DOMINIQUE LOUIS NESTOR GHISLAIN SURLERAUX,BERNHARD JOANNA BERNARD VERGOUWEN,HERMAN AUGUSTINUS DE KOCK
申请号：
TW92113367
公开号：
TWI356700B
申请日:
2003.05.16
申请国别(地区):
TW
年份:
2012
代理人:
摘要：
The present invention concerns the compounds having the formulaN-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters andmetabolites thereof, wherein R1and R8each are H, opdonally substituted C1-6allkyl,C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2 R1may also be a radical of formula(R11sR11b)NC(R10aR10b)CR9-tis0, 1 or 2 R2is 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(=0)2 R3is C1-6alkyl, aryl, C3-7cycloalkyl,C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl R4is H, C1-4alkylOC(=O), carboxyl,aminoC(=O), mono- or di(C1-4alkyl)aminoC(=O), C3-7cycloalkyl, C2-6alkenyl,C2-6alkynyl or optionally subsdtuted C1-6alkyl A is C1-6alkanediyl, -C(=0)-,-C(=S)-,-S(=O)2-,C1-6alkanediyl-C(=O)-,c1-6alkanediyl-C(=S)-or C1-6alkanediyl-S(=O)2- R5is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted amino-C1-6alkyl R6is C1-6alkylO,Het1,Het1O,Het2,Het2O,aryl,arylO, C1-6alkyloxy-carbonylamio or amino and in case-A-is other than C1-6alkanediyl then R6mayalso be C1-6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl,arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl whereby each of the amiono groups inthe definition of R6may optionally be substituted R5and-A-R6taken together withthe nitrogen atom to which they are attached may also form Het1or Her2It furtherrelates to their use as broadspectrum HIV protease inhibitors, processes for theirpreparation as well as pharmaceutical compositions and diagnostic kits comprisingthem. It also concerns combinations thereof with another anti-retroviral agent, and totheir use in assays as reference compounds or as reagents.
