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1. 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。

2. 发明申请

WO2008151258A3 O-LINKED GLYCOSYLATION USING N-ACETYLGLUCOSAMINYL TRANSFERASES 审中-公开
标题翻译：使用N-乙酰氨基葡萄糖转移的O-连接的糖蛋白
公开(公告)号：WO2008151258A3
公开(公告)日：2009-02-12
申请号：PCT/US2008065825
申请日：2008-06-04
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN
发明人： DEFREES SHAWN
IPC分类号： C12N9/10 , C12Q1/48
CPC分类号： C07K14/51 , A61K47/60 , C07K14/535 , C07K14/56 , C07K14/61 , C07K2319/00
摘要： The present invention provides covalent conjugates between a polypeptide and a modifying group, such as a water-soluble polymer (e.g., PEG). The amino acid sequence of the polypeptide includes one or more O-linked glycosylation sequence, each being a substrate for a GIcNAc transferase. The modifying group is covalently linked to the polypeptide via a glycosyl-linking group interposed between and covalently linked to both the polypeptide and the modifying group. In one embodiment, a glucosamine linking group is directly attached to an amino acid residue of the O-linked glycosylation sequence. The invention further provides methods of making polypeptide conjugates. The present invention also provides non-naturally ocurring polypeptides that include at leats one O-linked linked glycosylation sequence of the invention, wherein each glycosylation sequence is a substrate for a GIcNAc transferase. The invention further provides pharmaceutical compositions that include a polypeptide conjugate of the invention.
摘要翻译：本发明提供多肽和修饰基团之间的共价缀合物，例如水溶性聚合物（例如PEG）。多肽的氨基酸序列包括一个或多个O-连接的糖基化序列，各自为GlcNAc转移酶的底物。修饰基团通过插入在多肽和修饰基团之间并且共价连接的糖基连接基团与多肽共价连接。在一个实施方案中，葡糖胺连接基团直接连接到O-连接的糖基化序列的氨基酸残基。本发明进一步提供了制备多肽缀合物的方法。本发明还提供了非天然的多肽，其包括在本发明的一个O-连接的糖基化序列中，其中每个糖基化序列是GlcNAc转移酶的底物。本发明进一步提供包含本发明的多肽缀合物的药物组合物。

3. 发明申请

WO2007056191A3 NUCLEOTIDE SUGAR PURIFICATION USING MEMBRANES 审中-公开
标题翻译：使用膜的核糖体净化
公开(公告)号：WO2007056191A3
公开(公告)日：2007-10-25
申请号：PCT/US2006043048
申请日：2006-11-03
申请人： NEOSE TECHNOLOGIES INC , FELO MICHAEL , DEFREES SHAWN
发明人： FELO MICHAEL , DEFREES SHAWN
IPC分类号： C12N9/10 , C12N9/12 , C12P19/00 , C12P19/18
CPC分类号： C12P19/305 , C07H19/06 , Y02P20/582
摘要： The invention provides methods of removing contaminants from a mixture of a desired product and contaminants by pH adjustments and molecular weight cut-offs. The contaminants include phosphate groups, magnesium sulfate, sodium pyruvate and tetrasodium pyrophosphate groups. The desired product includes nucleotide sugars, glycolipids, LnNT, sialyl lactose, and salts.
摘要翻译：本发明提供了通过pH调节和分子量截留从所需产物和污染物的混合物中除去污染物的方法。污染物包括磷酸盐基团，硫酸镁，丙酮酸钠和焦磷酸四钠基团。所需产物包括核苷酸糖，糖脂，LnNT，唾液酸乳糖和盐。

4. 发明申请

WO2005118798A3 MUTANT ENDOGLYCOCERAMIDASES WITH ENHANCED SYNTHETIC ACTIVITY 审中-公开
标题翻译：具有增强合成活性的突变内毒素
公开(公告)号：WO2005118798A3
公开(公告)日：2007-05-10
申请号：PCT/US2005019451
申请日：2005-06-01
申请人： NEOSE TECHNOLOGIES INC , UNIV BRITISH COLUMBIA UNIVERSI , JOHNSON KARL F , DEFREES SHAWN , WITHERS STEPHEN , VAUGHAN MARK
发明人： JOHNSON KARL F , DEFREES SHAWN , WITHERS STEPHEN , VAUGHAN MARK
IPC分类号： C12N9/24 , C12N9/00 , C12N9/14 , C12N9/16 , C12N9/20
CPC分类号： C12P19/26 , C12N9/2402 , C12Y302/01123
摘要： The present invention relates to a novel endoglycoceramidase whose hydrolytic activity has been substantially reduced or eliminated, such that the enzyme is useful for synthesis of glycolipids from a monosaccharide or oligosaccharide and a ceramide. More specifically, the endoglycoceramidase is a mutant version of a naturally occurring endoglycoceramidase, preferably comprising a mutation within the active site or the nucleophilic site of the enzyme and more preferably comprising a substitution mutation of the Glu residue within the active site or the nucleophilic site. Also disclosed are a method for generating the mutant endoglycoceramidase and a method for enzymatically synthesizing glycolipids using this mutant enzyme.
摘要翻译：本发明涉及其水解活性已经显着降低或消除的新型神经酰胺糖内切酶，使得该酶可用于从单糖或寡糖和神经酰胺合成糖脂。更具体地，神经酰胺糖内切酶是天然存在的神经酰胺糖内切酶的突变形式，优选地包含酶的活性位点或亲核位点内的突变，更优选地包含活性位点或亲核位点内的Glu残基的取代突变。还公开了产生突变型神经酰胺糖内切酶的方法和使用该突变酶酶促合成糖脂的方法。

