Claims
- 1. An amide selected from the group consisting of a compound of the formula
- 2. The amide of claim 1 wherein said compound is
- 3. The amide of claim 2 wherein z is 0.
- 4. The amide of claim 3 wherein R1 is cyclopentyl.
- 5. The amide of claim 4 wherein R is aryl.
- 6. The amide of claim 5 wherein R4 is a substituted or unsubstituted five-membered heteroaromatic ring.
- 7. The amide of claim 6 wherein said heteroaromatic ring defined by R4 is an unsubstituted thiazolyl.
- 8. The amide of claim 7 wherein said compound is 2-biphenyl-4-yl-3-cyclopentyl-N-thiazol-2-yl-propionamide.
- 9. The amide of claim 8 wherein said compound is (2R)-2-biphenyl-4-yl-3-cyclopentyl-N-thiazol-2-yl-propionamide.
- 10. The amide of claim 6 wherein said compound is 3-cyclopentyl-2-(4-naphthalen-1-yl-phenyl)-N-thiazol-2-yl-propionamide.
- 11. The amide of claim 6 wherein R4 is thiazolyl which is substituted with
- 12. The amide of claim 11 wherein said compound is [2-(2-biphenyl-4-yl-3-cyclopentyl-propionylamino)-thiazol-4-yl]-acetic acid methyl ester.
- 13. The amide of claim 11 wherein said compound is [2-(2-biphenyl-4-yl-3-cyclopentyl-propionylamino)-thiazol-4-yl]-acetic acid ethyl ester.
- 14. The amide of claim 11 wherein said compound is 2-(2-biphenyl-4-yl-3-cyclopentyl-propionylamino)-thiazole-4-carboxylic acid ethyl ester.
- 15. The amide of claim 11 wherein said compound is 2-(2-biphenyl-4-yl-3-cyclopentyl-propionylamino)-thiazole-4-carboxylic acid methyl ester.
- 16. The amide of claim 11 wherein said compound is {2-[3-cyclopentyl-2-(4-naphthalen-1-yl-phenyl)-propionylamino]-thiazol-4-yl}-acetic acid methyl ester.
- 17. The amide of claim 11 wherein said compound is {2-[3-cyclopentyl-2-(4-naphthalen-1-yl-phenyl)-propionylamino]-thiazol-4-yl}-acetic acid ethyl ester.
- 18. The amide of claim 11 wherein said compound is 2-[3-cyclopentyl-2-(4-naphthalen-1-yl-phenyl)-propionylamino]-thiazole-4-carboxylic acid methyl ester.
- 19. The amide of claim 6 wherein R2 is thiazolyl substituted with —(CH2)n—OR6 or
- 20. The amide of claim 19 wherein said compound is [2-(2-biphenyl-4-yl-3-cyclopentyl-propionylamino)-thiazol-4-yl]-oxo-acetic acid ethyl ester.
- 21. The amide of claim 19 wherein said compound is 2-biphenyl-4-yl-3-cyclopentyl-N-(4-hydroxymethyl-thiazol-2-yl)-propionamide.
- 22. The amide of claim 19 wherein said compound is 2-biphenyl-4-yl-3-cyclopentyl-N-[4-(2-hydroxyethyl)-thiazol-2-yl]-propionamide.
- 23. The amide of claim 19 wherein said compound is 3-cyclopentyl-N-[4-(2-hydroxyethyl)-thiazol-2-yl]-2-(4-naphthalen-1-yl-phenyl)-propionamide.
- 24. The amide of claim 19 wherein said compound is 3-cyclopentyl-N-(4-hydroxymethyl-thiazol-2-yl)-2-(4-naphthalen-1-yl-phenyl)-propionamide.
- 25. The amide of claim 5 wherein R4 is unsubstituted pyridinyl.
- 26. The amide of claim 25 wherein said compound is 2-biphenyl-4-yl-3-cyclopentyl-N-pyridin-2-yl-propionamide.
- 27. The amide of claim 25 wherein said compound is 3-cyclopentyl-2-(4-naphthalen-1-yl-phenyl)-N-pyridin-2-yl-propionamide.
- 28. The amide of claim 5 wherein said compound is pyridine monosubstituted with a —(CH2)n—OR6 or
- 29. The compound of claim 28 wherein said compound is 6-(2-biphenyl-4-yl-3-cyclopentyl-propionylamino)-nicotinic acid methyl ester.
- 30. The compound of claim 28 wherein said compound is 6-(2-biphenyl-4-yl-3-cyclopentyl-propionylamino)-nicotinic acid.
- 31. The compound of claim 28 wherein said compound is 2-biphenyl-4-yl-3-cyclopentyl-N-(5-hydroxymethyl-pyridin-2-yl)-propionamide.
