WO2018177444A3 - 一种氮杂非那烯-3-酮的衍生物及其制备方法与应用 - Google Patents

一种氮杂非那烯-3-酮的衍生物及其制备方法与应用 Download PDF

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Publication number
WO2018177444A3
WO2018177444A3 PCT/CN2018/088201 CN2018088201W WO2018177444A3 WO 2018177444 A3 WO2018177444 A3 WO 2018177444A3 CN 2018088201 W CN2018088201 W CN 2018088201W WO 2018177444 A3 WO2018177444 A3 WO 2018177444A3
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WIPO (PCT)
Prior art keywords
derivative
azaphenalene
preparation
application
method therefor
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PCT/CN2018/088201
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English (en)
French (fr)
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WO2018177444A2 (zh
Inventor
张�浩
王小东
徐卫良
徐炜政
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苏州康润医药有限公司
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Priority to US16/497,773 priority Critical patent/US10669274B2/en
Publication of WO2018177444A2 publication Critical patent/WO2018177444A2/zh
Publication of WO2018177444A3 publication Critical patent/WO2018177444A3/zh

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/16—Peri-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

一种氮杂非那烯-3-酮的衍生物及其制备方法与应用，属于药物合成技术领域。其结构如式（I）所示，其中R为氢，2-氟乙胺基，2，2，2-三氟乙胺基，二乙胺基，吡咯烷基，咪唑基，哌啶基，吗啡啉基，4-一甲氨基哌啶基，4-二甲氨基哌啶基，1-甲基-4-(甲氨基)哌啶基，1-苯基-4-甲氨基哌啶基，1-苄基-4-甲氨基哌啶基或者7-氟-1，2，3，4-四氢异喹啉基，本发明所述氮杂非那烯-3-酮衍生物制备过程简单，合成率高，后处理容易，并且纯度高，具有很高的抑制PARP酶的活性，为研发出活性更好的抗肿瘤药物提供基础，应用于PARP抑制剂。
PCT/CN2018/088201 2017-03-31 2018-05-24 一种氮杂非那烯-3-酮的衍生物及其制备方法与应用 WO2018177444A2 (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US16/497,773 US10669274B2 (en) 2017-03-31 2018-05-24 Azaphenalene-3-one derivative, preparation method therefor, and application therof

Applications Claiming Priority (2)

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CN201710205740.2A CN106883232B (zh) 2017-03-31 2017-03-31 一种氮杂非那烯-3-酮的衍生物及其制备方法与应用
CN201710205740.2 2017-03-31

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WO2018177444A2 WO2018177444A2 (zh) 2018-10-04
WO2018177444A3 true WO2018177444A3 (zh) 2018-11-22

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CN (1) CN106883232B (zh)
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Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106883232B (zh) * 2017-03-31 2019-01-22 苏州康润医药有限公司 一种氮杂非那烯-3-酮的衍生物及其制备方法与应用
CN113527332B (zh) * 2020-04-13 2022-07-26 南开大学 具有生物活性的卡波特韦衍生物及其制备方法和应用
CN112851558B (zh) * 2021-02-05 2022-01-07 大连理工大学 2-氰基非那烯酮类化合物及其在白血病治疗中的应用
CN116253655A (zh) * 2023-03-10 2023-06-13 宁夏顺邦达新材料有限公司 一种合成邻氨基苯甲酸甲酯的方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102341394A (zh) * 2009-01-23 2012-02-01 武田药品工业株式会社 聚(adp-核糖)聚合酶(parp)抑制剂
CN103703004A (zh) * 2011-12-31 2014-04-02 百济神州有限公司 作为parp抑制剂的稠合的四环或五环的二氢二氮杂*并咔唑酮
CN106083849A (zh) * 2011-12-31 2016-11-09 百济神州有限公司 作为parp抑制剂的稠合的四元或五元环吡啶并酞嗪酮类化合物
CN106883232A (zh) * 2017-03-31 2017-06-23 苏州康润医药有限公司 一种氮杂非那烯‑3‑酮的衍生物及其制备方法与应用

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102341394A (zh) * 2009-01-23 2012-02-01 武田药品工业株式会社 聚(adp-核糖)聚合酶(parp)抑制剂
CN103703004A (zh) * 2011-12-31 2014-04-02 百济神州有限公司 作为parp抑制剂的稠合的四环或五环的二氢二氮杂*并咔唑酮
CN106083849A (zh) * 2011-12-31 2016-11-09 百济神州有限公司 作为parp抑制剂的稠合的四元或五元环吡啶并酞嗪酮类化合物
CN106883232A (zh) * 2017-03-31 2017-06-23 苏州康润医药有限公司 一种氮杂非那烯‑3‑酮的衍生物及其制备方法与应用

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Publication number Publication date
US10669274B2 (en) 2020-06-02
US20200031828A1 (en) 2020-01-30
WO2018177444A2 (zh) 2018-10-04
CN106883232B (zh) 2019-01-22
CN106883232A (zh) 2017-06-23

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