Heteroaromatic glucokinase activators

1. A compound comprising an amide of the formula:

wherein, the * indicates an asymmetric carbon atom,

R 1 and R 2 are independently hydrogen, halo, amino, hydroxyamino, cyano, nitro, lower alkyl, —OR 5 , —C(O)OR 6 , perfluoro-lower alkyl, lower alkyl thio, perfluoro-lower alkyl thio, lower alkyl sulfonyl, lower alkoxy lower alkyl sulfonyl, perfluoro-lower alkyl sulfonyl, lower alkyl sulfinyl, or sulfonamido; R 3 is cycloalkyl having from 3 to 7 carbon atoms or lower alkyl having from 2 to 4 carbon atoms;

R 4 is an unsubstituted or mono-substituted thiazole or thiadiazole connected by a ring carbon atom to the amide group shown, with one heteroatom being nitrogen which is adjacent to the connecting ring carbon atom; said mono-substituted thiazole or thiadiazole being monosubstituted at a position on a ring carbon atom other than adjacent to said connecting carbon atom with a substituent selected from the group consisting of lower alkyl, halo, nitro, cyano, perfluoro-lower alkyl, oxo, —(CH 2 ) n —OR 7 , —(CH 2 ) n —C(O)—OR 7 , —(CH 2 )—C(O)—NH—R 7 , —C(O)C(O)—OR 7 , or —(CH 2 ) n —NHR 7 ;

n is 0, 1, 2, 3 or 4;

R 5 is hydrogen, lower alkyl, or perfluoro-lower alkyl; R 6 is lower alkyl; and R 7 is hydrogen or lower alkyl;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein the amide is the R configuration at the asymmetric carbon shown.

3. The compound of claim 1 , wherein R 3 is cycloalkyl having from 3 to 7 carbon atoms.

4. The compound of claim 3 , wherein R 3 is cyclopentyl.

5. The compound of claim 4 , wherein R 4 is unsubstituted thiazole.

6. The compound of claim 5 , wherein one of R 1 and R 2 is hydrogen, halo, perfluoro-lower alkyl and the other of said R 1 and R 2 is halo, nitro or perfluoro-lower alkyl.

7. The compound of claim 6 , wherein said amide is 2-(3-chloro-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.

8. The compound of claim 6 , wherein said amide is 2-(4-bromo-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.

9. The compound of claim 6 , wherein said amide is 2-(4-chloro-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.

10. The compound of claim 6 , wherein said amide is 3-cyclopentyl-2-(3,4-dichlorophenyl)-N-thiazol-2-yl-propionamide.

11. The compound of claim 6 , wherein said amide is 3-cyclopentyl-N-thiazol-2-yl-2-(4-trifluoromethyl-phenyl)-propionamide.

12. The compound of claim 6 , wherein said amide is 3-cyclopentyl-2-(3-fluoro-4-trifluoromethyl-phenyl)-N-thiazol-2-yl-propionamide.

13. The compound of claim 6 , wherein said amide is 3-cyclopentyl-2-(4-fluoro-3-trifluoromethyl-phenyl)-N-thiazol-2-yl-propionamide.

14. The compound of claim 6 , wherein said amide is 3-cyclopentyl-N-thiazol-2-yl-2-(3-trifluoromethyl-phenyl)-propionamide.

15. The compound of claim 6 , wherein said amide is 3-cyclopentyl-2(R)-(3,4-dichloro-phenyl)-N-thiazol-2-yl-propionamide.

16. The compound of claim 5 , wherein one of R 1 and R 2 is amino, nitro, halo or hydrogen and the other of said R 1 and R 2 is amino, cyano or nitro.

17. The compound of claim 16 , wherein said amide is 3-cyclopentyl-2-(4-nitrophenyl)-N-thiazol-2-yl-propionamide.

18. The compound of claim 16 , wherein said amide is 2-(4-amino-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.

19. The compound of claim 16 , wherein said amide is 2-(3-amino-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.

20. The compound of claim 16 , wherein said amide is 2-(4-chloro-3-nitro-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.

