AU731267B2 - Mesylate dihydrate salts of 5-(2-(4-(1,2-benzis othiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2 (1H)-indol-2-one (=ziprasidone), its preparation and its use as dopamine D2 antagonist - Google Patents

Mesylate dihydrate salts of 5-(2-(4-(1,2-benzis othiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2 (1H)-indol-2-one (=ziprasidone), its preparation and its use as dopamine D2 antagonist Download PDF

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Publication number
AU731267B2
AU731267B2 AU21747/97A AU2174797A AU731267B2 AU 731267 B2 AU731267 B2 AU 731267B2 AU 21747/97 A AU21747/97 A AU 21747/97A AU 2174797 A AU2174797 A AU 2174797A AU 731267 B2 AU731267 B2 AU 731267B2
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AU
Australia
Prior art keywords
compound
disorder
composition
chloro
schizophrenia
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.)
Ceased
Application number
AU21747/97A
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English (en)
Other versions
AU2174797A (en
Inventor
Frank Robert Busch
Carol Anne Rose
Russell James Shine
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Pfizer Corp SRL
Original Assignee
Pfizer Corp Belgium
Pfizer Inc
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Application filed by Pfizer Corp Belgium, Pfizer Inc filed Critical Pfizer Corp Belgium
Publication of AU2174797A publication Critical patent/AU2174797A/en
Application granted granted Critical
Publication of AU731267B2 publication Critical patent/AU731267B2/en
Anticipated expiration legal-status Critical
Ceased 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
    • C07D417/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • 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
    • A61P25/06Antimigraine agents
    • 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
    • A61P25/22Anxiolytics

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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)
AU21747/97A 1996-05-07 1997-04-10 Mesylate dihydrate salts of 5-(2-(4-(1,2-benzis othiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2 (1H)-indol-2-one (=ziprasidone), its preparation and its use as dopamine D2 antagonist Ceased AU731267B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US1675796P 1996-05-07 1996-05-07
US60/016757 1996-05-07
PCT/IB1997/000393 WO1997042191A1 (en) 1996-05-07 1997-04-10 Mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2(1h)-indol-2-one (=ziprasidone), its preparation and its use as dopamine d2 antagonist

Publications (2)

Publication Number Publication Date
AU2174797A AU2174797A (en) 1997-11-26
AU731267B2 true AU731267B2 (en) 2001-03-29

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AU21747/97A Ceased AU731267B2 (en) 1996-05-07 1997-04-10 Mesylate dihydrate salts of 5-(2-(4-(1,2-benzis othiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2 (1H)-indol-2-one (=ziprasidone), its preparation and its use as dopamine D2 antagonist

Country Status (40)

