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1. 发明申请

WO2006094826A3 METHOD FOR COUPLING ENZYMATICALLY ACTIVATED GLYCOCONJUGATES TO A HYDROXYALKYL STARCH 审中-公开
标题翻译：将酶促活化的甘氨酸偶联于羟基烷基淀粉的方法
公开(公告)号：WO2006094826A3
公开(公告)日：2007-08-23
申请号：PCT/EP2006002236
申请日：2006-03-10
申请人： FRESENIUS KABI DE GMBH , HEMBERGER JUERGEN , MERKEL DIRK , MITSCH ANDREAS , ORLANDO MICHELE , DELBOS-KRAMPE JEANNE
发明人： HEMBERGER JUERGEN , MERKEL DIRK , MITSCH ANDREAS , ORLANDO MICHELE , DELBOS-KRAMPE JEANNE
IPC分类号： A61K47/48
CPC分类号： A61K47/61
摘要： The present invention relates to a method for coupling of enzymatically activated glycoconjugates to modifying compounds as well as a glycoconjugate coupled to a modifying compound obtainable by said method. Furthermore, the present invention is directed to the use of an oxidase enzyme in said method and also to pharmaceutical compositions comprising a coupled glycoconjugate obtained by said method.
摘要翻译：本发明涉及一种将酶促活化的糖缀合物偶联至修饰化合物的方法以及与通过所述方法获得的修饰化合物偶联的糖缀合物。此外，本发明涉及氧化酶在所述方法中的用途，还涉及包含通过所述方法获得的偶联糖缀合物的药物组合物。

2. 发明申请

WO2005092390A9 CONJUGATES OF HYDROXYALKYL STARCH AND A PROTEIN 审中-公开
标题翻译：羟丙基淀粉和蛋白质的结合
公开(公告)号：WO2005092390A9
公开(公告)日：2006-12-28
申请号：PCT/EP2005002637
申请日：2005-03-11
申请人： FRESENIUS KABI DE GMBH , EICHNER WOLFRAM , SCHIMMEL MARTIN , HACKET FRANK , KRAUS ELMAR , ZANDER NORBERT , FRANK RONALD , CONRADT HARALD , LANGER KLAUS , ORLANDO MICHELE , SOMMERMEYER KLAUS
发明人： EICHNER WOLFRAM , SCHIMMEL MARTIN , HACKET FRANK , KRAUS ELMAR , ZANDER NORBERT , FRANK RONALD , CONRADT HARALD , LANGER KLAUS , ORLANDO MICHELE , SOMMERMEYER KLAUS
IPC分类号： A61K47/48
CPC分类号： A61K47/61 , A61K47/50
摘要： The present invention relates to conjugates of hydroxyalkyl starch and a protein wherein these conjugates are formed by a convalent linkage between the hydroxyalkyl starch or a derivative of the hydroxyalkyl starch and the protein. The present invention also relates to the method of producing these conjugates and the use of these conjugates.
摘要翻译：本发明涉及羟烷基淀粉和蛋白质的缀合物，其中这些缀合物通过羟烷基淀粉或羟烷基淀粉和蛋白质的衍生物之间的共价键形成。本发明还涉及生产这些缀合物的方法和这些共轭物的用途。

3. 发明申请

WO2006094826A2 METHOD FOR COUPLING ENZYMATICALLY ACTIVATED GLYCOCONJUGATES TO A MODIFYING COMPOUND 审中-公开
标题翻译：将酶促活化的甘氨酸转化为修饰化合物的方法
公开(公告)号：WO2006094826A2
公开(公告)日：2006-09-14
申请号：PCT/EP2006/002236
申请日：2006-03-10
申请人： FRESENIUS KABI DEUTSCHLAND GMBH , HEMBERGER, Jürgen , MERKEL, Dirk , MITSCH, Andreas , ORLANDO, Michele , DELBOS-KRAMPE, Jeanne
发明人： HEMBERGER, Jürgen , MERKEL, Dirk , MITSCH, Andreas , ORLANDO, Michele , DELBOS-KRAMPE, Jeanne
IPC分类号： A61K47/48
CPC分类号： A61K47/61
摘要： The present invention relates to a method for coupling of enzymatically activated glycoconjugates to modifying compounds as well as a glycoconjugate coupled to a modifying compound obtainable by said method. Furthermore, the present invention is directed to the use of an oxidase enzyme in said method and also to pharmaceutical compositions comprising a coupled glycoconjugate obtained by said method.
摘要翻译：本发明涉及一种将酶促活化的糖缀合物偶联至修饰化合物的方法以及与通过所述方法获得的修饰化合物偶联的糖缀合物。此外，本发明涉及氧化酶在所述方法中的用途，还涉及包含通过所述方法获得的偶联糖缀合物的药物组合物。

