| 摘要 |
The present invention relates to a compound of Formula III or a salt, solvate, or hydrate thereof:
for treating or preventing a condition involving activation of TRPV3 or for which reduced TRPV3 activity can reduce the severity, wherein Ar represents a substituted or unsubstituted aryl or heteroaryl ring; Q represents O, S, NR, or CH 2 ; R represents H or lower alkyl; R' represents H or a substituted or unsubstituted lower alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, cycloalkylalkyl, heterocyclylalkyl, aralkyl, or heteroaralkyl; R" represents H or lower alkyl; V is absent or represents C=O, C=S, or SO 2 ; W represents a hydrogen-bond acceptor, such as =0, =S, amino, hydroxyl, or ether; E represents H, a substituted or unsubstituted lower alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, cycloalkylalkyl, heterocyclylalkyl, aralkyl, or heteroaralkyl, or halogen, carbonyl (e.g., ester, carboxyl, or formyl), thiocarbonyl (e.g., thioester, thiocarboxylate, or thioformate), ketone, aldehyde, amino, acylamino, amido, amidino, cyano, nitro, azido, sulfonyl, sulfoxido, sulfate, sulfonate, sulfamoyl, sulfonamido, or phosphoryl; x represents 0 or 1 wherein when x is 0, the carbons bearing W and V are directly linked by a single or double bond; and wherein said compound inhibits TRPV3 with an with an IC 50 of 10 micromolar or less; and wherein the term "lower alkyl" represents a substituted or unsubstituted straight chain or branched chain alkyl having from one to ten carbon atoms in its backbone structure. |
