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    • 6. 发明申请
    • SMALL-MOLECULE INHIBITORS OF THE ANDROGEN RECEPTOR
    • 雄性受体的小分子抑制剂
    • WO2008128100A1
    • 2008-10-23
    • PCT/US2008/060107
    • 2008-04-11
    • THE REGENTS OF THE UNIVERSITY OF CALIFORNIADIAMOND, MarcJONES, JeremyRENSLO, Adam
    • DIAMOND, MarcJONES, JeremyRENSLO, Adam
    • C07K1/00C07K14/00
    • C07D401/06
    • 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 R 1 , R 2 , R 3 and R 8 are each independently hydrogen or C 1-6 alkyl. R 4 is absent or is hydrogen, C 1-6 alkyl or C 1-6 alkyl-OH. R 5 is hydrogen, C 1-6 alkyl or -NR 6 R 7 , R 6 and R 7 are each independently hydrogen or C 1-6 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 Ci-6 alkylene, C 2-6 alkenylene, C 2-6 alkynylene or C 3-6 cycloalkylene. The compounds of Formula I include the salts, hydrates and prodrugs thereof. Each R 9 is H, C 1-6 alkyl, -OH or -0-C 1-6 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.
    • 本发明提供通过给予式(I)的化合物或式(II)的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。 R 4不存在或为氢,C 1-6烷基或C 1-6烷基-OH。 R 5是氢,C 1-6烷基或-NR 6 R 7,R 6, R 7和R 7各自独立地为氢或C 1-6烷基,或者与它们所连接的氮组合,形成具有5个以上的杂环烷基 到7个戒指成员。 L是C 1-6亚烷基,C 2-6亚烯基,C 2-6亚炔基或C 3-6亚环烷基的连接体。 式I的化合物包括其盐,水合物和前药。 每个R 9是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。