5. 发明申请

WO2006052841A2 GLYCOLIPIDS 审中-公开
标题翻译：糖脂
公开(公告)号：WO2006052841A2
公开(公告)日：2006-05-18
申请号：PCT/US2005040195
申请日：2005-11-03
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , WANG ZHI-GUANG
发明人： DEFREES SHAWN , WANG ZHI-GUANG
IPC分类号： A61K38/14
CPC分类号： C07H15/06 , A61K38/00 , C07H15/10
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 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。还描述了制备新型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领域的应用。

6. 发明申请

WO2005055950A3 GLYCOPEGYLATED FACTOR IX 审中-公开
标题翻译：糖蛋白因子九
公开(公告)号：WO2005055950A3
公开(公告)日：2005-10-20
申请号：PCT/US2004041070
申请日：2004-12-03
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , BAYER ROBERT J , BOWE CARYN , PANNEERSELVAM KRISHNASAMY
发明人： DEFREES SHAWN , BAYER ROBERT J , BOWE CARYN , PANNEERSELVAM KRISHNASAMY
IPC分类号： A61K20060101 , A61K31/00 , C07K1/00
CPC分类号： C12N9/644 , A61K47/60 , C12Y304/21022
摘要： The present invention provides conjugates between Factor IX 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：本发明提供因子IX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。

7. 发明申请

WO0029603A2 LOW COST MANUFACTURE OF OLIGOSACCHARIDES 审中-公开
标题翻译：低密度脂蛋白的低成本制造
公开(公告)号：WO0029603A2
公开(公告)日：2000-05-25
申请号：PCT/US9927599
申请日：1999-11-18
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , JOHNSON KARL
发明人： DEFREES SHAWN , JOHNSON KARL
IPC分类号： C12N15/09 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/10 , C12P19/18 , C12P19/28 , C12P
CPC分类号： C12P19/18
摘要： This invention provides recombinant cells, reaction mixtures, and methods that are useful for the enzymatic synthesis of product saccharides. The recombinant cells contain a heterologous gene that encodes a glycosyltransferase which catalyzes at least one step of the enzymatic synthesis, as well a system for generating a nucleotide sugar that can serve as a substrate for the glycosyltransferase. The recombinant cells, reaction mixtures, and methods are useful for efficiently synthesizing a large variety of saccharides, including polysaccharides, oligosaccharides, glycoproteins and glycolipids, using relatively low-cost starting materials.
摘要翻译：本发明提供可用于酶合成产物糖的重组细胞，反应混合物和方法。重组细胞含有编码糖基转移酶的异源基因，其催化至少一个酶促合成步骤，以及用于产生可用作糖基转移酶底物的核苷酸糖的系统。重组细胞，反应混合物和方法可用于使用相对低成本的起始材料有效合成多种糖类，包括多糖，寡糖，糖蛋白和糖脂。

