Beiersdorf-lilly Gmbh

Eli Lilly and Company

Gerd R Uhter

Theo Schotten

Wolfgang Stenzel

Michael Paal

William F Heath, Jr

John H McDonald, Iii

Compounds having the formula ##STR1## and the other variables are as defined herein, and are indicated for use in the treatment and prophylaxis of, for example, hypertension, congestive heart failure, ocular hypertension, renal failure, and CNS disorders, or are intermediates thereto.

Pyrimidine compounds and their use as pharmaceuticals

Compounds for treating cardiovascular or circulatory disorders of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.7, Ar.sup.1, Ar.sup.2, X, Y, and n are defined herein.

Pharmaceutical compounds which are azolo-fused pyrimidine compounds having the formula ##STR1## in which .dbd.A--B-- together with the pyrimidine ring forms a) a pyrazolo[1,5-a]pyrimidine of formula (A), ##STR2## b) a [1,2,4]triazolo[1,5-a]pyrimidine of formula (B), ##STR3## c) an imidazo[1,5-a]pyrimidine of formula (C), ##STR4## or d) an imidazo[1,2-a]pyrimidine of formula (D), ##STR5##

Fused pyrimidine compounds and their use as pharmaceuticals

The present invention discloses compounds of the general formula: ##STR1## The compounds 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.

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Hamburg, Germany

Gerd R Uhter