ALBRECHT, Brian, K.,TAYLOR, Alexander, M.,COTE, Alexandre,GEHLING, Victor,HSIAO-WEI TSUI, Vickie,KIEFER, James, Richard, Jr.,LIANG, Jun,MAGNUSON, Steven,NASVESCHUK, Christopher, G.,ROMERO, F. Anthony
申请号：
USUS2016/012588
公开号：
WO2016/112251A1
申请日:
2016.01.08
申请国别(地区):
US
年份:
2016
代理人:
摘要：
The present invention relates to compounds of formula (I), (formula I) wherein: X is C(=0) or S(0)2； R1 is selected from the group consisting of N-linked piperazinyl, relinked piperidine, and N-linked diazabicyclo[3.2.1]octane, wherein R1 is optionally substituted with one or more groups； R2 and R3 are each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, and C3-8cycloalkyl, wherein any C1-6alkyl, C2-6alkenyl, C2-6alkynyl, and C3-8cycloalkyl is optionally substituted with one or more groups； or R2 and R3 taken together with the carbon to which they are attached form a 3-, 4-, 5-, or 6-membered carbocyclic ring that is optionally substituted with one or more groups； R4 and R5 are each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, and C3-8cycloalkyl, wherein any C1-6alkyl, C2-6alkenyl, C2-6alkynyl, and C3-8cycloalkyl is optionally substituted with one or more groups； or R4 and R5 taken together with the carbon to which they are attached form a 3-, 4-, 5-, or 6-membered carbocyclic ring that is optionally substituted with one or more groups； and R6 is a 5-10 membered heteroaryl, 5-10 membered heterocycle, or a 6-10 membered aryl, which 5-10 membered heteroaryl, 5-10 membered heterocycle, and 6-10 membered aryl is optionally substituted with one or more groups； useful as inhibitors of one or more histone demethylses, such as KDM2b. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.La présente invention concerne des composés de formule (I), (formule I) dans laquelle : X est C(=O) ou S(O)2 ； R1 est choisi dans le groupe constitué de pipérazinyle N-lié, pipéridine N-liée, et diazabicyclo[3.2.1]octane N-lié, dans laquelle R1 est éventuellement substitué par un ou plusieurs groupes ； R2 et R3 sont choisis chacun indépendamment parmi un H, un alkyle en C1-6, un alcényle en C2-6, un alcynyle en C2
