- Synthesis and antiplatelet effects of an isoxazole series of glycoprotein IIb/IIIa antagonists
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Despite the excellent in vitro potency of a series of benzamide glycoprotein IIb/IIIa antagonists, which have been reported previously, poor in vivo potency in the inhibition of platelet aggregation was observed when the most potent inhibitor XU057 was dosed intravenously to dogs. In this communication, we report that replacement of the benzamide in XU057 with an isoxazolecarboxamide resulted in significant improvement in in vivo potency. More importantly, the analogue XU065 showed an excellent oral antiplatelet effect in dogs.
- Xue, Chu-Biao,Roderick, John,Mousa, Shaker,Olson, Richard E.,DeGrado, William F.
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- Aromatic compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
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This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
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