Use of peptide isosteres as retroviral protease inhibitors

A - Human Necessities – 61 – K

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A61K 38/55 (2006.01) A61K 38/03 (2006.01) C07K 5/02 (2006.01) C07K 7/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2005337

Use of peptide isosteres as retroviral protease inhibitors Abstract The invention relates to the use of compounds of the renin inhibitor type or related aspartate proteinase inhibitors as gag protease inhibitors. It relates especially to the use of those compounds for the manufacture of pharmaceutical preparations for use as gag protease inhibitors, there being used compounds of the formula R2 - AAN - Q - AAC - R1 wherein AAN is a bivalent radical, consisting of from one to five bivalent .alpha.-amino acid residues, which is bonded N-terminally to the radical R2 and C-terminally to the radical Q, AAC is a bond or a bivalent radical, consisting of from one to five bivalent .alpha.-amino acid residues, which is bonded N-terminally to the radical Q and C-terminally to the radical R1, R1 is hydroxy, etherified hydroxy, amino or substituted amino with the exception of an amino radical derived from an .alpha.-amino acid, R2 is hydrogen or an acyl radical with the exception of an unsubstituted or N-substituted acyl radical of a natural amino acid, and Q is a bivalent radical that is an isostere of a dipeptide, and salts thereof.

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