Country Link
US (1) US6245765B1 (cg-RX-API-DMAC10.html)
EP (1) EP0918772B1 (cg-RX-API-DMAC10.html)
JP (1) JP3494659B2 (cg-RX-API-DMAC10.html)
KR (1) KR100333215B1 (cg-RX-API-DMAC10.html)
CN (1) CN1091769C (cg-RX-API-DMAC10.html)
AP (1) AP765A (cg-RX-API-DMAC10.html)
AR (1) AR007004A1 (cg-RX-API-DMAC10.html)
AT (1) ATE278689T1 (cg-RX-API-DMAC10.html)
AU (1) AU731267B2 (cg-RX-API-DMAC10.html)
BG (1) BG63544B1 (cg-RX-API-DMAC10.html)
BR (1) BR9709889A (cg-RX-API-DMAC10.html)
CA (1) CA2252898C (cg-RX-API-DMAC10.html)
CO (1) CO4940466A1 (cg-RX-API-DMAC10.html)
CZ (1) CZ289215B6 (cg-RX-API-DMAC10.html)
DE (1) DE69731094T2 (cg-RX-API-DMAC10.html)
DK (1) DK0918772T3 (cg-RX-API-DMAC10.html)
DZ (1) DZ2222A1 (cg-RX-API-DMAC10.html)
EA (1) EA001190B1 (cg-RX-API-DMAC10.html)
EG (1) EG24076A (cg-RX-API-DMAC10.html)
ES (1) ES2229342T3 (cg-RX-API-DMAC10.html)
GT (1) GT199700052A (cg-RX-API-DMAC10.html)
HR (1) HRP970236B1 (cg-RX-API-DMAC10.html)
ID (1) ID16867A (cg-RX-API-DMAC10.html)
IL (1) IL126591A (cg-RX-API-DMAC10.html)
IS (1) IS2080B (cg-RX-API-DMAC10.html)
MA (1) MA24171A1 (cg-RX-API-DMAC10.html)
MY (1) MY119997A (cg-RX-API-DMAC10.html)
NO (1) NO312514B1 (cg-RX-API-DMAC10.html)
NZ (1) NZ332218A (cg-RX-API-DMAC10.html)
OA (1) OA10909A (cg-RX-API-DMAC10.html)
PL (1) PL188330B1 (cg-RX-API-DMAC10.html)
PT (1) PT918772E (cg-RX-API-DMAC10.html)
SI (1) SI0918772T1 (cg-RX-API-DMAC10.html)
SK (1) SK282837B6 (cg-RX-API-DMAC10.html)
TN (1) TNSN97074A1 (cg-RX-API-DMAC10.html)
TR (1) TR199802240T2 (cg-RX-API-DMAC10.html)
TW (1) TW491847B (cg-RX-API-DMAC10.html)
UA (1) UA46840C2 (cg-RX-API-DMAC10.html)
WO (1) WO1997042191A1 (cg-RX-API-DMAC10.html)
ZA (1) ZA973876B (cg-RX-API-DMAC10.html)

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
CZ20023860A3 (cs) * 2000-06-02 2004-01-14 Pfizer Products Inc. S-Methyldihydroziprasidon pro léčení psychických a očních poruch
US20040048876A1 (en) * 2002-02-20 2004-03-11 Pfizer Inc. Ziprasidone composition and synthetic controls
UY27668A1 (es) 2002-02-20 2003-10-31 Pfizer Prod Inc Composición de ziprasidona y controles sintéticos
JP2006528676A (ja) 2003-05-16 2006-12-21 ファイザー・プロダクツ・インク 非定形型抗精神病薬と、gaba調節薬及び/又は抗痙攣薬の治療上の組合せ
WO2005016325A2 (en) * 2003-06-03 2005-02-24 Teva Pharmaceutical Industries Ltd. CRISTALLINE ZIPRASIDONE HCl AND PROCESSES FOR PREPARATION THEREOF
WO2005040160A2 (en) 2003-10-24 2005-05-06 Teva Pharmaceutical Industries Ltd. Processes for preparation of ziprasidone
BRPI0510942A (pt) * 2004-05-11 2007-07-17 Pfizer Prod Inc combinação de antipsicóticos atìpicos e antagonistas do receptor 5-ht1b
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
EP1827374B1 (en) * 2004-11-16 2014-11-05 Alkermes Pharma Ireland Limited Injectable nanoparticulate olanzapine formulations
EP1742943A1 (en) * 2005-02-11 2007-01-17 Teva Pharmaceutical Industries Ltd Process of preparing ziprasidone mesylate
EP1863806A1 (en) * 2005-02-11 2007-12-12 Teva Pharmaceutical Industries Ltd Amorphous ziprasidone mesylate
WO2006096462A1 (en) * 2005-03-03 2006-09-14 Elan Pharma International Limited Nanoparticulate compositions of heterocyclic amide derivatives
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
WO2006099452A1 (en) * 2005-03-14 2006-09-21 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.
EP2321011A1 (en) * 2008-06-25 2011-05-18 Pfizer Inc. Diaryl compounds and uses thereof
US9469630B2 (en) * 2010-10-18 2016-10-18 Sumitomo Dainippon Pharma Co., Ltd. Sustained-release formulation for injection
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
JP6440625B2 (ja) 2012-11-14 2018-12-19 ザ・ジョンズ・ホプキンス・ユニバーシティー 精神分裂病を処置するための方法および組成物

