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1. 发明授权

US06303638B1 Substituted pyridines as modulators of the mammalian neuronal nicotinic acetylcholine receptor 失效
标题翻译：取代的吡啶作为哺乳动物神经元烟碱乙酰胆碱受体的调节剂
公开(公告)号：US06303638B1
公开(公告)日：2001-10-16
申请号：US09372114
申请日：1999-08-20
申请人： Bachir Latli , John E. Casida
发明人： Bachir Latli , John E. Casida
IPC分类号： C07D41706
CPC分类号： C07D401/06 , C07D413/06 , C07D417/06
摘要： Novel compounds are provided that modulate the neuronal nicotinic acetylcholine receptor (nAChR), particularly the mammalian nAChR (m-nAChR). The compounds are substituted pyridine derivatives such as analogs of 1-[(6-chloro-3-pyridinyl)methyl]-2-imidazolidine and 1-[(6-chloro-3-pyridinyl)methyl]-2-iminothiazole. Methods of using the novel m-nAChR modulators are also provided, including methods of using the compounds as m-nAChR probes and as therapeutic agents to treat mammalian individuals suffering from conditions, disorders or diseases that are responsive to administration of an m-nAChR modulator. The compounds are useful in treating (1) CNS disorders such as Alzheimer's disease, AIDS-associated dementia, Tourette's Syndrome, attention deficit disorder, and attention deficit disorder, (2) inflammation and inflammatory diseases, (3) conditions caused by or associated with smooth muscle contractions, and (4) withdrawal symptoms associated with cessation of chemical substance abuse. The compounds are also useful as non-opiate analgesics, to treat mild, moderate or severe pain. Pharmaceutical formulations containing an m-nAChR modulator of the invention are provided as well.
摘要翻译：提供调节神经元烟碱乙酰胆碱受体（nAChR），特别是哺乳动物nAChR（m-nAChR）的新型化合物。化合物是取代的吡啶衍生物，例如1 - [（6-氯-3-吡啶基）甲基] -2-咪唑烷和1 - [（6-氯-3-吡啶基）甲基] -2-亚氨基噻唑的类似物。还提供了使用新的m-nAChR调节剂的方法，包括使用化合物作为m-nAChR探针和作为治疗剂治疗患有对施用m-nAChR调节物的病症，病症或疾病的哺乳动物个体的方法。该化合物可用于治疗（1）中枢神经系统疾病如阿尔茨海默病，艾滋病相关性痴呆，图雷特综合征，注意缺陷障碍和注意力缺陷障碍，（2）炎症和炎性疾病，（3）由或由平滑肌收缩，和（4）与化学物质滥用停止相关的戒断症状。这些化合物也可用作非阿片类止痛药，用于治疗轻度，中度或重度疼痛。还提供含有本发明的m-nAChR调节剂的药物制剂。

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