SUBSTITUTED DERIVATIVES OF BENZOQUINOLISINE Russian patent published in 2010 - IPC C07D471/04 A61K31/4745 A61P3/10 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of general formula: I, where R¹ is selected from hydrogen or methoxy; R² is selected from a group consisting of hydroxy, lower alkoxy, provided that R² does not denoe methoxy when R¹ denotes methoxy, lower alkoxy, mono- or di-substituted with a hydroxy group, benzyloxy, amino, alkylamino, dialkylamino, cyano group, unsubstituted phenyl or tetrazolyl, -O-(CH₂)_m-C(O)-NR⁸R⁹, where m equals 1 or 2, and where R⁸ and R⁹ are independently selected from hydrogen, lower alkyl or tetrazolyl, or R⁸ and R⁹ together with the nitrogen atom with which they are bonded form morpholinyl or piperazinyl, -O-(CH₂)_n-COOR¹⁰, where n equals 1 or 2 and R¹⁰ denotes hydrogen or lower alkyl, -O-(CH₂)_p-NH-C(O)-OR¹¹, where p equals 1 or 2,and where R¹¹ denotes lower alkyl, -O-SO₂-R¹², where R¹² denotes lower alkyl, -NR¹³R¹⁴, where R¹³ denotes hydrogen or lower alkyl, and R¹⁴ denotes lower alkyl or benzyl, and -NH-CO-(CH₂)_q-R¹⁵, where q equals 1 or 2, and where R⁵ denotes tetrazolyl; R³ is selected from a group consisting of hydrogen, hydroxy, lower alkoxy, lower alkoxy which is mono- or di-substituted with a hydroxy group, alkoxy or unsubstituted phenyl, and -O-(CH₂)_m-C(O)-NR⁸R⁹, where m equals 1 or 2, and where R⁸ and R⁹ are independently selected from hydrogen or lower alkyl, or R⁸ and R⁹ together with the nitrogen atom with which they are bonded form morpholinyl or piperazinyl, which can be substituted with lower alkyl; R⁴ is or , where R⁵ is selected from lower alkyl; or R5 can also denote hydrogen when selected from a group consisting of -(CH₂)_m-C(O)-NR⁸R⁹, -O-(CH₂)_p-NH-C(O)-OR¹¹, -O-SO₂-R¹², -NR¹³R¹⁴, -NH-CO-(CH₂)_q-R¹⁵ and lower alkoxy which is mono- or di-substituted with a group selected from hydroxy, benzyloxy, amino or cyano; R⁶ is selected from a group consisting of hydrogen and lower alkyl; R⁷ is selected from a group consisting of lower alkyl and lower halogenalkyl; and to pharmaceutically acceptable salts of said compounds. The invention also pertains to a pharmaceutical composition.

EFFECT: obtaining novel biologically active compounds having DPP-IV enzyme inhibiting activity.

22 cl, 50 ex