8. 发明申请

WO2009089396A2 GLYCOCONJUGATION OF POLYPEPTIDES USING OLIGOSACCHARYLTRANSFERASES 审中-公开
标题翻译：低聚糖基转移酶对多肽的糖苷键合
公开(公告)号：WO2009089396A2
公开(公告)日：2009-07-16
申请号：PCT/US2009030503
申请日：2009-01-08
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN
发明人： DEFREES SHAWN
IPC分类号： A61K38/21
CPC分类号： C12Y304/21022 , A61K38/00 , A61K47/543 , A61K47/549 , A61K47/60 , C07K14/48 , C07K14/50 , C07K14/51 , C07K14/755 , C12N9/6437 , C12N9/644 , C12Y204/99018 , C12Y304/21021
摘要： The current invention provides polypeptides and polypeptide conjugates that include an exogenous N-linked glycosylation sequence. The N-linked glycosylation sequence is preferably a substrate for an oligosaccharyltransferase (e.g., bacterial PgIB), which can catalyze the transfer of a glycosyl moiety from a lipid-bound glycosyl donor molecule (e.g., a lipid-pyrophosphate-linked glycosyl moiety) to an asparagine (N) residue of the glycosylation sequence. In one example, the asparagine residue is part of an exogenous N-linked glycosylation sequence of the invention. The invention further provides methods of making the polypeptide conjugates that include contacting a polypeptide having an N-linked glycosylation sequence of the invention and a lipid-pyrophosphate-linked glycosyl moiety (or phospholipid-linked glycosyl moiety) in the presence of an oligosaccharyltransferase under conditions sufficient for the enzyme to transfer the glycosyl moiety to an asparagine residue of the N-linked glycosylation sequence. Exemplary glycosyl moieties that can be conjugated to the glycosylation sequence include GlcNAc, GlcNH, bacillosamine, 6-hydroybacillosamine, GalNAc, GaINH, GlcNAc-GlcNAc, GlcNAc-GlcNH, GlcNAc-Gal, GlcNAc-GlcNAc-Gal-Sia, GlcNAc-Gal-Sia, GlcNAc-GlcNAc-Man, and GlcNAc-GlcNAc-Man(Man)2. The transferred glycosyl moiety is optionally modified with a modifying group, such as a polymer (e.g., PEG). In one example, the modified glycosyl moiety is a GIcNAc or a sialic acid moiety.
摘要翻译：本发明提供了包含外源N联糖基化序列的多肽和多肽缀合物。 N-连接的糖基化序列优选是用于寡糖转移酶（例如细菌PgIB）的底物，其可以催化糖基部分从脂质结合的糖基供体分子（例如，脂质 - 焦磷酸连接的糖基部分）转移至糖基化序列的天冬酰胺（N）残基。在一个实例中，天冬酰胺残基是本发明的外源N联糖基化序列的一部分。本发明进一步提供了制备多肽缀合物的方法，其包括在寡糖转移酶存在下，在具有本发明的N-连接糖基化序列的多肽和脂质 - 焦磷酸酯连接的糖基部分（或磷脂连接的糖基部分）足以使酶将糖基部分转移至N-连接的糖基化序列的天冬酰胺残基。可以与糖基化序列偶联的示例性糖基部分包括GlcNAc，GlcNH，杆菌胺，6-氢溴吡啶胺，GalNAc，GaINH，GlcNAc-GlcNAc，GlcNAc-GlcNH，GlcNAc-Gal，GlcNAc-GlcNAc-Gal-Sia，GlcNAc- Sia，GlcNAc-GlcNAc-Man和GlcNAc-GlcNAc-Man（Man）2。转移的糖基部分任选用修饰基团如聚合物（例如PEG）修饰。在一个实例中，修饰的糖基部分是GlcNAc或唾液酸部分。

9. 发明申请

WO2006034225A2 PRODUCTION OF OLIGOSACCHARIDES BY MICROORGANISMS 审中-公开
标题翻译：微生物生产低聚糖
公开(公告)号：WO2006034225A2
公开(公告)日：2006-03-30
申请号：PCT/US2005033532
申请日：2005-09-19
申请人： NEOSE TECHNOLOGIES INC , JOHNSON KARL , BYRNE NOEL J , DEFREES SHAWN
发明人： JOHNSON KARL , BYRNE NOEL J , DEFREES SHAWN
IPC分类号： C12P19/04
CPC分类号： C12P19/02 , C12P13/02 , C12P19/04
摘要： The present invention relates to the enzymatic synthesis of oligosaccharides, including sialylated product saccharides. In particular, it relates to the use of recombinant cells to take up low cost precursors such as glucose, pyruvate and N-actylglucosamine, and to synthesize activated sugar moieties that are used in oligosaccharide synthesis. The methods make possible the synthesis of many oligosaccharides using microorganisms and readily available, relatively inexpensive starting materials.
摘要翻译：本发明涉及寡糖的酶促合成，包括唾液酸化产物糖。特别涉及使用重组细胞来摄取低成本前体如葡萄糖，丙酮酸和N-酰氨基葡糖胺，以及合成用于寡糖合成的活性糖部分。该方法使得可以使用微生物和易于获得的相对便宜的起始材料合成许多寡糖。

10. 发明申请

WO2005055946A3 GLYCOPEGYLATED GRANULOCYTE COLONY STIMULATING FACTOR 审中-公开
公开(公告)号：WO2005055946A3
公开(公告)日：2006-03-30
申请号：PCT/US2004041004
申请日：2004-12-03
申请人： NEOSE TECHNOLOGIES INC , DEFREES SHAWN , CLAUSEN HENRIK , ZOPF DAVID A , WANG ZHI-GUANG , BOWE CARYN
发明人： DEFREES SHAWN , CLAUSEN HENRIK , ZOPF DAVID A , WANG ZHI-GUANG , BOWE CARYN
IPC分类号： A01N43/04 , A61K20060101
CPC分类号： A61K38/193 , A61K47/60 , C07K14/535
摘要： The present invention provides conjugates between Granulocyte Colony Stimulating Factor 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：本发明提供粒细胞集落刺激因子和PEG部分之间的缀合物。缀合物经由完整的糖基连接基团连接，该基团介于并共价连接到肽和修饰基团之间。通过糖基转移酶的作用，缀合物由糖基化和未糖基化的肽形成。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。还提供了包括缀合物的药物制剂。缀合物的制备方法也在本发明的范围内。

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