CA2386149A1 - Sites allosteriques sur des recepteurs muscariniques - Google Patents
Sites allosteriques sur des recepteurs muscariniques Download PDFInfo
- Publication number
- CA2386149A1 CA2386149A1 CA002386149A CA2386149A CA2386149A1 CA 2386149 A1 CA2386149 A1 CA 2386149A1 CA 002386149 A CA002386149 A CA 002386149A CA 2386149 A CA2386149 A CA 2386149A CA 2386149 A1 CA2386149 A1 CA 2386149A1
- Authority
- CA
- Canada
- Prior art keywords
- binding
- compound
- nms
- muscarinic receptor
- allosteric
- 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.)
- Abandoned
Links
Classifications
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- 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
- G01N33/944—Acetylcholine
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- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- 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
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
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- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
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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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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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
- A61P25/20—Hypnotics; Sedatives
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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
- A61P25/22—Anxiolytics
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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
- A61P25/24—Antidepressants
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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
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Molecular Biology (AREA)
- Diabetes (AREA)
- Ophthalmology & Optometry (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- General Physics & Mathematics (AREA)
- Cardiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Biotechnology (AREA)
- Cell Biology (AREA)
- Anesthesiology (AREA)
- Microbiology (AREA)
Abstract
L'invention concerne un site sur des récepteurs muscariniques et son utilisation dans le but de cribler des composés capables de moduler la liaison d'un ligand primaire tel que l'acétycholine au récepteur. Ce site est caractérisé ici par une série d'indolocarbazoles représentés par la formule générale (1) et un série de composés associés représentés par la formule générale (2). Ces composés sont capables de se fixer sur le site allostérique pour moduler la liaison d'un ligand primaire sur des récepteurs, offrant une coopérativité et une sélectivité positives, négatives et neutres pour les sous-types de récepteurs muscariniques.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB9924962.5 | 1999-10-21 | ||
GBGB9924962.5A GB9924962D0 (en) | 1999-10-21 | 1999-10-21 | Allosteric sites on muscarinic receptors |
PCT/GB2000/004064 WO2001029036A2 (fr) | 1999-10-21 | 2000-10-20 | Sites allosteriques sur des recepteurs muscariniques |
Publications (1)
Publication Number | Publication Date |
---|---|
CA2386149A1 true CA2386149A1 (fr) | 2001-04-26 |
Family
ID=10863158
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA002386149A Abandoned CA2386149A1 (fr) | 1999-10-21 | 2000-10-20 | Sites allosteriques sur des recepteurs muscariniques |
Country Status (6)
Country | Link |
---|---|
EP (1) | EP1222463A2 (fr) |
JP (1) | JP2003512607A (fr) |
AU (1) | AU779391B2 (fr) |
CA (1) | CA2386149A1 (fr) |
GB (1) | GB9924962D0 (fr) |
WO (1) | WO2001029036A2 (fr) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2004084889A1 (fr) * | 2003-03-28 | 2004-10-07 | Pfizer Inc. | Utilisation de l'inhibiteur de la proteinekinase c pour supprimer l'excitation postsynaptique lente soutenue (sspe) de neurones enteriques |
DK1807434T3 (da) * | 2004-10-25 | 2010-11-22 | Lilly Co Eli | Thienopyridiner som allosteriske potentiatorer af M4- muscarinreceptoren |
WO2007002670A2 (fr) * | 2005-06-28 | 2007-01-04 | Bausch & Lomb Incorporated | Procede pour faire baisser la pression intraoculaire |
WO2008063888A2 (fr) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Composés modulant l'activité de c-fms et/ou de c-kit et utilisations associées |
WO2009012283A1 (fr) | 2007-07-17 | 2009-01-22 | Plexxikon Inc. | Composés et procédés pour la modulation des kinases et leurs indications |
SG173178A1 (en) | 2009-04-03 | 2011-09-29 | Hoffmann La Roche | Propane- i-sulfonic acid {3- [5- (4 -chloro-phenyl) -1h-pyrrolo [2, 3-b] pyridine-3-carbonyl] -2, 4-difluoro-pheny l } -amide compositions and uses thereof |
NZ629615A (en) | 2009-11-06 | 2016-01-29 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
EA028821B9 (ru) | 2011-02-07 | 2018-10-31 | Плексксикон, Инк. | Соединения и способы для модуляции киназ, а также показания к их применению |
TWI558702B (zh) | 2011-02-21 | 2016-11-21 | 普雷辛肯公司 | 醫藥活性物質的固態形式 |
US9150570B2 (en) | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5747336A (en) * | 1988-09-08 | 1998-05-05 | The United States Of America As Represented By The Department Of Health And Human Services | Cloned human genes for muscarinic acetylcholine receptors and cells lines expressing same |
US5756494A (en) * | 1992-07-24 | 1998-05-26 | Cephalon, Inc. | Protein kinase inhibitors for treatment of neurological disorders |
GB2292685A (en) * | 1994-07-27 | 1996-03-06 | Sankyo Co | Allosteric effectors at muscarinic receptors |
NZ290199A (en) * | 1994-07-27 | 1999-06-29 | Sankyo Co | Nitrogen containing heterocyclic compounds, selective allosteric effectors to regulate m1 receptors |
EP0711556A1 (fr) * | 1994-11-09 | 1996-05-15 | Ciba-Geigy Ag | Solutions intraveineuses contenant des dérivés de staurosporine |
US5677327A (en) * | 1995-06-22 | 1997-10-14 | Allergan | Method for identifying muscarinic agents lacking miotic side effects |
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1999
- 1999-10-21 GB GBGB9924962.5A patent/GB9924962D0/en not_active Ceased
-
2000
- 2000-10-20 WO PCT/GB2000/004064 patent/WO2001029036A2/fr not_active Application Discontinuation
- 2000-10-20 AU AU10383/01A patent/AU779391B2/en not_active Ceased
- 2000-10-20 CA CA002386149A patent/CA2386149A1/fr not_active Abandoned
- 2000-10-20 JP JP2001531835A patent/JP2003512607A/ja active Pending
- 2000-10-20 EP EP00971543A patent/EP1222463A2/fr not_active Withdrawn
Also Published As
Publication number | Publication date |
---|---|
WO2001029036A2 (fr) | 2001-04-26 |
AU779391B2 (en) | 2005-01-20 |
WO2001029036A3 (fr) | 2002-05-10 |
GB9924962D0 (en) | 1999-12-22 |
AU1038301A (en) | 2001-04-30 |
EP1222463A2 (fr) | 2002-07-17 |
JP2003512607A (ja) | 2003-04-02 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FZDE | Dead |