4. 发明申请

WO2004033424A1 WATERSOLUBLE PRODRUGS OF PROPOFOL 审中-公开
标题翻译：丙泊酚的防腐剂
公开(公告)号：WO2004033424A1
公开(公告)日：2004-04-22
申请号：PCT/EP2003/003642
申请日：2003-04-08
申请人： BIOTECHNOLOGIE-GESELL SCHAFT MITTELHESSEN MBH , ORLANDO, Michele , HEMBERGER, Jürgen , TRAPANI, Giuseppe , LISO, Gaetano , ALTOMARE, Cosimo , LATROFA, Andrea , BIGGIO, Giovanni , SERRA, Mariangela , SANNA, Enrico , LAQUINTANA, Valentino
发明人： ORLANDO, Michele , HEMBERGER, Jürgen , TRAPANI, Giuseppe , LISO, Gaetano , ALTOMARE, Cosimo , LATROFA, Andrea , BIGGIO, Giovanni , SERRA, Mariangela , SANNA, Enrico , LAQUINTANA, Valentino
IPC分类号： C07D207/16
CPC分类号： C07H15/203 , A61K47/54 , A61K47/61 , A61K47/64 , C07C229/08 , C07C229/22 , C07C229/24 , C07C237/06 , C07C323/58 , C07D207/16 , C07D211/60 , C07D211/62
摘要： The present invention relates to propofol derivatives comprising a cyclic or linear amino acid, or a poly- or (oligo)saccharide moiety, a process for preparing said derivatives, a method for anesthetizing a mammal as well as a method for treating convulsions, migraine or related diseases, or for the inhibition of free radicals in a mammal to which said compounds are administered. Furthermore, the present invention relates to said compounds for use as a medicament and the use of said compounds for the preparation of a medicament for anesthetizing a mammal or for treating convulsions, migraine or related diseases, or for inhibition of free radicals in a mammal.
摘要翻译：本发明涉及包含环状或线性氨基酸或多糖或（寡糖）糖部分的异丙酚衍生物，制备所述衍生物的方法，麻醉哺乳动物的方法以及治疗惊厥，偏头痛或或用于抑制施用所述化合物的哺乳动物中的自由基。此外，本发明涉及用作药物的所述化合物和所述化合物在制备用于麻醉哺乳动物或用于治疗惊厥，偏头痛或相关疾病或用于抑制哺乳动物中的自由基的药物中的用途。

5. 发明申请

WO2005092390A3 CONJUGATES OF HYDROXYALKYL STARCH AND A PROTEIN 审中-公开
标题翻译：羟烷基淀粉和蛋白质的结合物
公开(公告)号：WO2005092390A3
公开(公告)日：2006-06-08
申请号：PCT/EP2005002637
申请日：2005-03-11
申请人： FRESENIUS KABI DE GMBH , EICHNER WOLFRAM , SCHIMMEL MARTIN , HACKET FRANK , KRAUS ELMAR , ZANDER NORBERT , FRANK RONALD , CONRADT HARALD , LANGER KLAUS , ORLANDO MICHELE , SOMMERMEYER KLAUS
发明人： EICHNER WOLFRAM , SCHIMMEL MARTIN , HACKET FRANK , KRAUS ELMAR , ZANDER NORBERT , FRANK RONALD , CONRADT HARALD , LANGER KLAUS , ORLANDO MICHELE , SOMMERMEYER KLAUS
IPC分类号： A61K47/48
CPC分类号： A61K47/61 , A61K47/50
摘要： The present invention relates to conjugates of hydroxyalkyl starch and a protein wherein these conjugates are formed by a convalent linkage between the hydroxyalkyl starch or a derivative of the hydroxyalkyl starch and the protein. The present invention also relates to the method of producing these conjugates and the use of these conjugates.
摘要翻译：本发明涉及羟烷基淀粉和蛋白质的缀合物，其中这些缀合物通过羟烷基淀粉或羟烷基淀粉的衍生物与蛋白质之间的共价键形成。本发明还涉及生产这些缀合物的方法以及这些缀合物的用途。

