| 摘要 |
The present invention concerns the compounds having the formula (I), wherein N- oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1 - 6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aRl0b)CR9-; t is 0, 1 or 2; R2 is H or C1 - 6alkyl; L is -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-C1-6alkanediyl-C(=O)-, -NR8 - C1-6alkanediyl-C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2 ; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1 - 4alkylOC(=O), carboxyl, aminoC(=O), mono- or di(C1-4alkyl)aminoC(=O), C3- 7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, -C(=O)-, -C(=S)-, -S(=O)2-, C1-6alkanediyl-C(=O)-, C1-6 alkanediyl-C(=S)- or C1-6alkanediyl-S(=O)2-; R5 is H, OH, C1-6alkyl, Het1C1- 6alkyl, Het2C1-6 alkyl, optionally substituted amino~-C1-6alkyl; R6 is C1- 6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6 alkyloxy~carbonylamino or amino; and in case _A- is other than C1-6alkanediyl then R6 may also be C1- 6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1 - 4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups i n the definitionof R6 may optionally be substituted; R5 and _A-R6 taken together with the nitrogen atom to which they are attached may also form Het 1 or Het2, R12 , is H, - NH2, _NR5AR6, - C1-6alkyl or alkyl-W-R14 , wherein sa id alkyl is optionally substituted with halogen, hydroxy, aryl, heteroaryl, Het 1, Het2, or amino wherein said amino is optionally mono- or di-substituted with C1-4alkyl 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 C1-4alkyl.
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