ANTI-TROP2 ANTIBODY-DRUG CONJUGATE Russian patent published in 2021 - IPC A61K31/4745 C07D491/22 A61K39/395 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a method for preparing an antibody-drug conjugate comprising reacting a compound represented by the following formula: (maleimide-N-yl) -CH₂CH₂CH₂CH₂CH₂-C(=O)-GGFG-NH-CH₂-O-CH₂-C(=O)-(NH-DX), with an anti-TROP2 antibody or a reactive derivative thereof and conjugating a drug-linker fragment with the antibody by a thioether bonding method in the disulphide bond region present in the hinge portion of the antibody, where (maleimide-N-yl)- is a group represented by the following formula:

, where the nitrogen atom is a binding position, and -(NH-DX) is a group represented by the following formula: , where the nitrogen atom of the amino group in position 1 is a binding position, and -GGFG- is a tetrapeptide residue -Gly-Gly-Phe-Gly-.

EFFECT: technical result is a method for preparing a novel antibody-drug conjugate exhibiting an antitumour effect.

15 cl, 27 dwg, 2 tbl, 22 ex