JP2013520488A - ペルフェナジン−gabaのトリメシラート塩の結晶性形態物及びその製法方法 - Google Patents

ペルフェナジン−gabaのトリメシラート塩の結晶性形態物及びその製法方法 Download PDF

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JP2013520488A
JP2013520488A JP2012554446A JP2012554446A JP2013520488A JP 2013520488 A JP2013520488 A JP 2013520488A JP 2012554446 A JP2012554446 A JP 2012554446A JP 2012554446 A JP2012554446 A JP 2012554446A JP 2013520488 A JP2013520488 A JP 2013520488A
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Prior art keywords
perphenazine
crystalline form
aminobutyrate
trimesylate
aminobutyrate trimesylate
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Pending
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JP2012554446A
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English (en)
Japanese (ja)
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JP2013520488A5 (enExample
Inventor
アブラハム ヌデルマン,
アダ レファエリ,
イリット ギル−アド,
アブラハム ウェイズマン,
マザル シャウル,
エフラット ハルブフィンガー,
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Ramot at Tel Aviv University Ltd
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Ramot at Tel Aviv University Ltd
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Application filed by Ramot at Tel Aviv University Ltd filed Critical Ramot at Tel Aviv University Ltd
Publication of JP2013520488A publication Critical patent/JP2013520488A/ja
Publication of JP2013520488A5 publication Critical patent/JP2013520488A5/ja
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D279/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/101,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/141,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/18[b, e]-condensed with two six-membered rings
    • C07D279/22[b, e]-condensed with two six-membered rings with carbon atoms directly attached to the ring nitrogen atom
    • C07D279/24[b, e]-condensed with two six-membered rings with carbon atoms directly attached to the ring nitrogen atom with hydrocarbon radicals, substituted by amino radicals, attached to the ring nitrogen atom
    • C07D279/28[b, e]-condensed with two six-membered rings with carbon atoms directly attached to the ring nitrogen atom with hydrocarbon radicals, substituted by amino radicals, attached to the ring nitrogen atom with other substituents attached to the ring system
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10TTECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T428/00Stock material or miscellaneous articles
    • Y10T428/29Coated or structually defined flake, particle, cell, strand, strand portion, rod, filament, macroscopic fiber or mass thereof
    • Y10T428/2982Particulate matter [e.g., sphere, flake, etc.]

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
JP2012554446A 2010-02-24 2011-02-24 ペルフェナジン−gabaのトリメシラート塩の結晶性形態物及びその製法方法 Pending JP2013520488A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US30748110P 2010-02-24 2010-02-24
US30748210P 2010-02-24 2010-02-24
US61/307,482 2010-02-24
US61/307,481 2010-02-24
PCT/IB2011/000915 WO2011104637A2 (en) 2010-02-24 2011-02-24 Crystalline forms of the tri-mesylate salt of perphenazine-gaba and process of producing the same

Publications (2)

Publication Number Publication Date
JP2013520488A true JP2013520488A (ja) 2013-06-06
JP2013520488A5 JP2013520488A5 (enExample) 2014-01-30

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ID=44507308

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JP2012554446A Pending JP2013520488A (ja) 2010-02-24 2011-02-24 ペルフェナジン−gabaのトリメシラート塩の結晶性形態物及びその製法方法

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Country Link
US (2) US8377929B2 (enExample)
EP (1) EP2539857A4 (enExample)
JP (1) JP2013520488A (enExample)
CN (1) CN102858345A (enExample)
AU (1) AU2011219529A1 (enExample)
CA (1) CA2789654A1 (enExample)
IL (1) IL221461A0 (enExample)
MX (1) MX2012009821A (enExample)
WO (1) WO2011104637A2 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7544681B2 (en) * 2001-09-27 2009-06-09 Ramot At Tel Aviv University Ltd. Conjugated psychotropic drugs and uses thereof
JP5284779B2 (ja) * 2005-06-07 2013-09-11 ラモット・アット・テル・アビブ・ユニバーシテイ・リミテッド コンジュゲート化された向精神薬の新規な塩およびその調製方法
WO2008010223A2 (en) * 2006-07-17 2008-01-24 Ramot At Tel Aviv University Ltd. Conjugates comprising a psychotropic drug or a gaba agonist and an organic acid and their use in treating pain and other cns disorders
US8207369B2 (en) * 2008-02-11 2012-06-26 Ramot At Tel-Aviv University Ltd. Conjugates for treating neurodegenerative diseases and disorders
CN102762211A (zh) 2009-12-09 2012-10-31 拜欧利纳斯有限公司 改善认知功能的方法
MX2012009821A (es) 2010-02-24 2012-10-09 Univ Ramot Formas cristalinas de la sal de tri-mesilato de perfenazina-gaba y proceso para producirlas.
US8916610B2 (en) 2010-09-22 2014-12-23 Ramot At Tel-Aviv University Ltd. Acid addition salt of a nortriptyline-GABA conjugate and a process of preparing same
US10562930B1 (en) * 2018-08-31 2020-02-18 Praxis Precision Medicines, Inc. Salts and crystal forms of GABAA positive allosteric modulator

