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Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.
Wang, Xiaojing; Barbosa, James; Blomgren, Peter; Bremer, Meire C; Chen, Jacob; Crawford, James J; Deng, Wei; Dong, Liming; Eigenbrot, Charles; Gallion, Steve; Hau, Jonathon; Hu, Huiyong; Johnson, Adam R; Katewa, Arna; Kropf, Jeffrey E; Lee, Seung H; Liu, Lichuan; Lubach, Joseph W; Macaluso, Jen; Maciejewski, Pat; Mitchell, Scott A; Ortwine, Daniel F; DiPaolo, Julie; Reif, Karin; Scheerens, Heleen; Schmitt, Aaron; Wong, Harvey; Xiong, Jin-Ming; Xu, Jianjun; Zhao, Zhongdong; Zhou, Fusheng; Currie, Kevin S; Young, Wendy B.
Afiliação
  • Wang X; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Barbosa J; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Blomgren P; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Bremer MC; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Chen J; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Crawford JJ; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Deng W; ChemPartner, No. 1 Building, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area, Shanghai, China 201203.
  • Dong L; ChemPartner, No. 1 Building, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area, Shanghai, China 201203.
  • Eigenbrot C; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Gallion S; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Hau J; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Hu H; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Johnson AR; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Katewa A; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Kropf JE; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Lee SH; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Liu L; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Lubach JW; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Macaluso J; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Maciejewski P; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Mitchell SA; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Ortwine DF; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • DiPaolo J; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Reif K; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Scheerens H; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Schmitt A; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Wong H; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
  • Xiong JM; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Xu J; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Zhao Z; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Zhou F; ChemPartner, No. 1 Building, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area, Shanghai, China 201203.
  • Currie KS; Gilead Sciences (formerly CGI Pharmaceuticals), 199 East Blaine Street, Seattle, Washington 98102, United States.
  • Young WB; Genentech, Inc., Research and Early Development, 1 DNA Way, South San Francisco, California 94080, United States.
ACS Med Chem Lett ; 8(6): 608-613, 2017 Jun 08.
Article em En | MEDLINE | ID: mdl-28626519
ABSTRACT
In our continued effort to discover and develop best-in-class Bruton's tyrosine kinase (Btk) inhibitors for the treatment of B-cell lymphomas, rheumatoid arthritis, and systemic lupus erythematosus, we devised a series of novel tricyclic compounds that improved upon the druglike properties of our previous chemical matter. Compounds exemplified by G-744 are highly potent, selective for Btk, metabolically stable, well tolerated, and efficacious in an animal model of arthritis.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Estados Unidos