CN102858345A - 奋乃静-gaba的三甲磺酸盐的晶型及其制备方法 - Google Patents

奋乃静-gaba的三甲磺酸盐的晶型及其制备方法 Download PDF

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Publication number
CN102858345A
CN102858345A CN2011800207232A CN201180020723A CN102858345A CN 102858345 A CN102858345 A CN 102858345A CN 2011800207232 A CN2011800207232 A CN 2011800207232A CN 201180020723 A CN201180020723 A CN 201180020723A CN 102858345 A CN102858345 A CN 102858345A
Authority
CN
China
Prior art keywords
perphenazine
trimesylate
aminobutyrate
xrpd
crystal form
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN2011800207232A
Other languages
English (en)
Chinese (zh)
Inventor
亚伯拉罕·努德尔曼
阿达·雷帕埃利
埃利特·吉尔-阿德
亚伯拉罕·魏茨曼
马扎尔·肖尔
埃弗拉特·哈尔布芬格尔
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ramot at Tel Aviv University Ltd
Bar Ilan University
BiolineRx Ltd
Original Assignee
Ramot at Tel Aviv University Ltd
Bar Ilan University
BiolineRx Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ramot at Tel Aviv University Ltd, Bar Ilan University, BiolineRx Ltd filed Critical Ramot at Tel Aviv University Ltd
Publication of CN102858345A publication Critical patent/CN102858345A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/06—Heterocyclic 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
    • 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
    • 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
    • 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
    • A61P25/28—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-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
    • Y—GENERAL 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
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T428/00—Stock material or miscellaneous articles
    • Y10T428/29—Coated or structually defined flake, particle, cell, strand, strand portion, rod, filament, macroscopic fiber or mass thereof
    • Y10T428/2982—Particulate 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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN2011800207232A 2010-02-24 2011-02-24 奋乃静-gaba的三甲磺酸盐的晶型及其制备方法 Pending CN102858345A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US30748210P 2010-02-24 2010-02-24
US30748110P 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 (1)

Publication Number Publication Date
CN102858345A true CN102858345A (zh) 2013-01-02

Family

ID=44507308

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2011800207232A Pending CN102858345A (zh) 2010-02-24 2011-02-24 奋乃静-gaba的三甲磺酸盐的晶型及其制备方法

Country Status (9)

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

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
EP2051735B1 (en) 2006-07-17 2012-08-29 Ramot, at Tel Aviv University Ltd. Conjugates comprising a psychotropic drug or a gaba agonist and an organic acid and their use treating pain and other cns disorders
WO2009101616A1 (en) 2008-02-11 2009-08-20 Ramot At Tel Aviv University Ltd. Novel conjugates for treating neurodegenerative diseases and disorders
WO2011070579A1 (en) * 2009-12-09 2011-06-16 Biolinerx Ltd. Methods of improving cognitive functions
US8377929B2 (en) 2010-02-24 2013-02-19 Ramot At Tel-Aviv University Ltd. Crystalline forms of the tri-mesylate salt of perphenazine-GABA and process of producing the same
WO2012038963A1 (en) 2010-09-22 2012-03-29 Ramot At Tel-Aviv University Ltd. An 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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005092392A2 (en) * 2004-03-25 2005-10-06 Ramot At Tel Aviv University Ltd. Conjugated psychotropic drugs and uses thereof
CN101247837A (zh) * 2005-06-07 2008-08-20 特拉维夫大学拉莫特有限公司 新的轭合精神活性药物的盐及其制备方法
US20090215809A1 (en) * 2008-01-25 2009-08-27 Xenoport, Inc. Crystalline form of a (3s)-aminomethyl-5-methyl-hexanoic acid prodrug and methods of use

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US5525727A (en) 1982-05-18 1996-06-11 University Of Florida Brain-specific drug delivery
GB8608335D0 (en) 1986-04-04 1986-05-08 Pfizer Ltd Pharmaceutically acceptable salts
US5145684A (en) * 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
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
US5952365A (en) 1995-07-13 1999-09-14 Anormed Inc. 2- 2-(Dimethylamino)ethyl!-8,8-dipropyl-2-azaspiro 4.5!decane dimaleate
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
CA2475026A1 (en) 1999-12-01 2001-06-07 Ucb, S.A. 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
JP4521187B2 (ja) 2001-09-27 2010-08-11 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 コンジュゲートされた抗精神病薬およびこれらの使用
US7005138B2 (en) 2001-12-21 2006-02-28 Duramed Pharmaceuticals, Inc. Method of systematically delivering SSRIs
US20040092504A1 (en) 2002-11-12 2004-05-13 Anuthep Benja-Athon Definitive medications for treating fibromyalgia
TW200616604A (en) 2004-08-26 2006-06-01 Nicholas Piramal India Ltd Nitric oxide releasing prodrugs containing bio-cleavable linker
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
TWI378091B (en) 2006-03-09 2012-12-01 Eisai R&D Man Co Ltd Multi-cyclic cinnamide derivatives
US8377929B2 (en) 2010-02-24 2013-02-19 Ramot At Tel-Aviv University Ltd. Crystalline forms of the tri-mesylate salt of perphenazine-GABA and process of producing the same
WO2012038963A1 (en) 2010-09-22 2012-03-29 Ramot At Tel-Aviv University Ltd. An acid addition salt of a nortriptyline-gaba conjugate and a process of preparing same

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005092392A2 (en) * 2004-03-25 2005-10-06 Ramot At Tel Aviv University Ltd. Conjugated psychotropic drugs and uses thereof
CN101247837A (zh) * 2005-06-07 2008-08-20 特拉维夫大学拉莫特有限公司 新的轭合精神活性药物的盐及其制备方法
US20090215809A1 (en) * 2008-01-25 2009-08-27 Xenoport, Inc. Crystalline form of a (3s)-aminomethyl-5-methyl-hexanoic acid prodrug and methods of use

Also Published As

Publication number Publication date
CA2789654A1 (en) 2011-09-01
IL221461A0 (en) 2012-10-31
WO2011104637A2 (en) 2011-09-01
EP2539857A4 (en) 2013-07-24
AU2011219529A1 (en) 2012-08-30
US20130150352A1 (en) 2013-06-13
US20110312948A1 (en) 2011-12-22
WO2011104637A3 (en) 2012-02-23
MX2012009821A (es) 2012-10-09
WO2011104637A9 (en) 2012-01-05
US8377929B2 (en) 2013-02-19
JP2013520488A (ja) 2013-06-06
EP2539857A2 (en) 2013-01-02

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Application publication date: 20130102