DE69314024T2 - NEUE GABAa-REZEPTORSUBTYPEN UND VERFAHREN ZUM SCREENING VON ARZNEIMITTELVERBINDUNGEN UNTER VERWENDUNG VON GABAa-REZEPTORSUBTYPEN BINDENDE IMIDAZOCHINOXALINE UND PYRROLOPYRIMIDINE - Google Patents
NEUE GABAa-REZEPTORSUBTYPEN UND VERFAHREN ZUM SCREENING VON ARZNEIMITTELVERBINDUNGEN UNTER VERWENDUNG VON GABAa-REZEPTORSUBTYPEN BINDENDE IMIDAZOCHINOXALINE UND PYRROLOPYRIMIDINEInfo
- Publication number
- DE69314024T2 DE69314024T2 DE69314024T DE69314024T DE69314024T2 DE 69314024 T2 DE69314024 T2 DE 69314024T2 DE 69314024 T DE69314024 T DE 69314024T DE 69314024 T DE69314024 T DE 69314024T DE 69314024 T2 DE69314024 T2 DE 69314024T2
- Authority
- DE
- Germany
- Prior art keywords
- receptor subtypes
- gabaa receptor
- binding
- imidazochinoxaline
- pyrrolopyrimidine
- 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.)
- Expired - Fee Related
Links
- 102000027484 GABAA receptors Human genes 0.000 title abstract 3
- 108091008681 GABAA receptors Proteins 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- 230000027455 binding Effects 0.000 title abstract 2
- 238000009739 binding Methods 0.000 title abstract 2
- 238000012216 screening Methods 0.000 title abstract 2
- YELMWJNXDALKFE-UHFFFAOYSA-N 3h-imidazo[4,5-f]quinoxaline Chemical compound N1=CC=NC2=C(NC=N3)C3=CC=C21 YELMWJNXDALKFE-UHFFFAOYSA-N 0.000 title 1
- KDOPAZIWBAHVJB-UHFFFAOYSA-N 5h-pyrrolo[3,2-d]pyrimidine Chemical compound C1=NC=C2NC=CC2=N1 KDOPAZIWBAHVJB-UHFFFAOYSA-N 0.000 title 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/94—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving narcotics or drugs or pharmaceuticals, neurotransmitters or associated receptors
- G01N33/9406—Neurotransmitters
- G01N33/9426—GABA, i.e. gamma-amino-butyrate
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/28—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
- G01N33/566—Immunoassay; Biospecific binding assay; Materials therefor using specific carrier or receptor proteins as ligand binding reagents where possible specific carrier or receptor proteins are classified with their target compounds
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/94—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving narcotics or drugs or pharmaceuticals, neurotransmitters or associated receptors
- G01N33/948—Sedatives, e.g. cannabinoids, barbiturates
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2500/00—Screening for compounds of potential therapeutic value
- G01N2500/20—Screening for compounds of potential therapeutic value cell-free systems
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Food Science & Technology (AREA)
- Pharmacology & Pharmacy (AREA)
- Analytical Chemistry (AREA)
- Biochemistry (AREA)
- Physics & Mathematics (AREA)
- General Physics & Mathematics (AREA)
- Biotechnology (AREA)
- Cell Biology (AREA)
- Pathology (AREA)
- Microbiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Anesthesiology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US07/876,050 US5597920A (en) | 1992-04-30 | 1992-04-30 | Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes |
| PCT/US1993/003920 WO1993022681A1 (en) | 1992-04-30 | 1993-04-30 | NOVEL GABAa RECEPTOR SUBTYPES AND METHODS FOR SCREENING DRUG COMPOUNDS USING IMIDAZOQUINOXALINES AND PYRROLOPYRIMIDINES TO BIND TO GABAa RECEPTOR SUBTYPES |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE69314024D1 DE69314024D1 (de) | 1997-10-23 |
| DE69314024T2 true DE69314024T2 (de) | 1998-04-16 |
Family
ID=25366890
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE69314024T Expired - Fee Related DE69314024T2 (de) | 1992-04-30 | 1993-04-30 | NEUE GABAa-REZEPTORSUBTYPEN UND VERFAHREN ZUM SCREENING VON ARZNEIMITTELVERBINDUNGEN UNTER VERWENDUNG VON GABAa-REZEPTORSUBTYPEN BINDENDE IMIDAZOCHINOXALINE UND PYRROLOPYRIMIDINE |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US5597920A (de) |
| EP (1) | EP0639275B1 (de) |
| JP (1) | JPH08500333A (de) |
| KR (1) | KR950702032A (de) |
| AT (1) | ATE158414T1 (de) |
| AU (1) | AU691470B2 (de) |
| CA (1) | CA2134227A1 (de) |
| DE (1) | DE69314024T2 (de) |
| DK (1) | DK0639275T3 (de) |
| ES (1) | ES2110090T3 (de) |
| GR (1) | GR3025698T3 (de) |
| WO (1) | WO1993022681A1 (de) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6010861A (en) * | 1994-08-03 | 2000-01-04 | Dgi Biotechnologies, Llc | Target specific screens and their use for discovering small organic molecular pharmacophores |
| DE69715231T2 (de) * | 1996-10-25 | 2003-05-22 | Neurosearch As Ballerup | Methode zur identifizierung von verbindungen mit anxiolytischem potential |
| US6737242B1 (en) | 1999-05-07 | 2004-05-18 | Neurogen Corporation | Methods for screening GABA-modulatory compounds for specified pharmacological activities |
