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Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Boga, Sobhana Babu; Alhassan, Abdul-Basit; Liu, Jian; Guiadeen, Deodial; Krikorian, Arto; Gao, Xiaolei; Wang, James; Yu, Younong; Anand, Rajan; Liu, Shilan; Yang, Chundao; Wu, Hao; Cai, Jiaqiang; Zhu, Hugh; Desai, Jagdish; Maloney, Kevin; Gao, Ying-Duo; Fischmann, Thierry O; Presland, Jeremy; Mansueto, My; Xu, Zangwei; Leccese, Erica; Knemeyer, Ian; Garlisi, Charles G; Bays, Nathan; Stivers, Peter; Brandish, Philip E; Hicks, Alexandra; Cooper, Alan; Kim, Ronald M; Kozlowski, Joseph A.
Affiliation
  • Boga SB; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA. Electronic address: sobhana.babu.boga@merck.com.
  • Alhassan AB; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Liu J; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Guiadeen D; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Krikorian A; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Gao X; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Wang J; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Yu Y; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Anand R; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Liu S; WuXi PharmaTech Co. Ltd, 288 FuTe Zhong Road, No. 1 Building, WaiGaoQiao Free Trade Zone, Shanghai 200131, PR China.
  • Yang C; WuXi PharmaTech Co. Ltd, 288 FuTe Zhong Road, No. 1 Building, WaiGaoQiao Free Trade Zone, Shanghai 200131, PR China.
  • Wu H; WuXi PharmaTech Co. Ltd, 288 FuTe Zhong Road, No. 1 Building, WaiGaoQiao Free Trade Zone, Shanghai 200131, PR China.
  • Cai J; WuXi PharmaTech Co. Ltd, 288 FuTe Zhong Road, No. 1 Building, WaiGaoQiao Free Trade Zone, Shanghai 200131, PR China.
  • Zhu H; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Desai J; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Maloney K; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Gao YD; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Fischmann TO; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Presland J; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Mansueto M; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Xu Z; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Leccese E; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Knemeyer I; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Garlisi CG; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Bays N; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Stivers P; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Brandish PE; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Hicks A; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Cooper A; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Kim RM; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
  • Kozlowski JA; Department of Early Development and Discovery Sciences, MRL, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
Bioorg Med Chem Lett ; 27(16): 3939-3943, 2017 08 15.
Article in En | MEDLINE | ID: mdl-28720503
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Arthritis, Rheumatoid / Protein-Tyrosine Kinases / Morpholines / Protein Kinase Inhibitors / Drug Discovery / Imidazoles Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2017 Document type: Article
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Arthritis, Rheumatoid / Protein-Tyrosine Kinases / Morpholines / Protein Kinase Inhibitors / Drug Discovery / Imidazoles Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2017 Document type: Article