Claims
- 1. A compound of the formula
- 2. The compound according to claim 1 provided that
Z3 is other than phenyl when substituted by a moiety of the formula 71wherein R8 and R9 together are =NR11, wherein R10 and R11 are independently optionally substituted lower alkyl.
- 3. The compound according to claim 1 wherein
R8 and R9 together are=NR11; R10 and R11 are independently hydrogen, HO—, or R hu 12O2C—.
- 4. The compound according to claim 1 wherein
R2 is hydrogen, —CO2R5, —CH2OR6 or —CH2SR6
- 5. The compound according to claim 1 wherein
R2 is hydrogen, —CO2R5 or —CH2OR6.
- 6. The compound according to claim 1 wherein R2 is —CO2R5 and R5 is lower alkyl.
- 7. The compound according to claim 1 wherein R2 is —CH2OR6 or —CH2SR6 and R6 is hydrogen or lower alkyl.
- 8. The compound according to claim 1 wherein R3 is lower alkyl R6O(lower alkyl)-, or a group of formula
- 9. The compound according to claim 1 wherein
R4 is optionally substituted cycloalkyl, optionally substituted heterocyclyl optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl or optionally substituted aralkynyl.
- 10. The compound according to claim 1 wherein
R4 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted heteroaryl.
- 11. The compound according to claim 1 wherein
R4 as optionally substituted phenyl or optionally substituted heteroaryl is optionally substituted (phenyl substituted phenyl), optionally substituted (heteroaryl substituted phenyl), optionally substituted (phenyl substituted heteroaryl) or optionally substituted (heteroaryl substituted heteroaryl).
- 12. The compound according to claim 1 wherein
R5 is lower alkyl.
- 13. The compound according to claim 1 wherein
R6 is hydrogen or lower alkyl.
- 14. The compound according to claim 1 wherein
R7 is hydrogen.
- 15. The compound according to claim 1 wherein R8 and R9 are hydrogen.
- 16. The compound according to claim 1 wherein
R12 is lower alkyl.
- 17. The compound according to claim 1 wherein
n is 1.
- 18. The compound according to claim 1 wherein Z3 is substituted by, at least, an amidinio group in the meta or para position of the ring system ofZ3, relative to the position of attachment Z3 to the rest of the molecule.
- 19. The compound according to claim 1 wherein Z1 is optionally substituted aryl.
- 20. The compound according to claim 1 wherein
Z1 is phenyl.
- 21. The compound according to claim 1 wherein R1 is a group of formula
- 22. The compound according to claim 1 wherein
R8 and R9 together are=NR11, R11 is hydrogen; R10 are hydrogen; R2 is hydrogen, —CO2R5, —C(O)R5, —CH2OR6 or —CH2SR6; R3 is hydrogen, alkyl or Z1-alkyl, or a group of formula 74R4 is optionally substituted cycloalkyl, optionally substituted cycloalkenyl, optionally substituted heteroaryl, optionally substituted fused arylcycloalkyl, optionally substituted fused arylcycloalkyl, optionally substituted fused arylcycloalkenyl, optionally substituted fused arylheteroaryl, optionally substituted fused heteroarylaryl, optionally substituted fused heteroarylcycloalkyl, optionally substituted fused heteroarylcycloalkenyl, optionally substituted fused heteroarylheterocyclyl, optionally substituted fused heteroarylheterocyclenyl; R6 is hydrogen or lower alkyl; A, B, C and D, R7 are hydrogen: R8 and R9 together are=NR11: R11 is hydrogen; Q is R6O—; o and m are 1; n is 1 or 3; or a pharmaceutically acceptable salt thereof, an N-oxide thereof or prodrug thereof.
- 23. A compound according to claim 1 which is:
- 24. A compound according to claim 1 which is:
- 25. A compound according to 1 which is:
- 26. A compound according to claim 1 which is:
- 27. A compound according to claim 1 which is:
- 28. A compound according to claim 1 which is:
- 29. A pharmaceutical composition comprising a pharmaceutically acceptable amount of the compound according to claim 1 and a pharmaceutically acceptable carrier.
- 30. A method for inhibiting the activity of Factor Xa, comprising a pharmaceutically effective amount of the compound of formula I with a composition containing Factor Xa.
- 31. A method for inhibiting the formation of thrombin comprising combining a pharmaceutically effective amount of the compound of formula I with a composition containing Factor Xa.
- 32. A method for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess of Factor Xa activity comprising administering to said patient a pharmaceutically effective amount of the compound according to claim 1.
- 33. A method for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin, comprising administering to said patient a pharmaceutically effective amount of the compound according to claim 1.
Parent Case Info
[0001] This application is a continuation-in-part application of U.S. provisional application Ser. No. 60/079,002, filed Mar. 23, 1998.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60079002 |
Mar 1998 |
US |
Divisions (1)
|
Number |
Date |
Country |
Parent |
09273618 |
Mar 1999 |
US |
Child |
09922906 |
Aug 2001 |
US |