利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

20 条记录 (耗时 0.042 秒)

    Small-molecule inhibitors of the androgen receptor
    10.
    发明授权
    Small-molecule inhibitors of the androgen receptor 有权
    雄激素受体的小分子抑制剂

    公开(公告)号：US07696227B2

    公开(公告)日：2010-04-13

    申请号：US12101680

    申请日：2008-04-11

    申请人： Marc Diamond ,  Jeremy Jones ,  Adam Renslo

    发明人： Marc Diamond ,  Jeremy Jones ,  Adam Renslo

    IPC分类号： A61K31/4709 ,  C07D403/06

    CPC分类号： C07D401/06

    摘要： The present invention provides a method of inhibiting an androgen receptor by administering a compound of Formula I: or a compound of Formula II: wherein R1, R2, R3 and R8 are each independently hydrogen or C1-6 alkyl. R4 is absent or is hydrogen, C1-6 alkyl or C1-6 alkyl-OH. R5 is hydrogen, C1-6 alkyl or —NR6R7. R6 and R7 are each independently hydrogen or C1-6 alkyl, or are combined with the nitrogen to which they are attached to form a heterocycloalkyl having from 5 to 7 ring members. L is a linker of C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene or C3-6 cycloalkylene. The compounds of Formula I include the salts, hydrates and prodrugs thereof. Each R9 is H, C1-6 alkyl, —OH or —O—C1-6 alkyl. The compounds of Formulas I and II include the salts, hydrates and prodrugs thereof. By administering the compound of Formula I or II, the method inhibits the androgen receptor.

    摘要翻译： 本发明提供通过给予式I化合物或式II化合物来抑制雄激素受体的方法：其中R 1，R 2，R 3和R 8各自独立地为氢或C 1-6烷基。 R4不存在或为氢，C 1-6烷基或C 1-6烷基-OH。 R5是氢，C1-6烷基或-NR6R7。 R 6和R 7各自独立地为氢或C 1-6烷基，或与它们所连接的氮原子结合形成具有5-7个环成员的杂环烷基。 L是C 1-6亚烷基，C 2-6亚烯基，C 2-6亚炔基或C 3-6亚环烷基的接头。 式I的化合物包括其盐，水合物和前药。 每个R 9为H，C 1-6烷基，-OH或-O-C 1-6烷基。 式I和II的化合物包括其盐，水合物和前药。 通过施用式I或II的化合物，该方法抑制雄激素受体。