Claims
- 1. A compound represented by the structural formula
- 2. A compound of claim 1 wherein n is 0.
- 3. A compound of claim 1 wherein the optional double bond is not present.
- 4. A compound of claim 1 wherein R1 and R2 are independently selected from the group consisting of H and (C1-C6)alkyl.
- 5. A compound of claim 4 wherein R1 is (C1-C6)alkyl and R2 is H.
- 6. A compound of claim 1 wherein R3 is H, —OH, (C1-C6)alkyl, (C1-C6)alkoxy, halogen, (C3-C6)cycloalkyl, —C(O)OR17 or —NR22R23.
- 7. A compound of claim 6 wherein R3 is H or (C1-C6)alkyl.
- 8. A compound of claim 1 wherein Het is pyridyl attached to B by a carbon ring member, and is substituted by 1 or 2 substituents selected from W.
- 9. A compound of claim 8 wherein W is R21-phenyl or R2-pyridyl.
- 10. A compound of claim 1 wherein R8, R10 and R11 are each independently selected from the group consisting of H and (C1-C6)alkyl and R9 is H.
- 11. A compound of claim 1 wherein B is —CH═CH—.
- 12. A compound of claim 1 wherein the optional single bond is present, X is —O—, Y is ═O, and R15 is absent.
- 13. A compound of claim 1 wherein Q is
- 14. A compound of claim 13 wherein Q is
- 15. A compound of claim 1 wherein R is —(CH2)n6NHC(O)OR16b, —(CH2)n6NHCOR16b, —(CH2)n6NHC(O)NR4R5, —(CH2)n6NHSO2R16 or —(CH2)n6NHSO2NR4R5; R16b, R16 and R4 are (C1-C6)alkyl; and R5 is H, where n6 is 0-4.
- 16. A compound of claim 15 wherein R is —NHC(O)OR16b, —NHC(O)R16b or —NHC(O)NR4R5, R16b and R4 are (C1-C6)alkyl, and R5 is H.
- 17. A compound of claim 16 wherein R is —NHC(O)OR16b wherein R16b is (C1-C6)alkyl.
- 18. A compound of claim 1 wherein n is 0, the optional single bond is present, X is —O—, Y is ═O and R15 is absent.
- 19. A compound of claim 18 wherein R2, R3, R8, R9, R10 and R11 are each hydrogen, R1 is —CH3, B is —CH═CH—, Het is W-pyridyl, W is R21-phenyl or R21-pyridyl, and R21 is —CF3 or F.
- 20. A compound of claim 19 wherein R is —NHC(O)OR16b and R16b is —CH3 or —CH2CH3.
- 21. A compound of claim 1 selected from the group consisting of
- 22. The compound of claim 1 wherein said salt is a bisulfate.
- 23. A pharmaceutical composition comprising an effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.
- 24. A method of inhibiting thrombin receptors comprising administering to a mammal in need of such treatment an effective amount of a compound of claim 1.
- 25. A method of treating thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, myocardial infarction, glomerulonephritis, thrombotic stroke, thromboembolic stroke, peripheral vascular diseases, inflammatory disorders, cerebral ischemia or cancer, comprising administering to a mammal in need of such treatment an effective amount of a compound of claim 1.
- 26. A method of treating thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, myocardial infarction, glomerulonephritis, thrombotic stroke, thromboembolytic stroke, peripheral vascular diseases, inflammatory disorders, cerebral ischemia or cancer, comprising administering to a mammal in need of such treatment an effective amount of a compound of claim 1 in combination with an additional cardiovascular agent.
- 27. The method of claim 26 wherein the additional cardiovascular agent is selected from the group consisting of thromboxane A2 biosynthesis inhibitors, GP IIb/IIIa antagonists, thromboxane antagonists, adenosine diphosphate inhibitors, cyclooxygenase inhibitors, angiotensin antagonists, endothelin antagonists, angiotensin converting enzyme inhibitors, neutral endopeptidase inhibitors, anticoagulants, diuretics, and platelet aggregation inhibitors.
- 28. The method of claim 27 wherein the additional cardiovascular agent is aspirin or clopidogrel bisulfate.
Parent Case Info
[0001] The present application claims priority under 35 USC section 119(e) of U.S. Provisional application Serial No. 60/373,072, filed Apr. 16, 2002, the complete text, claims and figures of which are incorporated by reference herein as if fully set forth.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60373072 |
Apr 2002 |
US |