WO2021008588A9 - 一类嘧啶喹啉衍生物及其制备方法和应用 - Google Patents

一类嘧啶喹啉衍生物及其制备方法和应用 Download PDF

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Publication number
WO2021008588A9
WO2021008588A9 PCT/CN2020/102462 CN2020102462W WO2021008588A9 WO 2021008588 A9 WO2021008588 A9 WO 2021008588A9 CN 2020102462 W CN2020102462 W CN 2020102462W WO 2021008588 A9 WO2021008588 A9 WO 2021008588A9
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WIPO (PCT)
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substituted
compounds
application
quinoline derivatives
class
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PCT/CN2020/102462
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English (en)
French (fr)
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WO2021008588A1 (zh
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陈新滋
黄沃林
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广州新民培林医药科技有限公司
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Publication of WO2021008588A1 publication Critical patent/WO2021008588A1/zh
Publication of WO2021008588A9 publication Critical patent/WO2021008588A9/zh

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

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

Abstract

本发明公开了一类嘧啶喹啉衍生物包括前药及其制备方法和应用。所述嘧啶喹啉衍生物的结构如式(I)所示;其中,R 1为氢、C 1~4烷基、C 1~4卤代烷基、C4~7杂环芳基、C4~7取代杂环芳基、苄基或取代苄基、糖基、氨基酸;R 2、R 3、R 4和R 5各自独立地为氢、C 1~4烷基、C 1~4烷氧基、羟基、氨基或取代氨基、C 1~4卤代烷基或卤素、糖基、氨基酸;R 6为取代或非取代五元杂环、取代或非取代六元杂环、取代或非取代的C 8~12稠和杂环。本发明化合物对于5种癌细胞具有很好的抑制作用,大部分化合物的抑制IC 50值低于20μM;部分化合物的IC 50值甚至低于5μM,抑制作用极为显著,可制备成为抗癌药物进行应用。
PCT/CN2020/102462 2019-07-16 2020-07-16 一类嘧啶喹啉衍生物及其制备方法和应用 WO2021008588A1 (zh)

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CN201910641563.1 2019-07-16
CN201910641563.1A CN110240590A (zh) 2019-07-16 2019-07-16 一类嘧啶喹啉衍生物及其制备方法和应用

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WO2021008588A1 WO2021008588A1 (zh) 2021-01-21
WO2021008588A9 true WO2021008588A9 (zh) 2021-03-18

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Publication number Priority date Publication date Assignee Title
CN110240590A (zh) * 2019-07-16 2019-09-17 广州新民培林医药科技有限公司 一类嘧啶喹啉衍生物及其制备方法和应用
CN112062758A (zh) * 2020-08-28 2020-12-11 广州新民培林医药科技有限公司 一种硒酚喹啉衍生物及其制备方法和应用
CN113501783B (zh) * 2021-06-30 2022-11-15 上海应用技术大学 一种毛兰素杂环衍生物及其制备方法与应用
CN113387884A (zh) * 2021-07-05 2021-09-14 艾美科健(中国)生物医药有限公司 一种孟鲁司特钠杂质h的制备方法
CN114409590B (zh) * 2021-12-28 2023-08-01 河南新中飞科技有限公司 一种具有二氢吡啶腈结构的化合物及其制备方法和应用
CN114380741B (zh) * 2022-01-11 2023-03-24 济南大学 一种2-甲基喹啉类化合物的4号位烷基化衍生物的制备方法
CN114409710B (zh) * 2022-01-19 2024-01-09 西藏大学 Nir-ii多吡啶钌配合物及其制备方法和应用
CN115093369B (zh) * 2022-07-12 2024-05-10 浙大城市学院 一种3,4-二氢异喹啉-1-酮类化合物的合成方法
CN116217475A (zh) * 2023-02-21 2023-06-06 中国医学科学院阜外医院深圳医院(深圳市孙逸仙心血管医院) 一种多取代喹啉类衍生物的制备方法

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ES2474865T3 (es) * 2006-06-22 2014-07-09 Prana Biotechnology Limited Método de tratamiento de un tumor cerebral glioma
EP2994142A4 (en) * 2013-05-08 2017-03-29 Colorado Seminary, Which Owns and Operates The University of Denver Antibiotic and anti-parasitic agents that modulate class ii fructose 1,6-bisphosphate aldolase
HUP1600234A2 (en) * 2016-04-05 2017-12-28 Mta Termeszettudomanyi Kutatokoezpont Mdr-reversing 8-hydroxy-quinoline derivatives
KR102002446B1 (ko) * 2017-03-16 2019-07-22 재단법인 대구경북첨단의료산업진흥재단 TGase 2 억제제로서의 퀴놀린-5,8-디온 유도체 및 이를 포함하는 약제학적 조성물
CN110240590A (zh) * 2019-07-16 2019-09-17 广州新民培林医药科技有限公司 一类嘧啶喹啉衍生物及其制备方法和应用

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