| 摘要 |
<p>A novel bivalent serine protease inhibitor (I) of coagulation factor VIIa and factor Xa comprises: (i) a first serine protease inhibitor binding to factor VIIa; (ii) a linker moiety; and (iii) a second serine protease inhibitor binding to factor Xa. Also claimed are a method for inhibiting the two different serine proteases factor VIIa and factor Xa simultaneously and selectively when the two serine proteases becomes localised on the membrane protein tissue factor. The compounds and method are useful for prevention or treatment of FVIIa/TF-related diseases or disorders such as deep venous thrombosis, arterial thrombosis, post surgical thrombosis, coronary artery bypass graft (CABG), percutaneous transdermal coronary angioplastry (PTCA), stroke, tumour metastasis, inflammation, septic chock, hypotension, ARDS, pulmonary embolism, disseminated intravascular coagulation (DIC), vascular restenosis, platelet deposition, myocardial infarction, angiogenesis, or the prophylactic treatment of mammals with atherosclerotic vessels at risk for thrombosis.</p> |
