申请人:SYNTEX (U.S.A.) INC.
公开号:EP0467325A2
公开(公告)日:1992-01-22
Carbostyril derivatives of Formula I:
wherein:
m is 0, 1, or 2;
n is 0, 1, or 2;
R1 is hydrogen or lower alkyl;
R2 is hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, aralkoxy, or acyloxy;
R3 is hydrogen, halogen, lower alkyl, or lower alkoxy;
R4 is hydrogen, hydroxy, lower alkyl, or acyloxy,
provided that when R4 is hydroxy or acyloxy, m and n are both 1;
R5 is hydrogen or lower alkyl; and R6 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, and their formulations are also disclosed.
式 I 的
喹诺酮衍
生物:
其中
m 是 0、1 或 2
n 是 0、1 或 2
R1 是
氢或低级烷基
R2 是
氢、卤素、羟基、低级烷基、低级烷
氧基、芳基
氧基或酰
氧基;
R3 是
氢、卤素、低级烷基或低级烷
氧基;
R4 是
氢、羟基、低级烷基或酰
氧基、
但当 R4 为羟基或酰
氧基时,m 和 n 均为 1;
R5 是
氢或低级烷基;R6 是烷基、羟基烷基、烷
氧基烷基或(二烷基
氨基)烷基;
及其药学上可接受的酸加成盐和 N-
氧化物(
碳氮基),以及含有它们的组合物,可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、化合物及其制剂的方法。