New mandelic acid derivatives and their use as thrombin...

Details New mandelic acid derivatives and their use as thrombin... New mandelic acid derivatives and their use as thrombin...

C - Chemistry, Metallurgy

07

D

C07D 205/04 (2006.01) A61K 31/397 (2006.01) A61K 31/401 (2006.01) A61K 31/4427 (2006.01) A61K 31/506 (2006.01) A61P 7/02 (2006.01) C07C 45/00 (2006.01) C07C 45/29 (2006.01) C07C 45/51 (2006.01) C07C 45/67 (2006.01) C07C 45/71 (2006.01) C07C 47/575 (2006.01) C07C 59/52 (2006.01) C07C 59/56 (2006.01) C07C 59/64 (2006.01) C07C 69/732 (2006.01) C07C 69/734 (2006.01) C07C 69/738 (2006.01) C07C 205/59 (2006.01) C07D 207/10 (2006.01) C07D 207/16 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01)

Patent

CA 2436220

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.

L'invention concerne des composés de formule (I), dans laquelle R?a¿, R?1¿, R?2¿, Y et R?3¿ sont tels que décrits dans le descriptif, ainsi que des dérivés (notamment des promédicaments) acceptables sur le plan pharmaceutique de ceux-ci. Ces composés et dérivés sont utilisés comme inhibiteurs compétitifs de protéases de type trypsine, tels que la thrombine, ou sont utilisés comme promédicaments de ceux-ci, et surtout utilisés, par conséquent, dans le traitement d'états pathologiques dans lesquels l'inhibition de la thrombine est nécessaire (par exemple la thrombose), ou comme agents anticoagulants.

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