CN1091769C - 5-(2-(4-(1,2-苯并异噻唑-3-基)-1-哌嗪基)乙基)-6-氯-1,3-二氢-2(1h)-吲哚-2-酮(=ziprasidone)的甲磺酸盐二水合物,它的制备及其作为多巴胺d2拮抗剂的用途 - Google Patents

5-(2-(4-(1,2-苯并异噻唑-3-基)-1-哌嗪基)乙基)-6-氯-1,3-二氢-2(1h)-吲哚-2-酮(=ziprasidone)的甲磺酸盐二水合物,它的制备及其作为多巴胺d2拮抗剂的用途 Download PDF

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Publication number
CN1091769C
CN1091769C CN97194244A CN97194244A CN1091769C CN 1091769 C CN1091769 C CN 1091769C CN 97194244 A CN97194244 A CN 97194244A CN 97194244 A CN97194244 A CN 97194244A CN 1091769 C CN1091769 C CN 1091769C
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degree
dihydro
chloro
ethyl
dihydrate
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Expired - Fee Related
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Chinese (zh)
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CN1216991A (zh
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弗兰克·R·布希
卡罗尔·A·罗斯
拉塞尔·J·夏因
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Pfizer Inc
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Pfizer Inc
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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
    • C07D417/12—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 chain containing hetero atoms as chain links
    • 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
    • A61P25/18—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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
  • Saccharide Compounds (AREA)
CN97194244A 1996-05-07 1997-04-10 5-(2-(4-(1,2-苯并异噻唑-3-基)-1-哌嗪基)乙基)-6-氯-1,3-二氢-2(1h)-吲哚-2-酮(=ziprasidone)的甲磺酸盐二水合物,它的制备及其作为多巴胺d2拮抗剂的用途 Expired - Fee Related CN1091769C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US1675796P 1996-05-07 1996-05-07
US60/016,757 1996-05-07

Publications (2)

Publication Number Publication Date
CN1216991A CN1216991A (zh) 1999-05-19
CN1091769C true CN1091769C (zh) 2002-10-02

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CN97194244A Expired - Fee Related CN1091769C (zh) 1996-05-07 1997-04-10 5-(2-(4-(1,2-苯并异噻唑-3-基)-1-哌嗪基)乙基)-6-氯-1,3-二氢-2(1h)-吲哚-2-酮(=ziprasidone)的甲磺酸盐二水合物,它的制备及其作为多巴胺d2拮抗剂的用途

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US (1) US6245765B1 (enExample)
EP (1) EP0918772B1 (enExample)
JP (1) JP3494659B2 (enExample)
KR (1) KR100333215B1 (enExample)
CN (1) CN1091769C (enExample)
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Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HN1996000101A (es) * 1996-02-28 1997-06-26 Inc Pfizer Terapia combinada para la osteoporosis
UA57734C2 (uk) 1996-05-07 2003-07-15 Пфайзер Інк. Комплекси включення арилгетероциклічних солей
IL127497A (en) * 1997-12-18 2002-07-25 Pfizer Prod Inc Medicinal products containing piperazinyl-heterocyclic compounds for the treatment of psychiatric disorders
US20080113025A1 (en) * 1998-11-02 2008-05-15 Elan Pharma International Limited Compositions comprising nanoparticulate naproxen and controlled release hydrocodone
KR20030007824A (ko) * 2000-06-02 2003-01-23 화이자 프로덕츠 인크. 정신의학적 장애 및 안질환의 치료를 위한ｓ-메틸-디히드로-지프라시돈
UY27668A1 (es) * 2002-02-20 2003-10-31 Pfizer Prod Inc Composición de ziprasidona y controles sintéticos
US20040048876A1 (en) * 2002-02-20 2004-03-11 Pfizer Inc. Ziprasidone composition and synthetic controls
CA2525366A1 (en) 2003-05-16 2004-11-25 Pfizer Products Inc. Therapeutic combinations of atypical antipsychotics with gaba modulators, anticonvulsants or benzodiazapines
US20050043324A1 (en) * 2003-06-03 2005-02-24 Tamas Koltai Polymorphic forms of ziprasidone HCI and processes for their preparation
EP1628973A2 (en) 2003-10-24 2006-03-01 Teva Pharmaceutical Industries Ltd. Processes for preparation of ziprasidone
JP2007537232A (ja) * 2004-05-11 2007-12-20 ファイザー・プロダクツ・インク 非定型抗精神病薬と５−ｈｔ１ｂ受容体拮抗薬の組合せ
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
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)
US7777037B2 (en) * 2004-10-27 2010-08-17 Dr. Reddy's Laboratories Limited Ziprasidone process
EA200701065A1 (ru) * 2004-11-16 2007-12-28 Элан Фарма Интернэшнл Лтд. Инъецируемые составы, содержащие нанодисперсный оланзапин
CA2593497A1 (en) * 2005-02-11 2006-08-17 Judith Aronhime Amorphous ziprasidone mesylate
CA2591670A1 (en) * 2005-02-11 2006-08-17 Teva Pharmaceutical Industries Ltd. Process of preparing ziprasidone mesylate
JP2008531721A (ja) * 2005-03-03 2008-08-14 エラン・ファルマ・インターナショナル・リミテッド 複素環式アミド誘導体のナノ粒子状組成物
ITMI20050346A1 (it) 2005-03-07 2006-09-08 Dipharma Spa Forma solida di ziprasidone cloridrato
CA2500667C (en) 2005-03-11 2013-01-15 Apotex Pharmachem Inc. Preparation of acid addition salts of ziprasidone and intermediates thereof by solid phase-gas phase reactions
WO2006098834A2 (en) * 2005-03-14 2006-09-21 Teva Pharmaceutical Industries Ltd. Crystalline forms of ziprasidone mesylate
EP1858892A1 (en) * 2005-03-14 2007-11-28 Teva Pharmaceutical Industries Ltd Anhydrous ziprasidone mesylate and a process for its preparation
ITMI20052216A1 (it) * 2005-11-18 2007-05-19 Dipharma Spa Procedimento per la preparazione di ziprasidone
MX2009011681A (es) * 2007-05-18 2009-11-10 Scidose Llc Formulaciones de ziprasidona.
WO2009156889A1 (en) * 2008-06-25 2009-12-30 Pfizer Inc. Diaryl compounds and uses thereof
EP2629775A4 (en) * 2010-10-18 2014-06-11 Dainippon Sumitomo Pharma Co INJECTABLE FORMULATION WITH DELAYED RELEASE
SI23610A (sl) 2011-01-13 2012-07-31 Diagen@d@o@o Nove adicijske soli ziprasidona postopek za njihovo pripravo in njihova uporaba v terapiji
US10154988B2 (en) 2012-11-14 2018-12-18 The Johns Hopkins University Methods and compositions for treating schizophrenia

