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59 条记录 (耗时 0.042 秒)

    N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
    41.
    发明授权
    N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them 有权
    N-胍基烷基酰胺，它们的制备方法，它们的用途以及包含它们的药物制剂

    公开(公告)号：US06472562B1

    公开(公告)日：2002-10-29

    申请号：US09697188

    申请日：2000-10-27

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

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

    IPC分类号： C07C23305

    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, 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 I, their use, in particular 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的不需要的活性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I化合物，其用途，特别是药物中的活性成分以及包含它们的药物制剂的方法。

    Factor VIIa inhibitors
    44.
    发明授权
    Factor VIIa inhibitors 有权
    因子VIIa抑制剂

    公开(公告)号：US06500803B1

    公开(公告)日：2002-12-31

    申请号：US09588651

    申请日：2000-06-07

    申请人： Otmar Klingler ,  Manfred Schudok ,  Gerhard Zoller ,  Uwe Heinelt ,  Elisabeth Defossa ,  Hans Matter ,  Pavel Safar

    发明人： Otmar Klingler ,  Manfred Schudok ,  Gerhard Zoller ,  Uwe Heinelt ,  Elisabeth Defossa ,  Hans Matter ,  Pavel Safar

    IPC分类号： A61K3805

    CPC分类号： C07K5/06086 ,  A61K38/00

    摘要： The present invention relates to compounds of formula I, in which R1, R2, R91, R92, R93, R94, R95, R96, R97, r, s, and t have the meanings indicated in the claims. Compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of 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R1，R2，R91，R92，R93，R94，R95，R96，R97，r，s和t具有权利要求中所示的含义。 式I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血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa活性的条件下或用于治疗或预防预期因子VIIa的抑制的病症。 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。

    Indole derivatives as inhibitors or factor Xa
    45.
    发明授权
    Indole derivatives as inhibitors or factor Xa 有权
    吲哚衍生物作为抑制剂或因子Xa

    公开(公告)号：US06337344B1

    公开(公告)日：2002-01-08

    申请号：US09582344

    申请日：2000-08-14

    申请人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose ,  Hans Matter

    发明人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose ,  Hans Matter

    IPC分类号： A61K3144

    CPC分类号： C07D401/06 ,  C07D209/42 ,  C07D401/12 ,  C07D403/10 ,  C07D471/04

    摘要： The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R1a, R1b, R1c R1d, R2, R3, R4 and A are defined as indicated in the claims. The compounds of formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to use of the compounds of formula (I) in the treatment and prophylaxis of diseases which can be cured or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (I) in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (I) together with pharmaceutically acceptable carrier substances and/or auxiliary substances.

    摘要翻译： 本发明涉及抑制血液凝固蛋白质，更具体地说，涉及式（I）的吲哚衍生物，其中R1a，R1b，R1c R1d，R2，R3，R4和A如权利要求中所示定义。 式（I）的化合物是凝血酶因子Xa的抑制剂。 本发明还涉及制备式（I）化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，使用式（I）化合物治疗和预防可以 通过抑制诸如血栓栓塞性疾病的因子Xa活性而被治愈或预防，以及式（I）化合物在制备用于这些疾病的药物中的用途。 本发明还涉及包含与惰性载体混合或以其它方式结合的式（I）化合物的组合物，特别是含有式（I）化合物与药学上可接受的载体物质和/或辅助物质的药物组合物。

    Diastereomers of 1-(isopropoxycarbonyloxy) ethyl 3-cephem 4-carboxylate
    47.
    发明授权
    Diastereomers of 1-(isopropoxycarbonyloxy) ethyl 3-cephem 4-carboxylate 失效
    1-（异丙氧基羰基氧基）乙基3-头孢烯-4-羧酸酯的非对映异构体

    公开(公告)号：US5550232A

    公开(公告)日：1996-08-27

    申请号：US447229

    申请日：1995-05-22

    申请人： Gerd Fischer ,  Elisabeth Defossa ,  Uwe Gerlach ,  Rolf H orlein ,  Norbert Krass ,  Rudolf Lattrell ,  Ulrich Stache ,  Theodor Wollmann ,  Dieter Isert

    发明人： Gerd Fischer ,  Elisabeth Defossa ,  Uwe Gerlach ,  Rolf H orlein ,  Norbert Krass ,  Rudolf Lattrell ,  Ulrich Stache ,  Theodor Wollmann ,  Dieter Isert

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/06 ,  C07D501/34 ,  C07D501/56 ,  C07D501/14

    CPC分类号： C07D501/00

    摘要： Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(methoxymethyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.2-2 equivalents of a solution of the acid component HY and separating it off by filtration, then precipitating the more readily soluble diastereomer of the formula IV from the filtration solution, it being possible for the acid component HY to be identical or different in the consecutive partial steps and any desired sequence of addition of different acid components HY being possible, and optionally further purifying the obtained salts by crystallization, are described.

    摘要翻译： 1-（异丙氧羰基氧基）乙基（6R，7R）-7- [2-（2-氨基噻唑-4-基）-2-（Z） - （甲氧基亚氨基）乙酰氨基] -3-（甲氧基甲基）-3 式I的化合物 - 头孢烯-4-羧酸酯及其生理学上可接受的盐以及式II化合物的非对映体纯盐，其中HX是单或多元酸，其中X是无机或有机的 生理学上可接受的阴离子，以及制备这些式I或II化合物的方法，其包括首先将式IV的较微溶的非对映体沉淀在1当量的式（I）的非对映体混合物的溶液中， III与0.2-2当量的酸组分HY的溶液并通过过滤分离，然后从过滤溶液中沉淀出更容易溶解的式IV的非对映异构体，酸组分HY可能相同或不同 在一起 描述了部分步骤和任何期望的不同酸组分HY的加入顺序是可能的，并且任选地通过结晶进一步纯化得到的盐。