21. The compound of claim 16 , wherein said amide is 2-(4-cyano-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.

22. The compound of claim 16 , wherein said amide is 3-cyclopentyl-2-(3-nitrophenyl)-N-thiazol-2-yl-propionamide.

23. The compound of claim 5 , wherein one of R 1 and R 2 is lower alkylthio, perfluoro-lower alkyl thio, halo or hydrogen and the other is perfluoro-lower alkylthio, lower alkylsulfinyl or lower alkylthio.

24. The compound of claim 23 , wherein said amide is 3-cyclopentyl-N-thiazol-2-yl-2-(4-trifluoromethylsulfanyl-phenyl)-propionamide.

25. The compound of claim 23 , wherein said amide is 3-cyclopentyl-2-(4-methylsulfanyl-phenyl)-N-thiazol-2-yl-propionamide.

26. The compound of claim 23 , wherein said amide is 3-cyclopentyl-2-(4-methylsulfanyl-3-trifluoromethyl-phenyl)-N-thiazol-2-yl-propionamide.

27. The compound of claim 23 , wherein said amide is 3-cyclopentyl-2-(4-methanesulfinyl-phenyl)-N-thiazol-2-yl-propionamide.

28. The compound of claim 5 , wherein one of R 1 and R 2 is lower alkyl sulfonyl, hydrogen, nitro, amino, cyano, hydroxylamino, sulfonamido or halo, and the other of said R 1 and R 2 is lower alkyl sulfonyl.

29. The compound of claim 28 , wherein said amide is 3-cyclopentyl-2-(4-methanesulfonyl-phenyl)-N-thiazol-2-yl-propionamide.

30. The compound of claim 28 , wherein said amide is 3-cyclopentyl-2-(4-methanesulfonyl-3-nitrophenyl)-N-thiazol-2-yl-propionamide.

31. The compound of claim 28 , wherein said amide is 2-(3-amino-4-methanesulfonyl-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.

32. The compound of claim 28 , wherein said amide is 3-cyclopentyl-2-(3-hydroxyamino-4-methanesulfonyl-phenyl)-N-thiazol-2-yl-propionamide.

33. The compound of claim 28 , wherein said amide is 2-(3-cyano-4-methanesulfonyl-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.

34. The compound of claim 28 , wherein said amide is 3-cyclopentyl-2-(4-ethanesulfonyl-phenyl)-N-thiazol-2-yl-propionamide.

35. The compound of claim 28 , wherein said amide is 2-(3,4-bis-methanesulfonyl-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.

36. The compound of claim 28 , wherein said amide is 3-cyclopentyl-2-(4-sulfamoyl-phenyl)-N-thiazol-2-yl-propionamide.

37. The compound of claim 28 , wherein said amide is 2-[4-(butane-1-sulfonyl)-phenyl]-3-cyclopentyl-N-thiazol-2-yl-propionamide.

38. The compound of claim 28 , wherein said amide is 3-cyclopentyl-2-[4-(propane-1-sulfonyl)-phenyl]-N-thiazol-2-yl-propionamide.

39. The compound of claim 28 , wherein said amide is (2R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N-thiazol-2-yl-propionamide.

40. The compound of claim 5 , wherein one of R 1 and R 2 is lower alkyl sulfonyl, and the other is halo or perfluoro-lower alkyl.

41. The compound of claim 40 , wherein said amide is 3-cyclopentyl-2-(3-fluoro-4-methanesulfonyl-phenyl)-N-thiazol-2-yl-propionamide.

42. The compound of claim 40 , wherein said amide is 3-cyclopentyl-2(R)-(4-methanesulfonyl-3-trifluoromethyl-phenyl)-N-thiazol-2-yl-propionamide.

43. The compound of claim 40 , wherein said amide is 3-cyclopentyl-2-(4-methanesulfonyl-3-trifluoromethyl-phenyl)-N-thiazol-2-yl-propionamide.

