 2-Fluoro-N-5-5-(pyridine-4-carbonyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0224 153. 2-Methoxy-5-methyl-N-5-5-(pyridine-4-carbonyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0225 154. 2-Fluoro-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0226 155. 4-Methoxy-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0227 156. Thiophene-2-sulfonic acid 5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-amide 0228 157. 2-Methoxy-5-methyl-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0229 158. 4-Fluoro-N-5-5-(2-methyl-benzoyl) -thiazol-2-ylamino-pentyl-benzenesulfonamide 0230 159. 2-Methyl-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0231 160. 3-Fluoro-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0232 161. 2-Chloro-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-5-trifluoromethyl-benzenesulfonamide 0233 162. N-5-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0234 163. 3-Methoxy-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0235 164. N-5-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-pentyl-2-fluoro-benzenesulfonamide 0236 165. N-5-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-pentyl-4-methoxy-benzenesulfonamide 0237 166. Thiophene-2-sulfonic acid 5-5-(2-chloro-benzoyl) -thiazol-2-ylamino-pentyl-amide 0238 167. N-5-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-pentyl-2-methoxy-5-methyl-benzenesulfonamide 0239 168. N-5-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-pentyl-4-fluoro-benzenesulfonamide 0240 169. N-5-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-pentyl-2-methyl-benzenesulfonamide 0241 170. N-5-5-(2-Chloro-benzoyl) -thiazol-2-ylamino-pentyl-3-fluoro-benzenesulfonamide 0242 171. 2-Chloro-N-5-5-(2-chloro-benzoyl)-thiazol-2-ylamino-pentyl-5-trifluoromethyl-benzenesulfonamide 0243 172. N-5-4-Methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0244 173. 2-Methyl-N-5-4-methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0245 174. 2-Fluoro-N-5-4-methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0246 175. 3-Fluoro-N-5-4-methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0247 176. 4-Fluoro-N-5-4-methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0248 177. 2-Methoxy-5-methyl-N-5-4-methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0249 178. 3-Methoxy-N-5-4-methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0250 179. 4-Methoxy-N-5-4-methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0251 180. Thiophene-2-sulfonic acid 2-5-(2-methyl-benzoyl)-thiazol-2-ylamino-ethyl-amide 0252 181. 2,5-Dimethoxy-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0253 182. Thiophene-3-sulfonic acid 4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-amide 0254 183. 2,5-Dimethoxy-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0255 184. Thiophene-3-sulfonic acid 2-5-(2-methyl-benzoyl)-thiazol-2-ylamino-ethyl-amide 0256 185. 2,5-Dimethyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0257 186. 5-Chloro-2-methoxy-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0258 187. 2-Methyl-N-4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-benzenesulfonamide 0259 188. 5-Fluoro-2-methyl-N-4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-benzenesulfonamide 0260 189. 2-Chloro-N-4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-5-trifluoromethyl-benzenesulfonamide 0261 190. 2,5-Dimethyl-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0262 191. N-3-5-(2-Methyl-benzoyl) -thiazol-2-ylamino-propyl-4-trifluoromethoxy-benzenesulfonamide 0263 192. 4-Fluoro-N-4-5-(2-methyl-benzoyl) -thiazol-2-ylamino-butyl-benzenesulfonamide 0264 193. 2,4-Difluoro-N-4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-benzenesulfonamide 0265 194. N-5-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-pentyl-4-trifluoromethoxy-benzenesulfonamide 0266 195. 2-Chloro-N-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-4-trifluoromethyl-benzenesulfonamide 0267 196. 2-Fluoro-N-4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-benzenesulfonamide 0268 197. 5-Chloro-thiophene-2-sulfonic acid 4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-amide 0269 198. 2-Chloro-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-4-trifluoromethyl-benzenesulfonamide 0270 199. Thiophene-3-sulfonic acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0271 200. 5-Fluoro-2-methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0272 201. 3-Fluoro-N-4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-benzenesulfonamide 0273 202. 2-Methoxy-5-methyl-N-4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-benzenesulfonamide 0274 203. Thiophene-3-sulfonic acid 5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-amide 0275 204. 5-Fluoro-2-methyl-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0276 205. 5-Chloro-2-methoxy-N-2-5-(2-methyl-benzoyl)-thiazol-2-ylamino-ethyl-benzenesulfonamide 0277 206. 2,4-Difluoro-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0278 207. 2,5-Dimethyl-N-4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-benzenesulfonamide 0279 208. 2,5-Dimethoxy-N-4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-benzenesulfonamide 0280 209. 2,4-Difluoro-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0281 210. 5-Chloro-thiophene-2-sulfonic acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0282 211. 4-Methoxy-N-4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-benzenesulfonamide 0283 212. 5-Chloro-2-methoxy-N-4-5-(2-methyl-benzoyl) -thiazol-2-ylamino-butyl-benzenesulfonamide 0284 213. 5-Chloro-thiophene-2-sulfonic acid 5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-amide 0285 214. Thiophene-2-sulfonic acid 4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-amide 0286 215. 3-Methoxy-N-4-5-(2-methyl-benzoyl) -thiazol-2-ylamino-butyl-benzenesulfonamide 0287 216. N-4-5-(2-Methyl-benzoyl) -thiazol-2-ylamino-butyl-4-trifluoromethoxy-benzenesulfonamide 0288 217. Thiophene-2-sulfonic acid methyl-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0289 218. 3-Methoxy-N-methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0290 219. 2-Chloro-N-methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-4-trifluoromethyl-benzenesulfonamide 0291 220. 2,N-Dimethyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0292 221. 5-Fluoro-2,N-dimethyl-N-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-benzenesulfonamide 0293 222. 2-Chloro-N-methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-5-trifluoromethyl-benzenesulfonamide 0294 223. 4-Fluoro-N-methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0295 224. 2,4-Difluoro-N-methyl-N-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-benzenesulfonamide 0296 225. 2-Fluoro-N-methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0297 226. 5-Chloro-thiophene-2-sulfonic acid methyl-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0298 227. 3-Fluoro-N-methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0299 228. 2-Methoxy-5,N-dimethyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0300 229. 4-Chloro-N-methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0301 230. 2,5,N-Trimethyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0302 231. N-Methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-4-nitro-benzenesulfonamide 0303 232. 4-Methoxy-N-methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0304 233. 5-Chloro-2-methoxy-N-methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0305 Examples of particularly preferred compounds of formula I are: 0306 Thiophene-2-sulfonic acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide; 0307 2-methoxy-5-methyl-N-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-benzene sulfonamide; 0308 2-chloro-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-5-trifluoromethyl-benzenesulfonamide; 0309 thiophene-2-sulfonic acid 3-5-(2-chloro-benzoyl) -thiazol-2-ylamino-propyl-amide; 0310 N-3-5-(2-chloro-benzoyl)-thiazol-2-ylamino-propyl-2-methoxy-5-methyl-benzene sulfonamide; 0311 2-chloro-N-3-5-(2-chloro-benzoyl)-thiazol-2-ylamino-propyl-5-trifluoromethyl-benzenesulfonamide; 0312 2-chloro-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-5-trifluoromethyl-benzenesulfonamide; 0313 2-methoxy-5-methyl-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzene sulfonamide; 0314 2-methoxy-5-methyl-N-5-5-(pyridine-2-carbonyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide; 0315 4-methoxy-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide; 0316 2-methoxy-5-methyl-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzene sulfonamide; 0317 2-methyl-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide; 0318 3-fluoro-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide; 0319 2-chloro-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-5-trifluoromethyl-benzenesulfonamide; 0320 N-5-5-(2-chloro-benzoyl)-thiazol-2-ylamino-pentyl-2-fluoro-benzenesulfonamide; 0321 N-5-5-(2-chloro-benzoyl)-thiazol-2-ylamino-pentyl-2-methoxy-5-methyl-benzene sulfonamide; 0322 N-5-5-(2-chloro-benzoyl)-thiazol-2-ylamino-pentyl-2-methyl-benzenesulfonamide; 0323 2-methoxy-5-methyl-N-5-4-methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide; 0324 2-chloro-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-4-trifluoromethyl-benzenesulfonamide; 0325 5-fluoro-2-methyl-N-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-benzenesulfonamide; 0326 2,5-dimethoxy-N-4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-benzenesulfonamide; 0327 5-chloro-thiophene-2-sulfonic acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide; 0328 thiophene-2-sulfonic acid 4-5-(2-methyl-benzoyl)-thiazol-2-ylamino-butyl-amide; 0329 thiophene-2-sulfonic acid methyl-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide; 0330 2,N-dimethyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide; 0331 5-chloro-thiophene-2-sulfonic acid methyl-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide; 0332 4-chloro-N-methyl-N-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-benzenesulfonamide and 0333 N-methyl-N-3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-4-nitro-benzenesulfonamide. 0334 Examples of particularly preferred compounds of formula I are: 0335 Thiophene-2-sulfonic acid 3-5-(2-methyl-benzoyl) -thiazol-2-ylamino-propyl-amide; 0336 2-methoxy-5-methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzene sulfonamide; 0337 2-chloro-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-5-trifluoromethyl-benzenesulfonamide; 0338 thiophene-2-sulfonic acid 3-5-(2-chloro-benzoyl)-thiazol-2-ylamino-propyl-amide; 0339 N-3-5-(2-chloro-benzoyl)-thiazol-2-ylamino-propyl-2-methoxy-5-methyl-benzene sulfonamide; 0340 2-chloro-N-3-5-(2-chloro-benzoyl)-thiazol-2-ylamino-propyl-5-trifluoromethyl-benzenesulfonamide; 0341 2-chloro-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-5-trifluoromethyl-benzenesulfonamide; 0342 2-methoxy-5-methyl-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzene sulfonamide; 0343 2-methoxy-5-methyl-N-5-5-(pyridine-2-carbonyl)-thiazol-2-ylamino-pentyl-benz enesulfonamide; 0344 4-methoxy-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide; 0345 2-methoxy-5-methyl-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzene sulfonamide; 0346 2-methyl-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide; 0347 3-fluoro-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide; 0348 2-chloro-N-5-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-5-trifluoromethyl-benzenesulfonamide; 0349 N-5-5-(2-chloro-benzoyl)-thiazol-2-ylamino-pentyl-2-fluoro-benzenesulfonamide; 0350 N-5-5-(2-chloro-benzoyl)-thiazol-2-ylamino-pentyl-2-methoxy-5-methyl-benzene sulfonamide; 0351 N-5-5-(2-chloro-benzoyl)-thiazol-2-ylamino-pentyl-2-methyl-benzenesulfonamide; and 0352 2-methoxy-5-methyl-N-5-4-methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide. 0353 Processes for the manufacture of compounds of formula I are an object of the invention. 0354 The preparation of compounds of formula I of the present invention may be carried out in sequential or convergent synthetic routes. Syntheses of the invention are shown in the following Schemes. The skills required for carrying out the reaction and purification of the resulting products are known to those in the art. The substituents and indices used in the following description of the processes have the significance given above unless indicated to the contrary. 0355 Compounds of general formula IH (R2 means hydrogen) can be prepared according to scheme 1 as follows: 0356 a) Bis amino derivatives IA, either commercially available or prepared from commercially available precursors by methods taught in the art, are mono-protected with a suitable protecting group (PG i.e. Boc, Fmoc , and the like), provided that PG has no adverse effect on the reaction or on the reagents involved in the synthetic route, by reaction of IA with preferably Boc2O, preferably in the presence or the absence of a base such as triethylamine, diisopropylethylamine, and the like, preferably in the presence of a solvent. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dichloromethane, chloroform, or dioxane, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice. (literature: J. Med. Chem., 32(2), 391-6; 1989). 0357 b) Thioureas can be prepared from suitable starting materials according to methods known in the art. The elaboration of the thiourea-moiety in ID starting from an amino functionality, like in IB can be affected by methods described in literature. For example mono-protected derivatives IB are condensed with benzoyl isothiocyanate in a solvent. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dichloromethane, chloroform, or dioxane, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield the protected urea derivatives IC. (literature: Organic Letters, 2(20), 3237-3240;2000). The urea derivatives IC are subjected to basic cleavage conditions such as. K2CO3 aq., and the like, in a solvent such as methanol, and the like, to liberate the urea functionality and access ureas ID. (for reaction conditions described in literature affecting such a reaction see for example: J. Med. Chem., 32(8), 1963-70; 1989). 0358 c) The conversion of the liberated ureas ID to Dimethylaminomethylene-thioureido derivatives IE (R2 means hydrogen) was affected by reaction of derivatives ID with N,N-Dimethylformamide dimethyl acetal either neat or in a solvent. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dichloromethane, chloroform, or dioxane, DMF and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield the protected urea derivatives IC. For reaction conditions described in literature affecting such a reaction see for example: Heterocycles, 11, 313-18; 1978. 0359 d) Dimethylaminomethylene-thioureido derivatives IE can be converted to thiazole derivatives IF (R2 means hydrogen) by reaction of IE with -bromoketones (a known compound or compound prepared by known methods. The source for -Bromoketones employed is indicated as appropriate) in a solvent such as ethanol, and the like, in the presence or the absence of a base. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dichloromethane, chloroform, or dioxane, methanol, ethanol and the like. There is no particular restriction on the nature of the base used in this stage, and any base commonly used in this type of reaction may equally be employed here. Examples of such bases include triethylamine and diisopropylethylamine, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield the protected thiazole derivatives IF. For reaction conditions described in literature affecting such a reaction see for example: J. Heterocycl. Chem., 16(7), 1377-83; 1979. The resulting compound of formula IF is a compound of the present invention and may be the desired product; alternatively it may be subjected to consecutive reactions. 0360 e) Cleavage of the protecting group PG such as Boc, Fmoc, and the like from thiazole derivatives IF to access free amines IG or various salts thereof, IF is in the case PG means Boc subjected to suitable reaction conditions like acidic cleavage. There is no particular restriction on the nature of the acid used in this stage, and any acid commonly used in this type of reaction may equally be employed here. Examples of such acids include: HCl, TFA, and the like in a solvent. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dioxane, water, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield thiazole derivatives IG. For conditions described in literature affecting the cleavage of a protecting group see for example: Protecting Groups, Kocienski, P. Thieme Verlag New York 1994. 0361 f) Sulfonamides, amides, carbamates and ureas can be prepared from suitable starting materials according to methods known in the art. The conversion of the amino-moiety in IG to access sulfonamides, amides, carbamates and can be affected by methods described in literature. For example the conversion of the amine derivatives IG or their respective salts to access compounds of the general formula IH is affected by reaction of IG with suitable acid chlorides, sulfonyl chlorides, isocyanates, chloroformates, or carbonate esters (compounds known or compound prepared by known methods) respectively in a solvent like dichloromethane and in the presence or the absence of a base. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: chloroform, or dioxane, THF, and the like. There is no particular restriction on the nature of the base used in this stage, and any base commonly used in this type of reaction may equally be employed here. Examples of such bases include triethylamine and diisopropylethylamine, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield thiazole derivatives IH. For reaction conditions described in literature affecting such reactions see for example: Comprehensive Organic Transformations: A Guide to Functional Group Preparations, 2nd Edition, Richard C. Larock. John Wiley & Sons, New York, N.Y. 1999. 9

