CN112119062A - 化合物晶型、其制备方法、药物组合物以及应用 - Google Patents

化合物晶型、其制备方法、药物组合物以及应用 Download PDF

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CN112119062A
CN112119062A CN202080002626.XA CN202080002626A CN112119062A CN 112119062 A CN112119062 A CN 112119062A CN 202080002626 A CN202080002626 A CN 202080002626A CN 112119062 A CN112119062 A CN 112119062A
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degrees
crystal
compound
crystal form
cancer
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CN112119062B (zh
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孙效华
王龙
杨红振
胡怀忠
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Beijing Konruns Pharmaceutical Co Ltd
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Beijing Konruns Pharmaceutical 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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明涉及制药技术领域，提供了用于治疗蛋白激酶AXL和/或VEGFR2相关疾病的化合物6‑[[4‑[2‑氟‑4‑[[1‑[(4‑氟苯基)氨基甲酰基]环丙烷羰基]氨基]苯氧基]‑6‑甲氧基‑7‑喹啉基]氧基]己酸的三种晶型：晶型AB、晶型M和晶型F。本发明还提供了用于制备这三种晶型的方法及包含这三种晶型的药物组合物。本发明的晶型AB、晶型M和晶型F均具有良好的化学稳定性，并且本发明的三种晶型的制备方法简单易行，产物收率和纯度高，能够稳定且批量化生产，有利于推广和应用。本发明的晶型AB、晶型M、晶型F在高温、高湿、氧化条件下也较为稳定，有利于储存和运输，有利于工业化生产。此外，本发明的晶型AB、晶型M和晶型F具有较高的生物利用度，符合临床用药要求。

Description

PCT国内申请，说明书已公开。

Claims (10)

  1. PCT国内申请，权利要求书已公开。
CN202080002626.XA 2019-04-22 2020-04-20 化合物晶型、其制备方法、药物组合物以及应用 Active CN112119062B (zh)

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CN201910324939.6A CN111825609A (zh) 2019-04-22 2019-04-22 化合物晶型、其制备方法、药物组合物以及应用
CN2019103249396 2019-04-22
PCT/CN2020/085695 WO2020216188A1 (zh) 2019-04-22 2020-04-20 化合物晶型、其制备方法、药物组合物以及应用

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EP (1) EP3964499A4 (zh)
JP (1) JP2022524011A (zh)
KR (1) KR20210126629A (zh)
CN (2) CN111825609A (zh)
CA (1) CA3137209A1 (zh)
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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005030140A2 (en) * 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and methods of use
CN102408411A (zh) * 2011-09-19 2012-04-11 广州盈升生物科技有限公司 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
WO2018072614A1 (zh) * 2016-10-18 2018-04-26 北京康辰药业股份有限公司 一种喹啉基取代的羧酸化合物或其药学上可接受的盐、其药物组合物及应用

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106632253B (zh) * 2015-11-02 2019-03-22 广东东阳光药业有限公司 一种取代的喹啉化合物的晶型及其药物组合物和用途
WO2018196687A1 (zh) * 2017-04-25 2018-11-01 苏州科睿思制药有限公司 乐伐替尼甲磺酸盐的新晶型及其制备方法
CN109384799B (zh) * 2018-11-12 2020-07-14 深圳海王医药科技研究院有限公司 一种多靶点激酶抑制剂化合物的晶型a及制备方法和含有其的药物组合物

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005030140A2 (en) * 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and methods of use
CN102408411A (zh) * 2011-09-19 2012-04-11 广州盈升生物科技有限公司 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
WO2018072614A1 (zh) * 2016-10-18 2018-04-26 北京康辰药业股份有限公司 一种喹啉基取代的羧酸化合物或其药学上可接受的盐、其药物组合物及应用

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CA3137209A1 (en) 2020-10-29
JP2022524011A (ja) 2022-04-27
WO2020216188A1 (zh) 2020-10-29
EP3964499A4 (en) 2022-12-28
KR20210126629A (ko) 2021-10-20
CN111825609A (zh) 2020-10-27
US20220259152A1 (en) 2022-08-18
SG11202111558VA (en) 2021-11-29
EP3964499A1 (en) 2022-03-09
CN112119062B (zh) 2023-09-05

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