Claims
- 1. A compound selected from the group consisting of:
- 2. A compound, pharmaceutically acceptable salt, prodrug, active metabolite, or solvate according to claim 1, having a PARP-inhibiting activity corresponding to a K1 of 100 μM or less in a PARP enzyme inhibition assay.
- 3. A compound, pharmaceutically acceptable salt, prodrug, active metabolite, or solvate according to claim 1, having a cytotoxicity potentiation activity corresponding to a PF50 of at least 1 in a cytotoxicity potentiation assay.
- 4. A pharmaceutical composition comprising:
(a) an effective amount of a PARP-inhibiting agent that is:
(i) a compound selected from the group consisting of: 126(ii) a pharmaceutically acceptable salt, prodrug, active metabolite, or solvate thereof; and (b) a pharmaceutically acceptable carrier for said PARP-inhibiting agent.
- 5. A method of inhibiting PARP activity of an enzyme, comprising contacting the enzyme with an effective amount of a compound, pharmaceutically acceptable salt, prodrug, active metabolite, or solvate according to claim 1.
- 6. A method according to claim 5, wherein the enzyme is poly(ADP-ribose) polymerase or tankyrase.
- 7. A method of inhibiting PARP enzyme activity in mammalian tissue by administering to a mammal a therapeutically effective amount of a compound, pharmaceutically acceptable salt, prodrug, active metabolite, or solvate according to claim 1.
- 8. A method of inhibiting PARP activity of an enzyme, comprising contacting the enzyme with an effective amount of a compound of the formula:
- 9. A compound of the formula:
- 10. A compound of the formula:
- 11. A compound of the formula
- 12. A compound selected from the group consisting of
- 13. A compound, pharmaceutically acceptable salt, prodrug, active metabolite, or solvate according to claim 9, having a PARP-inhibiting activity corresponding to a Ki of 100 μM or less in a PARP enzyme inhibition assay.
- 14. A compound, pharmaceutically acceptable salt, prodrug, active metabolite, or solvate according to claim 9, having a cytotoxicity potentiation activity corresponding to a PF50 of at least 1 in a cytotoxicity potentiation assay.
- 15. A pharmaceutical composition comprising:
(a) an effective amount of a PARP-inhibiting agent that is a compound according to claim 9; or a pharmaceutically acceptable salt, prodrug, active metabolite, or solvate thereof; and (b) a pharmaceutically acceptable carrier for said PARP-inhibiting agent.
- 16. A method of inhibiting PARP activity of an enzyme, comprising contacting the enzyme with an effective amount of a compound, pharmaceutically acceptable salt, prodrug, active metabolite, or solvate according to claim 9.
- 17. A method according to claim 16, wherein the enzyme is poly(ADP-ribose) polymerase or tankyrase.
- 18. A method of inhibiting PARP enzyme activity in mammalian tissue by administering to a mammal a therapeutically effective amount of a compound, pharmaceutically acceptable salt, prodrug, active metabolite, or solvate according to claim 9.
- 19. A method of inhibiting PARP activity of an enzyme, comprising contacting the enzyme with an effective amount of a compound, pharmaceutically acceptable salt, prodrug, active metabolite, or solvate according to claim 12.
Parent Case Info
[0001] This application claims priority from Provisional Application No. 60/115,431 filed Jan. 11, 1999, which is incorporated herein by reference in its entirety.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60115431 |
Jan 1999 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
09479896 |
Jan 2000 |
US |
Child |
10264018 |
Oct 2002 |
US |