NOVEL HYDRAZONE DERIVATIVE IN WHICH THE TERMINAL AMINO GROUP IS REPLACED BY AN ARYL GROUP OR A HETEROARYL GROUP AND ITS USE Russian patent published in 2023 - IPC C07D213/04 A61K31/425 A61K31/505 C07D209/04 C07D217/04 C07D231/56 C07D241/10 C07D249/08 C07D277/20 C07D487/04 

FIELD: medicine, therapy.

SUBSTANCE: group of inventions is intended for the prevention or treatment of diseases caused by tau protein aggregation or hyperphosphorylation. New hydrazone derivatives of formula (4) are presented. In another embodiment, a process of their preparation is provided, comprising the reaction of a C_1-6alkyl, aryl, or heteroaryl carboxylic acid, or its anhydride with

to form an amide bond, where Y is either an unprotected or protected amine or nitro group; and the reaction of sodium nitrite, the heterocycle linked to the carboxamido group obtained in the previous step, and malononitrile in the presence of an acid to form an imino bond. Also the pharmaceutical compositions containing these compounds and used to inhibit tau protein aggregation are provided, to inhibit tau protein hyperphosphorylation, to prevent or treat diseases caused by tau protein aggregation or hyperphosphorylation.

EFFECT: group of inventions provides new hydrazone derivatives of formula (4) having inhibitory activity against tau protein aggregation and tau protein hyperphosphorylation.

10 cl, 8 tbl, 176 ex