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1. 发明授权

US07956046B2 Oligosaccharide mixtures derived from heparin, preparation thereof and pharmaceutical compositions containing them 有权
标题翻译：衍生自肝素的寡糖混合物，其制备物和含有它们的药物组合物
公开(公告)号：US07956046B2
公开(公告)日：2011-06-07
申请号：US10899618
申请日：2004-07-27
申请人： Volker Laux , Pierre Mourier , Christian Viskov
发明人： Volker Laux , Pierre Mourier , Christian Viskov
IPC分类号： A61K31/715 , C07H1/00
CPC分类号： C08B37/0078
摘要： Oligosaccharide mixtures comprising anti-Xa activities of from 190 IU/mg to 450 IU/mg and anti-IIa activities of less than 0.2 IU/mg; and having constituent oligosaccharides with an average molecular weight of from 1800 to 2400 Daltons, constituent oligosaccharides comprise from 2 to 16 saccharide units, a 4,5-unsaturated uronic acid 2-O-sulfate unit at one end, and comprising at least one ΔIIa-IIs-Is hexasaccharide sequence are described. Processes for preparing the oligosaccharide mixtures, pharmaceutical compositions and articles of manufacture comprising the oligosaccharide mixtures are described. Methods of treatment and prevention comprising administering the oligosaccharide mixtures are described.
摘要翻译：包含190 IU / mg至450 IU / mg的抗Xa活性和小于0.2 IU / mg的抗IIa活性的寡糖混合物; 并且具有平均分子量为1800至2400道尔顿的构成寡糖，构成寡糖包含2至16个糖单元，一端为4个不饱和糖醛酸2-O-硫酸酯单元，并且包含至少一个Dgr ; IIa-IIs-是六糖序列。描述了制备包含寡糖混合物的寡糖混合物，药物组合物和制品的方法。描述了施用寡糖混合物的治疗和预防方法。

2. 发明授权

US07393840B2 Formulation based on heparin, glycosaminoglycan or heparinoid, use of the formulation and the formulation base 失效
标题翻译：基于肝素，糖胺聚糖或类肝素的制剂，使用制剂和制剂基础
公开(公告)号：US07393840B2
公开(公告)日：2008-07-01
申请号：US10296441
申请日：2001-05-29
申请人： Jörg Rosenberg , Jörg Breitenbach , Dieter Herr , Volker Laux , Robert Heger
发明人： Jörg Rosenberg , Jörg Breitenbach , Dieter Herr , Volker Laux , Robert Heger
IPC分类号： A61N31/747
CPC分类号： A61K9/1635 , A61K9/1617 , A61K9/1652 , A61K31/726 , A61K31/727
摘要： The present invention relates to formulations based on at least one heparin, glycosaminoglycan or heparinoid and on a formulation base with a lipid component and a polymer component. The use of this formulation as drug form for oral administration of at least one heparin, glycosaminoglycan or heparinoid, and also a process for producing the formulations by mixing the formulation components to form a plastic mixture and, where appropriate, to manufacture the formulations as drug form, advantageously using melt extrusion, are described. The lipid component advantageously has active ingredient-promoting properties, while the polymer component is soluble or swellable. At least parts of the lipid component are embedded in a polymer matrix, preferably in the form of a molecular dispersion. The formulations can form emulsions in water or aqueous liquids.
摘要翻译：本发明涉及基于至少一种肝素，糖胺聚糖或类肝素的制剂，以及具有脂质组分和聚合物组分的制剂基质。使用这种制剂作为口服给药至少一种肝素，糖胺聚糖或类肝素的药物形式，以及通过混合制剂组分以形成塑料混合物并在适当时制备制剂作为药物来制备制剂的方法描述了有利地使用熔体挤出的形式。脂质组分有利地具有活性成分促进性质，而聚合物组分是可溶的或可溶胀的。至少部分脂质组分嵌入聚合物基质中，优选以分子分散体的形式。制剂可以在水或含水液体中形成乳液。

3. 发明授权

US06313104B1 Organoprotective solutions 失效
标题翻译：有机保护措施
公开(公告)号：US06313104B1
公开(公告)日：2001-11-06
申请号：US09235235
申请日：1999-01-22
申请人： F. J. van der Woude , Benito Yard , Dieter Herr , Volker Laux
发明人： F. J. van der Woude , Benito Yard , Dieter Herr , Volker Laux
IPC分类号： A61K31715
CPC分类号： A61K31/737 , A01N1/02 , A01N1/0226
摘要： The invention relates to the use of polysulfated glycosaminoglycans having a sulfur content of at least 12.5% for producing pharmaceutical preparations for inhibiting the &ggr;-interferon-induced upregulation of the MHC Class I and MHC Class II proteins and ICAM-1. The invention furthermore relates to organoprotective solutions comprising polysulfated glycosaminoglycans and to a process for the ex-vivo protection of transplant organs.
摘要翻译：本发明涉及硫磺含量至少12.5％的多硫酸糖胺聚糖用于制备抑制MHC I类和II类蛋白质和ICAM-1的γ-干扰素诱导的上调的药物制剂。本发明还涉及包含多硫酸化糖胺聚糖的有机保护溶液以及用于离体保护移植器官的方法。

