pf-3246799 and Urinary-Incontinence

pf-3246799 has been researched along with Urinary-Incontinence* in 1 studies

Other Studies

1 other study(ies) available for pf-3246799 and Urinary-Incontinence

Article	Year
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. Bioorganic & medicinal chemistry letters, 2011, May-01, Volume: 21, Issue:9 New pyrimido[4,5-d]azepines 7 are disclosed as potent 5-HT(2C) receptor agonists. A preferred example, 7b had minimal activation at either the 5-HT(2A) or 5-HT(2B) 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. Topics: Animals; Azepines; Disease Models, Animal; Dogs; Male; Molecular Structure; Pyrimidines; Rats; Serotonin 5-HT2 Receptor Agonists; Urinary Incontinence	2011

Article

Year

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.

Bioorganic & medicinal chemistry letters, 2011, May-01, Volume: 21, Issue:9

New pyrimido[4,5-d]azepines 7 are disclosed as potent 5-HT(2C) receptor agonists. A preferred example, 7b had minimal activation at either the 5-HT(2A) or 5-HT(2B) 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.

Topics: Animals; Azepines; Disease Models, Animal; Dogs; Male; Molecular Structure; Pyrimidines; Rats; Serotonin 5-HT2 Receptor Agonists; Urinary Incontinence

2011