Bioorganic and Medicinal Chemistry Letters p. 2715 - 2720 (2011)
Update date:2022-07-30
Topics:
Andrews, Mark D.
Fish, Paul V.
Blagg, Julian
Brabham, Tiffini K.
Brennan, Paul E.
Bridgeland, Alison
Brown, Alan D.
Bungay, Peter J.
Conlon, Kelly M.
Edmunds, Nicholas J.
Af Forselles, Kerry
Gibbons, Colleen P.
Green, Martin P.
Hanton, Giles
Holbrook, Mark
Jessiman, Alan S.
McIntosh, Karin
McMurray, Gordon
Nichols, Carly L.
Root, James A.
Storer, R. Ian
Sutton, Michael R.
Ward, Robin V.
Westbrook, Dominique
Whitlock, Gavin A.
New pyrimido[4,5-d]azepines 7 are disclosed as potent 5-HT2C receptor agonists. A preferred example, 7b had minimal activation at either the 5-HT2A or 5-HT2B receptors combined with robust efficacy in a preclinical canine model of stress urinary incontinence (SUI) and attractive pharmacokinetic and safety properties. Based on this profile, 7b (PF-3246799) was identified as a candidate for clinical development for the treatment of SUI. In addition, it proved to be critical to build an understanding of the translation between recombinant cell-based systems, native tissue preparations and in vivo preclinical models. This was a significant undertaking and proved to be crucial in compound selection.
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