Importance

Loading Importance Indicators...

Abstract

The present invention provides substituted amino bicyclic-.beta.-lactam penam derivatives and substituted amino bicyclic-.beta.-lactam cepham derivatives and their diastereoisomers of formula I, as well as compositions, methods of making, and methods of using, which exhibit excellent cysteine protease inhibitory activity and which may be used for treatment of different diseases such as cancer (including cancer metastasis), osteoporosis, rheumatoid arthritis. muscular dystrophy, myocardial infarction, pulmonary emphysema, septic shock, cerebral ischemia, decreased memory function, Alzheimer, cataract, malaria, glomerular basement membrane degradation, bacterial infection, inflammatory diseases, parasitic infections and viral infections, ##STR1## wherein R is a peptidyl residue of a single natural .alpha.-amino acid selected from a specific group of natural .alpha.-amino acids or a peptidyl residue of a single non-natural amino acid selected from a specified group of non-natural amino acids, in which natural or non-natural peptidyl residue the terminal --NH.sub.2 group is unsubstituted or substituted once or twice with group R.sub.4, wherein R.sub.4 is selected from the group consisting of --COOR.sub.5, --COR.sub.5, --SO.sub.2 R.sub.5, and --COR.sub.6, R.sub.6 is an amino group which is unsubstituted or substituted at least once with a C.sub.1 -C.sub.6 alkyl group which is unsubstituted or substituted, R.sub.1 is selected from the group consisting of hydrogen, hydroxy, carboxy, --COOR.sub.6, --OR.sub.7, --CONHR.sub.7, and C.sub.1 -C.sub.5 alkyl, in which the C.sub.1 -C.sub.6 alkyl is unsubstituted or substituted, R.sub.2 and R.sub.3 are independently hydrogen or C.sub.1 -C.sub.3 alkyl which is unsubstituted or substituted, n is 0, 1, or 2, and n.sub.1 is 0 or 1.

Loading the Abstract Image...

First Claim