초록

.alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

대표청구항 ▼

[ What is claimed is:] [1.] A compound represented by the formula: [ STR 495 ] or a pharmaceutically acceptable salt thereof wherein R.sup.2 is an alkyl, aryl, cycloalkyl, cycloalkylalkyl or aralkyl radical, which radical is optionally substituted with a radical selected from the group consisting of

[ What is claimed is:] [1.] A compound represented by the formula: [ STR 495 ] or a pharmaceutically acceptable salt thereof wherein R.sup.2 is an alkyl, aryl, cycloalkyl, cycloalkylalkyl or aralkyl radical, which radical is optionally substituted with a radical selected from the group consisting of alkyl, halo, nitro, cyano, CF.sub.3, --OR.sup.9, and --SR.sup.9 radicals, wherein R.sup.9 is hydrogen or alkyl radicals;R.sup.3 is alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfonylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heteroaryl, heterocycloalkylalkyl, aryl, aralkyl or heteroaralkyl radicals;R.sup.4 is heterocycloalkyl, heteroaryl or aryl radicals;Y is O or S; andA is heterocycloalkyl, heterocycloalkoxy, heterocycloalkylalkyl, heterocycloalkylalkoxy, heteroaralkyl, heteroaralkoxy, heteroaryloxy or heteroaryl radicals; andwherein alkyl, alone or in combination, is a straight-chain or branched-chain alkyl radical containing 1 to 8 carbon atoms; alkenyl, alone or in combination, is a straight-chain or branched-chain hydrocarbon radial having at least one double bond and containing 2 to 8 carbon atoms; alkynyl, alone or in combination, is a straight-chain or branched chain hydrocarbon radical having at least one triple bond and containing 2 to 10 carbon atoms; aryl, alone or in combination, is an unsubstituted phenyl or naphthyl radical or a phenyl or naphthyl radical substituted with alkyl, alkoxy, halogen, hydroxy, amino, alkylamino, dialkylamino, nitro, cyano, carboxy, alkoxycarbonyl, amido, alkylamido, dialkylamido, trifluoromethyl, methylthio, methylsulfinyl or methylsulfonyl radicals; cycloalkyl, alone or in combination, is a saturated or partially saturated monocyclic, bicyclic or tricyclic alkyl radical wherein each cyclic moiety contains 3 to 8 carbon atoms; heterocycloalkyl, alone or in combination, is a monocyclic, bicyclic or tricyclic heterocycle radical having 1-4 nitrogen, nitrogen oxide, oxygen, sulphur, sulfone or sulfoxide heteroatom ring members, optionally benz-fused and optionally substituted on one or more carbon atoms by halogen, alkyl, alkoxy, hydroxy, oxo, aryl or aralkyl radicals, or on a secondary nitrogen atom by hydroxy, alkyl, aralkoxycarbonyl, alkanoyl, phenyl or phenylalkyl radicals; and heteroaryl, alone or in combination, is an aromatic heterocycloalkyl, optionally substituted with respect to aryl and heterocycloalkyl radicals.