JP2008526839A - １１−ピペラジン−１−イルジベンゾ［ｂ，ｆ］［１，４］チアゼピン又はその薬学的に許容される塩の新規な使用及び経口医薬組成物への新規な使用 - Google Patents

１１−ピペラジン−１−イルジベンゾ［ｂ，ｆ］［１，４］チアゼピン又はその薬学的に許容される塩の新規な使用及び経口医薬組成物への新規な使用 Download PDF

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Publication number: JP2008526839A
Authority: JP; Japan
Prior art keywords: disorder; composition; disorders; pharmaceutically acceptable; related disorders
Prior art date: 2005-01-07
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.): Pending

Application number

JP2007550327A

Other languages

English (en)

Japanese (ja)

Other versions

JP2008526839A5 (fr

Inventor

パトリシア・シー・デイヴィス

ジェフリー・エム・ゴールドスタイン

スコット・ダブルュー・グリム

レイモンド・エフ・サッコウ

ヘレン・アール・ウィンター

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

AstraZeneca AB

Original Assignee

AstraZeneca AB

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.)

2005-01-07

Filing date

2006-01-04

Publication date

2008-07-24

2006-01-04 Application filed by AstraZeneca AB filed Critical AstraZeneca AB

2008-07-24 Publication of JP2008526839A publication Critical patent/JP2008526839A/ja

2009-02-26 Publication of JP2008526839A5 publication Critical patent/JP2008526839A5/ja

Status Pending legal-status Critical Current

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- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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JP2007550327A 2005-01-07 2006-01-04 １１−ピペラジン−１−イルジベンゾ［ｂ，ｆ］［１，４］チアゼピン又はその薬学的に許容される塩の新規な使用及び経口医薬組成物への新規な使用 Pending JP2008526839A (ja)

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US64226205P	2005-01-07	2005-01-07
US73788705P	2005-11-18	2005-11-18
US73786405P	2005-11-18	2005-11-18
US73786505P	2005-11-18	2005-11-18
PCT/SE2006/000009 WO2006073360A1 (fr)	2005-01-07	2006-01-04	Nouvelle utilisation de 11-piperazine-1-yldibenzo [b,f] [1,4] thiazepine ou de son sel pharmaceutiquement acceptable et compositions pharmaceutiques orales

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EP (1)	EP1838325A1 (fr)
JP (1)	JP2008526839A (fr)
AR (1)	AR052191A1 (fr)
TW (1)	TW200640466A (fr)
UY (1)	UY29326A1 (fr)
WO (1)	WO2006073360A1 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
WO2007062339A2 (fr) *	2005-11-18	2007-05-31	Astrazeneca Ab	Formulations liquides
MX2010014203A (es)	2008-06-20	2011-02-22	Astrazeneca Ab	Derivados de dibenzotiazepina y sus usos - 424.
WO2010085976A1 (fr) *	2009-01-30	2010-08-05	F.I.S. Fabbrica Italiana Sintetici S.P.A.	Procédé pour la synthèse de quétiapine

Citations (4)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US3539573A (en) *	1967-03-22	1970-11-10	Jean Schmutz	11-basic substituted dibenzodiazepines and dibenzothiazepines
JPS638378A (ja) *	1986-03-27	1988-01-14	アイ・シ−・アイ・アメリカス・インコ−ポレイテツド	ジベンゾチアゼピン化合物、その製造法、ならびに該化合物を含有する、抗精神作用および神経弛緩作用を有する製薬学的組成物
JP2006518324A (ja) *	2003-02-21	2006-08-10	ピーピージー・インダストリーズ・オハイオ・インコーポレイテッド	透過色ずれが減少されている着色ガラス組成物及び自動車用視野パネル
JP2007534656A (ja) *	2003-12-22	2007-11-29	アカディアファーマシューティカルズ，インコーポレーテッド	ムスカリンアゴニストとしてのアミノ置換ジアリール［ａ，ｄ］シクロヘプテン類似体および精神神経疾患の治療方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5602124A (en) *	1994-12-12	1997-02-11	Allelix Biopharmaceuticals, Inc.	5-HT2 receptor ligands
SE0003126D0 (sv) *	2000-09-05	2000-09-05	Astrazeneca Ab	Method of treatment
ATE360425T1 (de) *	2001-02-06	2007-05-15	Astrazeneca Ab	Verwendung von quetiapin für die behandlung von kokain-abhängigkeit
WO2004034996A2 (fr) *	2002-10-18	2004-04-29	Massachusetts Mental Health Institute	Traitement de l'abus d'alcool et/ou de substances par antagonisme vis-a-vis des recepteurs alpha2-adrenergiques avec fabile blocage de la dopamine
ES2349091T3 (es) *	2003-07-02	2010-12-27	Astrazeneca Ab	Metabolito de quetiapina.
WO2005053619A2 (fr) *	2003-12-04	2005-06-16	The Research Foundation Of The City University Of New York	Effets de la clozapine et de la cocaine sur la liberation de dopamine et de serotonine dans le noyau accumbens pendant un comportement psychostimulant et sevrage
US20050171088A1 (en) *	2004-01-30	2005-08-04	Astrazeneca Ab	Treatment of psychoses with dibenzothiazepine antipsychotic

2006
- 2006-01-04 WO PCT/SE2006/000009 patent/WO2006073360A1/fr not_active Ceased
- 2006-01-04 EP EP06700349A patent/EP1838325A1/fr not_active Withdrawn
- 2006-01-04 JP JP2007550327A patent/JP2008526839A/ja active Pending
- 2006-01-05 UY UY29326A patent/UY29326A1/es not_active Application Discontinuation
- 2006-01-06 AR ARP060100058A patent/AR052191A1/es not_active Application Discontinuation
- 2006-01-06 TW TW095100687A patent/TW200640466A/zh unknown

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US3539573A (en) *	1967-03-22	1970-11-10	Jean Schmutz	11-basic substituted dibenzodiazepines and dibenzothiazepines
JPS638378A (ja) *	1986-03-27	1988-01-14	アイ・シ−・アイ・アメリカス・インコ−ポレイテツド	ジベンゾチアゼピン化合物、その製造法、ならびに該化合物を含有する、抗精神作用および神経弛緩作用を有する製薬学的組成物
JP2006518324A (ja) *	2003-02-21	2006-08-10	ピーピージー・インダストリーズ・オハイオ・インコーポレイテッド	透過色ずれが減少されている着色ガラス組成物及び自動車用視野パネル
JP2007534656A (ja) *	2003-12-22	2007-11-29	アカディアファーマシューティカルズ，インコーポレーテッド	ムスカリンアゴニストとしてのアミノ置換ジアリール［ａ，ｄ］シクロヘプテン類似体および精神神経疾患の治療方法

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
HASSELSTROM J ET AL, J CHROMATGR B, vol. 798, JPN6012011562, 2003, pages 9 - 16, ISSN: 0002163717 *
SATTAR SP ET AL, J PSYCHIATRY NEUROSCI, vol. 29, no. 6, JPN6012011563, 2004, pages 452 - 7, ISSN: 0002163718 *
最新創薬化学上巻, JPN6012011560, 2001, pages 96 - 103, ISSN: 0002163719 *

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AR052191A1 (es)	2007-03-07
WO2006073360A1 (fr)	2006-07-13
EP1838325A1 (fr)	2007-10-03
UY29326A1 (es)	2006-08-31
TW200640466A (en)	2006-12-01

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