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

✍ Scribed by Lyn H. Jones; Helen Baldock; Mark E. Bunnage; Jane Burrows; Nick Clarke; Michele Coghlan; David Entwistle; David Fairman; Neil Feeder; Craig Fulton; Laura Hilton; Kim James; Rhys M. Jones; Amy S. Kenyon; Stuart Marshall; Sandra D. Newman; Rachel Osborne; Sheena Patel; Matthew D. Selby; Emilio F. Stuart; Michael A. Trevethick; Karen N. Wright; David A. Price

• Publisher: Elsevier Science
• Year: 2011
• Tongue: English
• Weight: 877 KB
• Volume: 21
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.10.132

✦ Synopsis

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.