Cytotoxic agents comprising maytansinoids and their therapeutic use
    11.
    发明授权
    Cytotoxic agents comprising maytansinoids and their therapeutic use 失效
    含美登木素生物碱的细胞毒素及其治疗用途

    公开(公告)号:US5416064A

    公开(公告)日:1995-05-16

    申请号:US986578

    申请日:1992-12-07

    CPC分类号: A61K47/48384 A61K31/535

    摘要: A cytotoxic agent comprising one or more maytansinoids linked to a cell binding agent. A therapeutic agent for killing selected cell populations comprising: (a) a cytotoxic amount of one or more maytansinoids linked to a cell binding agent, and (b) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting a cell population or tissue suspected of containing cells from said selected cell population with a cytotoxic amount of a cytotoxic agent comprising one or more maytansinoids linked to a cell binding agent. An N-methyl-alanine-containing ester of maytansinol or an analogue of maytansinol, said N-methyl-alanine-containing ester comprising a linking group capable of linking an N-methyl-alanine-containing maytansinoid ester to a chemical moiety. N-methyl-cysteine-containing ester of maytansinol or an analogue of maytansinol.

    摘要翻译: 包含与细胞结合剂连接的一种或多种美登木素生物碱的细胞毒性剂。 一种用于杀死所选细胞群的治疗剂,包括:(a)细胞毒性量的与细胞结合剂连接的一种或多种美登木素生物碱,和(b)药学上可接受的载体,稀释剂或赋形剂。 一种用于杀死所选择的细胞群的方法,包括使来自所述选择的细胞群的怀疑含有细胞的细胞群体或组织与细胞毒性量的细胞毒性剂接触,所述细胞毒性剂包含与细胞结合剂连接的一种或多种美登木素生物碱。 含有N-甲基 - 丙氨酸的美登素的酯或美登素的类似物,所述含有N-甲基 - 丙氨酸的酯包含能够将含有N-甲基 - 丙氨酸的美登木素生物酯与化学部分连接的连接基团。 美登素的N-甲基 - 半胱氨酸酯或美登醇的类似物。

    Acid-cleavable compound
    12.
    发明授权
    Acid-cleavable compound 失效
    酸可切割化合物

    公开(公告)号:US4764368A

    公开(公告)日:1988-08-16

    申请号:US908388

    申请日:1986-09-17

    CPC分类号: C07D207/452 C07D405/12

    摘要: Heterobifunctional reagents that are cleavable under mildly acidic conditions are disclosed. The reagents include an acid cleavable cyclohexene-1,2,-dicarboxylic acid monoamide group. Also disclosed are methods of making the cross-linkers, as well as methods of using the cross-linkers, e.g., to deliver a biologically active substance across the membranes of selected cells in a heterogeneous cell population; once inside the cell the active substance is released, intact, by the transient, mild acidity of certain cell structures. Finally, a method of characterizing complex multi-chain protein structures is disclosed.

    摘要翻译: 公开了在弱酸性条件下可切割的异双功能试剂。 试剂包括可酸裂解的环己烯-1,2-二羧酸单酰胺基团。 还公开了制备交联剂的方法,以及使用交联剂的方法,例如将生物活性物质跨越异种细胞群体中所选细胞的膜递送; 一旦在细胞内,活性物质通过某些细胞结构的瞬时,温和的酸度被完全释放。 最后,公开了一种表征复合多链蛋白结构的方法。