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Details for Patent: 4,312,875

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Details for Patent: 4,312,875

Title: 5-(Pyridinyl)-6-(lower-alkyl)-2(1H)-pyridinones, 1,2-dihydro-2-oxo-5-(pyridinyl)-6-(lower-alkyl)nicotinic acids and lower-alkyl esters thereof, and cardiotonic use thereof
Abstract:1-R.sub.1 -6-(lower-alkyl)-5-(pyridinyl)-2(1H)-pyridinones or 1-R.sub.1 -1,2-dihydro-2-oxo-6-(lower-alkyl)-5-(pyridinyl)nicotinic acids or lower-alkyl esters thereof or pharmaceutically-acceptable acid-addition or cationic salts thereof are useful as cardiotonic agents, where R.sub.1 is hydrogen, lower-alkyl or lower-hydroxyalkyl. These compounds are prepared by hydrolyzing the corresponding 3-cyano compounds to produce the corresponding 3-carboxylic acids and then either by decarboxylating or esterifying the acids.
Inventor(s): Lesher; George Y. (Schodack, NY), Opalka, Jr.; Chester J. (Schodack, NY), Page; Donald F. (East Greenbush, NY)
Assignee: Sterling Drug Inc. (New York, NY)
Filing Date:Nov 06, 1980
Application Number:06/204,726
Claims:1. A 1-R.sub.1 -5-PY-6-R-2(1H)-pyridinone having the formula ##STR3## where R.sub.1 is hydrogen, R is methyl or ethyl and PY if 4-, 3- or 2-pyridinyl or 4-, 3- or 2-pyridinyl having one or two lower-alkyl substitutents, or pharmaceutically-acceptable acid-addition or cationic salt thereof.

2. A compound according to claim 1 where PY is 4-pyridinyl.

3. 6-Methyl-5-(4-pyridinyl)-2(1H)-pyridinone or pharmaceutically-acceptable acid-addition salt thereof.

4. 6-Ethyl-5-(4-pyridinyl)-2(1H)-pyridinone or pharmaceutically-acceptable acid-addition salt thereof.

5. A 1-R.sub.1 -1,2-dihydro-5-PY-2-oxo-6-R-nicotonic acid or lower-alkyl ester thereof having the formula ##STR4## where R.sub.1 is hydrogen, R is methyl or ethyl, R' is hydrogen or lower-alkyl and PY is 4-, 3- or 2-pyridinyl or 4-, 3- or 2-pyridinyl having one or two lower-alkyl substituents, or pharmaceutically-acceptable acid-addition or cationic salt thereof.

6. A compound according to claim 5 where R' is hydrogen.

7. A compound according to claim 5 where R' is lower-alkyl.

8. A compound according to claim 5 wherein PY is 4-pyridinyl or 3-pyridinyl.

9. 1,2-Dihydro-6-methyl-2-oxo-5-(4-pyridinyl)nicotinic acid or pharmaceutically-acceptable acid-addition salt thereof.

10. 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 a 1-R.sub.1 -5-PY-6-R-2(1H)-pyridinone having the formula ##STR5## where R.sub.1 is hydrogen, R is methyl or ethyl and PY is 4-, 3- or 2-pyridinyl or 4-, 3- or 2-pyridinyl having one or two lower-alkyl substituents, or pharmaceutically-acceptable acid-addition or cationic salt thereof.

11. A composition according to claim 10 where the active component is 6-methyl-5-(4-pyridinyl)-2(1H)-pyridinone or pharmaceutically-acceptable acid-addition salt thereof.

12. A composition according to claim 10 where the active component is 6-ethyl-5-(4-pyridinyl)-2(1H)-pyridinone or pharmaceutically-acceptable acid-addition salt thereof.

13. The method for increasing cardiac contractility in a patient requiring such treatment which comprises administering orally or parenterally in a solid or liquid dosage form to such a patient a cardiotonically-effective amount of a 1-R.sub.1 -5-PY-6-R-2(1H)-pyridinone having the formula ##STR6## where R.sub.1 is hydrogen, R is methyl or ethyl and PY is 4-, 3- or 2-pyridinyl or 4-, 3- or 2-pyridinyl having one or two lower-alkyl substitutents, or pharmaceutically-acceptable acid-addition or cationic salt thereof.

14. The method according to claim 13 where PY is 4-pyridinyl or 3-pyridinyl.

15. 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 a 1-R.sub.1 -1,2-dihydro-2-oxo-5-PY-6-R-nicotinic acid or lower-alkyl ester thereof having the formula ##STR7## where R.sub.1 is hydrogen, R is methyl or ethyl, R' is hydrogen or lower-alkyl and PY is 4-, 3- or 2-pyridinyl or 4-, 3- or 2-pyridinyl having one or two lower-alkyl substituents, or pharmaceutically-acceptable acid-addition or cationic salt thereof.

16. A composition according to claim 15 where the active component is 1,2-dihydro-6-methyl-2-oxo-5-(4-pyridinyl)nicotinic acid or pharmaceutically-acceptable acid-addition salt thereof.

17. The method for increasing cardiac contractility in a patient requiring such treatment which comprises administering orally or parenterally in a solid or liquid dosage form to such patient a cardiotonically-effective amount of a 1-R.sub.1 -1,2-dihydro-2-oxo-5-PY-6-R-nicotinic acid or lower-alkyl ester thereof having the formula ##STR8## where R.sub.1 is hydrogen, R is methyl or ethyl, R' is hydrogen or lower-alkyl and PY is 4-, 3- or 2-pyridinyl or 4-, 3- or 2-pyridinyl having one or two lower-alkyl substituents, or pharmaceutically-acceptable acid-addition or cationic salt thereof.

18. The method according to claim 17 where PY is 4-pyridinyl or 3-pyridinyl.
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