(3R,5S,E)-7-(4-(4-Fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1H-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic Acid (BMS-644950): A Rationally Designed Orally Efficacious 3-Hydroxy-3-methylglutaryl Coenzyme-A Reductase Inhibitor with Reduced Myotoxicity Potential
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Published:2008-04-15
Issue:9
Volume:51
Page:2722-2733
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ISSN:0022-2623
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Container-title:Journal of Medicinal Chemistry
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language:en
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Short-container-title:J. Med. Chem.
Author:
Ahmad Saleem1, Madsen Cort S.1, Stein Philip D.1, Janovitz Evan1, Huang Christine1, Ngu Khehyong1, Bisaha Sharon1, Kennedy Lawrence J.1, Chen Bang-Chi1, Zhao Rulin1, Sitkoff Doree1, Monshizadegan Hossain1, Yin Xiaohong1, Ryan Carol S.1, Zhang Rongan1, Giancarli Mary1, Bird Eileen1, Chang Ming1, Chen Xing1, Setters Robert1, Search Debra1, Zhuang Shaobin1, Nguyen-Tran Van1, Cuff Carolyn A.1, Harrity Thomas1, Darienzo Celia J.1, Li Tong1, Reeves Richard A.1, Blanar Michael A.1, Barrish Joel C.1, Zahler Robert1, Robl Jeffrey A.1
Affiliation:
1. Bristol-Myers Squibb Research & Development, P.O. Box 4000, Princeton, New Jersey 08543
Publisher
American Chemical Society (ACS)
Subject
Drug Discovery,Molecular Medicine
Reference58 articles.
1. Third Report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel III) final report.Circulation2002,106,3143–3421. 2. Clinical Outcomes in Statin Treatment Trials 3. A Receptor-Mediated Pathway for Cholesterol Homeostasis 4. SREBPs: activators of the complete program of cholesterol and fatty acid synthesis in the liver 5. Willard, A. K. Smith, R. L. Hoffman, W. F.6(R)-[2-(8-Acyloxy-2-methyl-6-methyl (or hydrogen)-polyhydro-1-naphthyl)ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones, the hydroxy acid forms of these pyranones, salts and esters thereof, and a pharmaceutical antihypercholesterolemic composition containing themEur. Pat. Appl.EP 33538, 1981.
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