BR0013664A - Composto, uso de um composto, composição farmacêutica, e, métodos para o tratamento de uma doença ou distúrbio associado com agonismo patogênico, agonismo invertido ou antagonismo do receptor de gabaa, para localizar os receptores de gabaa, para inibir a ligação de um composto de benzodiazepina a um receptor de gabaa, e para alterar a atividade de transdução de sinal de receptores gabaa - Google Patents
Composto, uso de um composto, composição farmacêutica, e, métodos para o tratamento de uma doença ou distúrbio associado com agonismo patogênico, agonismo invertido ou antagonismo do receptor de gabaa, para localizar os receptores de gabaa, para inibir a ligação de um composto de benzodiazepina a um receptor de gabaa, e para alterar a atividade de transdução de sinal de receptores gabaaInfo
- Publication number
- BR0013664A BR0013664A BR0013664-6A BR0013664A BR0013664A BR 0013664 A BR0013664 A BR 0013664A BR 0013664 A BR0013664 A BR 0013664A BR 0013664 A BR0013664 A BR 0013664A
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- gabaa
- agonism
- inverted
- gaba
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 230000008484 agonism Effects 0.000 title abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 4
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 title abstract 2
- 230000008485 antagonism Effects 0.000 title abstract 2
- 229940049706 benzodiazepine Drugs 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 title abstract 2
- 230000000694 effects Effects 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 230000001717 pathogenic effect Effects 0.000 title abstract 2
- 230000019491 signal transduction Effects 0.000 title abstract 2
- 102000027484 GABAA receptors Human genes 0.000 title 4
- 108091008681 GABAA receptors Proteins 0.000 title 4
- 208000035475 disorder Diseases 0.000 title 1
- 239000000556 agonist Substances 0.000 abstract 2
- 210000004556 brain Anatomy 0.000 abstract 2
- 239000000018 receptor agonist Substances 0.000 abstract 2
- 229940044601 receptor agonist Drugs 0.000 abstract 2
- 239000002464 receptor antagonist Substances 0.000 abstract 2
- 229940044551 receptor antagonist Drugs 0.000 abstract 2
- RLOQBKJCOAXOLR-UHFFFAOYSA-N 1h-pyrrole-2-carboxamide Chemical class NC(=O)C1=CC=CN1 RLOQBKJCOAXOLR-UHFFFAOYSA-N 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- -1 BENZODIAZEPIN COMPOUND Chemical class 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 238000003745 diagnosis Methods 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 230000004807 localization Effects 0.000 abstract 1
- 230000006993 memory improvement Effects 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 239000000523 sample Substances 0.000 abstract 1
- 208000019116 sleep disease Diseases 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/041—Heterocyclic compounds
- A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
- A61K51/0468—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K51/047—Benzodiazepines
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
-
- 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
- A61P25/24—Antidepressants
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/14—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 three or more hetero rings
-
- 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
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
- G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
