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    • 5. 发明授权
    • Amino-acid derivatives, their preparation and their use as
pharmaceuticals
    • 氨基酸衍生物,其制备及其作为药物的用途
    • US4545942A
    • 1985-10-08
    • US597817
    • 1984-04-09
    • Mitsuo NaganoKoichi HiraiKouichi KitamuraKenkichi ShinkaiHiroshi Yasuda
    • Mitsuo NaganoKoichi HiraiKouichi KitamuraKenkichi ShinkaiHiroshi Yasuda
    • A61K31/275A61K20060101A61K31/165A61K31/19A61K31/195A61K31/215A61P35/00A61P37/04C07C20060101C07C67/00C07C253/00C07C255/24C07C255/26C07C255/29C07C255/32C07C255/44C07C255/56C07C255/66C07D317/68C07C121/78
    • C07C255/00
    • New compounds useful as immunoregulatory and antineoplastic agents are amino-acid derivatives of formula: ##STR1## wherein: n is an integer from 1 to 5;R.sup.1 is a hydrogen atom, an alkyl group, a haloalkyl group, a halogen atom, a mercapto group, an alkylmercapto group, a hydroxy group, an alkoxy group, an acyloxy group, a carboxyl group, an alkoxycarbonyl group, an amino group, an alkyl-substituted amino group, an aryl-substituted amino group, an acylamino group, a haloalkoxycarbonylamino group, an alkanesulphonyl group, a nitro group or a cyano group (and, when n is an integer from 2 to 5, the radicals R.sup.1 may be the same or different);R.sup.2 and R.sup.3 may be the same or different and each is a hydrogen atom or an alkyl group;R.sup.4 is a hydrogen atom, an alkyl group, a cyano group, a cyanoalkyl group, a hydroxyalkyl group, an alkoxycarbonyl group, a carboxyl group, an aryl group, an aralkyl group, a mercaptoalkyl group, an alkylthioalkyl group, or a thioalkyl group (the free bond of the sulphur in said thioalkyl group being joined to the sulphur of another moiety of the same formula); andA is a hydroxy group, an alkoxy group, an amino group, an alkyl-substituted amino group (optionally halogen- or carbamoyl- substituted in the alkyl moiety), a hydrazino group, an alkyl- or aryl- substituted hydrazino group, a hydroxylamino group, an alkoxyamino group or an aralkyloxyamino group;and the pharmaceutically acceptable salts thereof.
    • 可用作免疫调节和抗肿瘤剂的新化合物是下式的氨基酸衍生物:其中:n是1至5的整数; R1是氢原子,烷基,卤代烷基,卤素原子,巯基,烷基巯基,羟基,烷氧基,酰氧基,羧基,烷氧基羰基,氨基, 烷基取代的氨基,芳基取代的氨基,酰氨基,卤代烷氧基羰基氨基,链烷磺酰基,硝基或氰基(当n为2至5的整数时,基团R 1可以 相同或不同); R2和R3可以相同或不同,各自为氢原子或烷基; R4是氢原子,烷基,氰基,氰基烷基,羟基烷基,烷氧基羰基,羧基,芳基,芳烷基,巯基烷基,烷硫基烷基或硫代烷基 (所述硫代烷基中的硫的游离键与相同式的另一部分的硫连接); 并且A是羟基,烷氧基,氨基,烷基取代的氨基(在烷基部分中任选被卤素取代或氨基甲酰基取代),肼基,烷基或芳基取代的肼基, 羟基氨基,烷氧基氨基或芳烷氧基氨基; 及其药学上可接受的盐。