CN112888692A - 一种Upadacitinib的晶型及其制备方法和用途 - Google Patents

一种Upadacitinib的晶型及其制备方法和用途 Download PDF

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CN112888692A
CN112888692A CN202080005328.6A CN202080005328A CN112888692A CN 112888692 A CN112888692 A CN 112888692A CN 202080005328 A CN202080005328 A CN 202080005328A CN 112888692 A CN112888692 A CN 112888692A
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crystal form
degrees
crystalline form
preparation
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陈敏华
史佳明
张婧
荆慧泽
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Crystal Pharmaceutical Suzhou Co Ltd
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    • 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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Engineering & Computer Science (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
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  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明涉及Upadacitinib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抑制剂和治疗类风湿性关节炎药物中的用途。本发明提供的Upadacitinib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 DDA0002990852500000011

Description

PCT国内申请，说明书已公开。

Claims (9)

  1. PCT国内申请，权利要求书已公开。
CN202080005328.6A 2019-03-01 2020-02-29 一种Upadacitinib的晶型及其制备方法和用途 Pending CN112888692A (zh)

Applications Claiming Priority (5)

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CN2019101569559 2019-03-01
CN201910156955 2019-03-01
CN201910358029 2019-04-30
CN201910358029X 2019-04-30
PCT/CN2020/077327 WO2020177645A1 (zh) 2019-03-01 2020-02-29 一种Upadacitinib的晶型及其制备方法和用途

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Cited By (1)

* 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

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023532787A (ja) 2020-07-08 2023-07-31 ▲蘇▼州科睿思制▲葯▼有限公司 結晶形態のウパダシチニブ（ｕｐａｄａｃｉｔｉｎｉｂ）、その調製方法及びその使用
WO2022217257A1 (en) * 2021-04-07 2022-10-13 Abbvie Inc. Cocrystals of upadacitinib
EP4215196A1 (en) * 2022-01-24 2023-07-26 Abivax Combination of 8-chloro-n-(4-(trifluoromethoxy)phenyl)quinolin-2-amine and its derivatives with a jak inhibitor

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015061665A1 (en) * 2013-10-24 2015-04-30 Abbvie Inc. Jak1 selective inhibitor and uses thereof
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
WO2019016745A1 (en) * 2017-07-19 2019-01-24 Dr. Reddy's Laboratories Limited ALTERNATIVE METHODS FOR THE PREPARATION OF PYRROLIDINE DERIVATIVES
CN109369659A (zh) * 2018-12-06 2019-02-22 浙江师范大学 一种jak抑制剂的合成方法

Family Cites Families (1)

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KR20170118230A (ko) * 2009-12-01 2017-10-24 애브비 인코포레이티드 신규한 트리사이클릭 화합물

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015061665A1 (en) * 2013-10-24 2015-04-30 Abbvie Inc. Jak1 selective inhibitor and uses thereof
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
WO2019016745A1 (en) * 2017-07-19 2019-01-24 Dr. Reddy's Laboratories Limited ALTERNATIVE METHODS FOR THE PREPARATION OF PYRROLIDINE DERIVATIVES
CN109369659A (zh) * 2018-12-06 2019-02-22 浙江师范大学 一种jak抑制剂的合成方法

Cited By (1)

* 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

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Application publication date: 20210601