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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.

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Title: 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.
Authors: 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.
Source: Journal of medicinal chemistry [J Med Chem] 2020 May 14; Vol. 63 (9), pp. 4517-4527. Date of Electronic Publication: 2020 Apr 28.
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
Description
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.9b01392