JP5139446B2 - グルタミン酸作動性シナプス応答を増強する3−置換−[1,2,3]−ベンゾトリアジノン化合物 - Google Patents
グルタミン酸作動性シナプス応答を増強する3−置換−[1,2,3]−ベンゾトリアジノン化合物 Download PDFInfo
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- JP5139446B2 JP5139446B2 JP2009544857A JP2009544857A JP5139446B2 JP 5139446 B2 JP5139446 B2 JP 5139446B2 JP 2009544857 A JP2009544857 A JP 2009544857A JP 2009544857 A JP2009544857 A JP 2009544857A JP 5139446 B2 JP5139446 B2 JP 5139446B2
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- treatment
- prevention
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- schizophrenia
- medicament
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Description
I.定義
上記のとおり、本発明の化合物および方法は、AMPA受容体介在性応答を増加させ、低グルタミン酸作動性状態の処置に有用である。該化合物は、興奮性シナプスの数もしくは強度、またはAMPA受容体の数の欠損を起こした、記憶または他の認知機能の障害などの状態の処置にも有用である。該化合物は、皮質/線条体不均衡による統合失調症または統合失調症様挙動の処置、およびAPMA受容体による挙動の学習の促進に用いてもよい。
8−シクロプロピル−3−[2−(3−フルオロフェニル)エチル]−7,8−ジヒドロ−3H−[1,3]オキサジノ[6,5−g][1,2,3]ベンゾトリアジン−4,9−ジオン
Claims (16)
- 8−シクロプロピル−3−[2−(3−フルオロフェニル)エチル]−7,8−ジヒドロ−3H−[1,3]オキサジノ[6,5−g][1,2,3]ベンゾトリアジン−4,9−ジオン、または酸もしくは塩基の薬学的に許容され得るその付加塩である、請求項1記載の式で示される化合物。
- 請求項1〜2のいずれか記載の化合物の有効量を、薬学的に許容され得る担体、添加剤または賦形剤と共に含む医薬組成物。
- 低グルタミン酸作動性状態、または興奮性シナプスの数もしくは強度の欠損、またはAMPA受容体数の欠損により、記憶障害または他の認知機能障害をきたしたほ乳類対象の予防及び治療のための請求項3記載の医薬組成物。
- 低グルタミン酸作動性状態、または興奮性シナプスの数もしくは強度の欠損、またはAMPA受容体数の欠損により、皮質/線条体不均衡が生じて、統合失調症または統合失調症様挙動をきたしたほ乳類の予防及び治療のための請求項3記載の医薬組成物。
- 前記状態が、統合失調症である、請求項5記載の医薬組成物。
- 前記状態が、パーキンソン病である、請求項4記載の医薬組成物。
- 前記状態が、アルツハイマー病である、請求項4記載の医薬組成物。
- 前記化合物が、前記組成物の0.5〜75重量%含まれ、前記担体、添加剤または賦形剤が、前記組成物の25〜95.5%含まれる、請求項3〜8のいずれか記載の組成物。
- 低グルタミン酸作動性状態、または興奮性シナプスの数もしくは強度の欠損、またはAMPA受容体数の欠損により、記憶障害または他の認知機能障害をきたしたほ乳類対象の予防及び治療に使用される医薬の製造における、請求項1〜2のいずれか記載の化合物の使用。
- 統合失調症の予防及び治療に使用される医薬の製造における、請求項1および2のいずれか記載の化合物の使用。
- パーキンソン病の予防及び治療に使用される医薬の製造における、請求項1および2のいずれか記載の化合物の使用。
- ADHDの予防及び治療に使用される医薬の製造における、請求項1および2のいずれか記載の化合物の使用。
- レット症候群の予防及び治療に使用される医薬の製造における、請求項1および2のいずれか記載の化合物の使用。
- 脆弱X症候群の予防及び治療に使用される医薬の製造における、請求項1および2のいずれか記載の化合物の使用。
- アルツハイマー病の予防及び治療用の医薬の製造における、請求項1および2のいずれか記載の化合物の使用。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US87850307P | 2007-01-03 | 2007-01-03 | |
US60/878,503 | 2007-01-03 | ||
US92143307P | 2007-04-02 | 2007-04-02 | |
US60/921,433 | 2007-04-02 | ||
PCT/US2007/026416 WO2008085506A1 (en) | 2007-01-03 | 2007-12-28 | 3-substituted-[1,2,3]-benzotriazinone compound for enhancing glutamatergic synaptic responses |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2010514838A JP2010514838A (ja) | 2010-05-06 |
JP5139446B2 true JP5139446B2 (ja) | 2013-02-06 |
Family
ID=39608956
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009544857A Expired - Fee Related JP5139446B2 (ja) | 2007-01-03 | 2007-12-28 | グルタミン酸作動性シナプス応答を増強する3−置換−[1,2,3]−ベンゾトリアジノン化合物 |
Country Status (38)
Country | Link |
---|---|
US (1) | US8173644B2 (ja) |
EP (1) | EP2144506B1 (ja) |
JP (1) | JP5139446B2 (ja) |
CN (1) | CN101616592B (ja) |
AP (1) | AP2502A (ja) |
