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CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
专利权人:
ABBOTT LABORATORIES;ABBVIE DEUTSCHLAND GMBH & CO KG
发明人:
KLING ANDREAS,MACK HELMUT,HORNBERGER WILFRIED,LAO YANBIN,JANTOS KATJA,MOLLER ACHIM,BACKFISCH GISELA,NIJSEN MARJOLEEN
申请号:
ZA201204496
公开号:
ZA201204496B
申请日:
2012.06.18
申请国别(地区):
ZA
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, R3 R4, R5, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted phenyl-C1-C2-alkyl or hetaryl-C1-C2-alkyl, R2 is optionally substituted aryl, hetaryl, aryl-C1-C6-alkyl, aryl-C2-C6-alkenyl or hetaryl-C1-C4-alkyl, R3 is C1-C3-alkyl, C1-C3-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, or phenyl-C1-C3-alkyl, R4 and R5 independently of one another are halogen, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.
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