CN114206877A - 一种乌帕替尼的晶型及其制备方法和用途 - Google Patents

一种乌帕替尼的晶型及其制备方法和用途 Download PDF

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CN114206877A
CN114206877A CN202180004686.XA CN202180004686A CN114206877A CN 114206877 A CN114206877 A CN 114206877A CN 202180004686 A CN202180004686 A CN 202180004686A CN 114206877 A CN114206877 A CN 114206877A
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crystalline form
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crystal form
crystal
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CN114206877B (zh
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陈敏华
张婧
史佳明
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Crystal Pharmaceutical Suzhou Co Ltd
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    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • C07D487/12Heterocyclic 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
    • C07D487/14Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明公开了乌帕替尼的新晶型及其制备方法,含有该晶型的药物组合物,以及该晶型在制备JAK抑制剂药物和治疗类风湿性关节炎、克罗恩病、溃疡性结肠炎、异位性皮炎和银屑病关节炎药物中的用途。本发明提供的乌帕替尼晶型比现有技术具有一种或多种改进的特性,对未来该药物的优化和开发具有重要价值。
Figure DDA0003484802050000011

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。
CN202180004686.XA 2020-06-05 2021-05-21 一种乌帕替尼的晶型及其制备方法和用途 Active CN114206877B (zh)

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CN2020105065563 2020-06-05
CN202010506556 2020-06-05
CN2020105348505 2020-06-12
CN202010534850 2020-06-12
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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112770756A (zh) * 2018-09-29 2021-05-07 苏州科睿思制药有限公司 一种Upadacitinib的晶型及其制备方法和用途
CN114380837A (zh) * 2021-12-27 2022-04-22 上海邈金医药科技有限公司 一种具有Janus激酶抑制活性的化合物、包括该化合物的组合物及其应用
CN117447481A (zh) * 2023-12-23 2024-01-26 潍坊医学院 一种乌帕替尼-焦谷氨酸盐的无定形物及其制备方法与应用

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111909160B (zh) 2019-05-09 2024-05-28 苏州鹏旭医药科技有限公司 一种乌帕替尼盐类化合物及其制备方法
AU2021303629A1 (en) 2020-07-08 2023-03-09 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystal form of upadacitinib, preparation method therefor, and use thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108368121A (zh) * 2015-10-16 2018-08-03 艾伯维公司 制备(3S,4R)-3-乙基-4-(3H-咪唑并[1,2-a]吡咯并[2,3-e]吡嗪-8-基)-N-(2,2,2-三氟乙基)吡咯烷-1-甲酰胺及其固态形式的方法
WO2020063939A1 (zh) * 2018-09-29 2020-04-02 苏州科睿思制药有限公司 一种Upadacitinib的晶型及其制备方法和用途

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DK2506716T3 (en) * 2009-12-01 2017-09-04 Abbvie Inc HIS UNKNOWN TRICYCLIC RELATIONS
WO2018056269A1 (ja) * 2016-09-20 2018-03-29 参天製薬株式会社 Jak阻害剤を含有する点眼剤

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108368121A (zh) * 2015-10-16 2018-08-03 艾伯维公司 制备(3S,4R)-3-乙基-4-(3H-咪唑并[1,2-a]吡咯并[2,3-e]吡嗪-8-基)-N-(2,2,2-三氟乙基)吡咯烷-1-甲酰胺及其固态形式的方法
WO2020063939A1 (zh) * 2018-09-29 2020-04-02 苏州科睿思制药有限公司 一种Upadacitinib的晶型及其制备方法和用途

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112770756A (zh) * 2018-09-29 2021-05-07 苏州科睿思制药有限公司 一种Upadacitinib的晶型及其制备方法和用途
CN114380837A (zh) * 2021-12-27 2022-04-22 上海邈金医药科技有限公司 一种具有Janus激酶抑制活性的化合物、包括该化合物的组合物及其应用
CN117447481A (zh) * 2023-12-23 2024-01-26 潍坊医学院 一种乌帕替尼-焦谷氨酸盐的无定形物及其制备方法与应用

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