Carbostyril derivatives as combined thromboxane synthetase and cyclic-AMP phosphodiesterase inhibitors
AssigneeSyntex (U.S.A.) Inc.
InventorsKeith A. M. Walker, John J. Bruno, Gregory R. Martinez
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AssigneeSyntex (U.S.A.) Inc.
InventorsKeith A. M. Walker, John J. Bruno, Gregory R. Martinez
Estimating the term…
The invention concerns a method of inhibiting both thromboxane synthetase and cyclic-AMP phosphodiesterase in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclin/thromboxane levels with a compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or ester thereof, wherein: X is chosen from the group consisting of: ##STR2## and a covalent bond in which R.sup.1 is H, alkyl having 1-6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl lower alkyl, when R.sup.2 is H or OH, or R.sup.1 and R.sup.2 taken together represent oxo, alkylidene having 1-6 carbon atoms or optionally substituted benzylidene; R.sup.3 is H or alkyl having 1-6 carbon atoms, R.sup.4 is H and R.sup.3 and R.sup.4 are either cis or trans to each other, or R.sup.3 and R.sup.4 taken together represent a covalent bond; n is an integer from 0-3; Het is 1-imidazolyl or 3-pyridyl; and the dotted line represents an optional covalent bond.
A compound of the formula:
Dependencies are inferred from the claim text.