Claims
- 1. A compound represented by formula I:
- 2. A compound, according to claim 1, wherein
R2 is selected from the group consisting of H, F, Cl, NHNH2, (C1-4 alkyl), and CF3; R4 is H or Me; R5 is H or Me; R11 is (C1-4 alkyl), or (C3-7cycloalkyl); and Q is selected from the group consisting of: 69 wherein
R12 is selected from the group consisting of: COOH, (C1-6 alkyl)COOH, (C2-6alkenyl)COOH, (C1-6 alkyl)COO(C1-6 alkyl), (C1-6 alkyl)CONH2, (C3-7cycloalkyl)COOH, (C1-6 alkyl)CONHNH2, CH2CONHSO2CH3, NHSO2CH3, NHSO2CF3, SO2NHCOCH3, SO2NH2, NHCO(C1-4alkyl)COOH, NHCOCH2C(CH3)2COOH, and SO2NHCH2COOH; or a salt thereof, or a prodrug thereof.
- 3. A compound according to claim 1 wherein R2 is selected from the group consisting of H, Cl, F, NHNH2, CH3, and OMe.
- 4. A compound according to claim 3, wherein R2 is H, Cl, F, or CH3.
- 5. A compound according to claim 4, wherein R2 is H, Cl, or F.
- 6. A compound according to claim 1 wherein R4 is H.
- 7. A compound according to claim 1 wherein R5 is Me.
- 8. A compound according to claim 1 wherein R11 is Et.
- 9. A compound according to claim 1 wherein Q is naphthyl, fused phenyl(C4-7)cycloalkyl and fused phenyl-5, 6, or 7-membered saturated heterocycle having one N atom, said Q being substituted with from 1 to 4 R12 substituents.
- 10. A compound according to claim 9 wherein Q is selected from the group consisting of: naphthyl, tetrahydronaphthyl, indanyl, tetrahydroquinolinyl, and tetrahydroisoquinolinyl,
said Q being mono- or disubstituted with R12.
- 11. A compound according to claim 1, wherein R12 is (C1-6)alkyl, (C2-4)alkenyl or (C3-7)cycloalkyl, said alkyl, cycloalkyl or alkenyl being optionally substituted with R13 wherein R13 is selected from the group consisting of:
a) COOH; b) CONR13gR13h wherein R13g and R13h are both independently H, or (C1-6)alkyl optionally substituted with COOH; or R13h is NH2; and c) CONHSO2CH3; or R12 is. a) NHCO(C1-6)alkyl-COOH; b) NHSO2CH3 or NHSO2CF3; c) COCH3 or COCH2COOH; d) COOR13f wherein R13f is H or (C1-6)alkyl; e) CONR13gR13h wherein R13g and R13h are both independently H, or (C1-6)alkyl optionally substituted with COOH; or R13h is NH2; f) CONHSO2CH3; or g) SO2Me, SO2NH2, SO2NHCOCH3, SO2NHCH2COOH, or SO2N(CH3)2.
- 12. A compound according to claim 11, wherein R12 is CH3, CH2COOH, (CH2)2COOH, CH(Me)COOH, CH(Me)CH2COOH, CH2CH(Me)COOH, CH2CONH2, CH2CONHNH2, CH2CH2CONHNH2, CH2CONHSO2Me,
- 13. A compound according to claim 12 wherein R12 is CH3, CH2COOH, (CH2)2COOH, CH2CONH2, CH2CONHNH2,
- 14. A compound according to claim 13 wherein R12 is CH2CONH2, CH2CONHNH2, COOH, CONMe2, NHSO2Me, SO2Me, SO2NMe2, SO2NH2, or SO2NHCH2COOH.
- 15. A compound according to claim 10 wherein Q is
- 16. A compound according to claim 15 wherein R12 is CH2COOH, (CH2)2COOH, CH(Me)COOH, CH(Me)CH2COOH, CH2CH(Me)COOH, CH2CONH2, CH2CONHNH2, CH2CONHSO2Me,
- 17. A compound according to claim 16 wherein R12 is CH2COOH, (CH2)2COOH, CH2CH(Me)COOH, CH2CONH2, CH2CONHNH2,
- 18. A compound according to claim 17 wherein R12 is CH2COOH, (CH2)2COOH, CH2CH(Me)COOH, CH2CONH2, CH2CONHNH2, or COOH.
- 19. A compound according to claim 10 wherein Q is
- 20. A compound according to claim 19 wherein R12 is CH2COOH, (CH2)2COOH, CH2CH(Me)COOH, CH2CH2CONHNH2, CH2CONHSO2Me,
- 21. A compound according to claim 20 wherein R12 is (CH2)2COOH,
- 22. A compound according to claim 21 wherein R12 is (CH2)2COOH, NHSO2Me, SO2NH2, or SO2NHCH2COOH.
- 23. A compound according to claim 10, wherein Q is
- 24. A compound according to claim 23 wherein R12b is CH2COOH and R12a is CH3.
- 25. A compound according to claim 10 wherein Q is
- 26. A compound according to claim 10 wherein Q is
- 27. A compound according to claim 26 wherein R12 is CH2COOH, CH2CH2COOH or COOH.
- 28. A compound according to claim 10 wherein Q is
- 29. A compound according to claim 10 wherein Q is
- 30. A compound according to claim 29 wherein R12 is COMe, CONMe2, COOMe, COOtBu, SO2Me, or SO2NMe2.
- 31. A compound according to claim 30 wherein R12 is CONMe2, CO2Me, COOTBu or SO2NMe2.
- 32. A compound selected from the group consisting of species 1001 through 1051, or a pharmaceutically acceptable salt or ester thereof, wherein each of said species is a compound of the formula
- 33. A compound selected from the group consisting of species 2001 through 1022, or a pharmaceutically acceptable salt or ester thereof, wherein each of said species is a compound of the formula
- 34. A compound selected from the group consisting of species 3001 through 3006, or a pharmaceutically acceptable salt or ester thereof, wherein each of said species is a compound of the formula
- 35. A compound of the formula
- 36. A compound selected from the group consisting of species 5001 through 5010, or a pharmaceutically acceptable salt or ester thereof, wherein each of said species is a compound of the formula
- 37. A compound of the formula:
- 38. A compound selected from the group consisting of species 7001 through 7008, or a pharmaceutically acceptable salt or ester thereof, wherein each of said species is a compound of the formula
- 39. A pharmaceutical composition comprising a compoundaccording to claim 1 and a pharmaceutically acceptable carrier.
- 40. A method for the treatment of HIV-1 infection, which comprises administering to a patient atherapeutic amount of a compound according to claim 1.
- 41. A method for preventing perinatal transmission of HIV-1 from mother to baby, comprising administering a compound according to claim 1 to the mother before giving birth.
RELATED APPLICATIONS
[0001] Benefit of U.S. Provisional Application Serial No. 60/308,710, filed on Jul. 30, 2001 is hereby claimed.
Provisional Applications (1)
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Number |
Date |
Country |
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60308710 |
Jul 2001 |
US |