CN114269741A - 环烷基类和杂环烷基类抑制剂及其制备方法和应用 - Google Patents

环烷基类和杂环烷基类抑制剂及其制备方法和应用 Download PDF

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CN114269741A
CN114269741A CN202080048031.8A CN202080048031A CN114269741A CN 114269741 A CN114269741 A CN 114269741A CN 202080048031 A CN202080048031 A CN 202080048031A CN 114269741 A CN114269741 A CN 114269741A
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group
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cycloalkyl
compound
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吕彬华
崔大为
刘连军
韩涛
王润卿
倪沛钟
盛泽林
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Suzhou Zelgen Biopharmaceutical Co Ltd
Shanghai Zelgen Pharmatech Co Ltd
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Suzhou Zelgen Biopharmaceutical Co Ltd
Shanghai Zelgen Pharmatech Co Ltd
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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
    • C07D471/02—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
    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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

Abstract

本发明涉及环烷基类和杂环烷基类抑制剂及其制备方法和应用。具体地，本发明化合物具有式(I)所示结构，本发明还公开了所述化合物的制备方法及其作为KRASG12C抑制剂的用途，对KRASG12C具有很好的选择性抑制作用且具有更好的药效学、药代动力学性能和更低的毒副作用。

Description

PCT国内申请，说明书已公开。

Claims (12)

  1. PCT国内申请，权利要求书已公开。
CN202080048031.8A 2019-10-23 2020-10-23 环烷基类和杂环烷基类抑制剂及其制备方法和应用 Pending CN114269741A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201911013680 2019-10-23
CN201911013680X 2019-10-23
CN2019113306592 2019-12-20
CN201911330659.2A CN112694475A (zh) 2019-10-23 2019-12-20 环烷基类和杂环烷基类抑制剂及其制备方法和应用
PCT/CN2020/123405 WO2021078285A1 (zh) 2019-10-23 2020-10-23 环烷基类和杂环烷基类抑制剂及其制备方法和应用

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CN114269741A true CN114269741A (zh) 2022-04-01

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CN202080048031.8A Pending CN114269741A (zh) 2019-10-23 2020-10-23 环烷基类和杂环烷基类抑制剂及其制备方法和应用

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US11932633B2 (en) 2018-05-07 2024-03-19 Mirati Therapeutics, Inc. KRas G12C inhibitors
WO2020085493A1 (ja) 2018-10-26 2020-04-30 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
WO2020146613A1 (en) 2019-01-10 2020-07-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
CN110078597A (zh) * 2019-03-13 2019-08-02 杭州盛弗泰新材料科技有限公司 一种甘油1,3-二乙醚的制备方法
EP4021444A4 (en) 2019-08-29 2023-01-04 Mirati Therapeutics, Inc. G12D KRAS INHIBITORS
CA3152025A1 (en) 2019-09-24 2021-04-01 David BRIERE Combination therapies
JP7340100B2 (ja) 2019-10-28 2023-09-06 メルク・シャープ・アンド・ドーム・エルエルシー Ｋｒａｓ ｇ１２ｃ変異型の小分子阻害薬
CN115135315A (zh) 2019-12-20 2022-09-30 米拉蒂治疗股份有限公司 Sos1抑制剂
CN113666923A (zh) * 2020-05-15 2021-11-19 苏州泽璟生物制药股份有限公司 烷氧基烷基取代杂环基类抑制剂及其制备方法和应用
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
TW202317580A (zh) * 2021-06-18 2023-05-01 大陸商南京燧坤智能科技有限公司 用作ｋｒａｓ ｇ１２ｄ抑制劑的氘代化合物
MX2024000965A (es) 2021-07-27 2024-02-09 Toray Industries Medicamento para el tratamiento y/o prevencion de cancer.
CN117164581A (zh) * 2022-05-27 2023-12-05 苏州泽璟生物制药股份有限公司 一种kras抑制剂或其盐的多晶型物及其制剂制备
CN117164580A (zh) * 2022-05-27 2023-12-05 苏州泽璟生物制药股份有限公司 一种kras g12c抑制剂的制备方法及其中间体
CN117327103A (zh) * 2022-07-01 2024-01-02 苏州泽璟生物制药股份有限公司 取代嘧啶并环类抑制剂及其制备方法和应用
WO2024081674A1 (en) 2022-10-11 2024-04-18 Aadi Bioscience, Inc. Combination therapies for the treatment of cancer

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US20190144444A1 (en) * 2017-11-15 2019-05-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
CN109843856A (zh) * 2016-05-18 2019-06-04 米拉蒂治疗股份有限公司 Kras g12c抑制剂
WO2020055756A1 (en) * 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020118066A1 (en) * 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies

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JP2019529484A (ja) * 2016-09-29 2019-10-17 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質の阻害剤
CN110312711A (zh) * 2016-10-07 2019-10-08 亚瑞克西斯制药公司 作为ras抑制剂的杂环化合物及其使用方法
TW201942115A (zh) * 2018-02-01 2019-11-01 美商輝瑞股份有限公司 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物
TW202110837A (zh) * 2019-05-24 2021-03-16 大陸商江蘇恆瑞醫藥股份有限公司 氫化吡啶并嘧啶類衍生物、其製備方法及其在醫藥上的應用
CN112174950A (zh) * 2019-07-02 2021-01-05 津福医药(苏州)有限公司 杂环衍生物、包含其的药物组合物及其用途

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CN109843856A (zh) * 2016-05-18 2019-06-04 米拉蒂治疗股份有限公司 Kras g12c抑制剂
US20190144444A1 (en) * 2017-11-15 2019-05-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
WO2020055756A1 (en) * 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020118066A1 (en) * 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies

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US20230105745A1 (en) 2023-04-06
CN112694475A (zh) 2021-04-23
WO2021078312A1 (zh) 2021-04-29
US11459327B1 (en) 2022-10-04

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