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0281309A1 (en) * 1987-03-02 1988-09-07 Pfizer Inc. Piperazinyl-heterocyclic compounds
EP0584903A1 (en) * 1992-08-26 1994-03-02 Pfizer Inc. Process for preparing aryl piperazinyl-heterocyclic compounds
EP0586191A1 (en) * 1992-09-01 1994-03-09 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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4831031A (en) * 1988-01-22 1989-05-16 Pfizer Inc. Aryl piperazinyl-(C2 or C4) alkylene heterocyclic compounds having neuroleptic activity
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
US6110918A (en) 1996-05-07 2000-08-29 Pfizer Inc Mesylate trihydrate salt of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihy dro-2(1H)-indol-2-one (=ziprasidone), its preparation and its use as dopamine D2 antagonist

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0281309A1 (en) * 1987-03-02 1988-09-07 Pfizer Inc. Piperazinyl-heterocyclic compounds
EP0584903A1 (en) * 1992-08-26 1994-03-02 Pfizer Inc. Process for preparing aryl piperazinyl-heterocyclic compounds
EP0586191A1 (en) * 1992-09-01 1994-03-09 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

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AU2174797A (en) 1997-11-26
ZA973876B (en) 1998-11-06
TR199802240T2 (enExample) 1999-02-22
CN1216991A (zh) 1999-05-19
PL188330B1 (pl) 2005-01-31
DE69731094D1 (de) 2004-11-11
EA001190B1 (ru) 2000-12-25
TNSN97074A1 (fr) 2005-03-15
AR007004A1 (es) 1999-10-13
BG63544B1 (bg) 2002-04-30
TW491847B (en) 2002-06-21
CZ349398A3 (cs) 1999-09-15
SK150898A3 (en) 2000-02-14
NO312514B1 (no) 2002-05-21
EP0918772B1 (en) 2004-10-06
BR9709889A (pt) 1999-08-10
EG24076A (en) 2008-05-11
ES2229342T3 (es) 2005-04-16
HRP970236B1 (en) 2002-12-31
KR100333215B1 (ko) 2002-06-20
AU731267B2 (en) 2001-03-29
EA199800912A1 (ru) 1999-04-29
IL126591A0 (en) 1999-08-17
HRP970236A2 (en) 1998-06-30
EP0918772A1 (en) 1999-06-02
CA2252898C (en) 2003-04-08
HK1017892A1 (en) 1999-12-03
NO985194D0 (no) 1998-11-06
CO4940466A1 (es) 2000-07-24
GT199700052A (es) 2001-08-29
CA2252898A1 (en) 1997-11-13
NO985194L (no) 1998-11-06
NZ332218A (en) 2005-02-25
IS2080B (is) 2006-02-15
MA24171A1 (fr) 1997-12-31
MY119997A (en) 2005-08-30
DE69731094T2 (de) 2006-02-23
ID16867A (id) 1997-11-20
PL329884A1 (en) 1999-04-12
CZ289215B6 (cs) 2001-12-12
AP9700976A0 (en) 1997-07-31
IS4874A (is) 1998-10-20
DK0918772T3 (da) 2005-01-10
DZ2222A1 (fr) 2002-12-03
UA46840C2 (uk) 2002-06-17
AP765A (en) 1999-09-17
KR20000010824A (ko) 2000-02-25
OA10909A (en) 2001-10-26
US6245765B1 (en) 2001-06-12
ATE278689T1 (de) 2004-10-15
JPH11509867A (ja) 1999-08-31
WO1997042191A1 (en) 1997-11-13
IL126591A (en) 2001-11-25
SI0918772T1 (en) 2005-02-28
SK282837B6 (sk) 2002-12-03
PT918772E (pt) 2004-12-31
BG102892A (en) 1999-09-30
JP3494659B2 (ja) 2004-02-09

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