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J-GLOBAL ID：201702255670305836   整理番号：17A1214985

BMS-961955,C型肝炎ウイルスNS5Bポリメラーゼのアロステリック阻害剤の発見【Powered by NICT】

Discovery of BMS-961955, an allosteric inhibitor of the hepatitis C virus NS5B polymerase

著者 (22件)： Zheng Barbara Zhizhen (Department of Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  D’Andrea Stanley V. (Department of Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Hanumegowda Umesh (Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Knipe Jay O. (Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Mosure Kathy (Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Zhuo Xiaoliang (Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Lemm Julie A. (Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Liu Mengping (Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Rigat Karen L. (Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Wang Ying-Kai (Department of Lead Evaluation, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Fang Hua (Department of Lead Evaluation, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Poronsky Chris (Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Cutrone Jingfang (Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Wu Dauh-Rurng (Department of Discovery Synthesis, Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States) ,  Arunachalam Pirama Nayagam (Biocon Bristol-Myers Squibb R&D Center, Biocon Park, Bommasandra IV phase, Jigani Link Road, Bengaluru 560099, India) ,  Balapragalathan T.J. (Biocon Bristol-Myers Squibb R&D Center, Biocon Park, Bommasandra IV phase, Jigani Link Road, Bengaluru 560099, India) ,  Arumugam Arunachalam (Biocon Bristol-Myers Squibb R&D Center, Biocon Park, Bommasandra IV phase, Jigani Link Road, Bengaluru 560099, India) ,  Mathur Arvind (Department of Discovery Synthesis, Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States) ,  Meanwell Nicholas A. (Department of Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Gao Min (Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Roberts Susan B. (Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States) ,  Kadow John F. (Department of Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States)
資料名： Bioorganic & Medicinal Chemistry Letters  (Bioorganic & Medicinal Chemistry Letters)
巻： 27  号： 15  ページ： 3294-3300  発行年： 2017年 
JST資料番号： W0248A  ISSN： 0960-894X  資料種別： 逐次刊行物 (A)
記事区分： 原著論文  発行国： オランダ (NLD)  言語： 英語 (EN)

抄録/ポイント： 合成,構造活性相関(SAR)データ,および代謝安定性と以前に明らかにしたクラスシクロプロピル縮合indolobenzazepine HCV(C型肝炎ウイルス)NS5Bポリメラーゼ阻害剤の薬物動力学(PK)特性のさらなる最適化について述べた。これらの努力は,最近Ximency~TMとして市販されている三剤,単一錠剤併用の一部としてのHCVの治療に対して日本で承認されたbeclabuvirに対する実行可能な分割バックアップとしてBMS961955を発見した。Copyright 2017 Elsevier B.V., Amsterdam. All rights reserved. Translated from English into Japanese by JST.【Powered by NICT】

シソーラス用語： 化学合成 ,  バックアップ ,  構造活性相関 ,  薬物動力学 ,  *肝炎ウイルス ,  *C型肝炎ウイルス ,  最適化 ,  抗ウイルス薬 ,  縮合反応 ,  日本
準シソーラス用語： ポリメラーゼ阻害剤 ,  代謝安定性 ,  *アロステリック阻害 ,  *NS5B , 【Automatic Indexing@JST】

著者キーワード (6件)： HCV(C型肝炎ウイルス)NS5B ,  ポリメラーゼ ,  シクロプロピル縮合indolobenzazepine ,  代謝安定性 ,  直接作用抗ウイルス薬 ,  抗ウイルス剤

分類 (2件)： 酵素一般  (EB09010D) ,  薬物の構造活性相関  (GV01050B)

タイトルに関連する用語 (4件)： BMS ,  C型肝炎ウイルス ,  NS5Bポリメラーゼ ,  発見