申请人:Astra Pharmaceutical Products, Inc.
公开号:US04218477A1
公开(公告)日:1980-08-19
Primary amino acylanilides of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, methyl, ethyl and propyl, R.sub.2 is selected from the group consisting of methyl, ethyl, chlorine, methoxy and ethoxy, R.sub.3 is selected from the group consisting of hydrogen and methyl, R.sub.4 is selected from the group consisting of hydrogen, methyl, and a C.sub.1 -C.sub.4 alkoxy group, R.sub.6 is selected from the group consisting of methyl, ethyl, chlorine, methoxy and ethoxy, R.sub.7 is hydrogen, methyl or ethyl, R.sub.8 is hydrogen, R.sub.9 is hydrogen, methyl or ethyl, R.sub.10 is hydrogen, and n is 0 or 1, with the provisions that (a) when n is 0, R.sub.8 can also be methyl; (b) when n is 1, and R.sub.7 is hydrogen, and R.sub.9 is hydrogen or methyl, then R.sub.10 can also be methyl; (c) when R.sub.1 is hydrogen, R.sub.2 is methyl, R.sub.3 is hydrogen, R.sub.6 is methyl, R.sub.7 is hydrogen, R.sub.8 is hydrogen, and n is 0, then R.sub.4 can be ethoxy or propoxy only; (d) when R.sub.1 is hydrogen, R.sub.2 is methyl, R.sub.3, R.sub.4, R.sub.7 and R.sub.8 are hydrogen, and n is 0, then R.sub.6 is methoxy, ethoxy, or ethyl only; and the therapeutically acceptable salts thereof. Compounds of this type have been found to be effective longlasting cardiac antiarrhythmic agents, especially when administered by the oral route.
主要氨基酰基苯胺的结构式为##STR1##其中R.sub.1从氢、甲基、乙基和丙基中选择,R.sub.2从甲基、乙基、氯、甲氧基和乙氧基中选择,R.sub.3从氢和甲基中选择,R.sub.4从氢、甲基和C.sub.1 -C.sub.4烷氧基中选择,R.sub.6从甲基、乙基、氯、甲氧基和乙氧基中选择,R.sub.7为氢、甲基或乙基,R.sub.8为氢,R.sub.9为氢、甲基或乙基,R.sub.10为氢,n为0或1,具体规定如下:(a)当n为0时,R.sub.8也可以是甲基;(b)当n为1且R.sub.7为氢,R.sub.9为氢或甲基时,R.sub.10也可以是甲基;(c)当R.sub.1为氢,R.sub.2为甲基,R.sub.3为氢,R.sub.6为甲基,R.sub.7为氢,R.sub.8为氢,n为0时,R.sub.4只能是乙氧基或丙氧基;(d)当R.sub.1为氢,R.sub.2为甲基,R.sub.3、R.sub.4、R.sub.7和R.sub.8为氢,n为0时,R.sub.6只能是甲氧基、乙氧基或乙基;以及其治疗上可接受的盐。已发现这类化合物在口服给药时,特别是作为长效心脏抗心律失常药物,具有良好的疗效。