Pyridine modulators of acetylcholine receptors

Details Pyridine modulators of acetylcholine receptors Pyridine modulators of acetylcholine receptors

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/44 (2006.01) A61K 31/695 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 413/04 (2006.01) C07D 417/04 (2006.01) C07F 7/08 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2180843

In accordance with the present invention, there is provided a class of pyridine compounds of formula (I) which are modulators of acetylcholine receptors. The compounds of the in- vention displace acetylcholine receptor ligands from their binding sites. In- vention compounds may act as ago- nists partial agonists, antagonists or allosteric modulators of acetylcholine receptors and are useful for a variety of therapeutic applications, such as the treatment of Alzheimer's disease and other disorders involving memory loss and or dementia (including AIDS dementia): disorders of attention and focus (such as attention deficit disorder); disorders of extrapyramidal motor function such as Parkinson's disease, Hunting- ton's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, panic, anxiety and psychosis; substance abuse including withdrawal syndromes and substitution therapy; neuroendocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders of 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 se- cretion and ulcers; pheochromocytoma; cardiovascular dysfunction including hypertension and cardia arrhythmias, comedication in surgical procedures, and the like.

L'invention concerne une classe de composés de pyridine de formule (I) qui constituent des modulateurs des récepteurs de l'acétylcholine. Ces composés déplacent les ligands des récepteurs de l'acétylcholine de leurs sites de liaison. Ils peuvent agir comme agonistes, agonistes partiels, antagonistes ou modulateurs allostériques des récepteurs de l'acétylcholine et conviennent à diverses thérapies telles que les traitements de la maladie d'Alzheimer et d'autres troubles impliquant des pertes de mémoire et/ou la démence (y compris celle due au Sida); des troubles de l'attention et de la concentration (tels que le trouble déficitaire de l'attention); des troubles des fonctions motrices extrapyramidales tels que la maladie de Parkinson, la chorée de Huntington, la maladie de Gilles de la Tourette et les dyskinésies tardives; des troubles de l'humeur et des émotions tels que dépression, panique, anxiété et psychose; l'usage de drogues, y compris les syndromes de sevrage, et dans les thérapies de substitution; des troubles neuro-endocriniens et des dérèglements alimentaires, y compris la boulimie et l'anorexie; des troubles de la nociception et ceux dus à la lutte contre la douleur; des troubles du système nerveux autonome, y compris les dysfonctionnements de la motilité et des fonctions intestinaux, tels que maladie intestinale inflammatoire, syndrome du côlon irritable, diarrhée, constipation, troubles de la sécrétion d'acide gastrique et ulcères; du phéochromocytome; des dysfonctionnements cardiovasculaires, y compris l'hypertension et les arythmies cardiaques; des comédications relatives aux procédures chirurgicales, etc.

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