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COMPOSÉS CARBOXAMIDES ET LEUR UTILISATION COMME INHIBITEURS DE CALPAÏNE V
专利权人:
ABBVIE INC.;ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人:
KLING, Andreas,JANTOS, Katja,MACK, Helmut,MÖLLER, Achim,HORNBERGER, Wilfried,BACKFISCH, Gisela,LAO, Yanbin,NIJSEN, Marjoleen
申请号:
EPEP2013/055291
公开号:
WO2013/149800A1
申请日:
2013.03.14
申请国别(地区):
EP
年份:
2013
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 R1, R2 and n have the meanings mentioned in the claims and the description, Y is a radical of the formulae (Y1) or (Y2) where # indicates the point of attachment of Y to the pyridine ring, R3, R4, R5, Ry and m have the meanings mentioned in the claims and the description, A is is (CH2)p with p being 1, 2, 3 or 4, where one or two hydrogen atoms may be replaced by a radical R6, where A is attached to the 3-or 4-positon of the pyrazole radical and R6 has the meaning mentioned in the claims and the description; A1 is (CH2)q with q being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C1-C4-alkyl; and A2 is (CH2)r with r being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C1-C4-alkyl, provided that that r + q is 2, 3, 4, 5 or 6; their tautomers, the hydrates thereof, the pharmaceutically suitable salts of the carbox-amide compounds (I), the prodrugs of (I) and the pharmaceutically suitable salts of the prodrugs, tautomers or hydrates of (I).La présente invention concerne des nouveaux composés carboxamides et leur utilisation pour la fabrication d'un médicament. Les composés carboxamides sont des inhibiteurs de calpaïne (cystéine protéases dépendant du calcium). L'invention concerne donc aussi l'utilisation de ces composés carboxamides pour le traitement d'un trouble associé avec une activité élevée de calpaïne. Les composés carboxamides sont des composés de formule générale (I) dans laquelle R1, R2 et n ont les significations mentionnées dans les revendications et dans la description, Y est u
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