6,7,8,9-SUBSTITUTED 1-PHENYL-1,5-DIHYDRO-PYRIDO[3,2-B]INDOL-2-ONES USEFUL AS ANTI-INFECTIVE PHARMACEUTICAL AGENTS

摘要

This invention concerns the compounds (I); the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein X is NR<2>, O, S, SO, SO2; R<1> is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; n is 1, 2 or 3; R<2> is hydrogen, aryl substituted with a radical -COOR<4>; or R<2> is substituted C1-10alkyl, C2-10alkenyl or C3-7cycloalkyl; or R<2> is a radical of formula: (b-1); (b-2); -CpH2p-CH(OR<14>)-CqH2q-R<15> (b-3); -CH2-CH2-(O-CH2-CH2)m-OR<14> (b-4); -CH2-CH2-(O-CH2-CH2)m-NR<5a>R<5b> (b-5); -a<1>=a<2>-a<3>=a<4>- is -CH=CH-CH=CH- ; -N=CH-CH=CH- ;-CH=N-CH=CH- ; -CH=CH- N=CH- ; -CH=CH-CH=N- (c-5); wherein one of the hydrogen atoms in (c-1) - (c-5) is replaced by particular radicals; R<3> is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, substituted carbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy- methanimidamidyl or Het1.