초록 ▼

The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to phar

The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

대표청구항 ▼

ently selected from the group consisting of oxo, -OR2, -R2, -N(R2)(R2), -N(R2)-C(O)-R2, C1-C3 alkyl substituted with -OH and optionally substituted with R7, -CN, -CO2R2, -C(O)-N(R2)(R2), halo and -CF3; E is selected from the group consisting of Ht; O-Ht; Ht-Ht; -O-R3; -NR2R3; C1-C6 alkyl, which is o

ently selected from the group consisting of oxo, -OR2, -R2, -N(R2)(R2), -N(R2)-C(O)-R2, C1-C3 alkyl substituted with -OH and optionally substituted with R7, -CN, -CO2R2, -C(O)-N(R2)(R2), halo and -CF3; E is selected from the group consisting of Ht; O-Ht; Ht-Ht; -O-R3; -NR2R3; C1-C6 alkyl, which is optionally substituted with one or more groups independently selected from the group consisting of R4 and Ht; C2-C6 alkenyl, which is optionally substituted with one or more groups independently selected from the group consisting of R4 and Ht; C3-C6 saturated carbocycle, which is optionally substituted with one or more groups independently selected from the group consisting of R4 and Ht; and C5-C6 unsaturated carbocycle, which is optionally substituted with one or more groups independently selected from the group consisting of R4 and Ht; and each R4 is independently selected from the group consisting of -OR2, -C(O)-NHR2, -S(O)2-NHR2, halo, -NR2-C(O)-R2 and -CN.