申请人:Warner-Lambert Company
公开号:US05066662A1
公开(公告)日:1991-11-19
Oxazolidin-2-ones and 1,2,4-oxadiazolin-5-ones substituted in the 4-position of the oxazolidin-2-one ring and the 3-position of the 1,2,4-oxadiazolin-5-one ring with a 5- or 6-member heteroaromatic, a bicyclic heteroaromatic group or a 5- or 6-member heterocyclic group either directly or via a one or two carbon bridge and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetycholine production or release.
本文描述了在氧唑啉-2-酮环的4位和1,2,4-噁二唑啉-5-酮环的3位上,用5或6元杂环芳基、双环杂环芳基或5或6元杂环基直接或通过一或两个碳桥置换的氧唑啉-2-酮和1,2,4-噁二唑啉-5-酮及其衍生物,以及其制备方法和制药组合物。这些化合物是有用的中枢作用胆碱能药物,可用作镇痛剂治疗疼痛,作为助眠剂,以及用于治疗老年痴呆症、阿尔茨海默病、亨廷顿舞蹈症、迟发性运动障碍、多动症、躁狂症或类似的脑功能不足症状,其特征是脑内乙酰胆碱的产生或释放减少。