SULPHONAMIDE DERIVATIVES Russian patent published in 2010 - IPC C07D223/08 C07D403/12 C07D405/12 C07D409/12 A61K31/55 A61P35/00 A61P25/28 

FIELD: chemistry.

SUBSTANCE: present invention relates to novel sulphonamide derivatives of general formula (I) , where R¹ is phenyl, thiophenyl or furanyl, unsubstituted or substituted with one or two substitutes selected from a group consisting of halogen, lower alkyl, lower alkyl substituted with halogen, -O-lower alkyl substituted with halogen, NO₂ or CN; R²-R⁴ and R^2'-R^4' is hydrogen, lower alkyl, phenyl or lower alkyl substituted with halogen; R⁵ is phenyl, pyridinyl, benzo[1,3]dioxolyl or benzofuranyl, unsubstituted or substituted with 1-3 substitutes selected from a group consisting of halogen, lower alkyl, lower alkyloxy, CN, nitro, amino, hydroxy, lower alkyl substituted with hydroxy, lower alkyl substituted with halogen, or substituted with -C(O)-NR"₂, -(CR₂)_m-C(O)-R', -(CH₂)_m-heteroaryl, unsubstituted or monosubstituted -(CH₂)_m-lower alkoxy, lower alkyl, -(CH₂)_m-O-benzene or CH₂OH, -O-C(O)-lower alkyl, -O-C(O)-NR₂, -O-(CH₂)_m-C(O)OH, -O-lower alkynyl, -O-lower alkyl, substituted with halogen, -O-(CH₂)_m-heterocyclyl, -O-(CH₂)_m-phenyl, unsubstituted or monosubstituted hydroxy, -O-(CH₂)_m-heteroaryl, unsubstituted or monosubstituted with lower alkyl, -(CH₂)_m-NH-C(O)R', -(CH₂)_m-NH-S(O)₂-R', -S(O)₂-lower alkyl, -S(O)₂-heterocyclyl, -S(O)₂NH-cycloalkyl, or is C₃-₆cycloalkyl; R' is hydrogen, lower alkyl, lower alkynyloxy, hydroxy, C_3-6cycloalkyl, heterocyclyl, which is unsubstituted or substituted with one or two substitutes selected from COOH, -C(O)O-lower alkyl, halogen or lower alkyl, or is phenyl, benzyl, heteroaryl, -(CH₂)_m-lower alkoxy or -(CHR)_m-C(O)O-lower alkyl; R" is hydrogen, C_3-6cycloalkyl, which is unsubstituted or substituted with one or two substitutes selected from halogen, or is lower alkyl, lower alkyl substituted with halogen, lower alkyl substituted with hydroxy, -(CH₂)_m-heterocyclyl, -NR₂, heteroaryl, benzyl or -(CHR)_m-C(O)O-lower alkyl; R is hydrogen or lower alkyl; X is -CHR-; m equals 0, 1, 2 or 3; and its pharmaceutically acceptable salts of an acid compound, optically pure enantiomers, racemates or diastereomeric mixtures. The invention also relates to medicine containing a formula I compound.

EFFECT: obtaining novel compounds which inhibit γ-secretase.

16 cl, 230 ex