44. The compound of claim 40 , wherein said amide is 2(R)-(3-chloro-4-methanesulfonyl-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.

45. The compound of claim 40 , wherein said amide is 2-[3-chloro-4-methanesulfonyl-phenyl]-3-cyclopentyl-N-thiazol-2-yl-propionamide.

46. The compound of claim 40 , wherein said amide is 2-(3-bromo-4-methanesulfonyl-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.

47. The compound of claim 5 , wherein one of R 1 and R 2 is perfluoro-lower alkyl sulfonyl or hydrogen and the other is perfluoro-lower alkyl sulfonyl.

48. The compound of claim 47 , wherein said amide is 3-cyclopentyl-N-thiazol-2-yl-2-(4-trifluoromethanesulfonyl-phenyl)-propionamide.

49. The compound of claim 47 , wherein said amide is 3-cyclopentyl-N-thiazol-2-yl-2-(3-trifluoromethanesulfonyl-phenyl)-propionamide.

50. The compound of claim 5 , wherein one of R 1 and R 2 is —OR 5 , or —C(O)—OR 6 and the other of said R 1 and R 2 is hydrogen or —OR 5 ; and R 5 and R 6 are as above.

51. The compound of claim 50 , wherein said amide is 3-cyclopentyl-N-thiazol-2-yl-2-(4-trifluoromethoxy-phenyl)-propionamide.

52. The compound of claim 50 , wherein said amide is 3-cyclopentyl-2-(3-methoxy-phenyl)-N-thiazol-2-yl-propionamide.

53. The compound of claim 50 , wherein said amide is 3-cyclopentyl-2-(3-hydroxy-phenyl)-N-thiazol-2-yl-propionamide.

54. The compound of claim 50 , wherein said amide is 3-cyclopentyl-2-(3,4-dimethoxy-phenyl)-N-thiazol-2-yl-propionamide.

55. The compound of claim 50 , wherein said amide is 3-cyclopentyl-2-(3,4-dihydroxy-phenyl)-N-thiazol-2-yl-propionamide.

56. The compound of claim 50 , wherein said amide is 3-cyclopentyl-2-(4-methoxy-phenyl)-N-thiazol-2-yl-propionamide.

57. The compound of claim 50 , wherein said amide is 3-cyclopentyl-2-(4-hydroxy-phenyl)-N-thiazol-2-yl-propionamide.

58. The compound of claim 50 , wherein said amide is 4-[2-cyclopentyl-1-(thiazol-2-ylcarbamoyl)-ethyl]-benzoic acid methyl ester.

59. The compound of claim 5 , wherein one of R 1 and R 2 is —OR 5 and the other is halo.

60. The compound of claim 59 , wherein said amide is 3-cyclopentyl-2-(3-fluoro-4-methoxy-phenyl)-N-thiazol-2-yl-propionamide.

61. The compound of claim 59 , wherein said amide is 3-cyclopentyl-2-(3-fluoro-4-hydroxy-phenyl)-N-thiazol-2-yl-propionamide.

62. The compound of claim 5 , wherein one of R 1 and R 2 is hydrogen and the other is lower alkoxy lower alkyl sulfonyl.

63. The compound of claim 62 , wherein said amide is 3-cyclopentyl-2-(4-methoxymethanesulfonyl-phenyl)-N-thiazol-2-yl-propionamide.

64. The compound of claim 4 wherein R 4 is a mono-substituted thiazole with said substituent.

65. The compound of claim 64 , wherein said substituent is —(CH 2 ) n —OR 7 and n and R 7 are as above.

66. The compound of claim 65 , wherein one of R 1 and R 2 is halo and the other of said R 1 and R 2 is hydrogen or halo.

67. The compound of claim 66 , wherein said amide is 3-cyclopentyl-2-(3,4-dichlorophenyl)-N-(5-hydroxymethyl-thiazol-2-yl)-propionamide.

68. The compound of claim 66 , wherein said amide is 3-cyclopentyl-2-(3,4-dichlorophenyl)-N-[4-(2-hydroxyethyl)-thiazol-2-yl]-propionamide.

