1190897-45-0Relevant academic research and scientific papers
Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence
Brennan, Paul E.,Whitlock, Gavin A.,Ho, Danny K.H.,Conlon, Kelly,McMurray, Gordon
scheme or table, p. 4999 - 5003 (2010/03/31)
A range of heterocycle fused azepines were synthesized in order to find a CNS penetrant, selective 5-HT2C agonist for the treatment of incontinence. The pyridazo-azepines such as compound 11 were shown to be potent 5-HT2C agonists and have potential for CNS penetration and good in vitro ADME properties but lacked selectivity against 5-HT2B. Fusing a further heterocycle gave the selective triazolopyrimido-azepines. An example of this series, compound 36, was shown to be potent, selective, metabolically stable in vitro and efficacious in an in vivo model of stress urinary incontinence.
