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Improving Metabolic Stability with Deuterium: The Discovery of BMT-052, a Pan-genotypic HCV NS5B Polymerase Inhibitor.
Parcella, Kyle; Eastman, Kyle; Yeung, Kap-Sun; Grant-Young, Katharine A; Zhu, Juliang; Wang, Tao; Zhang, Zhongxing; Yin, Zhiwei; Parker, Dawn; Mosure, Kathy; Fang, Hua; Wang, Ying-Kai; Lemm, Julie; Zhuo, Xiaoliang; Hanumegowda, Umesh; Liu, Mengping; Rigat, Karen; Donoso, Maria; Tuttle, Maria; Zvyaga, Tatyana; Haarhoff, Zuzana; Meanwell, Nicholas A; Soars, Matthew G; Roberts, Susan B; Kadow, John F.
Affiliation
  • Parcella K; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Eastman K; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Yeung KS; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Grant-Young KA; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Zhu J; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Wang T; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Zhang Z; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Yin Z; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Parker D; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Mosure K; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Fang H; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Wang YK; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Lemm J; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Zhuo X; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Hanumegowda U; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Liu M; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Rigat K; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Donoso M; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Tuttle M; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Zvyaga T; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Haarhoff Z; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Meanwell NA; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Soars MG; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Roberts SB; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Kadow JF; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States.
ACS Med Chem Lett ; 8(7): 771-774, 2017 Jul 13.
Article de En | MEDLINE | ID: mdl-28740615
ABSTRACT
Iterative structure-activity analyses in a class of highly functionalized furo[2,3-b]pyridines led to the identification of the second generation pan-genotypic hepatitis C virus NS5B polymerase primer grip inhibitor BMT-052 (14), a potential clinical candidate. The key challenge of poor metabolic stability was overcome by strategic incorporation of deuterium at potential metabolic soft spots. The preclinical profile and status of BMT-052 (14) is described.
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Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Langue: En Journal: ACS Med Chem Lett Année: 2017 Type de document: Article Pays d'affiliation: États-Unis d'Amérique
Texte intégral
Ajouter à My VHL
Imprimer
XML
PubMed Links
Recherche sur Google

Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Langue: En Journal: ACS Med Chem Lett Année: 2017 Type de document: Article Pays d'affiliation: États-Unis d'Amérique