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008545777A (ja) * 2005-06-07 2008-12-18 ラモト アット テル アヴィヴ ユニヴァーシティ リミテッド コンジュゲート化された向精神薬の新規な塩およびその調製方法

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US5780590A (en) 1993-10-15 1998-07-14 Rhone-Poulenc Rorer Pharmaceuticals Inc. Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides
US5534522A (en) 1995-06-07 1996-07-09 Warner-Lambert Company (R)-(Z)-1-azabicyclo [2.2.1] heptan-3-one,O-[3-(3-methoxyphenyl)-2-propynyl] oxime maleate as a pharmaceutical agent
AU6636996A (en) 1995-07-13 1997-02-10 Anormed Inc. 2-{2-(dimethylamino)ethyl}-8,8-dipropyl-2-azaspiro{4.5}decan edimaleate
DE19622489A1 (de) 1996-06-05 1997-12-11 Hoechst Ag Salze des 3-(2-(4-(4-(Amino-imino-methyl)-phenyl)-4- methyl-2,5-dioxo-imidazolidin-1-yl)-acetylamino)-3- phenyl-propionsäure-ethylesters
US6130221A (en) 1997-03-05 2000-10-10 Nymox Corporation Pharmaceutical agents that impede the initiation and progression of primary and secondary DMS disruptions
TWI238062B (en) 1999-12-01 2005-08-21 Ucb Sa A pyrrolidineacetamide derivative alone or in combination for treatment of CNS disorders
JP2005097120A (ja) 2000-10-06 2005-04-14 Mochida Pharmaceut Co Ltd 4−ヒドロキシピペリジン誘導体の非潮解性塩
US7544681B2 (en) * 2001-09-27 2009-06-09 Ramot At Tel Aviv University Ltd. Conjugated psychotropic drugs and uses thereof
KR100996239B1 (ko) 2001-09-27 2010-11-23 바-일란 유니버시티 접합된 항-정신병 약물 및 그의 용도
US7005138B2 (en) 2001-12-21 2006-02-28 Duramed Pharmaceuticals, Inc. Method of systematically delivering SSRIs
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US8916610B2 (en) 2010-09-22 2014-12-23 Ramot At Tel-Aviv University Ltd. Acid addition salt of a nortriptyline-GABA conjugate and a process of preparing same

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008545777A (ja) * 2005-06-07 2008-12-18 ラモト アット テル アヴィヴ ユニヴァーシティ リミテッド コンジュゲート化された向精神薬の新規な塩およびその調製方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ABRAHAM NUDELMAN ET AL: "A Mutual Prodrug Ester of GABA and Perphenazine Exhibits Antischizophrenic Efficacy with Diminished", J. MED. CHEM, vol. 51, JPN6014042815, 2008, pages 2858 - 2862, ISSN: 0002914741 *

Also Published As

Publication number Publication date
WO2011104637A2 (en) 2011-09-01
US8377929B2 (en) 2013-02-19
WO2011104637A3 (en) 2012-02-23
CA2789654A1 (en) 2011-09-01
US20110312948A1 (en) 2011-12-22
WO2011104637A9 (en) 2012-01-05
US20130150352A1 (en) 2013-06-13
MX2012009821A (es) 2012-10-09
EP2539857A4 (en) 2013-07-24
CN102858345A (zh) 2013-01-02
AU2011219529A1 (en) 2012-08-30
EP2539857A2 (en) 2013-01-02
IL221461A0 (en) 2012-10-31

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