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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
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  Data: 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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  Data: <searchLink fieldCode="AU" term="%22Su+Q%22">Su Q</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Banks+E%22">Banks E</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Bebernitz+G%22">Bebernitz G</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Bell+K%22">Bell K</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Borenstein+CF%22">Borenstein CF</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Chen+H%22">Chen H</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Chuaqui+CE%22">Chuaqui CE</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Deng+N%22">Deng N</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Ferguson+AD%22">Ferguson AD</searchLink>; Discovery Sciences, R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Kawatkar+S%22">Kawatkar S</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Grimster+NP%22">Grimster NP</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Ruston+L%22">Ruston L</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Lyne+PD%22">Lyne PD</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Read+JA%22">Read JA</searchLink>; Discovery Sciences, R&D, AstraZeneca R&D, Cambridge CB4 0WG, U.K.<br /><searchLink fieldCode="AU" term="%22Peng+X%22">Peng X</searchLink>; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, China.<br /><searchLink fieldCode="AU" term="%22Pei+X%22">Pei X</searchLink>; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, China.<br /><searchLink fieldCode="AU" term="%22Fawell+S%22">Fawell S</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Tang+Z%22">Tang Z</searchLink>; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, China.<br /><searchLink fieldCode="AU" term="%22Throner+S%22">Throner S</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Vasbinder+MM%22">Vasbinder MM</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Wang+H%22">Wang H</searchLink>; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, China.<br /><searchLink fieldCode="AU" term="%22Winter-Holt+J%22">Winter-Holt J</searchLink>; Oncology R&D, AstraZeneca R&D, Cambridge CB4 0WG, U.K.<br /><searchLink fieldCode="AU" term="%22Woessner+R%22">Woessner R</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Wu+A%22">Wu A</searchLink>; Discovery Sciences, R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Yang+W%22">Yang W</searchLink>; Early Product Development, Pharmaceutical Sciences, R&D, Boston, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Zinda+M%22">Zinda M</searchLink>; Oncology R&D, AstraZeneca R&D, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Kettle+JG%22">Kettle JG</searchLink>; Oncology R&D, AstraZeneca R&D, Cambridge CB4 0WG, U.K.
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  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2020 May 14; Vol. 63 (9), pp. 4517-4527. <i>Date of Electronic Publication: </i>2020 Apr 28.
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