The present invention provides compounds which have a pyrazinone or pyridinone ring at P3 and an optionally substituted heteroaryl group at P1. These compounds have biological activity as active and potent inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds and pharmaceutical compositions comprising these compounds as therapeutic agents for treatment of disease states in mammals which are characterized by abnormal thrombosis are also described.
本发明提供了一些化合物,它们在P3处具有
吡唑酮或
吡啶酮环,并且在P1处有一个可选取代的杂环芳基基团。这些化合物具有
生物活性,作为凝血酶的活性和有效的
抑制剂。还描述了这些化合物的药学上可接受的盐、药物组成物以及使用这些化合物和包含这些化合物的药物组成物作为治疗哺乳动物疾病状态的治疗剂的方法,这些疾病状态以异常的血栓形成为特征。