BIS-BENZIMIDAZOLE DERIVATIVES AS HEPATITIS C VIRUS INHIBITORS Russian patent published in 2015 - IPC C07D403/14 C07D401/14 C07D405/14 A61K31/4402 A61K31/4184 A61P31/14 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to bis-benzimidazole derivatives of formula I and their optional stereoisomers, pharmaceutically acceptable salts and solvates, wherein R and R' are independently specified in -CR₁R₂R₃, phenyl substituted by 1 substitute specified in halogen; and tetrahydrofuranyl, wherein R₁ is specified in C_1-4alkyl optionally substituted by methoxy, hydroxyl or dimethylamino; C_3-6cycloalkyl; phenyl optionally substituted by 1, 2 or 3 substitutes optionally specified in halogen, C_1-4alkoxy, trifluoromethoxy, or 2 substitutes on adjoining atoms of the ring form 1,3-dioxolane group; benzyl substituted by halogen or methoxy; pyridinyl; indolyl; pyridinylmethyl or indolylmethyl; R₂ is specified in hydrogen, hydroxyl, di-C_1-4alkylamino, (C_3-6cycloalkyl) (C_1-4alkyl)amino, C_1-4alkylcarbonylamino, phenylamino, C_1-4alkyloxycarbonylamino, (C_1-4alkyloxycarbonyl)(C_1-4alkyl)amino, C_1-4alkylaminocarbonylamino, tetrahydro-2-oxo-1(2H)-pyrimidinyl, pyrrolidin-1-yl, piperidin-1-yl, 3,3-difluoropiperidin-1-yl, morpholin-1-yl, 7-azabicyclo[2.2.1]hept-7-yl and imidazol-1-yl; and R₃ represents hydrogen or C_1-4alkyl or CR₂R₃ together form carbonyl; or CR₁R₃ form cyclopropyl group. The invention also refers to a pharmaceutical composition based on a compound of formula I.

EFFECT: there are prepared bis-benzimidazole derivatives possessing the inhibitory activity on hepatitis C virus.

9 cl, 4 tbl, 3 ex