SMALL-MOLECULE INHIBITORS OF THE ANDROGEN RECEPTOR

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 R<SUP>1</SUP>, R<SUP>2</SUP>, R<SUP>3</SUP> and R<SUP>8</SUP> are each independently hydrogen or C<SUB>1-6</SUB> alkyl. R<SUP>4</SUP> is absent or is hydrogen, C<SUB>1-6</SUB> alkyl or C<SUB>1-6 </SUB>alkyl-OH. R<SUP>5</SUP> is hydrogen, C<SUB>1-6</SUB> alkyl or -NR<SUP>6</SUP>R<SUP>7</SUP>, R<SUP>6</SUP> and R<SUP>7</SUP> are each independently hydrogen or C<SUB>1-6</SUB> 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<SUB>2-6</SUB> alkenylene, C<SUB>2-6</SUB> alkynylene or C<SUB>3-6</SUB>cycloalkylene. The compounds of Formula I include the salts, hydrates and prodrugs thereof. Each R<SUP>9</SUP> is H, C<SUB>1-6</SUB> alkyl, -OH or -0-C<SUB>1-6</SUB> 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.