Carboxamide compounds and their use as calpain inhibitors
    53.
    发明授权
    Carboxamide compounds and their use as calpain inhibitors 有权
    羧酰胺化合物及其作为钙蛋白酶抑制剂的用途

    公开(公告)号:US08436034B2

    公开(公告)日:2013-05-07

    申请号:US11990652

    申请日:2007-12-28

    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, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a′ and I-A.a″ in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.

    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R1,R2,R3a,R3b,W,Y和X具有权利要求书和说明书中所述的含义,其互变异构体及其药学上合适的盐。 特别地,化合物具有通式IA.a'和IA.a“,其中m,E,R1,R3a,R3b,R2,Ry,Rw和Rw6 *具有权利要求中提及的含义,n为0 ,1或2,其互变异构体及其药学上合适的盐。

    Carboxamide compounds and their use as calpain inhibitors
    54.
    发明授权
    Carboxamide compounds and their use as calpain inhibitors 有权
    羧酰胺化合物及其作为钙蛋白酶抑制剂的用途

    公开(公告)号:US07799809B2

    公开(公告)日:2010-09-21

    申请号:US12072065

    申请日:2008-02-22

    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, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a′ and I-A.a″ in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.

    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R1,R2,R3a,R3b,W,Y和X具有权利要求书和说明书中所述的含义,其互变异构体及其药学上合适的盐。 特别地,化合物具有通式IA.a'和IA.a“,其中m,E,R1,R3a,R3b,R2,Ry,Rw和Rw6 *具有权利要求中提及的含义,n为0, 1或2,其互变异构体及其药学上合适的盐。

    Carboxamide compounds and their use as calpain inhibitors
    55.
    发明申请
    Carboxamide compounds and their use as calpain inhibitors 有权
    羧酰胺化合物及其作为钙蛋白酶抑制剂的用途

    公开(公告)号:US20080234329A1

    公开(公告)日:2008-09-25

    申请号:US12070941

    申请日:2008-02-22

    IPC分类号: A61K31/4439 C07D401/00

    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, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a′ and I-A.a″ in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.

    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 3,R 3, >,W,Y和X具有权利要求书和说明书中所述的含义,其互变异构体及其药学上合适的盐。 特别地,化合物具有通式IA.a'和IA.a“,其中m,E,R 1,R 3a,R 3b, R 2,R 2,R 2,W 2和R 6具有如下的含义: 权利要求书,n为0,1或2,其互变异构体及其药学上合适的盐。