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The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1- hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting ß2-adrenoceptor agonist
Authors
Alexandre Trifilieff (2044138)
Andrew Brearley (16205177)
+25 more
Andrew Tuffnell (16207880)
Christine Lewis (2299114)
Clive McCarthy (2044096)
Darryl Jones (3325716)
David Beattie (2299147)
David Farr (2299150)
David Sykes (2299132)
Diana Janus (2299159)
Friedrich Schuerch (9137027)
Helen Oakman (2044141)
Janet Maas (3965162)
Joe Fullerton (2299144)
John Fozard (16207868)
Julia Hatto (1663819)
Lyndon Brown (2044093)
Lynne Jordan (13565071)
Mark Mercer (16207871)
Martin Gosling (4465864)
Michelle Bradley (2299156)
Neil Press (16207874)
Nicola Arnold (2044117)
Rachel Profit (16207877)
Robin A Fairhurst (16205165)
Roger J Taylor (16205192)
Steven J Charlton (16205051)
Publication date
1 September 2014
Publisher
Abstract
The optimisation of two series of 4-hydroxybenzothiazolone derived ß2-adrenoceptor agonists, bearing a-substituted cyclopentyl and ß-phenethyl amino-substituents, as inhaled long-acting bronchodilators is described. Analogues were selected for synthesis using a lipophilicity based hypothesis to achieve the targeted rapid onset of action in combination with a long duration of action. The profiling of the two series led to identification of the a-substituted cyclopentyl analogue 2 as the optimal compound with a comparable profile to the inhaled once-daily long-acting ß2-adrenoceptor agonist indacaterol. On the basis of these data 2 was promoted as the backup development candidate to indacaterol from the Novartis LABA project. © 2014 Elsevier Ltd. All rights reserved
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Last time updated on 05/12/2023