发明名称 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V
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.
申请公布号 US2011152265(A1) 申请公布日期 2011.06.23
申请号 US20100972663 申请日期 2010.12.20
申请人 ABBOTT GMBH & CO. KG;ABBOTT LABORATORIES 发明人 KLING ANDREAS;JANTOS KATJA;MACK HELMUT;MOELLER ACHIM;HORNBERGER WILFRIED;BACKFISCH GISELA;LAO YANBIN;NIJSEN MARJOLEEN
分类号 A61K31/5355;A61K31/4439;A61P9/00;A61P13/12;A61P25/08;A61P25/16;A61P25/28;A61P31/18;A61P33/06;C07D401/04;C07D413/14 主分类号 A61K31/5355
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