321709-19-7Relevant academic research and scientific papers
A multivalent approach to the discovery of long-acting β2- adrenoceptor agonists for the treatment of asthma and COPD
Jacobsen, John R.,Choi, Seok Ki,Combs, Jesse,Fournier, Eric J.L.,Klein, Uwe,Pfeiffer, Juergen W.,Thomas, G. Roger,Yu, Cecile,Moran, Edmund J.
scheme or table, p. 1213 - 1218 (2012/03/11)
A multivalent approach was applied to the design of long-acting inhaled β2-adrenoceptor agonists. A series of dimeric arylethanolamines based on the short acting β2-adrenoceptor agonist albuterol were prepared, varying the nature and length of the linker between the basic nitrogens. None of the C2-symmetric dimers demonstrated increased potency, however dimer 5j, derived from 4-phenethylamine, was found to have increased binding potency in vitro relative to the parent monomer. Optimization of this structure led to the identification of 22 (milveterol) which demonstrates high potency in vitro and long duration of action in a guinea pig model of bronchoprotection.
CHEMICAL PROCESS AND NEW CRYSTALLINE FORM
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Page/Page column 23-24, (2010/02/14)
The present invention relates to the preparation of a ?2 adrenergic agonist in crystalline salt form. In particular the invention relates to preparation of a crystalline salt of compound (I): in particular a crystalline monohydrochloride salt. The inventi
CRYSTALLINE β2 ADRENERGIC RECEPTOR AGONIST
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Page/Page column 28, (2010/02/06)
The invention provides a crystalline salt form of a novel β2 adrenergic receptor agonist. The invention also provides pharmaceutical compositions comprising the crystalline form, formulations containing the pharmaceutical compositions, methods of using th
