Ortho-substituted benzoylguanidines, process for their...

C - Chemistry – Metallurgy – 07 – C

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C07C 317/32 (2006.01) A61K 31/155 (2006.01) A61K 31/16 (2006.01) A61K 31/275 (2006.01) A61K 31/395 (2006.01) A61K 49/00 (2006.01) C07C 311/47 (2006.01) C07C 323/44 (2006.01) C07D 295/26 (2006.01)

Patent

CA 2207886

Ortho-substituted benzoylguanidines a process for their preparation, their use as a medicament or diagnostic agent and a medicament comprising them. Benzoylguanidines of the formula I (see fig. I) in which: R(1) to R(4) have the meanings given in the claims, are antiarrhythmicpharmaceuticals having a cardioprotective component, which are also valuable forthe prevention of ischemically induced damage in particular in association with the triggering of ischemically induced cardiac arrhythmias. As a consequence of inhibiting the cellular Na+/H+ exchange mechanism they are used for treating acute or chronic damage triggered by ischemia. In addition to this they are notable for their strong inhibitory effect on the proliferation of cells. They are suitable for preventing the genesis of high blood pressure.

Benzoylguanidines ortho-substituées, procédé de préparation, leur utilisation comme médicament ou produit diagnostique, et médicament contenant ces composés. Les benzoylguanidines ortho-substituées de formule I (voir fig. I) où R(1) à R(4) ont les significations données dans les revendications et sont des produits pharmaceutiques antiarythmisants ayant un constituant cardioprotecteur; elles sont également utiles pour la prévention des lésions induites par l'ischémie, en particulier le déclenchement des arythmies cardiaques induites par l'ischémie. Du fait qu'elles inhibent le mécanisme d'échange du Na+/H+ cellulaire, elles sont utilisées pour traiter les lésions aiguës ou chroniques provoquées par l'ischémie. De plus, elles sont remarquables par leur effet inhibiteur puissant sur la prolifération cellulaire. Elles conviennent pour prévenir l'apparition de l'hypertension artérielle.

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