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Conjugates of methyltrithio antitumour agents and intermediates for their synthesis

机译:甲基三硫代抗肿瘤药及其中间体的缀合物

摘要

This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.
机译:本发明描述了由有效抗肿瘤抗生素的加利车霉素家族的二硫化物类似物及其衍生物,以及相关抗肿瘤抗生素例如esperamicins的类似物制备的载体-药物缀合物。载体可以是靶向不期望的细胞群(例如肿瘤细胞)的抗体,生长因子或类固醇。全蛋白载体以及它们的抗原识别片段以及它们的化学或遗传操作的对应物可用于缀合物的靶向部分。本发明包括合成这些缀合物所需的化合物,载体-药物缀合物的合适药物组合物及其使用方法。

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