Disubstituted bicyclic heterocycles, the preparation and the...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 277/64 (2006.01) A61K 31/425 (2006.01) C07D 209/14 (2006.01) C07D 235/06 (2006.01) C07D 235/12 (2006.01) C07D 235/14 (2006.01) C07D 235/16 (2006.01) C07D 235/28 (2006.01) C07D 241/44 (2006.01) C07D 277/74 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 409/06 (2006.01) C07D 417/12 (2006.01) C07D 471/04 (2006.01) C07D 495/04 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2277949

The invention relates to new disubstituted bicyclic heterocycles of the general formula (I): R a-A-Het-B-Ar-E, in which A, B, Ar, Het and R a are defined as in claim 1. The invention also relates to their tautomers, their stereoisomers, their mixtures, and their salts, which have valuable properties. The compounds of the above general formula (I), in which E is a cyano group, thus represent valuable intermediate products for the production of the other compounds of the general formula (I). Furthermore, the compounds of the above general formula (I), in which E stands for a R b NH-C(=NH)-group, have valuable pharmacological properties, in particular in inhibiting thrombin and prolonging thrombin time.

L'invention concerne de nouveaux hétérocycles bicycliques disubstitués de la formule générale (I): Ra-A-Het-B-Ar-E, où A, B, Ar, Het et Ra sont décrits dans la revendication 1. Elle concerne aussi leurs tautomères, stéréo-isomères, mélanges et sels, qui ont des propriétés utiles. Les composés de la formule générale ci-dessus (I), où E est un groupe cyano, représentent donc des produits intermédiaires utiles pour la production des autres composés de la formule générale (I). Par ailleurs, les composés de la formule générale (I), où E représente un groupe RbNH-C(=NH), ont de précieuses vertus pharmaceutiques et peuvent notamment inhiber la thrombine et prolonger le temps de thrombine.

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