1065113-76-9Relevant academic research and scientific papers
Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: Design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence
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.
, p. 2715 - 2720 (2011/06/22)
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.
PYRIMIDO [4, 5-D] AZEPINE DERIVATIVES AS 5-HT2C AGONISTS
-
Page/Page column 158, (2008/12/04)
The present invention relates to compounds of formula (I): wherein R1, R2, R3a,R3b, R3c, R3d and R100 are as defined in the specification. These compounds act as 5-HT2C agonists.