0362 Compounds of general formula IIE (R2 means alkyl or cycloalkyl) can be prepared according to scheme 2 as follows: 0363 a) Thioisocyanates can be prepared from suitable starting materials according to methods known in the art. The elaboration of the thioisocyanate-moiety in IIA (R3 means hydrogen) starting from an amino functionality, can be affected by methods described in literature. For example compounds of the general formula IB (PG for example Boc, Fmoc, and such like) are condensed with carbondisulfide, neat or in a solvent. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dichloromethane, chloroform, or dioxane, THF and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield an intermediate which is reacted with cyanamide in one-pot or after isolation of the intermediate. Elaboration of the thioisocanate derivatives IIA (R3 means hydrogen) is affected by addition of a base such as pyridine, or the like. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dichloromethane, chloroform, or dioxane, THF and the like. There is no particular restriction on the nature of the base used in this stage, and any base commonly used in this type of reaction may equally be employed here. Examples of such bases include pyridine, triethylamine and diisopropylethylamine, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield the thioisocyanate derivatives IIA. For reaction conditions described in literature affecting such a reaction see for example: Journal of Organic Chemistry, 65(19), 6069-6072; 2000. 0364 b) Thioureido derivatives can be prepared from suitable starting materials according to methods known in the art. The elaboration of the thioisocyanate-moiety in IIA (R3 means hydrogen) to a thioureido-moiety can be affected by methods described in literature. For example compounds of the general formula IIA are condensed with an amidine or their salts (R2 means alkyl, cycloakly), a known compound or compound prepared by known methods, in a solvent such as THF, or the like, and a base, such as NaOH, or the like. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dichloromethane, chloroform, dioxane, THF and the like. There is no particular restriction on the nature of the base used in this stage, and any base commonly used in this type of reaction may equally be employed here. Examples of such bases include NaOHaq, KOHaq, NEt3, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction from 0 C. to heating to reflux temperature of the solvent. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield the thioureido derivatives IIB. For reaction conditions described in literature affecting such a reaction see for example: C. R. Seances Acad. Sci., Ser. 2, 294(19), 1183-6; 1982. 0365 c) Dimethylaminomethylene-thioureido derivatives IIB can be converted to thiazole derivatives IIC (R2 means alkyl, cycloalkyl) by reaction of IIB with -bromoketones (a known compound or compound prepared by known methods) in a solvent such as ethanol, and the like, in the presence or the absence of a base. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dichloromethane, chloroform, DMF, dioxane, methanol, ethanol and the like. There is no particular restriction on the nature of the base used in this stage, and any base commonly used in this type of reaction may equally be employed here. Examples of such bases include triethylamine and diisopropylethylamine, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield the protected thiazole derivatives IIC (R3 means H). For reaction conditions described in literature affecting such a reaction see for example: Org. Chem., 65(21), 7244-7247; 2000. The resulting compound of formula IIC (R3 means H) is a compound of the present invention and may be the desired product; alternatively it may be subjected to consecutive reactions. Introduction of R3 means alkyl or cycloalkyl can be affected by reductive amination of IIC with the respective aldehyde under reducing conditions in a solvent. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dichloromethane, chloroform, dioxane, THF, and the like. There is no particular restriction on the nature of the reducing agent used in this stage, and any reducing agent commonly used in this type of reaction may equally be employed here. Examples of such reducing agents include NaBH4, NaCNBH3, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield the protected thiazole derivatives IIC (R3 means alkyl or cycloalkyl). For reaction conditions described in literature affecting a reductive amination see for example: Reductive amination in: A Guide to Functional Group Preparations, 2nd Edition, Richard C. Larock. John Wiley & Sons, New York, N.Y. 1999. The resulting compound of formula IIC (R3 means alkyl or cycloalkyl) is a compound of the present invention and may be the desired product; alternatively it may be subjected to consecutive reactions. 0366 d) Cleavage of the protecting group such as Boc and Fmoc, and the like from thiazole derivatives IIC to access free amines IID or various salts thereof, IIC is subjected to suitable reaction conditions like for example acidic cleavage for the cleavage of the Boc-protecting group. There is no particular restriction on the nature of the acid used in this stage, and any acid commonly used in this type of reaction may equally be employed here. Examples of such acids include: HCl, TFA, and the like in a solvent. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dioxane, water, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield thiazole derivatives IID. For conditions described in literature affecting the cleavage of a protecting group see for example: Protecting Groups, Kocienski, P. Thieme Verlag New York 1994. 0367 e) Sulfonamides, amides, carbamates and ureas can be prepared from suitable starting materials according to methods known in the art. The conversion of the amino-moiety in IID to access sulfonamides, amides, carbamates and ureas can be affected by methods described in literature. For example the conversion of the amine derivatives IID or their respective salts to access compounds of the general formula IIE is affected by reaction of IID with suitable acid chlorides, sulfonyl chlorides, isocyanates, chloroformates, or carbonate esters (compounds known or compound prepared by known methods) respectively in a solvent like dichloromethane and in the presence or the absence of a base. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: chloroform, dioxane, THF, and the like. There is no particular restriction on the nature of the base used in this stage, and any base commonly used in this type of reaction may equally be employed here. Examples of such bases include triethylamine and diisopropylethylamine, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield thiazole derivatives IIE. For reaction conditions described in literature affecting such reactions see for example: Comprehensive Organic Transformations: A Guide to Functional Group Preparations, 2nd Edition, Richard C. Larock. John Wiley & Sons, New York, N.Y. 1999. 10

0368 Compounds of general formula IIID can be prepared according to scheme 3 as follows: 0369 a) Aminothiazoles can be prepared from suitable starting materials according to methods known in the art. The conversion of a thiourea-moiety like in derivatives of the general formula ID can be affected by methods described in literature. For example thiourea derivatives of the general formula ID are reacted with a-bromo-diketones of the general formula IIIA (compounds known or compounds prepared by known methods) in a solvent such as methanol, or the like, in the presence or the absence of a base, such as triethylamine, or the like. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dichloromethane, chloroform, dioxane, ethanol, THF, and the like. There is no particular restriction on the nature of the base used in this stage, and any base commonly used in this type of reaction may equally be employed here. Examples of such bases include triethylamine and diisopropylethylamine, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield thiazole derivatives IIIB. For reaction conditions described in literature affecting such reactions see for example: J. Heterocycl. Chem., 16(7),1377-83; 1979. 0370 b) Cleavage of the protecting group such as Boc and Fmoc, and the like from thiazole derivatives IIIB to access free amines IIIC or various salts thereof, IIIB is subjected to suitable reaction conditions like for example acidic cleavage for the cleavage of the Boc-protecting group. There is no particular restriction on the nature of the acid used in this stage, and any acid commonly used in this type of reaction may equally be employed here. Examples of such acids include: HCl, TFA, and the like in a solvent. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dioxane, water, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield thiazole derivatives IIIC. For conditions described in literature affecting the cleavage of a protecting group see for example: Protecting Groups, Kocienski, P. Thieme Verlag New York 1994. 0371 c) Sulfonamides, amides, carbamates and ureas can be prepared from suitable starting materials according to methods known in the art. The conversion of the amino-moiety in IIIC to access sulfonamides, amides, carbamates and ureas can be affected by methods described in literature. For example the conversion of the amine derivatives IIIC or their respective salts to access compounds of the general formula IIID is affected by reaction of IIIC with suitable acid chlorides, sulfonyl chlorides, isocyanates, chloroformates, or carbonate esters (compounds known or compound prepared by known methods) respectively in a solvent, such as dioxane and methanol, and such like, and in the presence or the absence of a base, such as triethylamine, or the like. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. Examples for suitable solvents include: dichloromethane, chloroform, dioxane, THF, and the like. There is no particular restriction on the nature of the base used in this stage, and any base commonly used in this type of reaction may equally be employed here. Examples of such bases include triethylamine and diisopropylethylamine, and the like. The reaction can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. We find it convenient to carry out the reaction with heating from ambient temperature to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 h to several days will usually suffice to yield thiazole derivatives IIID. For reaction conditions described in literature affecting such reactions see for example: Comprehensive Organic Transformations: A Guide to Functional Group Preparations, 2nd Edition, Richard C. Larock. John Wiley & Sons, New York, N.Y. 1999. 11

0372 The conversion of a compound of formula I into a pharmaceutically acceptable salt can be carried out by treatment of such a compound with an inorganic acid, for example a hydrohalic acid, such as, for example, hydrochloric acid or hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid etc., or with an organic acid, such as, for example, acetic acid, citric acid, maleic acid, fumaric acid, tartaric acid, methanesulfonic acid or p-toluenesulfonic acid. 0373 The conversion of compounds of formula I into pharmaceutically usable esters or amides can be carried out e.g. by treatment of suited amino or hydroxyl groups present in the molecules with an carboxylic acid such as acetic acid, with a condensating reagent such as benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP) or N,N-dicyclohexylcarbodiimide (DCC) to produce the carboxylic ester or carboxylic amide. 0374 Preferred intermediates are: 0375 Example H 0376 2-(3-Amino-propylamino)-thiazol-5-yl-phenyl-methanone; hydrochloride 0377 Example I 0378 2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone; hydrochloride 0379 Example J 0380 2-(3-Amino-propylamino)-thiazol-5-yl-(2-ethyl-phenyl)-methanone; hydrochloride 0381 Example K 0382 2-(3-Amino-propylamino)-thiazol-5-yl-(2-fluoro-phenyl)-methanone; hydrochloride 0383 Example L 0384 2-(3-Amino-propylamino)-thiazol-5-yl-(2-chloro-phenyl)-methanone; hydrochloride 0385 Example M 2-(3-Amino-propylamino)-thiazol-5-yl-(2-trifluoromethyl-phenyl)-methanone; hydrochloride 0386 Example N 0387 2-(3-Amino-propylamino)-thiazol-5-yl-(4-methyl-pyridin-3-yl)-methanone; hydrochloride 0388 Example O 0389 2-(3-Amino-propylamino)-thiazol-5-yl-(3-methyl-pyridin-2-yl) -methanone; hydrochloride 0390 Example P 0391 2-(3-Amino-propylamino)-thiazol-5-yl-(2-methyl-pyridin-3-yl)-methanone; hydrochloride 0392 Example Q 0393 2-(3-Amino-propylamino)-thiazol-5-yl-(3-methyl-pyrazin-2-yl)-methanone; hydrochloride 0394 Example R 0395 2-(3-Amino-propylamino)-thiazol-5-yl-(3-methyl-thiophen-2-yl)-methanone; hydrochloride 0396 Example S 0397 2-(5-Amino-pentylamino)-thiazol-5-yl-o-tolyl-methanone; hydrochloride 0398 Example T 0399 2-(5-Amino-pentylamino)-thiazol-5-yl-pyridin-2-yl-methanone; hydrochloride 0400 Example U 0401 2-(5-Amino-pentylamino)-thiazol-5-yl-pyridin-4-yl-methanone; hydrochloride 0402 Example V 0403 2-(5-Amino-pentylamino)-thiazol-5-yl-(2-chloro-phenyl)-methanone; hydrochloride 0404 Example Y 0405 3-4-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester 0406 Example Z 0407 2-(3-Amino-propylamino)-thiazol-4-yl-o-tolyl-methanone; hydrochloride 0408 Example AC 0409 5-4-Methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-carbamic acid tert-butyl ester 0410 Example AD 0411 2-(5-Amino-pentylamino)-4-methyl-thiazol-5-yl-o-tolyl-methanone hydrochloride 0412 Also an object of the invention are compounds described above for the production of medicaments for the prophylaxis and therapy of illnesses which are caused by disorders associated with the NPY receptor, particularly for the production of medicaments for the prophylaxis and therapy of arthritis, cardiovascular diseases, diabetes, renal failure and particularly eating disorders and obesity. 0413 Likewise an object of the invention are pharmaceutical compositions containing a compound of formula I described above and a therapeutically inert carrier. 0414 An object of the invention is also the use of the compounds described above for the production of medicaments, particularly for the treatment and prophylaxis of arthritis, cardiovascular diseases, diabetes, renal failure and particularly eating disorders and obesity. 0415 A preferred object of the invention is the use of compounds as described before for the production of medicaments for the treatment of obesity. 0416 A further object of the invention comprises compounds which are manufactured according to one of the described processes. 0417 A further object of the invention is a method for the treatment and prophylaxis of arthritis, cardiovascular diseases, diabetes, renal failure and particularly eating disorders and obesity whereby an effective amount of a compound described above is administered. 0418 Particularly preferred is a method for the treatment of obesity whereby an effective amount of a compound as mentioned above is administered. 0419 According to a further aspect of the invention there is provided a method of treatment of obesity in a human in need of such treatment which comprises administration to the human a therapeutically effective amount of a compound according to formula I and a therapeutically effective amount of a lipase inhibitor, particularly preferred, wherein the lipase inhibitor is orlistat. Also subject of the present invention is the mentioned method, wherein the administration is simultaneous, separate or sequential. 0420 A further preferred embodiment of the present invention is the use of a compound of the formula I in the manufacture of a medicament for the treatment and prevention of obesity in a patient who is also receiving treatment with a lipase inhibitor, particularly preferred, wherein the lipase inhibitor is orlistat. 0421 A preferred process for the preparation of a compound of formula I comprises the reaction of a compound of formula (II) 12

0422 in the presence of a compound of formula (III)

R5CH2mA-X(III)

0423 wherein R1 to R5, A, m and n are defined as before and, wherein X means e.g. chloro or bromo. 0424 The compounds of formula I described above for use as therapeutically active substances are a further object of the invention. 0425 Also an object of the invention are compounds described above for the production of medicaments for the prophylaxis and therapy of illnesses which are caused by disorders associated with the NPY receptor, particularly for the production of medicaments for the prophylaxis and therapy of arthritis, cardiovascular diseases, diabetes, renal failure and particularly eating disorders and obesity. 0426 Likewise an object of the invention is a pharmaceutical composition comprising a compound of formula I described above and a therapeutically inert carrier. Preferred is this composition comprising further a therapeutically effective amount of a lipase inhibitor. Particularly preferred is the above composition, wherein the lipase inhibitor is orlistat. 0427 An object of the invention is also the use of the compounds described above for the production of medicaments, particularly for the treatment and prophylaxis of arthritis, cardiovascular diseases, diabetes, renal failure and particularly eating disorders and obesity. 0428 A further object of the invention comprises compounds which are manufactured according to one of the described processes. 0429 A further object of the invention is a method for the treatment and prophylaxis of arthritis, cardiovascular diseases, diabetes, renal failure and particularly eating disorders and obesity whereby an effective amount of a compound described above is administered. 0430 According to a further aspect of the invention there is provided a method of treatment of obesity in a human in need of such treatment which comprises administration to the human a therapeutically effective amount of a compound according to formula I and a therapeutically effective amount of a lipase inhibitor, particularly preferred, wherein the lipase inhibitor is orlistat. Also subject of the present invention is the mentioned method, wherein the administration is simultaneous, separate or sequential. 0431 A further preferred embodiment of the present invention is the use of a compound of the formula I in the manufacture of a medicament for the treatment and prevention of obesity in a patient who is also receiving treatment with a lipase inhibitor, particularly preferred, wherein the lipase inhibitor is orlistat.

Assay Procedures

Cloning of Mouse NPY5 Receptor cDNAs 0432 The full-length cDNA encoding the mouse NPY5 (mNPY5) receptor was amplified from mouse brain cDNA using specific primers, designed based on the published sequence, and Pfu DNA-Polymerase. The amplification product was subcloned into the mammalian expression vector pcDNA3 using Eco RI and XhoI restriction sites. Positive clones were sequenced and one clone, encoding the published sequence (see Borowsky, B., et al., Molecular biology and pharmacology of multiple NPY Y5 receptor species homologs, Regul. Pept. (1998) 75-76:45-53) was selected for generation of stable cell clones.

Stable Transfection 0433 Human embryonic kidney 293 (HEK293) cells were transfected with 10 g mNPY5 DNA using the lipofectamine reagent (Gibco BRL) according to the manufacturer's instruction. Two days after transfection, geneticin selection (1 mg/ml) was initiated and several stable clones were isolated. One clone was further used for pharmacological characterization.

Radioligand Competition Binding 0434 Human embryonic kidney 293 cells (HEK293), expressing recombinant mouse NPY5-receptor (mNPY5) were broken by three freeze/thawing cycles in hypotonic Tris buffer (5 mM, pH 7.4, 1 mM MgCl2), homogenized and centrifuged at 72,000g for 15 min. The pellet was washed twice with 75 mM Tris buffer, pH 7.4, containing 25 mM MgCl2 and 250 mM sucrose, 0.1 mM phenylmethylsulfonylfluoride and 0.1 mM 1,10-pheneanthrolin, resuspended in the same buffer and stored in aliquots at 80 C. Protein was determined according to the method of Lowry using bovine serum albumine (BSA) as a standard. 0435 Radioligand competition binding assays were performed in 250 l 25 mM Hepes buffer (pH 7.4,2.5 mM CaCl2, 1 mM MgCl2, 1% bovine serum albumine, and 0.01% NaN3 containing 5 g protein, 100 pM 125I labelled peptide YY (PYY) and 10 L DMSO containing increasing amounts of unlabeled test compounds. After incubation for 1 h at 22 C., bound and free ligand are separated by filtration over glass fibre filters. Non specific binding is assessed in the presence of 1 M unlabelled PYY. Specific binding is defined as the difference between total binding and non specific binding. IC50 values are defined as the concentration of antagonist that displaces 50% of the binding of 125I labelled neuropeptide Y. It is determined by linear regression analysis after logit/log transformation of the binding data. 0436 Results obtained in the foregoing test using representative compounds of the invention as the test compounds are shown in the following table: 1CompoundIC50Example No. 15.4 nM2-Fluoro-N-3-5-(pyridine-2-carbonyl)-thiazol-2-ylamino-propyl-benzenesulfonamideExample No. 1406 nM2-Methoxy-5-methyl-N-3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzene sulfonamide

0437 Compounds as described above have IC50 values below 1000 nM; more preferred compounds have IC50 values below 100 nM. Most preferred compounds have IC50 values below 10 nM. These results have been obtained by using the foregoing test. 0438 The in vitro assay published by D. Lachammer, et al., Reversal of NPY inhibition of forkelin-stimulated cAMP production, J. Biol. Chem. (1992) 267:10935-8, and M. H. Norman et al., J. Med. Chem. (2001) 44:2344-56, was used to confirm that the compounds of the present invention are antagonists of neuropeptide Y. 0439 The compounds of formula I and their pharmaceutically usable salts, solvates and esters can be used as medicaments (e.g. in the form of pharmaceutical preparations which include pharmaceutically acceptable carriers which are therapeutically inert). The pharmaceutical preparations can be administered internally, such as orally (e.g. in the form of tablets, coated tablets, dragees, hard and soft gelatin capsules, solutions, emulsions or suspensions), nasally (e.g. in the form of nasal sprays) or rectally (e.g. in the form of suppositories). However, the administration can also be effected parentally, such as intramuscularly or intravenously (e.g. in the form of injection solutions). 0440 The compounds of formula I and their pharmaceutically usable salts, solvates and esters can be processed with pharmaceutically inert, inorganic or organic adjuvants for the production of tablets, coated tablets, dragees and hard gelatin capsules. Lactose, corn starch or derivatives thereof, talc, stearic acid or its salts etc. can be used, for example, as such adjuvants for tablets, dragees and hard gelatin capsules. 0441 Suitable adjuvants for soft gelatin capsules, are, for example, vegetable oils, waxes, fats, semi-solid substances and liquid polyols, etc. 0442 Suitable adjuvants for the production of solutions and syrups are, for example, water, polyols, saccharose, invert sugar, glucose, etc. 0443 Suitable adjuvants for injection solutions are, for example, water, alcohols, polyols, glycerol, vegetable oils, etc. 0444 Suitable adjuvants for suppositories are, for example, natural or hardened oils, waxes, fats, semi-solid or liquid polyols, etc. 0445 Moreover, the pharmaceutical preparations can contain preservatives, solubilizers, viscosity-increasing substances, stabilizers, wetting agents, emulsifiers, sweeteners, colorants, flavorants, salts for varying the osmotic pressure, buffers, masking agents or antioxidants. They can also contain still other therapeutically valuable substances. 0446 In accordance with the invention the compounds of formula I and their pharmaceutically usable salts, solvates and esters can be used for the prophylaxis and treatment of arthritis, cardiovascular diseases, diabetes, renal failure and particularly eating disorders and obesity. The dosage can vary in wide limits and will, of course, be fitted to the individual requirements in each particular case. In general, in the case of oral administration a daily dosage of about 0.1 mg to 20 mg per kg body weight, preferably about 0.5 mg to 4 mg per kg body weight (e.g. about 300 mg per person), divided into preferably 1-3 individual doses, which can consist, for example, of the same amounts, should be appropriate. It will, however, be clear that the upper limit given above can be exceeded when this is shown to be indicated. 0447 The invention is illustrated hereinafter by the examples, which have no limiting character.