6. 发明申请

WO2005092928A1 CONJUGATES OF HYDROXYALKYL STARCH AND A PROTEIN, PREPARED BY REDUCTIVE AMINATION 审中-公开
标题翻译：通过还原胺化制备羟基链淀粉和蛋白质的结合
公开(公告)号：WO2005092928A1
公开(公告)日：2005-10-06
申请号：PCT/EP2005/002653
申请日：2005-03-11
申请人： FRESENIUS KABI DEUTSCHLAND GMBH , ZANDER, Norbert , EICHNER, Wolfram , CONRADT, Harald , HACKET, Frank , LANGER, Klaus , ORLANDO, Michele , FRANK, Ronald
发明人： ZANDER, Norbert , EICHNER, Wolfram , CONRADT, Harald , HACKET, Frank , LANGER, Klaus , ORLANDO, Michele , FRANK, Ronald
IPC分类号： C08B31/00
CPC分类号： A61K38/1816 , A61K38/193 , A61K38/2013 , A61K38/202 , A61K38/212 , A61K38/215 , A61K38/37 , A61K38/42 , A61K38/446 , A61K38/4846 , A61K38/4866 , A61K38/55 , A61K47/61 , A61K51/065 , C08B31/00 , C08B31/006 , C08B31/12 , C08B31/185
摘要： The present invention relates to conjugates of hydroxyalkyl starch, preferably hydroxyethyl starch, and a protein, wherein these conjugates are formed by a reductive amination reaction between at least one aldehyde group or keto group or hemiacetal group of the hydroxyalkyl starch or of a derivative of the hydroxyalkyl starch, and at least one amino group of the protein, so that the hydroxyalkyl starch or the derivative thereof is covalently linked to the protein via an azomethine linkage or a amino linkage. The present invention also relates to the method of producing these conjugates and specific uses of the conjugates.
摘要翻译：本发明涉及羟烷基淀粉，优选羟乙基淀粉和蛋白质的缀合物，其中这些缀合物通过至少一个醛基或羟基烷基淀粉的酮基或半缩醛基团或其衍生物的还原胺化反应形成羟烷基淀粉和蛋白质的至少一个氨基，使得羟烷基淀粉或其衍生物通过偶氮甲碱键或氨基键与蛋白质共价连接。本发明还涉及生产这些缀合物的方法和缀合物的具体用途。

7. 发明申请

WO2005092390A2 CONJUGATES OF HYDROXYALKYL STARCH AND A PROTEIN 审中-公开
标题翻译：羟丙基淀粉和蛋白质的结合
公开(公告)号：WO2005092390A2
公开(公告)日：2005-10-06
申请号：PCT/EP2005/002637
申请日：2005-03-11
申请人： FRESENIUS KABI DEUTSCHLAND GMBH , EICHNER, Wolfram , SCHIMMEL, Martin , HACKET, Frank , KRAUS, Elmar , ZANDER, Norbert , FRANK, Ronald , CONRADT, Harald , LANGER, Klaus , ORLANDO, Michele , SOMMERMEYER, Klaus
发明人： EICHNER, Wolfram , SCHIMMEL, Martin , HACKET, Frank , KRAUS, Elmar , ZANDER, Norbert , FRANK, Ronald , CONRADT, Harald , LANGER, Klaus , ORLANDO, Michele , SOMMERMEYER, Klaus
IPC分类号： A61K47/48
CPC分类号： A61K47/61 , A61K47/50
摘要： The present invention relates to conjugates of hydroxyalkyl starch and a protein wherein these conjugates are formed by a convalent linkage between the hydroxyalkyl starch or a derivative of the hydroxyalkyl starch and the protein. The present invention also relates to the method of producing these conjugates and the use of these conjugates.
摘要翻译：本发明涉及羟烷基淀粉和蛋白质的缀合物，其中这些缀合物通过羟烷基淀粉或羟烷基淀粉和蛋白质的衍生物之间的共价键形成。本发明还涉及生产这些缀合物的方法和这些共轭物的用途。

8. 发明申请

WO2004032971A1 PHARMACEUTICALLY ACTIVE OLIGOSACCHARIDE CONJUGATES 审中-公开
标题翻译：药物活性低聚糖结合物
公开(公告)号：WO2004032971A1
公开(公告)日：2004-04-22
申请号：PCT/EP2003/011129
申请日：2003-10-08
申请人： BIOTECHNOLOGIE-GESELL SCHAFT MITTELHESSEN MBH , ORLANDO, Michele , HEMBERGER, Jürgen , DELBOS-KRAMPE, Jeanne
发明人： ORLANDO, Michele , HEMBERGER, Jürgen , DELBOS-KRAMPE, Jeanne
IPC分类号： A61K47/48
CPC分类号： A61K47/64 , A61K47/61
摘要： The present invention relates to pharmaceutically active oligosaccharide conjugates having the formula: (X-Y m )- S, wherein component X is a pharmaceutically active compound, Y is a bifunctional linker, and S is an oligosaccharide, consisting of 1 to 20 saccharide units, n is equal or less than the number of the saccharide units in the oligosaccharide S, and m is, independent of n, O or 1. In addition, the present invention is directed to a process of preparing compounds of the present invention, comprising the step of coupling components X and S directly or indirectly by means of a bifunctional linker group. Furthermore, the present invention relates to the use of said pharmaceutically active oligosaccharide conjugates as a medicament as well as to pharmaceutical compositions, freeze-dried pharmaceutical compositions, and a kit, all of which comprise at least one of said pharmaceutically active oligosaccharide conjugates.
摘要翻译：本发明涉及具有下式的药物活性寡糖缀合物：（X-Ym）-S，其中组分X为药物活性化合物，Y为双功能连接体，S为寡糖，由1至20个糖单元组成， n等于或小于寡糖S中的糖单元数，m与n，O或1无关。此外，本发明涉及制备本发明化合物的方法，其包括通过双功能连接基团直接或间接连接组分X和S的步骤。此外，本发明涉及所述药学活性寡糖缀合物作为药物以及药物组合物，冷冻干燥的药物组合物和试剂盒的用途，所有试剂盒都包含至少一种所述药物活性寡糖缀合物。

