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公开(公告)号：US20130324706A1
公开(公告)日：2013-12-05
申请号：US14001237
申请日：2012-02-23
申请人： Laurent Ducry , Bernhard Stump , Heilam Wong , Jin She , Gayle Phillips
发明人： Laurent Ducry , Bernhard Stump , Heilam Wong , Jin She , Gayle Phillips
CPC分类号： C07K5/06043 , A61K47/60 , A61K47/64 , A61K47/65 , A61K47/6809 , A61K47/6845
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.
摘要翻译： 本发明涉及将蛋白质和药物连接到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，并衍生自邻羟基对氨基 苄基醇，其中肽链通过对氨基与苯环连接，药物通过苄醇部分连接到苯环，并且蛋白质通过邻羟基连接到苯环上; 进一步涉及通过各种中间体制备所述蛋白质 - 药物偶联物的方法，将这种蛋白质药物偶联物的药物用途，例如控制不期望细胞生长的方法用于包含这种蛋白质药物偶联物的药物组合物，以及 中间体制备蛋白质药物偶联物。
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公开(公告)号：US10294270B2
公开(公告)日：2019-05-21
申请号：US14001237
申请日：2012-02-23
申请人： Laurent Ducry , Bernhard Stump , Heilam Wong , Jin She , Gayle Allway
发明人： Laurent Ducry , Bernhard Stump , Heilam Wong , Jin She , Gayle Allway
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.
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