Carboxamide compounds and their use as calpain inhibitors

Details Carboxamide compounds and their use as calpain inhibitors Carboxamide compounds and their use as calpain inhibitors

C - Chemistry, Metallurgy

07

D

C07D 207/26 (2006.01) A61K 31/4412 (2006.01) C07D 211/76 (2006.01) C07D 233/34 (2006.01) C07D 239/10 (2006.01)

Patent

CA 2760464

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, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula (Ia) and (Ib) in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2-CH2, CH2-CH2-CH2, N(Ry#)-CH2, N(Ry#)-CH2-CH2 or CH=CH-CH=, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.

La présente invention a pour objet de nouveaux composés de carboxamide et leur utilisation pour la fabrication d'un médicament. Les composés de carboxamide sont des inhibiteurs de la calpaïne (cystéine protéases dépendantes du calcium). L'invention concerne également par conséquent l'utilisation de ces composés de carboxamide pour le traitement d'un trouble associé à une activité élevée de la calpaïne. Les composés de carboxamide sont des composés de la formule générale (I) dans laquelle R1, R2, R3a, R3b, R4, Q, Y, A et X ont les significations mentionnées dans les revendications et la description, leurs tautomères et leurs sels pharmaceutiquement acceptables. En particulier, les composés ont les formules générales (Ia) et (Ib) dans lesquelles R1, r, R2b, R3a, R3b, R4, Y et X ont les significations mentionnées dans les revendications, comprenant leurs tautomères et leurs sels pharmaceutiquement acceptables. Parmi ces composés, on préfère ceux dans lesquels Y est un groupement CH2-CH2, CH2-CH2-CH2, N(Ry#)-CH2, N(Ry#)-CH2-CH2 ou CH=CH-CH=, chacun ayant facultativement 1 ou 2 atomes d'hydrogène H remplacés par des radicaux Ry identiques ou différents, Ry et Ry# ayant les significations mentionnées dans les revendications.

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