Sulfamide linkers for use in bioconjugates
Abstract:
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:




wherein:



BM is a branching moiety;
E is a capping group;
SG is a sulfamide group;
b, c, d, e, g, i, k, l 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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