TETRASUBSTITUTED BENZENES Russian patent published in 2014 - IPC C07C59/72 C07C205/56 C07C211/44 C07C255/57 C07C311/29 C07C323/62 C07C59/64 C07C62/12 C07C62/14 C07D271/08 C07D277/62 C07D285/14 C07D309/08 C07C205/37 C07C205/55 C07C229/42 C07C323/18 C07C69/734 C07C69/757 C07D271/12 C07D277/64 A61K31/192 A61K31/196 A61K31/216 A61K31/351 A61K31/4245 A61K31/428 A61K31/433 A61P25/28 A61P43/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula III or to its pharmaceutically acceptable salts, in which: R₁ and R₂ are independently selected from group, consisting of: (a) H, (b) (C₂-C₆)alkyl, (c) C₁-C₆ alkyl, interrupted by one or more groups -O-, (d) (C₀-C₃)alkyl-(C₃-C₇)cycloalkyl and (e) (CH₂)_nQ, where n=1-2 and where Q stands for aromatic ring system, which has from 5 to 6 ring atoms C, and Q can be independently substituted with groups up to 3 in number, selected from halogen, on condition that R₁ and R₂ simultaneously do not stand for H, and each alkyl of R₁ and R₂ can be independently substituted with one or more groups, selected from group, consisting of halogen, hydroxy, cyano, CF₃ or C₁-C₄ alkyl, or R₁ and R₂ together with carbon, to which they are attached, form 3-7-member cycloalkyl or 6-member heterocycloalkyl ring, including one oxygen atom and which in case of necessity carries C₁-C₄ alkyl substituent, or R₁ and R₂ together with carbon, to which they are connected, form 3-7-member cycloalkyl ring, substituted with R₂₀ and R₂₁, and R₂₀ and R₂₁ together with carbon or carbons, to which they are connected, form 3-7-member cycloalkyl ring; R₆ stands for C₁-C₆ alkyl; each R₇ independently stands for C₁-C₆ alkyl; Y stands for -O-; R₄ is selected from group, consisting of: (a) (C₀-C₃)alkyl-(C₃-C₇)cycloalkyl, (b) trifluoroethyl, and (c) trifluoropropyl; Z stands for phenyl or bicyclic ring system, which has 9 ring atoms, independently selected from C, N, O and S, on condition that not more than 3 ring atoms in any single ring differs from C, and said ring system can carry to 3 substituents, independently selected from group, consisting of R₆, CF₃ and SR₆; and R₅ is selected from group, consisting of NO₂, NH₂, F, Cl, Br, CN, SR₆, S(O)₂N(R₇)₂ and (C₁-C₄)alkyl, and each alkyl can be independently substituted with one or more halogens or CF₃. Invention also relates to pharmaceutical composition for treatment of neurodegenerative disorder or improvement of cognitive function, containing therapeutically effective quantity of said compound; as well as to method of treatment of neurodegenerative disorder, for instance Alzheimer's disease, or improvement of cognitive function.

EFFECT: compounds act as modulators of gamma-secretase.

31 cl, 14 tbl, 3147 ex, 1 dwg