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    Azaindole-derivatives as factor Xa inhibitors
    21.
    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

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

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

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

    CPC classification number: C07D471/04

    Abstract: 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.

    Abstract translation: 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。

    Sulfonamides with heterocycle and oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals
    22.
    发明授权
    Sulfonamides with heterocycle and oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals 有权
    磺酰胺与杂环和恶二唑酮头基，其制备方法及其用作药物

    公开(公告)号：US08716317B2

    公开(公告)日：2014-05-06

    申请号：US12997095

    申请日：2009-05-22

    Applicant: Stefanie Keil ,  Matthias Urmann ,  Maike Glien ,  Hans Matter ,  Harry Randall Munson, Jr. ,  Ulrike Wendler

    Inventor： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Maike Glien ,  Hans Matter ,  Harry Randall Munson, Jr.

    IPC: C07D413/14 ,  A61K31/4439 ,  A61K31/4245 ,  A61K31/381

    CPC classification number: C07D413/14

    Abstract: The invention relates to Sulfonamides with heterocycle and oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

    Abstract translation: 本发明涉及具有杂环和恶二唑酮头基的磺酰胺及其生理上可接受的盐和生理功能衍生物，其显示PPARδ或PPARα和PPARα激动剂活性。 所描述的是式（I）的化合物，其中自由基如所定义，以及它们的生理上可接受的盐及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及其中涉及胰岛素抵抗和中枢神经和周围神经系统的脱髓鞘和其它神经变性疾病的疾病。

    4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, pharmaceutical compositions and methods for their therapeutic use
    26.
    发明授权
    4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, pharmaceutical compositions and methods for their therapeutic use 有权
    4-氧基-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺，其治疗用途的药物组合物和方法

    公开(公告)号：US07910612B2

    公开(公告)日：2011-03-22

    申请号：US12062769

    申请日：2008-04-04

    Applicant: Stefanie Keil ,  Karl Schoenafinger ,  Hans Matter ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Hans-Ludwig Schaefer ,  Eugen Falk

    Inventor： Stefanie Keil ,  Karl Schoenafinger ,  Hans Matter ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Hans-Ludwig Schaefer ,  Eugen Falk

    IPC: A61K31/433 ,  C07D285/12

    CPC classification number: C07D285/135 ,  C07D417/12

    Abstract: The present invention comprises 4-Oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, the derivatives thereof and salts thereof as well as processes for their preparation and methods for their use as pharmaceutical compositions. More specifically, the invention relates to 4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) PPARalpha, PPARdelta and PPARgamma agonist activity. The compounds themselves are defined by the structure of the formula I, wherein the various unnamed substituents are defined herein. The compounds are suitable for the treatment of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

    Abstract translation: 本发明包括4-氧基-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其衍生物及其盐，以及其制备方法及其用作药物组合物的方法。 更具体地，本发明涉及4-氧-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其生理上可接受的盐和生理功能衍生物，其表现出过氧化物酶体增殖物激活受体（PPAR）PPARα， PPARδ和PPARgamma激动剂活性。 化合物本身由式I的结构定义，其中各种未命名的取代基在本文中定义。 该化合物适用于治疗脂肪酸代谢紊乱和葡萄糖利用障碍以及涉及胰岛素抵抗的疾病以及中枢和周围神经系统的脱髓鞘和其它神经变性疾病。

    Transition metal catalyzed synthesis of N-aminoindoles
    28.
    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

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

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

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

    CPC classification number: C07D209/08

    Abstract: 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.

    Abstract translation: 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。

    Derivatives of 2-aminothiazoles and 2-amino-oxazoles, processes for their preparation and their use as pharmaceutical compositions
    29.
    发明授权
    Derivatives of 2-aminothiazoles and 2-amino-oxazoles, processes for their preparation and their use as pharmaceutical compositions 有权
    2-氨基噻唑和2-氨基 - 恶唑的衍生物，其制备方法及其作为药物组合物的用途

    公开(公告)号：US07655679B2

    公开(公告)日：2010-02-02

    申请号：US12055771

    申请日：2008-03-26

    Applicant: Stefanie Keil ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Karen Chandross ,  Lan Lee

    Inventor： Stefanie Keil ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Karen Chandross ,  Lan Lee

    IPC: A61K31/4025 ,  C07D413/10

    CPC classification number: C07D413/12 ,  C07D417/12

    Abstract: The present invention relates to derivatives of 2-aminothiazoles and 2-aminooxazoles in all its stereoisomeric forms, enantiomeric forms and mixtures in any ratio, and its physiologically acceptable salts and tautomeric forms showing peroxisome proliferators activator receptor (PPAR) delta agonist activity. These compounds are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

    Abstract translation: 本发明涉及所有其立体异构形式的2-氨基噻唑和2-氨基恶唑衍生物，对映体形式和任何比例的混合物，以及其生理上可接受的盐和互变异构体形式，其显示过氧化物酶体增殖物激活受体（PPAR）δ激动剂活性。 这些化合物是式I化合物，其中基团如上所定义，以及它们的生理上可接受的盐及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及其中涉及胰岛素抵抗和中枢神经和周围神经系统的脱髓鞘和其它神经变性疾病的疾病。

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