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    • 3. 发明申请
    • SMALL-MOLECULE INHIBITORS OF THE ANDROGEN RECEPTOR
    • 雄性受体的小分子抑制剂
    • US20100168128A1
    • 2010-07-01
    • US12717905
    • 2010-03-04
    • Marc DiamondJeremy JonesAdam Renslo
    • Marc DiamondJeremy JonesAdam Renslo
    • A61K31/4709A61K31/585A61K31/57A61K31/56A61K31/496A61P17/00A61P35/00A61P17/10
    • 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 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.
    • 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。
    • 4. 发明申请
    • SMALL-MOLECULE INHIBITORS OF THE ANDROGEN RECEPTOR
    • 雄性受体的小分子抑制剂
    • US20080293766A1
    • 2008-11-27
    • US12101680
    • 2008-04-11
    • Marc DiamondJeremy JonesAdam Renslo
    • Marc DiamondJeremy JonesAdam Renslo
    • A61K31/4709C07D215/38A61P35/00
    • 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 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.
    • 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。
    • 6. 发明授权
    • Small-molecule inhibitors of the androgen receptor
    • 雄激素受体的小分子抑制剂
    • US08119660B2
    • 2012-02-21
    • US12717905
    • 2010-03-04
    • Marc DiamondJeremy JonesAdam Renslo
    • Marc DiamondJeremy JonesAdam Renslo
    • A61K31/4709G01N33/53
    • 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 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.
    • 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。