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    Indole derivatives as inhibitors or factor Xa
    1.
    发明授权
    Indole derivatives as inhibitors or factor Xa 有权
    吲哚衍生物作为抑制剂或因子Xa

    公开(公告)号：US06337344B1

    公开(公告)日：2002-01-08

    申请号：US09582344

    申请日：2000-08-14

    申请人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose ,  Hans Matter

    发明人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose ,  Hans Matter

    IPC分类号： A61K3144

    CPC分类号： C07D401/06 ,  C07D209/42 ,  C07D401/12 ,  C07D403/10 ,  C07D471/04

    摘要： The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R1a, R1b, R1c R1d, R2, R3, R4 and A are defined as indicated in the claims. The compounds of formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to use of the compounds of formula (I) in the treatment and prophylaxis of diseases which can be cured or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (I) in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (I) together with pharmaceutically acceptable carrier substances and/or auxiliary substances.

    摘要翻译： 本发明涉及抑制血液凝固蛋白质，更具体地说，涉及式（I）的吲哚衍生物，其中R1a，R1b，R1c R1d，R2，R3，R4和A如权利要求中所示定义。 式（I）的化合物是凝血酶因子Xa的抑制剂。 本发明还涉及制备式（I）化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，使用式（I）化合物治疗和预防可以 通过抑制诸如血栓栓塞性疾病的因子Xa活性而被治愈或预防，以及式（I）化合物在制备用于这些疾病的药物中的用途。 本发明还涉及包含与惰性载体混合或以其它方式结合的式（I）化合物的组合物，特别是含有式（I）化合物与药学上可接受的载体物质和/或辅助物质的药物组合物。

    Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them
    3.
    发明授权
    Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them 有权
    丙二酸衍生物，其制备方法，用途及含有它们的药物组合物

    公开(公告)号：US06395737B1

    公开(公告)日：2002-05-28

    申请号：US09473053

    申请日：1999-12-28

    申请人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Hans Matter ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    发明人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Hans Matter ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    IPC分类号： A61K31165

    CPC分类号： C07C257/18 ,  C07C279/14

    摘要： New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

    摘要翻译： 用于抑制血液凝固蛋白质的新化合物，更具体地，涉及式I的丙二酸衍生物，其中R（1），R（2），R（3），R（4），R（5）和 R（6）具有权利要求中所示的含义。 式I化合物是凝血酶因子Xa的抑制剂。 用于制备式I化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，式I化合物在治疗和预防疾病中的用途，其可以通过抑制因子Xa来治疗或预防 活性如血栓栓塞性疾病，以及式I化合物在制备用于这些疾病的药物中的应用。 含有式I化合物的组合物与惰性载体混合或以其它方式结合，特别是含有式I化合物的药物组合物以及药学上可接受的载体物质和辅助物质。

    Factor VIIa inhibitors
    4.
    发明授权
    Factor VIIa inhibitors 有权
    因子VIIa抑制剂

    公开(公告)号：US06500803B1

    公开(公告)日：2002-12-31

    申请号：US09588651

    申请日：2000-06-07

    申请人： Otmar Klingler ,  Manfred Schudok ,  Gerhard Zoller ,  Uwe Heinelt ,  Elisabeth Defossa ,  Hans Matter ,  Pavel Safar

    发明人： Otmar Klingler ,  Manfred Schudok ,  Gerhard Zoller ,  Uwe Heinelt ,  Elisabeth Defossa ,  Hans Matter ,  Pavel Safar

    IPC分类号： A61K3805

    CPC分类号： C07K5/06086 ,  A61K38/00

    摘要： The present invention relates to compounds of formula I, in which R1, R2, R91, R92, R93, R94, R95, R96, R97, r, s, and t have the meanings indicated in the claims. Compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 本发明涉及式Ⅰ化合物，其中R1，R2，R91，R92，R93，R94，R95，R96，R97，r，s和t具有权利要求中所示的含义。 式I化合物是有价值的药理活性化合物。 它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa活性的条件下或用于治疗或预防预期因子VIIa的抑制的病症。 本发明还涉及制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

