申请人:Kyowa Hakko Co., Ltd.
公开号:EP0863144A1
公开(公告)日:1998-09-09
The present invention provides imidazoquinazoline derivatives represented by formula (I):
wherein R1 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted bicycloalkyl, substituted or unsubstituted tricycloalkyl or the like, R2 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted bicycloalkyl, substituted or unsubstituted tricycloalkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted aralkyl or the like, R3 represents hydrogen, substituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted bicycloalkyl, substituted or unsubstituted tricycloalkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted aralkyl or the like, and R2 and R3 are combined to represent a substituted or unsubstituted N-containing heterocyclic group, X represents O or S, or pharmaceutically acceptable salts thereof, which have potent and selective cyclic guanosine 3',5'-monophosphate (cGMP)-specific phosphodiesterase (PDE) inhibitory activity and are useful for treating or ameliorating cardiovascular diseases such as thrombosis, angina pectoris, hypertension, heart failure, arterial sclerosis, as well as asthma, impotence and the like.
本发明提供了由式(I)代表的咪唑喹唑啉衍生物:
其中 R1 代表氢、取代或未取代的低级烷基、取代或未取代的环烷基、取代或未取代的二环烷基、取代或未取代的三环烷基或类似物,R2 代表氢、取代或未取代的低级烷基、取代或未取代的环烷基、取代或未取代的二环烷基、取代或未取代的三环烷基、取代或未取代的四环烷基、取代或未取代的五环烷基或类似物、R3代表氢、取代或未取代的低级烷基、取代或未取代的环烷基、取代或未取代的双环烷基、取代或未取代的三环烷基、取代或未取代的低级烯基、取代或未取代的芳烷基或类似物、取代或未取代的三环烷基、取代或未取代的低级烯基、取代或未取代的芳烷基或类似基团,R2 和 R3 结合代表取代或未取代的含 N 杂环基团,X 代表 O 或 S 或其药学上可接受的盐、它们具有强效和选择性环鸟苷-3',5'-单磷酸(cGMP)特异性磷酸二酯酶(PDE)抑制活性,可用于治疗或改善心血管疾病,如血栓形成、心绞痛、高血压、心力衰竭、动脉硬化以及哮喘、阳痿等。