JP2005525392A - 減少された鎮静及び失調効果を有する抗不安薬剤 - Google Patents
減少された鎮静及び失調効果を有する抗不安薬剤 Download PDFInfo
- Publication number
- JP2005525392A JP2005525392A JP2003580300A JP2003580300A JP2005525392A JP 2005525392 A JP2005525392 A JP 2005525392A JP 2003580300 A JP2003580300 A JP 2003580300A JP 2003580300 A JP2003580300 A JP 2003580300A JP 2005525392 A JP2005525392 A JP 2005525392A
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- JP
- Japan
- Prior art keywords
- cyclopropyl
- thienyl
- phenyl
- ring
- substituted
- Prior art date
- 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
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- 0 C*C#Cc(cc1)cc(C(c2ccccc2)=[N+](C2)[O-])c1N=C2NC Chemical compound C*C#Cc(cc1)cc(C(c2ccccc2)=[N+](C2)[O-])c1N=C2NC 0.000 description 9
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
- A61P25/18—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/12—1,5-Benzodiazepines; Hydrogenated 1,5-benzodiazepines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
- C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
- C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
- C07D243/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
- C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
- C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
- C07D243/24—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/06—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US36840802P | 2002-03-28 | 2002-03-28 | |
PCT/US2003/009587 WO2003082832A2 (en) | 2002-03-28 | 2003-03-28 | Anxiolytic agents with reduced sedative and ataxic effects |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2005525392A true JP2005525392A (ja) | 2005-08-25 |
JP2005525392A5 JP2005525392A5 (US07794700-20100914-C00152.png) | 2008-01-24 |
Family
ID=28675480
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2003580300A Pending JP2005525392A (ja) | 2002-03-28 | 2003-03-28 | 減少された鎮静及び失調効果を有する抗不安薬剤 |
Country Status (16)
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2019532989A (ja) * | 2016-11-01 | 2019-11-14 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Cns関連疾患を処置するための1,3−ジヒドロ−1,4−ベンゾジアゼピン−2−チオン |
Families Citing this family (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
USRE47475E1 (en) * | 2002-03-28 | 2019-07-02 | Wisys Technology Foundation, Inc. | Selective agents for pain suppression |
AU2005260650A1 (en) * | 2004-06-30 | 2006-01-12 | Wisys Technology Foundation, Inc. | Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects |
US8119629B2 (en) * | 2007-10-03 | 2012-02-21 | Bristol-Meyers Squibb Company | Carboxamide GABAA α2 modulators |
CA2713025C (en) * | 2008-01-22 | 2012-12-04 | Eli Lilly And Company | Kappa selective opioid receptor antagonist |
US20100261711A1 (en) * | 2009-03-20 | 2010-10-14 | Wisys Technology Foundation | Selective anticonvulsant agents and their uses |
JP2013209292A (ja) * | 2010-07-23 | 2013-10-10 | Nippon Chemiphar Co Ltd | P2x4受容体拮抗剤 |
US9006233B2 (en) | 2011-04-28 | 2015-04-14 | Uwm Research Foundation, Inc. | Gabaergic receptor subtype selective ligands and their uses |
US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
WO2014047413A1 (en) | 2012-09-21 | 2014-03-27 | Uwm Research Foundation, Inc. | Novel gabaa agonists and methods of using to control airway hyperresponsiveness and inflammation in asthma |
