CN109563079A - 脱氢苯基阿夕斯丁类化合物的多晶型及其制备纯化方法和应用 - Google Patents

脱氢苯基阿夕斯丁类化合物的多晶型及其制备纯化方法和应用 Download PDF

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CN109563079A
CN109563079A CN201780049392.2A CN201780049392A CN109563079A CN 109563079 A CN109563079 A CN 109563079A CN 201780049392 A CN201780049392 A CN 201780049392A CN 109563079 A CN109563079 A CN 109563079A
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crystal form
tert
butyl
piperazine
imidazol
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CN109563079B (zh
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李文保
王世潇
丁忠鹏
侯英伟
管华诗
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Shenzhen Huahong Marine Biomedical Co ltd
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Qingdao Marine Biomedical Research Institute Co Ltd
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Priority claimed from CN201610665377.8A external-priority patent/CN107011331A/zh
Priority claimed from CN201610664196.3A external-priority patent/CN107778297B/zh
Priority claimed from CN201610664088.6A external-priority patent/CN107011322B/zh
Application filed by Qingdao Marine Biomedical Research Institute Co Ltd filed Critical Qingdao Marine Biomedical Research Institute Co Ltd
Priority to CN202111486744.5A priority Critical patent/CN114276332B/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

脱氢苯基阿夕斯丁类化合物的多晶型及其制备纯化方法和应用。其中(3Z,6Z)‑3‑苯亚甲基‑6‑[(5‑叔丁基‑1H‑咪唑‑4‑基)氘代亚甲基]哌嗪‑2,5‑二酮一水合物晶型和(3Z,6Z)‑3‑苯亚甲基‑6‑[(5‑叔丁基‑1H‑咪唑‑4‑基)亚甲基]哌嗪‑2,5‑二酮一水合物晶型为质量稳定的优势晶型，其制备纯化方法简单易操作，可有效的控制反式异构体杂质的产生，得到高纯度的产物。脱氢苯基阿夕斯丁类化合物的多种晶型在制备抗肿瘤的药物中具有一定的应用价值。

Description

PCT国内申请，说明书已公开。

Claims (28)

  1. PCT国内申请，权利要求书已公开。
CN201780049392.2A 2016-08-12 2017-07-24 脱氢苯基阿夕斯丁类化合物的多晶型及其制备纯化方法和应用 Active CN109563079B (zh)

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CN202111486744.5A CN114276332B (zh) 2016-08-12 2017-07-24 脱氢苯基阿夕斯丁类化合物的多晶型及其制备纯化方法和应用

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CN201610665377.8A CN107011331A (zh) 2016-08-12 2016-08-12 脱氢苯基阿夕斯丁类化合物的多晶型及其制备方法
CN201610664196.3A CN107778297B (zh) 2016-08-12 2016-08-12 氘代脱氢苯基阿夕斯丁类化合物的多晶型及其制备方法和应用
CN2016106653778 2016-08-12
CN2016106641963 2016-08-12
CN2016106640886 2016-08-12
CN201610664088.6A CN107011322B (zh) 2016-08-12 2016-08-12 一种脱氢苯基阿夕斯丁类化合物的制备纯化方法
PCT/CN2017/094066 WO2018028420A1 (zh) 2016-08-12 2017-07-24 脱氢苯基阿夕斯丁类化合物的多晶型及其制备纯化方法和应用

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CN202111486744.5A Active CN114276332B (zh) 2016-08-12 2017-07-24 脱氢苯基阿夕斯丁类化合物的多晶型及其制备纯化方法和应用

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WO2018028420A1 (zh) * 2016-08-12 2018-02-15 青岛海洋生物医药研究院股份有限公司 脱氢苯基阿夕斯丁类化合物的多晶型及其制备纯化方法和应用
WO2019028144A1 (en) 2017-08-03 2019-02-07 Teva Pharmaceuticals Usa, Inc. SALTS AND FORMS IN THE SOLID STATE OF PLINABULIN

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CN114276332B (zh) 2023-08-18
WO2018028420A1 (zh) 2018-02-15
US20190177302A1 (en) 2019-06-13
EP3498702A4 (en) 2020-06-03
US20210070738A1 (en) 2021-03-11
CN109563079B (zh) 2021-10-26
US10851086B2 (en) 2020-12-01
US11578057B2 (en) 2023-02-14
EP3498702B1 (en) 2022-05-25
CN114276332A (zh) 2022-04-05
EP4089085B1 (en) 2024-04-03
EP3498702A1 (en) 2019-06-19
US20210002259A1 (en) 2021-01-07
US11608325B2 (en) 2023-03-21
EP4089085A1 (en) 2022-11-16

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