JP2005504783A - イロペリドン代謝産物の光学異性体 - Google Patents

イロペリドン代謝産物の光学異性体 Download PDF

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Publication number
JP2005504783A
JP2005504783A JP2003524978A JP2003524978A JP2005504783A JP 2005504783 A JP2005504783 A JP 2005504783A JP 2003524978 A JP2003524978 A JP 2003524978A JP 2003524978 A JP2003524978 A JP 2003524978A JP 2005504783 A JP2005504783 A JP 2005504783A
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Japan
Prior art keywords
acid addition
free base
addition salt
pharmaceutically acceptable
formula
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JP2003524978A
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English (en)
Japanese (ja)
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JP2005504783A5 (enExample
Inventor
ドミニク・グリムレ
ハンス・オー・カルクマン
イン・ヘクン
Original Assignee
ノバルティス アクチエンゲゼルシャフト
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Publication of JP2005504783A publication Critical patent/JP2005504783A/ja
Publication of JP2005504783A5 publication Critical patent/JP2005504783A5/ja
Withdrawn legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Cosmetics (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
JP2003524978A 2001-08-31 2002-08-30 イロペリドン代謝産物の光学異性体 Withdrawn JP2005504783A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31639001P 2001-08-31 2001-08-31
PCT/EP2002/009700 WO2003020707A1 (en) 2001-08-31 2002-08-30 Optical isomers of an iloperidone metabolite

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2009281094A Division JP2010100633A (ja) 2001-08-31 2009-12-11 イロペリドン代謝産物の光学異性体

Publications (2)

Publication Number Publication Date
JP2005504783A true JP2005504783A (ja) 2005-02-17
JP2005504783A5 JP2005504783A5 (enExample) 2009-08-27

Family

ID=23228843

Family Applications (6)

Application Number Title Priority Date Filing Date
JP2003524978A Withdrawn JP2005504783A (ja) 2001-08-31 2002-08-30 イロペリドン代謝産物の光学異性体
JP2009281094A Withdrawn JP2010100633A (ja) 2001-08-31 2009-12-11 イロペリドン代謝産物の光学異性体
JP2013017050A Withdrawn JP2013116905A (ja) 2001-08-31 2013-01-31 イロペリドン代謝産物の光学異性体
JP2013142873A Pending JP2013227335A (ja) 2001-08-31 2013-07-08 イロペリドン代謝産物の光学異性体
JP2015156358A Pending JP2015227368A (ja) 2001-08-31 2015-08-06 イロペリドン代謝産物の光学異性体
JP2015156359A Pending JP2015214577A (ja) 2001-08-31 2015-08-06 イロペリドン代謝産物の光学異性体

Family Applications After (5)

Application Number Title Priority Date Filing Date
JP2009281094A Withdrawn JP2010100633A (ja) 2001-08-31 2009-12-11 イロペリドン代謝産物の光学異性体
JP2013017050A Withdrawn JP2013116905A (ja) 2001-08-31 2013-01-31 イロペリドン代謝産物の光学異性体
JP2013142873A Pending JP2013227335A (ja) 2001-08-31 2013-07-08 イロペリドン代謝産物の光学異性体
JP2015156358A Pending JP2015227368A (ja) 2001-08-31 2015-08-06 イロペリドン代謝産物の光学異性体
JP2015156359A Pending JP2015214577A (ja) 2001-08-31 2015-08-06 イロペリドン代謝産物の光学異性体

Country Status (9)

Country Link
US (4) US20050020632A1 (enExample)
EP (2) EP2305656B1 (enExample)
JP (6) JP2005504783A (enExample)
AT (1) ATE518845T1 (enExample)
CY (2) CY1112039T1 (enExample)
DK (2) DK1425272T3 (enExample)
ES (2) ES2398434T3 (enExample)
PT (2) PT2305656E (enExample)
WO (1) WO2003020707A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011506481A (ja) * 2007-12-13 2011-03-03 ヴァンダ ファーマシューティカルズ インコーポレイテッド αアドレナリン受容体介在状態を治療する方法及び組成物
JP2015510893A (ja) * 2012-03-14 2015-04-13 ヴァンダ ファーマシューティカルズ インコーポレイテッド 精神障害の治療における使用のためのイロペリドン代謝物

