CN113874374A - 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用 - Google Patents

氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用 Download PDF

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Publication number
CN113874374A
CN113874374A CN202080038170.2A CN202080038170A CN113874374A CN 113874374 A CN113874374 A CN 113874374A CN 202080038170 A CN202080038170 A CN 202080038170A CN 113874374 A CN113874374 A CN 113874374A
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haloalkyl
alkoxy
hydroxyalkyl
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CN202080038170.2A
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Inventor
陆标
张俊珍
张蔡华
贺峰
白昌
陶维康
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Publication of CN113874374A publication Critical patent/CN113874374A/zh
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/04—Ortho-condensed systems

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

Abstract

本发明提供了氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用。具体而言，本发明提供了一种通式(I)所示的氢化吡啶并嘧啶类衍生物、其制备方法及含有该衍生物的药物组合物以及其作为治疗剂，特别是作为KRAS抑制剂的用途，其中通式(I)的各取代基与说明书中的定义相同。

Description

PCT国内申请，说明书已公开。

Claims (23)

  1. PCT国内申请，权利要求书已公开。
CN202080038170.2A 2019-05-24 2020-05-22 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用 Pending CN113874374A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2019104374143 2019-05-24
CN201910437414 2019-05-24
CN2020101115421 2020-02-24
CN202010111542 2020-02-24
PCT/CN2020/091776 WO2020238791A1 (zh) 2019-05-24 2020-05-22 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用

Publications (1)

Publication Number Publication Date
CN113874374A true CN113874374A (zh) 2021-12-31

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Country Status (3)

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CN (1) CN113874374A (zh)
TW (1) TW202110837A (zh)
WO (1) WO2020238791A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
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CN112341457A (zh) * 2019-08-07 2021-02-09 北京加科思新药研发有限公司 Kras突变蛋白抑制剂

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JP7451419B2 (ja) 2018-10-26 2024-03-18 大鵬薬品工業株式会社 新規なインダゾール化合物又はその塩
CN112694475A (zh) * 2019-10-23 2021-04-23 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
IL292438A (en) 2019-10-28 2022-06-01 Merck Sharp & Dohme Small molecules that inhibit the g12c mutant of kras
CN113980014B (zh) * 2020-07-27 2023-05-12 江苏恒瑞医药股份有限公司 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用
TW202229285A (zh) * 2020-11-20 2022-08-01 大陸商北京加科思新藥研發有限公司 Kras g12d抑制劑
CN114591319B (zh) * 2020-12-04 2024-06-28 江苏先声药业有限公司 四氢吡啶并嘧啶类衍生物及其用途
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
CN115124524A (zh) * 2021-03-26 2022-09-30 浙江海正药业股份有限公司 三环类衍生物及其制备方法和用途
WO2022250170A1 (en) * 2021-05-28 2022-12-01 Taiho Pharmaceutical Co., Ltd. Small molecule inhibitors of kras mutated proteins
EP4361157A4 (en) 2021-06-21 2024-10-16 Jiangsu Hengrui Pharmaceuticals Co Ltd CONDENSED TETRACYCLIC COMPOUND, PRODUCTION PROCESS THEREOF AND APPLICATION THEREOF IN MEDICINE
WO2023031781A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
WO2024081674A1 (en) 2022-10-11 2024-04-18 Aadi Bioscience, Inc. Combination therapies for the treatment of cancer

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US20030191143A1 (en) * 2001-05-01 2003-10-09 Pitts William J. Fused heterocyclic compounds and use thereof
CN103635473A (zh) * 2011-03-10 2014-03-12 第一三共株式会社 二螺吡咯烷衍生物
US20180072723A1 (en) * 2016-05-18 2018-03-15 Mirati Therapeutics, Inc. Kras g12c inhibitors
US20190144444A1 (en) * 2017-11-15 2019-05-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
US20190270743A1 (en) * 2017-11-15 2019-09-05 Mirati Therapeutics, Inc. Kras g12c inhibitors
CN112341457A (zh) * 2019-08-07 2021-02-09 北京加科思新药研发有限公司 Kras突变蛋白抑制剂

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Publication number Priority date Publication date Assignee Title
BR112013021896A2 (pt) * 2011-02-28 2016-11-08 Array Biopharma Inc inibidores de serina/treonina cinase

Patent Citations (6)

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Publication number Priority date Publication date Assignee Title
US20030191143A1 (en) * 2001-05-01 2003-10-09 Pitts William J. Fused heterocyclic compounds and use thereof
CN103635473A (zh) * 2011-03-10 2014-03-12 第一三共株式会社 二螺吡咯烷衍生物
US20180072723A1 (en) * 2016-05-18 2018-03-15 Mirati Therapeutics, Inc. Kras g12c inhibitors
US20190144444A1 (en) * 2017-11-15 2019-05-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
US20190270743A1 (en) * 2017-11-15 2019-09-05 Mirati Therapeutics, Inc. Kras g12c inhibitors
CN112341457A (zh) * 2019-08-07 2021-02-09 北京加科思新药研发有限公司 Kras突变蛋白抑制剂

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112341457A (zh) * 2019-08-07 2021-02-09 北京加科思新药研发有限公司 Kras突变蛋白抑制剂

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TW202110837A (zh) 2021-03-16

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