| 摘要 |
Compounds having the structure, their salts or N-oxide derivatives:;
are used to treat or reduce le likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. They can be formulated together with pharmaceutically acceptable diluent or carrier or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed. |
| 主权项 |
1. A compound, 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 in R4 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. |
