CN110944982A - 奥扎莫德盐酸盐的晶型及其制备方法 - Google Patents

奥扎莫德盐酸盐的晶型及其制备方法 Download PDF

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Publication number
CN110944982A
CN110944982A CN201880047898.4A CN201880047898A CN110944982A CN 110944982 A CN110944982 A CN 110944982A CN 201880047898 A CN201880047898 A CN 201880047898A CN 110944982 A CN110944982 A CN 110944982A
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hydrochloride
preparation
degrees
crystal form
crystalline
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陈敏华
张炎锋
翟晓婷
鄢楷强
杨朝惠
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Receptos LLC
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Crystal Pharmaceutical Suzhou Co Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245Oxadiazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/061,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

本发明涉及奥扎莫德盐酸盐的晶型及其制备方法。本发明提供的奥扎莫德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。本发明提供的奥扎莫德盐酸盐的晶型在溶解度、熔点、稳定性、溶出度、生物有效性以及加工性能、提纯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,对于药物开发具有重要意义。
Figure DDA0002371847830000011

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。
CN201880047898.4A 2017-08-31 2018-08-23 奥扎莫德盐酸盐的晶型及其制备方法 Pending CN110944982A (zh)

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CN2017107686453 2017-08-31
CN201710768645 2017-08-31
PCT/CN2018/102034 WO2019042219A1 (zh) 2017-08-31 2018-08-23 奥扎莫德盐酸盐的晶型及其制备方法

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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
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 (1)

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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

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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
US20170165236A1 (en) 2013-11-01 2017-06-15 Celgene International Ii Sàrl Selective sphingosine 1 phosphate receptor modulators and combination therapy therewith
US20180016244A1 (en) 2015-04-06 2018-01-18 Auspex Pharmaceuticals, Inc. Deuterium-substituted oxadiazoles
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
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 (1)

* 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

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