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CN113490670A - 含氮多环稠环类化合物,其药物组合物、制备方法和用途 - Google Patents

含氮多环稠环类化合物,其药物组合物、制备方法和用途 Download PDF

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CN113490670A
CN113490670A CN202080012923.2A CN202080012923A CN113490670A CN 113490670 A CN113490670 A CN 113490670A CN 202080012923 A CN202080012923 A CN 202080012923A CN 113490670 A CN113490670 A CN 113490670A
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radical
group
ret
compound
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CN113490670B (zh
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钟俊
刘永波
刘利彬
陈肖虎
王皓
芦颖
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Beijing Zhijianjinrui Biomedical Technology Co ltd
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Beijing Zhijianjinrui Biomedical Technology Co ltd
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    • 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
    • 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
    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/496—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
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

本发明涉及药物化学领域，具体涉及式I所示含氮多环稠环类化合物，其药物组合物、制备方法和用途。本发明的化合物可以作为一种高度选择性和非常有效的RET抑制剂，此类化合物对RET看门残基突变体RET V804M突变、RET溶剂前沿残基突变体RET G810R和其他临床相关RET突变体以及RET wt均有较强的抑制作用，该化合物还能显著抑制甲状腺癌来源的TT细胞系和各种RET突变体转化的Ba/F3细胞的生长，并能显著诱导TT细胞死亡。

Description

PCT国内申请，说明书已公开。

Claims (107)

  1. PCT国内申请，权利要求书已公开。
CN202080012923.2A 2019-08-05 2020-08-05 含氮多环稠环类化合物,其药物组合物、制备方法和用途 Active CN113490670B (zh)

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CN201910719005 2019-08-05
CN2019107190052 2019-08-05
PCT/CN2020/107049 WO2021023209A1 (zh) 2019-08-05 2020-08-05 含氮多环稠环类化合物，其药物组合物、制备方法和用途

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CN113490670B CN113490670B (zh) 2023-06-02

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US (1) US20220332731A1 (zh)
EP (1) EP3992197A4 (zh)
JP (1) JP2022543713A (zh)
KR (1) KR20220042293A (zh)
CN (1) CN113490670B (zh)
WO (1) WO2021023209A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114907338A (zh) * 2021-02-08 2022-08-16 北京志健金瑞生物医药科技有限公司 含氮多环稠环类化合物，其药物组合物、制备方法和用途

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4316490A4 (en) * 2021-03-24 2025-03-05 Sichuan Kelun Biotech Biopharmaceutical Co Ltd USE OF HETEROCYCLIC COMPOUND IN TREATMENT OF DISEASES ASSOCIATED WITH DRUG RESISTANT KINASE MUTATION AND RELATED METHOD
CN115594678B (zh) * 2021-07-09 2024-11-15 北京志健金瑞生物医药科技有限公司 含氮多环稠环类化合物的制备方法及其中间体和用途
WO2024109909A1 (zh) * 2022-11-25 2024-05-30 北京志健金瑞生物医药科技有限公司 稠环化合物的固体形式及其制备方法和用途
WO2024240017A1 (zh) * 2023-05-19 2024-11-28 四川科伦博泰生物医药股份有限公司 杂环化合物治疗与ret基因改变相关疾病的用途和方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8426437B2 (en) * 2005-07-01 2013-04-23 Pierre Fabre Medicament Pyrroloquinoline derivatives and their use as protein kinases inhibitors
WO2017011776A1 (en) * 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
US10112942B2 (en) * 2016-10-10 2018-10-30 Array Biopharma Inc. Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
WO2020064009A1 (zh) * 2018-09-30 2020-04-02 北京志健金瑞生物医药科技有限公司 取代吡唑稠环类衍生物及其制备方法和应用
CN114907338A (zh) * 2021-02-08 2022-08-16 北京志健金瑞生物医药科技有限公司 含氮多环稠环类化合物，其药物组合物、制备方法和用途

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FR2502618A1 (fr) 1981-03-25 1982-10-01 Synthelabo Derives de pyridine, leur preparation et leur application en therapeutique
US20180050993A1 (en) 2015-02-03 2018-02-22 Trillium Therapeutics Inc. Novel fluorinated derivatives as egfr inhibitors useful for treating cancers

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8426437B2 (en) * 2005-07-01 2013-04-23 Pierre Fabre Medicament Pyrroloquinoline derivatives and their use as protein kinases inhibitors
WO2017011776A1 (en) * 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
US10112942B2 (en) * 2016-10-10 2018-10-30 Array Biopharma Inc. Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
WO2020064009A1 (zh) * 2018-09-30 2020-04-02 北京志健金瑞生物医药科技有限公司 取代吡唑稠环类衍生物及其制备方法和应用
CN114907338A (zh) * 2021-02-08 2022-08-16 北京志健金瑞生物医药科技有限公司 含氮多环稠环类化合物，其药物组合物、制备方法和用途

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114907338A (zh) * 2021-02-08 2022-08-16 北京志健金瑞生物医药科技有限公司 含氮多环稠环类化合物，其药物组合物、制备方法和用途
CN114907338B (zh) * 2021-02-08 2024-02-06 北京志健金瑞生物医药科技有限公司 含氮多环稠环类化合物，其药物组合物、制备方法和用途

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EP3992197A4 (en) 2023-08-30
US20220332731A1 (en) 2022-10-20
JP2022543713A (ja) 2022-10-14
CN113490670B (zh) 2023-06-02
KR20220042293A (ko) 2022-04-05
WO2021023209A1 (zh) 2021-02-11
EP3992197A1 (en) 2022-05-04

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