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1. 发明申请

US20100010045A1 PYRAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS 有权
标题翻译：吡唑衍生物作为因子Xa抑制剂
公开(公告)号：US20100010045A1
公开(公告)日：2010-01-14
申请号：US12562276
申请日：2009-09-18
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： A61K31/454 , C07D231/10 , A61K31/415 , A61K31/4245 , C07D413/02 , C07D419/02 , A61K31/41 , C07D401/04
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; R1; R2; R3; R4; 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。

2. 发明申请

US20080306056A1 PYRAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS 审中-公开
标题翻译：吡唑衍生物作为因子Xa抑制剂
公开(公告)号：US20080306056A1
公开(公告)日：2008-12-11
申请号：US12185388
申请日：2008-08-04
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 , C07D413/14 , A61K31/454 , A61K31/444 , C12N9/99 , A61K31/5377 , C07D417/14
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 in the claims. the compound of formula I is 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 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 processes for the preparation of a compound of 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 0; R1; R2; R3; R4; Q; V，G和M具有权利要求中所示的含义。式I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VIIa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制剂。

3. 发明申请

US20110117569A1 POLYMIDE NUCLEIC ACID DERIVATIVES, AND AGENTS AND PROCESSES FOR PREPARING THEM 失效
标题翻译：聚合核酸衍生物及其制备方法
公开(公告)号：US20110117569A1
公开(公告)日：2011-05-19
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
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。

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