9. 发明申请

WO2003074088A3 KOPPLUNG NIEDERMOLEKULARER SUBSTANZEN AN HYDROXYALKYLSTÄRKE 审中-公开
公开(公告)号：WO2003074088A3
公开(公告)日：2003-09-12
申请号：PCT/EP2003/002084
申请日：2003-02-28
申请人： BIOTECHNOLOGIE - GESELLSCHAFT MITTELHESSEN MBH , ORLANDO, Michele , HEMBERGER, Jürgen
发明人： ORLANDO, Michele , HEMBERGER, Jürgen
IPC分类号： A61K47/48
摘要： Die vorliegende Erfindung betrifft die Kopplung von niedermolekularen Substanzen an ein von Stärke abgeleitetes modifiziertes Polysaccharid, wobei die bindende Wechselwirkung zwischen dem modifizierten Polysaccharid und der niedermolekularen Substanz auf einer kovalenten Bindung beruht, welche das Ergebnis einer Kopplungsreaktion zwischen der endständigen Aldehydgruppe oder einer aus dieser Aldehydgruppe durch chemische Umsetzung hervorgegangenen funktionellen Gruppe des modifizierten Polysaccharidmoleküls und einer mit dieser Aldehydgruppe oder daraus hervorgegangenen funktionellen Gruppe des Polysaccharidmoleküls reaktionsfähigen funktionellen Gruppe der niedermolekularen Substanz ist, wobei die bei der Kopplungsreaktion unmittelbar resultierende Bindung gegebenenfalls durch eine weitere Reaktion zur obengenannten kovalenten Bindung modifiziert sein kann. Die Erfindung betrifft ferner pharmazeutische Zusammensetzungen, welche die bei der Kopplung gebildeten Konjugate umfassen, und die Verwendung dieser Konjugate und Zusammensetzungen zur prophylaktischen oder therapeutischen Behandlung des menschlichen oder tierischen Körpers.

10. 发明申请

WO03074088A2 COUPLING LOW-MOLECULAR SUBSTANCES TO A MODIFIED POLYSACCHARIDE 审中-公开
标题翻译：配对低分子物质改性多糖
公开(公告)号：WO03074088A2
公开(公告)日：2003-09-12
申请号：PCT/EP0302084
申请日：2003-02-28
申请人： BIOTECHNOLOGIE GES MITTELHESSE , ORLANDO MICHELE , HEMBERGER JUERGEN
发明人： ORLANDO MICHELE , HEMBERGER JUERGEN
IPC分类号： A61K47/36 , A61K47/48 , C08B31/00
CPC分类号： A61K47/61
摘要： The invention relates to a method for coupling low-molecular substances to a starch-derived modified polysaccharide. The binding interaction between the modified polysaccharide and the low-molecular substance is based on a covalent bond which is the result of a coupling reaction between the terminal aldehyde group or a functional group of the modified polysaccharide molecule resulting from the chemical reaction of this aldehyde group and a functional group of the low-molecular substance which reacts with this aldehyde group or with the resulting functional group of the polysaccharide molecule. The bond directly resulting from the coupling reaction can be optionally modified by a further reaction to the aforementioned covalent bond. The invention further relates to pharmaceutical compositions that comprise conjugates formed in this coupling process and to the use of said conjugates and compositions for the prophylaxis or therapy of the human or animal body.
摘要翻译：本发明涉及的低分子量物质的淀粉衍生的改性的多糖的联接器，其中所述改性多糖和低分子量物质之间的结合相互作用是基于共价键，其是末端醛基之间或通过从该醛基的偶联反应的结果化学反应中出现的改性多糖分子的功能团与功能与此醛基或从该组中的多糖分子反应性官能团的低分子量物质的，其中直接在偶合反应中接合导致可被修改酌情通过进一步的反应，得到上述的共价键合的出现了。本发明还涉及一种包括形成在结合的缀合物，和用于人或动物体的预防或治疗药物中的用途，所述缀合物和组合物的药物组合物。

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