KR100333215B1 - 5-(2-(4-(1,2-벤즈이소티아졸-3-일)-1-피페라지닐)-에틸)-6-클로로-1,3-디하이드로-2(1에이치)-인돌-2-온(지프라시돈)의메실레이트디하이드레이트염,이의제조방법및도파민디2길항물질로서의이의용도 - Google Patents

5-(2-(4-(1,2-벤즈이소티아졸-3-일)-1-피페라지닐)-에틸)-6-클로로-1,3-디하이드로-2(1에이치)-인돌-2-온(지프라시돈)의메실레이트디하이드레이트염,이의제조방법및도파민디2길항물질로서의이의용도 Download PDF

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Publication number
KR100333215B1
KR100333215B1 KR1019980708960A KR19980708960A KR100333215B1 KR 100333215 B1 KR100333215 B1 KR 100333215B1 KR 1019980708960 A KR1019980708960 A KR 1019980708960A KR 19980708960 A KR19980708960 A KR 19980708960A KR 100333215 B1 KR100333215 B1 KR 100333215B1
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South Korea
Prior art keywords
ziprasidone
benzisothiazol
piperazinyl
dihydro
chloro
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Korean (ko)
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KR20000010824A (ko
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프랑크 로버트 부쉬
캐롤 앤 로즈
러쎌 제임스 신
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디. 제이. 우드, 스피겔 알렌 제이
화이자 인코포레이티드
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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)
  • Pain & Pain Management (AREA)
  • Psychiatry (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)
KR1019980708960A 1996-05-07 1997-04-10 5-(2-(4-(1,2-벤즈이소티아졸-3-일)-1-피페라지닐)-에틸)-6-클로로-1,3-디하이드로-2(1에이치)-인돌-2-온(지프라시돈)의메실레이트디하이드레이트염,이의제조방법및도파민디2길항물질로서의이의용도 Expired - Fee Related KR100333215B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US1675796P 1996-05-07 1996-05-07
US60/016,757 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
KR20000010824A KR20000010824A (ko) 2000-02-25
KR100333215B1 true KR100333215B1 (ko) 2002-06-20

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KR1019980708960A Expired - Fee Related KR100333215B1 (ko) 1996-05-07 1997-04-10 5-(2-(4-(1,2-벤즈이소티아졸-3-일)-1-피페라지닐)-에틸)-6-클로로-1,3-디하이드로-2(1에이치)-인돌-2-온(지프라시돈)의메실레이트디하이드레이트염,이의제조방법및도파민디2길항물질로서의이의용도

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

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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
EP1698338B1 (en) * 2000-06-02 2008-04-09 Pfizer Products Inc. S-methyl-dihydro-ziprasidone for the treatment of schizophrenia
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
WO2005016325A2 (en) * 2003-06-03 2005-02-24 Teva Pharmaceutical Industries Ltd. CRISTALLINE ZIPRASIDONE HCl AND PROCESSES FOR PREPARATION THEREOF
US7667037B2 (en) 2003-10-24 2010-02-23 Teva Pharmaceutical Industries Ltd. Processes for preparation of ziprasidone
MXPA06013163A (es) * 2004-05-11 2007-02-13 Pfizer Prod Inc Combinacion de antipsicoticos atipicos y antagonistas del 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
CN101106972A (zh) * 2004-11-16 2008-01-16 伊兰制药国际有限公司 注射用纳米微粒奥氮平制剂
WO2006086787A1 (en) * 2005-02-11 2006-08-17 Teva Pharmaceutical Industries Ltd. Process of preparing ziprasidone mesylate
US20070032511A1 (en) * 2005-02-11 2007-02-08 Judith Aronhime Amorphous ziprasidone mesylate
EP1855651A4 (en) * 2005-03-03 2011-06-15 Elan Pharma Int Ltd NANOPARTICLE COMPOSITIONS OF HETEROCYCLIC AMID 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
US20060270685A1 (en) * 2005-03-14 2006-11-30 Judith Aronhime Anhydrous ziprasidone mesylate and a process for its preparation
WO2006098834A2 (en) * 2005-03-14 2006-09-21 Teva Pharmaceutical Industries Ltd. Crystalline forms of ziprasidone mesylate
ITMI20052216A1 (it) * 2005-11-18 2007-05-19 Dipharma Spa Procedimento per la preparazione di ziprasidone
US20080286373A1 (en) * 2007-05-18 2008-11-20 Palepu Nageswara R Ziprasidone formulations
CA2727573A1 (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
US20140206667A1 (en) 2012-11-14 2014-07-24 Michela Gallagher Methods and compositions for treating schizophrenia

