Patent RU-2739356-C2 (RU)
Inventor: O'NILL Lyuk
IPC: C07D231/18
Filed: 2016-02-16
Granted: 2020-12-23
Abstract: 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 R 6  is independently selected from a group, consisting of hydrogen, halo, cyano, C 1 -C 6  alkyl, C 1 -C 6  alkylamino, C 1 -C 6  alkylhydroxy, C 3 -C 6  cycloalkyl, alkylphenyl, phenyl, benzyl, C 1 -C 6  ester, C 2 -C 6  alkenyl, C 1 -C 6  trifluoroalkyl and C 1 -C 6  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; C 6 -C 12  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; NO 2 ; N 3 ; CH 2 OH; CONH 2 ; CONR 24 R 25 ; CO 2 R 24 ; CH 2 OR 24 ; NHCOR 24 ; NHCO 2 R 24 ; C 1-3  alkylthio; sulphate; sulphonic acid; sulfonic acid esters; phosphonic acid; phosphate; phosphonate; mono-, di- or triphosphate esters; trityl; monomethoxytrityl; R 24 SO; R 24 SO 2 ; CF 3 S; CF 3 SO 2 ; and trialkylsilyl; where R 24  and R 25  are each independently selected from H and C 1-10  alkyl; and R 2  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; C 6 -C 12  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; NO 2 ; N 3 ; CH 2 OH; CONH 2 ; CONR 24 R 25 ; CO 2 R 24 ; CH 2 OR 24 ; NHCOR 24 ; NHCO 2 R 24 ; C 1-3  alkylthio; sulphate; sulphonic acid; sulfonic acid esters; phosphonic acid; phosphate; phosphonate; mono-, di- or triphosphate esters; trityl; monomethoxytrityl; R 24 SO; R 24 SO 2 ; CF 3 S; CF 3 SO 2 ; and trialkylsilyl; where R 24  and R 25  are each independently selected from H and C 1-10  alkyl; and R 5  is selected from a group, consisting of hydrogen, halo, cyano, amide, sulphonamide, acyl, hydroxyl, C 1 -C 6  alkyl, C 1 -C 6 -haloalkyl, C 3 -C 5  cycloalkyl and C 1 -C 6  alkoxy, all of which can optionally be optionally substituted with halo, cyano or C 1 -C 6  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