WILFRIED HORNBERGER,CHARLES W. HUTCHINS,ANDREAS KLING,ACHIM MOELLER,HELMUT MACK,KATJA JANTOS
申请号：
MX2011011764
公开号：
MX2011011764A
申请日:
2010.05.06
申请国别(地区):
MX
年份:
2012
代理人:
摘要：
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 R<；sup>；1<；/sup>；, R<；sup>；2<；/sup>；, R<；sup>；3a<；/sup>；, R<；sup>；3b<；/sup>；, R<；sup>；4<；/sup>；, 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 R<；sup>；1<；/sup>；, r, R<；sup>；2b<；/sup>；, R<；sup>；3a<；/sup>；, R<；sup>；3b<；/sup>；, R<；sup>；4<；/sup>；, 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 CH<；sub>；2<；/sub>；-CH<；sub>；2<；/sub>；, CH<；sub>；2<；/sub>；-CH<；sub>；2<；/sub>；-CH<；sub>；2<；/sub>；, N(R<；sup>；y#<；/sup>；)-CH2, N(R<；sup>；y#<；/sup>；)-CH<；sub>；2<；/sub>；-CH<；sub>；2<；/sub>； or CH=CH-CH=, each optionally having 1 or 2 H-atoms replaced with identical or different radicals R<；sup>；y<；/sup>；, wherein R<；sup>；y <；/sup>；and R<；sup>；y#<；/sup>； have the meanings mentioned in the claims.La presente invención se refiere a compuestos de carboxamida novedosos y su uso para la fabricación de un medicamento. Los compuestos de carboxamida son inhibidores de calpaína (cisteína proteasas dependientes de calcio). Por lo tanto, la invención también se refiere al uso de dichos compuestos de carboxamida para tratar un trastorno asociado con una alta actividad de calpaína. Los co