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CA2463158C (en) 2001-10-30 2013-07-30 Novartis Ag Depot formulations of iloperidone and a star polymer
ATE398108T1 (de) 2002-03-27 2008-07-15 Glaxo Group Ltd Chinolinderivate und deren verwendung als 5-ht6 liganden
GB0216416D0 (en) * 2002-07-15 2002-08-21 Novartis Ag Organic compounds
HRP20060100T3 (en) 2003-07-22 2007-03-31 Arena Pharmaceuticals Inc Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of disorders related thereto
GB0322994D0 (en) * 2003-10-01 2003-11-05 Novartis Ag Organic compounds
EP1799865B1 (en) 2004-09-30 2012-06-06 Vanda Pharmaceuticals Inc. Methods for the administration of iloperidone
US20100063093A1 (en) 2007-03-28 2010-03-11 Curt Wolfgang Methods for the administration of iloperidone
US20070262395A1 (en) 2006-05-11 2007-11-15 Gibbons Jasper S Memory cell access devices and methods of making the same
US8008144B2 (en) 2006-05-11 2011-08-30 Micron Technology, Inc. Dual work function recessed access device and methods of forming
BRPI0711872A2 (pt) * 2006-05-22 2011-12-06 Vanda Pharmaceuticals Inc tratamento para distúrbios depressivos
US20150259747A1 (en) 2007-03-29 2015-09-17 Vanda Pharmaceuticals Inc. Method of predicting a predisposition to qt prolongation
EP2134873B1 (en) 2007-03-29 2015-05-06 Vanda Pharmaceuticals Inc. Method of predicting a predisposition to qt prolongation
US8198305B2 (en) 2007-04-13 2012-06-12 Concert Pharmaceuticals Inc. 1,2-benzisoxazol-3-yl compounds
US9080214B2 (en) 2007-05-18 2015-07-14 Vanda Pharmaceuticals, Inc. Genetic markers for efficacy of iloperidone in the treatment of psychotic symptoms
US8652776B2 (en) 2007-09-10 2014-02-18 Vanda Pharmaceuticals, Inc. Prediction of QT prolongation based on SNP genotype
US9084742B2 (en) 2007-12-12 2015-07-21 Axovant Sciences Ltd. Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-Quinoline
HRP20140701T1 (hr) 2007-12-13 2014-11-21 Vanda Pharmaceuticals Inc. Metoda i spoj za lijeäśenje stanja posredovanih serotoninskim receptorom
US20110061014A1 (en) 2008-02-01 2011-03-10 Energyhub Interfacing to resource consumption management devices
WO2009123714A2 (en) 2008-04-02 2009-10-08 Arena Pharmaceuticals, Inc. Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor
WO2010062321A1 (en) 2008-10-28 2010-06-03 Arena Pharmaceuticals, Inc. Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea and crystalline forms related thereto
US7824986B2 (en) 2008-11-05 2010-11-02 Micron Technology, Inc. Methods of forming a plurality of transistor gates, and methods of forming a plurality of transistor gates having at least two different work functions
CA2757717C (en) 2009-04-06 2018-09-04 Vanda Pharmaceuticals, Inc. Method of predicting a predisposition to qt prolongation
WO2010117941A1 (en) 2009-04-06 2010-10-14 Vanda Pharmaceuticals, Inc. Method of predicting a predisposition to qt prolongation based on abcc2 gene sequence or product thereof
EP3354753B1 (en) 2009-04-06 2020-02-12 Vanda Pharmaceuticals Inc. Method of treatment based on polymorphisms of the kcnq1 gene
WO2010117943A1 (en) 2009-04-06 2010-10-14 Vanda Pharmaceuticals, Inc. Method of predicting a predisposition to qt prolongation based on bai3 gene sequence or product thereof
MX2012007365A (es) 2009-12-23 2012-08-15 Lupin Ltd Composiciones farmaceuticas de liberacion lenta de iloperidona.
WO2012032532A1 (en) * 2010-09-07 2012-03-15 Symed Labs Limited "processes for the preparation of 4'-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino]propoxy]-3'-methoxyacetophenone and intermediates thereof"
WO2012063269A2 (en) 2010-11-12 2012-05-18 Cadila Healthcare Limited Process for preparing iloperidone
US10441580B2 (en) 2015-02-17 2019-10-15 Vanda Pharmaceuticals, Inc. Iloperidone for the treatment of schizophrenia
JP2018516992A (ja) 2015-06-12 2018-06-28 アクソファント サイエンシーズ ゲーエムベーハーAxovant Sciences Gmbh レム睡眠行動障害の予防および処置のために有用なジアリールおよびアリールヘテロアリール尿素誘導体
WO2017011767A2 (en) 2015-07-15 2017-01-19 Axovant Sciences Ltd. Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of hallucinations associated with a neurodegenerative disease
IL285721B2 (en) 2019-02-21 2025-03-01 Obi Pharma Inc Methods of making high enantioselective secondary alcohols
US11607408B2 (en) 2019-10-15 2023-03-21 Vanda Pharmaceuticals Inc. Method of treatment of schizophrenia
EP4507698A1 (en) 2022-04-13 2025-02-19 Vanda Pharmaceuticals Inc. Treatment of parkinson's disease and parkinson's disease psychosis
CN120390640A (zh) 2022-12-19 2025-07-29 万达制药公司 治疗双相i型障碍和精神分裂症的伊潘立酮的给药方案
WO2024249952A1 (en) 2023-06-02 2024-12-05 Vanda Pharmaceuticals Inc. Method of treatment with iloperidone

