Nitrogen-containing compounds and pharmaceutical compositions thereof for the treatment of atrial fibrillation
申请人:Matsumura Shuuji
公开号:US08822453B2
公开(公告)日:2014-09-02
The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1)
or a salt thereof,
wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl;
R2 and R3 may be linked to form lower alkylene;
A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo;
Y1 and Y2 are each independently —N═ or —CH═;
and
R5 is group represented by
wherein R6 and R7 are each independently hydrogen or organic group;
R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—;
XA and XB are each independently a bond, lower alkylene, etc.
本发明提供了一种新型二氮杂烷化合物,可比其他K+通道更有效地和更选择性地阻断IKur电流或Kv1.5通道。本发明涉及一种由通式(1)表示的二氮杂烷化合物或其盐,其中R1、R2、R3和R4各自独立地为氢、低碳基、环低碳基或低烷氧基低碳基;R2和R3可以连接形成低碳烷基;A1是低碳烷基,可选地取代一个或多个取代基,所述取代基选择自羟基和氧代基;Y1和Y2各自独立地为—N═或—CH═;以及R5是由以下式子表示的基:其中R6和R7各自独立地为氢或有机基团;R6和R7可以与相邻的基团—XA—N—XB—一起形成环;XA和XB各自独立地为键、低碳烷基等。