CN109071531A - 用于治疗或预防jak相关疾病药物的盐酸盐晶型及其制备方法 - Google Patents

用于治疗或预防jak相关疾病药物的盐酸盐晶型及其制备方法 Download PDF

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Publication number
CN109071531A
CN109071531A CN201780013652.0A CN201780013652A CN109071531A CN 109071531 A CN109071531 A CN 109071531A CN 201780013652 A CN201780013652 A CN 201780013652A CN 109071531 A CN109071531 A CN 109071531A
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China
Prior art keywords
filgotinib
crystal form
hydrochloride form
preparation
filgotinib hydrochloride
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Pending
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CN201780013652.0A
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English (en)
Inventor
陈敏华
张炎锋
刘凯
张晓宇
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Crystal Pharmatech Co Ltd
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Crystal Pharmatech Co Ltd
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Publication of CN109071531A publication Critical patent/CN109071531A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

用于治疗或预防JAK相关疾病的药物(Filgotinib)盐酸盐的晶型、其制备方法、药物组合物、制剂以及它们在预防和/或治疗与JAK家族激酶相关疾病中的用途被公开。相对于已知晶型，所述新晶型具有在低水活度条件下更加稳定、制备工艺简单和/或溶解度更高等制剂学上更有利的性质。

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。
CN201780013652.0A 2016-03-21 2017-03-21 用于治疗或预防jak相关疾病药物的盐酸盐晶型及其制备方法 Pending CN109071531A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2016101602746 2016-03-21
CN201610160274 2016-03-21
PCT/CN2017/077492 WO2017162139A1 (zh) 2016-03-21 2017-03-21 用于治疗或预防jak相关疾病药物的盐酸盐晶型及其制备方法

Publications (1)

Publication Number Publication Date
CN109071531A true CN109071531A (zh) 2018-12-21

Family

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Family Applications (1)

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CN201780013652.0A Pending CN109071531A (zh) 2016-03-21 2017-03-21 用于治疗或预防jak相关疾病药物的盐酸盐晶型及其制备方法

Country Status (10)

Country Link
US (1) US20190100519A1 (zh)
EP (1) EP3434675A4 (zh)
JP (1) JP2019509306A (zh)
KR (1) KR20180120273A (zh)
CN (1) CN109071531A (zh)
AU (1) AU2017239301A1 (zh)
CA (1) CA3018610A1 (zh)
IL (1) IL261862A (zh)
MX (1) MX2018011422A (zh)
WO (1) WO2017162139A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020177705A1 (zh) * 2019-03-05 2020-09-10 苏州科睿思制药有限公司 Filgotinib的马来酸盐晶型CSI及其制备方法和用途

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10815227B2 (en) 2018-08-27 2020-10-27 Cadila Healthcare Limited Processes for the preparation of filgotinib
CN114042073A (zh) * 2021-11-01 2022-02-15 浙江大学 非洛替尼在抑制胰腺癌细胞和肿瘤组织增殖中的应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104262337A (zh) * 2009-06-26 2015-01-07 加拉帕戈斯股份有限公司 作为jak抑制剂的5-苯基-[1,2,4]三唑并[1,5-a]吡啶-2-甲酰胺化合物
WO2015117980A1 (en) * 2014-02-07 2015-08-13 Galapagos Nv Pharmaceutical compositions for the treatment of inflammatory disorders
WO2015117981A1 (en) * 2014-02-07 2015-08-13 Galapagos Nv Novel salts and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6048993B2 (ja) 2013-07-24 2016-12-21 三菱電機株式会社 界磁巻線方式回転電機の診断装置および界磁巻線方式回転電機の診断方法
WO2017012773A1 (en) * 2015-07-23 2017-01-26 Ratiopharm Gmbh Solid forms of filgotinib free base
CN105669669A (zh) * 2016-03-04 2016-06-15 上海宣创生物科技有限公司 一种环丙烷甲酰胺衍生物的a晶型、b晶型、d晶型、g晶型和m晶型及其制备方法

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104262337A (zh) * 2009-06-26 2015-01-07 加拉帕戈斯股份有限公司 作为jak抑制剂的5-苯基-[1,2,4]三唑并[1,5-a]吡啶-2-甲酰胺化合物
WO2015117980A1 (en) * 2014-02-07 2015-08-13 Galapagos Nv Pharmaceutical compositions for the treatment of inflammatory disorders
WO2015117981A1 (en) * 2014-02-07 2015-08-13 Galapagos Nv Novel salts and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020177705A1 (zh) * 2019-03-05 2020-09-10 苏州科睿思制药有限公司 Filgotinib的马来酸盐晶型CSI及其制备方法和用途

Also Published As

Publication number Publication date
EP3434675A4 (en) 2019-03-06
KR20180120273A (ko) 2018-11-05
CA3018610A1 (en) 2017-09-28
US20190100519A1 (en) 2019-04-04
IL261862A (en) 2018-10-31
EP3434675A1 (en) 2019-01-30
AU2017239301A1 (en) 2018-11-08
WO2017162139A1 (zh) 2017-09-28
JP2019509306A (ja) 2019-04-04
MX2018011422A (es) 2019-07-08

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