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31. 发明申请

WO2007022512A3 GLYCOPEGYLATED FACTOR VII AND FACTOR VIIA 审中-公开
标题翻译：糖基化因子VII和因子VIIA
公开(公告)号：WO2007022512A3
公开(公告)日：2007-10-04
申请号：PCT/US2006032649
申请日：2006-08-21
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , ZOPF DAVID A , TAUDTE SUSANN , WILLETT W SCOTT , BAYER ROBERT J , KALO MATTHEW
发明人： DEFREES SHAWN , ZOPF DAVID A , TAUDTE SUSANN , WILLETT W SCOTT , BAYER ROBERT J , KALO MATTHEW
IPC分类号： C07K14/745 , C12P19/00
CPC分类号： C07K14/745 , A61K47/549 , A61K47/60
摘要： The present invention provides conjugates between Factor VII or Factor Vila peptides and PEG moieties. The conjugates are linked via an intact glycosyl linking group that is interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from both glycosylated and unglycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto either an amino acid or glycosyl residue on the peptide. Also provided are pharmaceutical formulations including the conjugates. Methods for preparing the conjugates are also within the scope of the invention.
摘要翻译：本发明提供因子VII或因子VIIa肽与PEG部分之间的缀合物。偶联物通过介于肽和修饰基团之间并共价连接的完整糖基连接基团连接。通过糖基转移酶的作用从糖基化和非糖基化肽两者形成缀合物。糖基转移酶将修饰的糖部分连接到肽上的氨基酸或糖基残基上。还提供了包含缀合物的药物制剂。制备缀合物的方法也在本发明的范围内。

32. 发明申请

WO2005070138A3 O-LINKED GLYCOSYLATION OF PEPTIDES 审中-公开
标题翻译：肽连接的糖蛋白
公开(公告)号：WO2005070138A3
公开(公告)日：2007-05-31
申请号：PCT/US2005000799
申请日：2005-01-10
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , ZOPF DAVID A , WANG ZHI-GUANG , CLAUSEN HENRIK
发明人： DEFREES SHAWN , ZOPF DAVID A , WANG ZHI-GUANG , CLAUSEN HENRIK
IPC分类号： C07K1/00 , A61K38/14 , A61K38/19 , C07K1/107 , C07K9/00 , C07K14/535
CPC分类号： A61K38/193 , C07K1/1077 , C07K9/00 , C07K9/001 , C07K14/535
摘要： The present invention provides polypeptides that include an O-linked glycosylation site that is not present in the wild-type peptide. The polypeptides of the invention include glycoconjugates in which a species such as a water-soluble polymer, a therapeutic agent of a biomolecule is covalently linked through an intact O-linked glycosyl residue to the polypeptide. Also provided are methods of making the peptides of the invention and methods, pharmaceutical compositions containing the peptides and methods of treating, ameliorating or preventing diseased in mammals by administering an amount of a peptide of the invention sufficient to achieve the desired response.
摘要翻译：本发明提供了包含在野生型肽中不存在的O-连接的糖基化位点的多肽。本发明的多肽包括糖缀合物，其中诸如水溶性聚合物的物质，生物分子的治疗剂通过完整的O连接的糖基残基与多肽共价连接。还提供了制备本发明的肽和方法的方法，含有肽的药物组合物和通过施用足够达到所需反应的量的本发明的肽来治疗，改善或预防哺乳动物患病的方法。

33. 发明申请

WO2006127910A2 GLYCOPEGYLATED ERYTHROPOIETIN FORMULATIONS 审中-公开
标题翻译：糖尿病肾上腺素制剂
公开(公告)号：WO2006127910A2
公开(公告)日：2006-11-30
申请号：PCT/US2006020257
申请日：2006-05-25
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , BAYER ROBERT J , ZOPE DAVID A , KANG JICHAO , WILLETT WALTER SCOTT JR
发明人： DEFREES SHAWN , BAYER ROBERT J , ZOPE DAVID A , KANG JICHAO , WILLETT WALTER SCOTT JR
IPC分类号： A61K38/18 , C07K14/505
CPC分类号： C07K14/505 , A61K38/1816 , A61K47/549 , A61K47/60
摘要： The present invention provides conjugates between erythropoietin and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates.
摘要翻译：本发明提供红细胞生成素和PEG部分之间的缀合物。缀合物通过插入和共价连接到肽和修饰基团之间的完整糖基连接基团连接。通过糖基转移酶的作用由糖基化肽形成缀合物。糖基转移酶将修饰的糖部分连接到肽上的糖基残基上。还提供了制备缀合物的方法，用缀合物治疗各种疾病状况的方法，以及包括缀合物的药物制剂。

