| 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. |
| 主权项 |
1. A carboxamide compound of the formula I in which R1 is benzyl, which may be unsubstituted or carry 1 or 2 identical or different radicals selected from the group consisting of halogen, C1-C2-alkyl, and C1-C2-alkoxy; R2 is selected from the group consisting of aryl, aryl-C1-C6-alkyl, and aryl-C2-C6-alkenyl, where aryl in the last 3 radicals mentioned may be unsubstituted or carry 1, 2, 3, or 4 identical or different radicals R2c;
whereR2c is selected independently of one another from the group consisting of halogen, C1-C2-alkyl, where the alkyl may be partly or completely halogenated, C1-C2-alkoxy, and —(CH2)p—NRc6Rc7 with p=0, 1, or 2, where
Rc6 is selected from the group consisting of H and C1-C4-alkyl, andRc7 is selected from the group consisting of H and C1-C4-alkyl; R3 is selected from the group consisting of C1-C6-alkyl, C1-C3-haloalkyl, C3-C5-alkenyl, C3-C5-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C1-C2-alkoxy-C1-C2-alkyl, aryl, and aryl-C1-C3-alkyl;
R4 and R5 are selected independently of one another from the group consisting of halogen, NH2, CN, CF3, CHF2, CH2F, O—CF3, O—CHF2, O—CH2F, COOH, OCH2COOH, C1-C2-alkyl, C1-C2-alkoxy, C1-C2-alkoxy-C1-C2-alkyl, C1-C2-alkylthio, and CH2NRR′, whereR and R′ are selected independently of one another from the group consisting of hydrogen and C1-C4-alkyl; m is 0, 1, or 2; and n is 0, 1, or 2; or a tautomer thereof, or a pharmaceutically acceptable salt thereof. |
