DOMINIQUE LOUIS NESTOR GHISLAIN SURLERAUX,PIET TOM BERT PAUL WIGERINCK,MARIEKE CHRISTIANE JOHANNA VOETS,SANDRINE MARIE HELENE VENDEVILLE,HERMAN AUGUSTINUS DE KOCK,BERNHARD JOANNA BERNARD VERGOUWEN
申请号：
PL37415203
公开号：
PL213645B1
申请日:
2003.03.12
申请国别(地区):
PL
年份:
2013
代理人:
摘要：
The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2； R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9&mdash；； t is 0, 1 or 2； R2 is H or C1-6alkyl； L is &mdash；C(&boxH；O)&mdash；, &mdash；O&mdash；C(&boxH；O)&mdash；, &mdash；NR8&mdash；C(&boxH；O)&mdash；, &mdash；O&mdash；C1-6alkanediyl-C(&boxH；O)&mdash；, &mdash；NR8&mdash；C1-6alkanediyl-C(&boxH；O)&mdash；, &mdash；S(&boxH；O)2&mdash；, &mdash；O&mdash；S(&boxH；O)2&mdash；, &mdash；NR8&mdash；S(&boxH；O)2； R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl； R4 is H, C1-4alkylOC(&boxH；O), carboxyl, aminoC(&boxH；O), mono- or di(C1-4alkyl)aminoC(&boxH；O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl； A is C1-6alkanediyl, &mdash；C(&boxH；O)&mdash；, &mdash；C(&boxH；S)&mdash；, &mdash；S(&boxH；O)2&mdash；, C1-6alkanediyl-C(&boxH；O)&mdash；, C1-6alkanediyl-C(&boxH；S)&mdash； or C1-6alkanediyl-S(&boxH；O)2&mdash；； R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted amino-C1-6alkyl； R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxy-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 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 form Het1 or Het2&prime； R12 is H, &mdash；NH2, &mdash；NR5AR6, &mdash；C1-6alkyl or alkyl-W&mdash；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 C1-4alkyl and R13 is H, C1-6-alkyl, optiona
