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77 条记录 (耗时 0.058 秒)

    Thieno-imino acid derivatives for use as matrix metalloproteinase inhibitors
    41.
    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

    申请人： Manfred Schudok ,  Hans Matter ,  Armin Hofmeister ,  Maxime Lampilas

    发明人： Manfred Schudok ,  Hans Matter ,  Armin Hofmeister ,  Maxime Lampilas

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

    CPC分类号： C07D495/04

    摘要： 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.

    摘要翻译： 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。

    Bicyclic imino acid derivatives as inhibitors of matrix metalloproteinases
    48.
    发明申请
    Bicyclic imino acid derivatives as inhibitors of matrix metalloproteinases 有权
    双环亚氨基酸衍生物作为基质金属蛋白酶抑制剂

    公开(公告)号：US20050080127A1

    公开(公告)日：2005-04-14

    申请号：US10950802

    申请日：2004-09-27

    申请人： Manfred Schudok ,  Hans Matter ,  Armin Hofmeister

    发明人： Manfred Schudok ,  Hans Matter ,  Armin Hofmeister

    IPC分类号： C07D217/26 ,  C07D405/12 ,  A61K31/4035 ,  C07D209/48

    CPC分类号： C07D217/26 ,  C07D405/12

    摘要： The present invention is directed to a compound of formula (I), or a stereoisomer or a mixture of stereoisomer thereof in any ratio, or its physiologically tolerable salt, which is useful as an inhibitor of matrix metalloproteinase. The present invention is also directed to a pharmaceutical preparation comprising a pharmaceutically effective amount of at least one compound of formula (I); processes for their preparation; the use of a compound of formula (I) having activity as an matrix metalloproteinase inhibitor; and for the prophylaxis and therapy of disease states that involve an increase in the activity of matrix metalloproteinase.

    摘要翻译： 本发明涉及式（I）化合物或其任何比例的立体异构体或其立体异构体的混合物或其生理上可耐受的盐，其可用作基质金属蛋白酶的抑制剂。 本发明还涉及包含药学有效量的至少一种式（I）化合物的药物制剂; 其准备过程; 使用具有活性的式（I）化合物作为基质金属蛋白酶抑制剂; 以及用于预防和治疗涉及基质金属蛋白酶活性增加的疾病状态。

    Factor VIIa inhibitory (thio)urea derivatives, their preparation and their use
    50.
    发明授权
    Factor VIIa inhibitory (thio)urea derivatives, their preparation and their use 有权
    因子VIIa抑制（硫）脲衍生物，其制备及其应用

    公开(公告)号：US06743790B2

    公开(公告)日：2004-06-01

    申请号：US09874318

    申请日：2001-06-06

    申请人： Otmar Klingler ,  Manfred Schudok ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder

    发明人： Otmar Klingler ,  Manfred Schudok ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder

    IPC分类号： A61K31535

    CPC分类号： C07D213/40 ,  C07C275/42 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/18 ,  C07D211/96 ,  C07D319/18

    摘要： The present invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5, R6, A, X, m and n 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 thromboembolic diseases and 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 which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, for example 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 1，R 2，R 3，R 4，R 5，R 6，A，X，m和n 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和再狭窄。 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的活性或用于治疗或预防因子VIIa的抑制的条件下使用。 本发明还涉及制备式I化合物的方法，其用途，例如作为药物中的活性成分，以及包含它们的药物制剂。