EXAMPLES

Example A

(3-Thioureido-propyl)-carbamic Acid tert-butyl Ester 0448

0449 A solution of 2 g (11.47 mmol) (3-Amino-propyl)-carbamic acid tert-butyl ester in 20 ml THF was treated with 1.62 ml (11.47 mmol) Benzoyl isothiocyanate and stirred for 1 h at room temperature. After removal of the volatiles the residue was suspended in 50 ml methanol and 4.8 g (34.4 mmol) K2CO3 in 50 ml water was added. The mixture was stirred at room temperature for 16 h, concentrated, and extracted with ethyl acetate. The combined organic layers were washed with NaHCO3 sat., brine, dried with MgSO4 and evaporated under reduced pressure. The residue was purified by flash column chromatography on silica eluting with ethyl acetate/ heptane. The combined product fractions were evaporated under reduced pressure to yield 1.48 g (74%) of the title compound. 0450 1-H-NMR (300 MHz, DMSO-d6) 7.57 (s, br, 2H, NH2), 6.93 (s, br, 1H, NH), 6.80 (s, br, 1H, NH), 3.33 (m, 2H, CH2), 2.93 (m, 2H, CH2), 1.54 (m, 2H, CH2), 1.37 (s, 9H, CH3). 0451 MS (m/e): 234.3 (MH, 100%)

Example B

(5-Thioureido-pentyl)-carbamic Acid tert-butyl Ester 0452

0453 The title compound was synthesised from (5-Amino-pentyl)-carbamic acid tert-butyl ester according to the procedure described for Example A (MS (m/e): 262.4 (MH, 100%).

Example C

3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic Acid tert-butyl Ester 0454

0455 A mixture of 1.48 g (6.35 mmol) (3-Thioureido-propyl)-carbamic acid tert-butyl ester and 15 ml Dimethylformamide dimethyl acetal was heated to 100 C. for 16 h. The mixture was concentrated and the residue was purified by flash column chromatography on silica eluting with ethyl acetate/n-hexane 1/1 to yield 1.65 g (90%) of the title compound. 0456 1-H-NMR (300 MHz, DMSO-d6) 8.68 (s, 1H, CH), 8.63 (s, br, 1H, NH), 6.77 (s, br, 1H, NH), 3.44 (m, 2H, CH2), 3.11 (s, 3H, CH3), 2.97 (s, 3H, CH3), 2.87 (m, 2H, CH2), 1.57 (t, J5.1 Hz, 2H, CH2), 1.37 (s, 9H, CH3). 0457 MS (m/e): 289.3 (MH, 100%) Example D 5-(3-Dimethylaminomethylene-thioureido)-pentyl-carbamic acid tert-butyl ester 16

0458 The title compound was synthesized from (5-Thioureido-pentyl)-carbamic acid tert-butyl ester and Dimethylformamide dimethyl acetal according to the procedure described for Example C in 54% yield. 0459 1-H-NMR (300 MHz, DMSO-d6) 8.68 (s, 1H, CH), 8.66 (s, br, 1H, NH), 6.75 (s, br, 1H, NH), 3.45 (m, 2H, CH2), 3.11 (s, 3H, CH3), 2.97 (s, 3H, CH3), 2.90 (m, 2H, CH2), 1.50 (m, 2H, CH2), 1.20 (m, 2H, CH2), 1.36 (s, 9H, CH3). 0460 MS (m/e): 317.4 (MH, 100%)

Example E

2-Bromo-1-(3-methyl-pyrazin-2-yl)-ethanone Dihydrobromide 0461

0462 A solution of 5.4 g (40 mmol) 1-Pyrazin-2yl-ethanone in 21 ml HBr (33%) and 7 ml methanol was treated with 2.05 ml (40 mmol) bromine and heated to 60 C. for 7 h. The precipitate was filtered off, washed with ethyl acetate/diethyl ether 1/1 and dried to obtain 8.3 g (55%) of the title compound as grey solid. 0463 1-H-NMR (400 MHz, DMSO-d6) 8.78 (d, J2 Hz, 1H, H-5), 8.66 ((d, J2 Hz, 1H, H-6), 5.01 (s, 2H, CH2), 2.75 (s, 3H, CH3). 0464 MS (m/e): 215.0 (MH, 100%).

Example F

2-Bromo-1-(4-methyl-pyridin-3-yl)-ethanone Hydrobromide 0465

0466 The title compound was synthesised according to Example E 1-(4-methyl-pyridin-3-yl)-ethanone and HBr/bromine in 85% yield as grey solid. MS (m/e): 214.0 (MH, 100%).

Example G

2-Bromo-1-(2-ethyl-phenyl) -ethanone 0467

0468 To a solution of 15.2 g (88 mmol) dibromethane in 120 ml THF at 75 C. was added 44 ml (88 mmol) of a 2M solution of LDA in THF and subsequently 6.57 g (40 mmol) ethyl-benzoic acid methyl ester in 80 ml THF. 37.5 ml of a 1.6 M n-butyl lithium solution in n-hexane was added and after 30 min the mixture was treated carefully below 65 C. with 35 ml HCl (37%). The mixture was washed with water and NaHCO3 aq. and the organic phase was dried with MgSO4, filtered and concentrated under reduced pressure. The residue was purified by flash column chromatography on silica eluting with ethyl acetate/hexane 1:9 twice to afford 3.8 g (41%) of the title compound as yellow oil. MS (m/e): 227.1 (MH, 100%).

Example 25

3-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic Acid tert-butyl Ester 0469

0470 A mixture of 613 mg (2.9 mmol) 2-methyl phenacylbromide (literature: WO9907666), 691 mg (2.4 mmol) 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 1 ml (7.2 mmol) NEt3 in 20 ml ethanol was heated to 100 C. for 16 h. The mixture was concentrated and purified by flash column chromatography on silica eluting with ethyl acetate/n-hexane 1/1. The combined product fractions were evaporated and 693 mg (77%%) of the title compound (MS (m/e): 375.9 (MH, 100%)) were obtained.

Example 26

3-5-(2-Chloro-benzoyl)-thiazol-2-ylamino-propyl-carbamic Acid tert-butyl Ester 0471

0472 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 2-chloro phenacylbromide (commercially available) according to the procedure described for Example 25. MS (m/e): 395.8 (MH, 100%).

Example 27

3-5-(2-Ethyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic Acid tert-butyl Ester 0473

0474 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 2-ethyl phenacylbromide according to the procedure described for Example 25. MS (m/e): 389.9 (MH, 100%).

Example 28

3-5-(2-Trifluoromethyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic Acid tert-butyl Ester 0475

0476 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 2-trifluoromethyl phenacylbromide (literature: EP 432040) according to the procedure described for Example 25. MS (m/e): 429.9 (MH, 100%).

Example H

2-(3-Amino-propylamino)-thiazol-5-yl-phenyl-methanone; hydrochloride 0477

0478 A mixture of 0.5 g (1.73 mmol) 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester, 0.448 g (2.25 mmol) phenacyl bromide (commercially available) and 0.723 ml (5.2 mmol) NEt3 in 20 ml EtOH was heated to 100 C. for 16 h. After cooling to room temperature 3 ml of a 4N HCl solution in dioxane was added and the mixture was stirred for 2 h at 60 C. The mixture was concentrated, the precipitate was filtered off, washed with diethyl ether and dried to yield 0.505 g (81%) of the title compound. 1-H-NMR (300 MHz, DMSO-d6) 9.13 (s, br, 1H, NH), 8.04 (s, br, 2H, NH2), 7.60 (m, 6H, Ph/thiazole), 3.43 (m, 2H, CH2),2.85 (m, 2H, CH2), 1.85 (m, 2H, CH2). MS (m/e): 262.2 (MH, 100%)

Example I

2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone; Hydrochloride 0479

0480 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 2-methyl phenacyl bromide (literature: WO9907666) according to the procedure described for Example H. MS (m/e): 276.3 (MH, 100%).

Example J

2-(3-Amino-propylamino)-thiazol-5-yl-(2-ethyl-phenyl)-methanone; hydrochloride 0481

0482 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 2-ethyl phenacyl bromide according to the procedure described for Example H. MS (m/e): 290.3 (MH, 100%).

Example K

2-(3-Amino-propylamino)-thiazol-5-yl-(2-fluoro-phenyl)-methanone; Hydrochloride 0483

0484 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester 2-Fluoro-phenacyl bromide (commercially available) according to the procedure described for Example H. MS (m/e): 280.3 (MH, 100%).

Example L

2-(3-Amino-propylamino)-thiazol-5-yl-(2-chloro-phenyl)-methanone; hydrochloride 0485

0486 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester 2-Chloro-phenacyl bromide (commercially available) according to the procedure described for Example H. MS (m/e): 296.4 (MH, 100%).

Example M

2-(3-Amino-propylamino)-thiazol-5-yl-(2-trifluoromethyl-phenyl)-methanone; Hydrochloride 0487

0488 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester 2-Trifluoromethyl-phenacyl bromide (literature: EP432040) according to the procedure described for Example H. 0489 MS (m/e): 330.4 (MH, 100%).

Example N

2-(3-Amino-propylamino)-thiazol-5-yl-(4-methyl-pyridin-3-yl) -methanone; Hydrochloride 0490

0491 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 2-Bromo-1-(4-methyl-pyridin-3-yl)-ethanone according to the procedure described for Example H. MS (m/e): 277.3 0492 (MH, 100%).

Example O

2-(3-Amino-propylamino)-thiazol-5-yl-(3-methyl-pyridin-2-yl) -methanone; Hydrochloride 0493

0494 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 2-Bromo-1-(3-methyl-pyridin-2-yl)-ethanone (literature: WO9935130) according to the procedure described for Example H. MS (m/e): 277.3 (MH, 100%).

Example P

2-(3-Amino-propylamino)-thiazol-5-yl-(2-methyl-pyridin-3-yl) -methanone; Hydrochloride 0495

0496 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 2-Bromo-1-(2-methyl-pyridin-3-yl)-ethanone (Literature: J. Heterocycl. Chem. 1978, 15, 217) according to the procedure described for Example H. MS (m/e): 277.3 (MH, 100%).

Example Q

2-(3-Amino-propylamino)-thiazol-5-yl-(3-methyl-pyrazin-2-yl)-methanone; Hydrochloride 0497

0498 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 2-Bromo-1-(3-methyl-pyrazin-2-yl)-ethanone according to the procedure described for Example H. MS (m/e): 278.3 (MH, 100%).

Example R

2-(3-Amino-propylamino)-thiazol-5-yl-(3-methyl-thiophen-2-yl)-methanone; Hydrochloride 0499

0500 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 2-Bromo-1-(3-methyl-thiophen-2-yl)-ethanone (Literature: EP432040) according to the procedure described for Example H. MS (m/e): 282.2 (MH, 100%).

Example S

2-(3-Amino-propylamino)-thiazol-5-yl-pyridin-2-yl-methanone; Hydrochloride 0501

0502 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 2-(bromoacetyl)pyridine hydrobromide (commercially available) according to the procedure described for Example H. MS (m/e): 263.2 (MH, 100%).

Example Z

2-(3-Amino-propylamino)-thiazol-5-yl-pyridin-3-yl-methanone; Hydrochloride 0503

0504 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 3-(bromoacetyl)pyridine hydrobromide (commercially available) according to the procedure described for Example H. MS (m/e): 263.2 (MH, 100%).

Example U

2-(3-Amino-propylamino)-thiazol-5-yl-pyridin-4-yl-methanone; Hydrochloride 0505

0506 The title compound was synthesised from 3-(3-Dimethylaminomethylene-thioureido)-propyl-carbamic acid tert-butyl ester and 2-bromo-1-(4-pyridinyl)-1-ethanone hydrobromide (commercially available) according to the procedure described for Example H. MS (m/e): 263.2 (MH, 100%).

Example V

2-(5-Amino-pentylamino)-thiazol-5-yl-o-tolyl-methanone; Hydrochloride 0507

0508 A mixture of 396 mg (1.25 mmol) 5-(3-Dimethylaminomethylene-thioureido)-pentyl-carbamic acid tert-butyl ester, 388 mg (1.82 mmol) 2-methyl phenacylbromide (Literature: WO9907666) and 0.7 ml NEt3 in 8 ml ethanol was heated to 100 C. for 16 h. After evaporation to dryness the residue was taken up in 6 ml dioxane and treated with 3 ml of a 4N HCl in dioxane and stirred for 16 h at room temperature. After concentration the residue taken up in diethyl ether, the precipitate was filtered of and dried to yield 320 mg (75%) of the title compound. MS (m/e): 304.5 (MH, 100%)

Example W

2-(5-Amino-pentylamino)-thiazol-5-yl-pyridin-2-yl-methanone; Hydrochloride 0509

0510 The title compound was synthesised from 5-(3-Dimethylaminomethylene-thioureido)-pentyl-carbamic acid tert-butyl ester and 2-Bromo-1-pyridin-2-yl-ethanone (commercially available) according to the procedure described for Example V. MS (m/e): 291.4 (MH, 100%).

Example X

2-(5-Amino-pentylamino)-thiazol-5-yl-pyridin-4-yl-methanone; Hydrochloride 0511

0512 The title compound was synthesised from 5-(3-Dimethylaminomethylene-thioureido)-pentyl-carbamic acid tert-butyl ester and 2-Bromo-1-pyridin-4-yl-ethanone (commercially available) according to the procedure described for Example V. MS (m/e): 291.3 (MH, 100%).

Example Y

2-(5-Amino-pentylamino)-thiazol-5-yl-(2-chloro-phenyl)-methanone; Hydrochloride 0513

0514 The title compound was synthesised from 5-(3-Dimethylaminomethylene-thioureido)-pentyl-carbamic acid tert-butyl ester and 2-Bromo-1-(2-chloro-phenyl)-ethanone (commercially available) according to the procedure described for Example V. MS (m/e): 324.2 (MH, 100%).

Example 7

Thiophene-2-sulfonic Acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0515

0516 A mixture of 31.1 mg (0.1 mmol) 2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone hydrochloride in 1 ml methanol, 18.2 mg (0.1 mmol) Thiophene-2-sulfonyl chloride in 1 ml DCM and 0.15 ml NEt3 was stirred for 16 h at 50 C. After evaporation to dryness the residue was taken up in 1.5 ml MeOH/formic acid 1/1 and subjected to preparative HPLC separation on reversed phase eluting with an acetonitrile/water gradient. Evaporation of product fractions yielded 11.4 mg (27%) of the title compound. 0517 MS (m/e): 386.3 ((MH), 100%). 0518 According to the procedure described for the synthesis of Example 7 further sulfonamides have been synthesised from 2-(3-Amino-propylamino)-thiazolyl- or 2-(5-Amino-pentylamino)-thiazolyl derivatives and sulfonyl chlorides. The results are shown in table 1 and comprise Example 1 to Example 24, Example 119 to Example 123 and Example 142 to Example 171, and Examples 180 to Example 233.

Example 31

Pentanoic Acid 3-(5-benzoyl-thiazol-2-ylamino)-propyl-amide 0519

0520 A mixture of 11.9 mg (0.04 mmol) 2-(3-Amino-propylamino)-thiazol-5-yl-phenyl-methanone hydrochloride, 5.8 mg (0.048 mmol) pentanoyl chloride and 39 ul (0.28 mmol) NEt3 in 1 ml methanol and 0.5 ml DCM was stirred at room temperature for 16 h. After evaporation to dryness the residue was taken up in 1.5 ml MeOH/formic acid 1/1 and subjected to preparative HPLC separation on reversed phase eluting with an acetonitrile/water gradient. Evaporation of product fractions yielded 6 mg (43%) of the title compound. 0521 MS (m/e): 345.5 (MH, 100%). 0522 According to the procedure described for the synthesis of Example 31 further amides have been synthesised from 2-(3-Amino-propylamino)-thiazolyl derivatives and acid chlorides. The results are shown in table 1 and comprise Example 29 to Example 88.

