4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 9, Pages 2759-2763

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.10.132

Keywords

COPD; Inhalation; Dual pharmacology; MABA; Crystallinity

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This paper describes the successful design and development of dual pharmacology beta-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. (C) 2010 Elsevier Ltd. All rights reserved.

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