N-Hydroxy-1,2-dihydro-2-oxo-5-(pyridinyl)-nicotinimidamide and their cardiotonic use
AssigneeSterling Drug Inc.
InventorsMonte D. Gruett, George Y. Lesher
Life of this patent
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Abstract
N-Hydroxy-1-R.sub.1 -1,2-dihydro-2-oxo-5-PY-6-R-nicotinimidamides or pharmaceutically-acceptable acid-addition salts thereof, useful as cardiotonic agents, are prepared by reacting 1-R.sub.1 -1,2-dihydro-2-oxo-5-PY-6-R-nicotinonitriles with hydroxylamine and are converted by reaction with polyphosphoric acid to the corresponding cardiotonically useful 1-R.sub.1 -3-amino-5-PY-6-R-2(1H)-pyridinones, where R.sub.1 is hydrogen, lower-alkyl and lower-hydroxyalkyl, R is hydrogen or lower-alkyl, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents.
Claims8
N-Hydroxy-1-R.sub.1 -1,2-dihydro-2-oxo-5-PY-6-R-nicotinimidamide having the formula ##STR2## or pharmaceutically-acceptable acid-addition salt thereof, where R is hydrogen or lower-alkyl, R.sub.1 is hydrogen, lower-alkyl or lower-hydroxyalkyl, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents.
N-hydroxy-1,2-dihydro-2-oxo-5-(4-pyridinyl)nicotinimidamide or pharmaceutically-acceptable acid-addition salt thereof.
A cardiotonic composition for increasing cardiac contractility, said composition comprising a pharmaceutically-acceptable inert carrier and, as the active component thereof, a cardiotonically-effective amount of N-hydroxy-1-R.sub.1 -1,2-dihydro-2-oxo-5-PY-6-R-nicotinimidamide or pharmaceutically-acceptable acid-addition salt thereof, where R is hydrogen or lower-alkyl, R.sub.1 is hydrogen, lower-alkyl or lower-hydroxyalkyl, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents.
The method for increasing cardiac contractility in a patient requiring such treatment which comprises administering to such patient a composition comprising a pharmaceutically-acceptable carrier and, as the active component thereof, a cardiotonically-effective amount of N-hydroxy-1-R.sub.1 -1,2-dihydro-2-oxo-5-PY-6-R-nicotinimidamide or pharmaceutically-acceptable acid-addition salt thereof, where R is hydrogen or lower-alkyl, R.sub.1 is hydrogen, lower-alkyl or lower-hydroxyalkyl, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents.
Dependencies are inferred from the claim text.