Example 98

1-(2-Methoxy-phenyl)-3-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-urea 0523

0524 A mixture of 12.5 mg (0.04 mmol) 2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone hydrochloride, 7.6 mg (0.05 mmol) 2-Methoxyphenyl isocyanate and 39 ul NEt3 in 1 ml methanol was stirred for 16 h at room temperature. After evaporation to dryness the residue was taken up in 1.5 ml MeOH/formic acid 1/1 and subjected to preparative HPLC separation on reversed phase eluting with an acetonitrile/water gradient. Evaporation of product fractions yielded 7.9 mg (47%) of the title compound. 0525 MS (m/e): 424.3 (M, 100%) 0526 According to the procedure described for the synthesis of Example 98 further ureas have been synthesised from 2-(3-Amino-propylamino)-thiazolyl derivatives and isocyanates. The results are shown in table 1 and comprise Example 89 to Example 118.

Example Z

1-o-Tolyl-propane-1,2-dione 0527

0528 A mixture of 7 g (47.23 mmol) 1-o-Tolyl-propan-2-one, 30.5 g (0.141 mol) pyridinium chlorochromate and 11.2 g (0.141 mol) pyridine in 200 ml DCM was heated to reflux for 16 h. The mixture was filtered through a pad of silica and the filtrate was evaporated under reduced pressure. The residue was purified by flash column chromatography on silica eluting with ethyl acetate/n-hexane 1:4. The product fractions were evaporated to yield 1.178 g (15%) of the title compound. 0529 1-H-NMR (300 MHz, DMSO-d6) 7.64 d, J6 Hz, 1H, phenyl), 7.52 (d, J6 Hz, 1H, phenyl), 7.38 (d, J6 Hz, 2H, phenyl), 2.52 (s, 3H, CH3), 2.49 (s, 3H, CH3). 0530 MS (m/e): 162 (M, 100%)

Example AA

3-Bromo-1-o-tolyl-propane-1,2-dione 0531

0532 A mixture of 3 g (18.49 mmol) 1-o-Tolyl-propane-1,2-dione and 1.05 ml (20.34 mmol) bromine in 30 ml CHCl3 and 0.53 ml acetic acid was heated to 70 C. for 16 h. The mixture was evaporated under reduced pressure to yield 4.35 g (98%) of the title compound. 0533 1-H-NMR (300 MHz, DMSO-d6) 7.60 (m, 4H, phenyl), 2.52 (s, 2H, CH2), 2.51 (s, 3H, CH3). 0534 MS (m/e): 234.3 (MH, 100%)

Example AB

3-4-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic Acid tert-butyl Ester 0535

0536 A mixture of 2.55 g (10.6 mmol) 3-Bromo-1-o-tolyl-propane-1,2-dione, 1.9 g (8.1 mmol) (3-thioureido-propyl)-carbamic acid tert-butyl ester and 5.66 ml (40.6 mmol) NEt3 in 100 ml methanol was heated to 80 C. for 2 h. The reaction mixture was evaporated under reduced pressure and the residue was purifier by flash column chromatography on silica eluting with a gradient of heptane and ethyl acetate. Evaporation of the product fractions yielded 2.17 g (71%) of the title compound as dark red oil. 0537 1-H-NMR (300 MHz, DMSO-d6) 7.82 (s, br, 1H, NH), 7.38-7.27 (m, 5H, phenyl/thiazole), 6.84 (s, br, 1H, NH), 3.19 (m, 2H, CH2), 2.97 (m, 2H, CH2), 2.25 (s, 3H, CH3), 1.65 (m, 2H, CH2), 1.37 (s, 9H, CH3). 0538 MS (m/e): 376.5 (MH, 100%)

Example AC

2-(3-Amino-propylamino)-thiazol-4-yl-o-tolyl-methanone; Hydrochloride 0539

0540 A mixture of 2.17 g (5.8 mmol) 3-4-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester and 30 ml 4N HCl in dioxane and 20 ml ethanol was stirred at room temperature for 16 h. The mixture was concentrated to yield 1.8 g (quant.) of the title compound. 0541 1-H-NMR (300 MHz, DMSO-d6) 8.23 (s, br, 2H, NH2), 7.45-7.35 (m, 5H, phenyl/thiazole), 6.0 (s, br, 1H, NH), 3.39 (m, 2H, CH2), 2.86 (m, 2H, CH2), 2.29 (s, 3H, CH3), 1.91 (t, J6 Hz, 2H, CH2). 0542 MS (m/e): 276.3 (MH, 100%)

Example 138

Thiophene-2-sulfonic Acid 3-4-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0543

0544 A solution of 15.6 mg (0.5 mmol) 2-(3-Amino-propylamino)-thiazol-4-yl-o-tolyl-methanone hydrochloride in 1 ml methanol was treated with 11.9 mg (0.65 mmol) thiophene-2-sulfonyl chloride in 0.13 ml dioxane and 34.7 ul NEt3. The mixture was stirred at 60 C. for 16 h and after addition of 0.5 ml formic acid subjected to preparative HPLC separation on reversed phase eluting with an acetonitrile/water gradient. Evaporation of the product fractions yielded 6.2 mg (29%) of the title compound. 0545 MS (m/e): 422.3 (MH, 100%) 0546 According to the procedure described for the synthesis of Example 138 further sulfonamides have been synthesised from thiazole derivatives and sulfonylchlorides. The results are shown in table 1 and comprise Example 132 to Example 141. 0547 According to the procedure described for the synthesis of Example 138 amides have been synthesised with the temperature adjustment to room temperature from thiazole derivatives and acid chlorides. The results are shown in table 1 and comprise Example 126 to Example 129. 0548 According to the procedure described for the synthesis of Example 138 ureas have been synthesised with the temperature adjustment to room temperature from thiazole derivatives and isocyanates. The results are shown in table 1 and comprise Example 130 and Example 131.

Example AD

(5-Isothiocyanato-pentyl)-carbamic Acid tert-butyl Ester 0549

0550 To a solution of 2 g (9.9 mmol) (5-Amino-pentyl)-carbamic acid tert-butyl ester in 40 ml THF at 0 C. was added 896 l (14.83 mmol) CS2 and allowed to stir at room temperature for 14 h. 623 mg (14.83 mmol) cyanamide and 4 drops NEt3 was added and the mixture was heated to 4 C. for 3 h. The mixture was extracted with diethyl ether and the combined organic layers were dried with MgSO4. After filtration and removal of the volatiles the residue was purified by flash column chromatography on silica eluting with ethyl acetate/cyclohexane 1:1. The evaporation of the product fractions yielded 2.24 g (93%) of the title compound. 0551 1-H-NMR (250 MHz, CDCl3) 4.58 (s, br, 1H, NH), 3.52 (t, J6.5 Hz, 2H, NCH2), 3.13 (dd, J16.5 Hz, J24 Hz, 2H, NHCH2), 1.74 (m, 2H, CH2), 1.50 (m, 4H, CH2), 1.44 (s, 9H, CH3). 0552 MS (m/e): 262.3 (MNH4, 100%)

Example AE

5-3-(1-Amino-ethylidene)-thioureidol-pentyl-carbamic Acid tert-butyl Ester 0553

0554 A solution of 245 mg (1 mmol) (5-Isothiocyanato-pentyl)-carbamic acid tert-butyl ester in 1 ml 1N NaOH at 0 C. was treated with 94.5 mg (1 mmol) acetidine hydrochloride in 2 ml THF and allowed to stir for 5 h at 0 C. The mixture was extracted three times with 15 ml diethyl ether, the combined organic layers were dried with MgSO4 and after filtration evaporated under reduced pressure to yield 297 mg (98%) of the title compound. 0555 MS (m/e): 303.4 (MH, 100%)

Example AF

5-4-Methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-carbamic Acid tert-butyl Ester 0556

0557 To a solution of 290 mg (0.96 mmol) 5-3-(1-Amino-ethylidene)-thioureido-pentyl-carbamic acid tert-butyl ester in 5 ml ethanol was added 213 mg (1 mmol) o-Methylphenacyl bromide and 139 l NEt3 and allowed to stir for 5 h at room temperature. Afterwards the mixture was directly applied to preparative HPLC on reversed phase eluting with an acetonitrile/water gradient. The evaporation of the product fractions yielded 180 mg (45%) of the title compound. 0558 MS (m/e): 418.3 (MH, 100%)

Example AG

2-(5-Amino-pentylamino)-4-methyl-thiazol-5-yl-o-tolyl-methanone Hydrochloride 0559

0560 A solution of 170 mg (0.4 mmol) 5-4-Methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-carbamic acid tert-butyl ester in 2 ml dioxane was treated with 1 ml 4N HCl in dioxane and allowed to react for 5 h at room temperature. The mixture was evaporated under reduced pressure to afford 143 mg (99%) of the title compound. 0561 1-H-NMR (300 MHz, CDCl3) 8.72 (s, br, 1H, NH), 7.75 (m, 2H, H-3/H-6), 7.30 (m, 2H, H-4/H-5),4.80 (s, br, 2H, NH2), 3.68 (t, J6.4 Hz, 1H, NCH2), 3.23 (m, 1H, NCH2), 2.74 (m, 2H, NCH2), 2.21 (s, 3H, CH3), 1.91 (s, 3H, CH3), 1.54 (m, 4H, CH2), 1.37 (m, 2H, CH2). 0562 MS (m/e): 318.4 (MH, 100%)

Example 172

N-5-4-Methyl-5-(2-methyl-benzoyl)-thiazol-2-ylamino-pentyl-benzenesulfonamide 0563

0564 A solution of 18 mg (0.05 mmol) 2-(5-Amino-pentylamino)-4-methyl-thiazol-5-yl-o-tolyl-methanone hydrochloride in 1 ml ethanol was treated with 10.6 mg (0.06 mmol) benzenesulfonylchloride and 21 ml NEt3. The mixture was allowed to stir for 15 h at room temperature and afterwards subjected to preparative HPLC separation on reversed phase eluting with an acetonitrile/water gradient. Evaporation of the product fractions yielded 12.6 mg (55%) of the title compound. 0565 MS (m/e): 458.3 (MH, 100%)

(2-Thioureido-ethyl)-carbamic Acid tert-butyl Ester 0566

0567 The title compound was synthesised from (2-Amino-ethyl)-carbamic acid tert-butyl ester. The compound is described in literature: WO0121623A1

Example AI

2-(3-Dimethylaminomethylene-thioureido)-ethyl-carbamic Acid tert-butyl Ester 0568

0569 The title compound was synthesised from (2-Thioureido-ethyl)-carbamic acid tert-butyl esterand Dimethylformamide dimethyl acetal according to the procedure described for Example C in 51% yield. MS (m/e): 275.4 (MH, 100%)

Example AJ

2-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-ethyl-carbamic Acid tert-butyl Ester 0570

0571 The title compound was synthesised from 2-(3-Dimethylaminomethylene-thioureido)-ethyl-carbamic acid tert-butyl ester and 2-methyl phenacylbromide (Literature: WO9907666) according to the procedure described for Example 25 in 75% yield. MS (m/e): 362.1 (MH, 100%).

Example AK

2-(2-Amino-ethylamino)-thiazol-5-yl-o-tolyl-methanone; Hydrochloride 0572

0573 The title compound was synthesised from 2-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-ethyl-carbamic acid tert-butyl ester according to the procedure described for Example AC in quantitative yield. MS (m/e): 261.7 (MH, 100%).

Example AL

(4-Thioureido-butyl)-carbamic Acid tert-butyl Ester 0574

0575 The title compound was synthesised from (4-Amino-butyl)-carbamic acid tert-butyl ester. The compound is described in literature: WO0102379A1

Example AM

4-(3-Dimethylaminomethylene-thioureido) -butyl-carbamic Acid tert-butyl Ester 0576

0577 The title compound was synthesised from (4-Thioureido-butyl)-carbamic acid tert-butyl ester and Dimethylformamide dimethyl acetal according to the procedure described for Example C in 76% yield. MS (m/e): 303.3 (MH, 100%)

Example AN

4-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-butyl-carbamic Acid tert-butyl Ester 0578

0579 The title compound was synthesised from 4-(3-Dimethylaminomethylene-thioureido)-butyl-carbamic acid tert-butyl ester and 2-methyl phenacylbromide (Literature: WO9907666) according to the procedure described for Example 25 in 69% yield. MS (m/e): 390.2 (MH, 100%).

Example AO

2-(4-Amino-butylamino)-thiazol-5-yl-o-tolyl-methanone; Hydrochloride 0580

0581 The title compound was synthesised from 4-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-butyl-carbamic acid tert-butyl ester according to the procedure described for Example AC in quantitative yield. MS (m/e): 289.7 (MH, 100%).

Example AP

Methyl-(4-thioureido-propyl)-carbamic Acid tert-butyl Ester 0582

0583 The title compound was synthesised from (3-Amino-propyl)-methyl-carbamic acid tert-butyl ester according to the procedure described for Example A (MS (m/e): 234.3 (MH, 100%).

Example AQ

4-(3-Dimethylaminomethylene-thioureido)-propyl-methyl-carbamic Acid tert-butyl Ester 0584

0585 The title compound was synthesised from Methyl-(4-thioureido-butyl)-carbamic acid tert-butyl ester and Dimethylformamide dimethyl acetal according to the procedure described for Example C in 39% yield. MS (m/e): 328.9 (MH, 100%)

Example AR

Methyl-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic Acid tert-butyl Ester 0586

0587 The title compound was synthesised from 4-(3-Dimethylaminomethylene-thioureido)-butyl-methyl-carbamic acid tert-butyl ester and 2-methyl phenacylbromide (Literature: WO9907666) according to the procedure described for Example 25 in 78% yield. MS (m/e): 390.3 (MH, 100%).

Example AS

2-(3-Methylamino-propylamino)-thiazol-5-yl-o-tolyl-methanone; Hydrochloride 0588

0589 The title compound was synthesised from Methyl-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester according to the procedure described for Example AC in quantitative yield. MS (m/e): 289.1 (MH, 100%).

Example AT

2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone 0590

0591 339 mg 3-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester was added to a solution of 25% aqueous hydrochloric acid in dioxane. The mixture was stirred 1 h at room temperature and maintained overnight in the refrigerator. The mixture was poured into saturated aqueous sodium bicarbonate solution (50 ml). The organics were extracted with dichloromethane (350 ml), dried over magnesium sulfate and evaporated under reduced pressure to afford the title compound as yellow foam (254 mg) which was used without further purification.

Example AU

N-3-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-N-(1,1-dimethylethyl)-sulfamide 0592

0593 900 mg 3-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester was dissolved in diethyl ether and hydrogen chloride in ether added dropwise with stirring. The mixture was stirred overnight at room temperature and poured into saturated aqueous sodium bicarbonate solution. The organics were extracted with dichloromethane (325 ml), dried over magnesium sulfate and evaporated under reduced pressure to afford 2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone as a yellow gum (579 mg, 88%). A solution of 0.22 ml tert-butanol in hexane (2 ml) was cautiously added to a stirred solution of 0.2 ml chlorosulfonyl isocyanate in hexane (5 ml). The resulting white precipitate was stirred until it had dissolved (1.5 h) and the mixture cooled to 78 C. before the slow addition of a solution of 2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone and 0.4 ml triethylamine in dichloromethane. The cooling bath was removed and the yellow mixture allowed to reach room temperature and stirred 2 h at room temperature. The mixture was poured into water and the organics extracted with ethyl acetate (225 ml). The combined organics were washed with brine, dried over magnesium sulfate and evaporated. The resulting oil was purified by column chromatography on silica gel (150 g, 2:1 ethyl acetate/hexane) to afford the title compound (241 mg,24%) as a pale yellow oil. MS (m/e): 409.3 (MH, 100%)

Example AV

N-3-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-acetamide 0594

0595 25% Aqueous hydrochloric acid was added dropwise to a solution of R04386677-000 in 2-propanol. The mixture was stirred 1 h at room temperature and kept in the refrigerator over the week-end. The solvent was evaporated under reduced pressure and the residue triturated with diethyl ether. Ethyl acetate (40 ml) was added and the hydrochloride quenched by the addition of saturated aqueous sodium bicarbonate solution (50 ml). The aqueous phase was extracted with dichloromethane (575 ml).The combined organic phases were dried over sodium sulfate and evaporated. The residue was purified by column chromatography on silica gel. The only product isolated was the title compound, as a yellow oil which solidified on standing. Recrystallisation from a mixture of ethyl acetate, dichloromethane and hexane afforded the pure product as a light yellow solid (275 mg, 13%). MS (m/e): 318.3 (MH, 100%)

Example AW

4-Methyl-N-3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-benzenesulfonamide 0596

0597 2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone was dissolved in dichloromethane and triethylamine and toluene-4-sulfonyl chloride added. The mixture was stirred overnight at room temperature, poured into 1M pH 4 phosphate buffer (5 ml) and extracted with dichloromethane (310 ml). The combined organic phases were dried over magnesium sulfate and evaporated. The oily residue was purified by column chromatography on silica gel (13:7 hexane/acetone eluant), using a small amount of dichloromethane to apply the mixture to the column. The title compound was isolated as an off-white solid. MS (m/e): 428.3 (MH, 100%)

Example AX

Ethanesulfonic Acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0598

0599 The title compound was produced from2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone and ethanesulfonyl chloride according to the procedure described for Example AW. The product was isolated as an off-white solid. MS (m/e): 468.3 (MH, 100%)

Example AY

2,2,2-Trifluoro-ethanesulfonic Acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0600

0601 The title compound was produced from 2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone and 2,2,2-trifluoroethanesulfonyl chloride according to the procedure described for Example AW. The product was isolated as an orange gum. MS (m/e): 422.3 (MH, 100%)

Example AZ

Methanesulfonic acid 3-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0602

0603 The title compound was produced from 2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone and methanesulfonyl chloride according to the procedure described for Example AW. The product was isolated as an orange gum. MS (m/e): 352.2 (MH, 100%)

