BG63544B1 - Дихидратни соли на 5-(2-(4-(1,2-бензизотиазол-3- ил)-1-пиперазинил)-етил)-6-хлоро-1,3-дихидро-2(1н)-индол- 2-он (= ципразидон), мезилат, получаванетоим и използуването им като антагонист на допаминd2 - Google Patents

Дихидратни соли на 5-(2-(4-(1,2-бензизотиазол-3- ил)-1-пиперазинил)-етил)-6-хлоро-1,3-дихидро-2(1н)-индол- 2-он (= ципразидон), мезилат, получаванетоим и използуването им като антагонист на допаминd2 Download PDF

Info

Publication number: BG63544B1
Authority: BG; Bulgaria
Prior art keywords: common; mesylate; benzisothiazol; chloro; ethyl
Prior art date: 1996-05-07

Application number

BG102892A

Other languages

Bulgarian (bg)

English (en)

Other versions

BG102892A (en

Inventor

Frank BUSCH

Carol ROSE

Russell SHINE

Original Assignee

Pfizer Inc.

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.)

1996-05-07

Filing date

1998-11-03

Publication date

2002-04-30

1998-11-03 Application filed by Pfizer Inc. filed Critical Pfizer Inc.

1999-09-30 Publication of BG102892A publication Critical patent/BG102892A/xx

2002-04-30 Publication of BG63544B1 publication Critical patent/BG63544B1/bg

Links

AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 title abstract description 37
150000003839 salts Chemical class 0.000 title abstract 2
238000002360 preparation method Methods 0.000 title description 3
229940127333 Dopamine D2 Antagonists Drugs 0.000 title 1
208000028017 Psychotic disease Diseases 0.000 claims abstract description 12
238000000034 method Methods 0.000 claims abstract description 9
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 5
239000013078 crystal Substances 0.000 claims description 39
-1 2- (4- (1,2-benzisothiazol-3-yl) -1-piperazinyl) -ethyl Chemical group 0.000 claims description 19
201000000980 schizophrenia Diseases 0.000 claims description 5
241000124008 Mammalia Species 0.000 claims description 4
208000019695 Migraine disease Diseases 0.000 claims description 4
239000003937 drug carrier Substances 0.000 claims description 4
238000002347 injection Methods 0.000 claims description 4
239000007924 injection Substances 0.000 claims description 4
206010027599 migraine Diseases 0.000 claims description 4
238000007911 parenteral administration Methods 0.000 claims description 4
150000001875 compounds Chemical class 0.000 claims 4
210000003205 muscle Anatomy 0.000 claims 1
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 23
UAAKJEVCDBPTQS-UHFFFAOYSA-N methanesulfonic acid;dihydrate Chemical class O.O.CS(O)(=O)=O UAAKJEVCDBPTQS-UHFFFAOYSA-N 0.000 description 22
WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 16
239000011541 reaction mixture Substances 0.000 description 16
238000003756 stirring Methods 0.000 description 14
239000000243 solution Substances 0.000 description 12
239000000725 suspension Substances 0.000 description 12
229940098779 methanesulfonic acid Drugs 0.000 description 10
239000000523 sample Substances 0.000 description 9
238000002441 X-ray diffraction Methods 0.000 description 8
238000004128 high performance liquid chromatography Methods 0.000 description 8
239000000203 mixture Substances 0.000 description 8
150000004683 dihydrates Chemical class 0.000 description 7
238000001914 filtration Methods 0.000 description 7
238000010438 heat treatment Methods 0.000 description 7
239000000843 powder Substances 0.000 description 7
238000010992 reflux Methods 0.000 description 7
YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 7
DKAGJZJALZXOOV-UHFFFAOYSA-N hydrate;hydrochloride Chemical compound O.Cl DKAGJZJALZXOOV-UHFFFAOYSA-N 0.000 description 5
238000002156 mixing Methods 0.000 description 5
238000001228 spectrum Methods 0.000 description 5
KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 4
239000002552 dosage form Substances 0.000 description 4
239000012458 free base Substances 0.000 description 4
239000007787 solid Substances 0.000 description 4
LOQSYPGSAZUDJZ-UHFFFAOYSA-N 5-[2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl]-6-chloro-1,3-dihydroindol-2-one;methanesulfonic acid Chemical class CS(O)(=O)=O.C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CC(=O)NC=4C=C3Cl)=NSC2=C1 LOQSYPGSAZUDJZ-UHFFFAOYSA-N 0.000 description 3
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 3
229910052782 aluminium Inorganic materials 0.000 description 3
238000006243 chemical reaction Methods 0.000 description 3
239000011888 foil Substances 0.000 description 3
238000000634 powder X-ray diffraction Methods 0.000 description 3
150000004684 trihydrates Chemical class 0.000 description 3
MVWVFYHBGMAFLY-UHFFFAOYSA-N ziprasidone Chemical compound C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CC(=O)NC=4C=C3Cl)=NSC2=C1 MVWVFYHBGMAFLY-UHFFFAOYSA-N 0.000 description 3
