- THIAZOLE DERIVATIVES FOR THE TREATMENT OF ANIMAL TRYPANOSOMIASIS
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The present invention relates to a novel class of compounds of general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, X and Y are as defined herein, to their use in human and veterinary medicine, and in the treatment of animal trypanosomiasis in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
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Page/Page column 67
(2016/10/04)
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- Mandelic acid derivatives and their use as throbin inhibitors
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There is provided a compound of formula I wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
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Page/Page column 47
(2008/06/13)
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- A fluorine scan of the phenylamidinium needle of tricyclic thrombin inhibitors: Effects of fluorine substitution on pKa and binding affinity and evidence for intermolecular C-F...CN interactions
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The H-atoms of the phenylamidinium needle of tricyclic thrombin inhibitors, which interacts with Asp189 at the bottom of the selectivity pocket S1 of the enzyme, were systematically exchanged with F-atoms in an attempt to improve the pharmacokinetic prope
- Olsen, Jacob,Seiler, Paul,Wagner, Bjoern,Fischer, Holger,Tschopp, Thomas,Obst-Sander, Ulrike,Banner, David W.,Kansy, Manfred,Mueller, Klaus,Diederich, Francois
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p. 1339 - 1352
(2007/10/03)
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