American Hospital Supply Corporation

Forest Laboratories Holdings Limited

The United States of America As Represented by the Department of Health

Mylan Laboratories Limited

John P O'Donnell

Paul W Erhardt

Robert J Borgman

Sheung-tsam Kam

Eric Davis

Peter Bruce Bottini

R Preston Mason

Andrew Alan Shaw

Jeffrey S Fedan

G Kurt Hogaboom

Walter Owens

Jinn Wu

Andrew Shaw

Joseph Duncan

Nebivolol has been shown to be beneficial in the treatment of cardiovascular diseases such hypertension, congestive heart failure, arterial stiffness and endothelial dysfunction. The present invention features a pharmaceutical composition comprising nebivolol and at least one other active agent, wherein the at least one other active agent is a cardiovascular agent.

Compositions comprising nebivolol

A method for the treatment or prophylaxis of cardiac disorders in a mammal, comprising administering to such mammal a short-acting .beta.-blocking compound of the formula: ##STR1## wherein X is an ester-containing group; R may be lower alkyl, aralkyl or an ester-containing group; R.sub.1 may be lower alkyl; and Ar may be substituted or unsubstituted aromatic; or a pharmaceutically acceptable salt thereof. Novel compounds possessing short acting .beta.-adrenergic blocking activity are also disclosed.

Compounds for treatment or prophylaxis of cardiac disorders

A method for the treatment or prophylaxis of cardiac disorders in a mammal, comprising administering to such mammal a short-acting .beta.-blocking compound of the formula: ##STR1## wherein R may be lower alkyl, aryl, or aralkyl; n may be an integer from 0 to about 10; x may be an integer from 1 to 3; Ar may be substituted or unsubstituted aromatic; R.sub.1 may be lower alkyl, or aralkyl; and pharmaceutically accepted salts thereof. Novel compounds possessing short-acting .beta.-adrenergic blocking activity are also disclosed.

Method for treatment or prophylaxis of cardiac disorders

A method for the treatment of prophylaxis of cardiac disorders in a mammal, comprising administering to such mammal a short-acting .beta.-blocking compound of the formula: ##STR1## wherein R may be lower alkyl, aryl, or aralkyl; n may be an integer from 0 to about 10; x may be an integer from 1 to 3; Ar may be substituted or unsubstituted aromatic; R.sub.1 may be lower alkyl, or aralkyl; and pharmaceutically accepted salts thereof. Novel compounds possessing short-acting .beta.-adrenergic blocking activity are also disclosed.

Specific method of irreversible antagonism of histamine receptors, especially H.sub.1 receptors, in, for example, isolated guinea pig vas deferens by 4(5)-[2-(4-azido-2-nitroanilino)ethyl]imidazole (AAH), which is a photoaffinity analog of histamine actuated unusually by light in the visible spectrum. Additionally, compounds of the present invention are represented by the formula ##STR1## wherein R.sub.1 and R.sub.2 represent an electron withdrawing group of the formula, H, --NO.sub.2, --Cl, --F, --Br, --I, --SO.sub.3 H. When two groups occur, it is not necessary that those groups be identical. In preferred compounds R.sub.1 is --NO.sub.2 and R.sub.2 is H and R.sub.1 is ortho to amine group. R.sub.3, R.sub.4, R.sub.5 and R.sub.6 represent a proton or lower alkyl of straight and branched carbon chains. In preferred compounds R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are protons or methyl groups with not more than two of the four positions substituted with an alkyl group. Preference is given for R.sub.4 and R.sub.5.

Specific irreversible antagonism of histamine receptors by photoaffinity

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Morgantown, WV, United States of America

John P O'Donnell