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Last Updated: May 16, 2024

Claims for Patent: 9,951,043


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Summary for Patent: 9,951,043
Title:Therapeutic compounds
Abstract:Compounds of formula (I) or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
Inventor(s):Brizgys Gediminas, Canales Eda, Chou Chien-hung, Graupe Michael, Halcomb Randall L., Hu Yunfeng Eric, Lazerwith Scott E., Link John O., Liu Qi, Lu Yafan, Saito Roland D., Schroeder Scott D., Somoza John R., Tse Winston C., Zhang Jennifer R.
Assignee:Gilead Sciences, Inc.
Application Number:US14771779
Patent Claims: 6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein each Zis independently halogen claim 5 , —NRS(O)R claim 5 , or —NRS(O)NRR.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ais CH or C—Z; and Ais CH.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare each H.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris methyl and Ris H.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Zis (C-C)alkynyl claim 1 , optionally substituted with 1 claim 1 , 2 claim 1 , or 3 Zgroups.12. The compound of claim 11 , or a pharmaceutically acceptable salt thereof claim 11 , wherein each Zis independently halogen claim 11 , —OR claim 11 , NRR claim 11 , —NRCOR claim 11 , —C(O)OR claim 11 , or —C(O)NRR.14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Zis phenyl claim 1 , 5-6 membered monocyclic-heteroaryl claim 1 , 8-10 membered bicyclic-heteroaryl claim 1 , 8-10 membered bicyclic-heterocycle claim 1 , or 9-12 membered tricyclics heterocycle claim 1 , wherein any phenyl claim 1 , 5-6 membered monocyclic-heteroaryl claim 1 , 8-10 membered bicyclic-heteroaryl claim 1 , 8-10 membered bicyclic-heterocycle claim 1 , or 9-12 membered tricyclic-heterocycle of Zis optionally substituted with 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , or 5 Zor Zgroups.16. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.17. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and an additional therapeutic agent claim 1 , wherein the additional therapeutic agent is an HIV protease inhibiting compound claim 1 , an HIV non-nucleoside inhibitor of reverse transcriptase claim 1 , an HIV nucleoside inhibitor of reverse transcriptase claim 1 , an HIV nucleotide inhibitor of reverse transcriptase claim 1 , an HIV integrase inhibitor claim 1 , a gp41 inhibitor claim 1 , a CXCR4 inhibitor claim 1 , a gp120 inhibitor claim 1 , a CCR5 inhibitor claim 1 , a capsid polymerization inhibitor claim 1 , or a non-catalytic site HIV integrase inhibitor or combinations thereof.18. A method for treating a HIV infection in a patient in need thereof comprising administering a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , to the patient.19. A method for treating an HIV infection in a patient in need thereof comprising administering to the patient a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in combination with a therapeutically effective amount of an additional therapeutic agent claim 1 , wherein the additional therapeutic agent is an HIV protease inhibiting compound claim 1 , an HIV non-nucleoside inhibitor of reverse transcriptase claim 1 , an HIV nucleoside inhibitor of reverse transcriptase claim 1 , an HIV nucleotide inhibitor of reverse transcriptase claim 1 , an HIV integrase inhibitor claim 1 , a gp41 inhibitor claim 1 , a CXCR4 inhibitor claim 1 , a gp120 inhibitor claim 1 , a CCR5 inhibitor claim 1 , a capsid polymerization inhibitor claim 1 , or a non-catalytic site HIV integrase site inhibitor or combinations thereof.23. The compound of claim 20 , or a pharmaceutically acceptable salt thereof claim 20 , wherein:{'sup': 1a', 'n1', 'n1', 'p1', 'n1', 'q1', 'r1', 'q1', 'r1', 'n1', 'p1', 'n1', 'q1', 'r1', 'n1', 'p1, 'sub': 2', '2', '2, 'each Zis independently halogen, —CN, —OR, —NRS(O)R, —NRS(O)NRR, —NRR, —NRCOR, —NRCONRR, or —NRCOR;'}{'sup': '1b', 'sub': 1', '8', '1', '8, 'each Zis independently (C-Calkyl), wherein the (C-Calkyl) is optionally substituted with 1, 2, or 3 halogen, which are the same or different; and'}{'sup': 1w', '1a', '1b, 'at least one of Zis Zor Z.'