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IMPROVED SULFAMIDE LINKERS FOR USE IN BIOCONJUGATES
专利权人:
发明人:
申请号:
EP17703982.3
公开号:
EP3413922A1
申请日:
2017.02.08
申请国别(地区):
EP
年份:
2018
代理人:
摘要:
The invention relates to a novel linker for use in bioconjugates such as antibody-drug-conjugates. The linker according to the invention is represented by formula: (I) wherein: - BM is a branching moiety - E is a capping group - SG is a sulfamide group - b, c, d, e, g, i, k, I are independently 0 or 1 - f is an integer in the range of 1 to 10 - Sp1, Sp2, Sp3, Sp4, Sp5 and Sp6 are a spacer moieties - Z1 and Z2 are connecting groups. The linker according to the invention is useful in the preparation of linker-conjugates and bioconjugates, and can be used for (a) improving conjugation efficiency in the preparation of the bioconjugate, (b) reducing aggregation during the preparation of the bioconjugate and/or of the bioconjugate, (c) increasing stability of the bioconjugate, and/or (d) increasing therapeutic index of the bioconjugate.
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中国工程科技知识中心
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