CN109219597A - 奥扎莫德的晶型、其盐酸盐的晶型及其制备方法 - Google Patents

奥扎莫德的晶型、其盐酸盐的晶型及其制备方法 Download PDF

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Publication number
CN109219597A
CN109219597A CN201780029499.0A CN201780029499A CN109219597A CN 109219597 A CN109219597 A CN 109219597A CN 201780029499 A CN201780029499 A CN 201780029499A CN 109219597 A CN109219597 A CN 109219597A
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China
Prior art keywords
crystal form
zhamode
hydrochloride
ray powder
powder diffraction
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CN201780029499.0A
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English (en)
Inventor
陈敏华
张炎锋
翟晓婷
鄢楷强
杨朝惠
张晓宇
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Riseptos Co.,Ltd.
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Crystal Pharmaceutical Suzhou Co Ltd
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Priority to CN202210226424.4A priority Critical patent/CN114957157A/zh
Publication of CN109219597A publication Critical patent/CN109219597A/zh
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • 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
    • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

公开了奥扎莫德的晶型、其盐酸盐的晶型及其制备方法，所述奥扎莫德的晶型及其盐酸盐的晶型可用于治疗自身免疫疾病，特别是多发性硬化症和溃疡性结肠炎，在溶解度，熔点，稳定性、溶出度、生物有效性以及加工性能等方面中的至少一方面上存在优势，为含奥扎莫德的药物制剂的制备提供了新的更好的选择，对于药物开发具有非常重要的价值。

Description

PCT国内申请，说明书已公开。

Claims (36)

  1. PCT国内申请，权利要求书已公开。
CN201780029499.0A 2016-06-14 2017-06-14 奥扎莫德的晶型、其盐酸盐的晶型及其制备方法 Pending CN109219597A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202210226424.4A CN114957157A (zh) 2016-06-14 2017-06-14 奥扎莫德盐酸盐的晶型及其制备方法

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2016104161798 2016-06-14
CN201610416179 2016-06-14
CN201610493910 2016-06-29
CN2016104939107 2016-06-29
PCT/CN2017/088314 WO2017215617A1 (zh) 2016-06-14 2017-06-14 奥扎莫德的晶型、其盐酸盐的晶型及其制备方法

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US (2) US11111223B2 (zh)
EP (1) EP3470400A1 (zh)
CN (2) CN114957157A (zh)
WO (1) WO2017215617A1 (zh)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107840830A (zh) * 2017-09-20 2018-03-27 广东东阳光药业有限公司 盐酸奥扎莫德无水晶型i
CN109280035A (zh) * 2017-07-19 2019-01-29 广东东阳光药业有限公司 奥扎莫德的多晶型及其制备方法

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11111223B2 (en) 2016-06-14 2021-09-07 Receptos Llc Crystalline forms of ozanimod and ozanimod hydrochloride, and processes for preparation thereof
WO2018033149A1 (zh) 2016-08-19 2018-02-22 苏州科睿思制药有限公司 奥扎莫德的晶型及其制备方法
CN109640982A (zh) 2016-09-14 2019-04-16 苏州科睿思制药有限公司 奥扎莫德盐酸盐的晶型及其制备方法
EP3630738B1 (en) * 2017-05-22 2023-07-19 Egis Gyógyszergyár Zrt. Process for the production of ozanimod
US11117876B2 (en) 2017-08-31 2021-09-14 Receptos Llc Crystalline form of ozanimod hydrochloride, and processes for preparation thereof
WO2019094409A1 (en) 2017-11-07 2019-05-16 Teva Pharmaceuticals International Gmbh Salts and solid state forms of ozanimod
WO2020152718A1 (en) * 2019-01-25 2020-07-30 Mylan Laboratories Limited Polymorphic forms 5-[3-[(1s)-2,3-dihydro-1-[(2-hydroxyethyl) amino]-1h-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-methylethoxy)benzonitrile
MX2022000651A (es) 2019-07-16 2022-03-11 Synthon Bv Proceso mejorado para preparar ozanimod.
WO2021197852A1 (en) * 2020-04-02 2021-10-07 Synthon B.V. Crystalline form of ozanimod hydrochloride
WO2023152767A1 (en) 2022-02-11 2023-08-17 Mylan Laboratories Limited Polymorphic forms of ozanimod hydrochloride

