154212-61-0Relevant articles and documents
Preparation method of ritonavir
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Paragraph 0018, (2019/03/08)
The invention relates to the technical field of medicine, in particular to a preparation method of ritonavir. According to the preparation method of the ritonavir, (2-isopropyl thiazole-4-yl)-nitrogen-methyl methylamine is taken as a raw material, and the ritonavir is synthesized through a three-step reaction; a urea bond is built by trichloroethanol chloroformate, paratoluensulfonyl chloride which is cheap and easy to obtain is adopted as a condensing agent for amide, the ritonavir is synthesized with the high yield, and the yield of the ritonavir is 79%; and compared with an existing preparation method, the preparation method has the advantages of low cost, environment friendliness, easy scale production and the like, and has good application prospects.
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 199-200, (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.