Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Tripeptides – e.g. – tripeptide thyroliberin – etc.
Patent
1994-04-14
1997-05-13
Lukton, David
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
Tripeptides, e.g., tripeptide thyroliberin , etc.
548535, 562561, A61K 3806
Patent
active
056294069
ABSTRACT:
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.
REFERENCES:
Chemical Abstracts, vol. 116, No. 5, Feb. 3, 1992, Abstract No. 116: 42 041h of Tsutomu et al, "Rational design and synthesis of a novel class of active site-targeted HIV protease inhibitors containing a hydroxymethylcarbonyl isostere. Use of phenylnorstatine as a transition state mimic."
Chemical Abstracts, vol. 117, No. 1, Jul. 6, 1992, Abstract No. 117: 8 449h of Tsutomu et al, "Design and synthesis of HIV protease inhibitors containing a hydroxymethylcarbonyl isostere as a transition state mimic."
Handa Hiroshi
Higashida Susumu
Komai Tomoaki
Nishigaki Takashi
Sakurai Mitsuya
Lukton David
Sankyo Company Limited
LandOfFree
Inhibitors of HIV protease does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Inhibitors of HIV protease, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Inhibitors of HIV protease will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1386488