Carboxamide compounds and their use as calpain inhibitors

C - Chemistry – Metallurgy – 07 – D

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C07D 401/04 (2006.01) A61K 31/4439 (2006.01) A61P 25/00 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 493/04 (2006.01)

Patent

CA 2673580

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3a, R3b, W, Y and X have the meanings mentioned in the claims and 15 the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a' and I-A.a'' in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.

La présente invention porte sur de nouveaux composés de type carboxamide et sur leur utilisation pour la fabrication d'un médicament. Les composés de type carboxamide sont des inhibiteurs des calpaïnes (cystéine protéases dépendantes du calcium). L'invention porte donc également sur l'utilisation de ces composés de type carboxamide pour le traitement d'un trouble associé à une activité élevée des calpaïnes. Les composés de type carboxamide sont des composés de la formule générale (I), dans laquelle R1, R2, R3a, R3b, W, Y et X ont les significations mentionnées dans les revendications et dans la description ; leurs tautomères et leurs sels appropriés du point de vue pharmaceutique. En particulier, les composés ont la formule générale I-A.a' et I-A.a'', où m, E, R1, R3a, R3b, R2, Ry Rw et Rw6* ont les significations mentionnées dans les revendications, n est 0, 1 ou 2, leurs tautomères et leurs sels appropriés du point de vue pharmaceutique.

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