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    Benzylideneguanidine Derivatives and Therapeutic Use for the Treatment of Protein Misfolding Diseases
    6.
    发明申请
    Benzylideneguanidine Derivatives and Therapeutic Use for the Treatment of Protein Misfolding Diseases 有权
    亚苄基胍衍生物和治疗用于治疗蛋白质错折叠疾病的治疗用途

    公开(公告)号：US20160046589A1

    公开(公告)日：2016-02-18

    申请号：US14760350

    申请日：2014-01-10

    申请人： Philippe GUEDAT ,  MEDICAL RESEARCH COUNCIL

    发明人： Philippe Guedat ,  Anne Bertolotti

    IPC分类号： C07D253/075 ,  C07C281/16 ,  A61K31/165 ,  A61K31/216 ,  A61K31/44 ,  C07D213/61 ,  A61K31/155 ,  A61K31/53

    CPC分类号： C07D253/075 ,  A61K31/155 ,  A61K31/165 ,  A61K31/216 ,  A61K31/44 ,  A61K31/53 ,  A61K45/06 ,  C07C281/16 ,  C07C281/18 ,  C07D213/61 ,  A61K2300/00

    摘要： The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl, Cl, F or Br; R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H; or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups; R6 is selected from R7, OR7 and NR8R9; R7, R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN, NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy; X and Z are each independently CR11, and Y is selected from CR11 and N; and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.

    摘要翻译： 本发明涉及式（I）化合物或其互变异构体和/或其药学上可接受的盐，其中：R 1是烷基，Cl，F或Br; R2为H或F; R3选自H和烷基; R 4选自H和C（O）R 6; R5是H; 或R 4和R 5连接形成任选被一个或多个R 10基取代的杂环基; R6选自R7，OR7和NR8R9; R 7，R 8和R 9各自独立地选自烷基，环烷基，芳烷基，环烯基，杂环基和芳基，其各自任选被一个或多个R 10基团取代; 每个R 10独立地选自卤素，OH，CN，NO 2，COO-烷基，芳烷基，SO 2 - 烷基，SO 2 - 芳基，COOH，CO-烷基，CO-芳基，NH 2，NH-烷基，N（烷基） CF 3，烷基和烷氧基; X和Z各自独立地为CR11，Y选自CR11和N; R11为H或F; 用于治疗与蛋白质错误折叠应激相关的病症，特别是与错误折叠的蛋白质的积累相关。