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    LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS
    12.
    发明申请
    LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS 审中-公开
    包含聚羟基 - 烷基和聚羟基 - 环烷基基团的低分子丝氨酸蛋白酶抑制剂

    公开(公告)号：US20110071285A1

    公开(公告)日：2011-03-24

    申请号：US12850545

    申请日：2010-08-04

    申请人： Dieter Herr ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger

    发明人： Dieter Herr ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger

    IPC分类号： C07H15/26 ,  C07D277/30 ,  C07D409/12

    CPC分类号： A61K31/155 ,  C07H7/00 ,  C07H15/00

    摘要： The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases CIs and C1r. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or guanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates. Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained.

    摘要翻译： 本发明涉及新型脒和喹啉，其生产及其用途及其作为胰蛋白酶型丝氨酸蛋白酶竞争性抑制剂的用途，特别是血栓素和补体蛋白酶CI和C1r。 除了使用化合物作为血栓抑制剂，抗凝剂，补体抑制剂和抗炎剂之外，本发明还涉及含有所述化合物作为活性成分的药物组合物。 该新型组合物的特征在于具有脒或胍功能的丝氨酸蛋白酶抑制剂与具有两个或多个羟基官能团的烷基基团的连接，其中所述烷基衍生自糖衍生物。 因此，几种糖结构成分或来自糖的组分可以彼此连接。 所述连接糖衍生物的原理使得能够获得口服活性化合物。

    LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS
    13.
    发明申请
    LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS 审中-公开
    包含聚羟基 - 烷基和聚羟基 - 环烷基基团的低分子丝氨酸蛋白酶抑制剂

    公开(公告)号：US20120190832A1

    公开(公告)日：2012-07-26

    申请号：US13277829

    申请日：2011-10-20

    申请人： Dieter Herr ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger

    发明人： Dieter Herr ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger

    IPC分类号： C07H15/26

    CPC分类号： A61K31/155 ,  C07H7/00 ,  C07H15/00

    摘要： The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases CIs and C1r. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or guanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates. Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained.

    摘要翻译： 本发明涉及新型脒和喹啉，其生产及其用途及其作为胰蛋白酶型丝氨酸蛋白酶竞争性抑制剂的用途，特别是血栓素和补体蛋白酶CI和C1r。 除了使用化合物作为血栓抑制剂，抗凝剂，补体抑制剂和抗炎剂之外，本发明还涉及含有所述化合物作为活性成分的药物组合物。 该新型组合物的特征在于具有脒或胍功能的丝氨酸蛋白酶抑制剂与具有两个或多个羟基官能团的烷基基团的连接，其中所述烷基衍生自糖衍生物。 因此，几种糖结构成分或来自糖的组分可以彼此连接。 所述连接糖衍生物的原理使得能够获得口服活性化合物。

    Prodrugs of thrombin inhibitors
    14.
    发明授权
    Prodrugs of thrombin inhibitors 有权
    凝血酶抑制剂的前药

    公开(公告)号：US07144902B1

    公开(公告)日：2006-12-05

    申请号：US09958349

    申请日：2000-04-05

    申请人： Dorit Baucke ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger ,  Gisela Backfisch ,  Juergen Delzer

    发明人： Dorit Baucke ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger ,  Gisela Backfisch ,  Juergen Delzer

    IPC分类号： A61K31/425 ,  C07D277/20

    CPC分类号： C07K5/06078 ,  A61K38/00 ,  C07B43/00 ,  C07K5/0222

    摘要： The present invention relates to prodrugs of pharmacologically active five-membered heterocyclic amidines from which are produced in vivo compounds which are competitive inhibitors of trypsin-like serine proteases, in particular thrombin and kininogenases such as kallikrein, to the preparation thereof and to the use thereof as medicines. The invention also relates to pharmaceutical compositions which comprise the prodrugs of the active compounds as ingredients, and to the use of the compounds as thrombin inhibitors, anticoagulants and as antiinflammatory agents.

    摘要翻译： 本发明涉及药理活性五元杂环脒的前体药物，它们是体内化合物，其是胰蛋白酶样丝氨酸蛋白酶的竞争性抑制剂，特别是凝血酶和激肽释放酶如激肽释放酶对其制备及其用途 作为药物 本发明还涉及包含活性化合物作为成分的前药以及该化合物作为凝血酶抑制剂，抗凝剂和抗炎剂的用途的药物组合物。

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV
    16.
    发明申请
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV 有权
    羧酰胺化合物及其作为抑制剂的用途IV

    公开(公告)号：US20110152325A1

    公开(公告)日：2011-06-23

    申请号：US12972679

    申请日：2010-12-20

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

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

    IPC分类号： A61K31/4439 ,  C07D401/04 ,  A61P25/28 ,  A61P25/00 ,  A61P25/08 ,  A61P25/04 ,  A61P13/12 ,  A61P35/00 ,  A61P31/18 ,  A61P37/02 ,  A61P33/06

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14

    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 C3-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or 1,3-benzoxazol-2-yl-methyl, 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 3 -C 4 - 烷基，C 1 -C 4 - 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，C 3 -C 6 - 杂环烷基-C 1 -C 2 - 烷基，苯基-C 1 -C 3 - 烷基，吡啶-2-基-C 1 -C 3 - 烷基或1,3-苯并恶唑-2-基 - 甲基，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
    18.
    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：US20140005227A1

    公开(公告)日：2014-01-02

    申请号：US13992582

    申请日：2011-12-08

    申请人： Andreas Kling ,  Katja Jantos ,  Helmut Mack ,  Achim Moller ,  Wilfried Hornberger ,  Yanbin Lao ,  Gisela Backfisch ,  Marjoleen Nijsen

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

    IPC分类号： C07D401/04

    CPC分类号： C07D401/04 ,  A61K31/4439 ,  C07D401/14 ,  Y02A50/411

    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, X, 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 benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R2 is C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or CH2—C(O)OCH3, R3 and R4 independently of one another are halogen, CN, 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，X，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，其水合物和药学上合适的盐 其中。 在这些化合物中，优选其中R 1为任选取代的苄基或杂芳基 - 甲基，X为单键或氧原子，R 2为C 1 -C 4烷基，C 1 -C 4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，C 3 -C 6杂环烷基-C 1 -C 2烷基，苯基，苯基-C 1 -C 3 - 烷基，吡啶-2-基-C 1 -C 3 - 烷基或CH 2 -C（O）OCH 3，R 3和R 4彼此独立地是卤素，CN，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。

    3-Substituted 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof
    20.
    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。