- 32. The compound of claim 28 wherein said compound is 6-[3-cyclopentyl-2-(4-naphthalen-1-yl-phenyl)-propionylamino]-nicotinic acid methyl ester.
- 33. The compound of claim 28 wherein said compound is 6-[3-cyclopentyl-2-(4-naphthalen-1-yl-phenyl)-propionylamino]-nicotinic acid.
- 34. The compound of claim 28 wherein said compound is 3-cyclopentyl-N-(5-hydroxymethyl-pyridin-2-yl)-2-(4-naphthalen-1-yl-phenyl)-propionamide.
- 35. The compound of claim 4 wherein R is a heteroaromatic ring containing from 5 to 6 ring members with from 1 to 2 heteroatoms selected form the group consisting of oxygen, sulfur or nitrogen in the ring.
- 36. The compound of claim 35 wherein R4 selected from the group consisting of unsubstituted or monosubstituted pyridinyl or thiazolyl.
- 37. The compound of claim 36 wherein said compound is 3-cyclopentyl-N-thiazol-2-yl-2-(4-thiophen-2-yl-phenyl)-propionamide.
- 38. The compound of claim 36 wherein said compound is 3-cyclopentyl-2-(4-pyridin-3-yl-phenyl)-N-thiazol-2-yl-propionamide.
- 39. The compound of claim 36 wherein said compound is 3-cyclopentyl-2-(4-pyridin-4-yl-phenyl)-N-thiazol-2-yl-propionamide.
- 40. The amide of claim 36 wherein said compound is 3-cyclopentyl-N-pyridin-2-yl-2-(4-pyridin-4-yl-phenyl)-propionamide.
- 41. The amide of claim 36 wherein said compound is 3-cyclopentyl-N-pyridin-2-yl-2-(4-pyridin-3-yl-phenyl)-propionamide.
- 42. The amide of claim 4 wherein R is aryl fused to a heteroaromatic ring containing from 5 to 6 ring members with from 1 to 2 heteroatoms in the ring selected from the group consisting of oxygen, nitrogen or sulfur.
- 43. The amide of claim 42 wherein said compound R4 is thiazolyl.
- 44. The amide of claim 43 wherein said compound is 3-cyclopentyl-2-[4-(1H-indol-5-yl)-phenyl]-N-thiazol-2-yl-propionamide.
- 45. The amide of claim 4 wherein R is a saturated 5- or 6-membered cycloheteroalkyl.
- 46. The amide of claim 45 wherein R4 is thiazole.
- 47. The amide of claim 46 wherein said amide is 3-cyclopentyl-2-(4-morpholin-4-yl-phenyl)-N-thiazol-2-yl-propionamide.
- 48. The amide of claim 2 wherein said compound is the formula
- 49. The amide of claim 48 wherein R is aryl.
- 50. The amide of claim 49 wherein R4 is unsubstituted pyridinyl or thiazolyl.
- 51. The amide of claim 50 wherein said compound is 2-(4-benzyloxy-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.
- 52. The amide of claim 50 wherein said compound is 3-cyclopentyl-2-(4-phenoxy-phenyl)-N-thiazol-2-yl-propionamide.
- 53. The amide of claim 50 wherein said compound is 3-cyclopentyl-2-(4-phenoxy-phenyl)-N-pyridin-2-yl-propionamide.
- 54. The amide of claim 49 wherein R4 is substituted thiazolyl.
- 55. The amide of claim 54 wherein said compound is {2-[3-cyclopentyl-2-(4-phenoxy-phenyl)-propionylamino]-thiazol-4-yl}-acetic acid ethyl ester.
- 56. The amide of claim 54 wherein said compound is 3-cyclopentyl-N-(4-hydroxymethyl-thiazol-2-yl)-2-(4-phenoxy-phenyl)-propionamide.
- 57. The amide of claim 54 wherein said compound is 2-[3-cyclopentyl-2-(4-phenoxy-phenyl)-propionylamino]-thiazole-4-carboxylic acid methyl ester.
- 58. The amide of claim 54 wherein said compound is 3-cyclopentyl-N-[4-(2-hydroxy-ethyl)-thiazol-2-yl]-2-(4-phenoxy-phenyl)-propionamide.
- 59. The amide of claim 54 wherein said compound is {2-[3-cyclopentyl-2-(4-phenoxy-phenyl)-propionylamino]-thiazol-4-yl}-acetic acid.
- 60. The amide of claim 54 wherein said compound is {2-[3-cyclopentyl-2-(4-phenoxy-phenyl)-propionylamino]-thiazol-4-yl}-acetic acid methyl ester.
