申请人:Syntex (U.S.A.) Inc.
公开号:US05082847A1
公开(公告)日:1992-01-21
Carbostyril derivatives of Formula I: ##STR1## wherein: m is 0, 1, or 2; n is 0, 1, or 2; R.sup.1 is hydrogen or lower alkyl; R.sup.2 is hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, aralkoxy, or acyloxy; R.sup.3 is hydrogen, halogen, lower alkyl, or lower alkoxy; R.sup.4 is hydrogen, hydroxy, lower alkyl, acyloxy, provided that when R.sup.4 is hydroxy or acyloxy, m and n are both 1; R.sup.5 is hydrogen or lower alkyl; and R.sup.6 is alkyl, hydroxyalkyl, alkoxyalkyl, or (dialkylamino)alkyl; and the pharmaceutically acceptable acid addition salts and N-oxides (at the carbostyril nitrogen) thereof, and compositions containing them, are useful in treating cardiovascular diseases, particularly arrhythmias. Methods of preparing intermediates, the compounds, their formulations and methods of treatment therewith are also disclosed.
化合物I的Carbostyril衍生物:##STR1## 其中:m为0、1或2;n为0、1或2;R.sup.1为氢或低碳基;R.sup.2为氢、卤素、羟基、低碳基、低烷氧基、芳基氧基或酰氧基;R.sup.3为氢、卤素、低碳基或低烷氧基;R.sup.4为氢、羟基、低碳基、酰氧基,但当R.sup.4为羟基或酰氧基时,m和n都为1;R.sup.5为氢或低碳基;R.sup.6为烷基、羟基烷基、烷氧基烷基或(二烷基氨基)烷基;以及在其carbostyril氮原子处的药学上可接受的酸加成盐和N-氧化物,以及包含它们的组合物,用于治疗心血管疾病,特别是心律失常。还公开了制备中间体、化合物、它们的配方和治疗方法。