- G01N2333/70571—Assays involving receptors, cell surface antigens or cell surface determinants for neuromediators, e.g. serotonin receptor, dopamine receptor
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Epidemiology (AREA)
- Physics & Mathematics (AREA)
- Optics & Photonics (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
Abstract
"COMPOSTO, USO DE UM COMPOSTO, COMPOSIçãO FARMACêUTICA, E, MéTODOS PARA O TRATAMENTO DE UMA DOENçA OU DISTúRBIO ASSOCIADO COM AGONISMO PATOGêNICO, AGONISMO INVERTIDO OU ANTAGONISMO DO RECEPTOR DE GABA~ A~, PARA LOCALIZAR OS RECEPTORES DE GABA~ A~, PARA INIBIR A LIGAçãO DE UM COMPOSTO DE BENZODIAZEPINA A UM RECEPTOR DE GABA~ A~, E PARA ALTERAR A ATIVIDADE DE TRANSDUçãO DE SINAL DE RECEPTORES GABA~ A~". Compostos de pirrolcarboxamida substituída são apresentados. Estes compostos são agonistas, antagonistas ou agonistas invertidos altamente seletivos para receptores do cérebro de GABA~ A~ ou pró-medicamentos de agonistas, antagonistas ou agonistas invertidos para receptores do cérebro de GABA~ A~ e são por esse motivo úteis no diagnóstico e tratamento de ansiedade, depressão, demência de Alzheimer, distúrbios do sono e convulsão, dose excessiva com drogas de benzodiazepina e para o aumento da memória. Composições farmacêuticas, incluindo composições farmacêuticas embaladas, são ainda fornecidas. Os compostos da invenção são também úteis como sondas para a localização de receptores de GABA~ A~ em amostras de tecido.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15178999P | 1999-08-31 | 1999-08-31 | |
| US38731199A | 1999-08-31 | 1999-08-31 | |
| PCT/US2000/023862 WO2001016103A1 (en) | 1999-08-31 | 2000-08-30 | Fused pyrrolecarboxamides: gaba brain receptor ligands |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0013664A true BR0013664A (pt) | 2002-05-14 |
Family
ID=26848974
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0013664-6A BR0013664A (pt) | 1999-08-31 | 2000-08-30 | Composto, uso de um composto, composição farmacêutica, e, métodos para o tratamento de uma doença ou distúrbio associado com agonismo patogênico, agonismo invertido ou antagonismo do receptor de gabaa, para localizar os receptores de gabaa, para inibir a ligação de um composto de benzodiazepina a um receptor de gabaa, e para alterar a atividade de transdução de sinal de receptores gabaa |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US7109351B1 (pt) |
| EP (1) | EP1210328A1 (pt) |
| JP (1) | JP2003508385A (pt) |
| KR (1) | KR20020027613A (pt) |
| CN (1) | CN1372546A (pt) |
| AP (1) | AP2002002420A0 (pt) |
| AU (1) | AU7092800A (pt) |
| BG (1) | BG106459A (pt) |
| BR (1) | BR0013664A (pt) |
| CA (1) | CA2381553A1 (pt) |
| CR (1) | CR6581A (pt) |
| CZ (1) | CZ2002614A3 (pt) |
| EA (1) | EA200200188A1 (pt) |
| EE (1) | EE200200111A (pt) |
| HR (1) | HRP20020104A2 (pt) |
| HU (1) | HUP0202534A3 (pt) |
| IL (1) | IL147971A0 (pt) |
| IS (1) | IS6290A (pt) |
| MX (1) | MXPA02001709A (pt) |
| NO (1) | NO20020948L (pt) |
| OA (1) | OA12015A (pt) |
| PL (1) | PL354513A1 (pt) |
| SK (1) | SK2582002A3 (pt) |
| TR (1) | TR200200544T2 (pt) |
| WO (1) | WO2001016103A1 (pt) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050014939A1 (en) * | 1999-08-31 | 2005-01-20 | Neurogen Corporation | Fused pyrrolecarboxamides: GABA brain receptor ligands |
| AU2001241512A1 (en) * | 2000-03-13 | 2001-09-24 | Eli Lilly And Company | Sulfonamide derivatives |
