NEW DERIVATIVES OF BENZIMIDAZOLE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF Russian patent published in 2004 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of benzimidazole of the formula (I):

or its pharmaceutically acceptable salt wherein r' represents group of the formula: -(alk)_q-R¹ wherein (alk) represents alkyl, alkenyl or alkynyl; q = 0 or 1; R¹ represents group of the formula -CO₂R² wherein R² represents hydroxy-alkyl, alkoxy-alkyl or thioalkoxy-alkyl; R'' represents group of the formula:

,

wherein o = 0 or 1; n = 0, 1 or 2; X represents nitrogen atom (N) or CH; Y represents oxygen atom (O), NR¹¹ or CHR¹¹ wherein R¹¹ represents hydrogen atom, alkyl, hydroxy-alkyl, alkoxy-alkyl, carboxyl or acyl, or group of the formula: -(alkyl)_p-CN, -(alkyl)_p-aryl, -(alkyl)_p-O-aryl, -(alkyl)_p-O-aralkyl, -(alkyl)_p-"heterocycle", -(alkyl)_p-CO₂-"heterocycle" or -(alkyl-CO₂)_s-(alkyl)_t-COR⁵ wherein in these formulas p, s and t = 0 or 1 independently; "heterocycle" represents 5-membered monocyclic heterocyclic group that comprises one or more heteroatom representing nitrogen, oxygen or sulfur atom and that is substituted possibly once or more times with substitutes taken among the group consisting of halogen atom, alkyl and oxo-group; R⁵ represents hydroxy-, alkoxy-, hydroxy-(C₁-C₈)-alkoxy-, (C₁-C₈)-alkoxy-alkoxy-, thioalkoxy-alkoxy-group, aryl or aralkyl, or group of the formula -NR⁶R⁷ or -O-alkyl-NR⁶R⁷ wherein in these formulas R⁶ and R⁷ represent independently of one another hydrogen atom or alkyl; R¹⁴ and R¹⁵ represent independently of one another hydrogen atom, alkyl, hydroxy-alkyl, alkoxy-alkyl, carboxyl or acyl; either wherein R' represents group of the formula -(alk)_q-R¹ wherein (alk) represents alkyl, alkenyl or alkynyl; q = 0 or 1; R¹ represents furanyl group; R'' represents -(alkyl)_m-CO₂R⁸ wherein m = 0 or 1; R⁸ represents group of the formula -(alkyl)_p-NR⁹R¹⁰ wherein p = 0 or 1; R⁹ and R¹⁰ in common with nitrogen atom to which they are joined form piperazinyl group that can be substituted with acyl. Also, invention relates to a method for treatment and to pharmaceutical composition used for modulation of GABA_A-receptor complex based on these compounds. Invention provides preparing new compounds and pharmaceutical composition based on thereof for aims of treatment, prophylaxis or relief of small seizures or epileptic status.

EFFECT: valuable medicinal properties of compounds.

16 cl, 10 tbl, 34 ex