CN110167941A - 取代的稠合杂芳基化合物作为激酶抑制剂及其应用 - Google Patents

取代的稠合杂芳基化合物作为激酶抑制剂及其应用 Download PDF

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CN110167941A
CN110167941A CN201880006343.5A CN201880006343A CN110167941A CN 110167941 A CN110167941 A CN 110167941A CN 201880006343 A CN201880006343 A CN 201880006343A CN 110167941 A CN110167941 A CN 110167941A
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base
dimethyl
triazole simultaneously
quinoxaline
phenyl
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CN201880006343.5A
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CN110167941B (zh
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蔡遂雄
田野
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Impact Therapeutics Inc
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Impact Therapeutics Inc
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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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C07D487/04—Ortho-condensed systems

Abstract

本发明提供取代的稠合杂芳基化合物作为激酶抑制剂及其应用。具体而言，本发明提供下式I的化合物，或其可药用盐或前药，其中A1‑A4，B1‑B3，D1‑D4和R1‑R3为本文所定义。式I的化合物是激酶抑制剂。因此，本发明的化合物可用于治疗因为DDR功能缺陷而引起的临床病症，例如癌症。

Description

PCT国内申请，说明书已公开。

Claims (11)

  1. PCT国内申请，权利要求书已公开。
CN201880006343.5A 2017-01-09 2018-01-09 取代的稠合杂芳基化合物作为激酶抑制剂及其应用 Active CN110167941B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2017100145201 2017-01-09
CN201710014520 2017-01-09
PCT/CN2018/071851 WO2018127195A1 (zh) 2017-01-09 2018-01-09 取代的稠合杂芳基化合物作为激酶抑制剂及其应用

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CN110167941A true CN110167941A (zh) 2019-08-23
CN110167941B CN110167941B (zh) 2023-04-04

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US (1) US10874670B2 (zh)
EP (1) EP3567041B1 (zh)
JP (1) JP7247092B2 (zh)
KR (1) KR102660196B1 (zh)
CN (1) CN110167941B (zh)
AU (1) AU2018206111B2 (zh)
CA (1) CA3049608A1 (zh)
WO (1) WO2018127195A1 (zh)

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CN114728945A (zh) * 2019-09-06 2022-07-08 上海瑛派药业有限公司 3,5-二取代吡唑化合物作为激酶抑制剂及其应用

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* Cited by examiner, † Cited by third party
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US10981918B2 (en) * 2018-07-20 2021-04-20 Grünenthal GmbH Further substituted triazolo quinoxaline derivatives
US20220259211A1 (en) * 2019-07-10 2022-08-18 Impact Therapeutics (Shanghai), Inc Substituted pyrazoloquinazolinone compounds and application thereof
AU2020344050A1 (en) * 2019-09-12 2022-04-07 Impact Therapeutics (Shanghai), Inc Substituted imidazoquinoxaline compounds and uses thereof
KR102458689B1 (ko) * 2020-07-08 2022-10-25 원광대학교산학협력단 피페리딘 화합물 및 이의 제조 방법
EP4329739A1 (en) * 2021-04-26 2024-03-06 Ohio State Innovation Foundation Lipid nanomaterials and uses thereof

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WO2009155527A2 (en) * 2008-06-19 2009-12-23 Progenics Pharmaceuticals, Inc. Phosphatidylinositol 3 kinase inhibitors
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CN103080092A (zh) * 2010-07-01 2013-05-01 默克专利股份公司 吡唑并喹啉类化合物
CN103124731A (zh) * 2010-09-16 2013-05-29 和记黄埔医药（上海）有限公司 稠合的杂芳基化合物及其应用
CN106255692A (zh) * 2014-05-08 2016-12-21 阿斯利康(瑞典)有限公司 咪唑并[4,5‑c]喹啉‑2‑酮化合物以及它们在治疗癌症中的用途

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US3989816A (en) 1975-06-19 1976-11-02 Nelson Research & Development Company Vehicle composition containing 1-substituted azacycloheptan-2-ones
US4444762A (en) 1980-04-04 1984-04-24 Nelson Research & Development Company Vehicle composition containing 1-substituted azacyclopentan-2-ones
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WO2009155527A2 (en) * 2008-06-19 2009-12-23 Progenics Pharmaceuticals, Inc. Phosphatidylinositol 3 kinase inhibitors
CN103080092A (zh) * 2010-07-01 2013-05-01 默克专利股份公司 吡唑并喹啉类化合物
CN102399218A (zh) * 2010-09-16 2012-04-04 和记黄埔医药（上海）有限公司 一类并合三杂环及其作为pi3k抑制剂的用途
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CN114728945B (zh) * 2019-09-06 2024-01-16 上海瑛派药业有限公司 3,5-二取代吡唑化合物作为激酶抑制剂及其应用

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Publication number Publication date
CN110167941B (zh) 2023-04-04
AU2018206111B2 (en) 2022-07-21
EP3567041A9 (en) 2022-04-20
EP3567041C0 (en) 2023-12-27
EP3567041B1 (en) 2023-12-27
EP3567041A4 (en) 2020-08-05
WO2018127195A1 (zh) 2018-07-12
JP2020504139A (ja) 2020-02-06
KR102660196B1 (ko) 2024-04-24
EP3567041A1 (en) 2019-11-13
US20190358225A1 (en) 2019-11-28
AU2018206111A1 (en) 2019-08-22
JP7247092B2 (ja) 2023-03-28
US10874670B2 (en) 2020-12-29
CA3049608A1 (en) 2018-07-12
KR20190098266A (ko) 2019-08-21

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