Heterobifunctional linkers with polyethylene glycol segments and immune response modifier conjugates made therefrom

    公开(公告)号:US10723731B2

    公开(公告)日:2020-07-28

    申请号:US15905367

    申请日:2018-02-26

    Inventor: Paul D. Wightman

    Abstract: Conjugates of an immune response modifier, a linker, and an antigen are disclosed. The linker is represented by formula: wherein A is CH or N, p is in a range from 1 to 50, R″ is a bond or -alkylene-O—, R′ is alkylene that is optionally interrupted or terminated with one or more amide or ether groups, and E is an amine- or thiol-reactive group. Pharmaceutical compositions containing the compound or the conjugate, methods of making a conjugate, and methods of use of the compounds or conjugates as immunomodulators for inducing cytokine biosynthesis in an animal and for vaccinating an animal are also disclosed. An antigen modified by the linker is also disclosed.

    HETEROBIFUNCTIONAL LINKERS WITH POLYETHYLENE GLYCOL SEGMENTS AND IMMUNE RESPONSE MODIFIER CONJUGATES MADE THEREFROM
    9.
    发明申请
    HETEROBIFUNCTIONAL LINKERS WITH POLYETHYLENE GLYCOL SEGMENTS AND IMMUNE RESPONSE MODIFIER CONJUGATES MADE THEREFROM 有权
    具有聚乙二醇部分的互补连接体和免疫反应调节因子

    公开(公告)号:US20140227317A1

    公开(公告)日:2014-08-14

    申请号:US14123727

    申请日:2012-06-01

    Inventor: Paul D. Wightman

    CPC classification number: C07D471/04 A61K47/60 C07D207/46

    Abstract: Conjugates of an immune response modifier, a linker, and an antigen are disclosed. The linker is represented by formula (I): wherein A is CH or N, p is in a range from 1 to 50, R″ is a bond or -alkylene-O—, R′ is alkylene that is optionally interrupted or terminated with one or more amide or ether groups, and E is an amine- or thiol-reactive group. Pharmaceutical compositions containing the compound or the conjugate, methods of making a conjugate, and methods of use of the compounds or conjugates as immunomodulators for inducing cytokine biosynthesis in an animal and for vaccinating an animal are also disclosed. An antigen modified by the linker is also disclosed.

    Abstract translation: 公开了免疫应答调节剂,接头和抗原的缀合物。 接头由式(I)表示:其中A是CH或N,p在1至50的范围内,R“是键或 - 亚烷基-O-,R'是任选被中断或以 一个或多个酰胺或醚基团,E是胺或硫醇反应性基团。 还公开了含有化合物或缀合物的药物组合物,制备缀合物的方法,以及使用化合物或缀合物作为用于在动物中诱导细胞因子生物合成和接种疫苗的免疫调节剂的方法。 还公开了由接头修饰的抗原。

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