CN109153676A - Nbi-98854的晶型及其制备方法和用途 - Google Patents

Nbi-98854的晶型及其制备方法和用途 Download PDF

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Publication number
CN109153676A
CN109153676A CN201780029517.5A CN201780029517A CN109153676A CN 109153676 A CN109153676 A CN 109153676A CN 201780029517 A CN201780029517 A CN 201780029517A CN 109153676 A CN109153676 A CN 109153676A
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crystal form
nbi
solid
ray powder
powder diffraction
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CN201780029517.5A
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CN109153676B (zh
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陈敏华
张炎锋
邹坡
刘凯
王金秋
张晓宇
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Crystal Pharmaceutical Suzhou Co Ltd
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Crystal Pharmaceutical Suzhou Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/03—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/04—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine
    • C07D455/06—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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)
  • Neurology (AREA)
  • Psychology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

一种NBI‑98854(结构如式I所示)的晶型及其制备方法和用途。所述的NBI‑98854晶型分别命名为晶型CS1、晶型CS2，可用于制备治疗迟发性运动障碍的药物。所述的NBI‑98854晶型的溶解度、引湿性符合药用要求，稳定性好，能稳定储存，避免药物在开发过程中发生转晶，从而避免药物溶解度、溶出率、生物利用度以及药效的改变。为含NBI‑98854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意义。

Description

PCT国内申请，说明书已公开。

Claims (12)

  1. PCT国内申请，权利要求书已公开。
CN201780029517.5A 2016-06-29 2017-06-29 Nbi-98854的晶型及其制备方法和用途 Active CN109153676B (zh)

Applications Claiming Priority (3)

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CN201610488976 2016-06-29
CN2016104889767 2016-06-29
PCT/CN2017/090926 WO2018001335A1 (zh) 2016-06-29 2017-06-29 Nbi-98854的晶型及其制备方法和用途

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CN109153676A true CN109153676A (zh) 2019-01-04
CN109153676B CN109153676B (zh) 2021-08-10

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US (1) US10442800B2 (zh)
EP (1) EP3473623B1 (zh)
CN (1) CN109153676B (zh)
ES (1) ES2811048T3 (zh)
WO (1) WO2018001335A1 (zh)

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US10689380B1 (en) 2019-07-30 2020-06-23 Farmhispania S.A. Crystalline forms of valbenazine ditosylate

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101553487A (zh) * 2006-11-08 2009-10-07 纽罗克里生物科学有限公司 取代的3-异丁基-9,10-二甲氧基-1,3,4,6,7,11b-六氢-2H-吡啶并[2,1-a]异喹啉-2-醇化合物和与其相关的方法
WO2015120110A2 (en) * 2014-02-07 2015-08-13 Auspex Pharmaceuticals, Inc. Novel pharmaceutical formulations
WO2015171802A1 (en) * 2014-05-06 2015-11-12 Neurocrine Biosciences, Inc. Vmat2 inhibitors for the treatment of hyperkinetic movement disorders
WO2018067945A1 (en) * 2016-10-06 2018-04-12 Assia Chemical Industries Ltd. Solid state forms of valbenazine
WO2018130345A1 (en) * 2017-01-10 2018-07-19 Sandoz Ag Crystalline valbenazine free base

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3102239A1 (en) * 2014-02-07 2016-12-14 Neurocrine Biosciences, Inc. Pharmaceutical compositions comprising an antipsychotic drug and a vmat2 inhibitor and uses thereof
AU2018242134B2 (en) * 2017-04-01 2023-09-28 Adeptio Pharmaceuticals Limited (+)-alpha-dihydrotetrabenazine for use in the treatment a movement disorder

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101553487A (zh) * 2006-11-08 2009-10-07 纽罗克里生物科学有限公司 取代的3-异丁基-9,10-二甲氧基-1,3,4,6,7,11b-六氢-2H-吡啶并[2,1-a]异喹啉-2-醇化合物和与其相关的方法
WO2015120110A2 (en) * 2014-02-07 2015-08-13 Auspex Pharmaceuticals, Inc. Novel pharmaceutical formulations
WO2015171802A1 (en) * 2014-05-06 2015-11-12 Neurocrine Biosciences, Inc. Vmat2 inhibitors for the treatment of hyperkinetic movement disorders
WO2018067945A1 (en) * 2016-10-06 2018-04-12 Assia Chemical Industries Ltd. Solid state forms of valbenazine
WO2018130345A1 (en) * 2017-01-10 2018-07-19 Sandoz Ag Crystalline valbenazine free base

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ANON: ""A crystalline form of L-valine (2R,3R,11bR)-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo[a]quinolizin-2-yl ester"", 《IP.COM JOURNAL》 *
ANON: ""Novel preparation of crystalline forms L1 and L2 of L-valine, (2R,3R,11bR)-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo[a]quinolizin-2-yl ester"", 《IP.COM JOURNAL》 *

Also Published As

Publication number Publication date
ES2811048T3 (es) 2021-03-10
US10442800B2 (en) 2019-10-15
EP3473623B1 (en) 2020-07-15
EP3473623A4 (en) 2019-06-12
CN109153676B (zh) 2021-08-10
US20190218209A1 (en) 2019-07-18
WO2018001335A1 (zh) 2018-01-04
EP3473623A1 (en) 2019-04-24

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