Membrane stabilizing compounds having beta-receptor blocking activity, their preparation, method for treatment of arrhythmic conditions, and pharmaceutical preparations containing same
申请人:Aktiebolaget Hässle
公开号:EP0007294A2
公开(公告)日:1980-01-23
TThe present invention relates to new potent membrane stabilizing compounds of the formula
wherein R1 is alkoxyalkyl. hydroxyalkyl or alkyl, which alkyl groups may be branched or straight, R2 is halogen or hyd- rogsn, R3 is hydrogen or alkyl, R4 and R5 are sams or different and are each hydrogen, sikoxy, alkyl, alkoxyalkyl, cyano, or hydroxy, n is 0, 1, 2, or 3. and X is -O-, -CHr. or .
The present pounds are potent heart antiarrhythmic agents possessing membrane stabilizing effect and β-recsptor blocking effect in same clinical doses. The compounds are used In treating antiarrhythmic conditions. but can also be used in the trestment of hypertension. angina pectoris, or nervous heart The invention also relates to processes for preparing the compounds, method of treating anti- arrhythmic conditions and pharmaceutical preparations con- taining said compounds.
本发明涉及新的强效膜稳定化合物,其式为
其中 R1 是烷氧基烷基、羟基烷基或烷基,其中烷基可以是支链或直链;R2 是卤素或水基;R3 是氢或烷基;R4 和 R5 是相同或不同的,并且各自是氢、烷氧基、烷基、烷氧基烷基、氰基或羟基;n 是 0、1、2 或 3;X 是 -O-、-CHr 或 。
本化合物是强效的心脏抗心律失常药物,在相同的临床剂量下,具有膜稳定作用和 β-抑制剂阻断作用。本发明还涉及制备本发明化合物的工艺、治疗抗心律失常的方法以及含有本发明化合物的药物制剂。