Example BA

Propane-2-sulfonic acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0604

0605 The title compound was produced from 2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone and 2-propanesulfonyl chloride according to the procedure described for Example AW. The product was isolated as an orange gum. MS (m/e): 380.2 (MH, 100%)

Example BB

Naphthalene-1-sulfonic acid 3-5-(2-methyl-benzoyl)-thiazol-2-ylamino-propyl-amide 0606

0607 The title compound was produced from 2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone and 1-naphthalenesulfonyl chloride according to the procedure described for Example AW. The product was isolated as an off-white gum. MS (m/e): 464.1 (MH, 100%)

Example BC

1,1-dimethylethyl 3-5-(2-Methyl-benzoyl)-thiazol-2-ylamino-propylaminosulfonyl-carbamate 0608

0609 To a solution of 43 mg 2-(3-Amino-propylamino)-thiazol-5-yl-o-tolyl-methanone in dichloromethane was added 49 mg 4-(dimethylamino)-1-(1,1-dimethylethoxy) carbonylaminosulfonyl-pyridinium (Organic Letters, 2001,3,2241). The mixture was stirred overnight at room temperature. The solvent was evaporated under reduced pressure and the solid residue purified by column chromatography on silica gel (15 g, 7:3 ethyl acetate/hexane eluant), using a small amount of dichloromethane to apply the mixture to the column. The product was isolated as an off-white solid (28 mg, 40%). MS (m/e): 453.2 (MH, 100%)

Example BD

3-3-(1-Amino-ethylidene)-thioureido-propyl-carbamic Acid tert-butyl Ester 0610

0611 The title compound was prepared from (3-isothiocyanatopropyl)-carbamic acid tert-butyl ester and acetamidine hydrochloride as a colorless gum (quantitative yield) according to the procedure described for Example AE. MS (m/e): 275.2 (MH, 100%)

Example BE

3-5-(2-Ethyl-benzoyl)-4-methyl-thiazol-2-ylamino-propyl-carbamic Acid tert-butyl Ester 0612

0613 A mixture of 0.60 g 3-3-(1-Amino-ethylidene)-thioureido-propyl-carbamic acid tert-butyl ester and 0.54 g 2-bromo-1-(2-ethyl-phenyl)-ethanone (Example G) were dissolved in N,N-dimethylformamide and stirred overnight at room temperature. 0.33 ml Triethylamine were added and the mixture stirred 72 h at room temperature. The mixture was diluted with dichloromethane, washed twice with water and once with brine, dried over magnesium sulfate, filtered and evaporated to afford the title compound (435 mg) as a pale yellow solid (49%). MS (m/e): 404.5 (MH, 100%)

Example BF

Naphthalene-1-sulfonic acid 3-5-(2-ethyl-benzoyl)-4-methyl-thiazol-2-ylamino-propyl-amide 0614

0615 88 mg 3-5-(2-Ethyl-benzoyl)-4-methyl-thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester was dissolved in dioxane and 0.15 ml 25% aqueous hydrochloric acid added dropwise. The mixture was stirred 4 h at room temperature and evaporated to dryness. Toluene was added and the mixture evaporated to dryness and dried overnight in vacuo. The residue was taken up in dichloromethane and 50 mg naphthalene-1-sulfonyl chloride and 0.14 ml triethylamine added. The mixture was stirred overnight at room temperature and partitioned between water and dichloromethane. The organic phase was dried over magnesium sulfate and evaporated to afford the title compound (77 mg,71%) as a yellow oil. MS (m/e): 492.2 (MH, 100%)

Example BG

Thiophene-2-sulfonic acid 3-5-(2-ethyl-benzoyl)-4-methyl-thiazol-2-ylamino-propyl-amide 0616

0617 The title compound was prepared from 13-5-(2-Ethyl-benzoyl)-4-methyl-thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester and thiophene-2-sulfonyl chloride according to example BF. Off-white oil, 55%. MS (m/e): 448.1 (MH, 100%)

Example BH

N-3-5-(2-Ethyl-benzoyl)-4-methyl-thiazol-2-ylamino-propyl-2-methoxy-5-methyl-benzenesulfonamide 0618

