17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators

A pharmaceutical composition comprising a pharmaceutically acceptable diluent or carrier and a therapeutically effective amount of at least one compound, or a salt or an N-oxide thereof, having the following molecular formula:

• wherein n is an integer from 1 to 2;
• wherein R2 is selected from the group consisting of hydrogen and fluoro;
• wherein R3 is selected from the group consisting of hydrogen, cyano, chloro, methoxy, ethoxy, nitro, and propynyl;
• wherein R4 is selected from the group consisting of hydrogen, fluoro, chloro, bromo, cyano, amino, cyclopropyl, and C1 alkyl, wherein said cyclopropyl and C1 alkyl are optionally-substituted with fluoro;
• wherein R11β, is selected from the group consisting of hydrogen, fluoro, C1-C2 alkyl, and C2 alkenyl;
• wherein R17α and R17β are independently selected from the group consisting of hydroxyl, methoxy and -A-A′-Ar
• A and A′ being spacer groups independently selected from the group consisting of absent —CH2—, —CHF—, —CH(CH3)—, propynylene, and
• (B and C being independently selected from the group consisting of hydrogen, fluoro, and methyl),
• and Ar being selected from the group consisting of:
• (D being selected from the group consisting of hydrogen, fluoro, chloro, bromo, methyl, ethyl and methoxy and E being selected from the group consisting of hydrogen, cyano and methyl);
• (f is CH or nitrogen);
• and
• (G being selected from the group consisting of cyano, —CONR1R2 (R1 and R2 are independently selected from the group consisting of hydrogen and methyl) and —SOCH3
• wherein when R17α is hydroxyl or methoxy, R17β is -A-A′-Ar, and when R17β is hydroxyl or methoxy, R17α is -A-A′-Ar.