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US 5,672,618 AGranted
Protein kinase C inhibitors
AssigneeEli Lilly and Company
InventorsWilliam F. Heath, Jr., John H. McDonald, III, Michael Paal, Theo Schotten, Wolfgang Stenzel
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Abstract
The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention 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.
Claims6
A compound of the formula:
- ##STR68## wherein:
- ##STR69## R.sup.1 is --(CH.sub.2).sub.m --O--glycosyl;
- m=2, 3, or 4;
- R.sup.1' is hydrogen, C.sub.1 -C.sub.4 alkyl, cyclopropylmethyl, aminoalkyl, monoalkylaminoalkyl, or dialkylaminoalkyl;
- R.sup.2 and R.sup.2' are independently hydrogen, alkyl, alkoxyalkyl, hydroxyalkyl, C.sub.1 -C.sub.3 alkylthio, S(O)C.sub.1 -C.sub.3 alkyl, CF.sub.3 ;
- R.sup.3 is hydrogen or CH.sub.3 CO--;
- R.sup.4, R.sup.4', R.sup.5, R.sup.5', R.sup.6, R.sup.6', R.sup.7 and R.sup.7' are independently hydrogen, halogen, alkyl, hydroxy, alkoxy, --COO(C.sub.1 -C.sub.3 alkyl), CF.sub.3, nitro, amino, acetylamino, monoalkylamino, dialkylamino, alkylthio, C.sub.1 -C.sub.3 alkylthio, or S(O)C.sub.1 -C.sub.3 alkyl;
- n is 1, 2, 3, 4, 5 or 6;
- or
- pharmaceutically acceptable salts or solvates thereof.
7 more elements
Dependencies are inferred from the claim text.