AR (1) | AR064740A1 (ja) |
AT (1) | ATE527269T1 (ja) |
AU (1) | AU2007342365B2 (ja) |
BR (1) | BRPI0720749A2 (ja) |
CA (1) | CA2674460C (ja) |
CR (1) | CR10906A (ja) |
CU (1) | CU23804B7 (ja) |
CY (1) | CY1112493T1 (ja) |
DK (1) | DK2144506T3 (ja) |
EA (1) | EA017437B1 (ja) |
EC (1) | ECSP099499A (ja) |
ES (1) | ES2374995T3 (ja) |
GE (1) | GEP20125438B (ja) |
GT (1) | GT200900189A (ja) |
HK (1) | HK1140105A1 (ja) |
HN (1) | HN2009001268A (ja) |
HR (1) | HRP20110970T1 (ja) |
IL (1) | IL199651A (ja) |
MA (1) | MA31160B1 (ja) |
ME (1) | ME00819B (ja) |
MX (1) | MX2009007242A (ja) |
MY (1) | MY154877A (ja) |
NI (1) | NI200900131A (ja) |
NZ (1) | NZ578293A (ja) |
PL (1) | PL2144506T3 (ja) |
PT (1) | PT2144506E (ja) |
RS (1) | RS52108B (ja) |
SG (1) | SG163545A1 (ja) |
SI (1) | SI2144506T1 (ja) |
SV (1) | SV2009003322A (ja) |
TN (1) | TN2009000277A1 (ja) |
WO (1) | WO2008085506A1 (ja) |
ZA (1) | ZA200904826B (ja) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2114158B1 (en) * | 2007-01-03 | 2012-08-08 | Cortex Pharmaceuticals, Inc. | 3-substituted-[1,2,3]benzotriazinone compounds for enhancing glutamatergic synaptic responses |
KR101599661B1 (ko) | 2007-05-17 | 2016-03-03 | 코텍스 파마슈티칼스, 인크. | 글루타메이트에 의한 시냅스 반응을 향상시키기 위한 이치환된 아미드 화합물 |
US8168632B2 (en) | 2007-08-10 | 2012-05-01 | Cortex Pharmaceuticals, Inc. | Bicyclic amide derivatives for the treatment of respiratory disorders |
SG163526A1 (en) | 2007-08-10 | 2010-08-30 | Cortex Pharma Inc | Bicyclic amides for enhancing glutamatergic synaptic responses |
US20110257186A1 (en) * | 2010-04-15 | 2011-10-20 | Staubli Ursula V | Compositions and methods for treating visual disorders |
US9242938B2 (en) | 2011-11-22 | 2016-01-26 | Beijing Medisan Technology Co., Ltd | Glycine reuptake inhibitor and use thereof |
FR3019464B1 (fr) | 2014-04-07 | 2016-05-06 | Servier Lab | Nouvelle association entre le 8-cyclopropyl-3-[2-(3-fluorophenyl)ethyl]-7,8-dihydro-3h-[1,3]oxazino[6,5-g] [1,2,3]benzotriazine-4,9-dione et un inhibiteur de l'acetylcholinesterase et les compositions pharmaceutiques qui la contiennent |
FR3034019B1 (fr) * | 2015-03-26 | 2017-03-17 | Servier Lab | Nouvelle association entre le 8-cyclopropyl-3-[2-(3-fluorophenyl)ethyl]-7,8-dihydro-3h-[1,3]oxazino[6,5-g] [1,2,3]benzotriazine-4,9-dione et un antidepresseur et les compositions pharmaceutiques qui la contiennent |
MX2017016875A (es) | 2015-06-26 | 2018-04-24 | Takeda Pharmaceuticals Co | Derivados de 2,3-dihidro-4h-1,3-benzoxazin-4-ona como moduladores de receptor muscarinico colinergico m1. |
CN106226509B (zh) * | 2016-08-12 | 2019-09-06 | 中国人民解放军第四军医大学 | 一种在小鼠前扣带回皮层诱发dse现象的方法 |
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DK623586A (da) * | 1985-12-27 | 1987-06-28 | Eisai Co Ltd | Piperidinderivater eller salte deraf og farmaceutiske kompositioner indeholdende forbindelserne |
