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EA200400815A1 - Контролируемый синтез зипразидона и его композиции - Google Patents

Контролируемый синтез зипразидона и его композиции

Info

Publication number
EA200400815A1
EA200400815A1 EA200400815A EA200400815A EA200400815A1 EA 200400815 A1 EA200400815 A1 EA 200400815A1 EA 200400815 A EA200400815 A EA 200400815A EA 200400815 A EA200400815 A EA 200400815A EA 200400815 A1 EA200400815 A1 EA 200400815A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compositions
ziprazidona
controlled synthesis
undechloroziprasidone
synthesis
Prior art date
Application number
EA200400815A
Other languages
English (en)
Other versions
EA007866B1 (ru
Inventor
Фрэнк Роберт Буш
Адам Уорт Гроубин
Гарри Ральф мл. Хауард
Кайл Роберт Лиман
Original Assignee
Пфайзер Продактс Инк.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27761437&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA200400815(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Пфайзер Продактс Инк. filed Critical Пфайзер Продактс Инк.
Publication of EA200400815A1 publication Critical patent/EA200400815A1/ru
Publication of EA007866B1 publication Critical patent/EA007866B1/ru

Links

Classifications

    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Liquid Crystal Substances (AREA)
  • Indole Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medical Preparation Storing Or Oral Administration Devices (AREA)

Abstract

Согласно данному изобретению предложена композиция зипразидона, содержащая не более 1000 млндехлорзипразидона, предпочтительно не более чем приблизительно 500 млндехлорзипразидона и более предпочтительно не более чем приблизительно 100 млндехлорзипразидона. Также предложены способы синтеза и применения таких композиций зипразидона.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200400815A 2002-02-20 2003-02-17 Контролируемый синтез зипразидона и его композиции EA007866B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US35880602P 2002-02-20 2002-02-20
US35903802P 2002-02-21 2002-02-21
US36045902P 2002-02-27 2002-02-27
PCT/IB2003/000642 WO2003070246A1 (en) 2002-02-20 2003-02-17 Controlled synthesis of ziprasidone and compositions thereof

Publications (2)

Publication Number Publication Date
EA200400815A1 true EA200400815A1 (ru) 2004-12-30
EA007866B1 EA007866B1 (ru) 2007-02-27

Family

ID=27761437

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200400815A EA007866B1 (ru) 2002-02-20 2003-02-17 Контролируемый синтез зипразидона и его композиции

Country Status (41)

Country Link
EP (1) EP1476162B1 (ru)
JP (1) JP4554938B2 (ru)
KR (1) KR100773622B1 (ru)
CN (2) CN101735212A (ru)
AP (1) AP2004003103A0 (ru)
AR (1) AR038563A1 (ru)
AT (1) ATE359787T1 (ru)
AU (2) AU2003206035A1 (ru)
BR (1) BR0307833A (ru)
CA (1) CA2475302C (ru)
CO (1) CO5611138A2 (ru)
CY (1) CY1106467T1 (ru)
DE (1) DE60313289T2 (ru)
DK (1) DK1476162T3 (ru)
EA (1) EA007866B1 (ru)
EC (1) ECSP045239A (ru)
ES (1) ES2283745T3 (ru)
GE (1) GEP20074030B (ru)
GT (1) GT200300040A (ru)
HR (1) HRP20040711A2 (ru)
IL (1) IL163277A (ru)
IS (1) IS7344A (ru)
MA (1) MA27177A1 (ru)
MX (1) MXPA04006993A (ru)
MY (1) MY139523A (ru)
NO (2) NO20043902L (ru)
NZ (1) NZ534443A (ru)
OA (1) OA12774A (ru)
PA (1) PA8567001A1 (ru)
PE (1) PE20030942A1 (ru)
PL (1) PL372238A1 (ru)
PT (1) PT1476162E (ru)
RS (1) RS60404A (ru)
SI (1) SI1476162T1 (ru)
SV (1) SV2004001485A (ru)
TN (1) TNSN04159A1 (ru)
TW (1) TW200307546A (ru)
UA (1) UA77057C2 (ru)
UY (1) UY27668A1 (ru)
WO (1) WO2003070246A1 (ru)
ZA (1) ZA200406276B (ru)

