| 摘要 |
The present invention relates to novel substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss, muscle loss, acne and hirsutism. |
| 主权项 |
1. A compound of formula (I): or a pharmaceutically-acceptable salt, solvate or hydrate thereof, wherein R1 is selected from wherein Z is selected from CF3, alkoxy, CF3O, halogen, cyano and C1-C4 alkyl optionally substituted with one or more halogens; Y is selected from halogen, alkoxy, hydroxyl, CF3O and cyano; W is oxygen; R3 and R4 are independently selected from C1-C4 alkyl optionally substituted with one or more fluoro or hydroxyl groups, or R3 and R4 and the carbon to which they are attached together form a 3-6 membered cycloalkyl ring, wherein one or more carbons may be optional substituted with one or more fluoro or hydroxyl groups, and wherein one of the carbons is optionally an oxygen or nitrogen; and R2 is an aryl or heteroaryl group substituted with one or more C1-C6 alkyl, C(O)NHR″, SO2R″, SO2NHR″, cyano, hydroxyl, alkoxy, C(S)NHR″, C(O)OR″, CH2(CH2)mQ, halogen or a 5-6 membered heteroaryl group, where R″ is selected from hydrogen, C1-C6 alkyl, C1-C6 cycloalkyl and C1-C6 alkenyl; m is an integer selected from 0 to 6; and Q is selected from C(O)NHR″, SO2R″, SO2NHR″, cyano, hydroxyl, alkoxy, C(S)NHR″ and C(O)OR″; or R2 is a substituted or unsubstituted alkyl or heterocyclic group. |
