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    κ opioid receptor agonist comprising 2-phenylbenzothiazoline derivative
    2.
    发明授权
    κ opioid receptor agonist comprising 2-phenylbenzothiazoline derivative 有权
    κ阿片受体激动剂，其包含2-苯基苯并噻唑啉衍生物

    公开(公告)号：US07112598B2

    公开(公告)日：2006-09-26

    申请号：US10509549

    申请日：2003-03-28

    申请人： Maki Tokai ,  Takahiro Honda ,  Masashi Niwa ,  Yaeko Osumi ,  Ken-ichi Fujimura ,  Shin-ichi Kohno

    发明人： Maki Tokai ,  Takahiro Honda ,  Masashi Niwa ,  Yaeko Osumi ,  Ken-ichi Fujimura ,  Shin-ichi Kohno

    IPC分类号： C07D277/66 ,  C07D417/12 ,  A61K31/428 ,  A61P29/00 ,  A61P25/04

    CPC分类号： C07D417/12 ,  A61K31/428 ,  C07D277/66

    摘要： A compound or a salt thereof having the following formula wherein R1 is acyl, R2 is hydrogen, halogen, unsubstituted alkyl or alkyl substituted by halogen; R3 is halogen or alkoxy; R4 is cycloalkyl, unsubstituted alkyl or alkyl substituted by cycloalkyl, aryl or hydroxyl or an ester thereof or alkoxy; R5 is hydroxyl or an ester thereof, alkoxy or alkoxyalkyl; or R4 and R5 are bonded with each other to form a pyrrolidine ring substituted by hydroxyl or an ester thereof, alkoxy or alkoxyalkyl; R6 is hydroxyl or an ester thereof, alkoxy, alkoxyalkoxy, alkoxyalkoxyalkoxy, mercapto or alkylthio; and A1 and A2, are the same or different, and are alkylene, provided that (i) when R4 and R5 are bonded to each other to form the pyrrolidine ring substituted by hydroxyl or an ester thereof, R2 is halogen; (ii) when R4 and R5 are bonded to each other to form the pyrrolidine ring substituted by alkoxyalkyl, R2 is hydrogen; (iii) when R6 is hydroxyl or an ester thereof, R4 is isopropyl.

    摘要翻译： 具有下式的化合物或其盐，其中R 1是酰基，R 2是氢，卤素，未取代的烷基或被卤素取代的烷基; R 3是卤素或烷氧基; R 4是环烷基，未取代的烷基或被环烷基，芳基或羟基或其酯或烷氧基取代的烷基; R 5是羟基或其酯，烷氧基或烷氧基烷基; 或R 4和R 5彼此键合以形成被羟基或其酯取代的吡咯烷环，烷氧基或烷氧基烷基; R 6是羟基或其酯，烷氧基，烷氧基烷氧基，烷氧基烷氧基烷氧基，巯基或烷硫基; 和A 1和A 2各自相同或不同，并且是亚烷基，条件是（i）当R 4和R 0 > 5个彼此键合以形成被羟基或其酯取代的吡咯烷环，R 2是卤素; （ii）当R 4和R 5彼此键合以形成被烷氧基烷基取代的吡咯烷环时，R 2是氢; （iii）当R 6为羟基或其酯时，R 4为异丙基。