申请人:Banyu Pharmaceutical Co Ltd
公开号:US06140333A1
公开(公告)日:2000-10-31
The invention relates to compounds represented by the general formula [I] ##STR1## [wherein Ar means an aryl group or a heteroaryl group which may have a substitutive group selected from a group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group; R.sup.1 means a C.sub.3 -C.sub.6 cycloalkyl group which is substitutable with a fluorine atom; R.sup.2 and R.sup.4 mean hydrogen atoms, groups represented by --(A.sup.1).sub.m --NH--B or the like; R.sup.3 and R.sup.5 mean hydrogen atoms, C.sub.1 -C.sub.6 aliphatic hydrocarbon groups or the like which are substitutable with a lower alkyl group(s); n means 0 or 1; and X means an oxygen atom or a sulfur atom]. Compounds according to the invention, since they not only have potent selective antagonistic activity against muscarinic M.sub.3 receptors but also exhibit excellent oral activity, durability of action and pharmacokinetics, are very useful as safe and effective remedies against respiratory, urinary and digestive diseases with little adverse side effects.
该发明涉及由通式[I]表示的化合物 ##STR1## [其中Ar表示芳基或杂环基,可能具有从卤原子、较低烷基基团和较低烷氧基团中选择的取代基; R.sup.1表示可用氟原子取代的C.sub.3-C.sub.6环烷基基团; R.sup.2和R.sup.4表示氢原子,表示为--(A.sup.1).sub.m--NH--B或类似基团; R.sup.3和R.sup.5表示氢原子,可用较低烷基基团取代的C.sub.1-C.sub.6脂肪烃基团或类似基团; n表示0或1; X表示氧原子或硫原子]。根据该发明的化合物,由于它们不仅具有对M.sub.3胆碱能受体具有强效选择性拮抗活性,而且表现出优异的口服活性、持久作用和药代动力学特性,因此在对抗呼吸、泌尿和消化系统疾病时非常有用,且副作用很小,是安全有效的药物。