69. The compound of claim 66 , wherein said amide is 2-(4-chloro-phenyl)-3-cyclopentyl-N-(5-hydroxymethyl-thiazol-2-yl)-propionamide.

70. The compound of claim 66 , wherein said amide is 3-cyclopentyl-2-(3,4-dichlorophenyl)-N-(4-hydroxymethyl-thiazol-2-yl)-propionamide.

71. The compound of claim 65 , wherein one of R 1 and R 2 is lower alkyl sulfonyl, and the other of said R 1 and R 2 is lower alkyl sulfonyl or hydrogen.

72. The compound of claim 71 ,wherein said amide is 3-cyclopentyl-N-(4-hydroxymethyl-thiazol-2-yl)-2-(4-methanesulfonyl-phenyl)-propionamide.

73. The compound of claim 71 ,wherein said amide is 3-cyclopentyl-N-[4-(2-hydroxyethyl)-thiazol-2-yl]-2-(4-methanesulfonyl-phenyl)-propionamide.

74. The compound of claim 64 , wherein said substituent is lower alkyl.

75. The compound of claim 74 wherein one of R 1 and R 2 is hydrogen or halo and the other of said R 1 and R 2 is halo.

76. The compound of claim 75 , wherein said amide is 3-cyclopentyl-2-(3,4-dichlorophenyl)-N-(4-methyl-thiazol-2-yl)-propionamide.

77. The compound of claim 75 , wherein said amide is 3-cyclopentyl-2-(3,4-dichlorophenyl)-N-(5-methyl-thiazol-2-yl)-propionamide.

78. The compound of claim 74 wherein one of R 1 and R 2 is lower alkyl sulfonyl and the other is hydrogen or halo.

79. The compound of claim 78 , wherein said amide is 3-cyclopentyl-2(R)-(4-methanesulfonyl-phenyl)-N-(4-methyl-thiazol-2-yl)-propionamide.

80. The compound of claim 78 , wherein said amide is 3-cyclopentyl-2(R)-(4-methanesulfonyl-phenyl)-N-(5-methyl-thiazol-2-yl)-propionamide.

81. The compound of claim 78 , wherein said amide is 2(R)-(3-chloro-4-methanesulfonyl-phenyl)-3-cyclopentyl-N-(5-methyl-thiazol-2-yl)-propionamide.

82. The compound of claim 78 , wherein said amide is 2(R)-(3-chloro-4-methanesulfonyl-phenyl)-3-cyclopentyl-N-(4-methyl-thiazol-2-yl)-propionamide.

83. The compound of claim 64 , wherein said substituent is —(CH 2 ) n —C(O)—OR 7 wherein n is 0 or 1 and R 7 is hydrogen, or lower alkyl.

84. The compound of claim 83 , wherein one of R 1 and R 2 is hydrogen and the other is halo.

85. The compound of claim 84 , wherein said amide is {2-[2-(3-chloro-phenyl)-3-cyclopentyl-propionylamino]-thiazol-4-yl}-acetic acid ethyl ester.

86. The compound of claim 84 , wherein said amide is {2-[2-(3-chloro-phenyl)-3-cyclopentyl-propionylamino]-thiazol-4-yl}-acetic acid methyl ester.

87. The compound of claim 84 , wherein said amide is 2-[2-(3-chloro-phenyl)-3-cyclopentyl-propionylamino]-thiazole-4-carboxylic acid methyl ester.

88. The compound of claim 84 , wherein said amide is 2-[2-(3-chloro-phenyl)-3-cyclopentyl-propionylamino]-thiazole-4-carboxylic acid ethyl ester.

89. The compound of claim 84 , wherein said amide is {2-[2-(4-chloro-phenyl)-3-cyclopentyl-propionylamino]-thiazol-4-yl}-acetic acid ethyl ester.

90. The compound of claim 84 , wherein said amide is 2-[2-(4-chloro-phenyl)-3-cyclopentyl-propionylamino]-thiazole-4-carboxylic acid methyl ester.

