Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1992-06-25
1993-10-26
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514258, 544225, 544280, A61K 31505, A61K 3155, C07D48704, C07D47104
Patent
active
052566544
ABSTRACT:
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.
REFERENCES:
patent: 4916129 (1990-04-01), Carini
patent: 5039814 (1991-08-01), Shuman
Santilli, J. Het. Chem. 13, 135(1976).
Bagli Jehan
Ellingboe John W.
Nikaido Madelene
American Home Products Corporation
Berch Mark L.
Patton Walter
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