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35 条记录 (耗时 0.042 秒)

    3-piperazinosydnone imines, process for their preparation and their use
    23.
    发明授权
    3-piperazinosydnone imines, process for their preparation and their use 失效
    3-PIPERAZINOSYDNONE IMINES，其制备方法及其使用

    公开(公告)号：US5155109A

    公开(公告)日：1992-10-13

    申请号：US730491

    申请日：1991-07-16

    申请人： Karl Schonafinger ,  Helmut Bohn ,  Melitta Just

    发明人： Karl Schonafinger ,  Helmut Bohn ,  Melitta Just

    IPC分类号： A61K31/495 ,  A61P9/00 ,  C07D271/04 ,  C07D413/04 ,  C07D413/12

    CPC分类号： C07D413/10 ,  C07D271/04

    摘要： The invention relates to pharmacologically active substituted 3-aminosydnone imines of the general formula I ##STR1## in which R.sup.1 denotes (C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkylamino or (C.sub.6 -C.sub.12)-aryl, which can optionally be substituted by (C.sub.1 -C.sub.4)-alkyl;R.sup.2 denotes hydrogen or COR.sup.3 and R.sup.3 denotes (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy, (C.sub.1 -C.sub.4)-alkoxy-(C.sub.1 -C.sub.4)-alkyl, acetoxy-(C.sub.1 -C.sub.4)-alkyl, (C.sub.6 -C.sub.12)-aryl, which can be substituted by (C.sub.1 -C.sub.4)-alkyl or (C.sub.1 -C.sub.4)-alkoxy, pyridyl, pyridyl(C.sub.1 -C.sub.4)alkyl or (C.sub.3 -C.sub.8)-cycloalkyland their pharmacologically acceptable acid addition salts.

    摘要翻译： 本发明涉及通式I（I）的药理学活性的取代的3-氨基茚三酮亚胺，其中R 1表示（C 1 -C 4） - 烷基，二 - （C 1 -C 4） - 烷基氨基或（C 6 -C 12） - 芳基，其可任选被（C 1 -C 4） - 烷基取代; R2表示氢或COR3，R3表示（C1-C4） - 烷基，（C1-C4） - 烷氧基，（C1-C4） - 烷氧基 - （C1-C4） - 烷基，乙酰氧基 - （C1-C4） - 烷基， （C 1 -C 12） - 芳基，其可以被（C 1 -C 4） - 烷基或（C 1 -C 4） - 烷氧基，吡啶基，吡啶基（C 1 -C 4）烷基或（C 3 -C 8） - 环烷基取代， 酸加成盐。

    Quinoline-carboxamide derivatives as P2Y12 antagonists
    27.
    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。

    Pyrazole-carboxamide derivatives as P2Y12 antagonists
    28.
    发明授权
    Pyrazole-carboxamide derivatives as P2Y12 antagonists 有权
    吡唑 - 甲酰胺衍生物作为P2Y12拮抗剂

    公开(公告)号：US08598179B2

    公开(公告)日：2013-12-03

    申请号：US12817868

    申请日：2010-06-17

    申请人： Marc Nazaré ,  Gernot Zech ,  Jochen Goerlitzer ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Werngard Czechtizky ,  Sven Ruf

    发明人： Marc Nazaré ,  Gernot Zech ,  Jochen Goerlitzer ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Werngard Czechtizky ,  Sven Ruf

    IPC分类号： A61K31/496 ,  C07D231/22 ,  C07D413/12 ,  C07D417/12 ,  A61K31/454 ,  A61K31/506 ,  C07D401/12 ,  C07D401/04

    CPC分类号： C07D403/12

    摘要： The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; 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R1; R2; Z; 一个; B; D; 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并因此具有抗血栓形成作用，并且适合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。

    Pyrrole derivatives as P2Y12 antagonists
    29.
    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。

    Inhibitors of the GPIb-vWF interaction, their preparation and use
    30.
    发明授权
    Inhibitors of the GPIb-vWF interaction, their preparation and use 有权
    GPIb-vWF相互作用的抑制剂，其制备和使用

    公开(公告)号：US07745443B2

    公开(公告)日：2010-06-29

    申请号：US11731978

    申请日：2007-04-02

    申请人： Otmar Klingler ,  Melitta Just ,  Kuniya Sakurai ,  Naoyuki Fukuchi

    发明人： Otmar Klingler ,  Melitta Just ,  Kuniya Sakurai ,  Naoyuki Fukuchi

    IPC分类号： C07D215/46

    CPC分类号： C07D401/12 ,  C07D215/48 ,  C07D401/14 ,  C07D417/12

    摘要： The present invention relates to compounds of the formula I, in which R1, R2, A, B, D, E, n, m or o have the meanings indicated below. The compounds of the formula I 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). They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of atherothrombotic diseases.

    摘要翻译： 本发明涉及式Ⅰ化合物，其中R 1，R 2，A，B，D，E，n，m或o具有下述含义。 式I的化合物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）之间相互作用的可逆抑制剂。 它们具有抗血栓形成作用，并且适用于例如治疗和预防动脉粥样硬化血栓形成疾病。