Patent EA-001154-B1 (EA)
Title: (4r,5s,6s,7r)-hexahydro-1[5-(3-aminoinazole)methyl]-3-butyl-5,6-dihydroxy-4,7-bis[phenylmethyl]-2h-1,3-diazepin-2-one and its useas hiv protease inhibitor
Inventor: RODGERS JAMES DAVID
IPC: A61P31/18
Filed: 1997-11-04
Abstract: 1. A compound of formula I:   or a pharmaceutically acceptable salt or prodrug form thereof, wherein a prodrug of formula I is a compound wherein the two hydroxy groups join to form an epoxide, -OCH2SCH2O-; -OC (=O)O-; -OCH2O-; -OC(=S)O-; -OC(=O)C(=O)O-; -OC(CH3)2O-; -OC((CH2)3NH2) (CH3)O-; -OC(OCH3) (CH2CH2CH3)O-; or -OS(=O)O- group. 2. A compound according to claim 1, wherein the compound is of formula I.  3. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt or prodrug form thereof. 4. A composition according to claim 3, wherein the compound is of formula I. 5. Use of a compound of formula I or a pharmaceutically acceptable salt or prodrug form thereof for the manufacture of a medicament for treating HIV infection:   or a pharmaceutically acceptable salt or prodrug form thereof, wherein a prodrug of formula I is a compound wherein the two hydroxy groups join to form an epoxide, -OCH2SCH2O-; -OC (=O)O-; -OCH2O-; -OC(=S)O-; -OC(=O)C(=O)O-; -OC(CH3)2O-; -OC((CH2)3NH2) (CH3)O-; -OC(OCH3) (CH2CH2CH3)O-; or -OS(=O)O- group. 6. A use according to claim 5, wherein the compound is of formula I. 7. Use of a combination of (a) and (b) for the manufacture of a medicament for treating HIV infection, wherein: (a) is a compound of formula I or a pharmaceutically acceptable salt or prodrug form thereof:    wherein a prodrug of formula I is a compound wherein the two hydroxy groups join to form an epoxide, - OCH2SCH2O-; -OC (=O)O-; -OCH2O-; -OC(=S)O-; -OC(=O)C(=O)O-; -OC(CH3)2O-; -OC((CH2)3NH2) (CH3)O-; -OC(OCH3) (CH2CH2CH3)O-; or -OS(=O)O- group.and (b) is at least one compound selected from the group consisting of HIV reverse transcriptase inhibitors and HIV protease inhibitors. 8. A use according to claim 7, wherein the compound is of formula I. 9. A use according to claim 7, wherein the reverse transcriptase inhibitor is a nucleoside reverse transcriptase inhibitor. 10. A use according to claim 9, wherein the nucleoside reverse transcriptase inhibitor is selected from AZT, 3TC, ddI, ddC, and d4T and the protease inhibitor is selected from saquinavir, ritonavir, indinavir, VX-478, nelfinavir, KNI-272, CGP-61755, and U-103017. 11. A use according to claim 10, wherein the nucleoside reverse transcriptase inhibitor is selected from AZT and 3TC and the protease inhibitor is selected from saquinavir, ritonavir, and indinavir. 12. A use according to claim 11, wherein the nucleoside reverse transcriptase inhibitor is AZT. 13. a use according to claim 11, wherein the protease inhibitor is indinavir. 14. A pharmaceutical kit useful for the treatment of HIV infection, which comprises a therapeutically effective amount of: (a) a compound of claim 1; and, (b) at least one compound selected from the group consisting of HIV reverse transcriptase inhibitors and HIV protease inhibitors, in one or more sterile containers. 15. A kit according to claim 14, wherein component (a) is a compound of formula I.