公开(公告)号：US07358268B2

公开(公告)日：2008-04-15

申请号：US10728339

申请日：2003-12-04

申请人： Marc Nazare ,  Armin Bauer ,  Volkmar Wehner ,  David W. Will ,  Hans Matter ,  Michael Wagner ,  Herman Schreuder

发明人： Marc Nazare ,  Armin Bauer ,  Volkmar Wehner ,  David W. Will ,  Hans Matter ,  Michael Wagner ,  Herman Schreuder

IPC分类号： A61K31/42 ,  C07D261/04 ,  C07D413/04

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

摘要： This invention is directed to the compound of formula (I) which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as in inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.

摘要翻译： 本发明涉及可用于抑制因子Xa的活性的式（I）化合物。 本发明还涉及包含所述化合物的组合物，其制备方法，其用途，例如抑制凝血酶的形成或用于治疗或预防性地治疗患有或与疾病状态有关的患者或与之相关的患者 伴有心血管疾病。

公开(公告)号：US07429581B2

公开(公告)日：2008-09-30

申请号：US10744744

申请日：2003-12-23

申请人： Marc Nazare ,  Volkmar Wehner ,  David W. Will ,  Hans Matter

发明人： Marc Nazare ,  Volkmar Wehner ,  David W. Will ,  Hans Matter

IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/496

CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D417/14

摘要： The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor 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 is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.

摘要翻译： 本发明涉及式I化合物，其中R 0为0或0; R＆lt; 1＆gt;; R 2; 3＆lt; 3＆gt; R 4; Q; V，G和M具有以下含义。 式I化合物是药理活性化合物。 它表现出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，并且通常可以在其中存在因子Xa和/或因子VIIa的不希望的活性或对于 治疗或预防因素Xa和/或因子VIIa的抑制。 本发明还涉及制备式I化合物的方法和包含其的药物制剂。

公开(公告)号：US08268560B2

公开(公告)日：2012-09-18

申请号：US13012266

申请日：2011-01-24

申请人： Eugen Uhlmann ,  Gerhard Breipohl ,  David W. Will

发明人： Eugen Uhlmann ,  Gerhard Breipohl ,  David W. Will

IPC分类号： C12Q1/68 ,  A01N61/00 ,  A61K48/00

CPC分类号： C07K14/003 ,  A61K38/00 ,  Y10T436/143333

摘要： The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.

摘要翻译： 本发明涉及在C末端或在PNA主链的C和N末端携带一个或多个磷酰基的PNA衍生物。 磷酰基在适当的情况下携带一个或多个标记基团，用于交联的基团，促进细胞内摄取的基团，或增加PNA衍生物对核酸的结合亲和力的基团。 本发明还涉及制备上述PNA衍生物的方法及其作为药物或诊断剂的用途。

公开(公告)号：US20100022016A1

公开(公告)日：2010-01-28

申请号：US12474532

申请日：2009-05-29

申请人： Eugen UHLMANN ,  Gerhard Breipohl ,  David W. Will

发明人： Eugen UHLMANN ,  Gerhard Breipohl ,  David W. Will

IPC分类号： G01N33/50

CPC分类号： C07K14/003 ,  A61K38/00 ,  Y10T436/143333

摘要： The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.

摘要翻译： 本发明涉及在C末端或在PNA主链的C和N末端携带一个或多个磷酰基的PNA衍生物。 磷酰基在适当的情况下携带一个或多个标记基团，用于交联的基团，促进细胞内摄取的基团，或增加PNA衍生物对核酸的结合亲和力的基团。 本发明还涉及制备上述PNA衍生物的方法及其作为药物或诊断剂的用途。