BICYCLIC DERIVATIVES OF IMIDAZO-3-YLAMINE, METHOD FOR THEIR PREPARING AND MEDICINAL AGENT BASED ON THEREOF Russian patent published in 2005 - IPC

FIELD: organic chemistry, chemical technology, pharmacy.

SUBSTANCE: invention describes derivatives of imidazo-3-ylamine of the general formula (I):

wherein X and Y mean CH or nitrogen atom (N) under condition that X and Y don't mean nitrogen atom (N) simultaneously; R¹ means tert.-butyl, (CH₂)_nCN wherein n means 4, 5 or 6, phenyl substituted optionally with (C₁-C₄)-alkyl, (C₁-C₄)-alkoxy-group, (C₄-C₈)-cycloalkyl, 1,1,3,3-tetramethylbutyl or CH₂R^a wherein R^a represents hydrogen atom, branched or linear (C₁-C₈)-alkyl, phenyl substituted optionally with halogen atom, (C₁-C₄)-alkoxy-group, CO(OR') wherein R' means linear (C₁-C₄)-alkyl or branched (C₃-C₅)-alkyl, PO(OR')₂ wherein R' means linear (C₁-C₄)-alkyl or branched (C₃-C₅)-alkyl; R² means hydrogen atom, COR^b wherein R^b represents branched or linear (C₁-C₄)-alkyl; R³ means methyl, ethyl, tert.-butyl, (C₃-C₈)-cycloalkyl, phenyl monosubstituted optionally at position 3, 5 or 6 or optionally multisubstituted at position 4 and additionally at position 2 and/or 3, and/or 5, and/or 6 with halogen atom, hydroxyl group (OH), (C₁-C₄)-alkyl or (C₁-C₄)-alkoxy-group, naphthyl, optionally substituted (C₁-C₄)-alkoxy-group, di-(C₁-C₄)-alkylamino-group, pyrrole substituted optionally with (C₁-C₄)-alkyl, benzylsulfonyl, COOCH₃, pyridyl substituted optionally with (C₁-C₄)-alkyl, OH, hydroxy-(C₁-C₄)-alkyl, furan substituted optionally with (C₁-C₄)-alkyl, nitro-group (-NO₂), halogen-substituted phenyl, CH₂COOCH₃, COOH, thiophene substituted optionally with halogen atom, (C₁-C₄)-alkyl, (C₁-C₄)alkylsulfanyl, -NO₂, phenoxy-group, thiophene, alkynylphenyl, unsubstituted anthracene or quinoline substituted optionally with halogen atom under condition that R³ doesn't means cyclohexyl-unsubstituted phenyl or phenyl monosubstituted with carboxylic acid amide at position 3 if R¹ means tert.-butyl, n-propyl, n-butyl, 1,1,3,3-tetramethylbutyl, cyclohexyl, monosubstituted phenyl, 2,6-dimethylphenyl or benzyl, and R² means simultaneously hydrogen atom or -CO-(methyl) and under condition that R² doesn't mean hydrogen atom if R¹ means benzyl simultaneously and R³ means methyl or R¹ means simultaneously CH₂C(O)-tert.-butyl and R³ means unsubstituted phenyl, in forms of bases or pharmaceutically acceptable salts, and a method for their preparing and a medicinal agent based on thereof. Described compounds possess analgesic activity and can be used in medicine.

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

7 cl, 2 tbl, 33 ex