0619 The title compound was prepared from 3-5-(2-Ethyl-benzoyl)-4-methyl-thiazol-2-ylamino-propyl-carbamic acid tert-butyl ester and 6-methoxy-m-toluenesulfonyl chloride according to example XX. Light yellow oil, 67%. MS (m/e): 486.3 (MH, 100%) 0620 According to Example 172 further sulfonamide derivatives have been synthesised from the corresponding aminothiazole derivative and a sulfonylchloride. The results are compiled in the table and comprise Examples 172-179. 2Ex.EductsNameMass analysis1.2-(3-Amino-propylamino)-2-Fluoro-N-3-5-419.2 (M H)thiazol-5-yl-pyridin-2-yl-(pyridine-2-carbonyl)-methanone; hydrochloride and 2-thiazol-2-ylamino-Fluorophenylsulfonyl chloridepropylbenzene-sulfonamide2.2-(3-Amino-propylamino)-2-Methoxy-5-methyl-N-445.3 (M H)thiazol-5-yl-pyridin-2-yl-3-5-(pyridine-2-methanone; hydrochloride and 2-carbonyl)-thiazol-2-methoxy-5-methylphenylsulfonylylamino-propyl-chloridebenzenesulfonamide3.2-(3-Amino-propylamino)-2-Methoxy-5-methyl-N-445.3 (M H)thiazol-5-yl-pyridin-3-yl-3-5-(pyridine-3-methanone; hydrochloride and 2-carbonyl)-thiazol-2-methoxy-5-methylphenylsulfonylylamino-propyl-chloridebenzenesulfonamide4.2-(3-Amino-propylamino)-2-Methoxy-5-methyl-N-445.3 (M H)thiazol-5-yl-pyridin-4-yl-3-5-(pyridine-4-methanone; hydrochloride and 2-carbonyl)-thiazol-2-methoxy-5-methylphenylsulfonylylamino-propyl-chloridebenzenesulfonamide5.2-(3-Amino-propylamino)-2-Fluoro-N-3-5-(2-432.3 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-2-ylamino-propyl-Fluorophenylsulfonyl chloridebenzenesulfonamide6.2-(3-Amino-propylamino)-4-Methoxy-N-3-5-(2-444.3 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 4-2-ylamino-propyl-methoxyphenylsulfonyl chloridebenzenesulfonamide7.2-(3-Amino-propylamino)-Thiophene-2-sulfonic420.2 (M H)thiazol-5-yl-o-tolyl-methanone;acid 3-5-(2-methyl-hydrochloride and 2-benzoyl)-thiazol-2-thiophenylsulfonyl chlorideylamino-propyl-amide8.2-(3-Amino-propylamino)-2-Methoxy-5-methyl-N-458.3 (M H)thiazol-5-yl-o-tolyl-methanone;3-5-(2-methyl-hydrochloride and 2-methoxy-5-benzoyl)-thiazol-2-methylphenylsulfonyl chlorideylamino-propyl-benzenesulfonamide9.2-(3-Amino-propylamino)-4-Fluoro-N-3-5-(2-432.3 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 4-2-ylamino-propyl-fluorophenylsulfonyl chloridebenzenesulfonamide10.2-(3-Amino-propylamino)-2-Methyl-N-3-5-(2-428.4 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-2-ylamino-propyl-methylphenylsulfonyl chloridebenzenesulfonamide11.2-(3-Amino-propylamino)-3-Fluoro-N-3-5-(2-432.4 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 3-2-ylamino-propyl-fluorophenylsulfonyl chloridebenzenesulfonamide12.2-(3-Amino-propylamino)-2-Chloro-N-3-5-(2-516.1 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-chloro-5-2-ylamino-propyl-5-(trifluoromethyl)phenylsulfonyltrifluoromethyl-chloridebenzenesulfonamide13.2-(3-Amino-propylamino)-N-3-5-(2-Methyl-415.5 (M H)thiazol-5-yl-o-tolyl-methanone;benzoyl)-thiazol-2-hydrochloride and phenylsulfonylylamino-propyl-chloridebenzenesulfonamide14.2-(3-Amino-propylamino)-3-Methoxy-N-3-5-(2-444.3 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 3-2-ylamino-propyl-methoxyphenylsulfonyl chloridebenzenesulfonamide15.2-(3-Amino-propylamino)-N-3-5-(2-Chloro-452.2 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 2-ylamino-propyl-2-fluorophenylsulfonyl chloridefluoro-benzene-sulfonamide16.2-(3-Amino-propylamino)-N-3-5-(2-Chloro-464.2 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 4-ylamino-propyl-4-methoxyphenylsulfonyl chloridemethoxy-benzene-sulfonamide17.2-(3-Amino-propylamino)-Thiophene-2-sulfonic440.2 (M H)thiazol-5-yl-(2-chloro-phenyl)-acid 3-5-(2-chloro-methanone; hydrochloride and 2-benzoyl)-thiazol-2-thiophenylsulfonyl chlorideylamino-propyl-amide18.2-(3-Amino-propylamino)-N-3-5-(2-Chloro-478.2 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 2-ylamino-propyl-2-methoxy-5-methylphenylsulfonylmethoxy-5-methyl-chloridebenzenesulfonamide19.2-(3-Amino-propylamino)-N-3-5-(2-Chloro-452.2 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 4-ylamino-propyl-4-fluorophenylsulfonyl chloridefluoro-benzene-sulfonamide20.2-(3-Amino-propylamino)-N-3-5-(2-Chloro-448.2 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 2-ylamino-propyl-2-methylphenylsulfonyl chloridemethyl-benzene-sulfonamide21.2-(3-Amino-propylamino)-N-3-5-(2-Chloro-452.2 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 3-ylamino-propyl-3-fluorophenylsulfonyl chloridefluoro-benzene-sulfonamide22.2-(3-Amino-propylamino)-2-Chloro-N-3-5-(2-536.1 (M H)thiazol-5-yl-(2-chloro-phenyl)-chloro-benzoyl)-thiazol-methanone; hydrochloride and 2-2-ylamino-propyl-5-chloro-5-(trifluoromethyl)trifluoromethyl-phenylsulfonyl chloridebenzenesulfonamide23.2-(3-Amino-propylamino)-N-3-5-(2-Chloro-434.3 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride andylamino-propyl-phenylsulfonyl chloridebenzenesulfonamide24.2-(3-Amino-propylamino)-N-3-5-(2-Chloro-464.2 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 3-ylamino-propyl-3-methoxyphenylsulfonyl chloridemethoxy-benzene-sulfonamide25.2-methyl phenacylbromide and3-5-(2-Methyl-375.9 MH3-(3-dimethylaminomethylene-benzoyl)-thiazol-2-thioureido)-propyl-carbamicylamino-propyl-acid tert-butyl estercarbamic acid tert-butylester26.3-(3-dimethylaminomethylene-3-5-(2-Chloro-395.8 MHthioureido)-propyl-carbamicbenzoyl)-thiazol-2-acid tert-butyl ester and 2-chloroylamino-propyl-phenacylbromidecarbamic acid tert-butylester27.3-(3-dimethylaminomethylene-3-5-(2-Ethyl-benzoyl)-389.9 MHthioureido)-propyl-carbamicthiazol-2-ylamino-acid tert-butyl ester and 2-ethylpropyl-carbamic acidphenacylbromidetert-butyl ester28.3-(3-dimethylaminomethylene-3-5-(2-Trifluoro-429.9 MHthioureido)-propyl-carbamicmethyl-benzoyl)-thiazol-acid tert-butyl ester and 2-2-ylamino-propyl-trifluoromethyl phenacylbromidecarbamic acid tert-butylester29.2-(3-Amino-propylamino)-Cyclohexanecarboxylic386.4 MHthiazol-5-yl-o-tolyl-methanone;acid 3-5-(2-methyl-hydrochloride andbenzoyl)-thiazol-2-cyclohexanecarbonyl chlorideylamino-propyl-amide30.2-(3-Amino-propylamino)-Cyclohexanecarboxylic400.5 MHthiazol-5-yl-(2-ethyl-phenyl)-acid 3-5-(2-ethyl-methanone; hydrochloride andbenzoyl)-thiazol-2-cyclohexanecarbonyl chlorideylamino-propyl-amide31.2-(3-Amino-propylamino)-Pentanoic acid 3-(5-345.5 MHthiazol-5-yl-phenyl-methanone;benzoyl-thiazol-2-hydrochloride and pentanoylylamino)-propyl-amidechloride32.2-(3-Amino-propylamino)-Pentanoic acid 3-5-(2-360.4 MHthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and pentanoyl2-ylamino-propyl-chlorideamide33.2-(3-Amino-propylamino)-Pentanoic acid 3-5-(2-374.5 MHthiazol-5-yl-(2-ethyl-phenyl)-ethyl-benzoyl)-thiazol-2-methanone; hydrochloride andylamino-propyl-amidepentanoyl chloride34.2-(3-Amino-propylamino)-Pentanoic acid 3-5-(2-364.3 MHthiazol-5-yl-(2-fluoro-phenyl)-fluoro-benzoyl)-thiazol-methanone; hydrochloride and2-ylamino-propyl-pentanoyl chlorideamide35.2-(3-Amino-propylamino)-Pentanoic acid 3-5-(2-380.4 MHthiazol-5-yl-(2-chloro-phenyl)-chloro-benzoyl)-thiazol-methanone; hydrochloride and2-ylamino-propyl-pentanoyl chlorideamide36.2-(3-Amino-propylamino)-N-3-(5-Benzoyl-thiazol-414.35 MHthiazol-5-yl-phenyl-methanone;2-ylamino)-propyl-2-(4-hydrochloride and 4-chloro-phenyl)-Chlorophenylacetyl chlorideacetamide37.2-(3-Amino-propylamino)-2-(4-Chloro-phenyl)-N-428.5 MHthiazol-5-yl-o-tolyl-methanone;3-5-(2-methyl-hydrochloride and 4-benzoyl)-thiazol-2-Chlorophenylacetyl chlorideylamino-propyl-acetamide38.2-(3-Amino-propylamino)-2-(4-Chloro-phenyl)-N-442.4 MHthiazol-5-yl-(2-ethyl-phenyl)-3-5-(2-ethyl-benzoyl)-methanone; hydrochloride and 4-thiazol-2-ylamino-Chlorophenylacetyl chloridepropyl-acetamide39.2-(3-Amino-propylamino)-Thiophene-2-carboxylic386.3 MHthiazol-5-yl-o-tolyl-methanone;acid 3-5-(2-methyl-hydrochloride and thiophene-2-benzoyl)-thiazol-2-carbonyl chlorideylamino-propyl-amide40.2-(3-Amino-propylamino)-Thiophene-2-carboxylic400.5 MHthiazol-5-yl-(2-ethyl-phenyl)-acid 3-5-(2-ethyl-methanone; hydrochloride andbenzoyl)-thiazol-2-thiophene-2-carbonyl chlorideylamino-propyl-amide41.2-(3-Amino-propylamino)-Thiophene-2-carboxylic390.2 MHthiazol-5-yl-(2-fluoro-phenyl)-acid 3-5-(2-fluoro-methanone; hydrochloride andbenzoyl)-thiazol-2-thiophene-2-carbonyl chlorideylamino-propyl-amide42.2-(3-Amino-propylamino)-Thiophene-2-carboxylic406.4 MHthiazol-5-yl-(2-chloro-phenyl)-acid 3-5-(2-chloro-methanone; hydrochloride andbenzoyl)-thiazol-2-thiophene-2-carbonyl chlorideylamino-propyl-amide43.2-(3-Amino-propylamino)-N-3-5-(2-Ethyl-412.4 MHthiazol-5-yl-(2-ethyl-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 2-ylamino-propyl-2-Fluorobenzoyl chloridefluoro-benzamide44.2-(3-Amino-propylamino)-N-3-5-(2-Chloro-418.3 MHthiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 2-ylamino-propyl-2-Fluorobenzoyl chloridefluoro-benzamide45.2-(3-Amino-propylamino)-3-Fluoro-N-3-5-(2-398.4 MHthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 3-2-ylamino-propyl-Fluorobenzoyl chloridebenzamide46.2-(3-Amino-propylamino)-N-3-5-(2-Ethyl-412.4 MHthiazol-5-yl-(2-ethyl-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 3-ylamino-propyl-3-Fluorobenzoyl chloridefluoro-benzamide47.2-(3-Amino-propylamino)-3-Fluoro-N-3-5-(2-402.5 MHthiazol-5-yl-(2-fluoro-phenyl)-fluoro-benzoyl)-thiazol-methanone; hydrochloride and 3-2-ylamino-propyl-Fluorobenzoyl chloridebenzamide48.2-(3-Amino-propylamino)-N-3-5-(2-Chloro-418.3 MHthiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 3-ylamino-propyl-3-Fluorobenzoyl chloridefluoro-benzamide49.2-(3-Amino-propylamino)-4-Fluoro-N-3-5-(2-398.4 MHthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 4-2-ylamino-propyl-Fluorobenzoyl chloridebenzamide50.2-(3-Amino-propylamino)-N-3-5-(2-Ethyl-412.4 MHthiazol-5-yl-(2-ethyl-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 4-ylamino-propyl-4-Fluorobenzoyl chloridefluoro-benzamide51.2-(3-Amino-propylamino)-N-3-5-(2-Chloro-418.3 MHthiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 4-ylamino-propyl-4-Fluorobenzoyl chloridefluoro-benzamide52.2-(3-Amino-propylamino)-N-3-5-(2-Methyl-380.4 MHthiazol-5-yl-o-tolyl-methanone;benzoyl)-thiazol-2-hydrochloride and benzoylylamino-propyl-chloridebenzamide53.2-(3-Amino-propylamino)-N-3-5-(2-Ethyl-394.4 MHthiazol-5-yl-(2-ethyl-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride andylamino-propyl-benzoyl chloridebenzamide54.2-(3-Amino-propylamino)-N-3-5-(2-Chloro-400.4 MHthiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride andylamino-propyl-benzoyl chloridebenzamide55.2-(3-Amino-propylamino)-N-3-5-(2-Ethyl-424.5 MHthiazol-5-yl-(2-ethyl-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 4-ylamino-propyl-4-methoxybenzoyl chloridemethoxy-benzamide56.2-(3-Amino-propylamino)-N-3-(5-Benzoyl-thiazol-396.3 MHthiazol-5-yl-phenyl-methanone;2-ylamino)-propyl-2-hydrochloride and 2-methoxy-benzamidemethoxybenzoyl chloride57.2-(3-Amino-propylamino)-N-3-5-(2-Ethyl-424.5 MHthiazol-5-yl-(2-ethyl-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 2-ylamino-propyl-2-methoxybenzoyl chloridemethoxy-benzamide58.2-(3-Amino-propylamino)-4-Chloro-N-3-5-(2-414.3 MHthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 4-2-ylamino-propyl-chlorobenzoyl chloridebenzamide59.2-(3-Amino-propylamino)-4-Chloro-N-3-5-(2-428.5 MHthiazol-5-yl-(2-ethyl-phenyl)-ethyl-benzoyl)-thiazol-2-methanone; hydrochloride 4-ylamino-propyl-chlorobenzoyl chloridebenzamide60.2-(3-Amino-propylamino)-Cyclohexanecarboxylic440.5 MHthiazol-5-yl-(2-trifluoromethyl-acid 3-5-(2-phenyl)-methanone;trifluoromethyl-hydrochloride andbenzoyl)-thiazol-2-cyclohexyanecarbonyl chlorideylamino-propyl-amide61.2-(3-Amino-propylamino)-Cyclohexanecarboxylic387.4 MHthiazol-5-yl-(4-methyl-pyridin-acid 3-5-(4-methyl-3-yl)-methanone; hydrochloridepyridine-3-carbonyl)-and cyclohexyanecarbonylthiazol-2-ylamino-chloridepropyl-amide62.2-(3-Amino-propylamino)-Pentanoic acid 3-5-(2-414.4 MHthiazol-5-yl-(2-trifluoromethyl-trifluoromethyl-phenyl)-methanone;benzoyl)-thiazol-2-hydrochloride and pentanoylylamino-propyl-amidechloride63.2-(3-Amino-propylamino)-Pentanoic acid 3-5-(4-361.3 MHthiazol-5-yl-(4-methyl-pyridin-methyl-pyridine-3-3-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and pentanoyl chlorideylamino-propyl-amide64.2-(3-Amino-propylamino)-Pentanoic acid 3-5-(2-361.3 MHthiazol-5-yl-(2-methyl-pyridin-methyl-pyridine-3-3-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and pentanoyl chlorideylamino-propyl-amide65.2-(3-Amino-propylamino)-Pentanoic acid 3-5-(3-366.3 MHthiazol-5-yl-(3-methyl-thiophen-methyl-thiophene-2-2-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and pentanoyl chlorideylamino-propyl-amide66.2-(3-Amino-propylamino)-2-(4-Chloro-phenyl)-N-482.3 MHthiazol-5-yl-(2-trifluoromethyl-3-5-(2-trifluoromethyl-phenyl)-methanone;benzoyl)-thiazol-2-hydrochloride and 4-ylamino-propyl-Chlorophenylacetyl chlorideacetamide67.2-(3-Amino-propylamino)-2-(4-Chloro-phenyl)-N-429.5 MHthiazol-5-yl-(3-methyl-pyridin-3-5-(3-methyl-2-yl)-methanone; hydrochloridepyridine-2-carbonyl)-and 4-Chlorophenylacetylthiazol-2-ylamino-chloridepropyl-acetamide68.2-(3-Amino-propylamino)-2-(4-Chloro-phenyl)-N-430.5 MHthiazol-5-yl-(3-methyl-pyrazin-3-5-(3-methyl-2-yl)-methanone; hydrochloridepyrazine-2-carbonyl)-and 4-Chlorophenylacetylthiazol-2-ylamino-chloridepropyl-acetamide69.2-(3-Amino-propylamino)-Thiophene-2-carboxylic440.4 MHthiazol-5-yl-(2-trifluoromethyl-acid 3-5-(2-phenyl)-methanone;trifluoromethyl-hydrochloride and thiophene-2-benzoyl)-thiazol-2-carbonyl chlorideylamino-propyl-amide70.2-(3-Amino-propylamino)-Thiophene-2-carboxylic387.3 MHthiazol-5-yl-(3-methyl-pyridin-acid 3-5-(3-methyl-2-yl)-methanone; hydrochloridepyridine-2-carbonyl)-and thiophene-2-carbonylthiazol-2-ylamino-chloridepropyl-amide71.2-(3-Amino-propylamino)-2-Fluoro-N-3-5-(2-452.4 MHthiazol-5-yl-(2-trifluoromethyl-trifluoromethyl-phenyl)-methanone;benzoyl)-thiazol-2-hydrochloride and 2-ylamino-propyl-Fluorobenzoyl chloridebenzamide72.2-(3-Amino-propylamino)-2-Fluoro-N-3-5-(3-400.4 MHthiazol-5-yl-(3-methyl-pyrazin-methyl-pyrazine-2-2-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and 2-Fluorobenzoyl chlorideylamino-propyl-benzamide73.2-(3-Amino-propylamino)-3-Fluoro-N-3-5-(2-452.4 MHthiazol-5-yl-(2-trifluoromethyl-trifluoromethyl-phenyl)-methanone;benzoyl)-thiazol-2-hydrochloride and 3-ylamino-propyl-Fluorobenzoyl chloridebenzamide74.2-(3-Amino-propylamino)-3-Fluoro-N-3-5-(4-399.4 MHthiazol-5-yl-(4-methyl-pyridin-methyl-pyridine-3-3-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and 3-Fluorobenzoyl chlorideylamino-propyl-benzamide75.2-(3-Amino-propylamino)-3-Fluoro-N-3-5-(3-399.4 MHthiazol-5-yl-(3-methyl-pyridin-methyl-pyridine-2-2-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and 3-Fluorobenzoyl chlorideylamino-propyl-benzamide76.2-(3-Amino-propylamino)-3-Fluoro-N-3-5-(3-400.4 MHthiazol-5-yl-(3-methyl-pyrazin-methyl-pyrazine-2-2-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and 3-Fluorobenzoyl chlorideylamino-propyl-benzamide77.2-(3-Amino-propylamino)-4-Fluoro-N-3-5-(2-452.4 MHthiazol-5-yl-(2-trifluoromethyl-trifluoromethyl-phenyl)-methanone;benzoyl)-thiazol-2-hydrochloride and 4-ylamino-propyl-Fluorobenzoyl chloridebenzamide78.2-(3-Amino-propylamino)-4-Fluoro-N-3-5-(4-399.4 MHthiazol-5-yl-(4-methyl-pyridin-methyl-pyridine-3-3-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and 4-Fluorobenzoyl chlorideylamino-propyl-benzamide79.2-(3-Amino-propylamino)-4-Fluoro-N-3-5-(3-399.4 MHthiazol-5-yl-(3-methyl-pyridin-methyl-pyridine-2-2-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and 4-Fluorobenzoyl chlorideylamino-propyl-benzamide80.2-(3-Amino-propylamino)-4-Fluoro-N-3-5-(3-404.4 MHthiazol-5-yl-(3-methyl-thiophen-methyl-thiophene-2-2-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-3-methyl-2-thiophenecarbonylylamino-propyl-chloridebenzamide81.2-(3-Amino-propylamino)-N-3-5-(2-434.5 