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    Benzimidazole-derivatives as factor Xa inhibitors
    1.
    发明授权
    Benzimidazole-derivatives as factor Xa inhibitors 有权
    苯并咪唑衍生物作为因子Xa抑制剂

    公开(公告)号：US07741341B2

    公开(公告)日：2010-06-22

    申请号：US10849436

    申请日：2004-05-19

    申请人： Marc Nazare ,  Michael Wagner ,  Volkmar Wehner ,  Hans Matter ,  Matthias Urmann ,  Kurt Ritter

    发明人： Marc Nazare ,  Michael Wagner ,  Volkmar Wehner ,  Hans Matter ,  Matthias Urmann ,  Kurt Ritter

    IPC分类号： A61K31/4523 ,  C07D401/14 ,  C07D409/14

    CPC分类号： C07D235/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/08 ,  C07D495/04

    摘要： The present invention relates to compounds of the formula I, wherein 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。

    Azaindole-Derivatives As Factor Xa Inhibitors
    3.
    发明申请
    Azaindole-Derivatives As Factor Xa Inhibitors 审中-公开
    阿魏酸衍生物作为因子Xa抑制剂

    公开(公告)号：US20080280946A1

    公开(公告)日：2008-11-13

    申请号：US11934177

    申请日：2007-11-02

    申请人： Marc NAZARE ,  Volkmar Wehner ,  David William Will ,  Kurt Ritter ,  Matthias Urmann ,  Hans Matter

    发明人： Marc NAZARE ,  Volkmar Wehner ,  David William Will ,  Kurt Ritter ,  Matthias Urmann ,  Hans Matter

    IPC分类号： A61K31/437 ,  C07D471/02 ,  A61P7/00 ,  A61P9/00

    CPC分类号： C07D471/04

    摘要： Indazole-derivatives as factor Xa inhibitors The present invention relates to compounds of the formula I wherein R0, R1, R2, R3, 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 VIa 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： 作为因子Xa抑制剂的吲唑衍生物本发明涉及式I化合物，其中R 0，R 1，R 2，R 2， SEQ ID NO 3，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VIa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。

    Azaindole-derivatives as factor Xa inhibitors
    4.
    发明申请
    Azaindole-derivatives as factor Xa inhibitors 有权
    Azaindole衍生物作为因子Xa抑制剂

    公开(公告)号：US20050009828A1

    公开(公告)日：2005-01-13

    申请号：US10849089

    申请日：2004-05-19

    申请人： Marc Nazare ,  Volkmar Wehner ,  David Will ,  Kurt Ritter ,  Matthias Urmann ,  Hans Matter

    发明人： Marc Nazare ,  Volkmar Wehner ,  David Will ,  Kurt Ritter ,  Matthias Urmann ,  Hans Matter

    IPC分类号： C07D471/04 ,  A61K31/525 ,  A61K31/517 ,  A61K31/52

    CPC分类号： C07D471/04

    摘要： The present invention relates to compounds of the formula I wherein R0, R1, R2, R3, 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R 0，R 1，R 2，R 3，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。

    Azaindole-derivatives as factor Xa inhibitors
    5.
    发明授权
    Azaindole-derivatives as factor Xa inhibitors 有权
    Azaindole衍生物作为因子Xa抑制剂

    公开(公告)号：US07317027B2

    公开(公告)日：2008-01-08

    申请号：US10849089

    申请日：2004-05-19

    申请人： Marc Nazare ,  Volkmar Wehner ,  David William Will ,  Kurt Ritter ,  Matthias Urmann ,  Hans Matter

    发明人： Marc Nazare ,  Volkmar Wehner ,  David William Will ,  Kurt Ritter ,  Matthias Urmann ,  Hans Matter

    IPC分类号： A61K31/44 ,  C07D401/00

    CPC分类号： C07D471/04

    摘要： The present invention relates to compounds of the formula I wherein R0, R1, R2, R3, 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R 0，R 1，R 2，R 3，R 3， ，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。

    Pyrrole-derivatives as factor Xa inhibitors
    6.
    发明授权
    Pyrrole-derivatives as factor Xa inhibitors 有权
    吡咯衍生物作为因子Xa抑制剂

