Prodrugs of thrombin inhibitors

Details Prodrugs of thrombin inhibitors Prodrugs of thrombin inhibitors

C - Chemistry, Metallurgy

07

K

C07K 5/02 (2006.01) A61K 38/05 (2006.01) A61P 7/02 (2006.01) C07B 43/00 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2370267

The invention relates to prodrugs of pharmacologically active, five-membered heterocyclic amidines from which in vivo compounds are obtained, these compounds being competitive inhibitors of trypsin-type serin proteases, especially thrombin and kininogenases such as kallikrein. The invention also relates to the production of these prodrugs and to their use as medicaments, to pharmaceutical compositions that contain the prodrugs of the active compounds as components, and to the use of the compounds as thrombin inhibitors, anticoagulants and anti-inflammatory agents.

L'invention concerne des promédicaments d'amidines hétérocycliques à 5 éléments possédant une activité pharmacologique, à partir desquels sont générés in vivo des composés qui sont des inhibiteurs compétitifs des sérine-protéases de type trypsine, notamment la thrombine et des kininogénases telles que la kallikréine; ainsi que leur production et leur utilisation comme médicaments. L'invention concerne également des compositions pharmaceutiques contenant les promédicaments des composés actifs, ainsi que l'utilisation desdits composés comme inhibiteurs de la thrombine, anticoagulants et anti-inflammatoires.

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