| 摘要 |
Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein R1 to R5 and X1 to X5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.; |
| 主权项 |
1. A compound of Formula I: wherein R1 to R5 are the same or different and are each selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 hydroxyalkyl, C1-C6 alkoxy, C1-C6 alkoxy C1-C6 alkyl, C1-C6 alkylamino, di-C1-C6 alkylamino, C1-C6 dialkylamino C1-C6 alkyl, C1-C6 thioalkyl, C2-C6 thioalkenyl, C2-C6 thioalkynyl, C6-C22 aryloxy, C2-C6 acyloxy, C2-C6 thioacyl, C1-C6 amido, and C1-C6 sulphonamido; wherein X1 to X5 are the same or different and are each selected from the group consisting of H and electron withdrawing groups; and wherein bond “a” can be in either the E or Z form; or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof with the proviso that
R1 to R5 and X1 to X5 cannot all be H simultaneously; andwhen only one of R1 to R5 is methoxy and the others of R1 to R5 are H, and four of X1 to X5 are H, then the remaining one of X1 to X5 cannot be an electron withdrawing group which is either NO2, CN or CF3.
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