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1. 发明申请

WO2005014050A3 CONJUGATES OF HYDROXYALKYL STARCH AND G-CSF 审中-公开
标题翻译：羟烷基淀粉和G-CSF的共轭物
公开(公告)号：WO2005014050A3
公开(公告)日：2005-04-14
申请号：PCT/EP2004008818
申请日：2004-08-06
申请人： FRESENIUS KABI DE GMBH , EICHNER WOLFRAM , KNOLLER HELMUT , LUTTERBECK KATHARINA , ZANDER NORBERT , FRANK RONALD , SOMMERMEYER KLAUS , CONRADT HARALD S , GRABENHORST ECKART
发明人： EICHNER WOLFRAM , KNOLLER HELMUT , LUTTERBECK KATHARINA , ZANDER NORBERT , FRANK RONALD , SOMMERMEYER KLAUS , CONRADT HARALD S , GRABENHORST ECKART
IPC分类号： A61K47/48
CPC分类号： A61K47/61
摘要： The present invention relates to conjugates of hydroxyalkyl starch and a granulocyte colony stimulating factor protein (G-CSF) wherein these conjugates are formed by a covalent linkage between the hydroxyalkyl starch or a derivative of the hydroxyalkyl starch and the protein. The present invention also relates to the methods 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粒细胞集落刺激因子蛋白（G-CSF）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。

2. 发明申请

WO2006094810A2 PRODUCTION OF BIOACTIVE GLYCOPROTEINS FROM INACTIVE STARTING MATERIAL 审中-公开
标题翻译：从不活动起始材料生产生物糖蛋白
公开(公告)号：WO2006094810A2
公开(公告)日：2006-09-14
申请号：PCT/EP2006002179
申请日：2006-03-09
申请人： FRESENIUS KABI DE GMBH , FRANK RONALD , CONRADT HARALD , GRABENHORST ECKART , ZANDER NORBERT
发明人： FRANK RONALD , CONRADT HARALD , GRABENHORST ECKART , ZANDER NORBERT
IPC分类号： A61K47/48
CPC分类号： A61K47/61
摘要： The present invention relates to a method for preparing a conjugate comprising a glycoprotein and a polymer or a derivative of said polymer, wherein the polymer is a hydroxyalkylstarch (HAS), the method comprising the steps a) reacting said glycoprotein with a modified polyol carrying attached thereto, by a covalent linkage, a functional group Z, in the presence of a transferase capable of catalysing formation of a covalent linkage between the glycoprotein and said modified polyol, yielding a glycoprotein covalently linked to a polyol carrying attached thereto, by a covalent linkage, at least one functional group Z, and b) reacting at least one functional group A of the polymer or the derivative thereof with the at least one functional group Z of the glycoprotein added to said glycoprotein during step a), and thereby forming a covalent linkage.
摘要翻译：本发明涉及一种制备包含糖蛋白和所述聚合物的聚合物或衍生物的缀合物的方法，其中所述聚合物是羟烷基淀粉（HAS），所述方法包括以下步骤：a）使所述糖蛋白与带有附着物的改性多元醇反应通过共价连接，在能够催化糖蛋白与所述修饰的多元醇之间形成共价键的转移酶的存在下，通过共价连接，通过共价连接产生与携带有多元醇共价连接的糖蛋白，至少一个官能团Z，和b）在步骤a）期间使聚合物或其衍生物的至少一个官能团A与加入到所述糖蛋白的糖蛋白的至少一个官能团Z反应，从而形成共价连锁。

3. 发明专利

MX2010006175A DERIVADOS DE POLIPEPTIDOS CON HIDROXIALQUILALMIDON, ESPECIALMENTE DERIVADOS DE ERITROPOYETINA CON HIDROXIALQUILALMIDON. 未知
公开(公告)号：MX2010006175A
公开(公告)日：2010-07-05
申请号：MX2010006175
申请日：2010-06-04
申请人： FRESENIUS KABI DE GMBH
发明人： EICHNER WOLFRAM , CONRADT HARALD S , ZANDER NORBERT , FRANK RONALD , GRABENHORST ECKART , NIMTZ MANFRED
IPC分类号： A61K8/73 , A61K38/00 , A61K9/00 , A61K9/14 , A61K38/18 , A61K47/48 , C07K14/505 , C07K14/53 , C07K14/54 , C07K14/55 , C07K14/56 , C07K14/565 , C07K17/06 , C07K17/10 , C08B31/00 , C08B31/08 , C08B31/12 , C08B33/04 , C08B35/04 , C12N15/00 , C12N15/12
摘要： La presente invención se refiere a un conjugado (HAS-polipéptido) de hidroxialquilalmidón (HAS) -polipéptido que comprende una o más moléculas de HAS, en donde cada HAS se conjuga con el polipéptido mediante un radical carbohidratado o un tioéter así como a métodos para la producción del mismo. En una modalidad preferida, el polipéptido es eritropoyetina (EPO).