91. The compound of claim 84 , wherein said amide is 2-[2-(4-chloro-phenyl)-3-cyclopentyl-propionylamino]-thiazole-4-carboxylic acid ethyl ester.

92. The compound of claim 84 , wherein said amide is {2-[2-(4-chloro-phenyl)-3-cyclopentyl-propionylamino]-thiazol-4-yl}-acetic acid methyl ester.

93. The compound of claim 83 , wherein one of R 1 or R 2 is halo and the other is perfluoro-lower alkyl.

94. The compound of claim 93 wherein said amide is {2-[3-cyclopentyl-2-(4-fluoro-3-trifluoromethyl-phenyl)-propionylamino]-thiazol-4-yl}-acetic acid ethyl ester.

95. The compound of claim 83 , wherein R 1 and R 2 are each independently halo.

96. The compound of claim 95 , wherein said amide is {2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]-thiazol-4-yl}-acetic acid.

97. The compound of claim 95 , wherein said amide is {2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]-thiazol-4-yl}-acetic acid ethyl ester.

98. The compound of claim 95 , wherein said amide is 2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]-thiazole-5-carboxylic acid.

99. The compound of claim 95 , wherein said amide is 2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]-thiazole-4-carboxylic acid.

100. The compound of claim 95 , wherein said amide is {2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]-thiazol-4-yl} -acetic acid methyl ester.

101. The compound of claim 95 , wherein said amide is (2R)-2-[3-cyclopentyl-2-(3,4-dichloro-phenyl)-propionylamino]-thiazole-4-carboxylic acid methyl ester.

102. The compound of claim 95 , wherein said amide is 2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]-thiazole-5-carboxylic acid methyl ester.

103. The compound of claim 95 , wherein said amide is 2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]-thiazole-5-carboxylic acid ethyl ester.

104. The compound of claim 95 , wherein said amide is 2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]-thiazole-4-carboxylic acid ethyl ester.

105. The compound of claim 95 , wherein said amide is 2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]-thiazole-4-carboxylic acid methyl ester.

106. The compound of claim 83 , wherein one of R 1 or R 2 is nitro, amino or hydrogen and the other of said R 1 and R 2 is nitro or amino.

107. The compound of claim 106 , wherein said amide is {2-[3-cyclopentyl-2-(4-nitro-phenyl)-propionylamino]-thiazol-4-yl}-acetic acid ethyl ester.

108. The compound of claim 106 , wherein said amide is {2-[3-cyclopentyl-2-(4-nitro-phenyl)-propionylamino]-thiazol-4-yl}-acetic acid methyl ester.

109. The compound of claim 106 , wherein said amide is 2-[3-cyclopentyl-2-(4-nitro-phenyl)-propionylamino]-thiazole-4-carboxylic acid methyl ester.

110. The compound of claim 106 , wherein said amide is 2-[3-cyclopentyl-2-(4-nitro-phenyl)-propionylamino]-thiazole-4-carboxylic acid ethyl ester.

111. The compound of claim 106 , wherein said amide is {2-[2-(4-amino-phenyl)-3-cyclopentyl-propionylamino]-thiazol-4-yl}-acetic acid methyl ester.

112. The compound of claim 106 , wherein said amide is 2-[2-(4-amino-phenyl)-3-cyclopentyl-propionylamino]-thiazole-4-carboxylic acid methyl ester.

113. The compound of claim 83 , wherein one of R 1 and R 2 is lower alkyl sulfonyl, perfluoro-lower alkyl, halo or hydrogen and the other of said R 1 and R 2 is lower alkyl sulfonyl.

114. The compound of claim 113 , wherein said amide is (2-[3-cyclopentyl-2-(4-methanesulfonyl-phenyl)-propionylamino]-thiazole-4-carboxylic acid ethyl ester.

115. The compound of claim 113 , wherein said amide is (2-[3-cyclopentyl-2-(4-methanesulfonyl-phenyl)-propionylamino]-thiazole-4-carboxylic acid methyl ester.

