Back to results
US 5,491,242 AGranted
Protein kinase C inhibitors
AssigneeEli Lilly and Company
InventorsJames R. Gillig, Michael R. Jirousek
Life of this patent
Estimating the term…
Abstract
The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. The present invention also provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.
Claims28
A compound of the formula:
- ##STR18## wherein:
- R.sub.1 is of the formula:
- ##STR19## R.sub.2 is acyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, acylaminoalkyl, N.sub.3 -alkyl, or an amino acid of the formula:
- ##STR20## R.sub.3 is H or CH.sub.3 ;
- R.sub.4 is independently an amino acid side chain;
- X is --(CH.sub.2).sub.n --NH--, --(CH.sub.2).sub.n --O--, phenylene--NH--, phenylene--O--, or a bond;
- P.sub.1 is independently H, alkyl, or an amino protecting group;
- and
- n is independently 1, 2 or 3;
- or a pharmaceutically acceptable salt or solvate thereof.
7 more elements
Dependencies are inferred from the claim text.