申请人:THE UNIVERSITY OF MELBOURNE
公开号:US20030216477A1
公开(公告)日:2003-11-20
Compounds of formula (Ia) as potent, &bgr;
1
-specific beta blockers with a short duration of action in the systemic circulation, wherein R is 3′,4′-dimethoxyphenyl, R
1
is hydrogen, and R
2
is selected from methyl, ethyl, propyl, isobutyl and isopropyl; or R is 3′,4′-dimethoxyphenyl, R
1
is selected from fluorine, chlorine and bromine, and R
2
is selected from methyl, ethyl, propyl, isopropyl, isobutyl and cyclopropylmethyl; of R is 4′-methoxyphenoxy, R
1
is selected from hydrogen, fluorine, chlorine and bromine, and R
2
is selected from methyl, ethyl, propyl, isopropyl, isobutyl and cyclopropylmethyl; or R is 3′,4′-dimethoxyphenyl, R
1
is cyano, and R
2
is cyclopropylmethyl; or R is 4′-methoxyphenoxy, R
1
is cyano, and R
2
is isobutyl; and physiologically acceptable hydrolysable derivatives thereof having the hydroxy group in the 2-position of the 3-aminopropoxy side chain in esterified form, in their racemic and optically active forms, and their pharmaceutically acceptable acid addition salts.
化合物的公式(Ia),作为有效的、&bgr;1-特异性的短效系统循环β受体阻滞剂,其中R为3'-,4'-二甲氧基苯基,R1为氢,R2选自甲基、乙基、丙基、异丁基和异丙基;或R为3'-,4'-二甲氧基苯基,R1选自氟、氯和溴,R2选自甲基、乙基、丙基、异丙基、异丁基和环丙甲基;或R为4'-甲氧基苯氧基,R1选自氢、氟、氯和溴,R2选自甲基、乙基、丙基、异丙基、异丁基和环丙甲基;或R为3'-,4'-二甲氧基苯基,R1为氰,R2为环丙甲基;或R为4'-甲氧基苯氧基,R1为氰,R2为异丁基;以及其在酯化形式下的3-氨基丙氧基侧链的2-位羟基可水解衍生物,其为外消旋和手性活性形式,以及其药学上可接受的酸盐。