公开(公告)号：EP1395591B1

公开(公告)日：2008-06-04

申请号：EP02730487.2

申请日：2002-06-11

申请人： GLAXO GROUP LIMITED

发明人： DI FABIO, Romano, GlaxoSmithKline SpA ,  MARCHIONNI, Chiara, GlaxoSmithKline SpA ,  MICHELI, Fabrizio, GlaxoSmithKline SpA ,  PASQUARELLO, Alessandra, GlaxoSmithKline SpA ,  PERINI, Benedetta, GlaxoSmithKline SpA ,  ST-DENIS, Yves, GlaxoSmithKline SpA

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/517 ,  A61K51/00 ,  A61P25/00 ,  C07D239/70 ,  C07D401/04

CPC分类号： C07D487/04 ,  A61K51/0459 ,  C07B2200/05 ,  C07D239/70 ,  C07D239/94 ,  C07D471/04

摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof, wherein R is aryl or heteroaryl and each of the above groups R may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, -COR4, nitro, -NR3R4 cyano, or a group R5; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; R2 corresponds to a group CHR6R7; R3 is hydrogen, C1-C6 alkyl; R4 independently from R3, has the same meanings; R5 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle; wherein each of the above groups R5 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 dialkylamino, nitro or cyano; R6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R7 independently from R6, has the same meanings; X is carbon or nitrogen; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).