    Urea derivatives with antiproteolytic activity
    5.
    发明授权
    Urea derivatives with antiproteolytic activity 有权
    具有抗蛋白水解活性的尿素衍生物

    公开(公告)号：US06706715B2

    公开(公告)日：2004-03-16

    申请号：US10183848

    申请日：2002-06-26

    申请人： Manfred Schudok ,  Otmar Klingler ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder ,  Hauke Szillat

    发明人： Manfred Schudok ,  Otmar Klingler ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder ,  Hauke Szillat

    IPC分类号： A61K314425

    CPC分类号： C07C275/42 ,  C07C2601/14 ,  C07D333/38

    摘要： The present invention relates to compounds of the formula I, in which R1, R2, R4, R5, D1, D2, X1, X2, X3, A and B have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 本发明涉及式I化合物，其中R 1，R 2，R 4，R 5，D 1，D 2，X 1，X 2，X 3，A和B具有所指定的含义 在权利要求中。 式I的化合物是有价值的药理活性化合物。 它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防血栓栓塞性疾病和再狭窄。 它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa的活性或用于治疗或预防因子VIIa的抑制的条件下使用。 本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

    CYCLIC PEPTIDES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF THE PLATELET ADHESION
    6.
    发明申请
    CYCLIC PEPTIDES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF THE PLATELET ADHESION 有权
    循环肽，其制备及其作为平板胶粘剂的抑制剂

    公开(公告)号：US20140011734A1

    公开(公告)日：2014-01-09

    申请号：US13818444

    申请日：2011-07-27

    申请人： Otmar Klingler ,  Horst Blum ,  Andreas Lindenschmidt ,  Hans Matter

    发明人： Otmar Klingler ,  Horst Blum ,  Andreas Lindenschmidt ,  Hans Matter

    IPC分类号： C07K7/64

    CPC分类号： C07K7/64 ,  A61K38/00 ,  C07K7/06 ,  C07K7/56

    摘要： The present invention relates to compounds of the Formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, X1, X2, X3 and X4 have the meanings indicated in the claims, and which are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb), and are suitable, for example, for the therapy and prophylaxis of athero-thrombotic diseases. The invention furthermore relates to processes for the preparation of compounds of the Formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，R14，R15，R16，R17，R18 X1，X2，X3和X4具有权利要求中所示的含义，并且它们是有价值的药理活性化合物。 它们是血浆蛋白血管性血友病因子（vWF）和血小板受体糖蛋白Ib-IX-V复合物（GPIb）之间的相互作用的可逆抑制剂，并且适合于例如治疗和预防动脉粥样硬化血栓性疾病 。 本发明还涉及制备式（I）化合物，其用途，特别是作为药物中的活性成分的方法，以及包含它们的药物组合物。

    Factor VIIa inhibitory (thio)urea derivatives, their preparation and their use
    7.
    发明授权
    Factor VIIa inhibitory (thio)urea derivatives, their preparation and their use 有权
    因子VIIa抑制（硫）脲衍生物，其制备及其应用

    公开(公告)号：US06743790B2

    公开(公告)日：2004-06-01

    申请号：US09874318

    申请日：2001-06-06

    申请人： Otmar Klingler ,  Manfred Schudok ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder

    发明人： Otmar Klingler ,  Manfred Schudok ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder

    IPC分类号： A61K31535

    CPC分类号： C07D213/40 ,  C07C275/42 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/18 ,  C07D211/96 ,  C07D319/18

    摘要： The present invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5, R6, A, X, m and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, for example as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 本发明涉及式Ⅰ化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，A，X，m和n 具有权利要求中所示的含义。 式I的化合物是有价值的药理活性化合物。 它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防血栓栓塞性疾病和再狭窄。 它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa的活性或用于治疗或预防因子VIIa的抑制的条件下使用。 本发明还涉及制备式I化合物的方法，其用途，例如作为药物中的活性成分，以及包含它们的药物制剂。

    Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use
    8.
    发明授权
    Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use 有权
    丙二酰胺和丙二酸酯衍生物具有抗血栓活性，其制备及其用途

    公开(公告)号：US06645992B2

    公开(公告)日：2003-11-11

    申请号：US09965790

    申请日：2001-10-01

    申请人： Manfred Schudok ,  Otmar Klingler ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder

    发明人： Manfred Schudok ,  Otmar Klingler ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder

    IPC分类号： C07D25718

    CPC分类号： A61K31/27 ,  A61K31/167 ,  A61K31/225 ,  C07C257/18 ,  C07C257/20

    摘要： Compounds of formula I, in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 具有权利要求中所述定义的R 1，R 2，A和B的式I化合物是有价值的药理活性化合物，其表现出很强的抗血栓形成作用，并且适用于例如 治疗血栓栓塞性疾病和再狭窄。 它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa的活性或用于治疗或预防因子VIIa的抑制的条件下使用。 还公开了制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

    Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use
    9.
    发明授权
    Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use 有权
    丙二酰胺和丙二酸酯衍生物具有抗血栓活性，其制备及其用途

    公开(公告)号：US07153876B2

    公开(公告)日：2006-12-26

    申请号：US10634827

    申请日：2003-08-06

    申请人： Manfred Schudok ,  Otmar Klingler ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder

    发明人： Manfred Schudok ,  Otmar Klingler ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder

    IPC分类号： C07D213/75 ,  A61K31/44 ,  A61P7/02 ,  A61P9/10

    CPC分类号： A61K31/27 ,  A61K31/167 ,  A61K31/225 ,  C07C257/18 ,  C07C257/20

    摘要： Compounds of formula I, in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 具有权利要求中所述定义的R 1，R 2，A和B的式I化合物是有价值的药理学活性化合物，其表现出强烈的 抗血栓形成作用，并且适用于例如治疗血栓栓塞性疾病和再狭窄。 它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa的活性或用于治疗或预防因子VIIa的抑制的条件下使用。 还公开了制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

    Cyclic peptides, their preparation and their use as inhibitors of the platelet adhesion
    10.
    发明授权
    Cyclic peptides, their preparation and their use as inhibitors of the platelet adhesion 有权
    循环肽，它们的制备及其作为血小板粘附抑制剂的用途

    公开(公告)号：US09073975B2

    公开(公告)日：2015-07-07

    申请号：US13818444

    申请日：2011-07-27

    申请人： Otmar Klingler ,  Horst Blum ,  Andreas Lindenschmidt ,  Hans Matter

    发明人： Otmar Klingler ,  Horst Blum ,  Andreas Lindenschmidt ,  Hans Matter

    IPC分类号： C07K7/64 ,  C07K7/06 ,  C07K7/56 ,  A61K38/00

    CPC分类号： C07K7/64 ,  A61K38/00 ,  C07K7/06 ,  C07K7/56

    摘要： The present invention relates to compounds of the Formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, X1, X2, X3 and X4 have the meanings indicated in the claims, and which are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb), and are suitable, for example, for the therapy and prophylaxis of athero-thrombotic diseases. The invention furthermore relates to processes for the preparation of compounds of the Formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，R14，R15，R16，R17，R18 X1，X2，X3和X4具有权利要求中所示的含义，并且它们是有价值的药理活性化合物。 它们是血浆蛋白血管性血友病因子（vWF）和血小板受体糖蛋白Ib-IX-V复合物（GPIb）之间的相互作用的可逆抑制剂，并且适合于例如治疗和预防动脉粥样硬化血栓性疾病 。 本发明还涉及制备式（I）化合物，其用途，特别是作为药物中的活性成分的方法，以及包含它们的药物组合物。