4. 发明申请

US20110178039A1 OLIGOSACCHARIDE MIXTURES DERIVED FROM HEPARIN, PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：从HEPARIN衍生的寡糖混合物，其制备物和含有它们的药物组合物
公开(公告)号：US20110178039A1
公开(公告)日：2011-07-21
申请号：US13049549
申请日：2011-03-16
申请人： Volker LAUX , Pierre MOURIER , Christian VISKOV
发明人： Volker LAUX , Pierre MOURIER , Christian VISKOV
IPC分类号： A61K31/727 , G01N33/86 , A61P7/02 , A61P9/00
CPC分类号： C08B37/0078
摘要： Oligosaccharide mixtures comprising anti-Xa activities of from 190 IU/mg to 450 IU/mg and anti-IIa activities of less than 0.2 IU/mg; and having constituent oligosaccharides with an average molecular weight of from 1800 to 2400 Daltons, constituent oligosaccharides comprise from 2 to 16 saccharide units, a 4,5-unsaturated uronic acid 2-O-sulfate unit at one end, and comprising at least one ΔIIa-IIs-Is hexasaccharide sequence are described. Processes for preparing the oligosaccharide mixtures, pharmaceutical compositions and articles of manufacture comprising the oligosaccharide mixtures are described. Methods of treatment and prevention comprising administering the oligosaccharide mixtures are described.
摘要翻译：包含190 IU / mg至450 IU / mg的抗Xa活性和小于0.2 IU / mg的抗IIa活性的寡糖混合物; 并且具有平均分子量为1800至2400道尔顿的构成寡糖，构成寡糖包含2至16个糖单元，一端为4个不饱和糖醛酸2-O-硫酸酯单元，并且包含至少一个Dgr ; IIa-IIs-是六糖序列。描述了制备包含寡糖混合物的寡糖混合物，药物组合物和制品的方法。描述了施用寡糖混合物的治疗和预防方法。

5. 发明授权

US07365088B2 Indazole-derivatives as factor Xa inhibitors 有权
标题翻译：吲唑衍生物作为因子Xa抑制剂
公开(公告)号：US07365088B2
公开(公告)日：2008-04-29
申请号：US10849088
申请日：2004-05-19
申请人： Marc Nazare , Volkmar Wehner , Volker Laux , Matthias Urmann , Armin Bauer , Hans Matter
发明人： Marc Nazare , Volkmar Wehner , Volker Laux , Matthias Urmann , Armin Bauer , Hans Matter
IPC分类号： A16K31/42 , A16K31/4152 , C07D261/20 , C07D413/14
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14
摘要： The present invention relates to a compound of the formula I wherein J1, J2, R0, R1, R2, Q, V, G and M are as defined herein. 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 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 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J 1，J 2，R 0，R 1，O 2， >，R 2，Q，V，G和M如本文所定义。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。

6. 发明申请

US20050033049A1 Indole derivatives as factor Xa inhibitors 有权
标题翻译：吲哚衍生物作为因子Xa抑制剂
公开(公告)号：US20050033049A1
公开(公告)日：2005-02-10
申请号：US10848743
申请日：2004-05-19
申请人： Marc Nazare , Volkmar Wehner , Kurt Ritter , Volker Laux
发明人： Marc Nazare , Volkmar Wehner , Kurt Ritter , Volker Laux
IPC分类号： A61P7/02 , C07D413/14 , C07D473/02 , C07D475/02 , C07D487/02 , C07D43/02
CPC分类号： C07D413/14
摘要： The present 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 for 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。本发明还涉及含有所述化合物的组合物，其制备方法，其用途，例如用于抑制凝血酶的形成或用于治疗或预防性治疗患有或与疾病状态相关的患者或与之相关的患者伴有心血管疾病。

