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1. 发明申请

US20150080576A1 SUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES 审中-公开
标题翻译：亚类型的亚型选择性氨基酸
公开(公告)号：US20150080576A1
公开(公告)日：2015-03-19
申请号：US14551498
申请日：2014-11-24
申请人： Targacept, Inc.
发明人： Anatoly Mazurov , Lan Miao , Yunde Xiao , Philip S. Hammond , Craig H. Miller , Srinivasa Rao Akireddy , Srinivasa V. Murthy , Regina C. Whitaker , Scott R. Breining , Matt S. Melvin
IPC分类号： C07D487/04 , C07D471/08
CPC分类号： C07D487/04 , C07D471/08
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).
摘要翻译：公开了化合物，包括该化合物的药物组合物，及其制备和使用方法。这些化合物是可以由某些杂芳基羧酸和某些二氮杂双环烷烃制备的酰胺化合物。该化合物对中枢神经系统（CNS）中α4和bgr2亚型的神经元烟碱受体表现出选择性并且以高亲和力结合。化合物和组合物可用于治疗和/或预防多种病症或病症，特别是CNS疾病。化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）显示出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不利副作用因为血压和心率的显着增加，对胃肠道的显着的负面影响和对骨骼肌的显着影响）。

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