CN115135636A - 喹喔啉酮衍生物作为kras g12c突变蛋白的不可逆抑制剂 - Google Patents

喹喔啉酮衍生物作为kras g12c突变蛋白的不可逆抑制剂 Download PDF

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CN115135636A
CN115135636A CN202180015592.2A CN202180015592A CN115135636A CN 115135636 A CN115135636 A CN 115135636A CN 202180015592 A CN202180015592 A CN 202180015592A CN 115135636 A CN115135636 A CN 115135636A
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alkylene
haloalkyl
halogen
alkyl radical
alkynyl
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CN115135636B (zh
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赵焰平
王红军
张道广
肖绪枝
叶佳
冒莉
姜媛媛
禄立彦
黄淮
牛海涛
黄建宝
刘森
刘雪莲
周丽莹
刘亚男
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Beijing Tide Pharmaceutical Co Ltd
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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
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    • C07—ORGANIC CHEMISTRY
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    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/42—Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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Abstract

本发明涉及新的喹喔啉酮衍生物，其可作为KRAS G12C突变蛋白的不可逆抑制剂。本发明还涉及含有该喹喔啉酮衍生物的药物组合物，及其制备方法和用途。

Description

PCT国内申请，说明书已公开。

Claims (28)

  1. PCT国内申请，权利要求书已公开。
CN202180015592.2A 2020-04-29 2021-04-29 喹喔啉酮衍生物作为kras g12c突变蛋白的不可逆抑制剂 Active CN115135636B (zh)

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Application Number Priority Date Filing Date Title
CN202010354437 2020-04-29
CN2020103544347 2020-04-29
CN2020103544370 2020-04-29
CN202010354434 2020-04-29
CN2021103903607 2021-04-12
CN202110390360 2021-04-12
CN202110446892 2021-04-25
CN2021104468928 2021-04-25
PCT/CN2021/091102 WO2021219091A2 (zh) 2020-04-29 2021-04-29 喹喔啉酮衍生物作为kras g12c突变蛋白的不可逆抑制剂

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CN115135636B CN115135636B (zh) 2024-08-23

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CN202180015592.2A Active CN115135636B (zh) 2020-04-29 2021-04-29 喹喔啉酮衍生物作为kras g12c突变蛋白的不可逆抑制剂

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EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
EP4021444A4 (en) 2019-08-29 2023-01-04 Mirati Therapeutics, Inc. G12D KRAS INHIBITORS
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AU2020405170A1 (en) 2019-12-20 2022-06-30 Mirati Therapeutics, Inc. SOS1 inhibitors
WO2022111527A1 (zh) * 2020-11-24 2022-06-02 成都百裕制药股份有限公司 哌嗪-2,3-二酮衍生物及其在医药上的应用
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
CN117616031A (zh) 2021-05-05 2024-02-27 锐新医药公司 用于治疗癌症的ras抑制剂
JP2024517847A (ja) 2021-05-05 2024-04-23 レボリューション メディシンズ インコーポレイテッド Ｒａｓ阻害剤
US20240293558A1 (en) 2021-06-16 2024-09-05 Erasca, Inc. Kras inhibitor conjugates
AU2022320304A1 (en) 2021-07-27 2024-02-29 Toray Industries, Inc. Medicament for treatment and/or prevention of cancer
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WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
KR20230164602A (ko) * 2022-05-25 2023-12-04 주식회사 엘지화학 다이아실글리세롤 키나아제 저해제로서 헤테로사이클 화합물 및 이의 용도
WO2023229378A1 (ko) * 2022-05-25 2023-11-30 주식회사 엘지화학 다이아실글리세롤 키나아제 저해제로서 헤테로사이클 화합물 및 이의 용도
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WO2024019995A1 (en) * 2022-07-19 2024-01-25 Dana-Farber Cancer Institute, Inc. Quinoxalinedione and pyrido [2, 3-b]pyrazine-2, 3-dione b cell lymphoma 6 (bcl6) degraders and uses thereof
WO2024169848A1 (zh) * 2023-02-17 2024-08-22 南京同诺康医药科技有限公司 miR-124诱导剂及其制备方法和用途
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CN115151532B (zh) 2023-06-06
CN115135636B (zh) 2024-08-23
WO2021219091A3 (zh) 2021-12-23
CN115151532A (zh) 2022-10-04
WO2021219090A1 (zh) 2021-11-04
TW202200563A (zh) 2022-01-01
TW202200562A (zh) 2022-01-01

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