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    • 9. 发明申请
    • 3-amino-propoxphenyl derivatives (I)
    • 3-氨基 - 丙氧基苯基衍生物(I)
    • US20030216477A1
    • 2003-11-20
    • US10412408
    • 2003-04-14
    • THE UNIVERSITY OF MELBOURNE
    • William John LouisGraham Paul JackmanDimitrios IakovidisSimon Nicholas Stewart LouisOlaf Heino Drummer
    • A61K031/277A61K031/137
    • A61K31/137A61K31/277C07C217/34C07C217/60C07C219/06C07C219/12C07C219/14C07C255/54C07C2601/02
    • Compounds of formula (Ia) as potent, null1-specific beta blockers with a short duration of action in the systemic circulation, wherein R is 3null,4null-dimethoxyphenyl, R1 is hydrogen, and R2 is selected from methyl, ethyl, propyl, isobutyl and isopropyl; or R is 3null,4null-dimethoxyphenyl, R1 is selected from fluorine, chlorine and bromine, and R2 is selected from methyl, ethyl, propyl, isopropyl, isobutyl and cyclopropylmethyl; of R is 4null-methoxyphenoxy, R1 is selected from hydrogen, fluorine, chlorine and bromine, and R2 is selected from methyl, ethyl, propyl, isopropyl, isobutyl and cyclopropylmethyl; or R is 3null,4null-dimethoxyphenyl, R1 is cyano, and R2 is cyclopropylmethyl; or R is 4null-methoxyphenoxy, R1 is cyano, and R2 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)的化合物作为在全身循环中具有短暂作用时间的有效β1特异性β受体阻滞剂,其中R是3',4'-二甲氧基苯基,R 1是氢,并且R 2被选择 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; 的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。