ANMYWYIICWTDRR-UHFFFAOYSA-N 5-[2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl]-6-chloro-1,3-dihydroindol-2-one dihydrate Chemical compound O.O.C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CC(=O)NC=4C=C3Cl)=NSC2=C1 ANMYWYIICWTDRR-UHFFFAOYSA-N 0.000 description 2
229920000858 Cyclodextrin Polymers 0.000 description 2
239000001116 FEMA 4028 Substances 0.000 description 2
235000011175 beta-cyclodextrine Nutrition 0.000 description 2
229960004853 betadex Drugs 0.000 description 2
230000015572 biosynthetic process Effects 0.000 description 2
238000012512 characterization method Methods 0.000 description 2
238000001816 cooling Methods 0.000 description 2
210000003298 dental enamel Anatomy 0.000 description 2
239000003085 diluting agent Substances 0.000 description 2
238000001035 drying Methods 0.000 description 2
239000011521 glass Substances 0.000 description 2
238000010255 intramuscular injection Methods 0.000 description 2
239000007927 intramuscular injection Substances 0.000 description 2
230000014759 maintenance of location Effects 0.000 description 2
238000004519 manufacturing process Methods 0.000 description 2
238000001000 micrograph Methods 0.000 description 2
239000003960 organic solvent Substances 0.000 description 2
230000001698 pyrogenic effect Effects 0.000 description 2
239000002002 slurry Substances 0.000 description 2
239000008223 sterile water Substances 0.000 description 2
239000008227 sterile water for injection Substances 0.000 description 2
YPBPQOBJZVGEGA-UHFFFAOYSA-N 3-[4-[2-(6-chloro-2,3-dihydro-1h-indol-5-yl)ethyl]piperazin-1-yl]-1,2-benzothiazole Chemical compound C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CCNC=4C=C3Cl)=NSC2=C1 YPBPQOBJZVGEGA-UHFFFAOYSA-N 0.000 description 1
MCSXGCZMEPXKIW-UHFFFAOYSA-N 3-hydroxy-4-[(4-methyl-2-nitrophenyl)diazenyl]-N-(3-nitrophenyl)naphthalene-2-carboxamide Chemical compound Cc1ccc(N=Nc2c(O)c(cc3ccccc23)C(=O)Nc2cccc(c2)[N+]([O-])=O)c(c1)[N+]([O-])=O MCSXGCZMEPXKIW-UHFFFAOYSA-N 0.000 description 1
RGWUAFQDKPPEDI-UHFFFAOYSA-N 5-[2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl]-6-chloro-1,3-dihydroindol-2-one trihydrate Chemical compound O.O.O.Clc1cc2NC(=O)Cc2cc1CCN1CCN(CC1)c1nsc2ccccc12 RGWUAFQDKPPEDI-UHFFFAOYSA-N 0.000 description 1
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
239000007836 KH2PO4 Substances 0.000 description 1
239000004677 Nylon Substances 0.000 description 1
239000004480 active ingredient Substances 0.000 description 1
239000000164 antipsychotic agent Substances 0.000 description 1
239000012736 aqueous medium Substances 0.000 description 1
239000007864 aqueous solution Substances 0.000 description 1
WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 description 1
239000002775 capsule Substances 0.000 description 1
239000007963 capsule composition Substances 0.000 description 1
239000003153 chemical reaction reagent Substances 0.000 description 1
239000003795 chemical substances by application Substances 0.000 description 1
230000002860 competitive effect Effects 0.000 description 1
238000002425 crystallisation Methods 0.000 description 1
230000008025 crystallization Effects 0.000 description 1
238000001514 detection method Methods 0.000 description 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
208000035475 disorder Diseases 0.000 description 1
238000006073 displacement reaction Methods 0.000 description 1
239000000945 filler Substances 0.000 description 1
229910052736 halogen Inorganic materials 0.000 description 1
150000002367 halogens Chemical class 0.000 description 1
LKGCPYOBWLSCTK-UHFFFAOYSA-N methanesulfonic acid;trihydrate Chemical compound O.O.O.CS(O)(=O)=O LKGCPYOBWLSCTK-UHFFFAOYSA-N 0.000 description 1
125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 description 1
150000004682 monohydrates Chemical class 0.000 description 1
229910000402 monopotassium phosphate Inorganic materials 0.000 description 1
235000019796 monopotassium phosphate Nutrition 0.000 description 1
229920001778 nylon Polymers 0.000 description 1
239000008012 organic excipient Substances 0.000 description 1
GNSKLFRGEWLPPA-UHFFFAOYSA-M potassium dihydrogen phosphate Chemical compound [K+].OP(O)([O-])=O GNSKLFRGEWLPPA-UHFFFAOYSA-M 0.000 description 1
230000003389 potentiating effect Effects 0.000 description 1
238000010298 pulverizing process Methods 0.000 description 1
238000000746 purification Methods 0.000 description 1
239000010802 sludge Substances 0.000 description 1
239000002904 solvent Substances 0.000 description 1
239000007916 tablet composition Substances 0.000 description 1
238000005292 vacuum distillation Methods 0.000 description 1
238000010792 warming Methods 0.000 description 1
238000005406 washing Methods 0.000 description 1

