| 摘要 |
The present disclosure relates to cyclic sulfones and sulfoximines that are HIF-2a inhibitors and methods of making and using them for treating cancers. In another aspect, the present disclosure provides a pharmaceutical composition comprising a compound described herein and a pharmaceutically acceptable carrier or excipient. The compound may exist in an amorphous form, a crystalline form, or as a salt, solvate, or hydrate. In another aspect, the present disclosure provides a method of treating renal cell carcinoma by administrating a therapeutically effective amount of a compound described herein or a pharmaceutical composition thereof to a subject in need of such treatment. |
| 主权项 |
1. A compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein:
R1 is alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl;R2 is hydrogen, nitro, cyano, halo, alkyl, heteroalkyl, alkynyl or alkenyl;R3 is hydrogen, hydroxy or amino;each of R4 is independently selected from the group consisting of hydrogen, halo, alkyl, heteroalkyl and cycloalkyl, or two R4 groups and the carbon(s) to which they are attached form C3-C8 cycloalkyl or C5-C8 heterocycloalkyl;R5 is O or NR6, wherein R6 is selected from the group consisting of hydrogen, alkyl, and cyano;R7 is hydrogen, deuterium, or alkyl, or R3 and R7 in combination form oxo; andn is 1 or 2. |
