Back to results
US 4,906,629 AGranted
Pyridazinone and pyrazolone compounds, cardiotonic compositions including same, and their uses
AssigneeRorer Pharmaceutical Corporation
InventorsAlfred P. Spada, William L. Studt, Henry F. Campbell, Donald E. Kuhla, Thomas Tucker
Life of this patent
Estimating the term…
Abstract
This invention relates to substituted pyridooxazinone and naphtheridone pyridazinone and pyrazolone compounds which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.
Claims20
A compound of the formula ##STR13## wherein A is --C.dbd. or --N.dbd.;
- B is --C.dbd.C--, --C.dbd.N-- or --N.dbd.C--;
- provided that A or B represents a nitrogen-containing group;
- X is --(CR.sub.4 R.sub.5).sub.a --(O).sub.b --(CR.sub.6 R.sub.7).sub.c --;
- a and c are 0, 1 or 2;
- b and z are 0 or 1;
- provided that a+b+c=1,
- R.sub.n is hydrogen, alkyl, aralkyl, aryl, acyl, carbalkoxy, carbamyl, carbalkoxyalkyl, hydroxyalkyl, alkoxyalkyl, or amidino;
- R, R.sub.1, R.sub.2, R.sub.3, R.sub.5 and R.sub.6 are hydrogen, alkyl, or aralkyl;
- R.sub.4 is hydrogen, alkyl, aryl, or aralkyl;
- R.sub.7 is hydrogen, alkyl, aralkyl, aryl, acyl, carbalkoxy, carbalkoxyalkyl, hydroxyalkyl, alkoxyalkyl, amidino, alkoxy, amino, nitro, carboxy, cyano, alkyl amino, halo, hydroxy, mercaptyl, alkyl mercaptyl, carboalkyl or carbamoyl;
- R and groups on vicinal carbon atoms may together form a carbon-carbon double bond provided that R.sub.n is hydrogen and z=1;
- R.sub.6 and R.sub.7 geminal groups may together form a spiro substituent, --(CH.sub.2).sub.d --, where d is 2 to 5;
- R.sub.2 is hydrogen or --(CH.sub.2).sub.y --Y where y is 1-3;
- Y is hydrogen, --O--R.sub..alpha., --S--R.sub..alpha. or --NR.sub..alpha. R.sub..beta. ;
- R.sub..alpha. is hydrogen, alkyl or acyl;
- R.sub..beta. is hydrogen or alkyl;
- R.sub..alpha. and R.sub..beta. together with the nitrogen atom to which they are attached may form a 3-7 membered ring which may also contain 0-2 additional N, O or S atoms;
- or a pharmaceutically acceptable salt thereof.
15 more elements
Dependencies are inferred from the claim text.