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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Japan
Prior art keywords
asenapine maleate
monoclinic
less
asenapine
micronized
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JP2014510872A
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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 (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2011268335A1 (en) * 2010-06-18 2013-01-10 Dr. Reddy's Laboratories Ltd. Asenapine maleate
US10085971B2 (en) * 2016-08-22 2018-10-02 Navinta Iii Inc Pharmaceutical solution of asenapine for sublingual or buccal use
KR102614709B1 (ko) 2016-12-20 2023-12-18 에르테에스 로만 테라피-시스테메 아게 아세나핀 및 폴리실록산 또는 폴리이소부틸렌을 함유하는 경피흡수 치료 시스템
EP3338768B1 (en) 2016-12-20 2019-10-30 LTS Lohmann Therapie-Systeme AG Transdermal therapeutic system containing asenapine
US11033512B2 (en) 2017-06-26 2021-06-15 Lts Lohmann Therapie-Systeme Ag Transdermal therapeutic system containing asenapine and silicone acrylic hybrid polymer
US12329862B2 (en) 2018-06-20 2025-06-17 Lts Lohmann Therapie-Systeme Ag Transdermal therapeutic system containing asenapine
AU2019291060B2 (en) 2018-06-20 2024-09-05 Lts Lohmann Therapie-Systeme Ag Transdermal therapeutic system containing asenapine
US20250032451A1 (en) * 2021-11-24 2025-01-30 Oakwood Laboratories, Llc Microsphere formulations comprising asenapine and methods for making and using the same

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.
JP4099224B2 (ja) * 1994-03-02 2008-06-11 ナームローゼ・フエンノートチヤツプ・オルガノン 舌下又はバッカル医薬組成物
IL156532A0 (en) * 2000-12-27 2004-01-04 Ares Trading Sa Lipid microparticles, their preparation and pharmaceutical compositions containing them
ES2293626T3 (es) 2005-04-07 2008-03-16 N.V. Organon Forma cristalina del maleato de asenapina.
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
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
EP2170399A1 (en) * 2007-06-05 2010-04-07 Synthon B.V. Intranasal administration of asenapine and pharmaceutical compositions therefor
AU2011268335A1 (en) * 2010-06-18 2013-01-10 Dr. Reddy's Laboratories Ltd. Asenapine maleate
KR101810717B1 (ko) * 2010-07-29 2017-12-19 라보라토리오스 레스비, 에스.엘. 아세나핀을 제조하는 신규한 방법
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
US9533994B2 (en) * 2011-05-18 2017-01-03 Laboratorios Lesvi S.L. Monoclinic crystalline form of asenapine maleate with a specific particle size distribution

Also Published As

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

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