申请人:Banyu Pharmaceutical Co., Ltd.
公开号:US05750540A1
公开(公告)日:1998-05-12
This invention provides novel 1,4-di-substituted piperidine derivatives of the general formula \x9bI! ##STR1## and the pharmaceutically acceptable salts thereof, wherein: Ar represents a phenyl group or a five- or six-membered heteroaromatic group having one or two hetero atoms selected from the group consisting of an oxygen atom, a sulfur atom and a nitrogen atom in which one or two optional hydrogen atoms on the ring may be replaced by substituent groups selected from the group consisting of a halogen atom and a lower alkyl group; R.sup.1 represents a cycloalkyl group of 3 to 6 carbon atoms or a cycloalkenyl group of 3 to 6 carbon atoms; R.sup.2 represents a saturated or unsaturated aliphatic hydrocarbon radical of 5 to 15 carbon atoms; and X represents O or NH. These compounds have selective antagonistic activity against the muscarinic M.sub.3 receptors and can hence be used safely with a minimum of side effects.
该发明提供了一种新型的1,4-二取代哌啶衍生物,其通式为##STR1##及其药学上可接受的盐,其中:Ar代表苯基或含有一个或两个异原子(选自氧原子、硫原子和氮原子)的五元或六元杂环芳基,环上的一个或两个可选氢原子可被卤素原子和较低的烷基基团替代;R1代表3到6个碳原子的环烷基基团或3到6个碳原子的环烯烃基团;R2代表5到15个碳原子的饱和或不饱和脂肪烃基团;X代表O或NH。这些化合物对M.sub.3胆碱能受体具有选择性拮抗活性,因此可以安全地使用,并具有最少的副作用。