CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
    7.
    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:US20150045394A1

    公开(公告)日:2015-02-12

    申请号:US14522454

    申请日:2014-10-23

    摘要: The present invention relates to novel carboxamide compounds and their use as 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 and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds.The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y1, Y2, Y3 and Y4 are CRy, or one or two of the variables Y1 to Y4 are a nitrogen atom and the remaining variables are CRy, wherein the radicals Ry may be identical or different and have the meanings mentioned in the claims.

    摘要翻译: 本发明涉及新的羧酰胺化合物及其作为药物的用途。 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钙蛋白酶活性升高相关的疾病的用途,以及通过施用有效量的这些羧酰胺化合物中的至少一种来进行治疗和/或预防性治疗的方法。 羧酰胺化合物是其中W-R2选自并且R 1,R 2,R 3a,R 3b,Y 1,Y 2,Y 3,Y 4,X,Q,m,k,Rw和Rw *具有通式I的化合物 权利要求中提及的其互变异构体及其药学上合适的盐。 在这些化合物中,优选其中Y1,Y2,Y3和Y4为CRy,或变量Y1至Y4中的一个或两个为氮原子,剩余的变量为CRy,其中基团Ry可以相同或不同,并且具有 权利要求中提及的含义。

    Carboxamide compounds and their use as calpain inhibitors
    10.
    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:US09567325B2

    公开(公告)日:2017-02-14

    申请号:US14522454

    申请日:2014-10-23

    摘要: The present invention relates to novel carboxamide compounds and their use as 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 and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds.The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y1, Y2, Y3 and Y4 are CRy, or one or two of the variables Y1 to Y4 are a nitrogen atom and the remaining variables are CRy, wherein the radicals Ry may be identical or different and have the meanings mentioned in the claims.

    摘要翻译: 本发明涉及新的羧酰胺化合物及其作为药物的用途。 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钙蛋白酶活性升高相关的疾病的用途,以及通过施用有效量的这些羧酰胺化合物中的至少一种来进行治疗和/或预防性治疗的方法。 羧酰胺化合物是其中W-R2选自并且R 1,R 2,R 3a,R 3b,Y 1,Y 2,Y 3,Y 4,X,Q,m,k,Rw和Rw *具有通式I的化合物 权利要求中提及的其互变异构体及其药学上合适的盐。 在这些化合物中,优选其中Y1,Y2,Y3和Y4为CRy,或变量Y1至Y4中的一个或两个为氮原子,剩余的变量为CRy,其中基团Ry可以相同或不同,并且具有 意思是在权利要求中提及。