NOVEL BENZIMIDAZOLE DERIVATIVES AND BASED ON THEM PHARMACEUTICAL COMPOSITION, FOR APPLICATION IN TREATMENT OF VR1-MEDIATED DISORDERS Russian patent published in 2008 - IPC C07D235/08 C07D235/30 C07C205/06 A61K31/502 A61P29/00 

FIELD: chemistry, pharmacology.

SUBSTANCE: claimed invention relates to novel compounds of formula (I) , where R¹ represents H, NO₂, halogeno, NR⁶R⁷, C_1-6alkyl, C_1-6halogenoalkyl, C_1-6halogenoalkylO or R⁶OC_0-6alkyl; m stands for 0, 1, 2 or 3; R² represents NO₂, halogeno, NR⁶R⁷, C_1-6alkyl, C_1-6halogenoalkyl, C_1-6halogenoalkylO, cyano, R⁶C_0-6alkyl, R⁶CO, R⁶OCO, R⁶CONR⁷, R⁶R⁷NCO, R⁸SO₂, R⁸SO₂HN or heteroarylC_0-6alkyl; R³ and R⁹, each irrespectively represents H or C_1-4alkyl; p stands for 0, 1 or 2; n stands for 0, 2, 3 or 4; R⁵ represents C_1-10alkyl, C_6-10arylC_0-6alkyl, C_3-7cycloalkylC_0-6alkyl or C_5-6heteroarylC_0-6alkyl, where heteroaryl contains 1 heteroatom, selected from N, O or S, each aryl can be condensed with aryl, heteroaryl, C_3-7cycloalkyl or C_3-7heterocycloalkyl, which contains up to 2 heteroatoms, selected from N, O or S, and said R⁵ can be substituted with one or more A; A represents H, OH, cyano, R⁶CO, R⁶O(CO), halogeno, C_1-6alkyl, C₁-₆halogenoalkyl, C_1-6halogenoalkylO, R⁶OC_0-6alkyl, hydroxyC_1-6alkyl, R⁸SO₂ or C₆arylO; R⁶ and R⁷ each irrespectively represents H or C_1-6alkyl; and R⁸ represents NR⁶R⁷ or C_1-4alkyl; or its salts, solvates or solvated salts; on condition that said compound does not represent methyl-4-[[(7-methyl-1H-benzimidazole-1-yl)acetyl]-amino]benzoate. Invention also relates to pharmaceutical composition based on compounds of general formula I, application of formula I compounds for preparation of medicine for treating VR1-mediated disorders, to method of treating VR1-mediated disorders and to intermediate compounds.

EFFECT: novel derivatives of benzimidazole possess inhibitory activity with respect to vanilloid receptor.

22 cl, 110 ex