COMPOUNDS FOR MODULATING TRPV3 FUNCTION

摘要

The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.

主权项

1. A pharmaceutical preparation suitable for use in a human patient for treating or preventing a condition involving activation of TRPV3 or for which reduced TRPV3 activity can reduce the severity, comprising an effective amount of a compound of Formula I or a salt thereof, or a solvate, hydrate, oxidative metabolite or prodrug of the compound or its salt, and one or more pharmaceutically acceptable excipients:wherein
Ar and Ar′ each independently represent an aryl or heteroaryl group; G1 and G2 each independently represent lower alkyl, or together with the carbons to which they are attached, G1 and G2 form an aryl or heteroaryl group fused to the pyrimidinone ring; L represents a linker having 1-3 atoms; andwherein said compound inhibits TRPV3 with an IC50 of 10 micromolar or less.