}26. A pharmaceutical composition comprising a compound of claim 20 , or a pharmaceutically acceptable salt thereof claim 20 , and a pharmaceutically acceptable carrier.27. A pharmaceutical composition comprising a compound of claim 20 , or a pharmaceutically acceptable salt thereof claim 20 , and an additional therapeutic agent claim 20 , wherein the additional therapeutic agent is an HIV protease inhibiting compound claim 20 , an HIV non-nucleoside inhibitor of reverse transcriptase claim 20 , an HIV nucleoside inhibitor of reverse transcriptase claim 20 , an HIV nucleotide inhibitor of reverse transcriptase claim 20 , an HIV integrase inhibitor claim 20 , a gp41 inhibitor claim 20 , a CXCR4 inhibitor claim 20 , a gp120 inhibitor claim 20 , a CCR5 inhibitor claim 20 , a capsid polymerization inhibitor claim 20 , or a non-catalytic site HIV integrase inhibitor or combinations thereof.28. A method for treating a HIV infection in a patient in need thereof comprising administering a therapeutically effective amount of a compound of claim 20 , or a pharmaceutically acceptable salt thereof claim 20 , to the patient.29. A method for treating an HIV infection in a patient in need thereof comprising administering to the patient a therapeutically effective amount of a compound of claim 20 , or a pharmaceutically acceptable salt thereof claim 20 , in combination with a therapeutically effective amount of an additional therapeutic agent claim 20 , wherein the additional therapeutic agent is an HIV protease inhibiting compound claim 20 , an HIV non-nucleoside inhibitor of reverse transcriptase claim 20 , an HIV nucleoside inhibitor of reverse transcriptase claim 20 , an HIV nucleotide inhibitor of reverse transcriptase claim 20 , an HIV integrase inhibitor claim 20 , a gp41 inhibitor claim 20 , a CXCR4 inhibitor claim 20 , a gp120 inhibitor claim 20 , a CCR5 inhibitor claim 20 , a capsid polymerization inhibitor claim 20 , or a non-catalytic site HIV integrase site inhibitor or combinations thereof.31. A pharmaceutical composition comprising a compound of claim 30 , or a pharmaceutically acceptable salt thereof claim 30 , and a pharmaceutically acceptable carrier.32. A pharmaceutical composition comprising a compound of claim 30 , or a pharmaceutically acceptable salt thereof claim 30 , and an additional therapeutic agent claim 30 , wherein the additional therapeutic agent is an HIV protease inhibiting compound claim 30 , an HIV non-nucleoside inhibitor of reverse transcriptase claim 30 , an HIV nucleoside inhibitor of reverse transcriptase claim 30 , an HIV nucleotide inhibitor of reverse transcriptase claim 30 , an HIV integrase inhibitor claim 30 , a gp41 inhibitor claim 30 , a CXCR4 inhibitor claim 30 , a gp120 inhibitor claim 30 , a CCR5 inhibitor claim 30 , a capsid polymerization inhibitor claim 30 , or a non-catalytic site HIV integrase inhibitor and combinations thereof.33. A method for treating a HIV infection in a patient in need thereof comprising administering a therapeutically effective amount of a compound of claim 30 , or a pharmaceutically acceptable salt thereof claim 30 , to the patient.34. A method for treating an HIV infection in a patient in need thereof comprising administering to the patient a therapeutically effective amount of a compound of claim 30 , or a pharmaceutically acceptable salt thereof claim 30 , in combination with a therapeutically effective amount of an additional therapeutic agent claim 30 , wherein the additional therapeutic agent is an HIV protease inhibiting compound claim 30 , an HIV non-nucleoside inhibitor of reverse transcriptase claim 30 , an HIV nucleoside inhibitor of reverse transcriptase claim 30 , an HIV nucleotide inhibitor of reverse transcriptase claim 30 , an HIV integrase inhibitor claim 30 , a gp41 inhibitor claim 30 , a CXCR4 inhibitor claim 30 , a gp120 inhibitor claim 30 , a CCR5 inhibitor claim 30 , a capsid polymerization inhibitor claim 30 , or a non-catalytic site HIV integrase site inhibitor and combinations thereof.

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