Thrombin inhibiting 2-oxo-1, 2, 5, 6-tetrahydropyridine...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/12 (2006.01) A61K 31/4439 (2006.01) A61K 31/444 (2006.01) A61P 7/02 (2006.01) C07D 213/73 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2610428

There is provided a compound of formula (I) wherein R1, R2a, R2b, R3a, R3b, R4, R5a, R5b, R6 to R8, A and G have meanings given in the description, which compounds 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 beneficial (e.g. conditions, such as thrombo-embolisms, where inhibition of thrombin is required or desired, and/or conditions where anticoagulant therapy is indicated).

La présente invention a trait à un composé de formule (I), dans laquelle: R1, R2a, R2b, R3a, R3b, R4, R5a, R5b, R6 à R8, A et G sont tels que définis dans la description, lesdits composés étant utiles comme inhibiteurs compétitifs, ou leurs prodrogues, des protéases de type tripsyne, telles que la thrombine, et donc, en particulier, dans le traitement de conditions dans lesquelles l'inhibition de la thrombine est bénéfique (par exemple, des conditions telles que des thrombo-embolies, où l'inhibition de la thrombine est nécessaire ou souhaitée, et/ou des conditions où une thérapie d'anticoagulation est indiquée).

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