VENDEVILLE, SANDRINE MARIE HELENE,VERSCHUEREN, WIM GASTON,TAHRI, ABDELLAH,MOORS, SAMUEL LEO CHRISTIAAN,ERRA SOLA, MONTSERRAT
申请号：
CA2470964
公开号：
CA2470964C
申请日:
2002.12.20
申请国别(地区):
CA
年份:
2013
代理人:
摘要：
The present invention concerns the compounds having the formula (I), N-oxides,salts, stereoisomeric forms, racemic mixtures, prodrugs, esters andmetabolites thereof, wherein Haryl is an aromatic monocyclic, bicyclic ortricyclic heterocycle having 3 to 14 ring members which contains one or moreheteroatom ring members selected from nitrogen, oxygen and sulfur and whichmay 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 disubstitutedaminocarbonyl, methylthio, methylsulfonyl, aryl, -(R7a)n-M-R7b, Het1 and Het2whereby the optional substituents on any amino function are independentlyselected from R5 and -A-R6 and on (ii) a nitrogen atom if present by hydroxyor -A-R6. It further relates to their use as broadspectrum HIV proteaseinhibitors, processes for their preparation as well as pharmaceuticalcompositions and diagnostic kits comprising them. It also concernscombinations thereof with another anti-retroviral agent, and to their use inassays as reference compounds or as reagents.
