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CN109715626A - 作为fgfr抑制剂的杂环化合物 - Google Patents

作为fgfr抑制剂的杂环化合物 Download PDF

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Publication number
CN109715626A
CN109715626A CN201780045675.XA CN201780045675A CN109715626A CN 109715626 A CN109715626 A CN 109715626A CN 201780045675 A CN201780045675 A CN 201780045675A CN 109715626 A CN109715626 A CN 109715626A
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alkyl
ring group
independently selected
circle heterocyclic
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CN109715626B (zh
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孔祥龙
周超
陈向阳
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Nanjing Innocare Pharma Tech Co ltd
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Nanjing Innocare Pharma Tech Co ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525Isoalloxazines, e.g. riboflavins, vitamin B2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

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

Abstract

一类杂环化合物、含有其的药物组合物、以及它们的制备方法和其作为成纤维细胞生长因子受体FGFR抑制剂的用途。该抑制剂为式I所示的杂环化合物,或其药学上可接受的盐、前药、溶剂化合物、多晶型体、异构体、稳定同位素衍生物或含有其的药物组合物。上述化合物可用于治疗或预防由FGFR介导的相关疾病,如癌症。

Description

PCT国内申请,说明书已公开。

Claims (8)

  1. PCT国内申请,权利要求书已公开。
CN201780045675.XA 2016-08-09 2017-07-27 作为fgfr抑制剂的杂环化合物 Active CN109715626B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610647295.0A CN107698593A (zh) 2016-08-09 2016-08-09 作为fgfr抑制剂的杂环化合物
CN2016106472950 2016-08-09
PCT/CN2017/094620 WO2018028438A1 (zh) 2016-08-09 2017-07-27 作为fgfr抑制剂的杂环化合物

Publications (2)

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CN109715626A true CN109715626A (zh) 2019-05-03
CN109715626B CN109715626B (zh) 2022-04-26

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CN201610647295.0A Pending CN107698593A (zh) 2016-08-09 2016-08-09 作为fgfr抑制剂的杂环化合物
CN201780045675.XA Active CN109715626B (zh) 2016-08-09 2017-07-27 作为fgfr抑制剂的杂环化合物

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US (1) US10752631B2 (zh)
EP (1) EP3498706A4 (zh)
JP (1) JP6959663B2 (zh)
KR (1) KR20190035870A (zh)
CN (2) CN107698593A (zh)
CA (1) CA3032921A1 (zh)
WO (1) WO2018028438A1 (zh)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115043832A (zh) * 2021-03-08 2022-09-13 药雅科技(上海)有限公司 一种fgfr抑制剂炔代杂环类化合物及其制备方法和用途
CN116096707A (zh) * 2020-06-05 2023-05-09 金耐特生物制药公司 成纤维细胞生长因子受体激酶的抑制剂

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WO2018208856A1 (en) 2017-05-08 2018-11-15 Gritstone Oncology, Inc. Alphavirus neoantigen vectors
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
CN114127051A (zh) * 2019-05-17 2022-03-01 金耐特生物制药公司 成纤维细胞生长因子受体激酶的抑制剂
EP3976075A4 (en) 2019-05-30 2023-08-16 Gritstone bio, Inc. MODIFIED ADENOVIRUS
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム(インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル) キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
KR20230046313A (ko) 2020-08-06 2023-04-05 그릿스톤 바이오, 인코포레이티드 다중에피토프 백신 카세트
CN112480109B (zh) * 2020-11-16 2022-04-01 浙江大学 吡啶并[2,3-b]吡嗪-3(4H)-酮类衍生物及其用途
MX2023008186A (es) * 2021-01-12 2023-07-18 Beijing Innocare Pharma Tech Co Ltd Proceso para preparar (s)-1-(1-acriloilpirrolidin-3-il)-3-((3,5-di metoxifenil)etinil)-5-(metilamino)-1h-pirazol-4-carboxamida.
CN114853739B (zh) * 2021-02-03 2023-09-22 药雅科技(上海)有限公司 一种炔代吡嗪类fgfr抑制剂及其制备方法和用途
WO2024083111A1 (zh) * 2022-10-18 2024-04-25 首药控股(北京)股份有限公司 一种新型杂环化合物
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof

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WO2007087395A2 (en) * 2006-01-25 2007-08-02 Osi Pharmaceuticals, Inc. UNSATURATED mTOR INHIBITORS
CN103958512A (zh) * 2012-01-19 2014-07-30 大鹏药品工业株式会社 3,5-双取代炔基苯化合物及其盐
CN104341388A (zh) * 2013-10-16 2015-02-11 上海润诺生物科技有限公司 芳香族酰胺类衍生物、其制备方法及其在医药上的应用
EP3023100A1 (en) * 2013-07-18 2016-05-25 Taiho Pharmaceutical Co., Ltd. Antitumor drug for intermittent administration of fgfr inhibitor

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MX2015011456A (es) * 2013-03-13 2016-05-31 Boston Biomedical Inc Derivados de 3-(arilo o heteroailo) metilenindolino-2-ona como inhibidores de cinasas de la via de las celulas madres cancerosas para el tratamiento del cancer.
JP6084292B2 (ja) * 2013-07-18 2017-02-22 大鵬薬品工業株式会社 Fgfr阻害剤耐性癌の治療薬
CN104341425B (zh) * 2013-08-08 2018-11-02 上海医药集团股份有限公司 氘代乙炔衍生物、其药物组合物及应用
PE20170774A1 (es) * 2014-08-19 2017-07-04 Shanghai Haihe Pharmaceutical Co Ltd Compuestos de indazol como inhibidores de cinasa fgfr, preparacion y uso de los mismos

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007087395A2 (en) * 2006-01-25 2007-08-02 Osi Pharmaceuticals, Inc. UNSATURATED mTOR INHIBITORS
CN103958512A (zh) * 2012-01-19 2014-07-30 大鹏药品工业株式会社 3,5-双取代炔基苯化合物及其盐
EP3023100A1 (en) * 2013-07-18 2016-05-25 Taiho Pharmaceutical Co., Ltd. Antitumor drug for intermittent administration of fgfr inhibitor
CN104341388A (zh) * 2013-10-16 2015-02-11 上海润诺生物科技有限公司 芳香族酰胺类衍生物、其制备方法及其在医药上的应用

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116096707A (zh) * 2020-06-05 2023-05-09 金耐特生物制药公司 成纤维细胞生长因子受体激酶的抑制剂
CN115043832A (zh) * 2021-03-08 2022-09-13 药雅科技(上海)有限公司 一种fgfr抑制剂炔代杂环类化合物及其制备方法和用途
CN115043832B (zh) * 2021-03-08 2023-08-22 药雅科技(上海)有限公司 一种fgfr抑制剂炔代杂环类化合物及其制备方法和用途

Also Published As

Publication number Publication date
CN107698593A (zh) 2018-02-16
US10752631B2 (en) 2020-08-25
CA3032921A1 (en) 2018-02-15
WO2018028438A1 (zh) 2018-02-15
EP3498706A1 (en) 2019-06-19
JP2019524883A (ja) 2019-09-05
JP6959663B2 (ja) 2021-11-02
US20190177333A1 (en) 2019-06-13
EP3498706A4 (en) 2020-02-26
CN109715626B (zh) 2022-04-26
KR20190035870A (ko) 2019-04-03

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