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    CYCLIC PEPTIDES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF THE PLATELET ADHESION
    2.
    发明申请
    CYCLIC PEPTIDES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF THE PLATELET ADHESION 有权
    循环肽，其制备及其作为平板胶粘剂的抑制剂

    公开(公告)号：US20140011734A1

    公开(公告)日：2014-01-09

    申请号：US13818444

    申请日：2011-07-27

    Applicant: Otmar Klingler ,  Horst Blum ,  Andreas Lindenschmidt ,  Hans Matter

    Inventor： Otmar Klingler ,  Horst Blum ,  Andreas Lindenschmidt ,  Hans Matter

    IPC: C07K7/64

    CPC classification number: C07K7/64 ,  A61K38/00 ,  C07K7/06 ,  C07K7/56

    Abstract: The present invention relates to compounds of the Formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, X1, X2, X3 and X4 have the meanings indicated in the claims, and which are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb), and are suitable, for example, for the therapy and prophylaxis of athero-thrombotic diseases. The invention furthermore relates to processes for the preparation of compounds of the Formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

    Abstract translation: 本发明涉及式（I）化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，R14，R15，R16，R17，R18 X1，X2，X3和X4具有权利要求中所示的含义，并且它们是有价值的药理活性化合物。 它们是血浆蛋白血管性血友病因子（vWF）和血小板受体糖蛋白Ib-IX-V复合物（GPIb）之间的相互作用的可逆抑制剂，并且适合于例如治疗和预防动脉粥样硬化血栓性疾病 。 本发明还涉及制备式（I）化合物，其用途，特别是作为药物中的活性成分的方法，以及包含它们的药物组合物。

    BICYCLIC ARYL-SULFONIC ACID [1,3,4]-THIADIAZOL-2-YL-AMIDES, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE
    6.
    发明申请
    BICYCLIC ARYL-SULFONIC ACID [1,3,4]-THIADIAZOL-2-YL-AMIDES, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE 有权
    双环芳烃磺酸[1,3,4] - 十二烷基-2-酰胺，其制备方法，药物组合物及其使用方法

    公开(公告)号：US20080293780A1

    公开(公告)日：2008-11-27

    申请号：US12062759

    申请日：2008-04-04

    Applicant: Karl SCHOENAFINGER ,  Stefanie KEIL ,  Matthias URMANN ,  Hans MATTER ,  Maike GLIEN ,  Wolfgang WENDLER

    Inventor： Karl SCHOENAFINGER ,  Stefanie KEIL ,  Matthias URMANN ,  Hans MATTER ,  Maike GLIEN ,  Wolfgang WENDLER

    IPC: A61K31/41 ,  C07D285/08 ,  A61P3/10

    CPC classification number: C07D417/12 ,  C07D285/135

    Abstract: The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

    Abstract translation: 本发明包括双环芳基磺酸[1,3,4] - 噻二唑-2-基 - 酰胺，它们的功能衍生物及其生理上可接受的盐和药物组合物，其表现出过氧化物酶体增殖物激活受体（PPAR）PPARδ 和PPARγ激动剂活性。 本发明化合物的结构由下式I定义，其中各种取代基在本文中定义，包括其生理上可接受的盐。 还公开了化合物制备的方法。 该化合物适用于治疗脂肪酸代谢和葡萄糖利用障碍，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他神经变性疾病。

    Azaindole-Derivatives As Factor Xa Inhibitors
    7.
    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

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

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

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

    CPC classification number: C07D471/04

    Abstract: 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.

    Abstract translation: 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。

    Thieno-imino acid derivatives for use as matrix metalloproteinase inhibitors
    8.
    发明授权
    Thieno-imino acid derivatives for use as matrix metalloproteinase inhibitors 有权
    噻吩并亚氨基酸衍生物用作基质金属蛋白酶抑制剂

    公开(公告)号：US07399770B2

    公开(公告)日：2008-07-15

    申请号：US11461189

    申请日：2006-07-31

    Applicant: Manfred Schudok ,  Hans Matter ,  Armin Hofmeister ,  Maxime Lampilas

    Inventor： Manfred Schudok ,  Hans Matter ,  Armin Hofmeister ,  Maxime Lampilas

    IPC: A61K31/4365 ,  C07D409/02 ,  C07D495/06

    CPC classification number: C07D495/04

    Abstract: The invention is directed to a compound of the formula I wherein the variables are as defined herein, or a stereoisomeric form thereof, mixture of stereoisomeric forms, in any ratio, or a salt thereof. Another aspect of the present invention is directed to a pharmaceutical composition comprising, a pharmaceutically effective amount of one or more compounds of formula I according to claim 1 in admixture with a pharmaceutically acceptable carrier.The invention is also directed to a method for effecting the prophylaxis and therapy of degenerative joint diseases such as osteoarthroses, spondyloses, cartilage loss following joint trauma or a relatively long period of joint immobilization following meniscus or patella injuries or ligament ruptures, diseases of the connective tissue such as collagenoses, periodontal diseases, wound healing disturbances and chronic diseases of the locomotory apparatus such as inflammatory, immunological or metabolism-associated acute and chronic arthritides, arthropathies, myalgias and disturbances of bone metabolism, for the treatment of ulceration, atheroscleroses and stenoses, and for the treatment of inflammations, cancer diseases, tumor metastasis formation, cachexia, anorexia, cardiac insufficiency and septic shock or for the prophylaxis of myocardial and cerebral infarctions, in a patient in need thereof, comprising administering to the patient a pharmaceutically effective amount of the compound of formula I according to claim 1, or a pharmaceutically acceptable salt, solvate or prodrug thereof.Furthermore the invention is directed to a method for preparing a compound of formula I.

    Abstract translation: 本发明涉及式I化合物，其中变量如本文所定义，或其立体异构形式，立体异构体形式的任何比例的混合物或其盐。 本发明的另一方面涉及一种药物组合物，其包含药学有效量的一种或多种根据权利要求1的式I化合物与药学上可接受的载体的混合物。 本发明还涉及一种用于预防和治疗退行性关节疾病如骨关节炎，椎关节强硬，关节创伤后的软骨损失或半月板或髌骨损伤或韧带断裂后相对较长的关节固定的方法，连接性疾病 诸如胶原蛋白，牙周病，伤口愈合障碍和诸如炎症，免疫学或代谢相关的急性和慢性关节炎的关节病，关节病，肌痛和骨骼代谢紊乱的运动器官的组织，用于治疗溃疡，动脉粥样硬化和狭窄 ，并且用于在有需要的患者中治疗炎症，癌症疾病，肿瘤转移形成，恶病质，厌食症，心脏功能不全和败血性休克或用于预防心肌和脑梗死，包括向患者施用药学有效量 的compou 根据权利要求1的式I的或其药学上可接受的盐，溶剂合物或前药。 此外，本发明涉及制备式I化合物的方法。

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