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CN109563091A - Fgfr4抑制剂及其制备方法和应用 - Google Patents

Fgfr4抑制剂及其制备方法和应用 Download PDF

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Publication number
CN109563091A
CN109563091A CN201780032145.1A CN201780032145A CN109563091A CN 109563091 A CN109563091 A CN 109563091A CN 201780032145 A CN201780032145 A CN 201780032145A CN 109563091 A CN109563091 A CN 109563091A
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China
Prior art keywords
alkyl
heterocyclic ring
circle heterocyclic
base
halogen
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CN201780032145.1A
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CN109563091B (zh
Inventor
高鹏
孙广俊
谭松良
刘磊
包如迪
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical Co Ltd
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical Co Ltd
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    • 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
    • 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
    • C07D471/04—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

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

Abstract

提供一种具有式(Ⅰ)结构的FGFR4抑制剂及其制备方法和应用。所述式(Ⅰ)系列化合物对FGFR4激酶活性具有很强的抑制作用，并具有非常高的选择性，可广泛应用于制备治疗癌症特别是肝癌、胃癌、前列腺癌、皮肤癌、卵巢癌、肺癌、乳腺癌或结肠癌的药物，有望开发成新一代FGFR4抑制剂药物。

Description

PCT国内申请，说明书已公开。

Claims (17)

  1. PCT国内申请，权利要求书已公开。
CN201780032145.1A 2016-08-12 2017-08-11 Fgfr4抑制剂及其制备方法和应用 Active CN109563091B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201610668101 2016-08-12
CN2016106681015 2016-08-12
CN2016111876742 2016-12-20
CN201611187674 2016-12-20
PCT/CN2017/097044 WO2018028664A1 (zh) 2016-08-12 2017-08-11 Fgfr4抑制剂及其制备方法和应用

Publications (2)

Publication Number Publication Date
CN109563091A true CN109563091A (zh) 2019-04-02
CN109563091B CN109563091B (zh) 2022-04-29

Family

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CN201780032145.1A Active CN109563091B (zh) 2016-08-12 2017-08-11 Fgfr4抑制剂及其制备方法和应用

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US (1) US11608332B2 (zh)
EP (1) EP3498707A4 (zh)
JP (1) JP7088906B2 (zh)
CN (1) CN109563091B (zh)
TW (1) TWI800489B (zh)
WO (1) WO2018028664A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113072550A (zh) * 2020-01-06 2021-07-06 周龙兴 一种高选择性成纤维细胞生长因子受体抑制剂和应用

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110240598B (zh) * 2018-03-09 2023-07-25 上海翰森生物医药科技有限公司 甲酰胺衍生物的制备方法及其中间体化合物
CN108558869B (zh) * 2018-05-10 2019-04-09 西安培华学院 用于治疗肝癌的化合物及其制剂
TWI723480B (zh) 2018-07-27 2021-04-01 大陸商北京加科思新藥研發有限公司 用作fgfr4抑制劑的稠環衍生物
CN111138459B (zh) * 2018-11-06 2022-10-18 南京圣和药业股份有限公司 Fgfr4抑制剂的光学异构体及其应用
CN111662285B (zh) * 2019-03-07 2023-05-16 江苏豪森药业集团有限公司 2-氧代-1,3-氧杂氮杂环庚衍生物的制备方法
WO2020257527A1 (en) * 2019-06-21 2020-12-24 Terns, Inc. Compounds for inhibiting fgfr4
CN116528866A (zh) * 2020-11-02 2023-08-01 北京加科思新药研发有限公司 Fgfr4抑制剂的盐的晶型

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010119284A1 (en) * 2009-04-15 2010-10-21 Astex Therapeutics Limited Bicyclic heterocyclyl derivatives as fgfr kinase inhibitors for therapeutic use
CN104011051A (zh) * 2011-10-28 2014-08-27 阿斯特克斯治疗有限公司 通过fgfr激酶抑制抗癌的吡啶并吡嗪
CN105683188A (zh) * 2013-10-25 2016-06-15 诺华股份有限公司 作为fgfr4抑制剂的稠环二环吡啶基衍生物
CN109071532A (zh) * 2016-05-20 2018-12-21 江苏豪森药业集团有限公司 Fgfr4抑制剂、其制备方法和应用
CN109153678A (zh) * 2016-05-27 2019-01-04 杭州英创医药科技有限公司 作为fgfr4抑制剂的杂环化合物

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017164705A1 (ko) * 2016-03-24 2017-09-28 재단법인 대구경북첨단의료산업진흥재단 신규한 피리딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 fgfr 관련 질환의 예방 또는 치료용 약학적 조성물

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010119284A1 (en) * 2009-04-15 2010-10-21 Astex Therapeutics Limited Bicyclic heterocyclyl derivatives as fgfr kinase inhibitors for therapeutic use
CN104011051A (zh) * 2011-10-28 2014-08-27 阿斯特克斯治疗有限公司 通过fgfr激酶抑制抗癌的吡啶并吡嗪
CN105683188A (zh) * 2013-10-25 2016-06-15 诺华股份有限公司 作为fgfr4抑制剂的稠环二环吡啶基衍生物
CN109071532A (zh) * 2016-05-20 2018-12-21 江苏豪森药业集团有限公司 Fgfr4抑制剂、其制备方法和应用
CN109153678A (zh) * 2016-05-27 2019-01-04 杭州英创医药科技有限公司 作为fgfr4抑制剂的杂环化合物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
WENJUN ZHOU等: "A Structure-Guided Approach to Creating Covalent FGFR Inhibitors", 《CHEMISTRY & BIOLOGY》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113072550A (zh) * 2020-01-06 2021-07-06 周龙兴 一种高选择性成纤维细胞生长因子受体抑制剂和应用
CN113072550B (zh) * 2020-01-06 2023-08-08 周龙兴 一种高选择性成纤维细胞生长因子受体抑制剂和应用

Also Published As

Publication number Publication date
WO2018028664A1 (zh) 2018-02-15
EP3498707A4 (en) 2020-04-08
JP7088906B2 (ja) 2022-06-21
US20220024913A1 (en) 2022-01-27
US11608332B2 (en) 2023-03-21
CN109563091B (zh) 2022-04-29
JP2019527701A (ja) 2019-10-03
TW201805286A (zh) 2018-02-16
EP3498707A1 (en) 2019-06-19
TWI800489B (zh) 2023-05-01

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