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    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V
    4.
    发明申请
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V 审中-公开
    羧酰胺化合物及其作为钙抑制剂V

    公开(公告)号：US20150252017A1

    公开(公告)日：2015-09-10

    申请号：US14717787

    申请日：2015-05-20

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

    发明人： Andreas Kling ,  Katja Jantos ,  Helmut Mack ,  Achim Möller ,  Wilfried Hornberger ,  Gisela Backfisch ,  Yanbin Lao ,  Marjoleen Nijsen

    IPC分类号： C07D401/04

    CPC分类号： C07D401/04 ,  C07D207/28 ,  C07D401/14 ,  C07D409/14 ,  C07D417/14

    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.

    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，R 5，m和n具有权利要求书和描述中所述的含义，其互变异构体，其水合物及其药学上合适的盐。 在这些化合物中，优选其中R 1为任选取代的苯基-C 1 -C 2 - 烷基或杂芳基-C 1 -C 2烷基，R 2为任选取代的芳基，杂芳基，芳基-C 1 -C 6 - 烷基，芳基-C 2 -C 6 - 烯基 或杂芳基-C 1 -C 4 - 烷基，R 3是C 1 -C 3 - 烷基，C 1 -C 3 - 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烷基或苯基 - C 1 -C 3 - 烷基，R 4和R 5彼此独立地是卤素，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
    5.
    发明申请
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V 有权
    羧酰胺化合物及其作为钙抑制剂V

    公开(公告)号：US20150065477A1

    公开(公告)日：2015-03-05

    申请号：US14390381

    申请日：2013-03-14

    申请人： ABBVIE DEUTSCHLAND GMBH &CO. KG ,  ABBVIE INC.

    发明人： Andreas Kling ,  Katja Jantos ,  Helmut Mack ,  Achim Möller ,  Wilfried Hornberger ,  Gisela Backfisch ,  Yanbin Lao ,  Marjoleen Nijsen

    IPC分类号： C07D401/14 ,  C07D491/107 ,  C07D413/14 ,  C07D491/048 ,  C07D401/04 ,  C07D471/04

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/107

    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 and n have the meanings mentioned in the claims and the description, Y is a radical of the formulae (Y1) or (Y2) where # indicates the point of attachment of Y to the pyridine ring, R3, R4, R5, Ry and m have the meanings mentioned in the claims and the description, A is (CH2)p with p being 1, 2, 3 or 4, where one or two hydrogen atoms may be replaced by a radical R6, where A is attached to the 3- or 4-position of the pyrazole radical and R6 has the meaning mentioned in the claims and the description; A1 is (CH2)q with q being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C1-C4-alkyl; and A2 is (CH2)r with r being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C1-C4-alkyl, provided that that r+q is 2, 3, 4, 5 or 6; their tautomers, the hydrates thereof, the pharmaceutically suitable salts of the carbox-amide compounds (I), the prodrugs of (I) and the pharmaceutically suitable salts of the prodrugs, tautomers or hydrates of (I).

    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和n具有权利要求书和描述中所述的含义，Y是式（Y1）或（Y2）的基团，其中＃表示 Y连接到吡啶环，R3，R4，R5，Ry和m具有权利要求书和说明书中所述的含义，A是（CH 2）p，其中p是1,2,3或4，其中一个或两个氢 原子可以被基团R6代替，其中A连接到吡唑基团的3-或4-位，R6具有权利要求书和说明书中提及的含义; A 1是（CH 2）q，其中q是0,1,2或3，其中一个或两个氢原子可以被卤素或C 1 -C 4 - 烷基取代; 并且A 2为（CH 2）r，其中r为0,1,2或3，其中一个或两个氢原子可被卤素或C 1 -C 4 - 烷基取代，条件是该r + q为2,3,4,5 或6; 其互变异构体，其水合物，羧酰胺化合物（I）的药学上合适的盐，（I）的前药和（I）的前药，互变异构体或水合物的药学上合适的盐。

    Carboxamide compounds and their use as calpain inhibitors V
    9.
    发明授权
    Carboxamide compounds and their use as calpain inhibitors V 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：US09150545B2

    公开(公告)日：2015-10-06

    申请号：US14390381

    申请日：2013-03-14

    申请人： ABBVIE DEUTSCHLAND GMBH & CO. KG ,  ABBVIE INC.

    发明人： Andreas Kling ,  Katja Jantos ,  Helmut Mack ,  Achim Möller ,  Wilfried Hornberger ,  Gisela Backfisch ,  Yanbin Lao ,  Marjoleen Nijsen

    IPC分类号： A61K31/44 ,  C07D221/18 ,  C07D401/00 ,  C07D401/14 ,  C07D405/14 ,  C07D401/04 ,  C07D471/04 ,  C07D487/04 ,  C07D413/14 ,  C07D491/048 ,  C07D491/107

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/107

    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 and n have the meanings mentioned in the claims and the description, Y is a radical of the formulae (Y1) or (Y2) where # indicates the point of attachment of Y to the pyridine ring, R3, R4, R5, Ry and m have the meanings mentioned in the claims and the description, A is (CH2)p with p being 1, 2, 3 or 4, where one or two hydrogen atoms may be replaced by a radical R6, where A is attached to the 3- or 4-position of the pyrazole radical and R6 has the meaning mentioned in the claims and the description; A1 is (CH2)q with q being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C1-C4-alkyl; and A2 is (CH2)r with r being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C1-C4-alkyl, provided that that r+q is 2, 3, 4, 5 or 6; their tautomers, the hydrates thereof, the pharmaceutically suitable salts of the carbox-amide compounds (I), the prodrugs of (I) and the pharmaceutically suitable salts of the prodrugs, tautomers or hydrates of (I).

    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和n具有权利要求书和描述中所述的含义，Y是式（Y1）或（Y2）的基团，其中＃表示 Y连接到吡啶环，R3，R4，R5，Ry和m具有权利要求书和说明书中所述的含义，A是（CH 2）p，其中p是1,2,3或4，其中一个或两个氢 原子可以被基团R6代替，其中A连接到吡唑基团的3-或4-位，R6具有权利要求书和说明书中提及的含义; A 1是（CH 2）q，其中q是0,1,2或3，其中一个或两个氢原子可以被卤素或C 1 -C 4 - 烷基取代; 并且A 2为（CH 2）r，其中r为0,1,2或3，其中一个或两个氢原子可被卤素或C 1 -C 4 - 烷基取代，条件是该r + q为2,3,4,5 或6; 其互变异构体，其水合物，羧酰胺化合物（I）的药学上合适的盐，（I）的前药和（I）的前药，互变异构体或水合物的药学上合适的盐。