-
公开(公告)号:US6057314A
公开(公告)日:2000-05-02
申请号:US880885
申请日:1997-06-23
申请人: John Dimaio , M. Arshad Siddiqui , John W. Gillard , Yves St-Denis , Micheline Tarazi , Patrice Preville , Sophie Levesque , Benoit Bachand , Annette Marian Doherty , Jeremy John Edmunds
发明人: John Dimaio , M. Arshad Siddiqui , John W. Gillard , Yves St-Denis , Micheline Tarazi , Patrice Preville , Sophie Levesque , Benoit Bachand , Annette Marian Doherty , Jeremy John Edmunds
IPC分类号: C07D487/04 , C07D498/04 , C07D513/04 , A61K31/54 , A01N43/58 , C07D265/36 , C07D279/02
CPC分类号: C07D487/04 , C07D513/04
摘要: This invention relates to the discovery of heterocyclic competitive inhibitors of the enzyme thrombin, their preparation, and pharmaceutical compositions thereof. As well, this invention relates to the use of such compounds and compositions in vitro as anticoagulants and in vivo as agents for the treatment and prophylaxis of thrombotic disorders such as venous thrombosis, pulmonary embolism and arterial thrombosis resulting in acute ischemic events such as myocardial infarction or cerebral infarction. Moreover, these compounds and compositions have therapeutic utility for the prevention and treatment of coagulopathies associated with coronary bypass operations as well as restenotic events following transluminal angioplasty.
摘要翻译: 本发明涉及酶凝血酶的杂环竞争性抑制剂的发现,其制备及其药物组合物。 此外,本发明还涉及这些化合物和组合物在体外作为抗凝剂和体内作为治疗和预防血栓形成疾病例如静脉血栓形成,肺栓塞和动脉血栓形成作为导致急性缺血事件如心肌梗死的药物的用途 或脑梗塞。 此外,这些化合物和组合物具有治疗用途,用于预防和治疗与冠状动脉旁路手术相关的凝血病以及经腔血管成形术后的再狭窄事件。