ANTI-PROLIFERATIVE COMPOUNDS AND THEIR APPLICATIONS Russian patent published in 2024 - IPC C07D413/14 C07D403/04 C07D409/14 C07D413/04 C07D417/14 A61K31/553 A61P35/00 

FIELD: pharmaceutics.

SUBSTANCE: compounds of formula I' or their pharmaceutically acceptable salts, pharmaceutical compositions based on them, as well as a method for treating cancer, a method for inducing ER stress, a method for inducing an unfolded protein response (UPR), a method for inducing an unfolded protein response (UPR) and a method for inducing releasing calcium from the endoplasmic reticulum (ER) through a putative Ca²⁺ channel known as Wolframin (WFS1) using them. In the general formula I', ring A is a ring selected from phenyl, an 8-12 membered partially unsaturated bicyclic heterocyclic ring containing 1-2 heteroatoms independently selected from nitrogen, oxygen or sulfur, a 5-6 membered heteroaromatic ring containing 1 -4 heteroatoms independently selected from nitrogen or sulfur; or an 8-10 membered bicyclic heteroaromatic ring containing 1-5 heteroatoms independently selected from nitrogen; each R¹ independently represents hydrogen or straight or branched hydrocarbon chain C_1-3, optionally substituted with 1-6 halogens; each of R² independently represent hydrogen, halogen, -CN, -NO₂, -C(O)OR, -C(O)NR₂, -NR₂, -NRC(O)R, -NRC(O)OR , -NRS(O)₂R, -OR, -P(O)R₂, -SR, -S(O)R, -S(O)₂R, -S(O)(NH)R, -S(O)₂NR₂ or R; the two R² groups are optionally taken together to obtain =O; or two R ² groups are optionally taken together with their intermediate atoms, obtaining a 3-membered saturated spirocyclic ring containing 0 of the heteroatom; each R³ independently represents hydrogen, -OH or a linear or branched hydrocarbon chain C_1-3; or the two R³ groups are optionally taken together to give =O; or the two R³ groups are optionally taken together to give =CH₂ ; or the two R³ groups are optionally taken together with their intermediate atoms, yielding a 3-8 membered saturated spirocyclic ring containing 0-2 of the heteroatoms independently selected from oxygen; X represents -O- or -CH₂-; m is 0, 1 or 2; n is 0, 1, 2, 3, 4 or 5; and p is 0, 1 or 2.

EFFECT: anti-proliferative compounds are proposed.

67 cl, 6 tbl, 60 ex

I’