| BR0010344A (pt) * | 1999-05-07 | 2002-02-19 | Neurogen Corp | Métodos para examinar uma pluralidade de compostos para examinar compostos quanto à atividade de melhora cognitiva, para prover uma preparação farmacêutica a pacientes, para examinar uma pluralidade de compostos para a atividade de melhora de cognição, para examinar compostos quanto à atividade hipnótica, para examinar compostos tendo atividade ansiolìtica, para examinar compostos quanto à atividade antidepressiva e para prover compostos farmacêuticos a pacientes |
| ZA200301703B (en) * | 2000-09-15 | 2004-03-02 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors. |
| SI1318997T1 (sl) * | 2000-09-15 | 2006-12-31 | Vertex Pharma | Pirazolne spojine, uporabne kot inhibitorji protein-kinaze |
| US7473691B2 (en) | 2000-09-15 | 2009-01-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| DE60128709T2 (de) * | 2000-09-15 | 2007-12-27 | Vertex Pharmaceuticals Inc., Cambridge | Triazol-verbindungen als protein-kinase-inhibitoren |
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| KR100947185B1 (ko) | 2000-12-21 | 2010-03-15 | 버텍스 파마슈티칼스 인코포레이티드 | 단백질 키나제 억제제로서 유용한 피라졸 화합물 및 이를 포함하는 조성물 |
| DE60332604D1 (de) | 2002-03-15 | 2010-07-01 | Vertex Pharma | Azolylaminoazine als proteinkinasehemmer |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| CA2494100C (en) | 2002-08-02 | 2011-10-11 | Vertex Pharmaceuticals Incorporated | Pyrazole compositions useful as inhibitors of gsk-3 |
| NZ594385A (en) | 2005-11-03 | 2013-02-22 | Vertex Pharma | Aminopyrimidines useful as kinase inhibitors |
| MX2009011810A (es) | 2007-05-02 | 2010-01-14 | Vertex Pharma | Tiazoles y pirazoles utiles como inhibidores de cinasa. |
| WO2009018415A1 (en) | 2007-07-31 | 2009-02-05 | Vertex Pharmaceuticals Incorporated | Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof |
| EP2323622A1 (de) | 2008-09-03 | 2011-05-25 | Vertex Pharmaceuticals Incorporated | Co-kristalle und diese enthaltende pharmazeutische formulierungen |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2415303A1 (fr) * | 1978-05-31 | 1979-08-17 | Ferrosan As | Procede pour la determination de la concentration de benzodiazepines dans un fluide de l'organisme |
| IL90315A0 (en) * | 1988-06-01 | 1989-12-15 | Ferrosan As | Imidazoquinoxaline compounds,their preparation and pharmaceutical compositions containing them |
| US5185446A (en) * | 1990-09-04 | 1993-02-09 | Neurogen Corporation | Certain cycloalkyl imidazopyrimidines; a new class of gaba brainreceptor ligands |
| AU652968B2 (en) * | 1990-10-09 | 1994-09-15 | Neurogen Corporation | Certain cycloalkyl and azacycloalkyl pyrrolopyrimidines; a new class of gaba brain receptor ligands |
| US5130430A (en) * | 1990-10-31 | 1992-07-14 | Neurogen Corporation | 2-substituted imidazoquinoxaline diones, a new class of gaba brain receptor ligands |
| WO1994025463A1 (en) * | 1992-04-08 | 1994-11-10 | Neurogen Corporation | Certain aryl fused pyrrolopyrimidines; a new class of gaba brain receptor ligands |
-
1992
- 1992-04-30 US US07/876,050 patent/US5597920A/en not_active Expired - Fee Related
-
1993
- 1993-04-30 WO PCT/US1993/003920 patent/WO1993022681A1/en active IP Right Grant
- 1993-04-30 DE DE69314024T patent/DE69314024T2/de not_active Expired - Fee Related
- 1993-04-30 AT AT93910819T patent/ATE158414T1/de not_active IP Right Cessation
- 1993-04-30 DK DK93910819.7T patent/DK0639275T3/da active
- 1993-04-30 US US08/331,501 patent/US5688654A/en not_active Expired - Fee Related
- 1993-04-30 JP JP5519445A patent/JPH08500333A/ja active Pending
- 1993-04-30 AU AU41177/93A patent/AU691470B2/en not_active Ceased
- 1993-04-30 ES ES93910819T patent/ES2110090T3/es not_active Expired - Lifetime
- 1993-04-30 CA CA002134227A patent/CA2134227A1/en not_active Abandoned
- 1993-04-30 KR KR1019940703877A patent/KR950702032A/ko not_active Application Discontinuation
- 1993-04-30 EP EP93910819A patent/EP0639275B1/de not_active Expired - Lifetime
-
1997
- 1997-12-17 GR GR970403349T patent/GR3025698T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU4117793A (en) | 1993-11-29 |
| CA2134227A1 (en) | 1993-11-11 |
| WO1993022681A1 (en) | 1993-11-11 |
| GR3025698T3 (en) | 1998-03-31 |
| DK0639275T3 (da) | 1998-04-14 |
| US5688654A (en) | 1997-11-18 |
| ES2110090T3 (es) | 1998-02-01 |
| KR950702032A (ko) | 1995-05-17 |
| AU691470B2 (en) | 1998-05-21 |
| EP0639275B1 (de) | 1997-09-17 |
| US5597920A (en) | 1997-01-28 |
| DE69314024D1 (de) | 1997-10-23 |
| ATE158414T1 (de) | 1997-10-15 |
| EP0639275A1 (de) | 1995-02-22 |
| JPH08500333A (ja) | 1996-01-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8364 | No opposition during term of opposition | ||
| 8339 | Ceased/non-payment of the annual fee |