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    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

    Applicant: Hartmut Strobel ,  Paulus Wohlfart ,  Gerhard Zoller ,  David William Will

    Inventor： Hartmut Strobel ,  Paulus Wohlfart ,  Gerhard Zoller ,  David William Will

    IPC: C07D211/70 ,  A61K31/4418

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

    Abstract: 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.

    Abstract translation: 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。

    IMIDAZO[1,2-a]PYRIDINES AND THEIR USE AS PHARMACEUTICALS
    33.
    发明申请
    IMIDAZO[1,2-a]PYRIDINES AND THEIR USE AS PHARMACEUTICALS 有权
    咪唑并[1,2-a]吡啶并用作药物

    公开(公告)号：US20100113412A1

    公开(公告)日：2010-05-06

    申请号：US12548636

    申请日：2009-08-27

    Applicant: Gerhard ZOLLER ,  Hartmut STROBEL ,  David William WILL ,  Paulus WOHLFART

    Inventor： Gerhard ZOLLER ,  Hartmut STROBEL ,  David William WILL ,  Paulus WOHLFART

    IPC: A61K31/437 ,  A61K31/397 ,  A61P3/10 ,  A61P9/00 ,  C07D471/04

    CPC classification number: C07D471/04

    Abstract: The present invention relates to derivatives of imidazo[1,2-a]pyridines of formula I, in which R, R1 to R4 and n 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 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 formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I 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.

    Abstract translation: 本发明涉及式I的咪唑并[1,2-a]吡啶衍生物，其中R，R 1至R 4和n具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录和 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使用。 本发明还涉及制备式I化合物的方法，包含它们的药物组合物，以及式I化合物用于刺激内皮NO合成酶表达或用于治疗各种疾病，包括心血管疾病 例如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全。

    Pyrazole derivatives, their preparation and their use in pharmaceuticals
    36.
    发明授权
    Pyrazole derivatives, their preparation and their use in pharmaceuticals 有权
    吡唑衍生物，其制备及其在药物中的应用

    公开(公告)号：US07300950B2

    公开(公告)日：2007-11-27

    申请号：US11104556

    申请日：2005-04-13

    Applicant: Ursula Schindler ,  Karl Schönafinger ,  Hartmut Strobel

    Inventor： Ursula Schindler ,  Karl Schönafinger ,  Hartmut Strobel

    IPC: C07D403/04 ,  A61K31/416 ,  C07D405/04 ,  A61K31/4155

    CPC classification number: C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14

    Abstract: The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: in which X, R1, R1a, R2, R3, R4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate “cGMP” and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.

    Abstract translation: 本发明涉及式I的吡唑衍生物及其制备及其在药物中的用途：其中X，R 1，R 1a，R 2， R 3，R 4，R 4和n如权利要求中所定义，它们是用于治疗和预防疾病的有用的药物活性化合物，例如心血管 疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化。 式I的化合物能够调节身体产生的环鸟苷酸“cGMP”，通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病。 本发明还涉及用于制备式I化合物的方法，其用于治疗和预防上述疾病和用于制备用于该目的的药物，还涉及包含式I化合物的药物制剂。

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