2.3 - to - carboxaamidomethyl substituted oxirane as inhibitors of hiv protease and its use for treatment of hiv protease

摘要

The present invention provides novel HIV protease inhibitors of the formula CHEM wherein: R is C1-C6 alkyl, cycloalkyl, heterocycle, unsaturated heterocycle, aryl, cycloalkyl(C1-C4)alkyl, heterocycle(C1-C4)alkyl, unsaturated heterocycle(C1-C4)alkyl, aryl(C1-C4)alkyl, or a structure having the formula -A-(CH2)q-R0, where A is -O-, -NH- or -S-; q is 0, 1, 2 or 3; R0 is cycloalkyl, aryl, heterocycle or unsaturated heterocycle; X is CHEM where: R1 is aryl, cycloalkyl, heterocycle or unsaturated heterocycle; R2 is hydrogen or C1-C4 alkyl; R3 is an amino acid side chain, -CH2CH3, -CH2CH2CH3, -CH2-(CH2)2CH3, -C(CH3)3, cyano(C1-C4)alkyl, unsaturated heterocycle(C1-C4)alkyl, aryl(C1-C4)alkyl or a structure having the formula -(CH2)s-A0-(CH2)r-R4 or -CH2-C(O)-NR2-(CH2)r-R5, where s is 1, 2, 3 or 4; r is 0, 1, 2 or 3; A0 is -O-, -NH- or -S-; R4 is C1-C6 alkyl, cycloalkyl, aryl, heterocycle or unsaturated heterocycle; R5 is cycloalkyl, aryl, heterocycle or unsaturated heterocycle; j is 0, 1, 2, 3 or 4; k is 0 or 1; and Y is -O-, -N(R2)- or -S-; or a pharmaceutically acceptable salt thereof.