MHthiazol-5-yl-(2-trifluoromethyl-Trifluoromethyl-phenyl)-methanone;benzoyl)-thiazol-2-hydrochloride and benzoylylamino-propyl-chloridebenzamide82.2-(3-Amino-propylamino)-N-3-5-(4-Methyl-381.4 MHthiazol-5-yl-(4-methyl-pyridin-pyridine-3-carbonyl)-3-yl)-methanone; hydrochloridethiazol-2-ylamino-and benzoyl chloridepropyl-benzamide83.2-(3-Amino-propylamino)-4-Methoxy-N-3-5-(2-464.3 MHthiazol-5-yl-(2-trifluoromethyl-trifluoromethyl-phenyl)-methanone;benzoyl)-thiazol-2-hydrochloride and 4-ylamino-propyl-Methoxybenzoyl chloridebenzamide84.2-(3-Amino-propylamino)-4-Methoxy-N-3-5-(4-411.4 MHthiazol-5-yl-(4-methyl-pyridin-methyl-pyridine-3-3-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and 4-Methoxybenzoyl chlorideylamino-propyl-benzamide85.2-(3-Amino-propylamino)-2-Methoxy-N-3-5-(2-464.3 MHthiazol-5-yl-(2-trifluoromethyl-trifluoromethyl-phenyl)-methanone;benzoyl)-thiazol-2-hydrochloride and 2-ylamino-propyl-Methoxybenzoyl chloridebenzamide86.2-(3-Amino-propylamino)-4-Chloro-N-3-5-(2-468.2 MHthiazol-5-yl-(2-trifluoromethyl-trifluoromethyl-phenyl)-methanone;benzoyl)-thiazol-2-hydrochloride and 4-ylamino-propyl-Chlorobenzoyl chloridebenzamide87.2-(3-Amino-propylamino)-4-Chloro-N-3-5-(4-415.3 MHthiazol-5-yl-(4-methyl-pyridin-methyl-pyridine-3-3-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and 4-Chlorobenzoyl chlorideylamino-propyl-benzamide88.2-(3-Amino-propylamino)-4-Chloro-N-3-5-(2-415.3 MHthiazol-5-yl-(2-methyl-pyridin-methyl-pyridine-3-3-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and 4-Chlorobenzoyl chlorideylamino-propyl-benzamide89.2-(3-Amino-propylamino)-1-3-(5-Benzoyl-thiazol-386.5 MHthiazol-5-yl-phenyl-methanone;2-ylamino)-propyl-3-hydrochloride and cyclohexylcyclohexyl-ureaisocyanate90.2-(3-Amino-propylamino)-1-Cyclohexyl-3-3-5-(2-400.5 MHthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and cyclohexyl2-ylamino-propyl-ureaisocyanate91.2-(3-Amino-propylamino)-1-Cyclohexyl-3-3-5-(2-414.5 MHthiazol-5-yl-(2-ethyl-phenyl)-ethyl-benzoyl)-thiazol-2-methanone; hydrochloride andylamino-propyl-ureacyclohexyl isocyanate92.2-(3-Amino-propylamino)-1-3-5-(2-Chloro-420.9 MHthiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride andylamino-propyl-3-cyclohexyl isocyanatecyclohexyl-urea93.2-(3-Amino-propylamino)-1-3-(5-Benzoyl-thiazol-360.4 MHthiazol-5-yl-phenyl-methanone;2-ylamino)-propyl-3-hydrochloride and n-butylbutyl-ureaisocyanante94.2-(3-Amino-propylamino)-1-Butyl-3-3-5-(2-374.5 MHthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and n-butyl2-ylamino-propyl-ureaisocyanante95.2-(3-Amino-propylamino)-1-Butyl-3-3-5-(2-ethyl-388.5 MHthiazol-5-yl-(2-ethyl-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and n-ylamino-propyl-ureabutyl isocyanante96.2-(3-Amino-propylamino)-1-Butyl-3-3-5-(2-378.4 MHthiazol-5-yl-(2-fluoro-phenyl)-fluoro-benzoyl)-thiazol-methanone; hydrochloride and n-2-ylamino-propyl-ureabutyl isocyanante97.2-(3-Amino-propylamino)-1-Butyl-3-3-5-(2-394.9 MHthiazol-5-yl-(2-chloro-phenyl)-chloro-benzoyl)-thiazol-methanone; hydrochloride and n-2-ylamino-propyl-ureabutyl isocyanante98.2-(3-Amino-propylamino)-1-(2-Methoxy-phenyl)-3-424.5 MHthiazol-5-yl-o-tolyl-methanone;3-5-(2-methyl-hydrochloride and 2-benzoyl)-thiazol-2-Methoxyphenyl isocyanateylamino-propyl-urea99.2-(3-Amino-propylamino)-1-3-5-(2-Ethyl-438.5 MHthiazol-5-yl-(2-ethyl-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 2-ylamino-propyl-3-(2-Methoxyphenyl isocyanatemethoxy-phenyl)-urea100.2-(3-Amino-propylamino)-1-3-5-(2-Chloro-444.9 MHthiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 2-ylamino-propyl-3-(2-Methoxyphenyl isocyanatemethoxy-phenyl)-urea101.2-(3-Amino-propylamino)-1-(2-Fluoro-phenyl)-3-412.4 MHthiazol-5-yl-o-tolyl-methanone;3-5-(2-methyl-hydrochloride and 2-benzoyl)-thiazol-2-Fluorophenyl isocyanateylamino-propyl-urea102.2-(3-Amino-propylamino)-1-3-5-(2-Ethyl-426.5 MHthiazol-5-yl-(2-ethyl-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 2-ylamino-propyl-3-(2-Fluorophenyl isocyanatefluoro-phenyl)-urea103.2-(3-Amino-propylamino)-1-3-5-(2-Chloro-432.9 MHthiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 2-ylamino-propyl-3-(2-Fluorophenyl isocyanatefluoro-phenyl)-urea104.2-(3-Amino-propylamino)-1-(3-Fluoro-phenyl)-3-412.4 MHthiazol-5-yl-o-tolyl-methanone;3-5-(2-methyl-hydrochloride and 3-benzoyl)-thiazol-2-Fluorophenyl isocyanateylamino-propyl-urea105.2-(3-Amino-propylamino)-1-3-5-(2-Ethyl-426.5 MHthiazol-5-yl-(2-ethyl-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 3-ylamino-propyl-3-(3-Fluorophenyl isocyanatefluoro-phenyl)-urea106.2-(3-Amino-propylamino)-1-(4-Fluoro-phenyl)-3-412.4 MHthiazol-5-yl-o-tolyl-methanone;3-5-(2-methyl-hydrochloride and 4-benzoyl)-thiazol-2-Fluorophenyl isocyanateylamino-propyl-urea107.2-(3-Amino-propylamino)-1-3-5-(2-Ethyl-426.5 MHthiazol-5-yl-(2-ethyl-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 4-ylamino-propyl-3-(4-Fluorophenyl isocyanatefluoro-phenyl)-urea108.2-(3-Amino-propylamino)-1-3-(5-Benzoyl-thiazol-428.9 MHthiazol-5-yl-phenyl-methanone;2-ylamino)-propyl-3-(2-hydrochloride and 4-chloro-benzyl)-ureaChlorobenzyl isocyanate(WO0107436)109.2-(3-Amino-propylamino)-1-(2-Chloro-benzyl)-3-442.9 MHthiazol-5-yl-o-tolyl-methanone;3-5-(2-methyl-hydrochloride and 4-benzoyl)-thiazol-2-Chlorobenzyl isocyanateylamino-propyl-urea(WO0107436)110.2-(3-Amino-propylamino)-1-(2-Chloro-benzyl)-3-457.0 MHthiazol-5-yl-(2-ethyl-phenyl)-3-5-(2-ethyl-benzoyl)-methanone; hydrochloride and 4-thiazol-2-ylamino-Chlorobenzyl isocyanatepropyl-urea(WO0107436)111.2-(3-Amino-propylamino)-1-3-5-(2-Chloro-463.3 MHthiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 4-ylamino-propyl-3-(2-Chlorobenzyl isocyanatechloro-benzyl)-urea(WO0107436)112.2-(3-Amino-propylamino)-1-3-5-(2-Methyl-394.5 MHthiazol-5-yl-o-tolyl-methanone;benzoyl)-thiazol-2-hydrochloride and phenylylamino-propyl-3-isocyanatephenyl-urea113.2-(3-Amino-propylamino)-1-3-5-(2-Ethyl-408.5 MHthiazol-5-yl-(2-ethyl-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride andylamino-propyl-3-phenyl isocyanatephenyl-urea114.2-(3-Amino-propylamino)-1-3-5-(2-Chloro-414.9 MHthiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride andylamino-propyl-3-phenyl isocyanatephenyl-urea115.2-(3-Amino-propylamino)-1-Butyl-3-3-5-(4-375.5 MHthiazol-5-yl-(4-methyl-pyridin-methyl-pyridine-3-3-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and n-butyl isocyanateylamino-propyl-urea116.2-(3-Amino-propylamino)-1-3-5-(4-Methyl-395.5 MHthiazol-5-yl-(4-methyl-pyridin-pyridine-3-carbonyl)-3-yl)-methanone; hydrochloridethiazol-2-ylamino-and phenyl isocyanatepropyl-3-phenyl-urea117.2-(3-Amino-propylamino)-1-Cyclohexyl-3-3-5-(3-402.5 MHthiazol-5-yl-(3-methyl-pyrazin-methyl-pyrazine-2-2-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and cyclohexyl isocyanateylamino-propyl-urea118.2-(3-Amino-propylamino)-1-Cyclohexyl-3-3-5-(3-406.6 MHthiazol-5-yl-(3-methyl-thiophen-methyl-thiophene-2-2-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and cyclohexyl isocyanateylamino-propyl-urea119.2-(3-Amino-propylamino)-4-Fluoro-N-3-5-(4-434.5 MHthiazol-5-yl-(4-methyl-pyridin-methyl-pyridine-3-3-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and 4-Fluorophenylsulfonylylamino-propyl-chloridebenzenesulfonamide120.2-(3-Amino-propylamino)-4-Fluoro-N-3-5-(3-439.6 MHthiazol-5-yl-(3-methyl-thiophen-methyl-thiophene-2-2-yl)-methanone; hydrochloridecarbonyl)-thiazol-2-and 4-Fluorophenylsulfonylylamino-propyl-chloridebenzenesulfonamide121.2-(3-Amino-propylamino)-2-Methoxy-5-methyl-N-460.6 MHthiazol-5-yl-(4-methyl-pyridin-3-5-(4-methyl-3-yl)-methanone; hydrochloridepyridine-3-carbonyl)-and 2-Methoxy-5-thiazol-2-ylamino-methylphenylsulfonyl chloridepropyl-benzenesulfonamide122.2-(3-Amino-propylamino)-2-Methoxy-5-methyl-N-461.6 MHthiazol-5-yl-(3-methyl-pyrazin-3-5-(3-methyl-2-yl)-methanone; hydrochloridepyrazine-2-carbonyl)-and 2-Methoxy-5-thiazol-2-ylamino-methylphenylsulfonyl chloridepropyl-benzenesulfonamide123.2-(3-Amino-propylamino)-2-Methoxy-5-methyl-N-465.6 MHthiazol-5-yl-(3-methyl-thiophen-3-5-(3-methyl-2-yl)-methanone; hydrochloridethiophene-2-carbonyl)-and 2-Methoxy-5-thiazol-2-ylamino-methylphenylsulfonyl chloridepropyl-benzenesulfonamide124.2-(3-Amino-propylamino)-1-(4-Methoxy-phenyl)-3-425.5 MHthiazol-5-yl-(4-methyl-pyridin-3-5-(4-methyl-3-yl)-methanone; hydrochloridepyridine-3-carbonyl)-and 4-Methoxyphenylsulfonylthiazol-2-ylamino-chloridepropyl-urea125.3-Bromo-1-o-tolyl-propane-1,2-3-4-(2-Methyl-376.5 MHdione and (3-thioureido-propyl)benzoyl)-thiazol-2-carbamic acid tert-butyl esterylamino-propyl-carbamic acid tert-butylester126.2-(3-Amino-propylamino)-N-3-4-(2-Methyl-380.4 MHthiazol-4-yl-o-tolyl-methanone;benzoyl)-thiazol-2-hydrochloride and benzoylylamino-propyl-chloridebenzamide127.2-(3-Amino-propylamino)-2-Fluoro-N-3-4-(2-398.4 MHthiazol-4-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-2-ylamino-propyl-Fluorobenzoyl chloridebenzamide128.2-(3-Amino-propylamino)-3,5-Dimethoxy-N-3-4-440.5 MHthiazol-4-yl-o-tolyl-methanone;(2-methyl-benzoyl)-hydrochloride and 3,5-thiazol-2-ylamino-dimethoxybenzoyl chloridepropyl-benzamide129.2-(3-Amino-propylamino)-Pentanoic acid 3-4-(2-360.3 MHthiazol-4-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and pentanoyl2-ylamino-propyl-chlorideamide130.2-(3-Amino-propylamino)-1-3-4-(2-Methyl-401.5 MHthiazol-4-yl-o-tolyl-methanone;benzoyl)-thiazol-2-hydrochloride and 2-thiopheneylamino-propyl-3-isocyanatethiophen-2-yl-urea131.2-(3-Amino-propylamino)-1-(2-Fluoro-phenyl)-3-413.3 MHthiazol-4-yl-o-tolyl-methanone;3-4-(2-methyl-hydrochloride and 2-fluorophenylbenzoyl)-thiazol-2-isocyanateylamino-propyl-urea132.2-(3-Amino-propylamino)-2-Methyl-N-3-4-(2-430.5 MHthiazol-4-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-2-ylamino-propyl-methylbenzenesulfonyl chloridebenzenesulfonamide133.2-(3-Amino-propylamino)-4-Fluoro-N-3-4-(2-434.4 MHthiazol-4-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 4-2-ylamino-propyl-fluorobenzenesulfonyl chloridebenzenesulfonamide134.2-(3-Amino-propylamino)-3-Methoxy-N-3-4-(2-446.3 MHthiazol-4-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 3-2-ylamino-propyl-methoxybenzenesulfonyl chloridebenzenesulfonamide135.2-(3-Amino-propylamino)-4-Methoxy-N-3-4-(2-446.3 MHthiazol-4-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 3-2-ylamino-propyl-methoxybenzenesulfonyl chloridebenzenesulfonamide136.2-(3-Amino-propylamino)-N-3-4-(2-Methyl-416.3 MHthiazol-4-yl-o-tolyl-methanone;benzoyl)-thiazol-2-hydrochloride andylamino-propyl-benzenesulfonyl chloridebenzenesulfonamide137.2-(3-Amino-propylamino)-2-Chloro-N-3-4-(2-518.1 MHthiazol-4-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-chloro-5-2-ylamino-propyl-5-(trifluormethyl)benzenesulfonyltrifluoromethyl-chloridebenzenesulfonamide138.2-(3-Amino-propylamino)-Thiophene-2-sulfonic422.3 MHthiazol-4-yl-o-tolyl-methanone;acid 3-4-(2-methyl-hydrochloride and 2-benzoyl)-thiazol-2-thiophenesulfonyl chlorideylamino-propyl-amide139.2-(3-Amino-propylamino)-3-Fluoro-N-3-4-(2-434.4 MHthiazol-4-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 3-2-ylamino-propyl-fluorobenzenesulfonyl chloridebenzenesulfonamide140.2-(3-Amino-propylamino)-2-Methoxy-5-methyl-N-460.5 MHthiazol-4-yl-o-tolyl-methanone;3-4-(2-methyl-hydrochloride and 6-methoxy-m-benzoyl)-thiazol-2-toluenesulfonyl chlorideylamino-propyl-benzenesulfonamide141.2-(3-Amino-propylamino)-2,5-Dimethoxy-N-3-4-476.2 MHthiazol-4-yl-o-tolyl-methanone;(2-methyl-benzoyl)-hydrochloride and 2,5-thiazol-2-ylamino-dimethoxybenzenesulfonylpropyl-chloridebenzenesulfonamide142.2-(5-Amino-pentylamino)-2-Fluoro-N-5-5-447.2 (M H)thiazol-5-yl-pyridin-2-yl-(pyridine-2-carbonyl)-methanone; hydrochloride and 2-thiazol-2-ylamino-fluorobenzenesulfonyl chloridepentyl-benzenesulfonamide143.2-(5-Amino-pentylamino)-4-Methoxy-N-5-5-459.3 (M H)thiazol-5-yl-pyridin-2-yl-(pyridine-2-carbonyl)-methanone; hydrochloride andthiazol-2-ylamino-benzenesulfonyl chloridepentyl-benzenesulfonamide144.2-(5-Amino-pentylamino)-Thiophene-2-sulfonic435.3 (M H)thiazol-5-yl-pyridin-2-yl-acid 5-5-(pyridine-2-methanone; hydrochloride and 2-carbonyl)-thiazol-2-thiophenesulfonyl chlorideylamino-pentyl-amide145.2-(5-Amino-pentylamino)-2-Methoxy-5-methyl-N-473.2 (M H)thiazol-5-yl-pyridin-2-yl-5-5-(pyridine-2-methanone; hydrochloride and 6-carbonyl)-thiazol-2-methoxy-m-toluenesulfonylylamino-pentyl-chloridebenzenesulfonamide146.2-(5-Amino-pentylamino)-4-Fluoro-N-5-5-447.3 (M H)thiazol-5-yl-pyridin-2-yl-(pyridine-2-carbonyl)-methanone; hydrochloride and 4-thiazol-2-ylamino-fluorobenzenesulfonyl chloridepentyl-benzenesulfonamide147.2-(5-Amino-pentylamino-2-Methyl-N-5-5-443.3 (M H)thiazol-5-yl-pyridin-2-yl-(pyridine-2-carbonyl)-methanone; hydrochloride and 2-thiazol-2-ylamino-methyl benzenesulfonyl chloridepentyl-benzenesulfonamide148.2-(5-Amino-pentylamino)-3-Fluoro-N-5-5-447.2 (M H)thiazol-5-yl-pyridin-2-yl-(pyridine-2-carbonyl)-methanone; hydrochloride and 3-thiazol-2-ylamino-fluoro benzenesulfonyl chloridepentyl-benzenesulfonamide149.2-(5-Amino-pentylamino)-2-Chloro-N-5-5-531.1 (M H)thiazol-5-yl-pyridin-2-yl-(pyridine-2-carbonyl)-methanone; hydrochloride and 2-thiazol-2-ylamino-chloro-5-pentyl-5-trifluoro-(trifluoromethyl)benzenesulfonylmethyl-benzene-chloridesulfonamide150.2-(5-Amino-pentylamino)-N-5-5-(Pyridine-2-429.4 (M H)thiazol-5-yl-pyridin-2-yl-carbonyl)-thiazol-2-methanone; hydrochloride andylamino-pentyl-benzenesulfonyl chloridebenzenesulfonamide151.2-(5-Amino-pentylamino)-3-Methoxy-N-5-5-459.3 (M H)thiazol-5-yl-pyridin-2-yl-(pyridine-2-carbonyl)-methanone; hydrochloride and 3-thiazol-2-ylamino-methoxy benzenesulfonyl chloridepentyl-benzene-sulfonamide152.2-(5-Amino-pentylamino)-2-Fluoro-N-5-5-447.2 (M H)thiazol-5-yl-pyridin-4-yl-(pyridine-4-carbonyl)-methanone; hydrochloride and 2-thiazol-2-ylamino-fluoro benzenesulfonyl chloridepentyl-benzene-sulfonamide153.2-(5-Amino-pentylamino)-2-Methoxy-5-methyl-N-473.1 (M H)thiazol-5-yl-pyridin-4-yl-5-5-(pyridine-4-methanone; hydrochloride and 6-carbonyl)-thiazol-2-methoxy-m-toluenesulfonylylamino-pentyl-benzchlorideenesulfonamide154.2-(5-Amino-pentylamino)-2-Fluoro-N-5-5-(2-460.4 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-fluoro2-ylamino-pentyl-benzenesulfonyl chloridebenzenesulfonamide155.2-(5-Amino-pentylamino)-4-Methoxy-N-5-5-(2-472.1 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 4-methoxy2-ylamino-pentyl-benzenesulfonyl chloridebenzenesulfonamide156.2-(5-Amino-pentylamino)-Thiophene-2-sulfonic448.2 (M H)thiazol-5-yl-o-tolyl-methanone;acid 5-5-(2-methyl-hydrochloride and 2-benzoyl)-thiazol-2-thiophenesulfonyl chlorideylamino-pentyl-amide157.2-(5-Amino-pentylamino)-2-Methoxy-5-methyl-N-486.3 (M H)thiazol-5-yl-o-tolyl-methanone;5-5-(2-methyl-hydrochloride and 6-methoxy-m-benzoyl)-thiazol-2-toluenesulfonyl chlorideylamino-pentyl-benzene sulfonamide158.2-(5-Amino-pentylamino)-4-Fluoro-N-5-5-(2-460.4 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 4-fluoro2-ylamino-pentyl-benzenesulfonyl chloridebenzenesulfonamide159.2-(5-Amino-pentylamino)-2-Methyl-N-5-5-(2-456.4 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-methyl2-ylamino-pentyl-benzenesulfonyl chloridebenzenesulfonamide160.2-(5-Amino-pentylamino)-3-Fluoro-N-5-5-(2-460.3 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 3-2-ylamino-pentyl-fluorobenzenesulfonyl chloridebenzenesulfonamide161.2-(5-Amino-pentylamino)-2-Chloro-N-5-5-(2-544.1 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-chloro-5-2-ylamino-pentyl-5-(trifluoromethyl)benzenesulfonyltrifluoromethyl-chloridebenzenesulfonamide162.2-(5-Amino-pentylamino)-N-5-5-(2-Methyl-442.3 (M H)thiazol-5-yl-o-tolyl-methanone;benzoyl)-thiazol-2-hydrochloride