The present invention concerns the compounds having the formula ##STR00001## N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R.sub.1 and R.sub.8 each are H, optionally substituted C.sub.1-6alkyl, C.sub.2-6alkenyl, C.sub.3-7 cycloalkyl, aryl, Het.sup.1, Het.sup.2; R.sub.1 may also be a radical of formula (R.sub.11aR.sub.11b)NC(R.sub.10aR.sub.10b)CR.sub.9--; t is 0, 1 or 2; R.sub.2 is H or C.sub.1-6alkyl; L is --C(.dbd.O)--, --O--C(.dbd.O)--, --NR.sub.8--C(.dbd.O)--, --C.sub.1-6alkanediyl-C(.dbd.O)--, --NR.sub.8--C.sub.1-6alkanediyl-C(.dbd.O)--, --S(.dbd.O).sub.2--, --O--S(.dbd.O).sub.2--, --NR.sub.9-S(.dbd.O).sub.2; R.sub.3 is C.sub.1-6alkyl, aryl, C.sub.3-7cycloalkyl, C.sub.3-7cycloalkylC.sub.1-4alkyl, or arylC.sub.1-4alkyl; R.sub.4 is H, C.sub.1-4alkylOC(.dbd.O), carboxyl, aminoC(.dbd.O), mono- or di(C.sub.1-4alkyl)aminoC(.dbd.O), C.sub.3-7 cycloalkyl, C.sub.2-6alkenyl, C.sub.2-6alkynyl or optionally substituted C.sub.1-6alkyl; R.sub.5 and R.sub.6 are H or C.sub.1-6alkyl. 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.

 
Web www.patentalert.com

< Detection of human immunodeficiency virus

> Methylation markers for diagnosis and treatment of ovarian cancer

> Selective androgen receptor modulators and methods of use thereof

~ 00561