MOLLER ACHIM,NIJSEN MARJOLEEN,LAO YANBIN,BACKFISCH GISELA,HORNBERGER WILFRIED,JANTOS KATJA,KLING ANDREAS,MACK HELMUT
申请号：
NZ60034210
公开号：
NZ600342A
申请日:
2010.12.21
申请国别(地区):
NZ
年份:
2013
代理人:
摘要：
600342 Provided are carboxamide compounds of the general formula (I), where R1, R2, R3 R4, R5, m and n are as described in the specification. Preferred compounds are those where R1 is an optionally substituted phenyl-C1-C2-alkyl or hetaryl-C1-C2-alkyl, R2 is an 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. The compounds are inhibitors of calpain (calcium dependant cysteine proteases). Further provided is the use of the compounds for treating disorders associated with elevated calpain activity such as ischemias of the heart, the kidney, the lung, the liver or the central nervous system, muscular dystrophies, cataracts of the eyes, diabetes, HIV disorders, neurodegenerative diseases, multiple sclerosis and infectious diseases.
