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Discovery of (2R)-N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor.
Su, Qibin; Banks, Erica; Bebernitz, Geraldine; Bell, Kirsten; Borenstein, Cassandra F; Chen, Huawei; Chuaqui, Claudio E; Deng, Nanhua; Ferguson, Andrew D; Kawatkar, Sameer; Grimster, Neil P; Ruston, Linette; Lyne, Paul D; Read, Jon A; Peng, Xianyou; Pei, Xiaohui; Fawell, Stephen; Tang, Zhanlei; Throner, Scott; Vasbinder, Melissa M; Wang, Haoyu; Winter-Holt, Jon; Woessner, Richard; Wu, Allan; Yang, Wenzhan; Zinda, Michael; Kettle, Jason G.
Affiliation
  • Su Q; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Banks E; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Bebernitz G; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Bell K; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Borenstein CF; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Chen H; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Chuaqui CE; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Deng N; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Ferguson AD; Discovery Sciences, R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Kawatkar S; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Grimster NP; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Ruston L; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Lyne PD; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Read JA; Discovery Sciences, R&D, AstraZeneca R&D, Cambridge CB4 0WG, U.K.
  • Peng X; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, China.
  • Pei X; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, China.
  • Fawell S; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Tang Z; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, China.
  • Throner S; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Vasbinder MM; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Wang H; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, China.
  • Winter-Holt J; Oncology R&D, AstraZeneca R&D, Cambridge CB4 0WG, U.K.
  • Woessner R; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Wu A; Discovery Sciences, R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Yang W; Early Product Development, Pharmaceutical Sciences, R&D, Boston, Massachusetts 02451, United States.
  • Zinda M; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.
  • Kettle JG; Oncology R&D, AstraZeneca R&D, Cambridge CB4 0WG, U.K.
J Med Chem ; 63(9): 4517-4527, 2020 05 14.
Article in En | MEDLINE | ID: mdl-32297743
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Protein Kinase Inhibitors / Janus Kinase 1 / Indoles Type of study: Prognostic_studies Limits: Animals / Female / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2020 Document type: Article Affiliation country: United States
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Protein Kinase Inhibitors / Janus Kinase 1 / Indoles Type of study: Prognostic_studies Limits: Animals / Female / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2020 Document type: Article Affiliation country: United States