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公开(公告)号：US09561285B2
公开(公告)日：2017-02-07
申请号：US13574120
申请日：2011-01-21
申请人： Harald Rau , Torben Lessmann
发明人： Harald Rau , Torben Lessmann
IPC分类号： A61K47/48
CPC分类号： A61K47/48215 , A61K47/48338 , A61K47/60 , A61K47/65 , A61K47/6903
摘要： The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aromatic hydroxyl group is conjugated to one or more polymeric carriers via secondary carbamate-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.
摘要翻译： 本发明涉及其前体药物或其药学上可接受的盐，其包含药物连接物缀合物DL，其中D是含有芳族羟基的生物活性部分，通过含有次氨基甲酸酯的接头L与一个或多个聚合物载体缀合。 载体连接的前药实现具有治疗有用的半衰期的药物释放。 本发明还涉及包含所述前体药物及其用作药物的药物组合物。
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42.发明授权公开(公告)号：US09511122B2
公开(公告)日：2016-12-06
申请号：US13515621
申请日：2010-12-15
CPC分类号： A61K38/27 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K45/06 , A61K47/10 , A61K47/12 , A61K47/18 , A61K47/26 , A61K47/60 , A61M5/19
摘要： The present invention relates to dry compositions of rhGH polymer prodrug containing a lyoprotectant and, optionally, one or more than one excipient. Such compositions are stable for at least 1 year, when stored at 2-8° C. The invention further relates to methods of manufacturing said compositions, containers comprising such composition as well as a kit of parts.
摘要翻译： 本发明涉及含有冻干保护剂和任选的一种或多种赋形剂的rhGH聚合物前药的干组合物。 当2-8℃下储存时，这样的组合物至少存在1年是稳定的。本发明还涉及制备所述组合物的方法，包含这种组合物的容器以及一组成分。
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公开(公告)号：US20130035635A1
公开(公告)日：2013-02-07
申请号：US13574120
申请日：2011-01-21
申请人： Harald Rau , Torben Lessmann
发明人： Harald Rau , Torben Lessmann
IPC分类号： A61K31/27 , A61M5/31 , A61K31/4015 , A61P29/00 , C07C271/52 , C07D207/416
CPC分类号： A61K47/48215 , A61K47/48338 , A61K47/60 , A61K47/65 , A61K47/6903
摘要： The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aromatic hydroxyl group is conjugated to one or more polymeric carriers via secondary carbamate-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.
摘要翻译： 本发明涉及其前体药物或其药学上可接受的盐，其包含药物连接物缀合物DL，其中D是含有芳族羟基的生物活性部分，通过含有次氨基甲酸酯的接头L与一个或多个聚合物载体缀合。 载体连接的前药实现具有治疗有用的半衰期的药物释放。 本发明还涉及包含所述前体药物及其用作药物的药物组合物。
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44.发明申请公开(公告)号：US20120322721A1
公开(公告)日：2012-12-20
申请号：US13515621
申请日：2010-12-15
CPC分类号： A61K38/27 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K45/06 , A61K47/10 , A61K47/12 , A61K47/18 , A61K47/26 , A61K47/60 , A61M5/19
摘要： The present invention relates to dry compositions of rhGH polymer prodrug containing a lyoprotectant and, optionally, one or more than one excipient. Such compositions are stable for at least 1 year, when stored at 2-8° C. The invention further relates to methods of manufacturing said compositions, containers comprising such composition as well as a kit of parts.
摘要翻译： 本发明涉及含有冻干保护剂和任选的一种或多种赋形剂的rhGH聚合物前药的干组合物。 当2-8℃下储存时，这样的组合物至少存在1年是稳定的。本发明还涉及制备所述组合物的方法，包含这种组合物的容器以及一组成分。
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公开(公告)号：US20120058084A1
公开(公告)日：2012-03-08
申请号：US13254869
申请日：2010-03-04
申请人： Harald Rau , Silvia Kaden-Vagt
发明人： Harald Rau , Silvia Kaden-Vagt
CPC分类号： A61K47/60
摘要： The present invention relates to a pharmaceutical composition comprising a water-soluble polymeric carrier linked prodrug of interferon alpha, wherein the prodrug is capable of releasing free interferon alpha, wherein the release half life under physiological conditions is at least 4 days. The invention further relates to prodrugs for said pharmaceutical composition and their use for treating, controlling, delaying or preventing a condition that can benefit from interferon alpha treatment, such as hepatitis C.
摘要翻译： 本发明涉及包含干扰素α的水溶性聚合物载体连接的前药的药物组合物，其中前药能够释放游离的干扰素α，其中生理条件下的释放半衰期为至少4天。 本发明还涉及用于所述药物组合物的前体药物及其用于治疗，控制，延迟或预防可受益于干扰素α治疗的病症如丙型肝炎的用途。
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公开(公告)号：US20080167196A1
公开(公告)日：2008-07-10
申请号：US11980015
申请日：2007-10-30
申请人： Stefan Dickopf , Holger Ottleben , Harald Rau , Renate Sekul , Kristina Schmidt , Dirk Vetter
发明人： Stefan Dickopf , Holger Ottleben , Harald Rau , Renate Sekul , Kristina Schmidt , Dirk Vetter
CPC分类号： B82Y30/00 , B82Y5/00 , B82Y15/00 , G01N33/54353 , G01N33/553
摘要： The present invention relates to binding surfaces for the immobilization of ligands, ligand surfaces and structured surface arrays which present a plurality of identical or different ligands. The invention further relates to a process for the production and the use of such surfaces and to specific binder molecules which can be used for the preparation thereof.
