Sankyo Company, Limited

Ube Industries, Inc.

Takashi Nishigaki

Tomio Kimura

Hiroshi Handa

Tetsushi Katsube

Susumu Higashida

Yuichiro Yabe

Tomoaki Komai

Mitsuya Sakurai

This invention relates to a 8-trifluoromethylquinolinecaboxylic acid derivative represented by the following formula (I): ##STR1## (wherein R.sup.1 represents a lower alkyl group, a halogeno-lower alkyl group or a cycloalkyl group, R.sup.2 represents a phenyl group which may be substituted by R.sup.0, a 5-membered or 6-membered aromatic heteromonocyclic ring group containing 1 or 2 hetero atoms selected from N, O and S, which may be substituted by R.sup.0, or an aromatic heterocyclic fused ring group in which the said aromatic heteromonocyclic ring group and a benzene ring are fused, R.sup.0 represents a group selected from a halogen, a lower alkyl, a fluorine-substituted lower alkyl, a lower alkoxy or a lower alkylthio, R.sup.3 represents hydrogen or a lower alkyl group, and m represents an integer of 2 or 3.) or a pharmaceutically acceptable salt thereof or an ester thereof.

Trifluoromethylquinolinecarboxylic acid derivative

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

Tokyo, Japan

Takashi Nishigaki