CN111902417A - 一种二芳基巨环化合物、药物组合物以及其用途 - Google Patents

一种二芳基巨环化合物、药物组合物以及其用途 Download PDF

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CN111902417A
CN111902417A CN201980020599.6A CN201980020599A CN111902417A CN 111902417 A CN111902417 A CN 111902417A CN 201980020599 A CN201980020599 A CN 201980020599A CN 111902417 A CN111902417 A CN 111902417A
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formula
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CN111902417B (zh
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祝力
吴伟
杨艳青
胡伟
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Beijing Puqi Medicine Technology Co ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16—Peri-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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D515/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D515/16—Peri-condensed systems

Abstract

本发明提供了一种如式(1)所示的化合物或其药学上可接受的盐、溶剂化物、活性代谢物、多晶型物、同位素标记物、异构体或前药。本发明还提供了包含其的药物组合物以及所述化合物、药物组合物在制备用于治疗酪氨酸激酶介导的疾病的药物中的用途。本发明提供的化合物及其药物组合物具有显著的酪氨酸激酶抑制活性，能克服肿瘤耐药，能够突破血脑屏障，还具有优异的药代动力学性质以及极佳的口服生物利用度，可以以较小的剂量施用，从而可降低患者的治疗成本及可能的毒副作用，因而非常具备应用潜力。

Description

PCT国内申请，说明书已公开。

Claims (13)

  1. PCT国内申请，权利要求书已公开。
CN201980020599.6A 2018-04-25 2019-04-22 一种二芳基巨环化合物、药物组合物以及其用途 Active CN111902417B (zh)

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CN2018103778111 2018-04-25
CN201810377811 2018-04-25
PCT/CN2019/083644 WO2019206069A1 (zh) 2018-04-25 2019-04-22 一种二芳基巨环化合物、药物组合物以及其用途

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WO2022171139A1 (zh) * 2021-02-10 2022-08-18 北京国鸿生物医药科技有限公司 一种巨环化合物、药物组合物以及其用途

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JP7374532B2 (ja) * 2019-11-18 2023-11-07 クワンチョウ ジョーヨー ファーマテック カンパニー，リミティド 選択性の高いｒｏｓ１阻害剤としての化合物、及びその使用
CN112824417A (zh) * 2019-11-21 2021-05-21 上海天慈国际药业有限公司 一种劳拉替尼的制备方法
CN113004305B (zh) * 2019-12-19 2024-04-09 赛诺哈勃药业（成都）有限公司 大环化合物及其制备方法和用途
CN113121568A (zh) * 2019-12-31 2021-07-16 成都倍特药业股份有限公司 一种大环结构化合物的盐及其制备方法
EP4163283A1 (en) * 2020-06-04 2023-04-12 Scinnohub Pharmaceutical Co., Ltd Compound having macrocyclic structure and use thereof

Citations (2)

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CN102971322A (zh) * 2010-05-20 2013-03-13 阵列生物制药公司 作为trk激酶抑制剂的大环化合物
CN106170289A (zh) * 2014-01-24 2016-11-30 Tp生物医药公司 作为蛋白质激酶的调节剂的二芳基巨环

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CA2738026C (en) 2008-09-22 2017-01-24 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
DK3106463T6 (da) 2008-10-22 2020-02-24 Array Biopharma Inc Pyrazolo[1,5-]pyrimidinforbindelse som trk-kinasehæmmer
JP2021519297A (ja) 2018-03-28 2021-08-10 フォチョン・ファーマシューティカルズ・リミテッドＦｏｃｈｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｌｔｄ． Ｔｒｋキナーゼ阻害剤としての大環状化合物

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102971322A (zh) * 2010-05-20 2013-03-13 阵列生物制药公司 作为trk激酶抑制剂的大环化合物
CN106170289A (zh) * 2014-01-24 2016-11-30 Tp生物医药公司 作为蛋白质激酶的调节剂的二芳基巨环

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022171139A1 (zh) * 2021-02-10 2022-08-18 北京国鸿生物医药科技有限公司 一种巨环化合物、药物组合物以及其用途

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US20220162218A1 (en) 2022-05-26
EP3786167A1 (en) 2021-03-03
CN111902417B (zh) 2023-07-28
JP7128345B2 (ja) 2022-08-30
JP2021519828A (ja) 2021-08-12
EP3786167A4 (en) 2021-06-09
WO2019206069A1 (zh) 2019-10-31

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