Triphenylethanamine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors: Discovery of N-[(1R)-1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide (BMS-795311).

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Title: Triphenylethanamine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors: Discovery of N-[(1R)-1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide (BMS-795311).
Authors: Qiao JX; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Wang TC; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Adam LP; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Chen AY; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Taylor DS; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Yang RZ; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Zhuang S; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Sleph PG; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Li JP; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Li D; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Yin X; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Chang M; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Chen XQ; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Shen H; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Li J; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Smith D; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Wu DR; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Leith L; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Harikrishnan LS; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Kamau MG; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Miller MM; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Bilder D; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Rampulla R; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Li YX; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Xu C; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Lawrence RM; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Poss MA; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Levesque P; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Gordon DA; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Huang CS; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Finlay HJ; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Wexler RR; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States., Salvati ME; Departments of †Discovery Chemistry, ‡Discovery Biology, §Discovery Toxicology, ∥Preclinical Candidate Optimization, and ⊥Pharmaceutics, Bristol-Myers Squibb Company, Research and Development , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States.
Source: Journal of medicinal chemistry [J Med Chem] 2015 Nov 25; Vol. 58 (22), pp. 9010-26. Date of Electronic Publication: 2015 Nov 17.
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
Description
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.5b01363