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    • 2. 发明申请
    • IMMUNOGENIC GLYCOPROTEIN CONJUGATES
    • 免疫球蛋白结合蛋白
    • US20170007713A1
    • 2017-01-12
    • US15118038
    • 2015-02-06
    • PFIZER INC.
    • JIANXIN GURAJESH KUMAR KAINTHANJIN-HWAN KIMAVVARI KRISHNA PRASADYU-YING YANG
    • A61K47/48
    • The present invention relates generally to glycoconjugates comprising a saccharide covalently conjugated to a carrier protein through a spacer containing ((2-oxoethyl)thio)). In an aspect the invention provides oxo-eT linked glycoconjugates comprising a saccharide covalently conjugated to a carrier protein through a ((2-oxoethyl)thio) spacer having the formula (I): (I) wherein: A is a group (C═X)m wherein X is S or O and m is 0 or 1; B is a bond, O, or CH2; and when m is 0, B can also be (C═O); R is a C2-C16 alkylene, C2-C16 heteroakylene, NH—C(═O)—C2-C16 alkylene, or NH—C(═O)—C2-C16 heteroakylene, wherein said alkylene and heteroalkylene are optionally substituted by 1, 2 or 3 groups independently selected from COOR′ where R′ is selected from H, methyl, ethyl or propyl. The invention further relates to immunogenic compositions comprising such glycoconjugates, and to methods for the preparation and use of such glycoconjugates and immunogenic compositions.
    • 本发明一般涉及包含通过间隔基含有((2-氧代乙基)硫基))与载体蛋白共价轭合的糖的糖缀合物。 一方面,本发明提供了包含通过具有式(I)的((2-氧代乙基)硫代)间隔基共价结合于载体蛋白的糖的氧代eT连接的糖缀合物:(I)其中:A是一个基团(C = X)m其中X是S或O,m是0或1; B是键,O或CH2; 当m为0时,B也可以是(C = O); R是C 2 -C 16亚烷基,C 2 -C 16杂亚烷基,NH-C(= O)-C 2 -C 16亚烷基或NH-C(= O)-C 2 -C 16亚杂亚基,其中所述亚烷基和杂亚烷基任选被1 ,独立地选自COOR'的2或3个基团,其中R'选自H,甲基,乙基或丙基。 本发明还涉及包含这种糖缀合物的免疫原性组合物,以及制备和使用这些糖缀合物和免疫原性组合物的方法。