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    Immunologically active dipeptidyl saccharides and methods of preparation
    17.
    发明授权
    Immunologically active dipeptidyl saccharides and methods of preparation 失效
    免疫活性二肽基糖类及其制备方法

    公开(公告)号：US4377570A

    公开(公告)日：1983-03-22

    申请号：US193777

    申请日：1980-10-03

    申请人： Philippe L. Durette ,  Tsung-Ying Shen

    发明人： Philippe L. Durette ,  Tsung-Ying Shen

    IPC分类号： C07K9/00 ,  A61K39/00 ,  A61K37/02

    CPC分类号： C07K9/005

    摘要： 2-Amino-2-deoxy-glycoses of the general structural formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl (1-7C), substituted alkyl (1-7C), phenyl, substituted phenyl, benzyl, or substituted benzyl;R.sub.2 is alkyl, substituted alkyl, phenyl, or substituted phenyl;R.sub.3 is H or lower alkyl (1-10C) with the proviso that when the aminoglycose has the 2-amino-2-deoxy-D-glucose configuration, R.sub.3 cannot be H;R.sub.4 and R.sub.5 are same or different and are H, aliphatic or aromatic acyl (2-21C) or substituted acyl (2-21C);R.sub.6 is H, or R.sub.6 -R.sub.7 together is --CH.sub.2 --CH.sub.2 --CH.sub.2 --,R.sub.7 is H, alkyl (1-7C), hydroxymethyl, mercaptomethyl, benzyl, or substituted benzyl;R.sub.8 and R.sub.9 each is carboxyl, esterified carboxyl (1-7C), amidated carboxyl, or mono- or di-alkyl-(1-3C)-amidated carboxyl;provided that when R.sub.3 is lower alkyl, the stereochemistry at asymmetric center I can be either D or L, but that when the aminoglycose has the 2-amino-2-deoxy-D-glucose configuration, the stereochemistry at I cannot be D;when R.sub.7 is not H, the stereochemistry at asymmetric center II is either L or D; andthe stereochemistry at asymmetric center III is D.These compounds possess immunostimulatory properties.

    摘要翻译： 2-氨基-2-脱氧糖苷，其通式为：其中R1为氢，烷基（1-7C），取代的烷基（1-7C），苯基，取代的苯基，苄基或取代的苄基; R2是烷基，取代的烷基，苯基或取代的苯基; R3是H或低级烷基（1-10C），条件是当氨基糖类具有2-氨基-2-脱氧-D-葡萄糖构型时，R3不能是H; R4和R5相同或不同，为H，脂族或芳族酰基（2-21C）或取代的酰基（2-21C）; R6是H或R6-R7一起是-CH 2 -CH 2 -CH 2 - ，R 7是H，烷基（1-7C），羟甲基，巯基甲基，苄基或取代的苄基; R8和R9各自为羧基，酯化羧基（1-7C），酰胺化羧基或单 - 或二 - 烷基 - （1-3C） - 酰胺化羧基; 条件是当R3为低级烷基时，不对称中心I的立体化学可以是D或L，但当氨基糖类具有2-氨基-2-脱氧-D-葡萄糖构型时，I的立体化学不能是D; 当R7不为H时，不对称中心II的立体化学为L或D; 而不对称中心III的立体化学是D.这些化合物具有免疫刺激性质。