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    Carboxamide compounds and their use as calpain inhibitors
    3.
    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：US09018206B2

    公开(公告)日：2015-04-28

    申请号：US13610975

    申请日：2012-09-12

    申请人： Helmut Mack ,  Andreas Kling ,  Katja Jantos ,  Achim Moeller ,  Wilfried Hornberger ,  Charles W. Hutchins

    发明人： Helmut Mack ,  Andreas Kling ,  Katja Jantos ,  Achim Moeller ,  Wilfried Hornberger ,  Charles W. Hutchins

    IPC分类号： C07D211/76 ,  C07D233/34 ,  C07D239/10 ,  C07D207/22 ,  C07D211/78 ,  C07D233/32 ,  C07D275/03 ,  C07D401/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D207/26

    CPC分类号： C07D207/22 ,  C07D207/26 ,  C07D207/28 ,  C07D211/76 ,  C07D211/78 ,  C07D213/81 ,  C07D233/32 ,  C07D233/34 ,  C07D239/10 ,  C07D275/03 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    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, R4, Q, Y, A 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 Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2—CH2, CH2—CH2—CH2, N(Ry#)—CH2, N(Ry#)—CH2—CH2 or CH═CH—CH═, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# 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 3a，R 3b，R 4，Q，Y，A和X具有权利要求和说明书中所述的含义及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和Ib，其中R1，r，R2b，R3a，R3b，R4，Y和X具有权利要求中提及的含义，包括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Y为CH2-CH2，CH2-CH2-CH2，N（Ry＃）-CH2，N（Ry＃）-CH2-CH2或CH = CH-CH≡，各自任选具有1 或2个H原子被相同或不同的基团Ry取代，其中Ry和Ry＃具有权利要求中提及的含义。

    Substituted oxindole compounds
    9.
    发明授权
    Substituted oxindole compounds 有权
    取代的羟吲哚化合物

    公开(公告)号：US08486931B2

    公开(公告)日：2013-07-16

    申请号：US12529542

    申请日：2008-02-29

    申请人： Herve Genesle ,  Thorsten Oost ,  Charles W. Hutchins ,  Liliane Unger ,  Wilfried Hornberger ,  Wilfried Lubisch ,  Astrid Netz ,  Alfred Hahn

    发明人： Herve Genesle ,  Thorsten Oost ,  Charles W. Hutchins ,  Liliane Unger ,  Wilfried Hornberger ,  Wilfried Lubisch ,  Astrid Netz ,  Wolfgang Wernet

    IPC分类号： A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/551

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D401/12 ,  C07D471/08

    摘要： The present invention relates to compounds of the general formula (I) in which A, B, R1, R2 and Het have the meaning given in claim 1; Y is a bivalent group of the formula in which D is C1-C3-alkylene, where D may have a substituent R5; R3 is hydrogen, C1-C8-alkyl or together with R4 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, and R4 is hydrogen, C1-C8-alkyl or together with R3 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, where R5 together with R5a, where present, are a bond or C1-C3-alkylene; and where one of the following conditions is satisfied: R3 together with R4 is C1-C3-alkylene which may have a radical R5a; or R3 together with R5 is C1-C3-alkylene; or R4 together with R5 is C1-C3-alkylene where the radical A is different from phenyl when the radical B is phenyl or naphthyl; and medicaments which comprise such compounds and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.

    摘要翻译： 本发明涉及通式（I）的化合物，其中A，B，R1，R2和Het具有权利要求1中给出的含义; Y是下式的二价基团，其中D是C 1 -C 3 - 亚烷基，其中D可以具有取代基R 5; R 3是氢，C 1 -C 8烷基或与R 4一起是可以具有基团R 5a的C 1 -C 3亚烷基，或与R 5一起为C 1 -C 3 - 亚烷基，并且R 4是氢，C 1 -C 8 - 烷基或与 R 3是可以具有基团R 5a的C 1 -C 3亚烷基，或与R 5一起为C 1 -C 3 - 亚烷基，其中R 5与存在的R a a为键或C 1 -C 3 - 亚烷基; 并且其中满足以下条件之一：R 3与R 4一起可以具有基团R 5a的C 1 -C 3 - 亚烷基; 或R 3与R 5一起为C 1 -C 3 - 亚烷基; 或R 4与R 5一起为C 1 -C 3 - 亚烷基，其中基团B为苯基或萘基时，基团A不同于苯基; 以及包含这些化合物的药物及其用于预防和/或治疗加压素依赖性和/或催产素依赖性疾病的用途。

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
    10.
    发明申请
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
    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：US20130150367A1

    公开(公告)日：2013-06-13

    申请号：US13610975

    申请日：2012-09-12

    申请人： Helmut Mack ,  Andreas Kling ,  Katja Jantos ,  Achim Moeller ,  Wilfried Hornberger ,  Charles W. Hutchins

    发明人： Helmut Mack ,  Andreas Kling ,  Katja Jantos ,  Achim Moeller ,  Wilfried Hornberger ,  Charles W. Hutchins

    IPC分类号： C07D207/22 ,  C07D275/03 ,  C07D409/12 ,  C07D401/06 ,  C07D417/12 ,  C07D405/12 ,  C07D211/78 ,  C07D233/32

    CPC分类号： C07D207/22 ,  C07D207/26 ,  C07D207/28 ,  C07D211/76 ,  C07D211/78 ,  C07D213/81 ,  C07D233/32 ,  C07D233/34 ,  C07D239/10 ,  C07D275/03 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    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, R4, Q, Y, A 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 Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2—CH2, CH2—CH2—CH2, N(Ry#)—CH2, N(Ry#)—CH2—CH2 or CH═CH—CH═, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# 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 3a，R 3b，R 4，Q，Y，A和X具有权利要求和说明书中所述的含义及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和Ib，其中R1，r，R2b，R3a，R3b，R4，Y和X具有权利要求中提及的含义，包括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Y为CH2-CH2，CH2-CH2-CH2，N（Ry＃）-CH2，N（Ry＃）-CH2-CH2或CH = CH-CH =，各自任选具有1 或2个H原子被相同或不同的基团Ry取代，其中Ry和Ry＃具有权利要求中提及的含义。