Claims
- 1. A compound having the Formula I:
- 2. A compound having the Formula I:
- 3. The compound according to claim 2, wherein:
R1 is phenyl, pyrrolyl, pyrrolidinyl, isoxazolyl, pyrazolyl, thiazolyl, tetrahydrofuranyl, furanyl, thienyl or tetrahydropyridazinyl, where said phenyl, pyrrolyl, pyrrolidinyl, isoxazolyl, pyrazolyl, thiazolyl, tetrahydrofuranyl, furanyl, thienyl or tetrahydropyridazinyl is unsubstituted or substituted with one or more substituents independently selected from alkyl, haloalkyl, halogen, and hydroxyl; R2 is a substituted alkyl group, a substituted or unsubstituted C1-C6 alkenyl group, or a substituted or unsubstituted C1-C6 alkynyl group, wherein said alkyl, alkenyl or alkynyl group is a straight or branched chained group, and where said substituted alkyl, alkenyl or alkynyl group is substituted by one or more substituents independently selected from cyano, halogen and alkylamino; R2′ is H, methyl or ethyl; X is 343 wherein RX is H, halogen, or alkoxy; Z is S, O, CH2 or CFH; R3, R4, R5, R8 and R8′ are each H; and R6 and R7 are independently selected from H or methyl; or a prodrug, pharmaceutically active metabolite or pharmaceutically active salt or solvate thereof.
- 4. The compound according to claim 2, wherein:
R1 is phenyl, where said phenyl is substituted with one or more substituents independently selected from alkyl, halogen or hydroxyl; R2 is a C1-C6 alkenyl group or a C1-C6 alkynyl group, wherein said alkenyl or alkynyl group is a straight or branched chained group, and where said alkenyl or alkynyl group is unsubstituted or is substituted by one or more halogen substituents; R2′ is H; X is 344 wherein RX is H; Z is S; R3, R4, R5, R8 and R8′ are each H; and R6 and R7 are each methyl; or a prodrug, pharmaceutically active metabolite or pharmaceutically active salt or solvate thereof.
- 5. A compound having the Formula I:
- 6. The compound according to claim 5, wherein:
R1 is phenyl, pyrrolyl, pyrrolidinyl, isoxazolyl, pyrazolyl, thiazolyl, tetrahydrofuranyl, furanyl, thienyl or tetrahydropyridazinyl, where said phenyl, pyrrolyl, pyrrolidinyl, isoxazolyl, pyrazolyl, thiazolyl, tetrahydrofuranyl, furanyl, thienyl or tetrahydropyridazinyl is unsubstituted or substituted with one or more substituents independently selected from alkyl, haloalkyl, halogen, and hydroxyl; R2 is a substituted phenylalkyl group, where said alkyl moiety of said substituted phenylalkyl group is a straight or branched chain alkyl moiety; R2′ is H, methyl, ethyl or propyl, where said methyl, ethyl or propyl is unsubstituted or substituted with hydroxyl; X is 347 wherein RX is H, halogen, or alkoxy; Z is S, O, CH2 or CFH; R3, R4, R5, R8 and R8′ are each H; and R6 and R7 are independently selected from H or methyl; provided that R1 is selected from isoxazolyl, pyrazolyl, thiazolyl or tetrahydropyridazinyl, where said is isoxazolyl, pyrazolyl, thiazolyl or tetrahydropyridazinyl is unsubstituted or substituted with one or more substituents independently selected from alkyl, haloalkyl, halogen, and hydroxyl when R2 is a substituted or unsubstituted phenylalkyl group or provided that R1 is selected from phenyl, pyrrolyl, pyrrolidinyl, isoxazolyl, pyrazolyl, thiazolyl, tetrahydrofuranyl, furanyl, thienyl or tetrahydropyridazinyl when R2 is a substituted phenylalkyl group and said phenyl moiety of said substituted phenylalkyl group comprises one or more substituents other than halo or methyl, where said one or more substituents is independently selected from haloalkyl, amino, hydroxyl, alkoxy, haloalkoxy, alkylenedioxy, di-haloalkylenedioxy, cycloalkylalkyloxy, dialkylamino, alkylsulfonyl and alkylthio; or a prodrug, pharmaceutically active metabolite or pharmaceutically active salt or solvate thereof.
