Sankyo Company, Limited

Mitsuya Sakurai

Hiroaki Yanagisawa

Toshihiko Fujiwara

Hiroshi Handa

Susumu Higashida

Yuichiro Yabe

Tomoaki Komai

Makoto Takamura

Takashi Nishigaki

Amidocarboxylic acid derivatives

Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, alkyl, aralkyl, --COR.sup.a, --COR.sup.b, --CSR.sup.a, --CSR.sup.b, --SO.sub.2 R.sup.b, --CONHR.sup.b, --CSNHR.sup.b, --CONR.sup.b R.sup.b or --CSNR.sup.b R.sup.b ; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen, alkylidene, substituted alkyl, or R.sup.b ; R.sup.4 is optionally substituted alkyl, cycloalkyl, or aryl; R.sup.5 is R.sup.b O--, R.sup.b R.sup.b N--, R.sup.b HN--, aralkyloxycarbonyloxy or aralkyloxycarbonylamino, or R.sup.5 is --(CH.sub.2).sub.p --D--(CH.sub.2).sub.r --, where D is a single bond, carbonyl, oxygen, sulfur, --NH--, --(CH.sub.2 .dbd.CH.sub.2)-- or --NHCO--; and p and r are each 0 or an integer from 1 to 5; A is --(CH.sub.2).sub.m --B--(CH.sub.2).sub.n -- where B is a single bond, carbonyl, oxygen, sulfur, --NH--, --(CH.sub.2 .dbd.CH.sub.2)-- or --NHCO--; and m and n are each 0 or an integer from 1 to 5; R.sup.a is alkoxy, aralkyloxy, aryloxy or alkoxycarbonyl; R.sup.b is optionally substituted alkyl, cycloalkyl, heterocyclic, aryl or arylalkenyl; and pharmaceutically acceptable salts and esters thereof and pro-drugs therefor, have the ability to inhibit the activity of HIV protease and may thus be used for the treatment and prophylaxis of AIDS.

Inhibitors of HIV protease

Growing community of inventors

Abiko, Japan

Mitsuya Sakurai