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US 10,377,837 B2Granted
Antibody-drug conjugate having cyclic benzylidene acetal linker
AssigneeNof Corporation
InventorsTakuma Tsubusaki, Yuji Yamamoto
Life of this patent
Estimating the term…
Abstract
An antibody-drug conjugate having a cyclic benzylidene acetal linker represented by formula (1) or formula (2), wherein Y is an antibody; D is a drug; R1 and R6 are each independently a hydrogen atom or a hydrocarbon group; R2, R3, R4 and R5 are each independently an electron-withdrawing or electron-donating substituent or a hydrogen atom; s is 1 or 2, t is 0 or 1, and s+t is 1 or 2; w is an integer of 1 to 20; and Z1 and Z2 are each independently a selected divalent spacer:
Claims11
An antibody-drug conjugate having a cyclic benzylidene acetal linker represented by formula (1) or formula (2):
- wherein, in the formula (1) and the formula (2), Y is an antibody;
- D is a drug;
- R1 and R6 are each independently a hydrogen atom or a hydrocarbon group;
- R2, R3, R4 and R5 are each independently an electron-withdrawing or electron-donating substituent or a hydrogen atom;
- s is 1 or 2, t is 0 or 1, and s+t is 1 or 2;
- w is an integer of 1 to 20;
- and each of Z1 and Z2 is a divalent spacer composed of a structural unit independently selected from an ether group, an ester group, a carbonate group, a urethane group, an amide group, a thioether group, a disulfide group, a 1H-1,2,3-triazole-1,4-diyl group, a secondary amino group, an aliphatic hydrocarbon group containing any of these groups, or an aliphatic hydrocarbon group;
- or each of Z1 and Z2 is a divalent spacer composed of two identical structural units selected from an ether group, an ester group, a carbonate group, a urethane group, an amide group, a thioether group, a disulfide group, a 1H-1,2,3-triazole-1,4-diyl group, a secondary amino group or an aliphatic hydrocarbon group containing any of these groups.
5 more elements
Dependencies are inferred from the claim text.