116. The compound of claim 113 , wherein said amide is {2-[3-cyclopentyl-2-(4-methanesulfonyl-phenyl)-propionylamino]-thiazol-4-yl}-acetic acid ethyl ester.

117. The compound of claim 113 , wherein said amide is {2-[3-cyclopentyl-2-(4-methanesulfonyl-phenyl)-propionylamino]-thiazol-4-yl}-4-acetic acid methyl ester.

118. The compound of claim 113 , wherein said amide is {2-[3-cyclopentyl-2-(4-methanesulfonyl-3-trifluoromethyl-phenyl)-propionylamino]-thiazol-4-yl}-acetic acid methyl ester.

119. The compound of claim 113 , wherein said amide is 2-[3-cyclopentyl-2-(4-methanesulfonyl-3-trifluoromethyl-phenyl)-propionylamino]-thiazole-4-carboxylic acid methyl ester.

120. The compound of claim 83 , wherein one of R1 and R2 is perfluoro-lower lkyl sulfonyl and the other is hydrogen, halo, or perfluoro-lower alkyl.

121. The compound of claim 120 , wherein said amide is 2-[3-cyclopentyl-2-(4-trifluoromethanesulfonyl-phenyl)-propionylamino]-thiazole-4-carboxylic acid methyl ester.

122. The compound of claim 120 , wherein said amide is 2-[3-cyclopentyl-2-(4-trifluoromethanesulfonyl-phenyl)-propionylamino]-thiazole-4-carboxylic acid ethyl ester.

123. The compound of claim 120 , wherein said amide is 2-[3-cyclopentyl-2-(4-trifluoromethanesulfonyl-phenyl)-propionylamino]-thiazole-4-acetic acid methyl ester.

124. The compound of claim 120 , wherein said amide is {2-[3-cyclopentyl-2-(4-trifluoromethanesulfonyl-phenyl)-propionylamino]-thiazole-4-yl}-acetic acid ethyl ester.

125. The compound of claim 64 , wherein said substituent is —C(O)—C(O)—OR 7 wherein R 7 is as above.

126. The compound of claim 125 , wherein one of R 1 and R 2 are hydrogen and the other of said R 1 and R 2 is nitro or amino.

127. The compound of claim 126 , wherein said amide is {2-[3-cyclopentyl-2-(4-nitro-phenyl)-propionylamino]-thiazol-4-yl}-oxo-acetic acid ethyl ester.

128. The compound of claim 125 , wherein one of R 1 and R 2 is halo or perfluoro-lower alkyl and the other of said R 1 and R 2 is perfluoro-lower alkyl, halo or hydrogen.

129. The compound of claim 128 , wherein said amide is {2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]thiazol-5-yl}-oxo-acetic ethyl ester.

130. The compound of claim 128 , wherein said amide is {2-[3-cyclopentyl-2-(4-fluoro-3-trifluoromethyl-phenyl)-propionylamino]-thiazol-4-yl}-oxo-acetic acid ethyl ester.

131. The compound of claim 128 , wherein said amide is {2-[3-cyclopentyl 2-(3,4-dichlorophenyl)-propionylamino]-thiazol-4-yl}-oxo-acetic acid ethyl ester.

132. The compound of claim 128 , wherein said amide is (2R)-{2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]-thiazol-5-yl}-oxo-acetic acid ethyl ester.

133. The compound of claim 128 , wherein said amide is (2R)-{2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]-thiazol-4-yl}-oxo-acetic acid ethyl ester.

134. The compound of claim 125 , wherein said one of R 1 and R 2 is hydrogen or halo and the other of said R 1 and R 2 is lower alkyl sulfonyl.

135. The compound of claim 134 , wherein said compound is {2-[2-(3-chloro-4-methanesulfonyl-phenyl)-3-cyclopentyl-propionylamino]-thiazol-4-yl}-oxo-acetic acid ethyl ester.

