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    Bifunctional glycoproteins having a modified carbohydrate complement and their use in tumor-selective therapy
    1.
    发明授权
    Bifunctional glycoproteins having a modified carbohydrate complement and their use in tumor-selective therapy 失效
    具有修饰的碳水化合物补体的双功能糖蛋白及其在肿瘤选择性治疗中的用途

    公开(公告)号：US08552159B2

    公开(公告)日：2013-10-08

    申请号：US10815925

    申请日：2004-04-02

    申请人： Klaus Bosslet ,  Joerg Czech ,  Dieter Hoffmann

    发明人： Klaus Bosslet ,  Joerg Czech ,  Dieter Hoffmann

    IPC分类号： C07K1/00

    CPC分类号： C12N9/0002 ,  A61K38/00 ,  A61K47/62 ,  A61K47/6851 ,  A61K2039/505 ,  C07K16/30 ,  C07K16/3007 ,  C07K16/3046 ,  C07K19/00 ,  C07K2317/24 ,  C07K2317/622 ,  C07K2319/00 ,  C07K2319/02 ,  C07K2319/61

    摘要： Provided herein are carbohydrate complement-modified bifunctional glycoproteins, and their use in tumor-selective therapy. The bifunctional glycoproteins comprise a first component that specifically binds to a tumor-specific antigen and a second component having enzymatic activity by means of which a non-toxic prodrug is cleaved into a cytotoxic drug. The carbohydrate complement comprises at least one exposed carbohydrate residue selected from the group consisting of mannose, galactose, N-acetylglucosamine, N-acetyllactose, glucose and fucose. The modified carbohydrate complement contributes to increased relative concentration of the glycoproteins at the site of the tumor, and enhanced clearance from the general circulation and non-tumor sites.

    摘要翻译： 本文提供了碳水化合物补体修饰的双功能糖蛋白，以及它们在肿瘤选择性治疗中的用途。 双功能糖蛋白包含特异性结合肿瘤特异性抗原的第一组分和具有酶活性的第二组分，通过其将非毒性前体药物切割成细胞毒性药物。 碳水化合物补体包含至少一种选自甘露糖，半乳糖，N-乙酰葡糖胺，N-乙酰乳糖，葡萄糖和岩藻糖的暴露的碳水化合物残基。 修饰的碳水化合物补体有助于增加肿瘤位置处的糖蛋白的相对浓度，并且增强了与一般循环和非肿瘤部位的清除率。

    Quinoline-carboxamide derivatives as P2Y12 antagonists
    5.
    发明授权
    Quinoline-carboxamide derivatives as P2Y12 antagonists 有权
    喹啉 - 甲酰胺衍生物作为P2Y12拮抗剂

    公开(公告)号：US08669266B2

    公开(公告)日：2014-03-11

    申请号：US12573551

    申请日：2009-10-05

    申请人： Marc Nazare ,  Gernot Zech ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Joerg Czech

    发明人： Marc Nazare ,  Gernot Zech ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Joerg Czech

    IPC分类号： A01N43/42 ,  A61K31/44

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14

    摘要： The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; 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 anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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 1; R2; R3; R4; R5; R6; Z; 一个; B; E; X; Q; J; 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。 它们对血小板表现出强烈的抗凝集作用，因此表现出抗血栓形成的作用， 用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 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 P2Y12 antagonists
    6.
    发明授权
    Pyrrole derivatives as P2Y12 antagonists 有权
    吡咯衍生物作为P2Y12拮抗剂

    公开(公告)号：US07910576B2

    公开(公告)日：2011-03-22

    申请号：US12639500

    申请日：2009-12-16

    申请人： Otmar Klingler ,  Joerg Czech ,  Werngard Czechtizky ,  Tilo Weiss ,  Melitta Just

    发明人： Otmar Klingler ,  Joerg Czech ,  Werngard Czechtizky ,  Tilo Weiss ,  Melitta Just

    IPC分类号： A61K31/454 ,  A61K31/496 ,  C07D401/14 ,  C07D401/02 ,  C07D403/14 ,  C07D403/02

    CPC分类号： C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14

    摘要： 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; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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 1; R2; R3; R4; R5 R6; R7; R8; R9; R10; R11; R12; R13; 一个; B，D和E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。 它们对血小板表现出强烈的抗凝集作用，因此表现出抗血栓形成的作用， 用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 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 P2Y12 ANTAGONISTS
    7.
    发明申请
    PYRROLE DERIVATIVES AS P2Y12 ANTAGONISTS 有权
    PYRROLE DERIVATIVES作为P2Y12 ANTAGONISTS

    公开(公告)号：US20100226918A1

    公开(公告)日：2010-09-09

    申请号：US12639500

    申请日：2009-12-16

    申请人： Otmar KLINGLER ,  Joerg CZECH ,  Werngard CZECHTIZKY ,  Tilo WEISS ,  Melitta JUST

    发明人： Otmar KLINGLER ,  Joerg CZECH ,  Werngard CZECHTIZKY ,  Tilo WEISS ,  Melitta JUST

    IPC分类号： A61K31/496 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D401/14 ,  C07D401/06 ,  A61K31/454 ,  A61K31/727 ,  A61K31/616 ,  A61K39/395 ,  A61K38/12 ,  A61K31/551 ,  A61K31/5377 ,  A61P7/02 ,  A61P9/10 ,  A61P9/00

    CPC分类号： C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14

    摘要： 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; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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 1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; 一个; B，D和E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。 它们对血小板表现出强烈的抗凝集作用，因此表现出抗血栓形成的作用， 用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 本发明还涉及制备式I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。