SAR of a series of inhaled A sub(2A) agonists and comparison of inhaled pharmacokinetics in a preclinical model with clinical pharmacokinetic data

COPD is a major cause of mortality in the western world. A sub(2A) agonists are postulated to reduce the lung inflammation that causes COPD. The cardiovascular effects of A sub(2A) agonists dictate that a compound needs to be delivered by inhalation to be therapeutically useful. The pharmacological...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2009-08, Vol.19 (15), p.4471-4475
Hauptverfasser: Mantell, Simon J, Stephenson, Peter T, Monaghan, Sandra M, Maw, Graham N, Trevethick, Michael A, Yeadon, Michael, Walker, Don K, Selby, Matthew D, Batchelor, David V, Rozze, Stuart, Chavaroche, Helene, Lemaitre, Arnaud, Wright, Karen N, Whitlock, Lynsey, Stuart, Emilio F, Wright, Patricia A, Macintyre, Fiona
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Sprache:eng
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Zusammenfassung:COPD is a major cause of mortality in the western world. A sub(2A) agonists are postulated to reduce the lung inflammation that causes COPD. The cardiovascular effects of A sub(2A) agonists dictate that a compound needs to be delivered by inhalation to be therapeutically useful. The pharmacological and pharmacokinetic SAR of a series of inhaled A sub(2A) agonists is described leading through to human pharmacokinetic data for a clinical candidate.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.05.027