Family Cites Families (6)

* Cited by examiner, † Cited by third party
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
US5206366A (en) 1992-08-26 1993-04-27 Pfizer Inc. Process for preparing aryl piperazinyl-heterocyclic compounds
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
DK0904273T3 (da) 1996-05-07 2003-07-07 Pfizer Mesylat-trihydratsalt af 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl-6-chlor-1,3-dihydro-2(1H)-indol-2-on(=ziprasidon), dets fremstilling og dets anvendelse som dipamin D2 antagonist

Also Published As

Publication number Publication date
EA199800912A1 (ru) 1999-04-29
TNSN97074A1 (fr) 2005-03-15
BG102892A (en) 1999-09-30
CN1216991A (zh) 1999-05-19
SI0918772T1 (en) 2005-02-28
AU731267B2 (en) 2001-03-29
IL126591A (en) 2001-11-25
AU2174797A (en) 1997-11-26
MA24171A1 (fr) 1997-12-31
HK1017892A1 (en) 1999-12-03
SK282837B6 (sk) 2002-12-03
CA2252898C (en) 2003-04-08
IS2080B (is) 2006-02-15
AP765A (en) 1999-09-17
BR9709889A (pt) 1999-08-10
CO4940466A1 (es) 2000-07-24
BG63544B1 (bg) 2002-04-30
AR007004A1 (es) 1999-10-13
AP9700976A0 (en) 1997-07-31
CN1091769C (zh) 2002-10-02
EG24076A (en) 2008-05-11
SK150898A3 (en) 2000-02-14
DE69731094T2 (de) 2006-02-23
ZA973876B (en) 1998-11-06
JPH11509867A (ja) 1999-08-31
DZ2222A1 (fr) 2002-12-03
IS4874A (is) 1998-10-20
MY119997A (en) 2005-08-30
ID16867A (id) 1997-11-20
GT199700052A (es) 2001-08-29
DK0918772T3 (da) 2005-01-10
PT918772E (pt) 2004-12-31
NO985194D0 (no) 1998-11-06
PL329884A1 (en) 1999-04-12
US6245765B1 (en) 2001-06-12
NO985194L (no) 1998-11-06
NZ332218A (en) 2005-02-25
OA10909A (en) 2001-10-26
CZ289215B6 (cs) 2001-12-12
HRP970236A2 (en) 1998-06-30
WO1997042191A1 (en) 1997-11-13
HRP970236B1 (en) 2002-12-31
TW491847B (en) 2002-06-21
JP3494659B2 (ja) 2004-02-09
CZ349398A3 (cs) 1999-09-15
ES2229342T3 (es) 2005-04-16
EP0918772A1 (en) 1999-06-02
PL188330B1 (pl) 2005-01-31
NO312514B1 (no) 2002-05-21
IL126591A0 (en) 1999-08-17
KR20000010824A (ko) 2000-02-25
TR199802240T2 (https=) 1999-02-22
DE69731094D1 (de) 2004-11-11
EP0918772B1 (en) 2004-10-06
ATE278689T1 (de) 2004-10-15
CA2252898A1 (en) 1997-11-13
UA46840C2 (uk) 2002-06-17
EA001190B1 (ru) 2000-12-25

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St.27 status event code: A-5-5-R10-R18-oth-X000