| abstract |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel derivatives of 5-(2-imidazolinylamino)- benzimidazole of the general formula (I) where R 1 means methyl, ethyl, cyclopropyl; R 2 means hydrogen atom, C 1 -C 3 -alkyl, halogen atom; R 3 means hydrogen atom, methyl, hydroxy-, cyano-group; R 4 means hydrogen atom, methyl; R 5 means hydrogen atom, methyl, amino-group, halogen atom, cyano-group under condition that at least one of R 2 , R 3 , R 4 , R 5 differs from hydrogen or fluorine atom when R 1 means methyl and both R 2 and R 5 are hydrogen atoms; R 3 can not mean methyl under condition that when R 3 means cyano-group; R 1 means methyl, and any tautomer of the above given structure or pharmaceutically acceptable salt, or biohydrolyzable ester, amide or imide of this compound. Compounds are agonists of alpha-2 adrenoreceptors. Invention describes also pharmaceutical composition with agonistic properties with respect to alpha-2 adrenoreceptors comprising safety and effective amount of compound of the formula (I) and pharmaceutically acceptable carrier. EFFECT: valuable medicinal and pharmacological properties of compounds. 9 cl, 4 tbl |