Patent ID: 6184241
Filing Date: 2001-02-06
Classification: A61K,C07D

Abstract:
An aspartic protease/inhibitor complex comprising an aspartic protease and an aspartic protease inhibitor, said aspartic protease/inhibitor complex having said aspartic protease inhibitor chemically, physically and/or physicochemically interacting with said aspartic protease and said aspartic protease inhibitor having the following general formula (I):Z--Het--Z (I)wherein,a) Het is a saturated, partially unsaturated or unsaturated and substituted or unsubstituted 3 to 7-membered heterocyclic ring havingi) at least two heteroatoms, wherein the first heteroatom can interact with a first aspartate group in the active site of an aspartic protease and the second heteroatom can interact with a second aspartate group in the same active site, wherein at least one of the heteroatoms does interact with at least one of the first and second aspartate groups, andii) a pK.sub.a value in the range from about 2.5 to about 12, andb) wherein each Z can be the same or different, and hasi) a shape complementarity with at least a portion of the substrate binding site of the aspartic protease;ii) a chemical structure for contacting multiple atoms of the substrate binding site; andiii) at least one R group, which can be the same or different, at least one R group having a chemical structure for occupying at least one sub-site, proximate to the active site of the aspartic protease.