Conjugates of thrombin inhibitors and endogenes carriers

Details Conjugates of thrombin inhibitors and endogenes carriers Conjugates of thrombin inhibitors and endogenes carriers

C - Chemistry, Metallurgy

07

D

C07D 401/14 (2006.01) A61K 31/47 (2006.01) A61K 31/675 (2006.01) A61K 47/48 (2006.01) C07D 401/12 (2006.01) C07F 9/6558 (2006.01)

Patent

CA 2258516

Novel compounds comprising chemically reactive intermediates which can react with available reactive functionalities on blood components to form covalent linkages, where the resulting covalently-bound conjugates are found to have thrombin inhibition activity are provided. Specifically, the thrombin inhibitor compounds of the present invention are derivatives of the known thrombin inhibitor argatroban, which can be covalently linked to chemically reactive functionalities on various blood components. The conjugated thrombin inhibitors thereby have extended lifetimes in the blood stream, as compared to the unconjugated parent drug, and are, therefore, capable of maintaining thrombin inhibitory activity for extended periods to time as compared to the unconjugated parent drug. Also provided herein are methods for inhibiting thrombin activity in vivo comprising administering to the bloodstream of a mammalian host the novel compounds of the present invention.

La présente invention concerne des composés comprenant des intermédiaires chimiquement réactifs, capables de réagir avec des fonctionnalités réactives existantes pour former des liaisons covalentes sur des composants sanguins, les conjugués obtenus par ces liaisons covalentes faisant preuve d'une activité inhibitrice de la thrombine. En particulier, les composés inhibiteurs de la thrombine de l'invention, qui sont des dérivés de l'argatroban déjà connu comme inhibiteur de la thrombine, sont capables de se lier sur divers composants sanguins par covalence avec des fonctionnalités chimiquement réactives. Il en découle que les inhibiteurs conjugués de la thrombine présentent des durées de vie dans la circulation sanguine plus longues que celles du médicament mère non conjugué, d'où la possibilité de conserver une activité inhibitrice de la thrombine de plus longue durée que dans le cas du médicament mère non conjugué. L'invention concerne également des procédés d'inhibition in vivo de l'activité de la thrombine consistant en l'administration dans la circulation sanguine d'un mammifère hôte des composés de la présente invention.

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