Modified capsular saccharides comprising a blocking group at a hydroxyl group position on at least one of the monosaccharide units of the corresponding native capsular saccharide, wherein the blocking group is of the formula (Ia) or (Ib): -O-X-Y (Ia) or -O-R1 (Ib) wherein X is C(O), S(O) or SO2; Y is NR1R2 or R3; R1 is C1-6 alkyl substituted with 1, 2 or 3 groups independently selected from hydroxyl, sulphydryl and amine; R2 is H or C1-6 alkyl; and R3 is C1-6 alkyl; processes for modifying a capsular saccharide with the blocking groups; saccharide-protein conjugates comprising the modified capsular saccharide; processes for making the saccharide-protein conjugates, pharmaceutical compositions comprising the modified capsular saccharides and/or saccharide-protein conjugates; and methods and uses of the same.
在相应的原生胶囊糖的至少一个
单糖单元上的羟基位置上包含封端基团的改性胶囊糖,其中封端基团为式(Ia)或(Ib):-其中X是C(O)、S(O)或SO2;Y是NR1R2或R3;R1是被1、2或3个独立选自羟基、亚砜基和胺的基团取代的C1-6烷基;R2是H或C1-6烷基;R3是C1-6烷基;用封端基团修饰胶囊糖的工艺;包含改性胶囊糖的糖-蛋白共轭物;糖-蛋白共轭物的制造工艺,包含改性胶囊糖和/或糖-蛋白共轭物的药物组合物;以及其方法和用途。