- AMIDINOHYDRAZONES AS PROTEASE INHIBITORS
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Amidino and benzamidino compounds, including compounds of the formula: I wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I.
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Page/Page column 50
(2010/11/23)
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- Amidinohydrazones as guanidine bioisosteres: Application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors
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We describe a new class of potent, non-amide-based small molecule thrombin inhibitors in which an amidinohydrazone is used as a guanidine bioisostere on a non-peptide scaffold. Compound 4 exhibits nM inhibition of thrombin, is selective for thrombin, and
- Soll, Richard M.,Lu, Tianobao,Tomczuk, Bruce,Illig, Carl R.,Fedde, Cynthia,Eisennagel, Stephen,Bone, Roger,Murphy, Larry,Spurlino, John,Salemme, F. Raymond
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- AMIDINOHYDRAZONES AS PROTEASE INHIBITORS
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Amidino and benzamidino compounds, including compounds of the formula: STR1 wherein R 1-R 4, R 6-R 9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I.
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