136. The compound of claim 64 , wherein said substitutent is nitro.

137. The compound of claim 136 wherein R 1 and R 2 are each independently halo.

138. The compound of claim 136 , wherein said amide is 3-cyclopentyl-2-(3,4-dichlorophenyl)-N-(5-nitro-thiazol-2-yl)-propionamide.

139. The compound of claim 64 , wherein said substituent is —(CH 2 ) n —C(O)—NH—R 7 and n and R 7 are as in claim 1 .

140. The compound of claim 139 wherein one of R 1 and R 2 is halo or lower alkyl sulfonyl and the other is halo or hydrogen.

141. The compound of claim 140 , wherein said amide is 2-[3-cyclopentyl-2-(4-methanesulfonyl-phenyl)-propionylamino]-thiazole-5-carboxylic acid amide.

142. The compound of claim 140 , wherein said amide is 2-[3-cyclopentyl-2-(3,4-dichlorophenyl)-propionylamino]-thiazole-4-carboxylic acid amide.

143. The compound of claim 64 , wherein said substituent is halo.

144. The compound of claim 143 , wherein one of R 1 and R 2 is halo or hydrogen and the other is lower alkyl sulfonyl.

145. The compound of claim 144 , wherein said amide is N-(5-chloro-thiazol-2-yl)-3-cyclopentyl-2-(4-methanesulfonyl-phenyl)-propionamide.

146. The compound of claim 144 , wherein said amide is N-(5-chloro-thiazol-2-yl)-3-cyclopentyl-2(R)-(4-methanesulfonyl-phenyl)-propionamide.

147. The compound of claim 144 , wherein said amide is N-(5-bromo-thiazol-2-yl)-3-cyclopentyl-2-(4-methanesulfonyl-phenyl)-propionamide.

148. The compound of claim 144 , wherein said amide is N-(5-bromo-thiazol-2-yl)-3-cyclopentyl-2(R)-(4-methanesulfonyl-phenyl)-propionamide.

149. The compound of claim 144 , wherein said amide is N-(5-bromo-thiazol-2-yl)-2(R)-(3-chloro-4-methanesulfonyl-phenyl)-3-cyclopentyl-propionamide.

150. The compound of claim 4 wherein R 4 is an unsubstituted thiadiazolyl ring.

151. The compound of claim 150 , wherein one of R 1 or R 2 is halo, nitro or perfluoro-lower alkyl or lower alkyl sulfonyl and the other of said R 1 and R 2 is hydrogen or halo.

152. The compound of claim 151 , wherein said amide is 3-cyclopentyl-2-(3,4-dichlorophenyl)-N-[1,3,4]thiadiazol-2-yl-propionamide.

153. The compound of claim 1 , wherein R 3 is cyclohexyl.

154. The compound of claim 153 , wherein R 4 is unsubstituted thiazolyl.

155. The compound of claim 1541, wherein one of R 1 and R 2 is halo, lower alkyl sulfonyl, perfluoro-lower alkyl sulfonyl, perfluoro-lower alkyl, and the other of said R 1 and R 2 is halo, perfluoro-lower alkyl or hydrogen.

156. The compound of claim 155 , wherein said amide is 3-cyclohexyl-2-[4-methanesulfonyl-phenyl]-N-thiazol-2-yl-propionamide.

157. The compound of claim 155 , wherein said amide is 3-cyclohexyl-2-[4-methanesulfonyl-3-trifluoromethyl-phenyl]-N-thiazol-2-yl-propionamide.

158. The compound of claim 1 , wherein R 3 is cycloheptyl.

159. The compound of claim 155 , wherein R 4 is unsubstituted thiazolyl.

160. The compound of claim 158 , wherein one of R 1 and R 2 is halo, lower alkyl sulfonyl, perfluoro-lower alkyl sulfonyl, perfluoro-lower alkyl, and the other of said R 1 and R 2 is halo, perfluoro-lower alkyl or hydrogen.

161. The compound of claim 160 , wherein said amide is 3-cycloheptyl-2-(4-methanesulfonyl-phenyl)-N-thiazol-2-yl-propionamide.