851376-85-7Relevant 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.
FUSED HETEROCYCLIC COMPOUNDS
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Page/Page column 80-81, (2008/06/13)
Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
