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

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

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

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Citation Number: 138

Abstract

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 ...