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    • 7. 发明授权
    • Biologically active catecholamine derivatives
    • 生物活性儿茶酚胺衍生物
    • US4337207A
    • 1982-06-29
    • US184000
    • 1980-09-04
    • Murray GoodmanMichael S. VerlanderKenneth A. JacobsonKenneth L. MelmonNeal Castagnoli
    • Murray GoodmanMichael S. VerlanderKenneth A. JacobsonKenneth L. MelmonNeal Castagnoli
    • C07C233/00C07C103/29
    • C07C233/00
    • Biologically active derivatives of norepinephrine are disclosed. Such derivatives are catecholamines wherein isoproterenol is modified by extending the isopropyl functional grouping to an alkyl, aryl, or alkyl-aryl chain of variable length where said chain terminates in a carboxylic acid functional group, or in a substituted amide functional group. Such derivatives are .beta.-adrenergic and a number of such derivatives e.g., 6-(.beta.-3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid p-toluide, 6-(.beta.-3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid para-n-butyl anilide; 6-(.beta.,3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid para-methoxy anilide; 6-(.beta.-3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid paratrifluoromethyl anilide; and 6-(.beta.-3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid N-methyl para-toluide display a .beta.-adrenergic activity at least several orders of magnitude greater than isoproterenol itself. Several methods of producing such active derivatives are also disclosed.
    • 公开了去甲肾上腺素的生物活性衍生物。 这样的衍生物是儿茶酚胺,其中异丙肾上腺素通过将异丙基官能团延伸到可变长度的烷基,芳基或烷基 - 芳基链来修饰,其中所述链终止于羧酸官能团,或在取代的酰胺官能团中。 这样的衍生物是β-肾上腺素能的,并且许多这样的衍生物例如6-(β-3,4-二羟基苯基-β-羟基) - 乙基氨基庚酸对甲苯胺,6-(β-3,4-二羟基苯基-β- 羟基) - 乙基氨基庚酸对 - 丁基苯胺; 6-(β,3,4-二羟基苯基-β-羟基) - 乙基氨基庚酸对甲氧基苯胺; 6-(β-3,4-二羟基苯基-β-羟基) - 乙基氨基庚酸对三氟甲基苯胺; 和6-(β-3,4-二羟基苯基-β-羟基) - 乙基氨基庚酸N-甲基对甲苯甲酸显示比异丙肾上腺素本身至少几个数量级的β-肾上腺素能活性。 还公开了生产这种活性衍生物的几种方法。