| 摘要 |
PURPOSE: A thiocarbamate derivative as an antagonist for vanilloid receptor(VR) and a pharmaceutical composition containing the same compound are provided, thereby effectively inhibiting the diseases associated with the activation of vanilloid receptor(VR). CONSTITUTION: The thiocarbamate derivative as an antagonist for vanilloid receptor(VR) is represented by formula(I), in which R1 is Ar'-(CH3)m- wherein Ar' is phenyl substituted or unsubstituted with halogen or C1 to C5 lower alkyl, pyridinyl, thiophenyl, naphthalenyl or trifluoromethylphenyl and m is 1, 2, 3 or 4, or -(CH2)n-CHPh2, -CH2CH2CH(Ph)CH2Ph wherein n is 1 or 2; Y is S or O; Z is O, -CH2, NR3, CHR3 wherein R3 is hydrogen, C1 to C5 lower alkyl, benzyl or penethyl; R2 is hydrogen, C1 to C6 lower alkyl or cycloalkyl, dimethyl or Ar"-(CH2)p wherein Ar" is phenyl substituted or unsubstituted with halogen or trifluoromethyl, or pyridinyl substituted or unsubstituted with carboxyl, amino, methansulfonylamino or t-butoxycarbonyl, imidazol or indolyl wherein p is 0, 1, 2, 3 or 4; A is O or -CH2; and Ar is a compound wherein R4 and R5 is the same or different, and hydrogen, hydroxy, methoxy, nitro, cyano, benzyloxy, amino, methansulfonylamino, halogen, C1 to C5 lower alkyl, -NHCO2CH3, -NHC(=O)CH3, trifluoromethyl, sulfamoyl, carboxyl, -OCH2OCH3 or methoxycarbonyl, pyridine substituted or unsubstituted with carboxyl, amino, methansulfonylamino, penethylaminocarbonyl or t-butoxycarbonyl, indolyl or imidazolyl.
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