- 7. The compound according to claim 5, wherein:
R1 is phenyl, where said phenyl is substituted with one or more substituents independently selected from methyl, halogen or hydroxyl; R2 is a substituted phenylalkyl group, where said alkyl moiety of said substituted phenylalkyl group is a straight or branched chain alky moiety; where said phenyl moiety of said substituted phenylalkyl group comprises one or more substituents other than halo or methyl, where said one or more substituents is independently selected from trifluoromethyl, amino, hydroxyl, C1-C4alkoxy, alkylenedioxy, di-fluoralkylenedioxy, cyclopropylmethoxy, di-methyl-amino, methanesulfonyl and methylthio; R2′ is H, methyl or ethyl; X is 348 wherein RX is H; Z is S or O; and R3, R4, R5, R6 R7, R8 and R8′ are each H; or a prodrug, pharmaceutically active metabolite or pharmaceutically active salt or solvate thereof.
- 8. The compound, prodrug, pharmaceutically acceptable salt, pharmaceutically active metabolite, or pharmaceutically acceptable solvate according to any one of claims 1, 2 or 5, having the formula:
- 9. The compound, prodrug, pharmaceutically acceptable salt, pharmaceutically active metabolite, or pharmaceutically acceptable solvate according to any one of claims 1, 2 or 5, having the formula:
- 10. The compound, prodrug, pharmaceutically acceptable salt, pharmaceutically active metabolite, or pharmaceutically acceptable solvate according to any one of claims 1, 2 or 5, having the formula:
- 11. A pharmaceutical composition comprising:
a therapeutically effective amount of at least one HIV agent selected from compounds, prodrugs, pharmaceutically acceptable salts, pharmaceutically active metabolites, and pharmaceutically acceptable solvates defined in any one of claims 1, 2 or 5; and a pharmaceutically acceptable carrier, diluent, vehicle, or excipient.
- 12. The pharmaceutical composition according to claim 11, wherein the composition further comprises a therapeutically effective amount of at least one HIV infection/AIDS treatment agent selected from the group consisting of HIV/AIDS antiviral agents, immunomodulators, and anti-infective agents.
- 13. The pharmaceutical composition according to claim 12, wherein the composition further comprises a therapeutically effective amount of at least one antiviral agent selected from the group consisting of non-nucleoside HIV reverse transcriptase inhibitors and nucleoside HIV reverse transcriptase inhibitors.
- 14. The pharmaceutical composition according to claim 13, further comprising a therapeutically effective amount of at least one HIV protease inhibitor.
- 15. A method of treating a mammalian disease condition mediated by HIV protease activity, comprising administering to a mammal in need thereof a therapeutically effective amount of at least one compound, prodrug, pharmaceutically acceptable salt, pharmaceutically active metabolite, or pharmaceutically acceptable solvate defined in any one of claims 1, 2 or 5.
- 16. A method of inhibiting the activity of HIV protease in a subject in need thereof, comprising contacting the HIV protease with an effective amount of at least one compound, prodrug, pharmaceutically acceptable salt, pharmaceutically active metabolite, or pharmaceutically acceptable solvate defined in any one of claims 1, 2 or 5.
- 17. A method of preventing or treating infection by HIV in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound according to any one of claims 1, 2 or 5.
- 18. The method according to claim 17, wherein the compound is administered in combination with a therapeutically effective amount of at least one HIV infection/AIDS treatment agent selected from the group consisting of HIV/AIDS antiviral agents, immunomodulators, and anti-infective agents.
- 19. A compound selected from
Parent Case Info
[0001] This application claims the benefit of U.S. Provisional Application No. 60/297,460, filed on Jun. 11, 2001, and U.S. Provisional Application No. 60/297,729, filed on June 11, 2001.
Provisional Applications (2)
|
Number |
Date |
Country |
|
60297460 |
Jun 2001 |
US |
|
60297729 |
Jun 2001 |
US |