| WO2001092257A1 (en) * | 2000-05-26 | 2001-12-06 | Neurogen Corporation | Oxo-imidazopyrimidine-carboxamides and their use as gaba brain receptor ligands |
| US6743817B2 (en) | 2000-09-06 | 2004-06-01 | Neurogen Corporation | Substituted fused pyrroleimines and pyrazoleimines |
| WO2002020492A1 (en) * | 2000-09-06 | 2002-03-14 | Neurogen Corporation | Aryl substituted tetrahydroindazoles and their use as ligands for the gaba-a receptor |
| US6861529B2 (en) * | 2001-07-06 | 2005-03-01 | Pfizer Inc | Cycloalkypyrrole-3-carboxylic acid derivatives and heterocycloalkylpyrrole-3-carboxylic acid derivatives |
| AU2003212979A1 (en) | 2002-02-07 | 2003-09-02 | Neurogen Corporation | Substituted fused pyrazolecarboxylic acid arylamides and related compounds |
| WO2005016928A1 (ja) * | 2003-08-15 | 2005-02-24 | Banyu Pharmaceutical Co., Ltd. | イミダゾピリジン誘導体 |
| JP4964593B2 (ja) | 2003-09-25 | 2012-07-04 | セノメド バイオサイエンシーズ，エルエルシー | 神経学的病状の治療用のテトラヒドロインドロン誘導体 |
| US7566781B2 (en) * | 2004-05-10 | 2009-07-28 | Banyu Pharmaceutical Co., Ltd. | Imidazopyridine compound |
| WO2006010362A1 (de) * | 2004-07-23 | 2006-02-02 | Justus-Liebig-Universität Giessen | Aminoadamantan-derivate, verfahren zu ihrer herstellung und ihre verwendung |
| CA2670636A1 (en) * | 2006-11-27 | 2008-06-05 | H. Lundbeck A/S | Heteroaryl amide derivatives |
| JP2011506445A (ja) * | 2007-12-13 | 2011-03-03 | アムジエン・インコーポレーテツド | γ−セクレターゼ調節剤 |
| CA2732520A1 (en) * | 2008-08-05 | 2010-02-11 | Merck Sharp & Dohme Corp. | Therapeutic compounds |
| US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3455943A (en) | 1966-10-21 | 1969-07-15 | American Cyanamid Co | Certain 5,8-dihydro-beta-carbolines |
| US4075343A (en) | 1976-09-13 | 1978-02-21 | Pfizer Inc. | Anti-allergenic 5-alkoxyimidazo[1,2-A]quinoline-2-carboxylic acids and derivatives thereof |
| DE3029980A1 (de) | 1980-08-08 | 1982-03-11 | Boehringer Mannheim Gmbh, 6800 Mannheim | Indolderivate und verfahren zu ihrer herstellung |
| JPS57123180A (en) | 1980-12-17 | 1982-07-31 | Schering Ag | 3-substituted beta-carboline, manufacture and psychotropic drug containing same |
| DE3147276A1 (de) | 1981-11-28 | 1983-06-09 | Boehringer Mannheim Gmbh, 6800 Mannheim | Verfahren zur herstellung von indolderivaten, deren verwendung als wertvolle zwischenprodukte und neue 4-hydroxyindole |
| DE3246932A1 (de) | 1982-12-16 | 1984-06-20 | Schering AG, 1000 Berlin und 4709 Bergkamen | Substituierte 5h-pyrimido(5,4-b)indole |
| DE3335323A1 (de) | 1983-09-27 | 1985-04-04 | Schering AG, 1000 Berlin und 4709 Bergkamen | Substituierte ss-carboline, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel |
| GB8429739D0 (en) | 1984-11-24 | 1985-01-03 | Fbc Ltd | Fungicides |
| DE3535927A1 (de) | 1985-10-04 | 1987-04-09 | Schering Ag | 3-vinyl- und 3-ethinyl-ss-carbolinderivate, ihre herstellung und ihre verwendung als arzneimittel |
| EP0738717A1 (en) | 1990-10-09 | 1996-10-23 | Neurogen Corporation | Certain substituted pyrimidines as intermediates for production of cycloalkyl and azacycloalkyl pyrrolopyrimidines |
| US5243049A (en) | 1992-01-22 | 1993-09-07 | Neurogen Corporation | Certain pyrroloquinolinones: a new class of GABA brain receptor ligands |
| JPH07503970A (ja) | 1992-02-19 | 1995-04-27 | ジ・アップジョン・カンパニー | ＣＮＳ活性を有する３−置換イミダゾ（１，５−ａ）−キノキサリン類およびキナゾリン類 |
| US5266698A (en) | 1992-04-30 | 1993-11-30 | Neurogen Corporation | Certain aryl and cycloalkyl fused imidazopyrazinediones; a new class of GABA brain receptor ligands |