- 61. The amide of claim 49 wherein R4 is substituted pyridinyl.
- 62. The amide of claim 61 wherein said compound is 3-cyclopentyl-N-(5-methyl-pyridin-2-yl)-2-(4-phenoxy-phenyl)-propionamide.
- 63. The amide of claim 61 wherein said compound is 6-[3-cyclopentyl-2-(4-phenoxy-phenyl)-propionylamino]-nicotinic acid methylester.
- 64. The amide of claim 61 wherein said compound is 6-[3-cyclopentyl-2-(4-phenoxy-phenyl)-propionylamino]-nicotinic acid.
- 65. The amide of claim 61 wherein said compound is 3-cyclopentyl-N-(5-hydroxymethyl-pyridin-2-yl)-2-(4-phenoxy-phenyl)-propionamide.
- 66. The amide of claim 2 wherein said compound has the formula
- 67. The amide of claim 66 wherein R1 is cyclopentyl.
- 68. The amide of claim 67 wherein R4 is unsubstituted or monosubstituted thiazolyl.
- 69. The amide of claim 68 wherein R is aryl.
- 70. The amide of claim 69 wherein said compound is 2-(4-benzenesulfonyl-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.
- 71. The amide of claim 68 wherein R is cycloalkyl.
- 72. The amide of claim 71 wherein said compound is 2-(4-cyclopentanesulfonyl-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.
- 73. The amide of claim 71 wherein said compound is 2-(4-cyclohexanesulfonyl-phenyl)-3-cyclopentyl-N-thiazol-2-yl-propionamide.
- 74. The amide of claim 68 wherein R is a heteroaromatic ring.
- 75. The amide of claim 74 wherein said compound is 3-cyclopentyl-2-[4-(1H-imidazole -2-sulfonyl)-phenyl]-N-thiazol-2-yl-propionamide.
- 76. The amide of claim 1 being the formula:
- 77. The amide of claim 76 wherein R1 is cyclopentyl.
- 78. The amide of claim 77 wherein z is 0.
- 79. The amide of claim 78 wherein R is aryl.
- 80. The amide of claim 79 wherein said compound is (2-biphenyl-4-yl-3-cyclopentyl-propionyl)-urea.
- 81. The amide of claim 79 wherein said compound is 1-(2-biphenyl-4-yl-3-cyclopentyl-propionyl)-3-methyl-urea.
- 82. The amide of claim 79 wherein said compound is 1-[3-cyclopentyl-2-(4-naphthalen-1-yl-phenyl)-propionyl]-3-methyl-urea.
- 83. The amide of claim 78 wherein R is a heteroaromatic ring containing from 5 to 6 ring members with from 1 to 3 heteroatoms selected from the group consisting of oxygen, sulfur or nitrogen.
- 84. The amide of claim 83 wherein said compound is 1-[3-cyclopentyl-2-(4-pyridin-3-yl-phenyl)-propionyl]-3-methyl-urea.
- 85. The amide of claim 78 wherein R is aryl fused with a heteroaromatic containing from 5 to 6 ring members.
- 86. The amide of claim 85 wherein said compound is 1-{3-cyclopentyl-2-[4-(1H-indol-5-yl)-phenyl]-propionyl}-3-methyl-urea.
- 87. The amide of claim 78 wherein R is a saturated 5- or 6-membered cycloheteroalkyl ring containing from 1 to 2 heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur.
- 88. The amide of claim 87 wherein said compound is 1-[3-cyclopentyl-2-(4-morpholin-4-yl-phenyl)-propionyl]-3-methyl-urea.
- 89. The amide of claim 77 wherein y is 0 and z is 1.
- 90. The amide of claim 89 wherein R is a saturated cycloalkyl ring.
- 91. The amide of claim 90 wherein X is SO2.
- 92. The amide of claim 91 wherein said compound is 1-[2-(4-cyclohexanesulfonyl-phenyl)-3-cyclopentyl-propionyl]-3-methyl-urea.
- 93. The amide of claim 90 wherein X is oxygen.
- 94. The amide of claim 93 wherein R is aryl.
- 95. The amide of claim 94 wherein said compound is 1-[3-cyclopentyl-2-(4-phenoxy-phenyl)-propionyl]-3-methyl-urea.
PRIORITY TO PROVISIONAL APPLICATION(S) UNDER 35 U.S.C. § 119(e)
[0001] This application claims priority under 35 U.S.C. §119(e) of provisional application Ser. No. 60/202,387, filed on May 8, 2000.
Provisional Applications (1)
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Number |
Date |
Country |
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60202387 |
May 2000 |
US |