NITROGENATED FUSED RING DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND USE OF THE SAME FOR MEDICAL PURPOSES
                        
                            
                                申请人:Kissei Pharmaceutical Co., Ltd.
                            
                            
                                公开号:EP2143724A1
                            
                            
                                公开(公告)日:2010-01-13
                            
                            
[Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like.
[Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, -OW1, -SW1, -COW2, -NW3W4, -SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, -CO-Y, -SO2-Y -S-(alkylene)-Y, -O-(alkylene)-Y, -SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.
                            [目的]本发明提供了可作为预防或治疗性激素依赖性疾病或类似疾病的药物的化合物。
[解决方案] 本发明提供了由以下通式(I)表示的具有 GnRH 拮抗活性的含氮融合环衍
生物、原药、盐、含有这些衍
生物的药物组合物及其药用用途等。式(I)中,环 A 和 B 独立地为芳基或杂芳基;RA 和 RB 独立地为卤素、
氰基、烷基、烷基磺酰基、-OW1、-SW1、-COW2、-NW3W4、-SO2NW3W4、芳基等;RC 为 H 或烷基;E 为氧原子等。U 是单键或亚烷基;X 是 Y、-CO-Y、-SO2-Y -S-(亚烷基)-Y、-O-(亚烷基)-Y、-SO2-(亚烷基)-Y 等;Y 是 Z 或
氨基等;Z 是环烷基、杂环烷基、芳基、杂芳基等。