NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH

摘要

The novel class of substituted quinolines represented by the general formula (I): IMAGE (I) where each of R1 and R2 separately represents H or up to three of the groups lower alkyl, halogen, CF3, CN, SO2CH3, NO2, OH, NH2, NHSO2R3, NHCOOR3, OR3, SR3, NHR3or NR3R3 (where R3 is lower alkyl optionally substituted with hydroxy, amino or ether functions), and each of R1 and R2 may additionally separately represent the substitution of an aza (-N=) group for one or two of the methine (-CH=) groups in each of the carbocyclic rings, and R1 may also represent, at positions 2', 3' or 4' only, a phenyl ring optionally further substituted with lower alkyl, halogen, CF3, CN, SO2CH3, NO2, OH, NH2, NHCOR3, NHCOOR3, OR3, SR3, NHR3 or NR3R3 (where R3 is lower alkyl optionally substituted with hydroxy, amino or ether functions); Y represents C(NH)NH2, NHC(NH)NH2 or NR4R5, where each of R4 and R5 is H or lower alkyl optionally substituted with hydroxy, amino or ether functions, or R4 and R5 together with the nitrogen atom form a heterocyclic ring; and n is from 2 to 6; and the acid addition salts and 1-N-oxides thereof, possess antibacterial and antitumor properties.