Novel substituted pyridine compounds useful as modulators of...

C - Chemistry – Metallurgy – 07 – D

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C07D 451/04 (2006.01) A61K 31/44 (2006.01) A61K 31/4439 (2006.01) A61K 31/4545 (2006.01) A61K 31/46 (2006.01) A61P 25/04 (2006.01) A61P 25/16 (2006.01) A61P 25/28 (2006.01) C07D 213/04 (2006.01) C07D 401/02 (2006.01) C07D 401/12 (2006.01) C07D 451/02 (2006.01) C07D 471/08 (2006.01)

Patent

CA 2315941

In accordance with the present invention, a novel class of substituted pyridine compounds, optionally containing ether, ester, amide, ketone or thioether substitutions, that promote the release of ligands involved in neurotransmission have been discovered. The compounds of the present invention are capable of modulating acetylcholine receptors. Therapeutic indications for compounds with activity at acetylcholine receptors include diseases of the central nervous system such as Alzheimer's disease and other diseases involving memory loss and/or dementia, cognitive dysfunction; disorders of extrapyramidal motor function such as Parkinson's disease. Gilles de la Tourette syndrome and tardive dyskinesia, mood and emotional disorders such as depression, anxiety and psychosis, substance abuse including withdrawal symptoms and substitution therapy; neurocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders or nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function such as inflammatory bowel disease, irritable bowel syndrome, diarrhea, constipation, gastric acid secretion and ulcers, pheochromocytoma, cardiovascular dysfunction including hypertension and cardiac arrhythmias, as well as co-medication uses in surgical applications.

La présente invention se rapporte à une nouvelle classe de composés pyridine substitués comportant éventuellement des substitutions éther, ester, amide, cétone ou thioéther, qui favorisent la libération de ligands impliqués dans la neurotransmission. Ces composés peuvent moduler les récepteurs de l'acétylcholine. Parmi les indications thérapeutiques des composés présentant une activité au niveau des récepteurs de l'acétylcholine, on compte les maladies du système nerveux central, telles que la maladie d'Alzheimer et d'autres maladies associées à des pertes de mémoire et/ou à la démence; les dysfonctionnements cognitifs; les troubles de la fonction motrice extrapyramidale tels que la maladie de Parkinson, le syndrome de Gilles de la Tourette et la dyskinésie tardive; les troubles émotionnels et de l'humeur tels que la dépression, l'anxiété et la psychose; la toxicomanie et notamment les symptômes liés au sevrage et la thérapie de remplacement; les troubles de neurocrine et le dérèglement des rations alimentaires, et notamment la boulimie et l'anorexie; les troubles de la perception des stimulations nocives et de la maîtrise de la douleur; les troubles autonomiques et notamment les dysfonctionnements de la fonction et de la motilité gastro-intestinale tels que la maladie intestinale inflammatoire, le syndrome de l'intestin irrité, la diarrhée, la constipation, les sécrétions acides gastriques et les ulcères, le phéochromocytome, le dysfonctionnement cardio-vasculaire et notamment l'hypertension et les arythmies cardiaques. Ces composés peuvent également être utilisés en tant que co-médicaments dans des applications chirurgicales.

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