Benzimidazoles, the preparation thereof and their use as...

C - Chemistry – Metallurgy – 07 – D

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C07D 403/06 (2006.01) A61K 31/4184 (2006.01) A61K 31/4439 (2006.01) A61P 7/02 (2006.01) C07D 401/12 (2006.01) C07D 403/08 (2006.01) C07D 235/14 (2006.01)

Patent

CA 2337804

The invention relates to novel benzimidazoles of general formula (1), wherein R a to R c, A, Ar and B have the meanings given in Claim 1, to tautomers, stereoisomers, mixtures and pro-drugs thereof, derivatives thereof containing a group which is negatively charged under physiological conditions in place of a carboxy group, and salts thereof, especially their physiologically compatible salts with inorganic or organic acids or bases with useful properties. The compounds of general formula (I) above wherein R c represents a cyano group are useful intermediate products for the production of the other compounds of general formula (I) and the compounds of general formula (I) wherein R c represents one of the amidino groups cited in Claim I have useful pharmacological properties, especially an antithrombotic effect.

La présente invention concerne de nouveaux benzimidazoles de la formule générale (I) dans laquelle Ra à Rc, A, AR et B sont tels que définis dans la revendication 1, leurs tautomères, leurs stéréoisomères, leurs mélanges, leurs promédicaments, leurs dérivés, qui contiennent à la place d'un groupe carboxy un groupe chargé négativement dans des conditions physiologiques, et leurs sels, notamment leurs sels physiologiquement tolérables avec des acides ou des bases inorganiques ou organiques, lesquels composés présentent des caractéristiques précieuses. Les composés de la formule générale (I) précitée, dans lesquels Rc représente un groupe cyano, constituent des produits intermédiaires précieux pour la préparation des composés restants de la formule générale (I), et les composés de la formule générale (I) précitée dans lesquels Rc représente un des groupes amidino mentionnés dans la revendication 1, présentent de précieuses caractéristiques pharmacologiques, notamment un effet anti-thrombotique.

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