2-THIO SUBSTITUTED DERIVATIVES OF IMIDAZOLE AND THEIR USE IN PHARMACEUTICALS Russian patent published in 2008 - IPC C07D401/14 C07D401/04 C07D405/14 C07D409/14 A61K31/443 A61K31/4436 A61K31/4439 A61K31/444 

FIELD: chemistry, pharmaceuticals.

SUBSTANCE: invention pertains to 2-thio substituted derivatives of imidazole with formula I , where R¹ represents aryl, which can be substituted by a halogen atom or halogen-C₁-C₆-alkyl; R² is chosen from a group, containing a) aryl-C₁-C₄-alkyl, and b) C₁-C₆-alkyl; R³ is chosen from a group, containing (a) NR⁴R¹⁰, (b) NR⁷COR¹⁰, (c) OR¹⁰, (d) NH₂; R⁴ represents H; R³ and R⁶, which can be the same or different, represent H, halogen, OH, C₁-C₆-alkoxy, C₁-C₆-alkyl or halogen-C₁-C₆-alkyl; R⁷ represents R⁴; R¹⁰ has one of the following values: (a) A-B, (b)-(e), (f) C₁-C₆-alkyl, which is substituted with 2 phenyl groups; A represents linear or branched C₁-C₆-alkylene; B is chosen from a group, containing (a) H, (b)-(e), (f) OC₁-C₆-alkyl, (g) OH; Hy represents 3-10-member non-aromatic, mono-, bi- or tricyclic carbocycle, which can be or not be condensed with a benzene ring; Ar represents 5- or 6- member aromatic heterocycle, which has 1 heteroatom, chosen from a group, consisting of O, S, and N, and which may not be condensed with a benzene ring, Het represents 5- or 6-member non-aromatic heterocycle, which has 1 heteroatom, which represents O, which may not be condensed with a benzene ring; m is 0,1 or 2; or its optical isomers or physiologically used salts. Compounds with formula I are used when making pharmaceutical compositions with inhibiting effect on release of cytokines.

EFFECT: obtaining of derivatives, which have inhibiting action to release of cytokine action.

13 cl, 4 tbl, 148 ex