SULFONYL UREA AND RELATED COMPOUNDS AND USE THEREOF Russian patent published in 2020 - IPC C07D231/18 C07D307/64 C07D311/60 C07D401/06 C07D403/12 C07D405/12 C07D407/12 C07D413/12 C07D213/74 C07D249/12 C07D271/12 C07D333/34 C07D277/36 C07D241/24 C07D235/02 C07D261/18 C07D207/38 C07D495/06 C07D498/04 A61K31/64 A61P35/00 A61P25/00 

FIELD: pharmaceuticals.

SUBSTANCE: present invention relates to sulphonyl urea of formula (II) or pharmaceutically acceptable salts thereof:

,

where A, B, D and E are independently selected from C, N, O and S, but at least one of them is C and at least one of them is N; each dashed line can denote a link; each occurrence of R₆ is independently selected from a group, consisting of hydrogen, halo, cyano, C₁-C₆ alkyl, C₁-C₆ alkylamino, C₁-C₆ alkylhydroxy, C₃-C₆ cycloalkyl, alkylphenyl, phenyl, benzyl, C₁-C₆ ester, C₂-C₆ alkenyl, C₁-C₆ trifluoroalkyl and C₁-C₆ alkoxy, each of which can be optionally substituted, optionally, where any optional substitute is independently selected from a group consisting of C_1-10 alkyl; C_3-6 cycloalkyl; hydroxyalkyl; C_1-10 alkoxy; C_2-10 alkenyl; C_2-10 alkynyl; C₆-C₁₂ aryl; aryloxy; heteroaryl containing from one to four heteroatoms selected from N, O and S; heterocyclyl having from 5 to 8 atoms in the ring, and from said atoms from 1 to 4 are heteroatoms selected from N, O and S; halo; hydroxyl; halogenated alkyl; amino; alkylamino; arylamino; acyl; amido; CN; NO₂; N₃; CH₂OH; CONH₂; CONR₂₄R₂₅; CO₂R₂₄; CH₂OR₂₄; NHCOR₂₄; NHCO₂R₂₄; C_1-3 alkylthio; sulphate; sulphonic acid; sulfonic acid esters; phosphonic acid; phosphate; phosphonate; mono-, di- or triphosphate esters; trityl; monomethoxytrityl; R₂₄SO; R₂₄SO₂; CF₃S; CF₃SO₂; and trialkylsilyl; where R₂₄ and R₂₅ are each independently selected from H and C_1-10 alkyl; and R₂ is selected from 2,6-dialkylphenyl, 2,6-dialkyl-4-halophenyl, 2,6-dicycloalkylphenyl, 2,6-dicycloalkyl-4-halophenyl, and:

,

where each case Y is independently selected from C, N, S and O, which can be optionally substituted, optionally, where any optional substitute is independently selected from a group consisting of C_1-10 alkyl; C_3-6 cycloalkyl; hydroxyalkyl; C_1-10 alkoxy; C_2-10 alkenyl; C_2-10 alkynyl; C₆-C₁₂ aryl; aryloxy; heteroaryl containing from one to four heteroatoms selected from N, O and S; heterocyclyl having from 5 to 8 atoms in the ring, and from said atoms from 1 to 4 are heteroatoms selected from N, O and S; halo; hydroxyl; halogenated alkyl; amino; alkylamino; arylamino; acyl; amido; CN; NO₂; N₃; CH₂OH; CONH₂; CONR₂₄R₂₅; CO₂R₂₄; CH₂OR₂₄; NHCOR₂₄; NHCO₂R₂₄; C_1-3 alkylthio; sulphate; sulphonic acid; sulfonic acid esters; phosphonic acid; phosphate; phosphonate; mono-, di- or triphosphate esters; trityl; monomethoxytrityl; R₂₄SO; R₂₄SO₂; CF₃S; CF₃SO₂; and trialkylsilyl; where R₂₄ and R₂₅ are each independently selected from H and C_1-10 alkyl; and R₅ is selected from a group, consisting of hydrogen, halo, cyano, amide, sulphonamide, acyl, hydroxyl, C₁-C₆ alkyl, C₁-C₆-haloalkyl, C₃-C₅ cycloalkyl and C₁-C₆ alkoxy, all of which can optionally be optionally substituted with halo, cyano or C₁-C₆ alkoxy, having useful activity in inhibiting activation of the inflammasome NLRP3.

EFFECT: proposed are sulphonyl urea and related compounds and use thereof.

36 cl, 2 dwg, 10 tbl