877384-16-2Relevant articles and documents
Chiral purification method of drug intermediate
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, (2020/06/02)
The invention provides a chiral purification method of a drug intermediate. The chiral purification method of the drug intermediate comprises the following steps: (1) adding a low-optical-purity compound as shown in a formula A4 into a solvent A, carrying
NOVEL OXAZOLIDINONE DERIVATIVE AS CETP INHIBITOR, ITS PREPARATION METHOD, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 48, (2014/10/15)
Disclosed are a novel oxazolidinone derivative exhibiting inhibitory activity against CETP, a preparation method thereof, and a pharmaceutical composition comprising the same. Exhibiting excellent inhibitory activity against CETP, the oxazolidinone deriva
Biphenyl-substituted oxazolidinones as cholesteryl ester transfer protein inhibitors: Modifications of the oxazolidinone ring leading to the discovery of anacetrapib
Smith, Cameron J.,Ali, Amjad,Hammond, Milton L.,Li, Hong,Lu, Zhijian,Napolitano, Joann,Taylor, Gayle E.,Thompson, Christopher F.,Anderson, Matt S.,Chen, Ying,Eveland, Suzanne S.,Guo, Qiu,Hyland, Sheryl A.,Milot, Denise P.,Sparrow, Carl P.,Wright, Samuel D.,Cumiskey, Anne-Marie,Latham, Melanie,Peterson, Laurence B.,Rosa, Ray,Pivnichny, James V.,Tong, Xinchun,Xu, Suoyu S.,Sinclair, Peter J.
experimental part, p. 4880 - 4895 (2011/09/20)
The development of the structure-activity studies leading to the discovery of anacetrapib is described. These studies focused on varying the substitution of the oxazolidinone ring of the 5-aryloxazolidinone system. Specifically, it was found that substitution of the 4-position with a methyl group with the cis-stereochemistry relative to the 5-aryl group afforded compounds with increased cholesteryl ester transfer protein (CETP) inhibition potency and a robust in vivo effect on increasing HDL-C levels in transgenic mice expressing cynomolgus monkey CETP.