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    • 8. 发明公开
    • 신규 티오카르밤산 유도체 및 이를 함유하는 약제학적조성물
    • 作为VANILLOID受体(VR)的拮抗剂和含有该化合物的药物组合物的甲硫氨酸衍生物
    • KR1020020030010A
    • 2002-04-22
    • KR1020010050094
    • 2001-08-20
    • 주식회사 아모레퍼시픽그룹
    • 서영거오우택김희두이지우박형근박영호이정범
    • C07C333/02
    • C07D333/20A61K31/165A61K31/17A61K31/175C07C271/12C07C311/08C07C327/44C07C333/04C07C333/08C07C335/12C07D209/08C07D213/40C07D213/73C07D213/75C07D213/79
    • 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.
    • 目的:提供作为香草素受体(VR)拮抗剂的硫代氨基甲酸酯衍生物和含有相同化合物的药物组合物,从而有效抑制与香草素受体(VR)的活化相关的疾病。 构成:作为香草素受体(VR)的拮抗剂的硫代氨基甲酸酯衍生物由式(I)表示,其中R 1是Ar' - (CH 3)m - ,其中Ar'是被卤素取代或未取代的苯基或C 1至C 5的低级烷基 ,吡啶基,噻吩基,萘基或三氟甲基苯基,m为1,2,3或4,或 - (CH 2)n -CHCH 2,-CH 2 CH 2 CH(Ph)CH 2 Ph,其中n为1或2; Y为S或O; Z为O,-CH2,NR3,CHR3,其中R3为氢,C1至C5低级烷基,苄基或penethyl; R 2是氢,C 1至C 6低级烷基或环烷基,二甲基或Ar“ - (CH 2)p,其中Ar”是被卤素或三氟甲基取代或未取代的苯基,或被羧基,氨基,甲磺酰氨基或叔丁氧基羰基取代或未取代的吡啶基, 咪唑或吲哚基,其中p为0,1,2,3或4; A为O或-CH 2; 并且Ar是其中R 4和R 5相同或不同的化合物,氢,羟基,甲氧基,硝基,氰基,苄氧基,氨基,甲磺酰氨基,卤素,C1至C5低级烷基,-NHCO2CH3,-NHC(= O)CH3 三氟甲基,氨磺酰基,羧基,-OCH 2 OCH 3或甲氧基羰基,用羧基取代或未取代的吡啶,氨基,甲磺酰氨基,苯乙基氨基羰基或叔丁氧基羰基,吲哚基或咪唑基。