FR3010785B1 (fr) * | 2013-09-18 | 2015-08-21 | Snecma | Procede de controle de la densite d'energie d'un faisceau laser par analyse d'image et dispositif correspondant |
EP3407886A1 (en) | 2016-01-27 | 2018-12-05 | Universität Zürich | Use of gabaa receptor modulators for treatment of itch |
EP4129297A1 (en) | 2016-03-18 | 2023-02-08 | UWM Research Foundation, Inc. | Treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders with alpha5-containing gabaa receptor agonists |
JP7013446B2 (ja) | 2016-08-16 | 2022-02-15 | ユーダブリューエム・リサーチ・ファウンデーション,インコーポレーテッド | Gaba(a)受容体モジュレーター、及び、喘息における気道過敏及び炎症を抑制するための方法 |
CN107056760A (zh) * | 2017-01-22 | 2017-08-18 | 苏州楚凯药业有限公司 | 5,7位取代的1H‑苯并[e][1,4]二氮杂‑2(3H)‑酮衍生物的制备方法 |
CN107325101B (zh) * | 2017-06-29 | 2019-03-26 | 上海合全药物研发有限公司 | 6-羟甲基-6,7-二氢-5h,9h-咪唑并二氮杂卓-8-羧酸叔丁酯的合成方法 |
CN107216332B (zh) * | 2017-06-29 | 2019-04-30 | 上海药明康德新药开发有限公司 | 叔丁基-7-羟甲基-7,8-二氢4h吡唑并二氮杂卓5(6h)甲酸基酯的合成方法 |
US20200316087A1 (en) | 2017-10-03 | 2020-10-08 | Uwm Research Foundation, Inc. | Novel combination therapy for anxiety disorders, epilepsy, and pain |
BR112022018828A2 (pt) | 2020-03-31 | 2022-11-22 | Hoffmann La Roche | Derivados de benzodiazepina como gaba a gamma1 pams |
US20220370409A1 (en) | 2021-05-04 | 2022-11-24 | Janssen Pharmaceuticals, Inc. | Compositions And Methods For The Treatment Of Depression |
AR127127A1 (es) * | 2021-09-24 | 2023-12-20 | Hoffmann La Roche | NUEVOS DERIVADOS DE PIRIDODIAZEPINAS COMO PAM DE GABAA g1 |
WO2023170550A1 (en) | 2022-03-07 | 2023-09-14 | Janssen Pharmaceuticals, Inc. | Polymorph forms of aticaprant for use in treating major depressive disorder |
Family Cites Families (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2893992A (en) | 1959-07-07 | I ii i i | ||
US3886141A (en) * | 1971-10-07 | 1975-05-27 | Hoffmann La Roche | Preparation of 5-pyridyl benzodiazepine utilizing hexamethylenetetramine |
US4280957A (en) | 1974-09-11 | 1981-07-28 | Hoffmann-La Roche Inc. | Imidazodiazepines and processes therefor |
US4440685A (en) * | 1974-09-11 | 1984-04-03 | Hoffmann-La Roche Inc. | Imidazodiazepines and processes therefor |
US4401597A (en) | 1978-05-15 | 1983-08-30 | Hoffmann-La Roche Inc. | Imidazodiazepines and processes therefor |
DE3435973A1 (de) * | 1984-10-01 | 1986-04-10 | Boehringer Ingelheim KG, 6507 Ingelheim | Diazepine enthaltende pharmazeutische zusammensetzungen mit paf-antagonistischer wirkung |
EP0230942B1 (de) * | 1986-01-21 | 1992-04-29 | Boehringer Ingelheim Kg | Thieno-1,4-diazepine |
US4959361A (en) | 1987-12-18 | 1990-09-25 | Hoffmann-La Roche Inc. | Triazolo(4,3-A)(1,4)benzodiazepines and thieno (3,2-F)(1,2,4)triazolo(4,3-A)(1,4)diazepine compounds which have useful activity as platelet activating factor (PAF) antagonists |
MC1999A1 (fr) | 1987-12-18 | 1990-01-26 | Hoffmann La Roche | Composes tricycliques |
US5968176A (en) * | 1997-05-29 | 1999-10-19 | 3Com Corporation | Multilayer firewall system |
CZ20033003A3 (cs) * | 2001-04-12 | 2004-05-12 | F@Áhoffmann@Laárocheáag | Dihydrobenzo [b][�Ź@]diazepin@onové deriváty jako MGLUR@ antagonisty II |
US7161904B2 (en) * | 2002-06-04 | 2007-01-09 | Fortinet, Inc. | System and method for hierarchical metering in a virtual router based network switch |
