申请人:Sibia Neurosciences, Inc.
公开号:US05585388A1
公开(公告)日:1996-12-17
In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites. Invention compounds may act as agonists, 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, Huntington'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 secretion and ulcers; pheochromocytoma; cardiovascular dysfunction including hypertension and cardia arrhythmias, comedication in surgical procedures, and the like.
根据本发明,提供了一类吡啶化合物,这些化合物是乙酰胆碱受体的调节剂。该发明的化合物将乙酰胆碱受体配体从其结合位点上置换。发明的化合物可能作为乙酰胆碱受体的激动剂、部分激动剂、拮抗剂或变构调节剂,并且可用于各种治疗应用,如治疗阿尔茨海默病和其他涉及记忆丧失和/或痴呆的疾病(包括艾滋病痴呆);注意力和专注障碍(如注意力缺陷障碍);外囊运动功能障碍,如帕金森病、亨廷顿病、吉尔-德-拉-图雷特综合征和迟发性运动障碍;情绪和情感障碍,如抑郁症、恐慌、焦虑和精神病;物质滥用,包括戒断综合征和替代疗法;神经内分泌障碍和食物摄入失调,包括暴食症和厌食症;疼痛感知和疼痛控制障碍;自主神经障碍,包括胃肠动力功能和功能障碍,如炎症性肠病、肠易激综合征、腹泻、便秘、胃酸分泌和溃疡;嗜铬细胞瘤;心血管功能障碍,包括高血压和心律失常,手术程序中的联合用药等。