Classifications

- 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

Landscapes

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)

BG102892A 1996-05-07 1998-11-03 Дихидратни соли на 5-(2-(4-(1,2-бензизотиазол-3- ил)-1-пиперазинил)-етил)-6-хлоро-1,3-дихидро-2(1н)-индол- 2-он (= ципразидон), мезилат, получаванетоим и използуването им като антагонист на допаминd2 BG63544B1 (bg)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US1675796P	1996-05-07	1996-05-07
PCT/IB1997/000393 WO1997042191A1 (fr)	1996-05-07	1997-04-10	Dihydrate de sels mesylates de 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2(ih)-indol-2-one (=ziprasidone), leur preparation et leur utilisation en tant qu'antagonistes du recepteur dopaminergique d2

Publications (2)

Publication Number	Publication Date
BG102892A BG102892A (en)	1999-09-30
BG63544B1 true BG63544B1 (bg)	2002-04-30

Family

ID=21778804

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
BG102892A BG63544B1 (bg)	1996-05-07	1998-11-03	Дихидратни соли на 5-(2-(4-(1,2-бензизотиазол-3- ил)-1-пиперазинил)-етил)-6-хлоро-1,3-дихидро-2(1н)-индол- 2-он (= ципразидон), мезилат, получаванетоим и използуването им като антагонист на допаминd2

Country Status (40)

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

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
DE60124791T2 (de) *	2000-06-02	2007-09-13	Pfizer Products Inc., Groton	S-Methyl-Dihydro-Ziprasidone zur Behandlung von psychiatrischen Störungen.
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
CN1791430A (zh) *	2003-05-16	2006-06-21	辉瑞产品公司	非典型抗精神病药物和gaba调节剂、抗惊厥药物或苯并二氮杂䓬类的治疗性组合
WO2005035531A1 (fr) *	2003-06-03	2005-04-21	Teva Paharmaceutical Industries Ltd.	Formes polymorphes de ziprasidone chlorhydrate et procedes pour leur elaboration
US7667037B2 (en)	2003-10-24	2010-02-23	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 (fr)	2004-05-14	2010-08-24	Apotex Pharmachem Inc.	Nouveau chlorhydrate de ziprasidone amorphe (chlorhydrate de 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydr o-2h-indol-2-one) et procedes pour sa production
CA2471219A1 (fr)	2004-06-14	2005-12-14	Apotex Pharmachem Inc.	Preparation amelioree d'une forme anhydre du chlorhydrate de 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2h-indol-2-one (chlorhydrate de ziprasidone)
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
US20070032511A1 (en) *	2005-02-11	2007-02-08	Judith Aronhime	Amorphous ziprasidone mesylate
WO2006086787A1 (fr) *	2005-02-11	2006-08-17	Teva Pharmaceutical Industries Ltd.	Procede de preparation de ziprasidone mesylate
EP1855651A4 (fr) *	2005-03-03	2011-06-15	Elan Pharma Int Ltd	Compositions nanoparticulaires de derives d'amide heterocyclique
ITMI20050346A1 (it)	2005-03-07	2006-09-08	Dipharma Spa	Forma solida di ziprasidone cloridrato
CA2500667C (fr)	2005-03-11	2013-01-15	Apotex Pharmachem Inc.	Synthese de sels d'addition acide de ziprasidone et de produits intermediaires connexes au moyen de reactions solide-gaz
US20060270685A1 (en) *	2005-03-14	2006-11-30	Judith Aronhime	Anhydrous ziprasidone mesylate and a process for its preparation
EP1858891A2 (fr) *	2005-03-14	2007-11-28	Teva Pharmaceutical Industries Ltd.	Formes cristallines de mesylate de ziprasidone
ITMI20052216A1 (it) *	2005-11-18	2007-05-19	Dipharma Spa	Procedimento per la preparazione di ziprasidone
JP2010527925A (ja) *	2007-05-18	2010-08-19	サイドース・エルエルシー	ジプラシドン製剤
WO2009156889A1 (fr) *	2008-06-25	2009-12-30	Pfizer Inc.	Composés diaryle et leurs utilisations
WO2012053654A1 (fr) *	2010-10-18	2012-04-26	Dainippon Sumitomo Pharma Co., Ltd.	Formulation à libération prolongée pour 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
EP3610890A1 (fr)	2012-11-14	2020-02-19	The Johns Hopkins University	Procédés et compositions de traitement de la schizophrénie