7. 发明授权

US07223780B2 Triazole-derivatives as blood clotting enzyme factor Xa inhibitors 有权
标题翻译：三唑衍生物作为凝血酶因子Xa抑制剂
公开(公告)号：US07223780B2
公开(公告)日：2007-05-29
申请号：US10848916
申请日：2004-05-19
申请人： Marc Nazare , Volker Laux , Armin Bauer , Michael Wagner
发明人： Marc Nazare , Volker Laux , Armin Bauer , Michael Wagner
IPC分类号： A61K31/4196 , A61K31/4025 , A61K31/44 , A61K31/42 , C07D207/00 , C07D249/08 , C07D213/00
CPC分类号： C07D413/14
摘要： The present invention is directed to the compound of formula I which is useful for inhibiting the activity of blood clotting enzyme Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically treating a patient suffering from, or subject to, a disease state associated with a cardiovascular disorder.
摘要翻译：本发明涉及可用于抑制凝血酶因子Xa的活性的式I化合物。本发明还涉及含有所述化合物的组合物，其制备方法，其用途，例如用于抑制凝血酶的形成或用于治疗患有或与心血管疾病相关的疾病状态患者治疗。

8. 发明授权

US07196103B2 Indole derivatives as factor Xa inhibitors 有权
标题翻译：吲哚衍生物作为因子Xa抑制剂
公开(公告)号：US07196103B2
公开(公告)日：2007-03-27
申请号：US10848743
申请日：2004-05-19
申请人： Marc Nazare , Volkmar Wehner , Kurt Ritter , Volker Laux
发明人： Marc Nazare , Volkmar Wehner , Kurt Ritter , Volker Laux
IPC分类号： A61K31/44 , A61K31/445 , C07D413/00 , C07D401/00 , C07D211/68
CPC分类号： C07D413/14
摘要： The present 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 for 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。本发明还涉及含有所述化合物的组合物，其制备方法，其用途，例如用于抑制凝血酶的形成或用于治疗或预防性治疗患有或与疾病状态相关的患者或与之相关的患者伴有心血管疾病。

9. 发明申请

US20050090561A1 Oligosaccharide mixtures derived from heparin, preparation thereof and pharmaceutical compositions containing them 有权
标题翻译：衍生自肝素的寡糖混合物，其制备物和含有它们的药物组合物
公开(公告)号：US20050090561A1
公开(公告)日：2005-04-28
申请号：US10899618
申请日：2004-07-27
申请人： Volker Laux , Plerre Mourier , Christian Viskov
发明人： Volker Laux , Plerre Mourier , Christian Viskov
IPC分类号： A01N35/00 , A61K31/12 , C08B37/00
CPC分类号： C08B37/0078
摘要： Oligosaccharide mixtures comprising anti-Xa activities of from 190 IU/mg to 450 IU/mg and anti-IIa activities of less than 0.2 IU/mg; and having constituent oligosaccharides with an average molecular weight of from 1800 to 2400 Daltons, constituent oligosaccharides comprise from 2 to 16 saccharide units, a 4,5-unsaturated uronic acid 2-O-sulfate unit at one end, and comprising at least one ΔIIa-IIs-Is hexasaccharide sequence are described. Processes for preparing the oligosaccharide mixtures, pharmaceutical compositions and articles of manufacture comprising the oligosaccharide mixtures are described. Methods of treatment and prevention comprising administering the oligosaccharide mixtures are described.
摘要翻译：包含190 IU / mg至450 IU / mg的抗Xa活性和小于0.2 IU / mg的抗IIa活性的寡糖混合物; 并且具有平均分子量为1800至2400道尔顿的构成寡糖，构成寡糖包含2至16个糖单元，一端为4,5-不饱和糖醛酸2-O-硫酸酯单元，并且包含至少一个ΔIIa -II s是六糖序列。描述了制备包含寡糖混合物的寡糖混合物，药物组合物和制品的方法。描述了施用寡糖混合物的治疗和预防方法。

10. 发明申请

US20050009827A1 Triazole-derivatives as factor Xa inhibitors 有权
标题翻译：三唑衍生物作为因子Xa抑制剂
公开(公告)号：US20050009827A1
公开(公告)日：2005-01-13
申请号：US10848916
申请日：2004-05-19
申请人： Marc Nazare , Volker Laux , Armin Bauer , Michael Wagner
发明人： Marc Nazare , Volker Laux , Armin Bauer , Michael Wagner
IPC分类号： C07D413/14 , A61K31/517 , A61K31/4709 , A61K31/502 , A61K31/506 , C07
CPC分类号： C07D413/14
摘要： The present 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 for 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。本发明还涉及含有所述化合物的组合物，其制备方法，其用途，例如用于抑制凝血酶的形成或用于治疗或预防性治疗患有或与疾病状态相关的患者或与之相关的患者伴有心血管疾病。

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