VENDEVILLE SANDRINE MARIE HELENE,SANDRINE MARIE HELENE VENDEVILLE,VERSCHUEREN WIM GASTON,WIM GASTON VERSCHUEREN,TAHRI ABDELLAH,ABDELLAH TAHRI,MOORS SAMUEL LEO CHRISTIAAN,SAMUEL LEO CHRISTIAAN MOORS,ER,MO
申请号：
PL370801
公开号：
PL216539B1
申请日:
2002.12.20
申请国别(地区):
PL
年份:
2014
代理人:
摘要：
The present invention concerns the compounds having the formula (I), N-oxides, salt, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Haryl is an aromatic monocyclic, bicyclic or tricyclic heterocycle having 3 to 14 ring members which contains one or more heteroatom ring members selected from nitrogen, oxygen and sulfur and which may optionally be substituted on (i) one or more carbon atoms by C1-6alkyl, halogen, hydroxy, optionally mono- or disubstituted amino, nitro, cyano, haloC1-6alkyl, carboxyl, C3-7cycloalkyl, optionally mono- or disubstituted aminocarbonyl, methylthio, methylsulfonyl, aryl, &mdash；(R7a)n&mdash；M&mdash；R7b, Het1 and Het2； whereby the optional substituents on any amino function are independently selected from R5 and &mdash；A&mdash；R6； and on (ii) a nitrogen atom if present by hydroxy or &mdash；A&mdash；R6. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
