BENZIMIDAZOLON AND CHINAZOLIN DERIVATIVES AS HUMAN ORL1-RECEPTOR AGONISTS Russian patent published in 2009 - IPC C07D401/04 C07C251/20 C07D451/04 A61K31/46 A61K31/517 A61K31/454 A61P25/00 A61P1/14 A61P9/12 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of general formula (I), their optically active stereoisomers, as well as to pharmaceutically acceptable salts possessing properties of ORL1 and µ-opiate receptors. In general formula , R1 represents H, alkyl(1-6C), []_m represents-(CH₂)_m-, in which m equals 0 or 1, R₂ represents halogen, CF₃, alkyl(1-6C), phenyl, cyano, cyanoalkyl(1-3C), hydroxy, (1-3C)alkoxy, OCF₃, acyl(2-7C), trifluoroacetyl, (1-3C)alkylsulfonyl or trifluoromethylsulfonyl, and n represents integer number 0-4 on condition that when n equals 2, 3 or 4, R₂ substituents can be similar or different, A represents saturated ring, []₀ and []_p represents -(CH₂)_o and -(CH₂)_p, and o and p independently correspond to 0, 1 or 2, R₃, R₄, R₅ and R₆ independently represent hydrogen, alkyl(1-3C), or (R₄ and R₆) together can form alkylene bridge, containing 1-3 carbon atoms on condition that when o equals 2, R₃ represents hydrogen, and when p equals 2, R₅ represents hydrogen, R₇ represents H, halogen, alkyl(1-6C). Invention also relates to pharmaceutical composition, intermediate compounds for obtaining formula (1) compounds.

EFFECT: compounds can be used for preparing medication for treating disorders and diseases such as alimentary behaviour disturbances, arterial hypertension.

8 cl, 3 dwg, 1 tbl, 45 ex