| abstract |
The compounds of formula (I) and their pharmaceutically acceptable salts and esters and their prodrugs have the ability to inhibit the activity of HIV proteases and can therefore be used for the prevention and treatment of AIDS:n n n n n n n n [Wherein R 1 is hydrogen, alkyl, aralkyl, -COR a , -COR b , -CSR a , -CSR b , -SO 2 R b , -CONHR b , -CSNHRR b , -COR bb or -CSNR b R b ; R 2 is hydrogen or alkyl; R 3 is hydrogen, alkylidene, substituted alkyl or R b ; R 4 is optionally substituted alkyl, cycloalkyl or aryl; R 5 is R b O—R b R b N, —R b NH—, aralkyloxycarbonyloxy or aralkyloxycarbonylamino, or R 5 is — (CH 2 ) PD- (CH 2 ) r— Wherein D is a single bond, carbonyl, oxygen, sulfur, -NH-,-(CH 2 = CH 2 )-or -NHCO-, and p and r are 0 or an integer from 1 to 5; A is-(CH 2 ) mB- (CH 2 ) -n-, wherein B is a single bond, carbonyl, oxygen, sulfur, -NH-,-(CH 2 = CH 2 )-or-NHCO-; m and n are each 0 or an integer of 1 to 5); R a is alkoxy, aralkyloxy, aryloxy or alkoxy carbonyl; R b is optionally substituted alkyl, cycloalkyl, heterocyclic, aryl or arylalkenyl.) |