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Trioxacarcins, trioxacarcin-antibody conjugates, and uses thereof

机译:Trioxacarcins,trioxacarcin抗体结合物及其用途

摘要

Provided herein are trioxacarcin-antibody drug conjugates of Formula (A): and pharmaceutically acceptable salts thereof, comprising at least one instance of the group -L1-(A-L2)a-B attached thereto, wherein a is an integer between 1 and 10, inclusive, L1 is absent or is a linking group, A is a moiety formed from the reaction of two complimentary groups (X and Y), L2 is absent or is another linking group, and B is an antibody or antibody fragment. Also provided are methods of preparing these antibody-drug conjugates, pharmaceutically acceptable compositions thereof, and methods of their use and treatment. Further provided are precursors to the trioxacarcin-antibody drug conjugates, novel trioxacarcins without an antibody conjugated thereto, pharmaceutical compositions thereof, and methods of their use and treatment.; embedded image
机译:本文提供的是式(A)的三氧杂色胺-抗体药物偶联物:及其药学上可接受的盐,包含至少一个-L 1 -(AL 2 )基团与其连接的aB,其中a为1至10之间的整数(含1和10),不存在L 1 或为连接基团,A为由两个互补基团(X和Y)反应形成的部分,L 2 不存在或为另一个连接基团,B为抗体或抗体片段。还提供了制备这些抗体-药物缀合物的方法,其药学上可接受的组合物,以及它们的使用和治疗方法。还提供了三氧嘧啶-抗体药物偶联物的前体,没有与其偶联的抗体的新型三氧沙金菌素,其药物组合物以及它们的使用和治疗方法。 “嵌入式图像”

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