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Discovery of BMS-961955, an allosteric inhibitor of the hepatitis C virus NS5B polymerase.
Zheng, Barbara Zhizhen; D'Andrea, Stanley V; Hanumegowda, Umesh; Knipe, Jay O; Mosure, Kathy; Zhuo, Xiaoliang; Lemm, Julie A; Liu, Mengping; Rigat, Karen L; Wang, Ying-Kai; Fang, Hua; Poronsky, Chris; Cutrone, Jingfang; Wu, Dauh-Rurng; Arunachalam, Pirama Nayagam; Balapragalathan, T J; Arumugam, Arunachalam; Mathur, Arvind; Meanwell, Nicholas A; Gao, Min; Roberts, Susan B; Kadow, John F.
Affiliation
  • Zheng BZ; Department of Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States. Electronic address: zhizhenZheng@bms.com.
  • D'Andrea SV; Department of Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Hanumegowda U; Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Knipe JO; Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Mosure K; Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Zhuo X; Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Lemm JA; Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Liu M; Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Rigat KL; Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Wang YK; Department of Lead Evaluation, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Fang H; Department of Lead Evaluation, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Poronsky C; Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Cutrone J; Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Wu DR; Department of Discovery Synthesis, Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Arunachalam PN; Biocon Bristol-Myers Squibb R&D Center, Biocon Park, Bommasandra IV phase, Jigani Link Road, Bengaluru 560099, India.
  • Balapragalathan TJ; Biocon Bristol-Myers Squibb R&D Center, Biocon Park, Bommasandra IV phase, Jigani Link Road, Bengaluru 560099, India.
  • Arumugam A; Biocon Bristol-Myers Squibb R&D Center, Biocon Park, Bommasandra IV phase, Jigani Link Road, Bengaluru 560099, India.
  • Mathur A; Department of Discovery Synthesis, Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Meanwell NA; Department of Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Gao M; Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Roberts SB; Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
  • Kadow JF; Department of Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
Bioorg Med Chem Lett ; 27(15): 3294-3300, 2017 08 01.
Article in En | MEDLINE | ID: mdl-28633899
The synthesis, structure-activity relationship (SAR) data, and further optimization of the metabolic stability and pharmacokinetic (PK) properties for a previously disclosed class of cyclopropyl-fused indolobenzazepine HCV NS5B polymerase inhibitors are described. These efforts led to the discovery of BMS-961955 as a viable contingency backup to beclabuvir which was recently approved in Japan for the treatment of HCV as part of a three drug, single pill combination marketed as XimencyTM.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Antiviral Agents / Benzazepines / Hepatitis C / Viral Nonstructural Proteins / Hepacivirus Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2017 Type: Article
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Antiviral Agents / Benzazepines / Hepatitis C / Viral Nonstructural Proteins / Hepacivirus Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2017 Type: Article