US7415723B2 (en) * | 2002-06-11 | 2008-08-19 | Pandya Ashish A | Distributed network security system and a hardware processor therefor |
-
2003
- 2003-03-28 AT AT03723846T patent/ATE389640T1/de not_active IP Right Cessation
- 2003-03-28 MX MXPA04009332A patent/MXPA04009332A/es active IP Right Grant
- 2003-03-28 JP JP2003580300A patent/JP2005525392A/ja active Pending
- 2003-03-28 NZ NZ535517A patent/NZ535517A/en not_active IP Right Cessation
- 2003-03-28 KR KR1020087012062A patent/KR20080060286A/ko not_active Application Discontinuation
- 2003-03-28 BR BR0308918-5A patent/BR0308918A/pt not_active IP Right Cessation
- 2003-03-28 ES ES03723846T patent/ES2300576T3/es not_active Expired - Lifetime
- 2003-03-28 DE DE60319812T patent/DE60319812T2/de not_active Expired - Lifetime
- 2003-03-28 KR KR1020047015305A patent/KR100865410B1/ko not_active IP Right Cessation
- 2003-03-28 WO PCT/US2003/009587 patent/WO2003082832A2/en active Application Filing
- 2003-03-28 AU AU2003230754A patent/AU2003230754B2/en not_active Ceased
- 2003-03-28 IL IL16395803A patent/IL163958A0/xx unknown
- 2003-03-28 DK DK03723846T patent/DK1490344T3/da active
- 2003-03-28 EP EP03723846A patent/EP1490344B1/en not_active Expired - Lifetime
- 2003-03-28 US US10/402,538 patent/US7119196B2/en not_active Expired - Lifetime
- 2003-03-28 CN CNA038073439A patent/CN1642924A/zh active Pending
- 2003-03-28 CA CA002480869A patent/CA2480869A1/en not_active Abandoned
-
2006
- 2006-07-20 US US11/458,855 patent/US20070049580A1/en not_active Abandoned
- 2006-07-20 US US11/458,739 patent/US7235656B2/en not_active Expired - Fee Related
-
2007
- 2007-06-24 US US11/767,515 patent/US20070299058A1/en not_active Abandoned
- 2007-10-30 US US11/929,860 patent/US20080108605A1/en not_active Abandoned
-
2010
- 2010-01-08 US US12/684,845 patent/US20100130481A1/en not_active Abandoned
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2019532989A (ja) * | 2016-11-01 | 2019-11-14 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Cns関連疾患を処置するための1,3−ジヒドロ−1,4−ベンゾジアゼピン−2−チオン |
JP7139323B2 (ja) | 2016-11-01 | 2022-09-20 | エフ.ホフマン-ラ ロシュ アーゲー | Cns関連疾患を処置するための1,3-ジヒドロ-1,4-ベンゾジアゼピン-2-チオン |
Also Published As
Publication number | Publication date |
---|---|
DE60319812D1 (de) | 2008-04-30 |
EP1490344A2 (en) | 2004-12-29 |
EP1490344B1 (en) | 2008-03-19 |
AU2003230754A1 (en) | 2003-10-13 |
US20100130481A1 (en) | 2010-05-27 |
NZ535517A (en) | 2007-02-23 |
WO2003082832A2 (en) | 2003-10-09 |
ATE389640T1 (de) | 2008-04-15 |
WO2003082832A3 (en) | 2004-04-08 |
US20070049580A1 (en) | 2007-03-01 |
DK1490344T3 (da) | 2008-06-16 |
KR20040098029A (ko) | 2004-11-18 |
ES2300576T3 (es) | 2008-06-16 |
US20080108605A1 (en) | 2008-05-08 |
US7119196B2 (en) | 2006-10-10 |
US20040082573A1 (en) | 2004-04-29 |
CA2480869A1 (en) | 2003-10-09 |
MXPA04009332A (es) | 2005-12-12 |
US20070054881A1 (en) | 2007-03-08 |
IL163958A0 (en) | 2005-12-18 |
KR20080060286A (ko) | 2008-07-01 |
CN1642924A (zh) | 2005-07-20 |
AU2003230754B2 (en) | 2007-10-25 |
KR100865410B1 (ko) | 2008-10-24 |
BR0308918A (pt) | 2005-01-04 |
DE60319812T2 (de) | 2009-04-23 |
US7235656B2 (en) | 2007-06-26 |
US20070299058A1 (en) | 2007-12-27 |
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