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    Amino-acid derivatives, their preparation and their use as pharmaceuticals
    2.
    发明授权
    Amino-acid derivatives, their preparation and their use as pharmaceuticals 失效
    氨基酸衍生物，其制备及其作为药物的用途

    公开(公告)号：US4545942A

    公开(公告)日：1985-10-08

    申请号：US597817

    申请日：1984-04-09

    申请人： Mitsuo Nagano ,  Koichi Hirai ,  Kouichi Kitamura ,  Kenkichi Shinkai ,  Hiroshi Yasuda

    发明人： Mitsuo Nagano ,  Koichi Hirai ,  Kouichi Kitamura ,  Kenkichi Shinkai ,  Hiroshi Yasuda

    IPC分类号： A61K31/275 ,  A61K20060101 ,  A61K31/165 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61P35/00 ,  A61P37/04 ,  C07C20060101 ,  C07C67/00 ,  C07C253/00 ,  C07C255/24 ,  C07C255/26 ,  C07C255/29 ,  C07C255/32 ,  C07C255/44 ,  C07C255/56 ,  C07C255/66 ,  C07D317/68 ,  C07C121/78

    CPC分类号： C07C255/00

    摘要： 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.

    摘要翻译： 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。