申请人:BEECHAM GROUP PLC
公开号:EP0154298A2
公开(公告)日:1985-09-11
method for treatment or preventing diarrhoea or ecours which comprises administering to a human or non-human animal in need thereof an effective non toxic amount of a compound of formula (I);
or an N-oxide or pharmaceutically acceptable quaternised derivative or pharmaceutically acceptable salt thereof whereIn R, is hydrogen, C1-7 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl or C1-4 alkyl substituted by C2-7 alkenyl, C2-7 alkynyl, C3-7 cycoalkyl, hydroxy, thiol, C1-4 alkoxy, C1-4 alkylthio, carboxy, C1-4 alkoxycarbonyl, C1-4 alkanoyl, amino optionally substituted by one or two C1-4 alkyl or by C4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C1-4 alkyl, or benzoyl or phenyl either being optionally ring-substituted by C1-4 alkyl, C1-4 alkoxy, halogen or trifluoromethyl, R2 and R3 are the same or different and are hydrogen, hydroxy, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, halogen or trifluoromethyl, m is 1 to 3 and n is 1 or 2, the hydrogen atom bonded to the Ca carbon atom being trans to the hydrogen atom bonded to the Cb carbon atom.
Compounds and compositions for use in the method and for use in the preparation of medicaments are described.
治疗或预防腹泻或溃疡的方法,该方法包括向需要的人或非人 类动物施用有效无毒量的式(I)化合物;
或其 N-氧化物或药学上可接受的季铵化衍生物或药学上可接受的盐 其中 R 是氢、C1-7 烷基、C3-7 环烷基、C4-7 环烯基或被 C2-7 烯基、C2-7 炔基、C3-7 环烷基取代的 C1-4 烷基、羟基、硫醇、C1-4 烷氧基、C1-4 烷硫基、羧基、C1-4 烷氧羰基、C1-4 烷酰基、任选被一个或两个 C1-4 烷基或任选含有一个氧原子或氮原子的 C4-6 聚亚甲基取代的氨基、由一个或两个 C1-4 烷基任选 N 取代的氨基羰基,或由 C1-4 烷基、C1-4 烷氧基、卤素或三氟甲基任选环取代的苯甲酰基或苯基,R2 和 R3 相同或不同,且为氢、羟基、C1-4 烷基、C1-4 烷氧基、C1-4 烷硫基、卤素或三氟甲基,m 为 1 至 3,n 为 1 或 2,与 Ca 碳原子结合的氢原子反式为与 Cb 碳原子结合的氢原子。
描述了用于该方法和用于制备药物的化合物和组合物。