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Transition metal based functional segments for the preparation of cell target complexes

机译:基于过渡金属的功能区段,用于制备细胞靶络合物

摘要

The present invention relates to a transition metal based linker and a secondary functional portion comprising a primary functional portion coupled thereto.The secondary functional portion of the present invention comprises transition metal complexes, such as cis platinum (II) complexes, which have primary functional portions (e.g., unmodified or modified cytotoxic drugs) as the first ligand, and iodides, bromide or chlorides as the second ligand.Secondary functional portions containing iodide or bromide groups, especially the iodide group as the release ligand, were found to be more efficient binding efficiencies for cell binding sites (e.g. antibodies).Furthermore, the secondary functional moiety containing iodide or bromide as the release ligand is hydrolytically fairly stable compared to the secondary functional portion containing chloride as the release ligand.The present invention also relates to a cell target complex comprising a linker of the present invention.The present invention further relates to the drug containing the cell target complex, and the use of a cell target complex in the diagnosis and treatment of cancer.
机译:基于过渡金属的接头和辅助功能部分技术领域本发明涉及一种过渡金属的接头和次级功能部分,包括耦合到其上的主要功能部分。本发明的二次功能部分包括过渡金属配合物,例如CIS铂(II)复合物,其具有主要功能部分(例如,未改性或修饰的细胞毒性药物)作为第一配体,以及作为第二配体的碘化物,溴化物或氯化物。发现含碘或溴化物基团,特别是碘化物作为释放配体的碘化物,尤其是碘化物组更有效的结合细胞结合位点(例如抗体)的效率。与释放配体相比,含碘化物或溴化物作为释放配体的二次官能部分与含有氯化物作为释放配体的二次官能部分相比水解相当稳定。本发明还涉及细胞靶包含本发明的接头的络合物。目前的INVEN进一步涉及含有细胞靶复合物的药物,以及使用细胞靶复合物在癌症的诊断和治疗中的使用。

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