POTENT CONJUGATES AND HYDROPHILIC LINKERS
    62.
    发明申请
    POTENT CONJUGATES AND HYDROPHILIC LINKERS 审中-公开
    POTENT CONJUGATES和HYPOPHILIC LINKERS

    公开(公告)号:US20160114052A1

    公开(公告)日:2016-04-28

    申请号:US14835236

    申请日:2015-08-25

    Abstract: Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.

    Abstract translation: 用于将药物与细胞结合剂结合的接头通过并入聚乙二醇间隔物而被修饰成亲水接头。 细胞结合剂 - 药物偶联物的效力或功效令人惊奇地增加了多种癌细胞类型的几倍,包括在细胞表面上表达低数目抗原的那些或对治疗有抗性的癌细胞。 还提供了一种制备具有硫醚部分的美登木素生物碱和允许美登木素生物碱在基本上单一步骤中与细胞结合剂连接的反应性基团的方法。

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