594862-13-2Relevant academic research and scientific papers
The discovery of long-acting saligenin β2 adrenergic receptor agonists incorporating a urea group
Procopiou, Panayiotis A.,Barrett, Victoria J.,Ford, Alison J.,Looker, Brian E.,Lunniss, Gillian E.,Needham, Deborah,Smith, Claire E.,Somers, Graham
, p. 6026 - 6032 (2011)
A series of novel, potent and selective human β2 adrenoceptor agonists incorporating a urea moiety on the terminal right-hand side phenyl ring of (R)-salmeterol is presented. Urea 9j had long duration of action in vitro on guinea pig trachea, and also in vivo similar to that of salmeterol. It had lower oral absorption and bioavailability than salmeterol in both rat and dog. It had a turnover ratio similar to salmeterol, with no evidence for formation of any aniline metabolites in human liver microsomes and hepatocytes. However no crystalline salts suitable for inhaled delivery were identified.
PHENETHANOLAMINE DERIVATIVES FOR TREATMENT OF RESPIRATORY DISEASES
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Page/Page column 69, (2010/02/07)
The present invention relates to novel compounds of formula (I),to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.
