Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors |
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| Authors: | Tomczuk Bruce Lu Tianbao Soll Richard M Fedde Cynthia Wang Aihua Murphy Larry Crysler Carl Dasgupta Malini Eisennagel Stephen Spurlino John Bone Roger |
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| Institution: | 3-Dimensional Pharmaceuticals, Inc., 665 Stockton Drive, Exton, PA 19341, USA. bruce.tomczuk@3dp.com |
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| Abstract: | Although thrombin has been extensively researched with many examples of potent and selective inhibitors, the key characteristics of oral bioavailability and long half-life have been elusive. We report here a novel series non-peptidic phenyl-based, highly potent, highly selective and orally bioavailable thrombin inhibitors using oxyguanidines as guanidine-mimetics. |
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