4. 发明专利

MXPA06001358A CONJUGADOS DE HIDROXIALQUIL ALMIDON Y G-CSF. 未知
公开(公告)号：MXPA06001358A
公开(公告)日：2006-05-15
申请号：MXPA06001358
申请日：2004-08-06
申请人： FRESENIUS KABI DE GMBH
发明人： GRABENHORST ECKART
IPC分类号： A61K47/48
摘要： La presente invencion se refiere a conjugados de hidroxialquil almidon y una proteina factor estimulante de colonias de granulocitos (G-CSF), donde estos conjugados se forman por union covalente entre el hidroxialquil almidon o un derivado del hidroxialquil almidon y la proteina. La presente invencion tambien se refiere a los metodos para producir estos conjugados y al uso de estos conjugados.

5. 发明专利

BR0314106A 未知
公开(公告)号：BR0314106A
公开(公告)日：2005-07-19
申请号：BR0314106
申请日：2003-08-08
申请人： FRESENIUS KABI DE GMBH
发明人： CONRADT HARALD S , GRABENHORST ECKART , NIMTZ MANFRED , ZANDER NORBERT , FRANK RONALD , EICHNER WOLFRAM
IPC分类号： A61K8/73 , A61K9/00 , A61K9/14 , A61K38/00 , A61K38/18 , A61K47/48 , C07K14/505 , C07K14/53 , C07K14/54 , C07K14/55 , C07K14/56 , C07K14/565 , C07K17/06 , C07K17/10 , C08B31/00 , C08B31/08 , C08B31/12 , C08B33/04 , C08B35/04 , C12N15/12
摘要： Preparation of hydroxyalkyl starch derivatives involves reaction of hydroxyalkyl starch at its reducing end with amino compound. The reducing end is not oxidized prior to the reaction. Preparation of hydroxyalkyl starch derivatives involves reaction of hydroxyalkyl starch of formula (I) at its reducing end with amino compound of formula R a-NH-R b (II). [Image] R 1-R 3H, linear or branched hydroxyalkyl; R aat least one functional group X capable of reacting with at least one other compound prior to or after the reaction; R ba functional group X or W; W : -NH-, -NH-C(=G)-, -NH-C(=G)-G-, -NH-S(O) 2- or -NH-C(=G)-NH-; X : -SH, -NH 2, -O-NH 2, -NH-O-alkyl, -C(=G)-NH-NH 2, -G-C(=G)-NH-NH 2, -NH-C(=G)-NH-NH 2 or -S(O) 2-NH-NH 2; and G : O or S. An independent claim is included for a pharmaceutical composition comprising the hydroxyalkyl starch derivative (where the reaction product of (I) with (II) is reacted via the functional group X in (II) with the further compound (III) or (II) is reacted via the functional group X with (III) prior to the reaction with (I), and the reaction product of (I) and (II) with the crosslinking compound is reacted with a polypeptide). ACTIVITY : Antianemic. Hydroxyethyl starch-erythropoietin (HES-EPO) was tested by the EPO-bioassay in normocythaemic mouse system and showed specific activity of 344000 U/mg, which was 3 fold higher than international BRP-erythropoietin reference standard preparation. MECHANISM OF ACTION : None given.

6. 发明专利

ES2214166T1 未知
公开(公告)号：ES2214166T1
公开(公告)日：2004-09-16
申请号：ES02020425
申请日：2002-09-11
申请人： FRESENIUS KABI DE GMBH
发明人： CONRADT HARALD S , GRABENHORST ECKART , NIMTZ MANFRED , ZANDER NORBERT , FRANK RONALD , EICHNER WOLFRAM
IPC分类号： A61K8/73 , A61K9/00 , A61K9/14 , A61K38/00 , A61K38/18 , A61K47/48 , C07K14/505 , C07K14/53 , C07K14/54 , C07K14/55 , C07K14/56 , C07K14/565 , C07K17/06 , C07K17/10 , C08B31/00 , C08B31/08 , C08B31/12 , C08B33/04 , C08B35/04 , C12N15/12

