公开(公告)号：US06653340B1

公开(公告)日：2003-11-25

申请号：US09647154

申请日：2000-09-27

申请人： Yarlagadda S. Babu ,  J. Claude Bennett ,  Shri Niwas ,  R. Scott Rowland

发明人： Yarlagadda S. Babu ,  J. Claude Bennett ,  Shri Niwas ,  R. Scott Rowland

IPC分类号： A61K31343

CPC分类号： C07D277/68 ,  C07D307/84 ,  C07D333/70 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12

摘要： The present invention is concerned with new compounds, and particularly those having a fused bicyclic ring substituted with an amidine moiety. These compounds are each potent inhibitors of Factor D of the alternate pathway of complement, C1s of the classical pathway of complement, Factors Xa, XIIa, VIIa and thrombin of the coagulation pathway, plasmin in the fibrinolytic pathway, and kallikrein and high molecular weight kininogen in the inflammatory pathways. These proteases, which have serine in their active site, are called serine proteases and they are pivotal to most of the processes of inflammation and coagulation. In fact, these various systems are interactive with one another and it is difficult to activate one pathway without it influencing the others.

摘要翻译： 本发明涉及新化合物，特别是具有被脒部分取代的稠合双环的化合物。 这些化合物各自是补体交替途径因子D的功能抑制剂，补体经典途径的C1s，凝血途径的因子Xa，XIIa，VIIa和凝血酶，纤维蛋白溶解途径中的纤溶酶，激肽释放酶和高分子量激肽原 在炎症通路中。 这些在其活性位点具有丝氨酸的蛋白酶被称为丝氨酸蛋白酶，它们对炎症和凝血的大多数过程是至关重要的。 事实上，这些各种系统是相互交互的，并且难以激活一个路径而不影响其他路径。