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127 条记录 (耗时 0.029 秒)

    Substituted thiophenes: compositions, processes of making, and uses in disease treatment and diagnosis
    72.
    发明申请
    Substituted thiophenes: compositions, processes of making, and uses in disease treatment and diagnosis 有权
    取代的噻吩：组合物，制备方法和用于疾病治疗和诊断中的用途

    公开(公告)号：US20040006119A1

    公开(公告)日：2004-01-08

    申请号：US10448851

    申请日：2003-05-30

    申请人： Aventis Pharma Deutschland GmbH

    发明人： Hans-Jochen Lang ,  Uwe Heinelt ,  Armin Hofmeister ,  Klaus Wirth ,  Michael Gekle ,  Markus Bleich

    IPC分类号： A61K031/4178 ,  C07D49/02

    CPC分类号： C07D409/12 ,  A61K31/4184 ,  A61K31/454

    摘要： Substituted thiophenes, processes for their preparation, their use as medicament or diagnostic agent. The substituted thiophene derivatives have the following backbone structure: 1 Medicaments comprising compounds of this type are of use for preventing or treating various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.

    摘要翻译： 取代的噻吩，其制备方法，其用作药物或诊断剂。 取代的噻吩衍生物具有以下骨架结构：包含这种类型的化合物的药物可用于预防或治疗各种疾病，例如呼吸障碍和打鼾，急性和慢性疾病，由缺血和/或再灌注事件诱导的疾病，以及由 增生或纤维化事件，中枢神经系统疾病和脂质代谢，糖尿病，凝血和寄生虫感染。

    Cephaibols: novel antiparasitics from Acremonium tubakii, process for their production, and use thereof
    73.
    发明申请
    Cephaibols: novel antiparasitics from Acremonium tubakii, process for their production, and use thereof 有权
    头孢唑醇：来自Acremonium tubakii的新型抗寄生虫药，其生产方法及其用途

    公开(公告)号：US20030203848A1

    公开(公告)日：2003-10-30

    申请号：US10411144

    申请日：2003-04-11

    申请人： Aventis Pharma Deutschland GmbH

    发明人： Laszlo Vertesy ,  Michael Kurz ,  Matthias Schiell ,  Joachim Hofmann

    IPC分类号： A61K038/10 ,  C07K007/08

    CPC分类号： C07K7/08 ,  A61K38/00

    摘要： The invention relates to compounds of the formula I AcPhe-Aib-Aib-Aib-x-w-Leu-y-Aib-Hyp-Gln-z-Hyp-Aib-Pro-Rnullnull(I) in which R is Phe-ol or Phe-al and w, x, y, and z have the following meanings: a) w is Gly or Ala; x is Aib and y and z are Iva; b) w is Gly; x, y and z are Iva; c) w is Gly; x and z are Aib and y is Iva; d) w is Gly; x, y and z are Aib; or e) w is Gly; x and y are Aib and z is Iva; or of the formula II AcPhe-Iva-Gln-Aib-lle-Thr-Aib-Leu-Aib-x-Gln-Aib-Hyp-Aib-Pro-Phe-Sernullnull(II), wherein x is Hyp or Pro, which are synthesized by Acremonium tubakii FH 1685 DSM 12774 during fermentation and released into the culture medium, a process for the isolation of the cephaibols from the culture medium, and their purification, and the use of the cephaibols as pharmacologically active compounds, in particular for the control of parasites.

    摘要翻译： 本发明涉及式ⅠAcPhe-Aib-Aib-Aib-xw-Leu-y-Aib-Hyp-Gln-z-Hyp-Aib-Pro-R（Ⅰ）的化合物，其中R是Phe-ol或Phe -al和w，x，y和z具有以下含义：a）w是Gly或Ala; x是Aib，y和z是Iva; b）w是Gly; x，y和z是Iva; c）w是Gly; x和z是Aib，y是Iva; d）w是Gly; x，y和z是Aib; 或e）w是Gly; x和y是Aib，z是Iva; 或式II AcPhe-Iva-Gln-Aib-Lle-Thr-Aib-Leu-Aib-x-Gln-Aib-Hyp-Aib-Pro-Phe-Ser（II），其中x是Hyp或Pro， 在发酵过程中由Acremonium tubakii FH 1685 DSM 12774合成并释放到培养基中，从培养基中分离头孢胆素的方法及其纯化，以及使用头孢吡肟作为药理学活性化合物，特别是用于 控制寄生虫。

