NOVEL DNA GYRASE INHIBITORS, PROCESS FOR THEIR MANUFACTURE AND PHARMACEUTICAL PREPARATIONS CONTAINING SAME

摘要

Bicyclic derivatives of general formula (I), wherein X<1> is -S- or -SO-; X<2> is -CO- or -CS-; R<1> is hydrogen, halogen or lower alkyl optionally substituted by halogen or lower alkoxy; R<2> and R<3> are each independently hydrogen, lower alkyl, halogen, amino, lower alkylamino, di-lower alkylamino, acylamino, lower alkoxy, lower alkoxymethoxy or a group OR<4>; R<4> is hydrogen or an easily hydrolyzable group; R<5> is hydrogen, optionally esterified carboxy or amidated (thio)carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted acyl or heterocyclyl; R<6> and R<7a> are each independently hydrogen or lowe alkyl; R<7b> is hydrogen, optionally substituted hydroxy, -NR-A or -N=B, in which R is hydrogen or lower alkyl, A is hydrogen, optionally substituted alkyl, lower cycloalkyl, iminoyl, (thio)acyl, esterified carboxy or amidated (thio)carboxy and B is lower alkylidene; R<7a> and R<7b> together represent oxo, lower alkoxycarbonylmethylidene or optionally substituted hydroxyimino; and R<8> is hydrogen, optionally substituted alkyl, optionally esterified carboxy or amidated(thio)carboxy; provided that no more than two of R<1>-R<3> are nitrogen-containing groups; no more than two of R<1>-R<3> are oxygen containing groups and no more than two of R<1>-R<3> are either nitrogen containing or oxygen containing groups; and pharmaceutically acceptable salts of the compounds of formula (I) carrying an acidic and/or basic substituent. The products are antimicrobially active.