Disubstituted bicyclic heterocycles, the preparation thereof...

Details Disubstituted bicyclic heterocycles, the preparation thereof... Disubstituted bicyclic heterocycles, the preparation thereof...

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) A61K 31/4709 (2006.01) A61P 9/10 (2006.01)

Patent

CA 2337825

The present invention relates to disubstituted bicyclic heterocycles of general formula R a - Het- B- Ar - E ,(I) wherein R a, Ar, B, Het and E are defined as in claim 1, the tautomers, stereoisomers, the mixtures thereof, the salts thereof and their preparation, as well as that of the pharmaceutical com- positions containing the pharmacologically active compounds, and their use. The compounds of the above general formula I wherein E denotes a cyano group are valuable intermediates for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein E denotes a R b NH-C(=NH) group have valuable pharmacological properties, particularly a throm- bin-inhibiting action and the effect of prolonging the thrombin time.

L'invention concerne des hétérocycles bicycliques disubstitués de formule générale (I): Ra - Het - B - Ar - E, dans laquelle Ra, Ar, B, Het et E sont tels que définis dans la revendication 1, ainsi que leurs tautomères, leurs stéréoisomères, leurs mélanges et leurs sels. L'invention concerne en outre la fabrication de ces composés, ainsi que des médicaments renfermant lesdits composés pharmacologiquement efficaces et leur utilisation. Les composés de la formule (I), dans laquelle E représente un groupe cyano, constituent des produits intermédiaires précieux pour la fabrication des autres composés de formule générale (I), et les composés de la formule précitée (I) dans laquelle E désigne un groupe RbNH-C(=NH) présentent des propriétés pharmacologiques précieuses, en particulier, un effet inhibiteur de la thrombine et de prolongement du temps de thrombine.

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