FR2597103B1 (fr) * | 1986-04-15 | 1988-12-16 | Provesan Sa | Procede de preparation de derives d'oxazinobenzothiazine 6,6-dioxyde |
ATE215079T1 (de) | 1992-07-24 | 2002-04-15 | Univ California | Arzneimittel, die den durch ampa rezeptoren vermittelten synaptischen respons erhöhen |
US5962477A (en) * | 1994-04-12 | 1999-10-05 | Adolor Corporation | Screening methods for cytokine inhibitors |
DK0709384T3 (da) * | 1994-10-31 | 1999-08-23 | Merck Patent Gmbh | Benzylpiperidinderivater med høj affinitet til aminosyrereceptorers bindingssteder |
US5650409A (en) * | 1995-06-02 | 1997-07-22 | Cortex Pharmaceuticals, Inc. | Benzoyl piperidines/pyrrolidines for enhancing synaptic response |
US5736543A (en) * | 1996-04-03 | 1998-04-07 | The Regents Of The University Of California | Benzoxazines for enhancing synaptic response |
AU4416197A (en) | 1996-09-17 | 1998-04-14 | Regents Of The University Of California, The | Positive ampa receptor modulation to enhance brain neurotrophic factor expression |
US6110935A (en) * | 1997-02-13 | 2000-08-29 | The Regents Of The University Of California | Benzofurazan compounds for enhancing glutamatergic synaptic responses |
US5985871A (en) | 1997-12-24 | 1999-11-16 | Cortex Pharmaceuticals, Inc. | Benzoxazine compounds for enhancing synaptic response |
EP1071426A2 (en) | 1998-02-18 | 2001-01-31 | Neurosearch A/S | Novel compounds and their use as positive ampa receptor modulators |
US6713474B2 (en) * | 1998-09-18 | 2004-03-30 | Abbott Gmbh & Co. Kg | Pyrrolopyrimidines as therapeutic agents |
US6303542B1 (en) * | 2000-08-18 | 2001-10-16 | Rohm And Haas Company | Herbicidal 3-substituted-phenyl-1,2,3-benzotriazin-4-ones |
NZ532368A (en) * | 2001-11-26 | 2006-10-27 | Cortex Pharma Inc | Carbonylbenzoxazine compounds for enhancing glutamatergic synaptic responses |
JP2003238555A (ja) * | 2002-02-20 | 2003-08-27 | Sumitomo Pharmaceut Co Ltd | 細胞死抑制剤 |
AUPS255202A0 (en) * | 2002-05-27 | 2002-06-13 | Monash University | Agents and methods for the treatment of disorders associated with motor neuron degeneration |
JP2006516283A (ja) * | 2003-01-13 | 2006-06-29 | コーテックス ファーマシューティカルズ, インコーポレイテッド | 睡眠不足とストレスに起因する知覚衰退の処置方法 |
GB0317482D0 (en) * | 2003-07-25 | 2003-08-27 | Pfizer Ltd | Nicotinamide derivatives useful as pde4 inhibitors |
CN1897950A (zh) * | 2003-10-14 | 2007-01-17 | 惠氏公司 | 稠合芳基和杂芳基衍生物及其使用方法 |
EP2114158B1 (en) * | 2007-01-03 | 2012-08-08 | Cortex Pharmaceuticals, Inc. | 3-substituted-[1,2,3]benzotriazinone compounds for enhancing glutamatergic synaptic responses |
KR101599661B1 (ko) * | 2007-05-17 | 2016-03-03 | 코텍스 파마슈티칼스, 인크. | 글루타메이트에 의한 시냅스 반응을 향상시키기 위한 이치환된 아미드 화합물 |
SG163526A1 (en) | 2007-08-10 | 2010-08-30 | Cortex Pharma Inc | Bicyclic amides for enhancing glutamatergic synaptic responses |
US20100267728A1 (en) * | 2007-09-20 | 2010-10-21 | Cortex Pharmaceuticals, Inc. | 3-substituted-1,2,3-triazin-4-one's and 3 substituted 1,3-pyrimidinone's for enhancing glutamatergic synaptic responses |