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
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
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

1997
- 1997-04-01 TW TW086104173A patent/TW491847B/zh not_active IP Right Cessation
- 1997-04-10 WO PCT/IB1997/000393 patent/WO1997042191A1/fr not_active Ceased
- 1997-04-10 AU AU21747/97A patent/AU731267B2/en not_active Ceased
- 1997-04-10 DK DK97914520T patent/DK0918772T3/da active
- 1997-04-10 UA UA98115905A patent/UA46840C2/uk unknown
- 1997-04-10 CN CN97194244A patent/CN1091769C/zh not_active Expired - Fee Related
- 1997-04-10 CA CA002252898A patent/CA2252898C/fr not_active Expired - Lifetime
- 1997-04-10 PT PT97914520T patent/PT918772E/pt unknown
- 1997-04-10 CZ CZ19983493A patent/CZ289215B6/cs not_active IP Right Cessation
- 1997-04-10 ES ES97914520T patent/ES2229342T3/es not_active Expired - Lifetime
- 1997-04-10 SK SK1508-98A patent/SK282837B6/sk not_active IP Right Cessation
- 1997-04-10 SI SI9730676T patent/SI0918772T1/xx unknown
- 1997-04-10 BR BR9709889A patent/BR9709889A/pt not_active Application Discontinuation
- 1997-04-10 JP JP53967297A patent/JP3494659B2/ja not_active Expired - Lifetime
- 1997-04-10 EA EA199800912A patent/EA001190B1/ru not_active IP Right Cessation
- 1997-04-10 AT AT97914520T patent/ATE278689T1/de not_active IP Right Cessation
- 1997-04-10 US US09/180,455 patent/US6245765B1/en not_active Expired - Lifetime
- 1997-04-10 TR TR1998/02240T patent/TR199802240T2/xx unknown
- 1997-04-10 PL PL97329884A patent/PL188330B1/pl unknown
- 1997-04-10 KR KR1019980708960A patent/KR100333215B1/ko not_active Expired - Fee Related
- 1997-04-10 IL IL12659197A patent/IL126591A/en not_active IP Right Cessation
- 1997-04-10 NZ NZ332218A patent/NZ332218A/en unknown
- 1997-04-10 DE DE69731094T patent/DE69731094T2/de not_active Expired - Lifetime
- 1997-04-10 EP EP97914520A patent/EP0918772B1/fr not_active Expired - Lifetime
- 1997-04-29 GT GT199700052A patent/GT199700052A/es unknown
- 1997-04-29 CO CO97022872A patent/CO4940466A1/es unknown
- 1997-04-30 AP APAP/P/1997/000976A patent/AP765A/en active
- 1997-05-04 EG EG37997A patent/EG24076A/xx active
- 1997-05-05 ID IDP971492A patent/ID16867A/id unknown
- 1997-05-05 AR ARP970101856A patent/AR007004A1/es unknown
- 1997-05-06 ZA ZA973876A patent/ZA973876B/xx unknown
- 1997-05-06 DZ DZ970069A patent/DZ2222A1/fr active
- 1997-05-06 MA MA24595A patent/MA24171A1/fr unknown
- 1997-05-06 TN TNTNSN97074A patent/TNSN97074A1/fr unknown
- 1997-05-06 MY MYPI97001989A patent/MY119997A/en unknown
- 1997-05-07 HR HR970236A patent/HRP970236B1/xx not_active IP Right Cessation
1998
- 1998-10-20 IS IS4874A patent/IS2080B/is unknown
- 1998-10-30 OA OA9800206A patent/OA10909A/fr unknown
- 1998-11-03 BG BG102892A patent/BG63544B1/bg unknown
- 1998-11-06 NO NO19985194A patent/NO312514B1/no unknown

