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    4-Fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical
    51.
    发明授权
    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：US06812253B2

    公开(公告)日：2004-11-02

    申请号：US10623775

    申请日：2003-07-22

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

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

    IPC: A61K31165

    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. 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性心绞痛，Prinzmetal心绞痛（痉挛），急性冠状动脉综合征，心力衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病PAOD，动脉粥样硬化， PTCA后的再狭窄，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，以及降低绝经后妇女心血管危险或摄入避孕药后，治疗和预防糖尿病和糖尿病并发症 （肾病，视网膜病变），血管发生，支气管哮喘，慢性肾功能衰竭，肝硬化，受限的记忆力或受限的学习能力。

    Substituted 4-amino-2-aryl-cyclopenta[d]pyrimidines, their production and use and pharmaceutical preparations containing same
    52.
    发明授权
    Substituted 4-amino-2-aryl-cyclopenta[d]pyrimidines, their production and use and pharmaceutical preparations containing same 有权
    取代的4-氨基-2-芳基 - 环戊二烯并[d]嘧啶，其制备和用途以及含有它们的药物制剂

    公开(公告)号：US06627628B1

    公开(公告)日：2003-09-30

    申请号：US09856069

    申请日：2001-05-17

    Applicant: Ursula Schindler ,  Karl Schoenafinger ,  Hartmut Strobel

    Inventor： Ursula Schindler ,  Karl Schoenafinger ,  Hartmut Strobel

    IPC: C07D23970

    CPC classification number: C07D401/12 ,  C07D239/70

    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the treatment and prophylaxis of diseases, for example cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis and atherosclerosis. The compounds of formula (I) are able to modulate the body's own production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis ofisorders associated with an impaired cGMP balance. The invention also relates to methods for producing compounds of formula (I), to their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and to pharmaceutical preparations containing the compounds of formula (I).

    Abstract translation: 本发明涉及其中R 1，R 2和R 3具有权利要求中给出的含义的式（I）化合物。 所述化合物是药物中有价值的活性剂，用于治疗和预防疾病，例如高血压，心绞痛，心力衰竭，血栓形成和动脉粥样硬化等心血管疾病。 式（I）化合物能够调节人体自身产生的环鸟苷酸（cGMP），并且通常适用于与受损的cGMP平衡相关的疾病的治疗和预防。 本发明还涉及制备式（I）化合物的方法，用于治疗和预防上述疾病以及用于制备这些疾病的药物，以及含有式（I）化合物的药物制剂。

    Heteroarylacrylamides and their use as pharmaceuticals
    55.
    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

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

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

    IPC: C07D401/06 ,  A61K31/44

    CPC classification number: 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

    Abstract: 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.

    Abstract translation: 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。

    IMIDAZO[1,2-a]AZINES AND THEIR USE AS PHARMACEUTICALS
    58.
    发明申请
    IMIDAZO[1,2-a]AZINES AND THEIR USE AS PHARMACEUTICALS 有权
    咪唑并[1,2-a]三嗪及其作为药物的用途

    公开(公告)号：US20100137321A1

    公开(公告)日：2010-06-03

    申请号：US12548641

    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: A61K31/5025 ,  A61K31/519 ,  C07D487/04 ,  A61P11/06 ,  A61P9/04 ,  A61P9/00 ,  A61P9/10 ,  A61P3/10

    CPC classification number: C07D487/04 ,  A61K31/4188 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/519

    Abstract: The present invention relates to derivatives of imidazo[1,2-a]azines of formula I, in which R, R1 to R3, X, Y 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]吖嗪衍生物，其中R，R 1至R 3，X，Y和n具有权利要求中所示的含义，其调节内皮一氧化氮的转录（ NO）合酶，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。

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