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LINKER-DRUG AND ANTIBODY-DRUG CONJUGATE (ADC) EMPLOYING THE SAME
专利权人:
发明人:
申请号:
EP17207834.7
公开号:
EP3335734A1
申请日:
2017.12.15
申请国别(地区):
EP
年份:
2018
代理人:
摘要:
A linker-drug represented by formula (I). In formula (I), C is a conjugating linker, L is a linker unit, D is a drug unit, and n is an integer ranging from 1 to 4. The structure of the conjugating linker is represented by formula (II). In formula (II), X is a leaving group, both of R1 and R2 are single bond or -NH- and Z is aryl, substituted aryl, heteroaryl, substituted heteroaryl, linear alkyl, cycloalkyl, heterocycloalkyl, or a combination thereof. The wave line of formula (II) indicates the covalent attachment site to L. The antibody is conjugated to the linker unit through a cysteine residue of the antibody. An antibody-drug conjugate (ADC) is also provided.        C-(L-D)m     (I)
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