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The discovery of adamantyl-derived, inhaled, long acting beta(2)-adrenoreceptor agonists
Authors:Brown Alan D  Bunnage Mark E  Glossop Paul A  James Kim  Jones Rhys  Lane Charlotte A L  Lewthwaite Russell A  Mantell Simon  Perros-Huguet Christelle  Price David A  Trevethick Mike  Webster Rob
Affiliation:Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
Abstract:The design and profile of a series of adamantyl-containing long acting beta(2)-adrenoreceptor agonists are described. An optimal pharmacokinetic profile of low oral bioavailability was combined with a strong pharmacology profile when assessed using a guinea pig trachea tissue model. A focus was then placed on developing a robust synthetic route to ensure rapid delivery of material for clinical trials.
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