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    Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles
    1.
    发明申请
    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：US20090203912A1

    公开(公告)日：2009-08-13

    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： C07D471/04 ,  C07D235/08

    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。

    Transition metal catalyzed synthesis of N-aminoindoles
    6.
    发明申请
    Transition metal catalyzed synthesis of N-aminoindoles 有权
    过渡金属催化N-氨基吲哚的合成

    公开(公告)号：US20100168429A1

    公开(公告)日：2010-07-01

    申请号：US12576339

    申请日：2009-10-09

    申请人： Nis HALLAND ,  Marc NAZARE ,  Andreas LINDENSCHMIDT ,  Omar AKYEK ,  Matthias URMANN ,  Jorge ALONSO

    发明人： Nis HALLAND ,  Marc NAZARE ,  Andreas LINDENSCHMIDT ,  Omar AKYEK ,  Matthias URMANN ,  Jorge ALONSO

    IPC分类号： C07D471/04 ,  C07D209/04 ,  C07D401/04

    CPC分类号： C07D209/08

    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; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino-azaindoles of the formula I from 2-halo-phenylacetylenes or (2-sulfonato)phenyl-acetylenes and N,N-disubstituted hydrazines, 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; R6; A1; A2; A3; A4，Q，T和J具有权利要求中所示的含义。 本发明提供了从2-卤代 - 苯基乙炔或（2-磺酸根合）苯基 - 乙炔和N，N-二取代的，由式I表示的多种多官能N-氨基吲哚或N-氨基 - 氮杂吲哚的直接过渡金属催化方法 肼，可用于生产药物，诊断剂，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。

    N-[4-(1H-PYRAZOLO[3,4-b]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS
    7.
    发明申请
    N-[4-(1H-PYRAZOLO[3,4-b]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 审中-公开
    N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基] - 磺酰胺及其作为药物的用途

    公开(公告)号：US20130072493A1

    公开(公告)日：2013-03-21

    申请号：US13236027

    申请日：2011-09-19

    申请人： Marc NAZARE ,  Nis Halland ,  Friedemann Schmidt ,  Tilo Weiss ,  Uwe Dietz ,  Armin Hofmeister

    发明人： Marc NAZARE ,  Nis Halland ,  Friedemann Schmidt ,  Tilo Weiss ,  Uwe Dietz ,  Armin Hofmeister

    IPC分类号： A61K31/4985 ,  A61P19/02 ,  A61P19/04 ,  A61P9/10 ,  A61P9/00 ,  A61P43/00 ,  A61P29/00 ,  A61P35/00 ,  C07D487/04 ,  A61P3/10

    CPC分类号： A61K31/4985 ,  C07D487/04

    摘要： The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式I的N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基] - 磺酰胺，其中Ar，R 1，R 2和n具有如 索赔。 式I的化合物是调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶同工型1（SGK-1，SGK1）的活性的有价值的药理活性化合物，并且是 适合于治疗SGK活动不适当的疾病，例如退行性关节疾病或炎性过程如骨关节炎或风湿病。 本发明还涉及式I化合物的制备方法，它们作为药物的用途，以及包含它们的药物组合物。

    Azaindole-Derivatives As Factor Xa Inhibitors
    8.
    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。

    Pyrrole-Derivatives as Factor Xa Inhibitors
    10.
    发明申请
    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：US20070049573A1

    公开(公告)日：2007-03-01

    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： A61K31/553 ,  A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/52 ,  A61K31/4709 ,  A61K31/405 ,  A61K31/4025

    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， R＆lt; 1＆gt;; 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。