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IL151164A0 (en) 2000-03-06 2003-04-10 Acadia Pharm Inc Azacyclic compounds for use in the treatment of serotonin related diseases
DE60236206D1 (de) 2001-12-28 2010-06-10 Acadia Pharm Inc Spiroazacyclische verbindungen als monoaminrezeptormodulatoren
US7538222B2 (en) 2002-06-24 2009-05-26 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
MXPA04012893A (es) 2002-06-24 2005-03-31 Acadia Pharm Inc Derivados de piperidina n-substituidos como agentes receptores de serotonina.
US7253186B2 (en) 2002-06-24 2007-08-07 Carl-Magnus Andersson N-substituted piperidine derivatives as serotonin receptor agents
AU2003300814A1 (en) 2002-12-04 2004-06-23 Dr. Reddy's Laboratories Inc. Polymorphic forms of ziprasidone and its hydrochloride
WO2004050655A1 (en) * 2002-12-04 2004-06-17 Dr. Reddy's Laboratories Limited Polymorphic forms of ziprasidone and its hydrochloride
ATE407117T1 (de) 2003-01-16 2008-09-15 Acadia Pharm Inc Selektive serotonin 2a/2c inverse rezeptoragonisten als therapeutika für neurodegenerative erkrankungen
US7199144B2 (en) 2003-04-21 2007-04-03 Teva Pharmaceuticals Industries, Ltd. Process for the preparation of valsartan and intermediates thereof
ES2238022T3 (es) 2003-03-17 2008-11-01 Teva Pharmaceutical Industries Ltd. Poliformos de valsartan.
WO2004094392A1 (en) * 2003-04-21 2004-11-04 Teva Pharmaceutical Industries Ltd. Process for the preparation of valsartan
WO2005035531A1 (en) 2003-06-03 2005-04-21 Teva Paharmaceutical Industries Ltd. POLYMORPHIC FORMS OF ZIPRASIDONE HCl AND PROCESSES FOR THEIR PREPARATION
US7667037B2 (en) 2003-10-24 2010-02-23 Teva Pharmaceutical Industries Ltd. Processes for preparation of ziprasidone
CN1934108A (zh) * 2003-12-18 2007-03-21 特瓦制药工业有限公司 齐拉西酮碱的多晶型b2
PT1720867E (pt) 2004-02-27 2010-01-28 Ranbaxy Lab Ltd Processo para a preparação de ziprasidona
CA2467538C (en) 2004-05-14 2010-08-24 Apotex Pharmachem Inc. New amorphous ziprasidone hydrochloride (5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2h-indol-2-one hydrochloride) and processes to produce the same
US7820695B2 (en) 2004-05-21 2010-10-26 Acadia Pharmaceuticals, Inc. Selective serotonin receptor inverse agonists as therapeutics for disease
CA2471219A1 (en) 2004-06-14 2005-12-14 Apotex Pharmachem Inc. Improved preparation of an anhydrate form of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2h-indol-2-one hydrochloride (ziprasidone hydrochloride)
US7868176B2 (en) 2004-09-27 2011-01-11 Acadia Pharmaceuticals, Inc. Salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-y1)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and their preparation
US7790899B2 (en) 2004-09-27 2010-09-07 Acadia Pharmaceuticals, Inc. Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms
ES2250001B1 (es) * 2004-09-29 2007-06-01 Medichem, S.A. Proceso para la purificacion de ziprasidona.
ES2250000B1 (es) * 2004-09-29 2007-06-01 Medichem, S.A. Procedimiento para la preparacion de ziprasidona.
US20090163513A1 (en) * 2005-01-27 2009-06-25 Hetero Drugs Limited Process for ziprasidone using novel intermediates
ITMI20052216A1 (it) * 2005-11-18 2007-05-19 Dipharma Spa Procedimento per la preparazione di ziprasidone
CN100491375C (zh) * 2006-07-01 2009-05-27 浙江美诺华药物化学有限公司 一种齐拉西酮的制备方法
EP2134330B1 (en) 2007-03-19 2013-05-08 Acadia Pharmaceuticals Inc. Combinations of 5-ht2a inverse agonists and antagonists with antipsychotics
CN102234272A (zh) * 2010-04-21 2011-11-09 上海医药工业研究院 盐酸齐拉西酮半水合物的制备方法
CN102234273B (zh) * 2010-04-21 2015-08-05 上海医药工业研究院 甲磺酸齐拉西酮半水合物及其制备方法
EP3325444B1 (en) 2015-07-20 2021-07-07 Acadia Pharmaceuticals Inc. Methods for preparing n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form c
US10953000B2 (en) 2016-03-25 2021-03-23 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome P450 modulators
WO2017165635A1 (en) 2016-03-25 2017-09-28 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome p450 modulators
US11464768B2 (en) 2016-12-20 2022-10-11 Acadia Pharmaceuticals Inc. Pimavanserin alone or in combination for use in the treatment of Alzheimer's disease psychosis
CN108239085A (zh) * 2016-12-26 2018-07-03 四川科瑞德凯华制药有限公司 一种甲磺酸齐拉西酮的纯化及制备方法
US11135211B2 (en) 2017-04-28 2021-10-05 Acadia Pharmaceuticals Inc. Pimavanserin for treating impulse control disorder
US20210077479A1 (en) 2017-08-30 2021-03-18 Acadia Pharmaceuticals Inc. Formulations of pimavanserin
CN112724066B (zh) * 2021-02-04 2022-10-21 海南鑫开源医药科技有限公司 一种盐酸齐拉西酮中间体中的二卤杂质及其制备方法
CN116046966A (zh) * 2023-01-17 2023-05-02 北京协和建昊医药技术开发有限责任公司 一种流动相配置装置及其配置方法

