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US 2019/0127400 A1Published application
Charged linkers and their uses for conjugation
AssigneeHangzhou Dac Biotech Co., Ltd.
InventorsRobert Yongxin ZHAO, Xing LI, Yuangyuang HUANG, Qingliang YANG
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Abstract
Cell binding agent-drug conjugates comprising phosphinate-based charged linkers and methods of using such linkers and conjugates are provided.
Claims21
A compound of formula (III):
- wherein Z is a thiol, disulfide, unsubstituted or substituted pyridyldisulfide, unsubstituted or substituted amino, amino oxy, carboxy, aldehyde, ketone, azide, unsubstituted or substituted maleimido, haloacetyl, hydrazine, hydrazide or hydroxy group;
- Cb represents a cell-binding agent;
- n is an integer from 1 to 20;
- M is H, Na, K, N+R1R2R3 or a pharmaceutical salt thereof;
- R3 is absent, a linear alkyl having from 1 to 6 carbon atoms, branched or cyclic alkyl having from 3 to 6 carbon atoms, a linear, branched or cyclic alkenyl or alkynyl having from 2 to 6 carbon atoms, polyethyleneoxy unit of formula (OCH2CH2)p, wherein p is an integer from 1 to about 1000;
- or R1, R2 and R3 are respectively a chain of atoms selected from the group consisting of C, N, O, S, Si, and P that optionally covalently connects to each other;
- and
- R4, and R5, are the same or different and are absent, H, a linear alkyl having from 1 to 6 carbon atoms, branched or cyclic alkyl having from 3 to 6 carbon atoms, linear, branched or cyclic alkenyl or alkynyl having from 2 to 6 carbon atoms, or polyethyleneoxy unit of formula (OCH2CH2)p, wherein p is an integer from 1 to about 1000.
5 more elements
Dependencies are inferred from the claim text.