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72 条记录 (耗时 0.063 秒)

    Heteroarylcyclopropanecarboxamides and their use as pharmaceuticals
    32.
    发明授权
    Heteroarylcyclopropanecarboxamides and their use as pharmaceuticals 有权
    杂芳基环丙烷甲酰胺及其作为药物的用途

    公开(公告)号：US08299102B2

    公开(公告)日：2012-10-30

    申请号：US12486118

    申请日：2009-06-17

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

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

    IPC分类号： C07D211/70 ,  A61K31/4418

    CPC分类号： C07D213/56 ,  C07D271/113 ,  C07D333/24 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

    摘要： The present invention relates to heteroarylcyclopropanecarboxamides of the formula I, in which Het, X, Ra, Rb, Rc, Rd, 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的杂芳基环丙烷甲酰胺，其中Het，X，Ra，Rb，Rc，Rd，R1，R2和R3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。

    Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them
    35.
    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。

    Process for the preparation of pyrrole derivates
    39.
    发明授权
    Process for the preparation of pyrrole derivates 失效
    吡咯衍生物的制备方法

    公开(公告)号：US5290947A

    公开(公告)日：1994-03-01

    申请号：US33232

    申请日：1993-03-16

    申请人： Gerhard Zoller ,  Eckard Kujath ,  Klaus Delpy ,  Manfred Schrod

    发明人： Gerhard Zoller ,  Eckard Kujath ,  Klaus Delpy ,  Manfred Schrod

    IPC分类号： C07D207/32 ,  C07D207/333 ,  C07D207/323 ,  C07D207/325 ,  C07D207/327

    CPC分类号： C07D207/333

    摘要： The present invention relates to a process for the preparation of pyrrole derivatives of the general formula I ##STR1## by reaction of a compound of the general formula III ##STR2## where R, R.sup.1 and R.sup.2 are defined as specified in claim 1, in a Vilsmeier reaction. The reaction is carried out in an easily degradable solvent, the reaction product is isolated with the aid of a water-miscible extractant and is purified by high-vacuum distillation in the short path evaporator.

    摘要翻译： 本发明涉及制备通式I（*化学结构*）（I）的吡咯衍生物的方法，该方法通过使通式III的化合物（*化学结构*）（III）与R 和R 2如权利要求1中所定义，在Vilsmeier反应中。 反应在容易降解的溶剂中进行，反应产物借助水混溶萃取剂分离，并在短路蒸发器中通过高真空蒸馏纯化。