Also Published As

Publication number	Publication date
HRP970236B1 (en)	2002-12-31
DK0918772T3 (da)	2005-01-10
EA001190B1 (ru)	2000-12-25
BG102892A (en)	1999-09-30
NO312514B1 (no)	2002-05-21
NO985194D0 (no)	1998-11-06
EP0918772B1 (fr)	2004-10-06
PT918772E (pt)	2004-12-31
EA199800912A1 (ru)	1999-04-29
PL329884A1 (en)	1999-04-12
CA2252898C (fr)	2003-04-08
JPH11509867A (ja)	1999-08-31
JP3494659B2 (ja)	2004-02-09
CN1091769C (zh)	2002-10-02
OA10909A (en)	2001-10-26
TNSN97074A1 (fr)	2005-03-15
WO1997042191A1 (fr)	1997-11-13
HK1017892A1 (en)	1999-12-03
ID16867A (id)	1997-11-20
AR007004A1 (es)	1999-10-13
TW491847B (en)	2002-06-21
US6245765B1 (en)	2001-06-12
HRP970236A2 (en)	1998-06-30
DE69731094D1 (de)	2004-11-11
TR199802240T2 (fr)	1999-02-22
DE69731094T2 (de)	2006-02-23
EP0918772A1 (fr)	1999-06-02
MA24171A1 (fr)	1997-12-31
ES2229342T3 (es)	2005-04-16
CZ349398A3 (cs)	1999-09-15
SK282837B6 (sk)	2002-12-03
AP765A (en)	1999-09-17
ATE278689T1 (de)	2004-10-15
CO4940466A1 (es)	2000-07-24
MY119997A (en)	2005-08-30
AU2174797A (en)	1997-11-26
IL126591A0 (en)	1999-08-17
AU731267B2 (en)	2001-03-29
SK150898A3 (en)	2000-02-14
NO985194L (no)	1998-11-06
CA2252898A1 (fr)	1997-11-13
KR20000010824A (ko)	2000-02-25
KR100333215B1 (ko)	2002-06-20
IS4874A (is)	1998-10-20
UA46840C2 (uk)	2002-06-17
AP9700976A0 (en)	1997-07-31
DZ2222A1 (fr)	2002-12-03
ZA973876B (en)	1998-11-06
CN1216991A (zh)	1999-05-19
PL188330B1 (pl)	2005-01-31
BR9709889A (pt)	1999-08-10
SI0918772T1 (en)	2005-02-28
IS2080B (is)	2006-02-15
NZ332218A (en)	2005-02-25
GT199700052A (es)	2001-08-29
IL126591A (en)	2001-11-25
CZ289215B6 (cs)	2001-12-12
EG24076A (en)	2008-05-11

Publication	Publication Date	Title
BG63544B1 (bg)	2002-04-30	Дихидратни соли на 5-(2-(4-(1,2-бензизотиазол-3- ил)-1-пиперазинил)-етил)-6-хлоро-1,3-дихидро-2(1н)-индол- 2-он (= ципразидон), мезилат, получаванетоим и използуването им като антагонист на допаминd2
AP838A (en)	2000-05-03	Mesylate trihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-y1)-1-piperaziny1)-ethy1) -6-chloro-1,3-dihydro-2h-indol-2-one.
KR0163186B1 (ko)	1998-12-01	(1,2,3,4-테트라하이드로-9-아크리딘이미노)사이클로헥산 카복실산 및 관련 화합물, 이들의 제조방법 및 약제로서의 용도
PL185709B1 (pl)	2003-07-31	Nowy monohydrat polimorfu II 6-N-(L-Ala-L-Ala)-trowafloksacyny i środek farmaceutyczny
MXPA98009242A (en)	1999-09-01	Salt mesylate trihydrate 5 - (- 2- (4- (1,2-benzoisotiazol-3-il) -1-piperazinil) ethyl) -6-chlorine-1,3-dihydro-2h-indol-2-
HUP9902404A2 (hu)	2000-02-28	5-(2-(4-(1,2-Benzizotiazol-3-il)-1-piperazinil)-etil)-6-klór-1,3-dihidro-2-(2H)-indol-2-on (ziprazidon) mezilát-dihidrát sói, a vegyületek előállitása és dopamin D2 antagonistaként történő alkalmazása
NZ508304A (en)	2001-05-25	Mesylate dihydrate 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 dopamine D2 antagonist