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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。

    N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
    4.
    发明授权
    N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them 有权
    N-胍基烷基酰胺，它们的制备方法，它们的用途以及包含它们的药物制剂

    公开(公告)号：US06664393B2

    公开(公告)日：2003-12-16

    申请号：US10227222

    申请日：2002-08-26

    申请人： Otmar Klingler ,  Gerhard Zoller ,  Elisabeth Defossa ,  Fahad A. Al-Obeidi ,  Armin Walser ,  James Ostrem

    发明人： Otmar Klingler ,  Gerhard Zoller ,  Elisabeth Defossa ,  Fahad A. Al-Obeidi ,  Armin Walser ,  James Ostrem

    IPC分类号： C07D23924

    CPC分类号： C07D213/30 ,  C07C279/14 ,  C07D213/40 ,  C07D215/48 ,  C07D239/28

    摘要： The present invention relates to compounds of the formula I, in which A, L, Y, and k have the meanings indicated in the specification and 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 cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and/or factor VIIa and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor Xa and/or 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A，L，Y和k具有说明书和权利要求书中所示的含义。 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心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa和/或因子VIIa的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望的活性的条件或用于治愈或预防其中 旨在抑制因子Xa和/或因子VIIa。 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。

    N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
    5.
    发明授权
    N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them 有权
    N-胍基烷基酰胺，它们的制备方法，它们的用途以及包含它们的药物制剂

    公开(公告)号：US06472562B1

    公开(公告)日：2002-10-29

    申请号：US09697188

    申请日：2000-10-27

    申请人： Otmar Klingler ,  Gerhard Zoller ,  Elisabeth Defossa ,  Fahad A. Al-Obeidi ,  Armin Walser ,  James Ostrem

    发明人： Otmar Klingler ,  Gerhard Zoller ,  Elisabeth Defossa ,  Fahad A. Al-Obeidi ,  Armin Walser ,  James Ostrem

    IPC分类号： C07C23305

    CPC分类号： C07D213/30 ,  C07C279/14 ,  C07D213/40 ,  C07D215/48 ,  C07D239/28

    摘要： The present invention relates to compounds of the formula I, in which A, L, Y, and k have the meanings indicated in the specification and 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 cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and/or factor VIIa and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular 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A，L，Y和k具有说明书和权利要求书中所示的含义。 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心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa和/或因子VIIa的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不需要的活性或用于治愈或预防其中 旨在抑制因子Xa和/或因子VIIa。 本发明还涉及制备式I化合物，其用途，特别是药物中的活性成分以及包含它们的药物制剂的方法。

    Malonic acid derivatives, processes for their preparation their use and pharmaceutical compositions containing them
    6.
    发明授权
    Malonic acid derivatives, processes for their preparation their use and pharmaceutical compositions containing them 有权
    丙二酸衍生物，其制备方法，其用途和含有它们的药物组合物

    公开(公告)号：US06794365B2

    公开(公告)日：2004-09-21

    申请号：US09790641

    申请日：2001-02-23

    申请人： Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    发明人： Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    IPC分类号： C07K506

    CPC分类号： C07D213/56 ,  A61K38/00 ,  C07C257/18 ,  C07C279/14 ,  C07C2601/14 ,  C07K5/0202 ,  C07K5/06026 ,  C07K5/06034

    摘要： The present invention relates to new 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. 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 the 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 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 auxiliary substances.

    摘要翻译： 本发明涉及式I的新型丙二酸衍生物，其中R（1），R（2），R（3），R（4），R（5）和R（6） 索赔。 式I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治疗的疾病 或通过抑制诸如血栓栓塞性疾病的因子Xa活性来防止，以及式I化合物在制备用于这些疾病的药物中的用途。 本发明还涉及含有式I化合物的组合物，其与惰性载体混合或以其它方式结合，特别是含有式I化合物与药学上可接受的载体物质和辅助物质的药物组合物。