Citations (3)

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CN102762100A (zh) * 2009-11-13 2012-10-31 瑞塞普托斯公司 选择性的1-磷酸鞘氨醇受体调节剂及手性合成方法
WO2015066515A1 (en) * 2013-11-01 2015-05-07 Receptos, Inc. Selective sphingosine 1 phosphate receptor modulators and combination therapy therewith
WO2016164180A1 (en) * 2015-04-06 2016-10-13 Auspex Pharmaceuticals, Inc. Deuterium-substituted oxadiazoles

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KR101582910B1 (ko) 2008-05-14 2016-01-08 더 스크립스 리서치 인스티튜트 스핑고신 포스페이트 수용체의 신규한 모듈레이터
EA021672B1 (ru) 2008-05-14 2015-08-31 Дзе Скриппс Рисёч Инститьют Модуляторы рецепторов сфингозин-1-фосфата и их применение
US11111223B2 (en) 2016-06-14 2021-09-07 Receptos Llc Crystalline forms of ozanimod and ozanimod hydrochloride, and processes for preparation thereof
WO2018033149A1 (zh) 2016-08-19 2018-02-22 苏州科睿思制药有限公司 奥扎莫德的晶型及其制备方法
WO2018049632A1 (zh) 2016-09-14 2018-03-22 杭州领业医药科技有限公司 奥扎莫德的晶型、其制备方法及药物组合物
CN109640982A (zh) 2016-09-14 2019-04-16 苏州科睿思制药有限公司 奥扎莫德盐酸盐的晶型及其制备方法
CN110612292A (zh) * 2017-04-07 2019-12-24 杭州领业医药科技有限公司 奥扎莫德加成盐晶型、制备方法及药物组合物和用途
US11117876B2 (en) 2017-08-31 2021-09-14 Receptos Llc Crystalline form of ozanimod hydrochloride, and processes for preparation thereof
CN107840830A (zh) 2017-09-20 2018-03-27 广东东阳光药业有限公司 盐酸奥扎莫德无水晶型i

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102762100A (zh) * 2009-11-13 2012-10-31 瑞塞普托斯公司 选择性的1-磷酸鞘氨醇受体调节剂及手性合成方法
WO2015066515A1 (en) * 2013-11-01 2015-05-07 Receptos, Inc. Selective sphingosine 1 phosphate receptor modulators and combination therapy therewith
WO2016164180A1 (en) * 2015-04-06 2016-10-13 Auspex Pharmaceuticals, Inc. Deuterium-substituted oxadiazoles

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109280035A (zh) * 2017-07-19 2019-01-29 广东东阳光药业有限公司 奥扎莫德的多晶型及其制备方法
CN109280035B (zh) * 2017-07-19 2023-06-09 广东东阳光药业有限公司 奥扎莫德的多晶型及其制备方法
CN107840830A (zh) * 2017-09-20 2018-03-27 广东东阳光药业有限公司 盐酸奥扎莫德无水晶型i

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Publication number Publication date
US11680050B2 (en) 2023-06-20
WO2017215617A1 (zh) 2017-12-21
EP3470400A4 (en) 2019-04-17
CN114957157A (zh) 2022-08-30
US20190337908A1 (en) 2019-11-07
US11111223B2 (en) 2021-09-07
EP3470400A1 (en) 2019-04-17
US20200157065A1 (en) 2020-05-21

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Effective date of registration: 20200904

Address after: California, USA

Applicant after: Riseptos Co.,Ltd.

Address before: 215123 Biological Park B4301, No. 218 Xing Hu Street, Suzhou Industrial Park, Jiangsu

Applicant before: CRYSTAL PHARMACEUTICAL (SUZHOU) Co.,Ltd.

CI02 Correction of invention patent application
CI02 Correction of invention patent application

Correction item: Applicant|Address

Correct: RECEPTOS, Inc.|California, USA

False: RECEPTOS, Inc.|California, USA

Number: 39-02

Volume: 36

WD01 Invention patent application deemed withdrawn after publication
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20190115