| abstract |
The present invention concerns the compound having the formula: N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6 alkyl, C2-6 alkenyl, C3-7 cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC((R10aR10b)CR9-; t is 0, 1 or 2; R2 is H or C1-6 alkyl; L is -C(=O)-, -O-C(=O)-, NR8-C(=O)-, -O-C1-6 alkanediyl-C(=O)-, -NR8-C1-6 alkanediyl-C(=O)-, -S(=O)-, -O-S(=O)2-, -NR8-S(-O)2; R3 is C1-6 alkyl, aryl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl, or aryl C1-4 alkyl; R4 is C1-4 alkylOC(=O), carboxyl, aminoC(=O), mono- or di(C1-4 alkyl)amino(C1-4 alkyl)aminoC(=O), C3-7 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl or optionally substituted C1-6 alkyl; A is C1-6 alkanediyl, -C(=O)-, - C(=S)-; R5 is H, OH, C1-6 alkyl, Het1 C1-6 alkyl, Het2 C1-6 alkyl, optionally substituted amino- C1-6 alkyl; R6 is C1-6 alkylO, Het1 Het1O, Het2 Het2O, aryl, arylO, C1-6 alkyloxy-carbonyamino or amino; and in case -A- is other than C1-6 alkanediyl then R6 may also be C1-6 alkyl, Het1C1-4 alkyl, Het1OC1-4 alkyl, Het2C1-4 alkyl, Het2OC1-4 alkyl, arylC1-4 alkyl, arylOC1-4 alkyl or aminoC1-4 alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also from? Het1 or Het2-R12 is H, -NH2, -NR5AR6, -C1-4 alkyl or alkyl-W-R14, wherein said alkyl is optionally substituted with halogen, hydroxy, aryl, heteroaryl, Het1, Het2, or amino wherein said amino is optionally mono- or di-substituted with C1-4 alkyl and R13 is H, C1-6 alkyl, optionally substituted by aryl, Het1, Het2, hydroxy, halogen, amino whereby the amino group may be optionally be mono- or di-substituted with C1-4 alkyl. |