INHIBITORS, A METHOD OF THEIR PREPARATION AND USE Russian patent published in 2023 - IPC C07D417/14 C07D409/04 C07D417/04 C07D401/04 C07D241/20 C07D213/76 A61K31/4427 A61K31/4439 A61K31/4436 A61K31/444 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula Y or a pharmaceutically acceptable salt thereof, where A represents CH; Ar is either thiazolyl, pyrazolyl or pyridinyl; wherein the thiazolyl, pyrazolyl or pyridinyl is substituted with either one or two substituents independently selected from C_1-6 alkyl, C_3-6 cycloalkyl, 5–7 membered heterocyclyl containing 1–2 ring heteroatoms independently selected from O and N, -O-R¹⁰⁰ and -SR¹⁰⁷ wherein each R¹⁰⁰ is independently selected from phenyl; each R¹⁰⁷ is independently selected from C_1-6 alkyl; wherein each heterocyclyl is optionally substituted with one or more substituents, each independently selected from 1) C_1-7 alkyl, optionally substituted with 1–3 substituents, each independently selected from halogen, and 10) piperazinyl; L represents -O-(C_1-4 alkylene); and ring B is selected from

; n is either 0 or 1, each R^A is independently selected from halogen, optionally substituted with C_1-6 alkyl, wherein the substituent is selected from F, -NH₂, -N(CH₃)₂, optionally substituted with C_1-6 alkoxy, where the substituent is selected from F, R^B and R^C each independently selected from optionally substituted C_1-6 alkyl, where the substituent is selected from F, CF₃; unsubstituted C_2-6 alkenyl, or R^B and R^C together form an optionally substituted C_3-6 cycloalkyl, where the substituent is selected from oxo, -CH₃ where the triple bond in Formula Y is in the meta position relative to the linker L. The invention also relates to a pharmaceutical composition for inhibiting HPK1 activity based on these compounds.

Formula (Y)

EFFECT: obtaining new compounds and a pharmaceutical composition based on them which can be used in medicine in the treatment of cancer.

18 cl, 1 dwg, 2 tbl, 39 ex