Azaaspartic acid analogs as interleukin-1.beta. converting enzyme inhibitors
AssigneeSterling Winthrop Inc.
InventorsRoland E. Dolle, Todd L. Graybill
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Abstract
Disclosed are compounds, compositions and methods for inhibiting interleukinprotease activity. The compounds, .alpha.-substituted acetamides a ##STR1## wherein: R.sub.2 =H or alkyl; R.sup.3 =halo, O(CO).sub.0-1 aryl, OPOR.sup.4 R.sup.5 ; ##STR2## where R.sup.4 and R.sup.5 =aryl; R.sup.6 =H, aryl or aralkyl; R.sup.7 =independently selected from R.sup.6, CF.sub.3 and CF.sub.2 CF.sub.3 ; R.sup.1 =R.sup.6 -CO, heteroaryl-CO, heteroaralkyl-CO and amino acid.
Claims9
A compound of the formula (A) or a pharmaceutically acceptable salt thereof:
- ##STR19## wherein:
- R.sub.2 =H or alkyl;
- R.sup.3 =halo, O(CO).sub.0-1 aryl, OPOR.sup.4 R.sup.5, ##STR20## where R.sup.4 and R.sup.5 =aryl;
- R.sup.6 =H, aryl or aralkyl;
- R.sup.7 =R.sup.6, CF.sub.3 or CF.sub.2 CF.sub.3 ;
- R.sup.1 =R.sup.6 -CO, heteroaryl-CO, heteroaralkyl-CO or amino acid.
A method for inhibiting interleukin-1.beta. protease activity in a mammal in need of treatment for inflammatory and immune-based diseases of lung, central nervous system, or connective tissue comprising administering to said mammal an effective interleukin-1.beta. protease inhibitory amount of a composition comprising a compound of the formula (A) or a pharmaceutically acceptable salt thereof ##STR22## wherein:
- R.sub.2 =H or alkyl;
- R.sup.3 =halo, O(CO).sub.0-1 aryl, OPOR.sup.4 R.sup.5, ##STR23## where R.sup.4 and R.sup.5 =aryl;
- R.sup.6 =H, aryl or aralkyl;
- R.sup.7 =R.sup.6, CF.sub.3 or CF.sub.2 CF.sub.3 ;
- R.sub.1 =R.sup.6 -CO, heteroaryl-CO, heteroaralkyl-CO or amino acid.
Dependencies are inferred from the claim text.