| AU6098194A (en) | 1993-01-29 | 1994-08-15 | Ariad Pharmaceuticals, Inc. | Analogs of receptor tyrosine activation motifs and therapeutic uses thereof |
| US5750702A (en) * | 1993-10-27 | 1998-05-12 | Neurogen Corporation | Certain pyrrolo pyridine-3-carboxamides; a new class of GABA brain receptor ligands |
| US5484944A (en) * | 1993-10-27 | 1996-01-16 | Neurogen Corporation | Certain fused pyrrolecarboxanilides and their use as GABA brain receptor ligands |
| US6211365B1 (en) * | 1996-01-19 | 2001-04-03 | Neurogen Corporation | Fused pyrrolecarboxamides; a new class of GABA brain receptor ligands |
| US5804686A (en) | 1996-01-19 | 1998-09-08 | Neurogen Corporation | fused pyrrolecarboxamides; a new class of GABA brain receptor ligands |
| IT1287264B1 (it) * | 1996-03-21 | 1998-08-04 | Lino Crespan | Freno perfezionato per pattini con ruote in linea |
| US5677309A (en) | 1996-03-22 | 1997-10-14 | Neurogen Corporation | 1,2,4-triazolo 4,3-c! quinazolin-3-ones and 1,2,4-triazolo 4,3-c!quinazolin-3-thiones; a new class of GABA brain receptor ligands |
| US5955465A (en) | 1996-03-22 | 1999-09-21 | Neurogen Corporation | 1,2,4-triazolo 4,3-c!quinazolin-3-ones and 1,2,4-triazolo 4,3-c!quinazolin-3-thiones |
| WO1997034870A1 (en) * | 1996-03-22 | 1997-09-25 | Neurogen Corporation | Certain fused pyrrolecarboxamides as gaba brain receptor ligands |
| US5723462A (en) | 1996-04-26 | 1998-03-03 | Neurogen Corporation | Certain fused pyrrolecarboxamides a new class of GABA brain receptor ligands |
| CN1508129A (zh) | 1997-11-13 | 2004-06-30 | �Ʒ� | 吡咯酰胺的合成方法 |
-
2000
- 2000-08-30 HU HU0202534A patent/HUP0202534A3/hu unknown
- 2000-08-30 OA OA1200200063A patent/OA12015A/en unknown
- 2000-08-30 PL PL00354513A patent/PL354513A1/xx not_active Application Discontinuation
- 2000-08-30 CA CA002381553A patent/CA2381553A1/en not_active Abandoned
- 2000-08-30 BR BR0013664-6A patent/BR0013664A/pt not_active Application Discontinuation
- 2000-08-30 HR HR20020104A patent/HRP20020104A2/hr not_active Application Discontinuation
- 2000-08-30 US US09/651,207 patent/US7109351B1/en not_active Expired - Fee Related
- 2000-08-30 JP JP2001519673A patent/JP2003508385A/ja not_active Withdrawn
- 2000-08-30 EA EA200200188A patent/EA200200188A1/ru unknown
- 2000-08-30 KR KR1020027002757A patent/KR20020027613A/ko not_active Ceased
- 2000-08-30 MX MXPA02001709A patent/MXPA02001709A/es active IP Right Grant
- 2000-08-30 EE EEP200200111A patent/EE200200111A/xx unknown
- 2000-08-30 WO PCT/US2000/023862 patent/WO2001016103A1/en not_active Ceased
- 2000-08-30 EP EP00959643A patent/EP1210328A1/en not_active Withdrawn
- 2000-08-30 CN CN00812233A patent/CN1372546A/zh active Pending
- 2000-08-30 SK SK258-2002A patent/SK2582002A3/sk unknown
- 2000-08-30 AP APAP/P/2002/002420A patent/AP2002002420A0/en unknown
- 2000-08-30 TR TR2002/00544T patent/TR200200544T2/xx unknown
- 2000-08-30 CZ CZ2002614A patent/CZ2002614A3/cs unknown
- 2000-08-30 AU AU70928/00A patent/AU7092800A/en not_active Abandoned
- 2000-08-30 IL IL14797100A patent/IL147971A0/xx unknown
-
2002
- 2002-02-07 CR CR6581A patent/CR6581A/es not_active Application Discontinuation
- 2002-02-27 NO NO20020948A patent/NO20020948L/no unknown
- 2002-02-27 IS IS6290A patent/IS6290A/is unknown
- 2002-02-28 BG BG106459A patent/BG106459A/bg unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PL354513A1 (en) | 2004-01-26 |
| NO20020948D0 (no) | 2002-02-27 |
