Fused heterocyclic derivative, pharmaceutical composition comprising the derivative, and use of the composition for medical purposes
申请人:Ohno Kohsuke
公开号:US08426427B2
公开(公告)日:2013-04-23
The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides fused heterocyclic derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A is 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA is halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; ring B is aryl or heteroaryl; RB is halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; E1 and E2 are oxygen atom, etc.; Q is hydrogen atom, alkyl, alkylsulfonyl, acyl, etc.; X is -(alkylene)-Z, —CO—Y, —SO2—Y, etc. (in which Y is Z or amino, etc.; Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.
本发明提供了化合物,可用作预防或治疗性激素依赖性疾病等的药剂。即,本发明提供了融合的杂环衍生物,其表示为以下通式(I),具有GnRH拮抗活性,包括含有它们的制药组合物,药用途及其他。在式(I)中,环A是5-成员环未饱和碳氢化合物或5-成员杂芳基;RA是卤素,烷基,烯基,炔基,羧基,烷氧基,氨基甲酰基等;环B是芳基或杂芳基;RB是卤素,烷基,羧基,烷氧基,氨基甲酰基等;E1和E2是氧原子等;Q是氢原子,烷基,烷基磺酰基,酰基等;X是-(烷基)-Z,-CO-Y,-SO2-Y等(其中Y是Z或氨基等;Z是环烷基,杂环烷基,芳基,杂芳基等)。