7. 发明专利

ES2213505T1 未知
公开(公告)号：ES2213505T1
公开(公告)日：2004-09-01
申请号：ES03020423
申请日：2003-09-11
申请人： FRESENIUS KABI DE GMBH
发明人： CONRADT HARALD S , GRABENHORST ECKART , NIMTZ MANFRED , ZANDER NORBERT , FRANK RONALD , EICHNER WOLFRAM
IPC分类号： A61K8/73 , A61K9/00 , A61K9/14 , A61K38/00 , A61K38/18 , A61K47/48 , C07K14/505 , C07K14/53 , C07K14/54 , C07K14/55 , C07K14/56 , C07K14/565 , C07K17/06 , C07K17/10 , C08B31/00 , C08B31/08 , C08B31/12 , C08B33/04 , C08B35/04 , C12N15/12
摘要： Preparation of hydroxyalkyl starch derivatives involves reaction of hydroxyalkyl starch at its reducing end with amino compound. The reducing end is not oxidized prior to the reaction. Preparation of hydroxyalkyl starch derivatives involves reaction of hydroxyalkyl starch of formula (I) at its reducing end with amino compound of formula R a-NH-R b (II). [Image] R 1-R 3H, linear or branched hydroxyalkyl; R aat least one functional group X capable of reacting with at least one other compound prior to or after the reaction; R ba functional group X or W; W : -NH-, -NH-C(=G)-, -NH-C(=G)-G-, -NH-S(O) 2- or -NH-C(=G)-NH-; X : -SH, -NH 2, -O-NH 2, -NH-O-alkyl, -C(=G)-NH-NH 2, -G-C(=G)-NH-NH 2, -NH-C(=G)-NH-NH 2 or -S(O) 2-NH-NH 2; and G : O or S. An independent claim is included for a pharmaceutical composition comprising the hydroxyalkyl starch derivative (where the reaction product of (I) with (II) is reacted via the functional group X in (II) with the further compound (III) or (II) is reacted via the functional group X with (III) prior to the reaction with (I), and the reaction product of (I) and (II) with the crosslinking compound is reacted with a polypeptide). ACTIVITY : Antianemic. Hydroxyethyl starch-erythropoietin (HES-EPO) was tested by the EPO-bioassay in normocythaemic mouse system and showed specific activity of 344000 U/mg, which was 3 fold higher than international BRP-erythropoietin reference standard preparation. MECHANISM OF ACTION : None given.

8. 发明专利

AU2003253399A1 HASYLATED POLYPEPTIDES, ESPECIALLY HASYLATED ERYTHROPOIETIN 未知
公开(公告)号：AU2003253399A1
公开(公告)日：2004-04-30
申请号：AU2003253399
申请日：2003-08-08
申请人： FRESENIUS KABI DE GMBH
发明人： CONRADT HARALD S , GRABENHORST ECKART , NIMTZ MANFRED , ZANDER NORBERT , FRANK RONALD , EICHNER WOLFRAM
IPC分类号： A61K8/73 , A61K9/00 , A61K9/14 , A61K38/00 , A61K38/18 , A61K47/48 , C07K14/505 , C07K14/53 , C07K14/54 , C07K14/55 , C07K14/56 , C07K14/565 , C07K17/06 , C07K17/10 , C08B31/00 , C08B31/08 , C08B31/12 , C08B33/04 , C08B35/04 , C12N15/12
摘要： Preparation of hydroxyalkyl starch derivatives involves reaction of hydroxyalkyl starch at its reducing end with amino compound. The reducing end is not oxidized prior to the reaction. Preparation of hydroxyalkyl starch derivatives involves reaction of hydroxyalkyl starch of formula (I) at its reducing end with amino compound of formula R a-NH-R b (II). [Image] R 1-R 3H, linear or branched hydroxyalkyl; R aat least one functional group X capable of reacting with at least one other compound prior to or after the reaction; R ba functional group X or W; W : -NH-, -NH-C(=G)-, -NH-C(=G)-G-, -NH-S(O) 2- or -NH-C(=G)-NH-; X : -SH, -NH 2, -O-NH 2, -NH-O-alkyl, -C(=G)-NH-NH 2, -G-C(=G)-NH-NH 2, -NH-C(=G)-NH-NH 2 or -S(O) 2-NH-NH 2; and G : O or S. An independent claim is included for a pharmaceutical composition comprising the hydroxyalkyl starch derivative (where the reaction product of (I) with (II) is reacted via the functional group X in (II) with the further compound (III) or (II) is reacted via the functional group X with (III) prior to the reaction with (I), and the reaction product of (I) and (II) with the crosslinking compound is reacted with a polypeptide). ACTIVITY : Antianemic. Hydroxyethyl starch-erythropoietin (HES-EPO) was tested by the EPO-bioassay in normocythaemic mouse system and showed specific activity of 344000 U/mg, which was 3 fold higher than international BRP-erythropoietin reference standard preparation. MECHANISM OF ACTION : None given.

9. 发明专利

CA2495242A1 HASYLATED POLYPEPTIDES, ESPECIALLY HASYLATED ERYTHROPOIETIN 未知
公开(公告)号：CA2495242A1
公开(公告)日：2004-03-25
申请号：CA2495242
申请日：2003-08-08
申请人： FRESENIUS KABI DE GMBH
发明人： CONRADT HARALD S , NIMTZ MANFRED , GRABENHORST ECKART , EICHNER WOLFRAM , FRANK RONALD , ZANDER NORBERT
IPC分类号： A61K8/73 , A61K9/00 , A61K9/14 , A61K38/00 , A61K38/18 , A61K47/48 , C07K14/505 , C07K14/53 , C07K14/54 , C07K14/55 , C07K14/56 , C07K14/565 , C07K17/06 , C07K17/10 , C08B31/00 , C08B31/08 , C08B31/12 , C08B33/04 , C08B35/04 , C12N15/12
摘要： The present invention relates to hydroxyalkylstarch (HAS)-polypeptide- conjugate (HAS-polypeptide) comprising one or more HAS molecules, wherein ea ch HAS is conjugated to the polypeptide via a carbohydrate moiety or a thioethe r as well as to methods for the production thereof. In a preferred embodiment, the polypeptide is erythropoietin (EPO).

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