Transient receptor potential vanilloid-1 antagonists: a survey of recent patent literature.

IMPORTANCE OF THE FIELD: Transient receptor potential vanilloid-1 (TRPV1, vanilloid receptor-1) is a nonspecific cation channel that can be activated by multiple endogenous stimuli and by capsaicin, the active ingredient in chili peppers. TRPV1 is expressed predominantly on sensory neurons where it is proposed to serve as a key nodal point in pain transmission pathways. Pharmacological blockade of TRPV1 represents a compelling strategy for the treatment of a variety of disease states, particularly those requiring chronic pain management. AREA COVERED IN THE REVIEW: This review summarizes patent literature and progress in defining the utility of small molecule TRPV1 antagonists during 2008-2009. WHAT THE READER WILL GAIN: Representative compounds and key characterization data comprising multiple chemical series are highlighted. TAKE HOME MESSAGE: The continued profusion of reports, in both the primary and patent literature, attests to the sustained interest in the TRPV1 class of therapeutics. Although a number of compounds have now been brought forward for human clinical trials, the therapeutic utility of TRPV1 antagonists is yet to be validated unequivocally.