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US 4,728,666 AGranted
Heteroaromatic acetylenes useful as antihypertensive agents
AssigneeMcNeilab, Inc.
InventorJohn R. Carson
Life of this patent
Estimating the term…
Abstract
Heterocyclic acetylenes of the formula (I): ##STR1## wherein Y and R.sup.1 are substituents such as hydrogen, alkyl, alkoxy, chloro or fluoro, m is 0-2, R.sup.2 is branched alkyl and Het is an aromatic heterocycle. The acetylenes are useful in treating hypertension and/or angina.
Claims19
A heteroaromatic acetylene of the following formula (I):
- ##STR5## wherein Y is alkyl of about 1 to 6 carbons, alkoxy of about 1 to 6 carbons, alkoxyalkyl of about 2 to 8 carbons, chloro, fluoro, bromo or carboxamidoalkyl of about 2 to 7 carbons;
- m is 0, 1 or 2;
- R.sup.1 is hydrogen, alkyl of about 1 to 6 carbons, alkoxy of about 1 to 6 carbons, alkylthio of about 1 to 6 carbons, alkoxycarbonyl of about 2 to 7 carbons, chloro, fluoro or dialkylamino of about 2 to 8 carbons;
- R.sup.2 is branched chain alkyl of about 3 to 7 carbons with the carbon alpha to the nitrogen atom being branched;
- and
- Het is thienyl or furanyl;
- and
- the pharmaceutically acceptable acid addition salts thereof.
5 more elements
An acetylene of the following formula (IX):
- ##STR6## wherein Y is alkyl of about 1 to 6 carbons, alkoxy of about 1 to 6 carbons, alkoxyalkyl of about 2 to 8 carbons, chloro, fluoro, bromo or carboxamidoalkyl of about 2 to 7 carbons;
- m is 0, 1 or 2;
- R.sup.1 is hydrogen, alkyl of about 1 to 6 carbons, alkoxy of about 1 to 6 carbons, alkylthio of about 1 to 6 carbons, alkoxycarbonyl of about 2 to 7 carbons, chloro, fluoro or dialkylamino of about 2 to 8 carbons;
- R.sup.2 is branched chain alkyl of about 3 to 7 carbons with the carbon alpha to the nitrogen atom being branched;
- and
- Het is thienyl or furanyl;
- and
- R.sup.3 is an alkanoyl of 2 to 6 carbons or trialkylsilyl protecting group, and the acid addition salts thereof.
5 more elements
Dependencies are inferred from the claim text.