    Gabusectin derivatives, processes for preparing them and their use
    74.
    发明申请
    Gabusectin derivatives, processes for preparing them and their use 失效
    Gabusectin衍生物，其制备方法及其用途

    公开(公告)号：US20030187057A1

    公开(公告)日：2003-10-02

    申请号：US10290607

    申请日：2002-11-08

    申请人： Aventis Pharma Deutschland GmbH

    发明人： Matthias Schiell ,  Martin Knauf ,  Luigi Toti ,  Astrid Markus-Erb

    IPC分类号： A61K031/4015 ,  C07D207/273 ,  C12N001/20

    CPC分类号： C07D207/44

    摘要： The present invention relates to a compound of formula (I) 1 wherein the R, R2, R3, R4, R5, X, X2, X3, X4 and X5 are as defined herein, which are formed by the microorganism ST 003236 (DSM 14476) during fermentation, to a process for preparing and derivatizing the compound, to a pharmaceutical which comprises the compound and to a method for the treatment or prophylaxis of an infectious disease caused by bacteria comprising administering a pharmaceutically effective amount of the compound.

    摘要翻译： 本发明涉及式（I）化合物，其中R，R2，R3，R4，R5，X，X2，X3，X4和X5如本文所定义，由微生物ST 003236（DSM14476）形成， 在发酵过程中，涉及制备和衍生化合物的方法，涉及包含该化合物的药物和用于治疗或预防由细菌引起的感染性疾病的方法，包括施用药学有效量的该化合物。

    Novel N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
    76.
    发明申请
    Novel N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them 有权
    新型N-胍基烷基酰胺，其制备方法，用途及包含它们的药物制剂

    公开(公告)号：US20030162967A1

    公开(公告)日：2003-08-28

    申请号：US10227222

    申请日：2002-08-26

    申请人： Aventis Pharma Deutschland GmbH

    发明人： Otmar Klingler ,  Gerhard Zoller ,  Elisabeth Defossa ,  Fahad A. Al-Obeidi ,  Armin Walser ,  James Ostrem

    IPC分类号： C07D417/02 ,  C07D413/02 ,  C07D43/02 ,  C07C237/38

    CPC分类号： C07D213/30 ,  C07C279/14 ,  C07D213/40 ,  C07D215/48 ,  C07D239/28

    摘要： The present invention relates to compounds of the formula I, 1 in which A, L, Y, and k have the meanings indicated in the specification and claims. 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 and/or factor VIIa 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 conditions in 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 1, 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A，L，Y和k具有说明书和权利要求书中所示的含义。 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和/或因子VIIa的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望的活性的条件或用于治愈或预防其中 旨在抑制因子Xa和/或因子VIIa。 本发明还涉及制备式1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。

    1-(p-thienylbenzyl)imidazoles as agonists of angiotensin (1-7) receptors, processes for their preparation, their use, and pharmaceutical prepartions comprising them
    78.
    发明申请
    1-(p-thienylbenzyl)imidazoles as agonists of angiotensin (1-7) receptors, processes for their preparation, their use, and pharmaceutical prepartions comprising them 审中-公开
    1-（对噻吩基苄基）咪唑作为血管紧张素（1-7）受体的激动剂，其制备方法及其用途和药物制剂包含它们