| MXPA02001709A (es) | 2002-10-23 |
| EP1210328A1 (en) | 2002-06-05 |
| TR200200544T2 (tr) | 2002-06-21 |
| AP2002002420A0 (en) | 2002-03-31 |
| CR6581A (es) | 2004-03-31 |
| CA2381553A1 (en) | 2001-03-08 |
| WO2001016103A1 (en) | 2001-03-08 |
| EA200200188A1 (ru) | 2002-08-29 |
| US7109351B1 (en) | 2006-09-19 |
| CZ2002614A3 (cs) | 2002-08-14 |
| KR20020027613A (ko) | 2002-04-13 |
| HUP0202534A2 (hu) | 2002-11-28 |
| HRP20020104A2 (en) | 2004-02-29 |
| IS6290A (is) | 2002-02-27 |
| JP2003508385A (ja) | 2003-03-04 |
| OA12015A (en) | 2006-04-19 |
| NO20020948L (no) | 2002-02-28 |
| HUP0202534A3 (en) | 2002-12-28 |
| SK2582002A3 (en) | 2003-02-04 |
| CN1372546A (zh) | 2002-10-02 |
| IL147971A0 (en) | 2002-09-12 |
| BG106459A (bg) | 2002-12-29 |
| EE200200111A (et) | 2003-06-16 |
| AU7092800A (en) | 2001-03-26 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| BR0010308A (pt) | Composto, composição farmacêutica, uso de um composto, e, métodos para o tratamento de uma doença ou distúrbio associados com o agonismo patogênico, agonismo inverso ou antagonismo do receptor de gabaa, para localizar receptores de gabaa em uma amostra de tecido, para inibir a ligação de um composto de benzodiazepina a um receptor de gabaa e para alterar a atividade da transdução de sinal dos receptores de gabaa, e, composição farmacêutica embalada | |
| BR0113300A (pt) | Composto ou um sal deste farmaceuticamente aceitável, composição farmacêutica, método para o tratamento de uma doença ou distúrbio associados com o agonismo patogênico, agonismo inverso ou antagonismo do receptor de gabaa, uso de um composto ou um sal, é, métodos para localização dos receptores de gabaa em uma amostra de tecido, de inibição da ligação de um composto de benzodiazepina a um receptor de gabaa, e para a alteração da atividade de transdutora de sinal dos receptores de gabaa | |
| Carlsson et al. | Network interactions in schizophrenia—therapeutic implications | |
| File et al. | Intrinsic actions of the benzodiazepine receptor antagonist Ro 15-1788 | |
| Paolone et al. | Eltoprazine prevents levodopa‐induced dyskinesias by reducing striatal glutamate and direct pathway activity | |
| WO2002000623A3 (en) | Aryl fused substituted 4-oxy-pyridines | |
| Lagos et al. | Effects of the D3 preferring dopamine agonist pramipexole on sleep and waking, locomotor activity and striatal dopamine release in rats | |
| BR0009539A (pt) | composto, composição farmacêutica, método para tratamento ou prevenção de uma doença ou distúrbio associado com agonismo patogênico, agonismo inverso ou antagonismo do receptor gaba a, uso de um composto, método para localizar receptores gaba a em uma amostra de tecido, método para alterar a atividade transdutora de sinal de receptores gaba a, método para o tratamento ou prevenção de distúrbios psicológicos associados com modulação do complexo receptor gaba a, e, processo para a preparação de um composto | |
| BRPI0413563A (pt) | compostos e composições como inibidores de atividade do receptor de quìnase de tirosina | |
| CA2246839A1 (en) | Pharmaceutical compositions containing ampa receptor antagonists for treating dyskineslas associated with dopamine agonist therapy | |
| BRPI0413342A (pt) | composto, composição farmacêutica, métodos para aumentar seletivamente a ativação do receptor de 5-ht2c em mamìferos, para tratar obesidade em mamìferos, para tratar distúrbios obsessivo/compulsivo em mamìferos, para tratar depressão em mamìferos e para tratar ansiedade em mamìferos, e, uso de um composto | |
