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    4-Fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical
    13.
    发明申请
    4-Fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical 有权
    4-氟-N-茚满-2-基苯甲酰胺及其作为药物的用途

    公开(公告)号：US20050054729A1

    公开(公告)日：2005-03-10

    申请号：US10920395

    申请日：2004-08-18

    Applicant: Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    Inventor： Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    IPC: A61K31/00 ,  A61K31/166 ,  A61K31/66 ,  A61P1/16 ,  A61P5/48 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/12 ,  A61P15/10 ,  A61P19/10 ,  A61P25/28 ,  A61P27/06 ,  A61P43/00 ,  C07C233/65 ,  A61K31/165

    CPC classification number: C07C233/65 ,  A61K31/166 ,  C07C2602/08

    Abstract: The present invention relates to the method of stimulating the expression of endothelial NO-synthase in a mammal, which method comprises administering a physiologically active amount of 4-fluoro-N-indan-2-yl benzamide according to the formula (I) to the said mammal. The compound (I) can be used for the therapy and prophylaxis of cardiovascular diseases like stable and unstable angina pectoris, Prinzmetal angina (spasm), acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease PAOD, atherosclerosis, restenosis, endothelial damage after PTCA, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, and the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives, the therapy and prophylaxis of diabetes and diabetes complications (nephropathy, retinopathy), angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, restricted memory performance or a restricted ability to learn.

    Abstract translation: 本发明涉及刺激哺乳动物内皮细胞NO合成酶表达的方法，该方法包括将生理活性量的式（I）的4-氟-N-茚满-2-基苯甲酰胺给予 哺乳动物说 化合物（I）可用于治疗和预防心血管疾病如稳定和不稳定型心绞痛，Prinzmetal心绞痛（痉挛），急性冠状动脉综合征，心力衰竭，心肌梗死，中风，血栓形成，外周动脉闭塞性疾病PAOD，动脉粥样硬化 ，PTCA后再狭窄，内皮损伤，原发性高血压，肺动脉高压，继发性高血压，肾血管性慢性肾小球肾炎，勃起功能障碍，室性心律失常，绝经后妇女心血管危险降低或避孕药物摄入后，糖尿病和糖尿病的治疗和预防 并发症（肾病，视网膜病变），血管生成，哮喘支气管炎，慢性肾功能衰竭，肝硬化，限制性记忆能力或受限的学习能力。

    Sulfonylamino carboxylic acid N-arylamides as guanylate cyclase activators
    15.
    发明授权
    Sulfonylamino carboxylic acid N-arylamides as guanylate cyclase activators 有权
    磺酰氨基羧酸N-芳基酰胺作为鸟苷酸环化酶活化剂

    公开(公告)号：US06548547B1

    公开(公告)日：2003-04-15

    申请号：US09743199

    申请日：2001-03-08

    Applicant: Ursula Schindler ,  Karl Schoenafinger ,  Hartmut Strobel

    Inventor： Ursula Schindler ,  Karl Schoenafinger ,  Hartmut Strobel

    IPC: A61K3118

    CPC classification number: C07F9/4056 ,  C07C311/21 ,  C07D207/27 ,  C07D207/325 ,  C07D207/404 ,  C07D209/08 ,  C07D209/48 ,  C07D215/48 ,  C07D217/02 ,  C07D217/24 ,  C07D231/56 ,  C07D235/18 ,  C07D241/20 ,  C07D249/18 ,  C07D295/135 ,  C07D295/192 ,  C07D307/91 ,  C07D311/16 ,  C07D317/60 ,  C07D409/04 ,  C07F9/3882

    Abstract: The present invention relates to compounds of the formula I in which A1, A2, R2 and R3 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular disorders such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance. The invention relates to the use of compounds of the formula I for the therapy and prophylaxis of the designated disease states and for the production of pharmaceuticals therefor, novel compounds of the formula I, pharmaceutical preparations comprising them and processes for their preparation.

    Abstract translation: 本发明涉及式Iin化合物，其中A1，A2，R2和R3具有权利要求中所示的含义，它们是用于治疗和预防疾病的有价值的药物活性化合物，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的化合物具有调节环鸟苷酸（cGMP）的内源性产生的能力，并且通常适用于治疗和预防与受干扰的cGMP平衡相关的疾病状态。 本发明涉及式I化合物用于治疗和预防指定疾病状态及其制备药物的用途，式I化合物，包含它们的药物制剂及其制备方法。

    Imidazo[1,2-a]pyridines and their use as pharmaceuticals
    16.
    发明授权
    Imidazo[1,2-a]pyridines and their use as pharmaceuticals 有权
    咪唑并[1,2-a]吡啶及其作为药物的用途

    公开(公告)号：US08399476B2

    公开(公告)日：2013-03-19

    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: A01N43/42 ,  A61K31/44 ,  C07D491/02 ,  C07D498/02

    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。

    Imidazo[2,1-b]thiazoles and their use as pharmaceuticals
    18.
    发明授权
    Imidazo[2,1-b]thiazoles and their use as pharmaceuticals 有权
    咪唑并[2,1-b]噻唑及其作为药物的用途

    公开(公告)号：US08080569B2

    公开(公告)日：2011-12-20

    申请号：US12466576

    申请日：2009-05-15

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

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

    IPC: A61K31/429 ,  C07D513/04

    CPC classification number: C07D513/04

    Abstract: The present invention relates to derivatives of imidazo[2,1-b]thiazoles of formula I, in which R, R1 to R3 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 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的咪唑并[2,1-b]噻唑衍生物，其中R，R 1至R 3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应用。 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化合物在制备用于刺激内皮NO合成酶表达或用于治疗的药物中的用途 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。

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