Patent EA-003509-B1 (EA)
Title: Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors
Inventor: TUNG ROGER D
IPC: A61K31/215
Filed: 1998-03-09
Abstract: 1. A compound of formula I: wherein: R<7> is selected from -PO3<2->Na2<+>, -PO3<2->K2<+> or -PO3<2->Mg2<+>, 2. The compound according to claim 1, wherein R<7> is selected from -PO3<2->Na2<+>, -PO3<2->K2<+> or -PO3<2->Ca2<+>. 3. The compound according to claim 1, wherein R<7> is -PO3<2->Ca2<+>. 4. A pharmaceutical composition, comprising a compound according to any one of claims 1 to 3 in an amount effective to treat infection by a virus that is characterized by an aspartyl protease; and a pharmaceutically acceptable carrier, adjuvant or vehicle. 5. The pharmaceutical composition according to claim 4, wherein said virus is HIV. 6. The pharmaceutical composition according to claim 4, wherein said pharmaceutical composition is formulated for oral administration. 7. The pharmaceutical composition according to claim 4 further comprising one or more agents selected from an anti-viral agent, an HIV protease inhibitor other than a compound according to claim 1, and an immunostimulator. 8. The pharmaceutical composition according to claim 7, further comprising one or more agents selected from zidovudine (AZT), zalcitabine (ddC), didanosine (ddI), stavudine (d4T), lamivudine (3TC), abaquavir (1592U89), saquinavir (Ro 31-8959), indinavir (MK-639, L-735,524), ritonavir (ABT 538, A84538), nelphinavir (AG 1341), XM 450, CPG 53,437, 935U83, 524W91, SC-52151, XM 412, tuscarasol, polysulsulfonated polysacharides, gancyclovir, dideoxycytidine, ribavirine, axyclovir, TIBO, nevirapine, IL-2, GM-CSF, alpha interferon or erythropoetin (ETO). 9. A method for inhibiting aspartyl protease activity in a mammal, comprising the step of contacting said mammal with a pharmaceutical composition according to claim 4 or administering to said mammal a pharmaceutical composition according to claim 4. 10. The method for treating HIV infection in a mammal comprising the step of administering to said mammal a pharmaceutical composition according to claim 4. 11. The method according to claim 10, wherein said mammal is to be additionally administered one or more additional agents selected from an anti-viral agent, an HIV protease inhibitor other than a compound according to claim 1, and an immunostimulator either as a part of a single dosage form with said pharmaceutical composition or as a separate dosage form. 12. The method according to claim 11, wherein one or more of additional agents selected from zidovudine (AZT), zalcitabine (ddC), didanosine (ddI), stavudine (d4T), lamivudine (3TC), abaquavir (1592U89), saquinavir (Ro 31-8959), indinavir (MK-639, L-735,524), ritonavir (ABT 538, A84538), nelphinavir (AG 1341), XM 450, CPG 53,437, 935U83, 524W91, SC-52151, XM 412, tuscarasol, polysulsulfonated polysacharides, gancyclovir, dideoxycytidine, ribavirine, acyclovir, TIBO, nevirapine, IL-2, GM-CSF, alpha interferon or erythropoetin (ETO). 13. The method according to claim 11, wherein said step of administering comprises oral administration, wherein the pharmaceutical composition is to be administered by oral administration.