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.
式子为##STR1##其中R.sub.1选自氢、甲基、乙基和丙基的群组,R.sub.2选自甲基、乙基、氯、甲氧基和乙氧基的群组,R.sub.3选自氢和甲基的群组,R.sub.4选自氢、甲基和C.sub.1-C.sub.4烷氧基的群组,R.sub.6选自甲基、乙基、氯、甲氧基和乙氧基的群组,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,条件是(a)当n为0时,R.sub.8也可以是甲基;(b)当n为1时,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均为氢,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。已发现这种化合物是有效的长效心脏抗心律失常药物,特别是通过口服途径给予。