Method for the preparation of maytansinoid esters
    31.
    发明申请
    Method for the preparation of maytansinoid esters 有权
    美登木素生物酯酯的制备方法

    公开(公告)号:US20060167245A1

    公开(公告)日:2006-07-27

    申请号:US11334478

    申请日:2006-01-19

    IPC分类号: C07D491/04

    CPC分类号: C07D498/18

    摘要: Improved processes for the preparation and purification of maytansinoid esters, especially thiol and disulfide-containing maytansinoids are described. In one aspect the process comprises a process of making a maytansinoid ester comprising forming an anion of maytansinol or a maytansinoid bearing a free C-3 hydroxyl moiety and reacting the anion with an activated carboxyl compound to thereby produce the maytansinoid ester.

    摘要翻译: 描述了用于制备和纯化美登木素生物碱酯,特别是硫醇和二硫化物的美登木素生物碱的改进方法。 在一个方面,该方法包括制备美登木素生物碱酯的方法,其包括形成美登醇的阴离子或含有游离C-3羟基部分的美登木素生物碱,并使阴离子与活化的羧基化合物反应,从而产生美登木酯生物酯。

    Cytotoxic agents containing novel potent taxanes and their therapeutic use
    38.
    发明申请
    Cytotoxic agents containing novel potent taxanes and their therapeutic use 失效
    含有新型有效紫杉烷类及其治疗用途的细胞毒素

    公开(公告)号:US20050085513A1

    公开(公告)日:2005-04-21

    申请号:US10963711

    申请日:2004-10-14

    摘要: Included within the scope of the present invention are potent taxanes and taxanes containing a linking group. Also included is a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for inducing cell death in selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a link, and (B) a pharmaceutically acceptable carrier, diluent or excipient is also included. A method for inducing cell death in selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent is included as well.

    摘要翻译: 包括在本发明范围内的有效的紫杉烷类和含有连接基团的紫杉烷类。 还包括细胞毒性剂,其包含与细胞结合剂连接的一种或多种紫杉烷类。 一种用于在所选细胞群体中诱导细胞死亡的治疗组合物,包括:(A)细胞毒性量的一种或多种通过连接体与细胞结合剂共价结合的紫杉烷,和(B)药学上可接受的载体,稀释剂或赋形剂 。 还包括诱导选择的细胞群体中的细胞死亡的方法,包括使靶细胞或含有靶细胞的组织与有效量的包含与细胞结合剂连接的一种或多种紫杉烷的细胞毒性试剂接触。