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2007
- 2007-12-28 NZ NZ578293A patent/NZ578293A/en not_active IP Right Cessation
- 2007-12-28 SI SI200730806T patent/SI2144506T1/sl unknown
- 2007-12-28 ME MEP-2009-238A patent/ME00819B/me unknown
- 2007-12-28 ZA ZA200904826A patent/ZA200904826B/xx unknown
- 2007-12-28 BR BRPI0720749-2A patent/BRPI0720749A2/pt not_active Application Discontinuation
- 2007-12-28 RS RS20110587A patent/RS52108B/en unknown
- 2007-12-28 CA CA2674460A patent/CA2674460C/en not_active Expired - Fee Related
- 2007-12-28 MX MX2009007242A patent/MX2009007242A/es active IP Right Grant
- 2007-12-28 SG SG201004695-1A patent/SG163545A1/en unknown
- 2007-12-28 AP AP2009004931A patent/AP2502A/xx active
- 2007-12-28 EA EA200900925A patent/EA017437B1/ru not_active IP Right Cessation
- 2007-12-28 JP JP2009544857A patent/JP5139446B2/ja not_active Expired - Fee Related
- 2007-12-28 CN CN2007800508375A patent/CN101616592B/zh not_active Expired - Fee Related
- 2007-12-28 WO PCT/US2007/026416 patent/WO2008085506A1/en active Application Filing
- 2007-12-28 ES ES07868093T patent/ES2374995T3/es active Active
- 2007-12-28 PT PT07868093T patent/PT2144506E/pt unknown
- 2007-12-28 AU AU2007342365A patent/AU2007342365B2/en not_active Ceased
- 2007-12-28 US US12/448,784 patent/US8173644B2/en not_active Expired - Fee Related
- 2007-12-28 EP EP07868093A patent/EP2144506B1/en active Active
- 2007-12-28 PL PL07868093T patent/PL2144506T3/pl unknown
- 2007-12-28 GE GEAP200711384A patent/GEP20125438B/en unknown
- 2007-12-28 MY MYPI20092796A patent/MY154877A/en unknown
- 2007-12-28 DK DK07868093.1T patent/DK2144506T3/da active
- 2007-12-28 AT AT07868093T patent/ATE527269T1/de active
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2008
- 2008-01-03 AR ARP080100022A patent/AR064740A1/es not_active Application Discontinuation
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2009
- 2009-06-30 TN TNP2009000277A patent/TN2009000277A1/fr unknown
- 2009-07-01 NI NI200900131A patent/NI200900131A/es unknown
- 2009-07-02 IL IL199651A patent/IL199651A/en active IP Right Grant
- 2009-07-02 GT GT200900189A patent/GT200900189A/es unknown
- 2009-07-02 SV SV2009003322A patent/SV2009003322A/es unknown
- 2009-07-02 CR CR10906A patent/CR10906A/es not_active Application Discontinuation
- 2009-07-03 CU CU20090117A patent/CU23804B7/es active IP Right Grant
- 2009-07-03 HN HN2009001268A patent/HN2009001268A/es unknown
- 2009-07-07 EC EC2009009499A patent/ECSP099499A/es unknown
- 2009-07-31 MA MA32135A patent/MA31160B1/fr unknown
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2010
- 2010-06-29 HK HK10106349.3A patent/HK1140105A1/xx not_active IP Right Cessation
-
2011
- 2011-12-23 HR HR20110970T patent/HRP20110970T1/hr unknown
- 2011-12-28 CY CY20111101287T patent/CY1112493T1/el unknown
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