초록

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

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1. A compound represented by the formula (A): [EQU470]or a pharmaceutically acceptable salt, or ester thereof, wherein:R2 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

1. A compound represented by the formula (A): [EQU470]or a pharmaceutically acceptable salt, or ester thereof, wherein:R2 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, CF3, -OR9, and -SR9, wherein R9 is a radical selected from the group consisting of hydrogen and alkyl; R3 is a hydrogen, alkyl haloalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfonylalkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aminoalkyl or mono- or disubstituted aminoalkyl radicals, wherein said substituents are selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl and cycloalkylalkyl radicals; R4 is an alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, aminoalkyl or mono- or disubstituted aminoalkyl radical, wherein said substituents are selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl and cycloalkylalkyl radicals; R6 is a hydrogen or alkyl radical; x is 1 or 2; Y is 0 or S; and A is an alkoxy, alkenoxy, aralkoxy, alkyl, cycloalkyl, cycloalkylalkoxy, [EQU471]cycloalkylalkyl, aralkyl, aryl, aryloxy, alkenyl, aryloxyalkyl, hydroxyalkyl, amino, or mono- or disubstituted amino radical, wherein the substituents are selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl and cycloalkylalkyl radicals; or is represented by the formula (B): [EQU472]t is 0or 1; wherein R is a hydrogen, alkoxycarbonyl, aralkoxycarbonyl, alkylcarbonyl, cycloalkylcarbonyl, cycloalkylalkoxycarbonyl, cycloalkylalkanoyl, carboxyalkanoyl, alkanoyl, aralkanoyl, aroyl, aryloxycarbonyl, aryloxycarbonylalkyl, aryloxyalkanoyl, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, aryloxyalkyl, hydroxyalkyl, aminocarbonyl, aminoalkanoyl, or mono- or disubstituted aminocarbonyl or mon- or disubstituted aminoalkanoyl radical, wherein the substituents are selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl and cycloalkylalkyl radicals; R' is a radical as defined for R3 or R′SO2-, wherein R′ is a radical as defined for R3; R1 is a hydrogen, -CO2CH3, -CH2CO2CH3, -CO2H, -CH2CO2H, -CH2CH2CONH2, -CH2CONH2, -CONH2, -CH2C(O)NHCH3, -CH2C(O)N(CH3)2, -CONHCH3, -CONH(CH3)2, -CH2SO2NH2, -CH2CH2SO2NH2, -CH2S(O)CH3, -CH2S(O)2CH3, -C(CH3)2(S(O)CH3), -C(CH3)2(S(O)2CH3), alkyl, hydroxyalkyl, cyanoalkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkylthioalkyl, aralkyl, aminoalkyl or mono- or disubstituted aminoalkyl radical, wherein said substituents are selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl and cycloalkylalkyl radicals; and each of R1' and R1′ are independently a radical as defined for R1; or one of R1' and R1′ together with R1 and the carbon atoms to which R1, R1' and R1′ are attached, form a cycloalkyl radical.