American Home Products Corporation

Madelene Nikaido

John W Ellingboe

Jehan F Bagli

James J Bicksler

Dimitri Sarantakis

This invention relates to pyrrolo-, pyrido-, azepino-, and azocinopyrimidines of the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently H, lower alkyl containing 1 to 6 carbon atoms, or perfluoroalkyl containing 1 to 6 carbon atoms; R.sup.5 is H or, when n is 1, R.sup.5 taken together with R.sup.3 comprises a double bond, n is 0 or 1, p is 0 to 2, m is 0 to 3; Ar.sup.1 is ##STR2## wherein W is H, lower alkyl containing 1 to 6 carbon atoms, halogen, hydroxy, or lower alkoxy containing 1 to 6 carbon atoms; and Ar.sup.2 is ##STR3## wherein X is ##STR4## wherein R.sup.6 is H, tert-butyl, tri-n-butylstannyl, or triphenylmethyl; and the pharmaceutically acceptable salts thereof, which compounds are useful in the treatment of hypertension and congestive heart failure.

Substituted pyrrolopyrimidines and pyridopyrimidines useful as

This invention relates to substituted 4-aminopyrimidines, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension, congestive heart failure, and restenosis. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia. Also disclosed are processes for the production of said compounds and pharmaceutical compositions containing said compounds.

Substituted aminopyrimidines as antihypertensives

This invention relates to pyrrolo-, pyrido-, azepino-, and azocinopyrimidines of the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently H, lower alkyl containing 1 to 6 carbon atoms, or perfluoroalkyl containing 1 to 6 carbon atoms; R.sup.5 is H or when n is 1 R.sup.5 taken together with R.sup.3 comprises a double bond; n is 0 to 1; p is 0 to 2; m is 0 to 3; Ar.sup.1 is ##STR2## wherein W is H, lower alkyl containing 1 to 6 carbon atoms, halogen, hydroxy, or lower alkoxy containing 1 to 6 carbon atoms; Ar.sup.2 is ##STR3## wherein X is ##STR4## wherein R.sup.6 is H, tert-butyl, tri-n-butylstannyl, or triphenylmethyl; and the pharmaceutically acceptable salts thereof which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension, congestive heart failure, and restenosis. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia. Also disclosed are processes for the production of said compounds and pharmaceutical compositions containing said compounds.

Substituted pyrrolopyrimidines, azepinopyrimidines and pyridopyrimidines

This invention relates to pyrrolo-, pyrido-, azepino-, and azocinopyrimidines of the general formula I ##STR1## useful for treating hypertension and congestive heart failure, to pharmaceutical compositions, and to methods for production thereof.

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Plainsboro, NJ, United States of America

Madelene Nikaido