Antibody-drug conjugate having cyclic benzylidene acetal linker
AssigneeNof Corporation
InventorsTakuma TSUBUSAKI, Yuji YAMAMOTO
Life of this patent
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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:
Claims19
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 Z1 and Z2 are each independently a selected divalent spacer.
A compound having a cyclic benzylidene acetal linker represented by formula (3) or formula (4):
- wherein, in the formula (3) and the formula (4), Y is an antibody;
- 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;
- X1 is a reactive functional group capable of linking to a drug by a covalent bond;
- 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, Z2, Z3 and Z4 are each independently a selected divalent spacer.
A compound having a cyclic benzylidene acetal linker represented by formula (5) or formula (6):
- wherein, in the formula (5) and the formula (6), 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;
- X2 is a reactive functional group capable of linking to an antibody by a covalent bond;
- s is 1 or 2, t is 0 or 1, and s+t is 1 or 2;
- and Z1, Z2, Z3 and Z4 are each independently a selected divalent spacer.
Dependencies are inferred from the claim text.