34. 发明申请

WO03017949A3 NOVEL SYNTHETIC GANGLIOSIDE DERIVATIVES AND COMPOSITIONS THEREOF 审中-公开
标题翻译：新型合成神经鞘糖苷衍生物及其组合物
公开(公告)号：WO03017949A3
公开(公告)日：2003-12-04
申请号：PCT/US0227935
申请日：2002-08-29
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , WANG ZHI GUANG
发明人： DEFREES SHAWN , WANG ZHI GUANG
IPC分类号： C12P19/00 , A61K31/70 , A61K31/7034 , A61K31/7056 , A61K31/706 , A61K31/739 , A61P9/10 , A61P17/02 , A61P25/00 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , C07H3/06 , C07H15/00 , C07H15/04 , C07H15/18 , C07H15/26 , C07H17/02 , C12P19/28 , C12P7/64 , C12P19/04 , C12P19/12 , C12P19/26 , C12P19/44
CPC分类号： C12P19/28 , C07H3/06 , C07H17/02
摘要： Novel synthetic gangliosides and pharmaceutical compositions containing such synthetic gangliosides are described. Methods of making the novel synthetic ganglioside compounds and compositions as well as their use in the field of neuroprotection and cancer treatment is also described.
摘要翻译：描述了新的合成神经节苷脂和含有这种合成神经节苷脂的药物组合物。还描述了制备新的合成神经节苷脂化合物和组合物的方法以及它们在神经保护和癌症治疗领域的用途。

35. 发明申请

WO2008073620A3 MANUFACTURING PROCESS FOR THE PRODUCTION OF POLYPEPTIDES EXPRESSED IN INSECT CELL-LINES 审中-公开
标题翻译：用于生产在细胞细胞中表达的多肽的制造方法
公开(公告)号：WO2008073620A3
公开(公告)日：2009-05-28
申请号：PCT/US2007083538
申请日：2007-11-02
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , KINEALY KYLE , HERZER SIBYLLE
发明人： DEFREES SHAWN , KINEALY KYLE , HERZER SIBYLLE
IPC分类号： C07K1/18 , A61K38/16 , C07K1/20 , C07K1/22 , C07K1/36 , C07K14/47 , C12P19/18
CPC分类号： C12P21/02 , C07K1/165 , C07K1/18 , C07K1/20 , C07K1/36 , C12P21/005
摘要： The present invention provides a manufacturing method for polypeptides that are produced in insect cells using a baculoviral expression system. In one example, the insect cell culture is supplemented with a lipid mixture immediately prior to infection (e.g., one hour prior to infection). The polypeptides are isolated from the insect cell culture using a method that employs anion exchange or mixed-mode chromatography early in the purification process. This process step is useful to remove insect-cell derived endoglycanases and proteases and thus reduces the loss of desired polypeptide due to enzymatic degradation. In another example, mixed-mode chromatography is combined with dye-ligand affinity chromatography in a continuous-flow manner to allow for rapid processing of the insect-cell culture liquid and capture of the polypeptide. In yet another example, a polypeptide is isolated from an insect cell culture liquid using a process that combines hollow fiber filtration, mixed-mode chromatography and dye-ligand affinity in a single unit operation producing a polypeptide solution that is essentially free of endoglycanase and proteolytic activities. In a further example, the isolated polypeptides are glycopeptides having an insect specific glycosylation pattern, which are optionally conjugated to a modifying group, such as a polymer (e.g., PEG) using a glycosyltransferase and a modified nucleotide sugar.
摘要翻译：本发明提供了使用杆状病毒表达系统在昆虫细胞中产生的多肽的制备方法。在一个实例中，昆虫细胞培养物在感染之前（例如感染前一小时）补充有脂质混合物。使用在纯化过程早期采用阴离子交换或混合模式色谱法的方法从昆虫细胞培养物中分离多肽。该方法步骤可用于除去昆虫细胞来源的聚糖内切酶和蛋白酶，从而减少由于酶降解导致的期望多肽的损失。在另一个实例中，混合模式色谱法以连续流动方式与染料 - 配体亲和层析组合，以允许昆虫细胞培养液的快速加工和捕获多肽。在另一个实例中，使用在单一单元操作中组合中空纤维过滤，混合模式色谱和染料 - 配体亲和力的方法从昆虫细胞培养液中分离多肽，产生基本上不含内聚糖和多肽的多肽溶液和蛋白水解活动。在另一个实例中，分离的多肽是具有昆虫特异性糖基化图案的糖肽，其可任选地使用糖基转移酶和修饰的核苷酸糖缀合至修饰基团，例如聚合物（例如PEG）。

