Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor.
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| Title: | Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor. |
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| Authors: | Johannes JW; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Balazs AYS; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Barratt D; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Bista M; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Chuba MD; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Cosulich S; Oncology Projects, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Critchlow SE; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Degorce SL; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Di Fruscia P; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Edmondson SD; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Embrey KJ; New Modalities & Parenteral Development, Pharmaceutical Technology & Development, Operations, AstraZeneca, Macclesfield SK10 2NA, U.K., Fawell S; Oncology Discovery, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Ghosh A; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Gill SJ; Safety Sciences, Clinical Pharmacology and Safety Sciences R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Gunnarsson A; Discovery Sciences, R&D Gothenburg, AstraZeneca, Pepparedsleden 1, SE-431 83 Mölndal, Sweden., Hande SM; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Heightman TD; Chemistry, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Hemsley P; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Illuzzi G; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Lane J; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Larner CJB; Safety Sciences, Clinical Pharmacology and Safety Sciences R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Leo E; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Liu L; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China., Madin A; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., McWilliams L; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., O'Connor MJ; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Orme JP; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Pachl F; Discovery Sciences, R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Packer MJ; Computational Chemistry, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Pei X; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China., Pike A; DMPK, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Schimpl M; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., She H; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China., Staniszewska AD; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Talbot V; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Underwood E; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Varnes JG; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Xue L; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China., Yao T; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China., Zhang K; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China., Zhang AX; Discovery Sciences, R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States., Zheng X; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States. |
| Source: | Journal of medicinal chemistry [J Med Chem] 2024 Dec 26; Vol. 67 (24), pp. 21717-21728. Date of Electronic Publication: 2024 Dec 10. |
| 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 |
| FullText | Text: Availability: 0 |
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| Header | DbId: mdl DbLabel: MEDLINE Ultimate An: 39655996 AccessLevel: 2 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 0 |
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| Items | – Name: Title Label: Title Group: Ti Data: Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AU" term="%22Johannes+JW%22">Johannes JW</searchLink>; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Balazs+AYS%22">Balazs AYS</searchLink>; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Barratt+D%22">Barratt D</searchLink>; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Bista+M%22">Bista M</searchLink>; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Chuba+MD%22">Chuba MD</searchLink>; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Cosulich+S%22">Cosulich S</searchLink>; Oncology Projects, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Critchlow+SE%22">Critchlow SE</searchLink>; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Degorce+SL%22">Degorce SL</searchLink>; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Di+Fruscia+P%22">Di Fruscia P</searchLink>; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Edmondson+SD%22">Edmondson SD</searchLink>; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Embrey+KJ%22">Embrey KJ</searchLink>; New Modalities & Parenteral Development, Pharmaceutical Technology & Development, Operations, AstraZeneca, Macclesfield SK10 2NA, U.K.<br /><searchLink fieldCode="AU" term="%22Fawell+S%22">Fawell S</searchLink>; Oncology Discovery, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Ghosh+A%22">Ghosh A</searchLink>; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Gill+SJ%22">Gill SJ</searchLink>; Safety Sciences, Clinical Pharmacology and Safety Sciences R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Gunnarsson+A%22">Gunnarsson A</searchLink>; Discovery Sciences, R&D Gothenburg, AstraZeneca, Pepparedsleden 1, SE-431 83 Mölndal, Sweden.<br /><searchLink fieldCode="AU" term="%22Hande+SM%22">Hande SM</searchLink>; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Heightman+TD%22">Heightman TD</searchLink>; Chemistry, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Hemsley+P%22">Hemsley P</searchLink>; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Illuzzi+G%22">Illuzzi G</searchLink>; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Lane+J%22">Lane J</searchLink>; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Larner+CJB%22">Larner CJB</searchLink>; Safety Sciences, Clinical Pharmacology and Safety Sciences R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Leo+E%22">Leo E</searchLink>; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Liu+L%22">Liu L</searchLink>; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. 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China.<br /><searchLink fieldCode="AU" term="%22Madin+A%22">Madin A</searchLink>; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22McWilliams+L%22">McWilliams L</searchLink>; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22O'Connor+MJ%22">O'Connor MJ</searchLink>; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Orme+JP%22">Orme JP</searchLink>; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Pachl+F%22">Pachl F</searchLink>; Discovery Sciences, R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Packer+MJ%22">Packer MJ</searchLink>; Computational Chemistry, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Pei+X%22">Pei X</searchLink>; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China.<br /><searchLink fieldCode="AU" term="%22Pike+A%22">Pike A</searchLink>; DMPK, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Schimpl+M%22">Schimpl M</searchLink>; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22She+H%22">She H</searchLink>; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China.<br /><searchLink fieldCode="AU" term="%22Staniszewska+AD%22">Staniszewska AD</searchLink>; Bioscience, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Talbot+V%22">Talbot V</searchLink>; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Underwood+E%22">Underwood E</searchLink>; Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Varnes+JG%22">Varnes JG</searchLink>; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Xue+L%22">Xue L</searchLink>; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China.<br /><searchLink fieldCode="AU" term="%22Yao+T%22">Yao T</searchLink>; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China.<br /><searchLink fieldCode="AU" term="%22Zhang+K%22">Zhang K</searchLink>; Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing 100176, P. R. China.<br /><searchLink fieldCode="AU" term="%22Zhang+AX%22">Zhang AX</searchLink>; Discovery Sciences, R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Zheng+X%22">Zheng X</searchLink>; Chemistry, Oncology R&D, AstraZeneca, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States. – Name: TitleSource Label: Source Group: Src Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2024 Dec 26; Vol. 67 (24), pp. 21717-21728. <i>Date of Electronic Publication: </i>2024 Dec 10. – Name: TypePub Label: Publication Type Group: TypPub Data: Journal Article – Name: TitleSource Label: Journal Info Group: Src Data: <i>Publisher: </i><searchLink fieldCode="PB" term="%22American+Chemical+Society%22">American Chemical Society </searchLink><i>Country of Publication: </i>United States <i>NLM ID: </i>9716531 <i>Publication Model: </i>Print-Electronic <i>Cited Medium: </i>Internet <i>ISSN: </i>1520-4804 (Electronic) <i>Linking ISSN: </i><searchLink fieldCode="IS" term="%2200222623%22">00222623 </searchLink><i>NLM ISO Abbreviation: </i>J Med Chem <i>Subsets: </i>MEDLINE |
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