Patent ID: 6242457
Filing Date: 2001-06-05
Classification: A61P,C07D

Abstract:
A compound of tormula (I) ##STR8##wherein: R.sub.1 is a --C(R.sub.5).dbd.N--O.sub.(n) R.sub.4 group, wherein R.sub.4 is hydrogen or a C.sub.1 -C.sub.8 linear or branched alkyl or C.sub.1 -C.sub.8 linear or branched alkenyl group or C.sub.3 -C.sub.10 cycloalkyl, or (C.sub.3 -C.sub.10) cycloalkyl-(C.sub.1 -C.sub.8) linear or branched alkyl group, or C.sub.6 -C.sub.14 aryl, or (C.sub.6 -C.sub.14) aryl-(C.sub.1 -C.sub.8) linear or branched alkyl group, or a heterocyclic or heterocyclo-(C.sub.1 -C.sub.8) linear or branched alkyl group, said heterocyclic group containing at least a heteroatom selected from the group consisting of nitrogen atom, optionally substituted with a (C.sub.1 -C.sub.8) alkyl group, and/or oxygen and/or sulfur; said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aryl-alkyl, heterocyclic or heterocyclo alkyl groups, being optionally substituted with one or more groups selected from the group consisting of: halogen, hydroxy, keto, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, phenyl, cyano, nitro, --NR.sub.6 R.sub.7, wherein R.sub.6 and R.sub.7, the same or different between them, are hydrogen, (C.sub.1 -C.sub.8) linear or branched alkyl; the --COOH group or a pharmaceutically acceptable ester thereof; or the --CONR.sub.8 R.sub.9 group, wherein R.sub.8 and R.sub.9, the same or different between them, are hydrogen, (C.sub.1 -C.sub.8) linear or branched alkyl; phenyl; orR.sub.4 is a (C.sub.6 -C.sub.10) aroyl or (C.sub.6 -C.sub.10) arylsulfonyl group, optionally substituted with one or more groups selected from the group consisting of: halogen, hydroxy, C.sub.1 -C.sub.8 linear or branched alkyl, (C.sub.1 -C.sub.8) linear or branched alkoxy, phenyl, cyano, nitro, --NR.sub.10 R.sub.11, wherein R.sub.10 and R.sub.11, the same or different between them are hydrogen, C.sub.1 -C.sub.8 linear or branched alkyl; orR.sub.4 is a polyaminoalkyl group;n is the number 1;R.sub.5 is hydrogen, C.sub.1 -C.sub.8 linear or branched alkyl, C.sub.1 -C.sub.8 linear or branched alkenyl, C.sub.3 -C.sub.10 cycloalkyl, (C.sub.3 -C.sub.10) cycloalkyl-(C.sub.1 -C.sub.8) linear or branched alkyl, C.sub.6 -C.sub.14 aryl, (C.sub.6 -C.sub.14) aryl-(C.sub.1 -C.sub.8) linear or branched alkyl;R.sub.2 and R.sub.3, the same or different between them are hydrogen, hydroxy, C.sub.1 -C.sub.8 linear or branched alkoxy;their N.sub.1 -oxides, their single isomers, their possible enantiomers, diastereoisomers and relative admixtures, the pharmaceutically acceptable salts thereof and their active metabolites;with the proviso that when R.sub.5, R.sub.2 and R.sub.3 are hydrogen, then R.sub.4 is different from hydrogen.