andylamino-pentyl-benzenesulfonyl chloridebenzenesulfonamide163.2-(5-Amino-pentylamino)-3-Methoxy-N-5-5-(2-472.1 (M H)thiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 3-2-ylamino-pentyl-methoxybenzenesulfonyl chloridebenzenesulfonamide164.2-(5-Amino-pentylamino)-N-5-5-(2-Chloro-480.2 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 2-ylamino-pentyl-2-fluorobenzenesulfonyl chloridefluoro-benzene-sulfonamide165.2-(5-Amino-pentylamino)-N-5-5-(2-Chloro-492.2 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 4-ylamino-pentyl-4-methoxybenzenesulfonyl chloridemethoxy-benzene-sulfonamide166.2-(5-Amino-pentylamino)-Thiophene-2-sulfonic468.1 (M H)thiazol-5-yl-(2-chloro-phenyl)-acid 5-5-(2-chloro-methanone; hydrochloride and 2benzoyl)-thiazol-2-thiophenesulfonyl chlorideylamino-pentyl-amide167.2-(5-Amino-pentylamino)-N-5-5-(2-Chloro-506.2 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 6-ylamino-pentyl-2-methoxy-m-toluenesulfonylmethoxy-5-methyl-chloridebenzene sulfonamide168.2-(5-Amino-pentylamino)-N-5-5-(2-Chloro-480.3 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 4-ylamino-pentyl-4-fluorobenzenesulphonyl chloridefluorobenzene-sulfonamide169.2-(5-Amino-pentylamino)-N-5-5-(2-Chloro-476.2 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 2-ylamino-pentyl-2-methylbenzenesulphonyl chloridemethyl-benzene-sulfonamide170.2-(5-Amino-pentylamino)-N-5-5-(2-Chloro-480.3 (M H)thiazol-5-yl-(2-chloro-phenyl)-benzoyl)-thiazol-2-methanone; hydrochloride and 3-ylamino-pentyl-3-fluorobenzenesulphonyl chloridefluoro-benzene-sulfonamide171.2-(5-Amino-pentylamino)-2-Chloro-N-5-5-(2-564.0(M H)thiazol-5-yl-(2-chloro-phenyl)-chloro-benzoyl)-thiazol-methanone; hydrochloride and 2-2-ylamino-pentyl-5-chloro-5-(trifluoromethyl)-trifluoromethyl-benzenesulfonyl chloridebenzenesulfonamide172.2-(5-Amino-pentylamino)-4-N-5-4-Methyl-5-(2-458.1 MHmethyl-thiazol-5-yl-o-tolyl-methyl-benzoyl)-thiazol-methanone hydrochloride and2-ylamino-pentyl-benzenesulphonyl chloridebenzenesulfonamide173.2-(5-Amino-pentylamino)-4-2-Methyl-N-5-4-472.3 MHmethyl-thiazol-5-yl-o-tolyl-methyl-5-(2-methyl-methanone hydrochloride and 2-benzoyl)-thiazol-2-methybenzenesulphonyl chlorideylamino-pentyl-benzenesulfonamide174.2-(5-Amino-pentylamino)-4-2-Fluoro-N-5-4-476.3 MHmethyl-thiazol-5-yl-o-tolyl-methyl-5-(2-methyl-methanone hydrochloride and 2-benzoyl)-thiazol-2-fluorobenzenesulphonyl chlorideylamino-pentyl-benzenesulfonamide175.2-(5-Amino-pentylamino)-4-3-Fluoro-N-5-4-476.2 MHmethyl-thiazol-5-yl-o-tolyl-methyl-5-(2-methyl-methanone hydrochloride and 3-benzoyl)-thiazol-2-fluorobenzenesulphonyl chlorideylamino-pentyl-benzenesulfonamide176.2-(5-Amino-pentylamino)-4-4-Fluoro-N-5-4-476.2 MHmethyl-thiazol-5-yl-o-tolyl-methyl-5-(2-methyl-methanone hydrochloride and 4-benzoyl)-thiazol-2-fluorobenzenesulphonyl chlorideylamino-pentyl-benzenesulfonamide177.2-(5-Amino-pentylamino)-4-2-Methoxy-5-methyl-N-502.3 MHmethyl-thiazol-5-yl-o-tolyl-5-4-methyl-5-(2-methanone hydrochloride and 6-methyl-benzoyl)-thiazol-methoxy-m-toluenesulfonyl2-ylamino-pentyl-chloridebenzenesulfonamide178.2-(5-Amino-pentylamino)-4-3-Methoxy-N-5-4-488.3 MHmethyl-thiazol-5-yl-o-tolyl-methyl-5-(2-methyl-methanone hydrochloride and 3-benzoyl)-thiazol-2-methoxybenzenesulfonyl chlorideylamino-pentyl-benzene sulfonamide179.2-(5-Amino-pentylamino)-4-4-Methoxy-N-5-4-488.3 MHmethyl-thiazol-5-yl-o-tolyl-methyl-5-(2-methyl-methanone hydrochloride and 4-benzoyl)-thiazol-2-methoxybenzenesulfonyl chlorideylamino-pentyl-benzene sulfonamide180.2-(2-Amino-ethylamino)-Thiophene-2-sulfonic406.2 M Hthiazol-5-yl-o-tolyl-methanone;acid 2-5-(2-methyl-hydrochloride and 2-benzoyl)-thiazol 2thiophenylsulfonyl chlorideylamino-ethyl-amide181.2-(2-Amino-propylamino)-2,5-Dimethoxy-N-3-5-474.1 M Hthiazol-5-yl-o-tolyl-methanone;(2-methyl-benzoyl)-hydrochloride and 2,5-thiazol-2-ylamino-dimethoxyphenylsulfonyl chloridepropyl-benzenesulfonamide182.2-(2-Amino-butylamino)-Thiophene-3-sulfonic434.2 M Hthiazol-5-yl-o-tolyl-methanone;acid 4-5-(2-methyl-hydrochloride and 2-benzoyl)-thiazol-2-thiophenylsulfonyl chlorideylamino-butyl-amide183.2-(5-Amino-pentylamino)-2,5-Dimethoxy-N-5-5-502.0 M Hthiazol-5-yl-o-tolyl-methanone;(2-methyl-benzoyl)-hydrochloride and 2,5-thiazol-2-ylamino-dimethoxyphenylsulfonyl chloridepentyl-benzenesulfonamide184.2-(2-Amino-ethylamino)-Thiophene-3-sulfonic406.2 M Hthiazol-5-yl-o-tolyl-methanone;acid 2-5-(2-methyl-hydrochloride and 3-benzoyl)-thiazol-2-thiophenylsulfonyl chlorideylamino-ethyl-amide185.2-(2-Amino-propylamino)-2,5-Dimethyl-N-3-5-442.2 M Hthiazol-5-yl-o-tolyl-methanone;(2-methyl-benzoyl)-hydrochloride and 2,5-thiazol-2-ylamino-dimethylphenylsulfonyl chloridepropylbenzenesulfonamide186.2-(2-Amino-propylamino)-5-Chloro-2-methoxy-N-478.0 M Hthiazol-5-yl-o-tolyl-methanone;3-5-(2-methyl-hydrochloride and 2-chloro-5-benzoyl)-thiazol-2-methoxyphenylsulfonyl chlorideylamino-propyl-benzenesulfonamide187.2-(2-Amino-butylamino)-2-Methyl-N-4-5-(2-442.2 M Hthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-2-ylamino-butyl-methylbenzenesulfonyl chloridebenzenesulfonamide188.2-(2-Amino-butylamino)-5-Fluoro-2-methyl-N-4-460.2 M Hthiazol-5-yl-o-tolyl-methanone;5-(2-methyl-benzoyl)-hydrochloride and 2-methyl-5-thiazol-2-ylamino-fluoro-benzenesulfonyl chloridebutyl-benzenesulfonamide189.2-(2-Amino-butylamino)-2-Chloro-N-4-5-(2-530.0 M Hthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl) -thiazol-hydrochloride and 2-chloro-5-2-ylamino-butyl-5-trifluoromethyl-benzenesulfonyltrifluoromethyl-chloridebenzenesulfonamide190.2-(2-Amino-pentylamino)-2,5-Dimethyl-N-5-5-470.2 M Hthiazol-5-yl-o-tolyl-methanone;(2-methyl-benzoyl)-hydrochloride and 2,5-thiazol-2-ylamino-dimethylphenylsulfonyl chloridepentyl-benzenesulfonamide191.2-(2-Amino-propylamino)-N-3-5-(2-Methyl-498.0 M Hthiazol-5-yl-o-tolyl-methanone;benzoyl)-thiazol-2-hydrochloride and 4-ylamino-propyl-4-trifluoromethyloxyphenylsulfonyltrifluoromethoxy-chloridebenzenesulfonamide192.2-(2-Amino-butylamino)-4-Fluoro-N-4-5-(2-446.2 M Hthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 4-2-ylamino-butyl-fluorophenylsulfonyl chloridebenzenesulfonamide193.2-(2-Amino-butylamino)-2,4-Difluoro-N-4-5-(2-464.1 M Hthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2,4-2-ylamino-butyl-difluorophenylsulfonyl chloridebenzenesulfonamide194.2-(2-Amino-pentylamino)-N-5-5-(2-Methyl-525.9 M Hthiazol-5-yl-o-tolyl-methanone;benzoyl)-thiazol-2-hydrochloride and 4-ylamino-pentyl-4-trifluoromethyloxyphenylsulfonyltrifluoromethoxy-chloridebenzenesulfonamide195.2-(2-Amino-propylamino)-2-Chloro-N-3-5-(2-516.0 M Hthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-chloro-5-2-ylamino-propyl-4-trifluoromethyl-benzenesulfonyltrifluoromethyl-chloridebenzenesulfonamide196.2-(2-Amino-butylamino)-2-Fluoro-N-4-5-(2-446.1 M Hthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-2-ylamino-butyl-fluorophenylsulfonyl chloridebenzenesulfonamide197.2-(2-Amino-butylamino)-5-Chloro-thiophene-2-468.0 M Hthiazol-5-yl-o-tolyl-methanone;sulfonic acid 4-5-(2-hydrochloride and 5-methyl-benzoyl)-thiazol-chlorothiophenyl-2-2-ylamino-butyl-amidesulfonylchloride198.2-(2-Amino-pentylamino)-2-Chloro-N-5-5-(2-544.0 M Hthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2-chloro-5-2-ylamino-pentyl-4-trifluoromethyl-benzenesulfonyltrifluoromethyl-chloridebenzenesulfonamide199.2-(2-Amino-propylamino)-Thiophene-3-sulfonic420.1 M Hthiazol-5-yl-o-tolyl-methanone;acid 3-5-(2-methyl-hydrochloride and 2-benzoyl)-thiazol-2-thiophenesulfonylchlorideylamino-propyl-amide200.2-(2-Amino-propylamino)-5-Fluoro-2-methyl-N-3-446.2 M Hthiazol-5-yl-o-tolyl-methanone;5-(2-methyl-benzoyl)-hydrochloride and 2-methyl-5-thiazol-2-ylamino-fluorobenzenesulfonylchloridepropyl-benzenesulfonamide201.2-(2-Amino-butylamino)-3-Fluoro-N-4-5-(2-446.1 M Hthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 3-2-ylamino-butyl-fluorophenylsulfonyl chloridebenzenesulfonamide202.2-(2-Amino-butylamino)-2-Methoxy-5-methyl-N-475.1 M Hthiazol-5-yl-o-tolyl-methanone;4-5-(2-methyl-hydrochloride and 2-methoxy-5-benzoyl)-thiazol-2-methylphenylsulfonyl chlorideylamino-butyl-benzenesulfonamide203.2-(2-Amino-pentylamino)-Thiophene-3-sulfonic448.1 M Hthiazol-5-yl-o-tolyl-methanone;acid 5-5-(2-methyl-hydrochloride and 2-benzoyl)-thiazol-2-thiophenesulfonylchlorideylamino-pentyl-amide204.2-(2-Amino-pentylamino)-5-Fluoro-2-methyl-N-5-474.1 M Hthiazol-5-yl-o-tolyl-methanone;5-(2-methyl-benzoyl)-hydrochloride and 2-methyl-5-thiazol-2-ylamino-fluorophenylsulfonyl chloridepentyl-benzenesulfonamide205.2-(2-Amino-ethylamino)-5-Chloro-2-methoxy-N-464.0 M Hthiazol-5-yl-o-tolyl-methanone;2-5-(2-methyl-hydrochloride and 2-methoxy-5-benzoyl)-thiazol-2-chlorophenylsulfonyl chlorideylamino-ethyl-benzenesulfonamide206.2-(2-Amino-propylamino)-2,4-Difluoro-N-3-5-(2-450.2 M Hthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2,4-2-ylamino-propyl-difluorophenylsulfonyl chloridebenzenesulfonamide207.2-(2-Amino-butylamino)-2,5-Dimethyl-N-4-5-456.3 M Hthiazol-5-yl-o-tolyl-methanone;(2-methyl-benzoyl)-hydrochloride and 2,5-thiazol-2-ylamino-dimethylphenylsulfonyl chloridebutyl-benzenesulfonamide208.2-(2-Amino-butylamino)-2,5-Dimethoxy-N-4-5-488.1 M Hthiazol-5-yl-o-tolyl-methanone;(2-methyl-benzoyl)-hydrochloride and 2,5-thiazol-2-ylamino-dimethoxyphenylsulfonyl chloridebutyl-benzenesulfonamide209.2-(2-Amino-pentylamino)-2,4-Difluoro-N-5-5-(2-478.1 M Hthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 2,4-2-ylamino-pentyl-difluorophenylsulfonylchloridebenzenesulfonamide210.2-(2-Amino-propylamino)-5-Chloro-thiophene-2-454.2 M Hthiazol-5-yl-o-tolyl-methanone;sulfonic acid 3-5-(2-hydrochloride and 5-methyl-benzoyl)-thiazol-chlorothiophenyl-2-2-ylamino-propyl-sulfonylchlorideamide211.2-(2-Amino-butylamino)-4-Methoxy-N-4-5-(2-458.2 M Hthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 4-2-ylamino-butyl-methoxyphenylsulfonylchloridebenzenesulfonamide212.2-(2-Amino-butylamino)-5-Chloro-2-methoxy-N-492.0 M Hthiazol-5-yl-o-tolyl-methanone;4-5-(2-methyl-hydrochloride and 2-methoxy-5-benzoyl)-thiazol-2-chlorophenylsulfonylchlorideylamino-butyl-benzenesulfonamide213.2-(2-Amino-pentylamino)-5-Chloro-thiophene-2-482.1 M Hthiazol-5-yl-o-tolyl-methanone;sulfonic acid 5-5-(2-hydrochloride and 5-methyl-benzoyl)-thiazol-chlorothiophenyl-2-2-ylamino-pentyl-sulfonylchlorideamide214.2-(2-Amino-butylamino)-Thiophene-2-sulfonic434.2 M Hthiazol-5-yl-o-tolyl-methanone;acid 4-5-(2-methyl-hydrochloride and 2-benzoyl)-thiazol-2-thiophenylsulfonyl chlorideylamino-butyl-amide215.2-(2-Amino-butylamino)-3-Methoxy-N-4-5-(2-458.2 M Hthiazol-5-yl-o-tolyl-methanone;methyl-benzoyl)-thiazol-hydrochloride and 3-methoxy-2-ylamino-butyl-phenylsulfonylchloridebenzenesulfonamide216.2-(2-Amino-butylamino)-N-4-5-(2-Methyl-512.1 M Hthiazol-5-yl-o-tolyl-methanone;benzoyl)-thiazol-2-hydrochloride and 4-ylamino-butyl-4-trifluoromethyloxy-trifluoromethoxy-phenylsulfonylchloridebenzenesulfonamide217.2-(3-Methylamino-Thiophene-2-sulfonic434.2 M Hpropylamino)-thiazol-5-yl-o-acid methyl-3-5-(2-tolyl-methanone; hydrochloridemethyl-benzoyl)-thiazol-and 2-thiophenylsulfonyl chloride2-ylamino-propyl-amide218.2-(3-Methylamino-3-Methoxy-N-methyl-N-458.2 M Hpropylamino)-thiazol-5-yl-o-3-5-(2-methyl-tolyl-methanone; hydrochloridebenzoyl)-thiazol-2-and 3-methoxyphenylsulfonylylamino-propyl-chloridebenzenesulfonamide219.2-(3-Methylamino-2-Chloro-N-methyl-N-530.0 M Hpropylamino)-thiazol-5-yl-o-3-5-(2-methyl-tolyl-methanone; hydrochloridebenzoyl)-thiazol-2-and 2-chloro-4-ylamino-propyl-4-trifluoromethylphenylsulfonyltrifluoromethyl-chloridebenzenesulfonamide220.2-(3-Methylamino-2,N-Dimethyl-N-3-5-442.2 M Hpropylamino)-thiazol-5-yl-o-(2-methyl-benzoyl)-tolyl-methanone; hydrochloridethiazol-2-ylamino-and 2-methylphenylsulfonylpropyl-chloridebenzenesulfonamide221.2-(3-Methylamino-5-Fluoro-2,N-dimethyl-460.2 M Hpropylamino)-thiazol-5-yl-o-N-3-5-(2-methyl-tolyl-methanone; hydrochloridebenzoyl)-thiazol-2-and 2-methyl-5-ylamino-propyl-fluorophenylsulfonyl chloridebenzenesulfonamide222.2-(3-Methylamino-2-Chloro-N-methyl-N-530.0 M Hpropylamino)-thiazol-5-yl-o-3-5-(2-methyl-tolyl-methanone; hydrochloridebenzoyl)-thiazol-2-and 2-chloro-5-ylamino-propyl-5-trifluoromethylphenylsulfonyltrifluoromethyl-chloridebenzenesulfonamide223.2-(3-Methylamino-4-Fluoro-N-methyl-N-446.1 M Hpropylamino)-thiazol-5-yl-o-3-5-(2-methyl-tolyl-methanone; hydrochloridebenzoyl)-thiazol-2-and 4-fluorophenylsulfonylylamino-propyl-chloridebenzenesulfonamide224.2-(3-Methylamino-2,4-Difluoro-N-methyl-464.3 M Hpropylamino)-thiazol-5-yl-o-N-3-5-(2-methyl-tolyl-methanone; hydrochloridebenzoyl)-thiazol-2-and 2,4-difluorophenylsulfonylylamino-propyl-chloridebenzenesulfonamide225.2-(3-Methylamino-2-Fluoro-N-methyl-N-446.1 M Hpropylamino)-thiazol-5-yl-o-3-5-(2-methyl-tolyl-methanone; hydrochloridebenzoyl)-thiazol-2-and 2-fluorophenylsulfonylylamino-propyl-chloridebenzenesulfonamide226.2-(3-Methylamino-5-Chloro-thiophene-2-468.0 M Hpropylamino)-thiazol-5-yl-o-sulfonic acid methyl-3-tolyl-methanone; hydrochloride5-(2-methyl-benzoyl)-and 5-chlorothiophenyl-2-thiazol-2-ylamino-sulfonylchloridepropyl-amide227.2-(3-Methylamino-3-Fluoro-N-methyl-N-446.1 M Hpropylamino)-thiazol-5-yl-o-3-5-(2-methyl-tolyl-methanone; hydrochloridebenzoyl)-thiazol-2-and 3-fluorophenylsulfonylylamino-propyl-chloridebenzenesulfonamide228.2-(3-Methylamino-2-Methoxy-5,N-472.1 M Hpropylamino)-thiazol-5-yl-o-dimethyl-N-3-5-(2-tolyl-methanone; hydrochloridemethyl-benzoyl)-thiazol-and 2-methoxy-5-2-ylamino-propyl-methylphenylsulfonyl chloridebenzenesulfonamide228.2-(3-Methylamino-4-Chloro-N-methyl-N-462.1 M Hpropylamino)-thiazol-5-yl-o-3-5-(2-methyl-tolyl-methanone; hydrochloridebenzoyl)-thiazol-2-and 4-chlorophenylsulfonylylamino-propyl-chloridebenzenesulfonamide230.2-(3-Methylamino-2,5,N-Trimethyl-N-3-456.3 M Hpropylamino)-thiazol-5-yl-o-5-(2-methyl-benzoyl)-tolyl-methanone; hydrochloridethiazol-2-ylamino-and 2,5-methylphenylsulfonylpropyl-chloridebenzenesulfonamide231.2-(3-Methylamino-N-Methyl-N-3-5-(2-472.9 M Hpropylamino)-thiazol-5-yl-o-methyl-benzoyl)-thiazol-tolyl-methanone; hydrochloride2-ylamino-propyl-4-and 4-nitrophenylsulfonylnitro-chloridebenzenesulfonamide232.2-(3-Methylamino-4-Methoxy-N-methyl-N-458.2 M Hpropylamino)-thiazol-5-yl-o-3-5-(2-methyl-tolyl-methanone; hydrochloridebenzoyl)-thiazol-2-and 4-methoxyphenylsulfonylylamino-propyl-chloridebenzenesulfonamide233.2-(3-Methylamino-5-Chloro-2-methoxy-N-492.1 M Hpropylamino)-thiazol-5-yl-o-methyl-N-3-5-(2-tolyl-methanone; hydrochloridemethyl-benzoyl)-thiazol-and 2-methoxy-5-2-ylamino-propyl-chlorophenylsulfonyl chloridebenzenesulfonamide

Example A 0621 A compound of formula I can be used in a manner known per se as the active ingredient for the production of tablets of the following composition: 3Per tabletActive ingredient200 mgMicrocrystalline cellulose155 mgCorn starch25 mgTalc25 mgHydroxypropylmethylcellulose20 mg425 mg

Example B 0622 A compound of formula I can be used in a manner known per se as the active ingredient for the production of capsules of the following composition: 4Per capsuleActive ingredient100.0 mgCorn starch20.0 mgLactose95.0 mgTalc4.5 mgMagnesium stearate0.5 mg220.0 mg

Example C 0623 Tablets containing the following ingredients can be manufactured in a conventional manner: 5IngredientsPer tabletCompound of formula I10.0-100.0 mgLactose125.0 mgMaize starch75.0 mgTalc4.0 mgMagnesium stearate1.0 mg

Example D 0624 Capsules containing the following ingredients can be manufactured in a conventional manner: 6IngredientsPer capsuleCompound of formula I25.0 mgLactose150.0 mgMaize starch20.0 mgTalc5.0 mg

Example E 0625 Injection solutions can have the following composition: 7Compound of formula I3.0mgGelatin150.0mgPhenol4.7mgWater for injection solutionsad 1.0ml