CN111247150A - Fgfr抑制剂及其医药用途 - Google Patents

Fgfr抑制剂及其医药用途 Download PDF

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Publication number
CN111247150A
CN111247150A CN201880052899.8A CN201880052899A CN111247150A CN 111247150 A CN111247150 A CN 111247150A CN 201880052899 A CN201880052899 A CN 201880052899A CN 111247150 A CN111247150 A CN 111247150A
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compound
pharmaceutically acceptable
synthesis
acceptable salt
acid
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CN201880052899.8A
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CN111247150B (zh
Inventor
王一恺
张杨
陈正霞
陈琳琳
冯韬
黄荣新
李秋
李德尧
孙继奎
徐洋洋
李婕
黎健
陈曙辉
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CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co Ltd
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CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co Ltd
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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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • 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
    • 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
    • C07D487/10—Spiro-condensed systems

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

Abstract

本发明公开了一类FGFR抑制剂，及其在制备治疗与FGFR相关疾病的药物中的应用。具体公开了式（Ⅰ）所示化合物及其药学上可接受的盐。

Description

PCT国内申请，说明书已公开。

Claims (19)

  1. PCT国内申请，权利要求书已公开。
CN201880052899.8A 2017-08-15 2018-08-15 Fgfr抑制剂及其医药用途 Active CN111247150B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2017106980863 2017-08-15
CN201710698086 2017-08-15
PCT/CN2018/100638 WO2019034076A1 (zh) 2017-08-15 2018-08-15 Fgfr抑制剂及其医药用途

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CN111247150A true CN111247150A (zh) 2020-06-05
CN111247150B CN111247150B (zh) 2022-11-08

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US (1) US11236094B2 (zh)
EP (1) EP3670513B1 (zh)
JP (1) JP7341122B2 (zh)
KR (1) KR20200041361A (zh)
CN (1) CN111247150B (zh)
AU (1) AU2018317153B2 (zh)
CA (1) CA3072979A1 (zh)
RU (1) RU2771311C2 (zh)
WO (1) WO2019034076A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
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CN114712365A (zh) * 2022-06-07 2022-07-08 山东绿叶制药有限公司 Trk抑制剂在制备治疗迟发性运动障碍药物中的应用

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WO2019034076A1 (zh) * 2017-08-15 2019-02-21 南京明德新药研发股份有限公司 Fgfr抑制剂及其医药用途
US20220177475A1 (en) 2019-02-15 2022-06-09 Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd Fgfr inhibitor compound in solid form and preparation method therefor
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021089005A1 (zh) * 2019-11-08 2021-05-14 石药集团中奇制药技术（石家庄）有限公司 一种fgfr抑制剂的用途
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN114057749B (zh) * 2021-11-19 2023-12-22 药雅科技(上海)有限公司 不可逆炔类杂环化合物fgfr抑制剂的制备方法和用途
CN114853740B (zh) * 2021-02-03 2023-08-01 药雅科技(上海)有限公司 炔类嘧啶化合物作为fgfr抑制剂的制备方法和用途
US20240109896A1 (en) * 2021-02-03 2024-04-04 Ya Therapeutics Inc Fgfr kinase inhibitor and use thereof
CN115433190A (zh) * 2021-06-02 2022-12-06 药雅科技(上海)有限公司 不可逆杂环化合物fgfr抑制剂的制备方法和用途
CN115141176B (zh) * 2021-03-31 2023-08-22 药雅科技(上海)有限公司 炔代吲哚类fgfr抑制剂及其制备方法和用途
CN115215868A (zh) * 2021-04-14 2022-10-21 药雅科技(上海)有限公司 杂环化合物fgfr抑制剂的制备方法和用途

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WO2007056170A2 (en) * 2005-11-02 2007-05-18 Bayer Healthcare Ag Pyrrolo[2,1-f] [1,2,4] triazin-4-ylamines igf-1r kinase inhibitors for the treatment of cancer and other hyperproliferative diseases
WO2013087578A1 (en) * 2011-12-15 2013-06-20 Bayer Pharma Aktiengesellschaft Disubstituted benzothienyl-pyrrolotriazines and their use as fgfr kinase inhibitors
WO2013124316A1 (en) * 2012-02-23 2013-08-29 Bayer Intellectual Property Gmbh Substituted benzothienyl-pyrrolotriazines and uses thereof
CN104159900A (zh) * 2011-12-15 2014-11-19 拜耳知识产权有限责任公司 取代的苯并噻吩基-吡咯并三嗪及其在癌症治疗中的用途
WO2016091849A2 (en) * 2014-12-11 2016-06-16 Bayer Pharma Aktiengesellschaft Use of pan fgfr inhibitors and method of identifying patients with cancer eligible for treatment with a pan fgfr inhibitor
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CN104159900A (zh) * 2011-12-15 2014-11-19 拜耳知识产权有限责任公司 取代的苯并噻吩基-吡咯并三嗪及其在癌症治疗中的用途
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114712365A (zh) * 2022-06-07 2022-07-08 山东绿叶制药有限公司 Trk抑制剂在制备治疗迟发性运动障碍药物中的应用

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CA3072979A1 (en) 2019-02-21
RU2020110780A3 (zh) 2021-09-16
AU2018317153A1 (en) 2020-03-05
EP3670513A1 (en) 2020-06-24
AU2018317153B2 (en) 2021-12-23
RU2771311C2 (ru) 2022-04-29
WO2019034076A1 (zh) 2019-02-21
JP7341122B2 (ja) 2023-09-08
JP2020532500A (ja) 2020-11-12
US20200207773A1 (en) 2020-07-02
RU2020110780A (ru) 2021-09-16
US11236094B2 (en) 2022-02-01
EP3670513A4 (en) 2021-04-14
EP3670513B1 (en) 2023-09-20
KR20200041361A (ko) 2020-04-21
CN111247150B (zh) 2022-11-08

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