CN110799512A - 巴瑞克替尼的晶型及其制备方法 - Google Patents

巴瑞克替尼的晶型及其制备方法 Download PDF

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CN110799512A
CN110799512A CN201880031307.4A CN201880031307A CN110799512A CN 110799512 A CN110799512 A CN 110799512A CN 201880031307 A CN201880031307 A CN 201880031307A CN 110799512 A CN110799512 A CN 110799512A
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crystal form
preparation
ray powder
crystal
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陈敏华
张炎锋
刘启月
张晓宇
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Lilai Co.
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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
    • C07D487/02—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 two hetero rings
    • C07D487/04—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明公开了巴瑞克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激酶抑制剂和治疗类风湿性关节炎药物制剂中的用途。本发明提供的巴瑞克替尼新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 DDA0002269009370000011

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。
CN201880031307.4A 2017-06-22 2018-05-23 巴瑞克替尼的晶型及其制备方法 Pending CN110799512A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2017104791119 2017-06-22
CN201710479111 2017-06-22
PCT/CN2018/088068 WO2018233437A1 (zh) 2017-06-22 2018-05-23 巴瑞克替尼的晶型及其制备方法

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CN110799512A true CN110799512A (zh) 2020-02-14

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CN (1) CN110799512A (zh)
WO (1) WO2018233437A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115160221A (zh) * 2022-07-26 2022-10-11 上海歆贻医药科技有限公司 德立替尼晶型化合物和用途

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20220135566A1 (en) 2019-02-05 2022-05-05 Teva Pharmaceuticals International Gmbh Crystalline solid forms of baricitinib
EP3771715A1 (en) * 2019-08-02 2021-02-03 Zaklady Farmaceutyczne "Polpharma" S.A. Crystalline forms of baricitinib
CN115856141B (zh) * 2022-12-19 2024-07-23 上海博悦生物科技有限公司 Hplc分离测定替尼类关键中间体及其相关杂质的方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102026999A (zh) * 2008-03-11 2011-04-20 因塞特公司 作为jak抑制剂的氮杂环丁烷和环丁烷衍生物
WO2015166434A1 (en) * 2014-05-01 2015-11-05 Sun Pharmaceutical Industries Limited Crystalline form of baricitinib
CN105693731A (zh) * 2016-01-26 2016-06-22 上海宣创生物科技有限公司 巴瑞克替尼a晶型及其制备方法
CN105924444A (zh) * 2015-03-11 2016-09-07 苏州晶云药物科技有限公司 Jak抑制剂的晶型及其制备方法
CN106946917A (zh) * 2017-03-20 2017-07-14 杭州科巢生物科技有限公司 一种jak抑制剂巴瑞替尼及其中间体的新合成方法
CN107176955A (zh) * 2017-03-24 2017-09-19 南京优科制药有限公司 一种巴瑞替尼的制备方法

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102026999A (zh) * 2008-03-11 2011-04-20 因塞特公司 作为jak抑制剂的氮杂环丁烷和环丁烷衍生物
WO2015166434A1 (en) * 2014-05-01 2015-11-05 Sun Pharmaceutical Industries Limited Crystalline form of baricitinib
CN105924444A (zh) * 2015-03-11 2016-09-07 苏州晶云药物科技有限公司 Jak抑制剂的晶型及其制备方法
CN105693731A (zh) * 2016-01-26 2016-06-22 上海宣创生物科技有限公司 巴瑞克替尼a晶型及其制备方法
CN106946917A (zh) * 2017-03-20 2017-07-14 杭州科巢生物科技有限公司 一种jak抑制剂巴瑞替尼及其中间体的新合成方法
CN107176955A (zh) * 2017-03-24 2017-09-19 南京优科制药有限公司 一种巴瑞替尼的制备方法

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115160221A (zh) * 2022-07-26 2022-10-11 上海歆贻医药科技有限公司 德立替尼晶型化合物和用途

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