JP6014656B2 - 化合物の多形体 - Google Patents

化合物の多形体 Download PDF

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Publication number
JP6014656B2
JP6014656B2 JP2014510872A JP2014510872A JP6014656B2 JP 6014656 B2 JP6014656 B2 JP 6014656B2 JP 2014510872 A JP2014510872 A JP 2014510872A JP 2014510872 A JP2014510872 A JP 2014510872A JP 6014656 B2 JP6014656 B2 JP 6014656B2
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Prior art keywords
asenapine maleate
monoclinic
less
asenapine
micronized
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Japanese (ja)
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JP2014513712A (ja
JP2014513712A5 (enExample
Inventor
ベルトラン、アグスティ
テララダス、ヨセプ
Original Assignee
ラビラトリオス レスビ エス エレ
ラビラトリオス レスビ エス エレ
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/145—Maleic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrane Compounds (AREA)
JP2014510872A 2011-05-18 2012-05-18 化合物の多形体 Active JP6014656B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161487495P 2011-05-18 2011-05-18
US61/487,495 2011-05-18
PCT/GB2012/000450 WO2012156677A1 (en) 2011-05-18 2012-05-18 A stable micronised monoclinic form of asenapine maleate and its synthesis

Publications (3)

Publication Number Publication Date
JP2014513712A JP2014513712A (ja) 2014-06-05
JP2014513712A5 JP2014513712A5 (enExample) 2015-07-02
JP6014656B2 true JP6014656B2 (ja) 2016-10-25

Family

ID=46168537

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2014510872A Active JP6014656B2 (ja) 2011-05-18 2012-05-18 化合物の多形体

Country Status (5)

Country Link
US (1) US9505771B2 (enExample)
EP (1) EP2709616B1 (enExample)
JP (1) JP6014656B2 (enExample)
ES (1) ES2665843T3 (enExample)
WO (1) WO2012156677A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2582704A4 (en) * 2010-06-18 2014-04-02 Reddys Lab Ltd Dr Asenapine MALEATE
US10085971B2 (en) * 2016-08-22 2018-10-02 Navinta Iii Inc Pharmaceutical solution of asenapine for sublingual or buccal use
CN110087641B (zh) 2016-12-20 2024-03-12 罗曼治疗系统股份公司 含有阿塞那平和聚硅氧烷或聚异丁烯的透皮治疗系统
PL3338768T3 (pl) 2016-12-20 2020-05-18 Lts Lohmann Therapie-Systeme Ag Transdermalny system terapeutyczny zawierający asenapinę
JP2020525545A (ja) 2017-06-26 2020-08-27 エルテーエス ローマン テラピー−ジステーメ アーゲー アセナピンおよびシリコーンアクリルハイブリッドポリマーを含有する経皮治療システム
BR112020026099A2 (pt) 2018-06-20 2021-03-23 Lts Lohmann Therapie-Systeme Ag sistema terapêutico transdérmico que contém asenapina
CN118806732A (zh) 2018-06-20 2024-10-22 罗曼治疗系统股份公司 含有阿塞那平的透皮治疗系统
US20250032451A1 (en) * 2021-11-24 2025-01-30 Oakwood Laboratories, Llc Microsphere formulations comprising asenapine and methods for making and using the same
WO2026095022A1 (ja) * 2024-11-01 2026-05-07 大鵬薬品工業株式会社 キノリン置換化合物の結晶

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL7605526A (nl) 1976-05-24 1977-11-28 Akzo Nv Nieuwe tetracyclische derivaten.
ATE167057T1 (de) 1994-03-02 1998-06-15 Akzo Nobel Nv Sublinguales oder bukkales arzneimittel
ES2290095T3 (es) * 2000-12-27 2008-02-16 Ares Trading S.A. Microparticulas lipidicas por micronizacion criogenica.
US7872147B2 (en) 2005-04-07 2011-01-18 N. V. Organon Intermediate compounds for the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole
KR101422843B1 (ko) 2005-04-07 2014-07-24 머크 샤프 앤 도메 비.브이. 아세나핀 말레에이트의 결정형
US7741358B2 (en) * 2005-04-14 2010-06-22 N.V. Organon Crystal form of asenapine maleate
US7750167B2 (en) 2006-07-05 2010-07-06 N.V. Organon Process for the preparation of asenapine and intermediate products used in said process
WO2008148515A1 (en) * 2007-06-05 2008-12-11 Synthon B.V. Intranasal administration of asenapine and pharmaceutical compositions therefor
EP2582704A4 (en) * 2010-06-18 2014-04-02 Reddys Lab Ltd Dr Asenapine MALEATE
EP2598496B1 (en) * 2010-07-29 2014-03-19 Laboratorios Lesvi, S.L. Novel process for the preparation of asenapine
WO2012038975A2 (en) 2010-09-22 2012-03-29 Msn Laboratories Limited Process for the preparation of (3ars,12brs)-5-chloro-2-methyl-2,3,3a12b-tetrahydro-1hdibenzo[2,3:6,7] oxepino [4,5-c]pyrrole maleate and it's pharmaceutical composition thereof
WO2012066565A2 (en) * 2010-11-16 2012-05-24 Cadila Healthcare Limited Asenapine maleate amorphous and crystalline form and process for preparation thereof
EP2468750A1 (en) * 2010-12-13 2012-06-27 Chemo Ibérica, S.A. Polymorphic forms of asenapine maleate and processes for their preparation
ITMI20110734A1 (it) * 2011-05-02 2012-11-03 Olon Spa Sali cristallini di asenapina
WO2012156676A1 (en) * 2011-05-18 2012-11-22 Laboratorios Lesvi S.L. Monoclinic crystalline form of asenapine maleate with a specific particle size distribution

Also Published As

Publication number Publication date
JP2014513712A (ja) 2014-06-05
EP2709616B1 (en) 2018-01-24
US9505771B2 (en) 2016-11-29
US20140142158A1 (en) 2014-05-22
EP2709616A1 (en) 2014-03-26
ES2665843T3 (es) 2018-04-27
WO2012156677A1 (en) 2012-11-22

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