Irreversible HIV protease inhibitors, compositions containing same and process for the preparation thereof

摘要

The present invention relates to novel compounds of formula (I) which have inhibitory activity against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and compositions for prevention or treatment of AIDS by HIV infection comprising the above compounds as active ingredients. <IMAGE> (I) wherein: R1 is an aromatic group, a nitrogen-containing aromatic group, C1-4 alkyl group optionally substituted with an aromatic group or a nitrogen-containing aromatic group, C1-4 alkoxy group optionally substituted with an aromatic group or a nitrogen-containing aromatic group; R2 is an amino acid residue or a C1-8 alkyl group substituted with a C1-4 alkylsulfonyl group; R3 is a C1-4 alkyl group optionally substituted with an aromatic group; R4 is hydrogen or a C1-4 alkyl group; R5 is an aromatic group, a C1-10 alkyl group or a C1-4 alkyl groups optionally substituted with an aromatic group; and n is 1 or 2.