    公开(公告)号：US07465806B2

    公开(公告)日：2008-12-16

    申请号：US11467277

    申请日：2006-08-25

    申请人： Armin Bauer ,  Michael Wagner ,  Marc Nazare ,  Volkmar Wehner ,  Matthias Urmann ,  Hans Matter

    发明人： Armin Bauer ,  Michael Wagner ,  Marc Nazare ,  Volkmar Wehner ,  Matthias Urmann ,  Hans Matter

    IPC分类号： C07D261/06 ,  C07D207/32

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

    摘要： The present invention relates to compounds of the formulae I and Ia, wherein R0; R1; R3; R4; R22, Q; V, G and M have the meanings indicated in the claims. The compounds of the formulae I and Ia are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable 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 formulae I and Ia, 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和Ia的化合物，其中R 0; R1; R3; R4; R22，Q; V，G和M具有权利要求中所示的含义。 式I和Ia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，适用于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和Ia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。

    Beta-Aminoacid-Derivatives As Factor Xa Inhibitors
    7.
    发明申请
    Beta-Aminoacid-Derivatives As Factor Xa Inhibitors 审中-公开
    β-氨基酸衍生物作为因子Xa抑制剂

    公开(公告)号：US20070179122A1

    公开(公告)日：2007-08-02

    申请号：US11469513

    申请日：2006-09-01

    申请人： Matthias Urmann ,  Marc Nazare ,  Volkmar Wehner ,  Hans Matter ,  Armin Bauer ,  Michael Wagner

    发明人： Matthias Urmann ,  Marc Nazare ,  Volkmar Wehner ,  Hans Matter ,  Armin Bauer ,  Michael Wagner

    IPC分类号： A61K31/553 ,  A61K31/551 ,  A61K31/55 ,  A61K31/541 ,  A61K31/496 ,  A61K31/5377 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07K5/0202 ,  C07D265/32 ,  C07D265/33 ,  C07D291/06 ,  C07D295/112 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D419/12

    摘要： The present invention relates to compounds of the formula I, in which R0; R1; R2; R3; R4; R5, R, Q; V, G and M have the meanings indicated in the 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 thromboemboic 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R 0， R＆lt; 1＆gt;; R 2; 3＆lt; 3＆gt; R 4; R 5，R，Q; V，G和M具有权利要求中所示的含义。 式I的化合物是有价值的药理活性化合物。 它们表现出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。

    Indazole-derivatives as factor Xa inhibitors
    9.
    发明授权
    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：US07365088B2

    公开(公告)日：2008-04-29

    申请号：US10849088

    申请日：2004-05-19

    申请人： Marc Nazare ,  Volkmar Wehner ,  Volker Laux ,  Matthias Urmann ,  Armin Bauer ,  Hans Matter

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

    IPC分类号： A16K31/42 ,  A16K31/4152 ,  C07D261/20 ,  C07D413/14

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

    摘要： The present invention relates to a compound of the formula I 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，O 2， >，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。

    Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles
    10.
    发明授权
    Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles 有权
    苯并咪唑和氮杂苯并咪唑的区域选择性钯催化合成

    公开(公告)号：US08188282B2

    公开(公告)日：2012-05-29

    申请号：US12353271

    申请日：2009-01-14

    申请人： Jorge Alonso ,  Andreas Lindenschmidt ,  Marc Nazare ,  Nis Halland ,  Omar Rkyek ,  Matthias Urmann

    发明人： Jorge Alonso ,  Andreas Lindenschmidt ,  Marc Nazare ,  Nis Halland ,  Omar Rkyek ,  Matthias Urmann

    IPC分类号： C07D513/02 ,  C07D235/00

    CPC分类号： C07D235/10 ,  C07D235/08 ,  C07D235/16 ,  C07D401/04 ,  C07D471/04

    摘要： The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.

    摘要翻译： 本发明涉及一种用于区域选择性合成式I化合物的方法，其中R 0; R1; R2; R3; R4; R5; A1; A2; A3; A4，Q和J具有权利要求中所示的含义。 本发明提供了直接钯催化的区域选择性方法，用于从2-卤代 - 硝基芳烃和用于制备药物，诊断剂的N-取代酰胺开始的各种不对称，多官能的取代的苯并咪唑或式I的氮杂苯并咪唑， 液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。