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US4804663A (en) * 1985-03-27 1989-02-14 Janssen Pharmaceutica N.V. 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
US5158952A (en) * 1988-11-07 1992-10-27 Janssen Pharmaceutica N.V. 3-[2-[4-(6-fluoro-1,2-benzisoxozol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9 tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a]pyrimidin-4-one, compositions and method of use
US5364866A (en) * 1989-05-19 1994-11-15 Hoechst-Roussel Pharmaceuticals, Inc. Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analetics
US5776963A (en) 1989-05-19 1998-07-07 Hoechst Marion Roussel, Inc. 3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility
ES2076253T3 (es) 1989-05-19 1995-11-01 Hoechst Roussel Pharma N-(ariloxialquil)-heteroarilpiperidinas y -heteroarilpiperazinas, un procedimiento para su preparacion y su uso como medicamentos.
JPH05286868A (ja) 1992-04-03 1993-11-02 Kiyoshi Okawa 制がん剤複合体およびそのスクリーニング法
US5889006A (en) * 1995-02-23 1999-03-30 Schering Corporation Muscarinic antagonists
ES2149742T1 (es) * 1997-07-03 2000-11-16 Asahi Chemical Ind Nuevos compuestos triciclicos que tienen anillos saturados y composiciones medicinales que contienen los mismos.
MXPA05000294A (es) 2002-07-30 2005-08-19 Peter Migaly Terapia combinada para la depresion, prevencion de suicidios y varias condiciones medicas y psiquiatricas.

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011506481A (ja) * 2007-12-13 2011-03-03 ヴァンダ ファーマシューティカルズ インコーポレイテッド αアドレナリン受容体介在状態を治療する方法及び組成物
JP2015510893A (ja) * 2012-03-14 2015-04-13 ヴァンダ ファーマシューティカルズ インコーポレイテッド 精神障害の治療における使用のためのイロペリドン代謝物
JP2017061506A (ja) * 2012-03-14 2017-03-30 ヴァンダ ファーマシューティカルズ インコーポレイテッド 精神障害の治療における使用のためのイロペリドン代謝物
JP2018203774A (ja) * 2012-03-14 2018-12-27 ヴァンダ ファーマシューティカルズ インコーポレイテッド 精神障害の治療における使用のためのイロペリドン代謝物
US10874659B2 (en) 2012-03-14 2020-12-29 Vanda Pharmaceuticals Inc. Iloperidone metabolite for use in the treatment of psychiatric disorders
JP2021001221A (ja) * 2012-03-14 2021-01-07 ヴァンダ ファーマシューティカルズ インコーポレイテッド 精神障害の治療における使用のためのイロペリドン代謝物
JP7151029B2 (ja) 2012-03-14 2022-10-12 ヴァンダ ファーマシューティカルズ インコーポレイテッド 精神障害の治療における使用のためのイロペリドン代謝物
JP2023022243A (ja) * 2012-03-14 2023-02-14 ヴァンダ ファーマシューティカルズ インコーポレイテッド 精神障害の治療における使用のためのイロペリドン代謝物

Also Published As

Publication number Publication date
HK1156309A1 (en) 2012-09-07
DK2305656T3 (da) 2013-02-11
HK1066536A1 (en) 2005-03-24
EP2305656B1 (en) 2012-10-24
ES2370634T3 (es) 2011-12-21
PT2305656E (pt) 2013-01-10
ATE518845T1 (de) 2011-08-15
CY1113550T1 (el) 2016-06-22
US20130296366A1 (en) 2013-11-07
US7977356B2 (en) 2011-07-12
EP1425272B1 (en) 2011-08-03
US20110201646A1 (en) 2011-08-18
JP2015227368A (ja) 2015-12-17
US8314129B2 (en) 2012-11-20
ES2398434T3 (es) 2013-03-19
ES2398434T8 (es) 2017-10-09
DK1425272T3 (da) 2011-11-21
US20090176739A1 (en) 2009-07-09
EP1425272A1 (en) 2004-06-09
JP2013227335A (ja) 2013-11-07
PT1425272E (pt) 2011-10-19
JP2015214577A (ja) 2015-12-03
WO2003020707A1 (en) 2003-03-13
CY1112039T1 (el) 2015-11-04
JP2010100633A (ja) 2010-05-06
EP2305656A1 (en) 2011-04-06
JP2013116905A (ja) 2013-06-13
US20050020632A1 (en) 2005-01-27

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