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    Polyamide nucleic acid derivatives, and agents, and processes for preparing them
    1.
    发明申请
    Polyamide nucleic acid derivatives, and agents, and processes for preparing them 有权
    聚酰胺核酸衍生物和试剂，及其制备方法

    公开(公告)号：US20040265885A1

    公开(公告)日：2004-12-30

    申请号：US10863999

    申请日：2004-06-09

    申请人： Aventis Pharma Deutschland GmbH

    发明人： Eugen Uhlmann ,  Gerhard Breipohl ,  David William Will

    IPC分类号： C12Q001/68 ,  C07K014/00 ,  A61K048/00

    CPC分类号： C07H21/00

    摘要： The present invention relates to PNA derivatives which carry, at the N terminus of the PNA backbone, a phosphoryl radical. The phosphoryl radical can be, for example, a phosphate radical, or a substituted phosphoryl radical, with substituted phosphoryl derivatives carrying, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the abovementioned PNA derivatives and to their use as pharmaceuticals and diagnostic agents.

    Triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals
    2.
    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。

    Use of antagonists of the bradykinin B2 receptor for the treatment of osteoarthrosis
    3.
    发明申请
    Use of antagonists of the bradykinin B2 receptor for the treatment of osteoarthrosis 审中-公开
    使用缓激肽B2受体拮抗剂治疗骨关节病

    公开(公告)号：US20040248809A1

    公开(公告)日：2004-12-09

    申请号：US10773772

    申请日：2004-02-06

    申请人： Aventis Pharma Deutschland GmbH

    发明人： Martin Michaelis ,  Karl Rudolphi

    IPC分类号： A61K038/08

    CPC分类号： A61K38/08

    摘要： Peptides having bradykinin-antagonistic action are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases in whose course an increased activity of matrix metalloproteinases is involved. These include diseases such as degenerative joint diseases, for example osteoarthrosis, spondylosis and chondroporosis after joint trauma or relatively long immobilization of a joint after meniscus or patella injuries or torn ligaments. The invention therefore relates to the use of a compound of the formula I, A-B-X-E-F-K-(D)-TIC-G-M-Fnull-Inullnull(I) for the production of pharmaceuticals for the treatment of degenerative joint diseases, wherein A, B, X, E, F, K, (D)-TIC, G, M, Fnull and I are as defined herein.

    摘要翻译： 具有缓激肽拮抗作用的肽适用于生产用于预防和治疗涉及基质金属蛋白酶活性升高的疾病的药物。 这些疾病包括诸如退行性关节疾病之类的疾病，例如在关节创伤之后的关节骨关节病，脊椎软骨病和软骨病，或者在弯液面或髌骨损伤或撕裂的韧带之后关节相对较长的固定。 因此，本发明涉及式I化合物ABXEFK-（D）-TIC-GM-F'-I（I）用于制备用于治疗退行性关节病的药物，其中A，B， X，E，F，K，（D）-TIC，G，M，F'和I如本文所定义。

    Indazole-derivatives as factor Xa inhibitors
    5.
    发明申请
    Indazole-derivatives as factor Xa inhibitors 有权
    吲唑衍生物作为因子Xa抑制剂

    公开(公告)号：US20040235824A1

    公开(公告)日：2004-11-25

    申请号：US10849088

    申请日：2004-05-19

    申请人： Aventis Pharma Deutschland GmbH

    发明人： Marc Nazare ,  Volkmar Wehner ,  Volker Laux ,  Matthias Urmann ,  Armin Bauer ,  Hans Matter

    IPC分类号： A61K031/55 ,  A61K031/541 ,  A61K031/5377 ,  A61K031/501

    CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14

    摘要： The present invention relates to a compound of the formula I 1 wherein J1, J2, R0, R1, R2, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. 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化合物，其中J 1，J 2，R 0，R 1，R 2，Q，V，G和M如本文所定义。 式I的化合物是有价值的药理活性化合物。 它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望活性或用于治愈 或预防因子Xa和/或因子VIIa的抑制。 本发明还涉及制备式I化合物的方法，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。