120739-94-8Relevant articles and documents
Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350)
Xu, Lianhong,Liu, Hongtao,Hong, Allen,Vivian, Randy,Murray, Bernard P.,Callebaut, Christian,Choi, You-Chul,Lee, Melody S.,Chau, Jennifer,Tsai, Luong K.,Stray, Kirsten M.,Strickley, Robert G.,Wang, Jianhong,Tong, Leah,Swaminathan, Swami,Rhodes, Gerry R.,Desai, Manoj C.
, p. 995 - 999 (2014/02/14)
The HIV protease inhibitor (PI) ritonavir (RTV) has been widely used as a pharmacoenhancer for other PIs, which are substrates of cytochrome P450 3A (CYP3A). However the potent anti-HIV activity of ritonavir may limit its use as a pharmacoenhancer with other classes of anti-HIV agents. Ritonavir is also associated with limitations such as poor physicochemical properties. To address these issues a series of compounds with replacements at the P2 and/or P3 region was designed and evaluated as novel CYP3A inhibitors. Through these efforts, a potent and selective inhibitor of CYP3A, GS-9350 (cobicistat) with improved physiochemical properties was discovered.
MODULATORS OF PHARMACOKINETIC PROPERTIES OF THERAPEUTICS
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Page/Page column 244, (2008/06/13)
The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.