University of Washington through its Center for Commercialization;University of Montana;Guilloteau, Nicolas
发明人:
申请号：
EP14761747.6
公开号：
EP3044216A2
申请日:
2014.08.20
申请国别(地区):
EP
年份:
2016
代理人:
摘要：
The present disclosure is generally directed to compositions and methods for treating diseases that are ameliorated by the inhibition of CYP26 mediated retinoic acid metabolism. The compositions comprise compounds of formula (I). A repreid50000060307390 IB/345 nullsents aryl optionally substituted with one, two, three, or four groups that are each independently halogen, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, &mdash；NH2, &mdash；NH(C1-C6 alkyl), &mdash；N(C1-C6 alkyl)2, &mdash；OH, C1-C6 alkoxy, and C1-C6 haloalkoxy； X is a bond, &mdash；CH2&mdash；, &mdash；CHR5&mdash；, &mdash；C&boxH；CHR4&mdash；, &mdash；NR4&mdash；, &mdash；N&boxH；O&mdash；R4&mdash；, &mdash；O&mdash；, &mdash；S&mdash；, &mdash；SO&mdash；, &mdash；SO2&mdash；, &mdash；C(O)&mdash；, or &mdash；C(NR4)&mdash；, or X is of formula (a), (b) or (c), wherein each n is independently 1, 2, or 3； each R4 is independently hydrogen or C1-6 alkyl； R5 is independently hydrogen, C1-6 alkyl, or &mdash；OR6, where R6 is selected from the group consisting of hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyL C3-12 cycloalkyl, heterocyclyl, aryl, arylC1-6 alkyl, heteroaryl, or heteroarylC1-6 alkyl； Y is C1-6 alkylene, C2-6 alkenylene, or C2-6 alkylylene moiety.La présente invention concerne de manière générale des compositions et des procédés pour traiter des maladies qui sont améliorées par l'inhibition du métabolisme de l'acide rétinoïque médié par CYP26.