摘要翻译： 本发明涉及用于固定配体，配体表面和存在多个相同或不同配体的结构化表面阵列的结合表面。 本发明还涉及一种用于制备和使用这些表面的方法以及可用于其制备的特定粘合剂分子。
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47.发明授权公开(公告)号：US09062094B2
公开(公告)日：2015-06-23
申请号：US13574092
申请日：2011-01-21
申请人： Harald Rau , Torben Lessmann
发明人： Harald Rau , Torben Lessmann
CPC分类号： C07K1/13 , A61K47/48215 , A61K47/48338 , A61K47/60 , A61K47/65 , C07K1/1077
摘要： The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aliphatic amine group is conjugated to one or more polymeric carriers via dipeptide-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.
摘要翻译： 本发明涉及其前体药物或其药学上可接受的盐，其包含药物接头缀合物DL，其中D是含有脂族胺基团的生物活性部分通过含二肽的接头L与一个或多个聚合物载体缀合。这种载体 连接的前药实现具有治疗有用的半衰期的药物释放。 本发明还涉及包含所述前体药物及其用作药物的药物组合物。
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48.发明申请公开(公告)号：US20140249093A1
公开(公告)日：2014-09-04
申请号：US14238447
申请日：2012-08-10
申请人： Dirk Vetter , Harald Rau
发明人： Dirk Vetter , Harald Rau
IPC分类号： A61K47/48 , A61K31/216
CPC分类号： A61K31/216 , A61K31/25 , A61K47/60 , A61K47/64
摘要： The invention provides a carrier-linked prodrugs, wherein the biologically active moieties comprise at least one carboxylic acid and wherein the linkage between the drug moiety and linker is in the form of an ester wherein the hydroxyl group required for ester formation is provided by the linker moiety and the carboxyl group required for ester formation is provided by the drug moiety. The hydroxyl group of the linker is sterically hindered by the presence of an alkyl or aryl group on the carbon directly bound to or adjacent to the carbon carrying the hydroxyl group (α-carbon). The steric effect of the alkyl or aryl group enables greater control of the rate of hydrolytic degradation of such carrier-linked prodrugs.
摘要翻译： 本发明提供载体连接的前药，其中生物活性部分包含至少一种羧酸，并且其中药物部分和接头之间的连接是酯的形式，其中酯形成所需的羟基由连接体提供 部分和酯形成所需的羧基由药物部分提供。 在直接与携带羟基（α-碳）的碳上键合或相邻的碳上存在烷基或芳基，连接体的羟基被空间位阻。 烷基或芳基的立体效应能够更好地控制这种载体连接的前药的水解降解速率。
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49.发明授权公开(公告)号：US08408110B2
公开(公告)日：2013-04-02
申请号：US12354941
申请日：2009-01-16
申请人： Joachim Krauss , Georg Meissner , Harald Rau , Hans Schadl
发明人： Joachim Krauss , Georg Meissner , Harald Rau , Hans Schadl
CPC分类号： B26F1/40 , B26D7/18 , B26F3/002 , Y10T83/6654 , Y10T83/727 , Y10T83/8878 , Y10T83/9423 , Y10T83/9425 , Y10T83/9457 , Y10T83/9476
摘要： A flatbed punching module for punching a printing material includes an upper platen and a lower platen which can be moved by a drive relative to the upper platen that is fixed to a frame, in order to perform a punching stroke for punching the printing material passing between the upper platen and the lower platen, resulting in the lower platen engaging with or being thrown onto the upper platen. As a result, the printing material can be processed through the use of at least one punching die. At least one printing material transport device for guiding the printing material, is held fixedly on the movable lower platen. The flatbed punching module can advantageously be used in a flatbed punch for processing a printing material web.
摘要翻译： 用于冲压印刷材料的平板冲孔模块包括上压板和下压板，其可通过相对于固定到框架的上压板的驱动器移动，以便执行冲压行程以冲压印刷材料 上压板和下压板，导致下压板与上压板接合或被扔在上压板上。 结果，可以通过使用至少一个冲压模具来加工印刷材料。 用于引导印刷材料的至少一个印刷材料输送装置被固定地保持在可动下压板上。 平板冲孔模块可以有利地用于平板冲头中以处理印刷材料网。
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50.发明申请公开(公告)号：US20090183616A1
公开(公告)日：2009-07-23
申请号：US12354941
申请日：2009-01-16
申请人： Joachim Krauss , Georg Meissner , Harald Rau , Hans Schadl
发明人： Joachim Krauss , Georg Meissner , Harald Rau , Hans Schadl
IPC分类号： B26F1/14
CPC分类号： B26F1/40 , B26D7/18 , B26F3/002 , Y10T83/6654 , Y10T83/727 , Y10T83/8878 , Y10T83/9423 , Y10T83/9425 , Y10T83/9457 , Y10T83/9476
摘要： A flatbed punching module for punching a printing material includes an upper platen and a lower platen which can be moved by a drive relative to the upper platen that is fixed to a frame, in order to perform a punching stroke for punching the printing material passing between the upper platen and the lower platen, resulting in the lower platen engaging with or being thrown onto the upper platen. As a result, the printing material can be processed through the use of at least one punching die. At least one printing material transport device for guiding the printing material, is held fixedly on the movable lower platen. The flatbed punching module can advantageously be used in a flatbed punch for processing a printing material web.
摘要翻译： 用于冲压印刷材料的平板冲孔模块包括上压板和下压板，其可通过相对于固定到框架的上压板的驱动器移动，以便执行冲压行程以冲压印刷材料 上压板和下压板，导致下压板与上压板接合或被扔在上压板上。 结果，可以通过使用至少一个冲压模具来加工印刷材料。 用于引导印刷材料的至少一个印刷材料输送装置被固定地保持在可动下压板上。 平板冲孔模块可以有利地用于平板冲头中以处理印刷材料网。
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