    公开(公告)号：US20020077344A1

    公开(公告)日：2002-06-20

    申请号：US10013459

    申请日：2001-12-13

    申请人： Aventis Pharma Deutschland GmbH

    发明人： Holger Heitsch ,  Gabriele Wiemer

    IPC分类号： A61K031/4155 ,  C07D49/02

    CPC分类号： C07D409/10

    摘要： The invention relates to novel 1-(p-thienylbenzyl)imidazoles of formula (I) 1 where the radicals R(1) to R(6), X, and Y have the meaning indicated in the description, which are potent agonists of angiotensin (1-7) receptors and owing to the production and release of the vasorelaxant, antithrombotic, and cardioprotective messengers cyclic 3null,5null-guanosine monophosphate (cGMP) and nitrogen monoxide (NO) associated with the stimulation of these receptors on endothelial cells are valuable pharmaceuticals for the treatment and prophylaxis of high blood pressure, cardiac hypertrophy, cardiac insufficiency, coronary heart diseases such as angina pectoris, cardiac infarct, vascular restenosis after angioplasty, cardiomyopathies, endothelial dysfunction or endothelial damage, e.g., as a result of arteriosclerotic processes or diabetes mellitus, and also of arterial and venous thromboses.

    摘要翻译： 本发明涉及式（I）的新型1-（对噻吩基苄基）咪唑，其中基团R（1）至R（6），X和Y具有描述中指出的含义，其是血管紧张素的有效激动剂 1-7）受体，并且由于与内皮细胞上的这些受体的刺激相关的环状3'，5'-鸟苷一磷酸（cGMP）和一氧化氮（NO）的血管舒张剂，抗血栓形成和心脏保护性信使的产生和释放， 用于治疗和预防高血压，心脏肥大，心功能不全，冠心病如心绞痛，心肌梗塞，血管成形术后血管再狭窄，心肌病，内皮功能障碍或内皮损伤的有价值药物，例如作为动脉硬化过程的结果 或糖尿病，以及动脉和静脉血栓形成。

    1-(p-thienylbenzyl)imidazoles as agonists of angiotensin (1-7) receptors, processes for their preparation, their use, and pharmaceutical preparations comprising them
    80.
    发明申请
    1-(p-thienylbenzyl)imidazoles as agonists of angiotensin (1-7) receptors, processes for their preparation, their use, and pharmaceutical preparations comprising them 有权
    1-（对噻吩基苄基）咪唑作为血管紧张素（1-7）受体的激动剂，其制备方法及其应用，以及包含它们的药物制剂

    公开(公告)号：US20010018449A1

    公开(公告)日：2001-08-30

    申请号：US09809008

    申请日：2001-03-16

    申请人： Aventis Pharma Deutschland GmbH

    发明人： Holger Heitsch ,  Gabriele Wiemer

    IPC分类号： A61K031/4184 ,  C07D233/54

    CPC分类号： C07D409/10

    摘要： The invention relates to novel 1-(p-thienylbenzyl)imidazoles of formula (I) 1 where the radicals R(1) to R(6), X, and Y have the meaning indicated in the description, which are potent agonists of angiotensin (1-7) receptors and owing to the production and release of the vasorelaxant, antithrombotic, and cardioprotective messengers cyclic 3null,5null-guanosine monophosphate (cGMP) and nitrogen monoxide (NO) associated with the stimulation of these receptors on endothelial cells are valuable pharmaceuticals for the treatment and prophylaxis of high blood pressure, cardiac hypertrophy, cardiac insufficiency, coronary heart diseases such as angina pectoris, cardiac infarct, vascular restenosis after angioplasty, cardiomyopathies, endothelial dysfunction or endothelial damage, e.g., as a result of arteriosclerotic processes or diabetes mellitus, and also of arterial and venous thromboses.

    摘要翻译： 本发明涉及式（I）的新型1-（对噻吩基苄基）咪唑，其中基团R（1）至R（6），X和Y具有描述中指出的含义，其是血管紧张素的有效激动剂 1-7）受体，并且由于与内皮细胞上的这些受体的刺激相关的环状3'，5'-鸟苷一磷酸（cGMP）和一氧化氮（NO）的血管舒张剂，抗血栓形成和心脏保护性信使的产生和释放， 用于治疗和预防高血压，心脏肥大，心功能不全，冠心病如心绞痛，心肌梗塞，血管成形术后血管再狭窄，心肌病，内皮功能障碍或内皮损伤的有价值药物，例如作为动脉硬化过程的结果 或糖尿病，以及动脉和静脉血栓形成。