Orally active fibrinogen receptor antagonists. 2. Amidoximes as prodrugs of amidines

…, P Hadváry, M Hürzeler Müller, D Knopp…

文献索引：Alig; Edenhofer; Hadvary; Hurzeler; Knopp; Muller; Steiner; Trzeciak; Weller Journal of Medicinal Chemistry, 1992 , vol. 35, # 23 p. 4393 - 4407

全文：HTML全文

被引用次数: 138

摘要

The potent and selective GP IIb-IIIa antagonist lamifiban (1, Ro 44-9883) is currently in clinical development as an injectable antithrombotic agent for treating and preventing acute coronary syndromes. However, for secondary prevention of thrombotic occlusions, orally active inhibitors are needed. By means of a prodrug strategy, the modest oral absorption of 1 in mice was improved by a factor of 9. In addition, these studies demonstrated that an ...