发明授权
- 专利标题: Small-molecule inhibitors of the androgen receptor
- 专利标题(中): 雄激素受体的小分子抑制剂
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申请号: US12717905申请日: 2010-03-04
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公开(公告)号: US08119660B2公开(公告)日: 2012-02-21
- 发明人: Marc Diamond , Jeremy Jones , Adam Renslo
- 申请人: Marc Diamond , Jeremy Jones , Adam Renslo
- 申请人地址: US CA Oakland
- 专利权人: The Regents of the University of California
- 当前专利权人: The Regents of the University of California
- 当前专利权人地址: US CA Oakland
- 代理机构: Kilpatrick Townsend & Stockton LLP.
- 主分类号: A61K31/4709
- IPC分类号: A61K31/4709 ; G01N33/53
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.
公开/授权文献
- US20100168128A1 SMALL-MOLECULE INHIBITORS OF THE ANDROGEN RECEPTOR 公开/授权日:2010-07-01
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