Bridge Pharma Inc.

Jan L Chen

A K Gunnar Aberg

George Edward Wright

Andrew T Maioli

Gunnar A K Aberg

Racemic norketotifen, racemic 10-hydroxy-ketotifen, racemic 10-hydroxy-nor-ketotifen and optically active isomers of ketotifen, norketotifen, 10-hydroxy-ketotifen and 10-hydroxy-norketotifen were found to have antiallergic and anti-inflammatory effects while being devoid of the severe dose-limiting sedative side effects of Ketotifen.

Optically active isomers of ketotifen and therapeutically active metabolites thereof

Racemic norketotifen, racemic 10-hydroxy-ketotifen, racemic 10-hydroxy-nor-ketotifen and optically active isomers of ketotifen, norketotifen, 10-hydroxy-ketotifen and 10-hydroxy-norketotifen were found to have antiallergic and anti-inflammatory effects while being devoid of the severe dose-limiting sedative side effects of ketotifen.

The present invention relates to smooth muscle spasmolytic agents, pharmaceutical compositions containing them and method of using said compounds and compositions for the treatment of urinary incontinence, and other smooth muscle contractility conditions. More particularly, the present invention relates to certain metabolically stabilized secondary amines having smooth muscle relaxing properties while avoiding, on administration to a mammal, adverse side effects such as prominent antimuscarinic, arrhythmogenic and cardiodepressive effects.

Smooth muscle spasmolytic agents

The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.

Dermal anesthetic agents

Disclosed are N-substituted hydroxyalkyl or carboxyalkyloxyalkyl analogs of 9- and/or 10-oxo-4Hbenzo&lsqb;4,5&rsqb;cycloheptal&lsqb;1,2-b&rsqb;thiophene compounds, or 9-OH and/or 10-OH-substituted analogs thereof, which possess antihistaminic and antiasthmatic properties with reduced sedative side effects. The optically active isomers and pharmaceutically acceptable salts thereof are also described. The compounds were also found to prevent smooth muscle hyperreactivity.

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Shrewsbury, MA, United States of America

Jan L Chen