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    Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals
    25.
    发明授权
    Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals 有权
    包含不饱和或环状连接基团的杂芳基取代的酰胺及其作为药物的用途

    公开(公告)号：US08642620B2

    公开(公告)日：2014-02-04

    申请号：US11958503

    申请日：2007-12-18

    申请人： Harmut Strobel ,  Paulus Wohlfart ,  Gerhard Zoller ,  David William Will

    发明人： Harmut Strobel ,  Paulus Wohlfart ,  Gerhard Zoller ,  David William Will

    IPC分类号： A61K31/4545 ,  C07D401/06

    CPC分类号： C07D401/14 ,  C07D401/06 ,  C07D401/08 ,  C07D409/14 ,  C07D417/06

    摘要： The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

    摘要翻译： 本发明涉及式I的N-烷基酰胺，其中A，Het，X，R 1，R 2和R 3具有权利要求中所述的含义，其调节内皮一氧化氮（NO）合酶的转录并且是有价值的药理学 活性化合物。 具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。 本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于 治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

    Heteroarylacrylamides and their use as pharmaceuticals
    26.
    发明授权
    Heteroarylacrylamides and their use as pharmaceuticals 有权
    杂芳基丙烯酰胺及其作为药物的用途

    公开(公告)号：US08304438B2

    公开(公告)日：2012-11-06

    申请号：US12486117

    申请日：2009-06-17

    申请人： Hartmut Strobel ,  Paulus Wohlfart ,  Heinz-Werner Kleemann ,  Gerhard Zoller ,  David William Will

    发明人： Hartmut Strobel ,  Paulus Wohlfart ,  Heinz-Werner Kleemann ,  Gerhard Zoller ,  David William Will

    IPC分类号： C07D401/06 ,  A61K31/44

    CPC分类号： C07D213/56 ,  C07D213/64 ,  C07D213/73 ,  C07D213/75 ,  C07D215/12 ,  C07D233/64 ,  C07D233/68 ,  C07D239/26 ,  C07D277/30 ,  C07D277/46 ,  C07D333/24 ,  C07D333/60 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12

    摘要： The present invention relates to heteroarylacrylamides of the formula I, in which Het, X, Ra, Rb, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

    摘要翻译： 本发明涉及式I的杂芳基丙烯酰胺，其中Het，X，Ra，Rb，R 1，R 2和R 3具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录并且是有价值的药理学 活性化合物。 具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。 本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于 治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

    N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
    27.
    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
    28.
    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。