1041191-13-2Relevant academic research and scientific papers
Thienopyrimidines as β3-adrenoceptor agonists: Hit-to-lead optimization
Tasler, Stefan,Baumgartner, Roland,Ammendola, Astrid,Schachtner, Josef,Wieber, Tanja,Blisse, Marcus,Rath, Sandra,Zaja, Mirko,Klahn, Philipp,Quotschalla, Udo,Ney, Peter
supporting information; scheme or table, p. 6108 - 6115 (2010/11/19)
Resulting from a vHTS based on a pharmacophore alignment on known β3-adrenoceptor ligands, an aryloxypropanolamine scaffold comprising a thienopyrimidine moiety was further optimized as a human β3-AR agonist, yielding a lead compound with an excellent cellular activity of EC50 = 20 pM, selectivity over hβ1- and hβ2-adrenoceptors and a promising safety profile.
Aryloxypropanolamines, methods of preparation thereof and use of aryloxypropanolamines as medicaments
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Page/Page column 15, (2008/12/07)
This invention relates to novel aryloxypropanolamines. The invention also relates to the pharmaceutically acceptable salts and solvates containing said compounds, methods for the preparation thereof and to respective synthesis intermediates. Said compound