Citations (1)

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

Family Cites Families (5)

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Publication number Priority date Publication date Assignee Title
MX173362B (es) 1987-03-02 1994-02-23 Pfizer Compuestos de piperazinil heterociclicos y procedimiento para su preparacion
US4831031A (en) * 1988-01-22 1989-05-16 Pfizer Inc. Aryl piperazinyl-(C2 or C4) alkylene heterocyclic compounds having neuroleptic activity
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
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
JP3102896B2 (ja) 1996-05-07 2000-10-23 ファイザー インク. 5―(2―(4―(1,2―ベンズイソチアゾール―3―イル)―1―ピペラジニル)エチル)―6―クロロ―1,3―ジヒドロ―2(1h)―インドール―2―オン(=ジプラシドン)のメシレート三水和物、その調製法およびドーパミンd2アンタゴニストとしてのその使用

Patent Citations (1)

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

Also Published As

Publication number Publication date
NZ332218A (en) 2005-02-25
NO312514B1 (no) 2002-05-21
CN1216991A (zh) 1999-05-19
EA001190B1 (ru) 2000-12-25
ID16867A (id) 1997-11-20
NO985194D0 (no) 1998-11-06
DZ2222A1 (fr) 2002-12-03
WO1997042191A1 (en) 1997-11-13
IS4874A (is) 1998-10-20
CN1091769C (zh) 2002-10-02
TW491847B (en) 2002-06-21
MA24171A1 (fr) 1997-12-31
BG102892A (en) 1999-09-30
TNSN97074A1 (fr) 2005-03-15
JP3494659B2 (ja) 2004-02-09
CZ349398A3 (cs) 1999-09-15
IL126591A (en) 2001-11-25
ES2229342T3 (es) 2005-04-16
DK0918772T3 (da) 2005-01-10
BG63544B1 (bg) 2002-04-30
TR199802240T2 (cg-RX-API-DMAC10.html) 1999-02-22
KR100333215B1 (ko) 2002-06-20
EP0918772B1 (en) 2004-10-06
SK150898A3 (en) 2000-02-14
HRP970236A2 (en) 1998-06-30
CO4940466A1 (es) 2000-07-24
AP765A (en) 1999-09-17
DE69731094T2 (de) 2006-02-23
EG24076A (en) 2008-05-11
MY119997A (en) 2005-08-30
EP0918772A1 (en) 1999-06-02
JPH11509867A (ja) 1999-08-31
CA2252898A1 (en) 1997-11-13
IL126591A0 (en) 1999-08-17
US6245765B1 (en) 2001-06-12
GT199700052A (es) 2001-08-29
SK282837B6 (sk) 2002-12-03
DE69731094D1 (de) 2004-11-11
ZA973876B (en) 1998-11-06
PT918772E (pt) 2004-12-31
PL329884A1 (en) 1999-04-12
PL188330B1 (pl) 2005-01-31
AR007004A1 (es) 1999-10-13
ATE278689T1 (de) 2004-10-15
NO985194L (no) 1998-11-06
AP9700976A0 (en) 1997-07-31
CZ289215B6 (cs) 2001-12-12
HK1017892A1 (en) 1999-12-03
HRP970236B1 (en) 2002-12-31
UA46840C2 (uk) 2002-06-17
KR20000010824A (ko) 2000-02-25
AU2174797A (en) 1997-11-26
SI0918772T1 (en) 2005-02-28
BR9709889A (pt) 1999-08-10
IS2080B (is) 2006-02-15
EA199800912A1 (ru) 1999-04-29
OA10909A (en) 2001-10-26
CA2252898C (en) 2003-04-08

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