| BR0211124A (pt) | Composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, métodos para alterar a atividade de transdução de sinal de receptores gabaa, para o tratamento de ansiedade, depressão, distúrbio do sono, esquizofrenia, distúrbio de hiperatividade-falta de atenção, ou para a melhora de memória, e para demonstrar a presença de receptores gabaa em uma célula ou amostra de tecido, composição farmacêutica embalada, e, uso de um composto ou sal | |
| BR0011823A (pt) | Derivado de benzimidazol, composto, composição farmacêutica, uso de um derivado de benzimidazol, e, método para tratamento, prevenção ou alìvio de uma doença ou de um distúrbio ou de uma condição de um corpo animal vivo | |
| WO2000077008A3 (en) | Heteroaryl substituted piperidines as gaba brain receptor lingands | |
| AR029025A1 (es) | Derivados de adenosina n6 heterociclicos 5' modificados, composiciones farmaceuticas y el uso de dichos derivados para la manufactura de un medicamento | |
| MY144132A (en) | Polymorph forms of (2s)-(4e)-n-methyl-5-[3-(5-isoproproxypyridin)yl]-4-penten-2-amine | |
| AP2002002420A0 (en) | Fused pyrrolecarboxamides: gaba brain receptor ligands. | |
| BR0307504A (pt) | Composto ou sal farmaceuticamente aceitável, composição farmacêutica, métodos tratar doenças, para potencializar um efeito terapêutico de um agente para o snc, para melhorar a memória de curto prazo em um paciente, para determinar a presença ou ausência de receptores gabaa em uma amostra, e para alterar a atividade transdutora de sinal do receptor gabaa, embalagem, e, uso de um composto ou sal | |
| BRPI0809873A2 (pt) | "composto, processo para a preparação do composto, método para o tratamento de uma desordem do sistema nervoso central, composição farmacêutica, uso do composto, método para testar antagonistas e antagonistas com seletividade para o receptor 5-th6 e método de tratamento" | |
| Sills et al. | The adenosine A1 receptor agonist N6-cyclopentyladenosine blocks the disruptive effect of phencyclidine on prepulse inhibition of the acoustic startle response in the rat | |
| BRPI0409570A (pt) | derivados de 3-benzidrilideno-8-aza-biciclo[3.2.1]octano com atividade receptora de opióides | |
| Kasahara et al. | The effects of AP521, a novel anxiolytic drug, in three anxiety models and on serotonergic neural transmission in rats | |
| BRPI0412908A (pt) | composto ou um sal deste farmaceuticamente aceitável, composição farmacêutica, métodos para o tratamento de ansiedade, depressão, um distúrbio do sono, distúrbio de déficit de atenção ou demência de alzheimer, para potenciar um efeito terapêutico de um agente do cns, para melhorar a memória de curta duração em um paciente, para alterar a atividade de transdução de sinal de receptor gabaa, e para determinar a presença ou ausência de receptor gabaa em uma amostra, preparação farmacêutica acondicionada, e, uso de um composto ou sal | |
| Onali et al. | N-desmethylclozapine, a major clozapine metabolite, acts as a selective and efficacious δ-opioid agonist at recombinant and native receptors | |
| Peričić | Swim stress inhibits 5-HT2A receptor-mediated head twitch behaviour in mice |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B11A | Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing | ||
| B11Y | Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette] |