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BRANCHED LINKER FOR PROTEIN DRUG CONJUGATES

机译:蛋白质药物偶联物的分支连接器

摘要

The present invention relates to method for connecting a protein and a drug to a protein drug conjugate, wherein the drug is linked to the protein through a specific branched linker, said branched linker comprises a peptide chain and is derived from o-hydroxy p-amino benzylic alcohol, wherein the peptide chain is connected to the phenyl ring via the p-amino group, the drug is connected to the phenyl ring via the benzylic alcohol moiety, and the protein is connected to the phenyl ring via the o-hydroxy group; further to a process for the preparation of said protein-drug-conjugates via various intermediates, to the pharmaceutical use of such protein drug conjugates, such as methods of controlling the growth of undesirable cells, to pharmaceutical compositions comprising such protein drug conjugates, and to intermediates of the preparation of the protein drug conjugates.
机译:本发明涉及将蛋白质和药物连接至蛋白质药物缀合物的方法,其中药物通过特定的支链接头与蛋白质连接,所述支链接头包含肽链并且衍生自邻羟基对氨基苄醇,其中肽链通过对氨基与苯环相连,药物通过苄醇部分与苯环相连,蛋白质通过邻羟基与苯环相连;进一步涉及通过各种中间体制备所述蛋白质-药物-缀合物的方法,所述蛋白质-药物缀合物的药学用途,例如控制不良细胞生长的方法,包含所述蛋白质-药物缀合物的药物组合物,以及蛋白药物缀合物制备的中间体。

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