36. 发明申请

WO2008011633A3 GLYCOSYLATION OF PEPTIDES VIA O-LINKED GLYCOSYLATION SEQUENCES 审中-公开
标题翻译： O-连接糖基化序列肽的糖基化
公开(公告)号：WO2008011633A3
公开(公告)日：2008-12-04
申请号：PCT/US2007074139
申请日：2007-07-23
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN
发明人： DEFREES SHAWN
IPC分类号： A61K38/16 , C07K1/00
CPC分类号： C07K9/001 , A61K38/00 , A61K47/48092 , A61K47/48215 , A61K47/48246 , A61K47/48284 , A61K47/483 , A61K47/549 , A61K47/60 , A61K47/64 , A61K47/643 , A61K47/644 , C07K1/047 , C07K1/1077 , C12P21/005
摘要： The present invention provides sequon polypeptides with an amino acid sequence including one or more exogenous O-linked glycosylation sequence of the invention. In addition, the present invention provides methods of making polypeptide conjugates as well as methods of using such conjugates and their pharmaceutical compositions. The invention further provides libraries of sequon polypeptides, wherein each member of such library includes at least one exogenous O-linked glycosylation sequence of the invention. Also provided are methods of making and using such libraries.
摘要翻译：本发明提供具有包含本发明的一种或多种外源O-联糖基化序列的氨基酸序列的序列肽段多肽。此外，本发明提供了制备多肽缀合物的方法以及使用这种缀合物及其药物组合物的方法。本发明还提供了序列子多肽的文库，其中这种文库的每个成员包括至少一个本发明的外源O-联糖基化序列。还提供了制作和使用这些库的方法。

37. 发明申请

WO2008060780A3 GLYCEROL LINKED PEGYLATED SUGARS AND GLYCOPEPTIDES 审中-公开
标题翻译：甘油连接的PEG化的糖和糖肽
公开(公告)号：WO2008060780A3
公开(公告)日：2008-08-14
申请号：PCT/US2007080471
申请日：2007-10-04
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , ZENG XIAO
发明人： DEFREES SHAWN , ZENG XIAO
IPC分类号： A61K38/16
CPC分类号： A61K47/48215 , A61K38/4846 , A61K47/48092 , A61K47/549 , A61K47/60 , C12N9/6437 , C12N9/96 , C12Y304/21021 , C12Y304/21022
摘要： The present invention provides conjugates between peptides and PEG moieties through glycerol linkers.
摘要翻译：本发明提供了通过甘油接头的肽和PEG部分之间的缀合物。

