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    Heteroarylacrylamides and their use as pharmaceuticals
    5.
    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。

    Pentafluorosulfanylbenzoylguanidines, processes for their preparation, their use as medicaments or diagnostic aids, and medicaments comprising them
    6.
    发明授权
    Pentafluorosulfanylbenzoylguanidines, processes for their preparation, their use as medicaments or diagnostic aids, and medicaments comprising them 有权
    五氟硫烷基苯甲酰胍胺，其制备方法，用作药物或诊断助剂，以及包含它们的药物

    公开(公告)号：US08008352B2

    公开(公告)日：2011-08-30

    申请号：US12102446

    申请日：2008-04-14

    申请人： Heinz-Werner Kleemann

    发明人： Heinz-Werner Kleemann

    IPC分类号： A61K31/155

    CPC分类号： C07C381/00 ,  Y10S514/821

    摘要： Pentafluorosulfanylbenzoylguanidines, of the formula I and II in which R1 to R4 have the meanings stated in the claims, are suitable as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.

    摘要翻译： 其中R 1至R 4具有权利要求中所述含义的式I和II的五氟硫烷基苯甲酰基胍适合作为具有用于预防梗塞和治疗梗塞和用于治疗心绞痛的心脏保护组分的抗心律失常药物。 它们还预防性地抑制与缺血诱导的损伤的发展相关的病理生理过程，特别是在引发缺血诱发的心律失常中。

    Pentafluorosulfanylbenzoylguanidines, process for their preparation, use as a medicament or diagnostic aid, and medicament comprising same
    8.
    发明授权
    Pentafluorosulfanylbenzoylguanidines, process for their preparation, use as a medicament or diagnostic aid, and medicament comprising same 有权
    五氟硫烷基苯甲酰胍，其制备方法，用作药物或诊断助剂，以及包含其的药物

    公开(公告)号：US07622611B2

    公开(公告)日：2009-11-24

    申请号：US11972954

    申请日：2008-01-11

    申请人： Heinz-Werner Kleemann

    发明人： Heinz-Werner Kleemann

    IPC分类号： C07C233/65 ,  C07C255/50 ,  A61K31/165

    CPC分类号： C07C381/00

    摘要： Pentafluorosulfanylbenzoylguanidines of formula I wherein R1 to R4 have the meanings stated in the claims, are suitable, for example, as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.

    摘要翻译： 其中R 1至R 4具有权利要求中所述含义的式I的五氟硫烷基苯甲酰基胍适用于例如具有用于预防梗塞和治疗梗塞和用于治疗心绞痛的心脏保护组分的抗心律失常药物。 它们还预防性地抑制与缺血诱导的损伤的发展相关的病理生理过程，特别是在引发缺血诱发的心律失常中。

    Process for preparing 4-pentafluorosulfanylbenzoylguanidines
    10.
    发明授权
    Process for preparing 4-pentafluorosulfanylbenzoylguanidines 有权
    制备4-五氟硫基苯甲酰基胍的方法

    公开(公告)号：US07449594B2

    公开(公告)日：2008-11-11

    申请号：US11539237

    申请日：2006-10-06

    申请人： Gerrit Schubert ,  Heinz-Werner Kleemann

    发明人： Gerrit Schubert ,  Heinz-Werner Kleemann

    IPC分类号： C07C255/50 ,  C07C233/65

    CPC分类号： C07C381/00

    摘要： A process for preparing 4-pentafluorosulfanylbenzoylguanidines of formula I wherein R1 to R4 have the meanings indicated in the specification. The compounds of formula I are NEH1 inhibitors and can be employed, for example, for the treatment of cardiovascular disorders.

    摘要翻译： 一种制备式I的4-五氟硫烷基苯甲酰胍的方法，其中R1至R4具有说明书中所示的含义。 式I化合物是NEH1抑制剂，可用于例如治疗心血管疾病。