Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 16, Pages 5076-5092Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm900132z
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- Laboratorios Almirall SA, Barcelona. Spain
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The objective of this work was to discover a novel, long-acting muscarinic M-3 antagonist for the inhaled treatment of chronic obstructive pulmonary disease (COPD), with a potentially improved risk-benefit profile compared with current antimuscarinic agents. A series of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters were synthesized and evaluated. Oil the basis of its overall profile. (3R)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide) emerged as a candidate for once-dally maintenance treatment of COPD. This compound is a potent muscarinic antagonist, with long. duration of action ill vivo, and was found to have a rapid hydrolysis in human plasma, minimizing the potential to induce class-related systemic side effects. Aclidinium bromide is currently in phase III development for maintenance treatment of patients with COPD.
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