LINKER FOR ANTIBODY-DRUG CONJUGATES AND THEIR USE Russian patent published in 2023 - IPC C07D207/448 C07D207/452 C07D403/12 A61K47/68 A61K39/395 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a linker having a structure represented by formula I, in which each of M₁', M₂' is selected independently from , M₁', M₂' are the same or different; L₁, L₂ are chosen, each independently, from C₁-C₉-alkyl; Q chosen from , N; L₃' chosen from C (=O) R⁸C (=O), _NH2, OH, and any combination thereof; X is chosen from Br; Y represents , ; Z is selected from C; R¹ is selected from H, C₁-C₆-alkyl, R², R⁸, R¹⁰ are each independently selected from H, C₁-C₆-alkyl. The invention also relates to antibody-drug conjugates obtained using said linker, as well as to the use of antibody-drug conjugates in a preparation for the treatment of cancer associated with the HER2 antigen.

EFFECT: new linker is obtained, which is capable of simultaneously connecting with 2, 3 or 4 thiol groups of an antibody, which leads to a homogeneous and structurally stable coupling product.

19 cl, 14 dwg, 3 tbl, 30 ex

(I)