38. 发明申请

WO2008057683A2 METHODS FOR THE PURIFICATION OF POLYPEPTIDE CONJUGATES 审中-公开
标题翻译：多肽结合物的纯化方法
公开(公告)号：WO2008057683A2
公开(公告)日：2008-05-15
申请号：PCT/US2007080353
申请日：2007-10-03
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , KINEALY KYLE
发明人： DEFREES SHAWN , KINEALY KYLE
IPC分类号： C12P21/06
CPC分类号： C12P21/005 , A61K47/60 , C07K1/13 , C07K1/18 , C07K1/20 , C07K14/00 , C07K14/505 , Y10S930/09
摘要： The present invention provides processes for the manufacturing of polypeptide conjugates. In particular, the invention provides methods for the purification of polypeptide conjugates, which include at least one polymeric modifying groups, such as a poly(alkylene oxide) moiety. Exemplary poly(alkylene oxide) moieties include poly(ethylene glycol) (PEG) and poly(propylene glycol). In an exemplary process, hydrophobic interaction chromatography (HIC) is used to resolve different glycoforms of glycoPEGylated polypeptides.
摘要翻译：本发明提供了制备多肽缀合物的方法。特别地，本发明提供了多肽缀合物的纯化方法，其包括至少一个聚合修饰基团，例如聚（环氧烷）部分。示例性的聚（环氧烷）部分包括聚（乙二醇）（PEG）和聚（丙二醇）。在示例性方法中，使用疏水相互作用层析（HIC）来分解糖基化多肽的不同糖型。

39. 发明申请

WO2005012484A3 ANTIBODY-TOXIN CONJUGATES 审中-公开
标题翻译：抗体毒素结合
公开(公告)号：WO2005012484A3
公开(公告)日：2007-05-24
申请号：PCT/US2004024042
申请日：2004-07-26
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , WANG ZHI-GUANG
发明人： DEFREES SHAWN , WANG ZHI-GUANG
IPC分类号： C07K16/00 , A61K47/48 , C07K16/28 , C12N20060101
CPC分类号： C07K19/00 , A61K47/60 , A61K47/6803 , A61K47/6811 , A61K47/6839 , A61K47/6843 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K47/6889 , A61K47/6899 , B82Y5/00 , C12N9/96
摘要： The present invention provides conjugates formed between toxins and sugars and toxins and peptide, such as antibodies. In an exemplary embodiment, a toxin-sugar construct is conjugated to an antibody through and intact glycosyl linking group.
摘要翻译：本发明提供了在毒素和糖和毒素和肽之间形成的缀合物，例如抗体。在一个示例性实施方案中，毒素 - 糖构建体通过和完整的糖基连接基团与抗体缀合。

40. 发明申请

WO2006031811A3 GLYCOPEGYLATED INTERFERON ALPHA 审中-公开
标题翻译：甘氨酸干扰素ALPHA
公开(公告)号：WO2006031811A3
公开(公告)日：2006-09-21
申请号：PCT/US2005032565
申请日：2005-09-12
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , ZOPF DAVID A , CLAUSEN HENRIK , XING RUYE
发明人： DEFREES SHAWN , ZOPF DAVID A , CLAUSEN HENRIK , XING RUYE
IPC分类号： A61K38/21
CPC分类号： A61K38/212 , A61K47/60
摘要： The present invention provides IFN-a conjugates including IFN-a peptides and modifying groups such as PEG moieties. The IFN-a peptide and modifying group are linked via an intact glycosyl linking group interposed between and covalently attached to the IFN-a peptide and the modifying group. The IFN-a conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar onto an amino acid or a glycosyl residue on the IFN-a peptide. Also provided are methods for preparing the IFN-a conjugates, methods for treating various disease conditions with the IFN-a conjugates, and pharmaceutical formulations including the IFN-a conjugates.
摘要翻译：本发明提供IFN-α缀合物，包括IFN-α肽和修饰基团例如PEG部分。经由完整的糖基连接基团连接IFN-α肽和修饰基团并共价连接到IFN-α肽和修饰基团上。通过糖基转移酶的作用，由糖基化肽形成IFN-α缀合物。糖基转移酶将修饰的糖连接到IFN-α肽上的氨基酸或糖基残基上。还提供了制备IFN-α缀合物的方法，用IFN-α缀合物治疗各种疾病状况的方法，以及包含IFN-α缀合物的药物制剂。

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