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US 4,935,422 AGranted
Acyloxypropanolamines
AssigneeE. I. Du Pont de Nemours and Company
InventorsGhanshyam Patil, Khuong H. X. Mai
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AssigneeE. I. Du Pont de Nemours and Company
InventorsGhanshyam Patil, Khuong H. X. Mai
Estimating the term…
Compounds of the present invention, are represented by the general formula ##STR1## wherein R represents a straight or branched loweralkyl from 1 to about 6 carbon atoms, loweralkene from 2 to about 6 carbon atoms, or ##STR2## where m is o or 1 and n is 2, 3, 4, or 5 provided that when m is o, n is 2, 3, 4, or 5 and when m is 1, n is 3 or 4, and R.sub.1 is hydrogen, a straight, branched or cyclic loweralky from 1 to about 6 carbon atoms or loweralkoxy, phenyl or substituted phenyl, and R.sub.2 represents a straight or branched loweralkyl from 1 to about 6 carbon atoms or W-B wherein W represents alkylene of from 1 to about 10 carbon atoms which may be substituted with loweralkyl of from 1 to about 4 carbon atoms; and B represents hydrogen, --NHCOR.sub.4, or --NHCONR.sub.3 R.sub.4, wherein R.sub.3 and R.sub.4 may be the same or diffrent and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, phenyl or aralkyl wherein the alkyl group contains from 1 to about 6 carbon atoms and the aryl group represents phenyl which may be unsubstituted or substituted with lower alkyl from 1 to about 6 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, hydroxy, hydroxyalkyl of from 1 to about 10 carbon atoms; thiophenyl, imidazole, oxazole or indole, furanyl, tetrahydrofuranyl or R.sub.3 and R.sub.4 may together with N form a pyrrolidino, piperidino, piperazino, or morpholino ring, or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment or prophylaxis of cardiac disorder or in the treatment of glaucoma.
A compound of the formula ##STR30## wherein R represents a straight or branched loweralkyl from 1 to about 6 carbon atoms, loweralkene from 2 to about 6 carbon atoms, or ##STR31## where m is o or 1 and n is 2, 3, 4, or 5 provided that when m is o, n is 2, 3, 4, or 5 and when m is 1, n is 3 or 4, and R.sub.1 is hydrogen, a straight, branched or cyclic loweralkyl from 1 to about 6 carbon atoms or loweralkoxy, phenyl or substituted phenyl, and R.sub.2 represents W-B wherein W represents alkylene of from 1 to about 10 carbon atoms which may be substituted with loweralkyl of from 1 to about 4 carbon atoms;
A compound of the formula ##STR32## wherein R represents a straight or branched loweralkyl from 1 to about 6 carbon atoms, loweralkene from 2 to about 6 carbon atoms, cycloloweralkyl, cycloloweralkenyl or styryl and R.sub.2 is W-B where W is 1,1-dimethylethylene and B is --NHCONR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 together with N form a morpholino or piperidino ring, or a pharmaceutically acceptable salt thereof.
A compound of the formula ##STR33## where m is o or 1 and n is 2, 3, 4, or 5 provided that when m is o, n is 2, 3, 4, or 5 and when m is 1, n is 3 or 4, and R.sub.1 is hydrogen, a straight, branched or cyclic loweralkyl from 1 to about 6 carbon atoms or loweralkoxy, phenyl or substituted phenyl, and R.sub.2 represents W-B wherein W represents alkylene of from 1 to about 10 carbon atoms which may be substituted with loweralkyl of from 1 to about 4 carbon atoms;
A method of treating cardiac disorders in a patient comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of the formula. ##STR34## wherein R represents a straight or branched loweralkyl from 1 to about 6 carbon atoms, loweralkene from 2 to about 6 carbon atoms, or ##STR35## where m is o or 1 and n is 2, 3, 4, or 5 provided that when m is o, n is 2, 3, 4, or 5 and when m is 1, n is 3 or 4, and R.sub.1 is hydrogen, a straight, branched or cyclic loweralkyl from 1 to about 6 carbon atoms or loweralkoxy, phenyl or substituted phenyl, and R.sub.2 represents W-B wherein W represents alkylene of from 1 to about 10 carbon atoms which may be substituted with loweralkyl of from 1 to about 4 carbon atoms;
A pharmaceutical composition for treating cardiac conditions which composition contains an effective amount for treating such conditions of a compound having beta-adrenergic blocking activity of the formula ##STR38## wherein R represents a straight or branched loweralkyl from 1 to about 6 carbon atoms, loweralkene from 2 to about 6 carbon atoms, or ##STR39## where m is o or 1 and n is 2, 3, 4, or 5 provided that when m is o, n is 2, 3, 4, or 5 and when m is 1, n is 3 or 4, and R.sub.1 is hydrogen, a straight, branched or cyclic loweralkyl from 1 to about 6 carbon atoms or loweralkoxy, phenyl or substituted phenyl, and R.sub.2 represents W-B wherein W represents alkylene of from 1 to about 10 carbon atoms which may be substituted with loweralkyl of from 1 to about 4 carbon atoms;
Dependencies are inferred from the claim text.