OXADIAZOLE-BASED CHANNEL INHIBITORS WITH TRANSIENT POTENTIAL Russian patent published in 2024 - IPC C07D471/04 C07D473/30 C07D487/04 A61K31/427 A61K31/437 A61K31/4375 A61K31/4985 A61K31/5025 A61K31/519 A61K31/522 A61K31/53 A61P11/00 A61P29/00 

FIELD: medicine; pharmaceutics.

SUBSTANCE: invention relates to compounds based on oxadiazoles and pharmaceutically acceptable salts thereof, represented by general formula I, where A is heterocyclic structural fragments given in the claim; X is C_1-4alkylene; n is equal to 1; R¹ is H; each R² is independently H, D, -C_1-4alkyl, -C_1-4haloalkyl, C_1-4alkoxy, -CN, halogen and NR¹⁴R¹⁵; each R³ is independently H, D, -C_1-4alkyl, -CN, NR¹⁴R¹⁵ or halogen; R⁴ is unsubstituted phenyl or phenyl substituted with 1–3 substitutes selected from halogen, -CN, -C_1-4alkyl, unsubstituted C_3-6cycloalkyl, C_1-4haloalkyl, C_1-4haloalkoxy, C_1-4alkoxy, pentafluorosulfanyl or unsubstituted phenyl; unsubstituted heteroaryl or heteroaryl substituted with 1 substituent selected from halogen and C_1-4alkyl, where heteroaryl is selected from pyrazole, pyridine, benzothiazole; or unsubstituted naphthyl; or R¹ and R⁴ can together form unsubstituted C_3-6cycloalkyl, fused with unsubstituted phenyl; p is 0, 1 or 2; q is 0 or 1; each of R¹⁴ and R¹⁵ independently represents: H; substituted with one pyridine or unsubstituted -C_1-4alkyl; substituted with one C_1-4alkyl or unsubstituted 4–6 membered heterocycloalkyl containing one nitrogen atom; or R¹⁴ and R¹⁵ together with the atoms to which they are attached can form 6-member ring containing one additional heteroatom selected from O, N. Invention also relates to compounds represented by structural formulas IVa and IVb, specific compounds (shown in the claim), a pharmaceutical composition, use and a method of inhibiting TRPA1 activity.

EFFECT: compounds used to treat TRPA1-mediated diseases.

36 cl, 2 tbl, 9 ex