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    Substituted 2-phenyl-benzimidazoles and their use as pharmaceuticals
    3.
    发明授权
    Substituted 2-phenyl-benzimidazoles and their use as pharmaceuticals 有权
    取代的2-苯基 - 苯并咪唑及其作为药物的用途

    公开(公告)号：US08168665B2

    公开(公告)日：2012-05-01

    申请号：US12412481

    申请日：2009-03-27

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

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

    IPC: A01N43/50 ,  A01N43/52 ,  A61K31/415

    CPC classification number: C07D235/18 ,  C07D413/04

    Abstract: The present invention relates to derivatives of 2-phenyl-benzimidazoles of the formula I, in which X, 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 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2-苯基 - 苯并咪唑的衍生物，其中X，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，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。

    Acylated 6,7,8,9-tetrahydro-5H-benzocycloheptenyl amines and their use as pharmaceutical agents
    4.
    发明授权
    Acylated 6,7,8,9-tetrahydro-5H-benzocycloheptenyl amines and their use as pharmaceutical agents 有权
    酰化6,7,8,9-四氢-5H-苯并环庚烯基胺及其作为药剂的用途

    公开(公告)号：US07709478B2

    公开(公告)日：2010-05-04

    申请号：US10859773

    申请日：2004-06-03

    Applicant: Hartmut Strobel ,  Paulus Wohlfart

    Inventor： Hartmut Strobel ,  Paulus Wohlfart

    IPC: A61K31/166

    CPC classification number: C07C235/54 ,  C07C233/65 ,  C07C233/74 ,  C07C2602/12

    Abstract: The present invention relates to compounds according to the general formula (I), wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B, C and D are independently CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes, diabetes complications, nephropathy, retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, or restricted memory performance or for a restricted ability to learn, or the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.

    Abstract translation: 本发明涉及根据通式（I）的化合物，其中R 1 -R 4具有本说明书中给出的含义，A为CH 2，CHOH或CH-（C 1 -C 3 - 烷基），B，C和D独立地为 CH 2或CH-（C 1 -C 3 - 烷基），R 5是可以被描述中所列取代基取代的芳基或杂芳基。 这些化合物可用于制备用于治疗心血管疾病，稳定或不稳定心绞痛，冠心病，Prinzmetal心绞痛，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，内皮功能障碍的药物 ，动脉粥样硬化，再狭窄，PTCA后的内皮损伤，高血压，原发性高血压，肺动脉高压，继发性高血压，肾血管性高血压，慢性肾小球肾炎，勃起功能障碍，室性心律失常，糖尿病，糖尿病并发症，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，骨质疏松症或记忆障碍受限或受限制的学习能力，或降低绝经后妇女的心血管危险或摄入避孕药后。

    HETEROARYLCYCLOPROPANECARBOXAMIDES AND THEIR USE AS PHARMACEUTICALS
    6.
    发明申请
    HETEROARYLCYCLOPROPANECARBOXAMIDES AND THEIR USE AS PHARMACEUTICALS 有权
    异环戊二烯氧化酶及其作为药物的用途

    公开(公告)号：US20100016278A1

    公开(公告)日：2010-01-21

    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: A61K31/4418 ,  C07D211/70 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/397 ,  A61P9/00 ,  A61P3/00 ,  A61P19/00 ,  A61P25/00

    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。

    Triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals
    10.
    发明授权
    Triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals 有权
    三氮杂和四氮杂蒽醌二酮衍生物，其制备及其作为药物的用途

    公开(公告)号：US07132536B2

    公开(公告)日：2006-11-07

    申请号：US10829064

    申请日：2004-04-21

    Applicant: Andreas Weichert ,  Hartmut Strobel ,  Paulus Wohlfart ,  Marcel Patek ,  Martin Smrcina ,  Aleksandra Weichsel

    Inventor： Andreas Weichert ,  Hartmut Strobel ,  Paulus Wohlfart ,  Marcel Patek ,  Martin Smrcina ,  Aleksandra Weichsel

    IPC: C07D471/14

    CPC classification number: C07D471/14 ,  C07D487/04

    Abstract: The present invention relates to triaza- and tetraaza-anthracenedione derivatives of the formula I, wherein A, B and R1 to R5 are as defined herein. The compounds of formula I are valuable pharmacologically active compounds. They are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (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 furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    Abstract translation: 本发明涉及式I的三氮杂和四氮杂蒽并二酮衍生物，其中A，B和R 1至R 5如本文所定义。 式I的化合物是有价值的药理活性化合物。 它们可用于治疗各种疾病状态，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。 它们上调酶内皮一氧化氮（NO）合酶的表达，并且可以在需要所述酶的增加的表达或增加的NO水平或降低的NO水平的归一化的条件下应用。 本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

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