A compound of the formula (I): ##STR00001## wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is --COOR.sup.A wherein R.sup.A is hydrogen or ester residue, --CONR.sup.BR.sup.C wherein R.sup.B and R.sup.C each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A.sup.1 is optionally substituted heteroaryl; provided that a compound wherein Y and/or A.sup.1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.
This application is a divisional of Ser. No. 10/288,380 filed Nov. 6, 2002, now U.S. Pat. No. 6,645,956, which is a divisional of Ser. No. 09/857,632 filed Jun. 7, 2001, now U.S. Pat. No. 6,620,841, which is a U.S. national stage of PCT/JP99/07101 filed Dec. 17, 1999.
Priority Data
Dec 25, 1998 [JP] 10-371270 Sep 01, 1999 [JP] 11-247479
A new class of diketo acids constructed on nucleobase scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.
A new class of diketo acids constructed on nucleobase scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.