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US4831031A (en) 1988-01-22 1989-05-16 Pfizer Inc. Aryl piperazinyl-(C2 or C4) alkylene heterocyclic compounds having neuroleptic activity
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US5312925A (en) * 1992-09-01 1994-05-17 Pfizer Inc. Monohydrate of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one-hydrochloride
US5206366A (en) * 1992-08-26 1993-04-27 Pfizer Inc. Process for preparing aryl piperazinyl-heterocyclic compounds
US5359068A (en) * 1993-06-28 1994-10-25 Pfizer Inc. Processes and intermediates for the preparation of 5-[2-(4-(benzoisothiazol-3-yl)-piperazin-1-yl)ethyl]-6-chloro-1,3-dihydro-indol-2-one
AU698443B2 (en) 1995-11-07 1998-10-29 Pfizer Inc. Processes and intermediates for preparing 3-(1-piperazinyl)-1, 2-benzisothiazole
NZ508303A (en) * 1996-05-07 2001-07-27 Pfizer Mesylate trihydrate salt of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2(1H)-indol-2-one (ziprasidone) useful as a dopamine D2 antagonist
TW491847B (en) * 1996-05-07 2002-06-21 Pfizer Mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2h-indol-2-one
IL127497A (en) * 1997-12-18 2002-07-25 Pfizer Prod Inc Medicinal products containing piperazinyl-heterocyclic compounds for the treatment of psychiatric disorders
US6150366A (en) * 1998-06-15 2000-11-21 Pfizer Inc. Ziprasidone formulations

Also Published As

Publication number Publication date
SV2004001485A (es) 2004-05-07
ATE359787T1 (de) 2007-05-15
MA27177A1 (fr) 2005-01-03
AU2003206035A1 (en) 2003-09-09
DE60313289D1 (de) 2007-05-31
IL163277A (en) 2010-05-31
NO20100584L (no) 2004-09-17
RS60404A (sr) 2006-10-27
TNSN04159A1 (fr) 2007-03-12
PT1476162E (pt) 2007-06-25
UA77057C2 (en) 2006-10-16
CO5611138A2 (es) 2006-02-28
HRP20040711A2 (en) 2004-12-31
ZA200406276B (en) 2005-09-20
JP4554938B2 (ja) 2010-09-29
PE20030942A1 (es) 2003-11-08
GT200300040A (es) 2007-01-12
ES2283745T3 (es) 2007-11-01
NZ534443A (en) 2007-07-27
AU2009202008A1 (en) 2009-06-11
NO20043902L (no) 2004-09-17
CA2475302C (en) 2009-05-12
PL372238A1 (en) 2005-07-11
CN101735212A (zh) 2010-06-16
SI1476162T1 (sl) 2007-08-31
ECSP045239A (es) 2004-09-28
UY27668A1 (es) 2003-10-31
EA007866B1 (ru) 2007-02-27
EP1476162A1 (en) 2004-11-17
MY139523A (en) 2009-10-30
WO2003070246A1 (en) 2003-08-28
TW200307546A (en) 2003-12-16
JP2005525347A (ja) 2005-08-25
KR20040086417A (ko) 2004-10-08
AR038563A1 (es) 2005-01-19
EP1476162B1 (en) 2007-04-18
BR0307833A (pt) 2004-12-07
CY1106467T1 (el) 2012-01-25
MXPA04006993A (es) 2004-11-10
OA12774A (en) 2006-07-04
GEP20074030B (en) 2007-02-12
DK1476162T3 (da) 2007-07-02
KR100773622B1 (ko) 2007-11-05
DE60313289T2 (de) 2007-12-27
CA2475302A1 (en) 2003-08-28
AP2004003103A0 (en) 2004-09-30
CN1635892A (zh) 2005-07-06
IS7344A (is) 2004-07-05
PA8567001A1 (es) 2003-12-10

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Legal Events

Date Code Title Description
MH4D Revocation of a eurasian patent in part

Designated state(s): RU

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU