申请人:Allen & Hanburys Limited
公开号:US04101579A1
公开(公告)日:1978-07-18
Compounds of the general formula I and physiologically acceptable acid addition salts thereof:- ##STR1## in which R.sup.1 is a lower alkyl, lower alkenyl, or arylalkyl radical, which radicals may optionally be substituted by one or more alkoxy or hydroxy groups. R.sup.2 represents a hydrogen atom or a lower alkyl radical which may optionally be substituted by one or more hydroxy groups, amino groups, or heterocyclic rings containing one or more heteroatoms, or R.sup.2 represents a cycloalkyl, arylalkyl or aryloxyalkyl radical, which radicals may optionally be substituted by one or more alkoxy or hydroxy groups; R.sup.3 represents a hydrogen atom or a benzyl group; X represents a group of formula --CONR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 may be the same or different and each represents hydrogen or a lower alkyl group; With the proviso that when R.sup.2 is tertiary butyl and R.sup.1 is a benzyl group, R.sup.3 represents a hydrogen atom. The compounds have a blocking action on .beta.-adrenergic receptors and in some cases an antagonising effect on .alpha.-adrenergic receptors.
通式I和其生理学上可接受的酸盐包括以下化合物:- ##STR1## 其中R.sup.1是较低的烷基、较低的烯基或芳基烷基基团,这些基团可能被一个或多个烷氧基或羟基取代。R.sup.2代表氢原子或一个较低的烷基基团,该基团可能被一个或多个羟基、氨基或含有一个或多个杂原子的杂环的环取代,或者R.sup.2代表一个环烷基、芳基烷基或芳氧基烷基基团,这些基团可能被一个或多个烷氧基或羟基取代;R.sup.3代表氢原子或苄基;X代表一个公式--CONR.sup.4 R.sup.5的基团,其中R.sup.4和R.sup.5可以相同也可以不同,每个代表氢或较低的烷基基团;但有一个条件,即当R.sup.2是叔丁基且R.sup.1是苄基时,R.sup.3代表氢原子。这些化合物对β-肾上腺素受体具有阻断作用,并在某些情况下对α-肾上腺素受体具有拮抗作用。