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Claims for Patent: 6,436,989

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Claims for Patent: 6,436,989

Title: Prodrugs of aspartyl protease inhibitors
Abstract:The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
Inventor(s): Hale; Michael R. (Bedford, MA), Tung; Roger D. (Arlington, MA), Baker; Christopher T. (Waltham, MA), Spaltenstein; Andrew (Raleigh, NC)
Assignee: Vertex Pharmaceuticals, Incorporated (Cambridge, MA)
Application Number:08/998,050
Patent Claims: 1. A compound of the formula: ##STR137##

2. The compound according to claim 1, wherein: R.sup.7 is selected from --PO.sub.3.sup.2- Na.sub.2.sup.+, --PO.sub.3.sup.2- K.sub.2.sup.+, or --PO.sub.3.sup.2- Ca.sup.2+.

3. The compound according to claim 2, wherein R.sup.7 is --PO.sub.3.sup.2- Ca.sup.2+.

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 a virally-encoded 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 additional agents independently selected from an anti-viral agent, an HIV protease inhibitor, or an immunostimulator.

8. The pharmaceutical composition according to claim 7, wherein said additional agents are independently selected from zidovudine (AZT), zalcitabine (dideoxycytidine, ddC), didanosine (ddI), stavudine (d4T), lamivudine (3TC), abacavir (1592U89), saquinavir (Ro 31-8959), indinavir (L-735,524), ritonavir (ABT 538, A84538), nelfinavir (AG 1343), XM 450, CGP 53,437, polysulfated polysaccharides, ganciclovir, ribavirin, acyclovir, TIBO, nevirapine, IL-2, GM-CSF, interferon alpha, or erythropoietin (EPO).

9. A method for inhibiting aspartyl protease activity in a mammal, comprising the step of administering to said mammal a pharmaceutical composition according to claim 4.

10. A 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 additionally administered one or more additional agents independently selected from an anti-viral agent, an HIV protease inhibitor, or 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 said one or more additional agents are selected from zidovudine (AZT), zalcitabine (dideoxycytidine, ddC), didanosine (ddI), stavudine (d4T), lamivudine (3TC), abacavir (1592U89), saquinavir (Ro 31-8959), indinavir (L-735,524), ritonavir (ABT 538, A84538), nelfinavir (AG 1343), XM 450, CGP 53,437, polysulfated polysaccharides, ganciclovir, ribavirin, acyclovir, TIBO, nevirapine, IL-2, GM-CSF, interferon alpha, or erythropoietin (EPO).
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