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115 条记录 (耗时 0.047 秒)

    3-Substituted 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof
    57.
    发明授权
    3-Substituted 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof 有权
    3-取代的3,4-二氢 - 噻吩并[2,3-d]嘧啶-4-酮衍生物，的制备和用途

    公开(公告)号：US07491729B2

    公开(公告)日：2009-02-17

    申请号：US10539708

    申请日：2003-12-17

    申请人： Margaretha Bakker ,  Wilfried Hornberger ,  Andreas Kling ,  Udo Lange ,  Helmut Mack ,  Achim Moeller ,  Reinhold Mueller ,  Kurt Schellhaas ,  Martin Schmidt ,  Gerd Steiner ,  Karsten Wicke

    发明人： Margaretha Bakker ,  Wilfried Hornberger ,  Andreas Kling ,  Udo Lange ,  Helmut Mack ,  Achim Moeller ,  Reinhold Mueller ,  Kurt Schellhaas ,  Martin Schmidt ,  Gerd Steiner ,  Karsten Wicke

    IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

    CPC分类号： C07D495/14

    摘要： 3-Substituted 3,4-dihydrothieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof. The invention relates to 3,4-dihydrothieno[2,3-d]pyrimidin-4-one derivatives which are substituted in position 3 by 5-membered heteroaryl which may be fused to an aryl or heteroaryl radical, where the heteroaryl and, if appropriate, the fused aryl or heteroaryl radical may have 1, 2 or 3 substituents selected independently of one another from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halo-C1-5-alkyl, halo-C1-5-alkoxy, hydroxy, —NH2, —N(R6)2, —NH(R6), aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl, where the substituents aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl may have 1, 2 or 3 substituents selected independently of one another from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halo-C1-5-alkyl, halo-C1-5-alkoxy, hydroxy, —NH2, —N(R6)2 and —NH(R6). The preparation and use of these derivatives, especially for therapeutic purposes, e.g. for the treatment of depressions, are likewise described.

    摘要翻译： 3-取代的3,4-二氢噻吩并[2,3-d]嘧啶-4-酮衍生物，的制备和用途。 本发明涉及在3位被5位杂芳基取代的3,4-二氢噻吩并[2,3-d]嘧啶-4-酮衍生物，其可以与芳基或杂芳基稠合，其中杂芳基和 稠合的芳基或杂芳基可以具有1,2或3个彼此独立地选自C 1-5 - 烷基，C 1-5 - 烷氧基，C 1-5 - 烷硫基，卤素，CN，卤代-C 1-5 - 烷基，卤代C 1-5 - 烷氧基，羟基，-NH 2，-N（R 6）2，-NH（R 6），芳基，芳氧基，芳烷基，芳烷氧基和杂芳基，其中芳基，芳氧基，芳烷基，芳烷氧基和杂芳基 可以具有1,2或3个彼此独立地选自C 1-5 - 烷基，C 1-5 - 烷氧基，C 1-5 - 烷硫基，卤素，CN，卤代C 1-5 - 烷基，卤代-C 1-5 - 烷氧基，羟基，-NH 2，-N（R 6）2和-NH（R 6）。 这些衍生物的制备和使用，特别是用于治疗目的，例如 为了处理凹陷，同样地描述。

    Carboxamide compounds and their use as calpain inhibitors
    59.
    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

    申请人： Andreas Kling ,  Wilfried Hornberger ,  Helmut Mack ,  Achim Moeller ,  Volker Nimmrich ,  Dietmar Seemann ,  Wilfried Lubisch

    发明人： Andreas Kling ,  Wilfried Hornberger ,  Helmut Mack ,  Achim Moeller ,  Volker Nimmrich ,  Dietmar Seemann ,  Wilfried Lubisch

    IPC分类号： A61K31/4439 ,  C07D401/00

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D491/048 ,  C07D493/04 ,  C07D513/04

    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。