DERIVATIVES OF INDOLE ELICITING ANTIVIRAL ACTIVITY Russian patent published in 2003 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to new derivatives of indole of the formula (I): wherein R¹ means hydrogen atom, (lower) alkyl, (lower) alkylsulfonyl, optionally substituted aryl, optionally substituted aryl(lower)-alkyl, C₃-C₆-cycloalkyl-(lower)- alkyl, morpholinyl-(lower)-alkyl, sulfamoyl optionally substituted with lower alkyl, carbamoyl optionally substituted with lower alkyl or phenyl, lower alkylsulfinyl, morpholinylsulfonyl, thienyl-(lower)-alkyl optionally substituted with lower alkoxycarbonyl or carboxyl, pyridyl-(lower)-alkyl, optionally substituted phenylsulfonyl, thienylsulfonyl, phenylcarbonyl, lower alkoxycarbonyl; R² means hydrogen atom, optionally substituted phenyl, optionally substituted phenyl-(lower)-alkyl, phenylcarbonyl, lower alkyl, optionally substituted phenylsulfonyl, optionally substituted phenylsulfinyl, morpholino-(lower)-alkyl being each of mentioned substituted phenyl groups can carry substituents taken among halogen atom, trihaloidsubstituted lower alkyl, lower alkoxyl, azido, nitro, amino, phenyl, lower alkoxycarbonyl, amino-group (substituted with lower alkyl or lower alkylcarboxy), aryl-(lower)-alkyl, lower alkyl, carboxyl; among R³, R⁴, R⁵, R⁶ each means independently hydrogen, halogen atom, trihaloidsubstituted (lower)-alkyl, hydroxy, (lower)-alkoxy, nitro, phenylsulfonyloxy, phenyl-(lower)-alkoxy, carboxy, lower alkoxycarbonyl optionally substituted with phenyl; X means hydroxy, amino optionally substituted with lower alkyl or lower alkoxy-(lower)-alkyl; Y means COOR (wherein R means hydrogen atom, lower alkyl optionally substituted with phenyl), tetrazolyl optionally substituted with trityl, imidazolyl, triazolyl, pyrazolyl, phenyl optionally substituted with carboxy- group, lower alkoxyl or hydroxy-group; under condition that compounds where each of R¹, R², R³, R⁵, R⁶ means hydrogen atom are excluded; R⁴ means hydroxy-group; Y means COOC₂H₅, their tautomers, pharmaceutically acceptable salts or hydrates that elicit activity inhibiting activity of integrase that allows their using in pharmaceutical composition against HIV-infection. EFFECT: valuable medicinal properties of compounds. 16 cl, 16 tbl, 144 ex