BICYCLIC N-ACYLATED IMIDAZO-3-AMINE OR IMIDAZO-5-AMINE SALTS, METHOD FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2006 - IPC C07D471/04 C07D487/04 C07D513/04 A61K31/435 A61K31/495 A61K31/425 A61K31/415 

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention describes bicyclic N-acylated imidazo-3-amines or imidazo-5-amines salts of the general formula (I): wherein R¹ means tert.-butyl, 1,1,3,3-tetramethylbutyl, (C₄-C₈)-cycloalkyl, phenyl disubstituted with (C₁-C₄)-alkyl, -CH₂R^a wherein R^a means the group -CO(OR') wherein R' means (C₁-C₈)-alkyl; R² means hydrogen atom, the group -COR^b wherein R^b means (C₁-C₈)-alkyl or (C₃-C₈)-cycloalkyl; R³ means (C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl, phenyl, pyridyl, furfuryl or thiophenyl; A means tri-linked fragment of ring of the formula: wherein R⁶ and R⁷ mean hydrogen atom or tetra-linked fragment of ring of the following formulae: wherein R^4' means hydrogen atom or benzyloxy-group; R^5' means hydrogen atom; R^6' means hydrogen atom, (C₁-C₈)-alkyl or nitro- (NO₂)-group; R^7' means hydrogen atom, (C₁-C₈)-alkyl, or R^6' and R^7' mean in common the following fragment of ring: -CRⁱ=CR^j-CH=CH- wherein Rⁱ and R^j mean hydrogen atom; R^5'' means hydrogen, chlorine atom or (C₁-C₈)-alkyl; R^6'' means hydrogen atom; R^7''n means hydrogen atom, amino- (NH₂)-group or (C₁-C₈)-alkyl; R^4''', R^6''' and R^7''' mean hydrogen atom; R⁸ means (C₁-C₈)-alkyl or (C₃-C₈)-cycloalkyl; X means anion of inorganic or organic acid, or their acid-additive compounds. Also, invention relates to a method for their preparing and a pharmaceutical composition based on thereof. These new compounds show affinity to opiate μ-receptor and can be used, in particular, as analgesic agents.

EFFECT: improved preparing method, valuable medicinal properties of compounds and pharmaceutical compositions.

12 cl, 2 dwg, 32 ex