Inhalation by design: Dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD

Inhalation by design: Dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD

This paper describes the successful design and development of dual pharmacology β-2 agonists-M3 antagonists, for the treatment of chronic obstructive pulmonary disorder using the principles of ‘inhalation by design’. A key feature of this work is the combination of balanced potency and pharmacodynam...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2011-05, Vol.21 (9), p.2759-2763
Hauptverfasser: Jones, Lyn H., Baldock, Helen, Bunnage, Mark E., Burrows, Jane, Clarke, Nick, Coghlan, Michele, Entwistle, David, Fairman, David, Feeder, Neil, Fulton, Craig, Hilton, Laura, James, Kim, Jones, Rhys M., Kenyon, Amy S., Marshall, Stuart, Newman, Sandra D., Osborne, Rachel, Patel, Sheena, Selby, Matthew D., Stuart, Emilio F., Trevethick, Michael A., Wright, Karen N., Price, David A.
Format: Artikel
Sprache:eng
Schlagworte:
Administration, Inhalation
Adrenergic beta-2 Receptor Agonists - administration & dosage
Animals
antagonists
Benzhydryl Compounds - administration & dosage
Biological and medical sciences
breathing
Catecholaminergic system
chemistry
Cholinergic system
COPD
Cresols - administration & dosage
Crystallinity
Drug Design
Drug Therapy, Combination
Dual pharmacology
Guinea Pigs
Inhalation
MABA
Medical sciences
Molecular Structure
Muscarinic Antagonists - administration & dosage
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
pharmacokinetics
Pharmacology. Drug treatments
Phenylpropanolamine - administration & dosage
Pulmonary Disease, Chronic Obstructive - drug therapy
Respiratory system
Tolterodine Tartrate
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Zusammenfassung:This paper describes the successful design and development of dual pharmacology β-2 agonists-M3 antagonists, for the treatment of chronic obstructive pulmonary disorder using the principles of ‘inhalation by design’. A key feature of this work is the combination of balanced potency and pharmacodynamic duration with desirable pharmacokinetic and material properties, whilst keeping synthetic complexity to a minimum.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.10.132