申请人:ImmunoGen, Inc.
公开号:US20160058882A1
公开(公告)日:2016-03-03
New ansamitocin derivatives bearing a linking group are disclosed. Also disclosed are methods for the synthesis of these new ansamitocin derivatives and methods for their linkage to cell-binding agents. The ansamitocin derivative-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.
披露了带有连接基团的新型安沙米托辛衍生物。还披露了合成这些新型安沙米托辛衍生物的方法以及它们与细胞结合剂的连接方法。安沙米托辛衍生物-细胞结合剂偶联物作为治疗剂非常有用,它们能特异性地传递到目标细胞并具有细胞毒性。与先前描述的药物相比,这些偶联物在动物肿瘤模型中显示出显著提高的治疗效果。