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Bioorg Med Chem Lett. 2009 Sep 1;19(17):4999-5003. doi: 10.1016/j.bmcl.2009.07.063. Epub 2009 Jul 16.

Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence.

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Genito-Urinary Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent, UK.


A range of heterocycle fused azepines were synthesized in order to find a CNS penetrant, selective 5-HT(2C) agonist for the treatment of incontinence. The pyridazo-azepines such as compound 11 were shown to be potent 5-HT(2C) agonists and have potential for CNS penetration and good in vitro ADME properties but lacked selectivity against 5-HT(2B). 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.

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