HIV-1 protease inhibitors having gem-di-fluoro bicyclic P2-ligands

摘要

Various embodiments of the present invention relate to, among other things, compounds and methods of using those compounds to treat an HIV infection. The compounds of the various embodiments of the present invention provide, among other things, therapeutic agents having enhanced penetration capability across the blood-brain barrier, such that they can enter the CNS to treat an HIV-1 infection in the CNS.

主权项

1. A compound of the formula or a pharmaceutically acceptable salt thereof, wherein n is 1; R1 is phenyl which is unsubstituted or which bears a fluoro, hydroxymethyl, methoxy or 2-(morpholin-4-yl)ethoxy substituent at the 3- or 4-position, or is 3,5-difluorophenyl; R2 is 2-propyl or 2-fluoro-2-propyl; and —X—R3 is selected from the group consisting of —SO2—R3, —C(O)—N(R)—R3, —NH—SO2—R3, and —NH—C(O)—OR3; in which R is selected from the group consisting of (1-6C)alkyl, aryl, heteroaryl, aryl(1-6C)alkyl or heteroaryl(1-6C)alkyl, each of which is optionally substituted; and R3 is selected from the group consisting of (1-6C)alkyl, aryl, heteroaryl, aryl(1-6C)alkyl or heteroaryl(1-6C)alkyl, each of which is optionally substituted.