Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence

We have identified naphthol derivatives as inhibitors of the vanilloid receptor TRPV1 by high throughput screening. The initial lead showed high clearance in rats and has been optimized by enhancing the acidity of the phenol group. Compound 6b has reduced clearance, improved potency and is active in rat cystometry models of urinary incontinence after intravenous administration. (C) 2011 Elsevier Ltd. All rights reserved.