CN113993860A - 作为kras g12c突变蛋白抑制剂的七元杂环类衍生物 - Google Patents

作为kras g12c突变蛋白抑制剂的七元杂环类衍生物 Download PDF

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CN113993860A
CN113993860A CN202080043619.4A CN202080043619A CN113993860A CN 113993860 A CN113993860 A CN 113993860A CN 202080043619 A CN202080043619 A CN 202080043619A CN 113993860 A CN113993860 A CN 113993860A
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pharmaceutically acceptable
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acceptable salt
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CN113993860B (zh
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丁照中
陈曙辉
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
Medshine Discovery Inc
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
Medshine Discovery Inc
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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
    • C07D471/22—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 systems contains four or more hetero rings
    • 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
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings

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

Abstract

一类KRAS G12C突变蛋白抑制剂，具体公开了式(II)所示化合物及其异构体、药学上可接受的盐。

Description

PCT国内申请，说明书已公开。

Claims (21)

  1. PCT国内申请，权利要求书已公开。
CN202080043619.4A 2019-06-25 2020-06-24 作为kras g12c突变蛋白抑制剂的七元杂环类衍生物 Active CN113993860B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN2019105566526 2019-06-25
CN201910556652 2019-06-25
CN201910990276 2019-10-17
CN2019109902761 2019-10-17
CN201911410783 2019-12-31
CN201911410783X 2019-12-31
PCT/CN2020/098070 WO2020259573A1 (zh) 2019-06-25 2020-06-24 作为kras g12c突变蛋白抑制剂的七元杂环类衍生物

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CN113993860A true CN113993860A (zh) 2022-01-28
CN113993860B CN113993860B (zh) 2023-08-01

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US (1) US20220372036A1 (zh)
CN (1) CN113993860B (zh)
WO (1) WO2020259573A1 (zh)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2020372881A1 (en) 2019-10-28 2022-06-09 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS G12C mutant
WO2022161489A1 (zh) * 2021-02-01 2022-08-04 上海艾力斯医药科技股份有限公司 五并杂环类化合物、其制备方法及其应用
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
WO2023001141A1 (en) * 2021-07-23 2023-01-26 Shanghai Zion Pharma Co. Limited Kras g12d inhibitors and uses thereof
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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106008503A (zh) * 2015-03-31 2016-10-12 南京明德新药研发股份有限公司 螺环芳基砜作为蛋白激酶抑制剂
WO2018064510A1 (en) * 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2018206539A1 (en) * 2017-05-11 2018-11-15 Astrazeneca Ab Heteroaryl compounds that inhibit g12c mutant ras proteins
US20190177338A1 (en) * 2017-12-08 2019-06-13 Astrazeneca Ab Chemical compounds

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2014239542A1 (en) * 2013-03-15 2015-10-01 Araxes Pharma Llc Covalent inhibitors of KRas G12C
CN106488910B (zh) * 2013-10-10 2020-07-31 亚瑞克西斯制药公司 Kras g12c的抑制剂
JOP20190186A1 (ar) * 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
JOP20190272A1 (ar) * 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
CA3063440A1 (en) * 2017-05-25 2018-11-29 Araxes Pharma Llc Covalent inhibitors of kras
JP2020521741A (ja) * 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
MX2019014875A (es) * 2017-06-21 2021-01-29 SHY Therapeutics LLC Compuestos que interaccionan con la superfamilia ras para el tratamiento de cancer, enfermedades inflamatorias, rasopatias y enfermedad fibrotica.
AR112797A1 (es) * 2017-09-08 2019-12-11 Amgen Inc Inhibidores de kras g12c y métodos para utilizarlos

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106008503A (zh) * 2015-03-31 2016-10-12 南京明德新药研发股份有限公司 螺环芳基砜作为蛋白激酶抑制剂
WO2018064510A1 (en) * 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2018206539A1 (en) * 2017-05-11 2018-11-15 Astrazeneca Ab Heteroaryl compounds that inhibit g12c mutant ras proteins
US20190177338A1 (en) * 2017-12-08 2019-06-13 Astrazeneca Ab Chemical compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
吕莹雪等: "KRAS突变非小细胞肺癌的靶向治疗研究进展", 《中南药学》 *

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US20220372036A1 (en) 2022-11-24
WO2020259573A1 (zh) 2020-12-30

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