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    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V
    1.
    发明授权
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V 有权
    CARBOXAMIDVERBINDUNGEN UND IHRE VERWENDUNG ALS CALPAIN-HEMMER V

    公开(公告)号：EP2648731B1

    公开(公告)日：2017-01-25

    申请号：EP11796664.8

    申请日：2011-12-08

    申请人： Abbvie Deutschland GmbH & Co. KG ,  AbbVie Inc.

    发明人： KLING, Andreas ,  JANTOS, Katja ,  MACK, Helmut ,  MÖLLER, Achim ,  HORNBERGER, Wilfried ,  LAO, Yanbin ,  BACKFISCH, Gisela ,  NIJSEN, Marjoleen

    IPC分类号： A61K31/4439 ,  C07D401/04 ,  A61P25/28

    CPC分类号： C07D401/04 ,  A61K31/4439 ,  C07D401/14 ,  Y02A50/411

    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, X, 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 benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R2 is C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or CH2—C(O)OCH3, R3 and R4 independently of one another are halogen, CN, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.

    摘要翻译： 本发明涉及新的羧酰胺化合物及其用于制备药物的用途。 羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。 因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。 羧酰胺化合物是通式（I）的化合物，其中R 1，R 2，R 3，R 4，X，m和n具有权利要求书和说明书中所述的含义，其互变异构体，其水合物和药学上合适的盐 它们。 在这些化合物中，优选其中R 1为任选取代的苄基或杂芳基 - 甲基，X为单键或氧原子，R 2为C 1 -C 4烷基，C 1 -C 4卤代烷基，C 2 -C 4 - 烯基，C 3 -C 6 环烷基，C 3 -C 6 - 环烷基-C 1 -C 2 - 烷基，C 3 -C 6 - 杂环烷基-C 1 -C 2烷基，苯基，苯基-C 1 -C 3烷基，吡啶-2-基-C 1 -C 3 - 烷基或CH 2 -C（O）OCH 3，R 3和R 4彼此独立地是卤素，CN，CF 3，CHF 2，CH 2 F，C 1 -C 2烷基或C 1 -C 2烷氧基，m和n彼此独立地为0或1。

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V
    4.
    发明公开
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V 有权
    甲酰胺化合物和它们作为钙蛋白酶抑制剂V选用

    公开(公告)号：EP2648731A1

    公开(公告)日：2013-10-16

    申请号：EP11796664.8

    申请日：2011-12-08

    申请人： Abbvie Deutschland GmbH & Co. KG ,  AbbVie Inc.

    发明人： KLING, Andreas ,  JANTOS, Katja ,  MACK, Helmut ,  MÖLLER, Achim ,  HORNBERGER, Wilfried ,  LAO, Yanbin ,  BACKFISCH, Gisela ,  NIJSEN, Marjoleen

    IPC分类号： A61K31/4439 ,  C07D401/04 ,  A61P25/28

    CPC分类号： C07D401/04 ,  A61K31/4439 ,  C07D401/14 ,  Y02A50/411

    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, X, 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 benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R2 is C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or CH2—C(O)OCH3, R3 and R4 independently of one another are halogen, CN, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.