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    Triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals
    1.
    发明申请
    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：US20040248900A1

    公开(公告)日：2004-12-09

    申请号：US10829064

    申请日：2004-04-21

    申请人： Aventis Pharma Deutschland GmbH

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

    IPC分类号： A61K031/519 ,  C07D487/14

    CPC分类号： C07D471/14 ,  C07D487/04

    摘要： The present invention relates to triaza- and tetraaza-anthracenedione derivatives of the formula I, 1 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.

    摘要翻译： 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。

    Acylated 6,7,8,9-tetrahydro-5H-benzocycloheptenyl amines and their use as pharmaceutical agents
    5.
    发明申请
    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：US20040225013A1

    公开(公告)日：2004-11-11

    申请号：US10859773

    申请日：2004-06-03

    申请人： AVENTIS PHARMA DEUTSCHLAND GMBH

    发明人： Hartmut Strobel ,  Paulus Wohlfart

    IPC分类号： A61K031/195 ,  A61K031/16

    CPC分类号： C07C235/54 ,  C07C233/65 ,  C07C233/74 ,  C07C2602/12

    摘要： The present invention relates to compounds according to the general formula (I), 1 wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CHnull(C1-C3-alkyl), B, C and D are independently CH2 or CHnull(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.

    摘要翻译： 本发明涉及根据通式（I）的化合物，其中R 1 -R 4具有说明书中给出的含义，A是CH 2，CHOH或CH-（C 1 -C 3 - 烷基），B ，C和D独立地是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。

    4-Fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical
    7.
    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：US20040019114A1

    公开(公告)日：2004-01-29

    申请号：US10623775

    申请日：2003-07-22

    申请人： Aventis Pharma Deutschland GmbH

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

    IPC分类号： A61K031/165

    CPC分类号： C07C233/65 ,  A61K31/166 ,  C07C2602/08

    摘要： 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) 1 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.

    摘要翻译： 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。