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6 条记录 (耗时 0.017 秒)

    LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS
    1.
    发明申请
    LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS 审中-公开
    包含聚羟基 - 烷基和聚羟基 - 环烷基基团的低分子丝氨酸蛋白酶抑制剂

    公开(公告)号：US20110071285A1

    公开(公告)日：2011-03-24

    申请号：US12850545

    申请日：2010-08-04

    申请人： Dieter Herr ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger

    发明人： Dieter Herr ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger

    IPC分类号： C07H15/26 ,  C07D277/30 ,  C07D409/12

    CPC分类号： A61K31/155 ,  C07H7/00 ,  C07H15/00

    摘要： The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases CIs and C1r. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or guanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates. Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained.

    摘要翻译： 本发明涉及新型脒和喹啉，其生产及其用途及其作为胰蛋白酶型丝氨酸蛋白酶竞争性抑制剂的用途，特别是血栓素和补体蛋白酶CI和C1r。 除了使用化合物作为血栓抑制剂，抗凝剂，补体抑制剂和抗炎剂之外，本发明还涉及含有所述化合物作为活性成分的药物组合物。 该新型组合物的特征在于具有脒或胍功能的丝氨酸蛋白酶抑制剂与具有两个或多个羟基官能团的烷基基团的连接，其中所述烷基衍生自糖衍生物。 因此，几种糖结构成分或来自糖的组分可以彼此连接。 所述连接糖衍生物的原理使得能够获得口服活性化合物。

    LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS
    2.
    发明申请
    LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS 审中-公开
    包含聚羟基 - 烷基和聚羟基 - 环烷基基团的低分子丝氨酸蛋白酶抑制剂

    公开(公告)号：US20120190832A1

    公开(公告)日：2012-07-26

    申请号：US13277829

    申请日：2011-10-20

    申请人： Dieter Herr ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger

    发明人： Dieter Herr ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger

    IPC分类号： C07H15/26

    CPC分类号： A61K31/155 ,  C07H7/00 ,  C07H15/00

    摘要： The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases CIs and C1r. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or guanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates. Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained.

    摘要翻译： 本发明涉及新型脒和喹啉，其生产及其用途及其作为胰蛋白酶型丝氨酸蛋白酶竞争性抑制剂的用途，特别是血栓素和补体蛋白酶CI和C1r。 除了使用化合物作为血栓抑制剂，抗凝剂，补体抑制剂和抗炎剂之外，本发明还涉及含有所述化合物作为活性成分的药物组合物。 该新型组合物的特征在于具有脒或胍功能的丝氨酸蛋白酶抑制剂与具有两个或多个羟基官能团的烷基基团的连接，其中所述烷基衍生自糖衍生物。 因此，几种糖结构成分或来自糖的组分可以彼此连接。 所述连接糖衍生物的原理使得能够获得口服活性化合物。

    Organoprotective solutions
    3.
    发明授权
    Organoprotective solutions 失效
    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。

    Formulation based on heparin, glycosaminoglycan or heparinoid, use of the formulation and the formulation base
    5.
    发明授权
    Formulation based on heparin, glycosaminoglycan or heparinoid, use of the formulation and the formulation base 失效
    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。