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    • 8. 发明申请
    • 3-AMINO-PROPOXYPHENYL DERIVATIVES (I)
    • 3-氨基 - 丙氧基衍生物(I)
    • WO1997013744A1
    • 1997-04-17
    • PCT/AU1996000638
    • 1996-10-10
    • THE UNIVERSITY OF MELBOURNELOUIS, William, JohnJACKMAN, Graham, PaulIAKOVIDIS, DimitriosLOUIS, Simon, Nicholas, StewartDRUMMER, Olaf, Heino
    • THE UNIVERSITY OF MELBOURNE
    • C07C217/34
    • A61K31/137A61K31/277C07C217/34C07C217/60C07C219/06C07C219/12C07C219/14C07C255/54C07C2601/02
    • Compounds of formula (Ia) as potent, beta 1-specific beta blockers with a short duration of action in the systemic circulation, wherein R is 3',4'-dimethoxyphenyl, R is hydrogen, and R is selected from methyl, ethyl, propyl, isobutyl and isopropyl; or R is 3',4'-dimethoxyphenyl, R is selected from fluorine, chlorine and bromine, and R is selected from methyl, ethyl, propyl, isopropyl, isobutyl and cyclopropylmethyl; or R is 4'-methoxyphenoxy, R is selected from hydrogen, fluorine, chlorine and bromine, and R is selected from methyl, ethyl, propyl, isopropyl, isobutyl and cyclopropylmethyl; or R is 3',4'-dimethoxyphenyl, R is cyano, and R is cyclopropylmethyl; or R is 4'-methoxyphenoxy, R is cyano, and R 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.
    • 式(Ia)化合物作为在全身循环中具有短暂作用持续时间的有效的β1-特异性β受体阻滞剂,其中R为3',4'-二甲氧基苯基,R 1为氢,R 2为 选自甲基,乙基,丙基,异丁基和异丙基; 或R 3为3',4'-二甲氧基苯基,R 1选自氟,氯和溴,R 2选自甲基,乙基,丙基,异丙基,异丁基和环丙基甲基; 或R是4'-甲氧基苯氧基,R 1选自氢,氟,氯和溴,R 2选自甲基,乙基,丙基,异丙基,异丁基和环丙基甲基; 或R 3为3',4'-二甲氧基苯基,R 1为氰基,R 2为环丙基甲基; 或R是4'-甲氧基苯氧基,R 1是氰基,R 2是异丁基; 其在3-氨基丙氧基侧链的2-位具有羟基的生理上可接受的可水解的衍生物,其外消旋和旋光形式及其药学上可接受的酸加成盐。