Substituted pyrrolidine cardiovascular system regulators and antihypertensives, their preparation and use
申请人:SYNTEX (U.S.A.) INC.
公开号:EP0071399A2
公开(公告)日:1983-02-09
Compounds of the formula:
and the pharmaceutically acceptable acid addition salts thereof, wherein:
each X is indeoendently selected from
-F, -R1, -OR. -S(O)dR', -CONHR, -NHR, -CH2OR, -CN, -NHCONHR, -NHCSNHR, -NHCOR', -SO2NHR, -NHSO2R1, and -NHCO2R wherein R is either hydrogen or lower alkyl wherein lower alkyl is defined as a straight or branched hydrocarbon chain of 1-4 carbon atoms, R' is lower alkyl wherein alkyl is as defined above and d is 0, 1, or 2, or two Xs taken together are -OCH2O-;
each Y is independently selected from the same group as set forth for X;
B is hydrogen or hydroxyl;
a is 0, 1, or 2;
b is 0, 1, or 2;
c is 0, 1, 2 or 3; are useful as regulators of the cardiovascular system and are also bronchodilators.
式化合物
及其药学上可接受的酸加成盐,其中
每个 X 不可重复地选自
-F、-R1、-OR.-S(O)dR'、-CONHR、-NHR、-CH2OR、-CN、-NHCONHR、-NHCSNHR、-NHCOR'、-SO2NHR、-NHSO2R1 和 -NHCO2R,其中 R 是氢或低级烷基,其中低级烷基定义为 1-4 个碳原子的直链或支链烃链,R'是低级烷基,其中烷基定义如上,d 是 0、1 或 2,或两个 X 合在一起是 -OCH2O-;
每个 Y 独立地选自与 X 相同的组;
B 是氢或羟基;
a 是 0、1 或 2
b 是 0、1 或 2
c 是 0、1、2 或 3;可作为心血管系统的调节剂,也是支气管扩张剂。