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1. 发明申请

WO0064485A8 SPECIFICALLY TARGETED CATALYTIC ANTAGONISTS AND USES THEREOF 审中-公开
标题翻译：特异性靶向催化拮抗剂及其用途
公开(公告)号：WO0064485A8
公开(公告)日：2001-02-08
申请号：PCT/US0010988
申请日：2000-04-21
申请人： GENENCOR INT , DAVIS BENJAMIN G , JONES JOHN BRYAN , BOTT RICHARD R , SANFORD KARL JOHN , ESTELL DAVID AARON
发明人： DAVIS BENJAMIN G , JONES JOHN BRYAN , BOTT RICHARD R , SANFORD KARL JOHN , ESTELL DAVID AARON
IPC分类号： C12N9/50 , A45C15/06 , A61K38/43 , A61K38/55 , A61K45/00 , A61K47/48 , A61P3/06 , A61P3/10 , A61P5/26 , A61P5/28 , A61P5/30 , A61P7/02 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/02 , A61P11/08 , A61P21/02 , A61P25/04 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P29/00 , A61P31/12 , A61P43/00 , C12N9/54 , G08B5/00
CPC分类号： B82Y5/00 , A61K47/51 , A61K47/665 , A61K47/6898
摘要： The invention provides chimeric molecules that are catalytic antagonists of a target molecule. The catalytic antagonists of this invention preferably comprise a targeting moiety attached to an enzyme that degrades the molecule specifically bound by the targeting moiety. The catalytic antagonists of this invention thus bind to a target recognized by the targeting moiety (e.g., a receptor) the enzyme component of the chimera then degrades all or part of the target. This typically results in a reduction or loss of activity of the target and release of the chimeric molecule. The chimeric molecule is then free to attack and degrade another target molecule.
摘要翻译：本发明提供作为靶分子的催化拮抗剂的嵌合分子。本发明的催化拮抗剂优选包含与降解由靶向部分特异性结合的分子的酶连接的靶向部分。因此，本发明的催化拮抗剂与靶向部分识别的靶（例如受体）结合，嵌合体的酶组分然后降解靶的全部或部分。这通常导致靶的活性降低或丧失，并释放嵌合分子。然后嵌合分子可以自由地攻击和降解另一个靶分子。

2. 发明申请

WO0064485A9 SPECIFICALLY TARGETED CATALYTIC ANTAGONISTS AND USES THEREOF 审中-公开
公开(公告)号：WO0064485A9
公开(公告)日：2001-07-19
申请号：PCT/US0010988
申请日：2000-04-21
申请人： GENENCOR INT , DAVIS BENJAMIN G , JONES JOHN BRYAN , BOTT RICHARD R , SANFORD KARL JOHN , ESTELL DAVID AARON
发明人： DAVIS BENJAMIN G , JONES JOHN BRYAN , BOTT RICHARD R , SANFORD KARL JOHN , ESTELL DAVID AARON
IPC分类号： C12N9/50 , A45C15/06 , A61K38/43 , A61K38/55 , A61K45/00 , A61K47/48 , A61P3/06 , A61P3/10 , A61P5/26 , A61P5/28 , A61P5/30 , A61P7/02 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/02 , A61P11/08 , A61P21/02 , A61P25/04 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P29/00 , A61P31/12 , A61P43/00 , C12N9/54 , G08B5/00
CPC分类号： B82Y5/00 , A61K47/51 , A61K47/665 , A61K47/6898
摘要： The invention provides chimeric molecules that are catalytic antagonists of a target molecule. The catalytic antagonists of this invention preferably comprise a targeting moiety attached to an enzyme that degrades the molecule specifically bound by the targeting moiety. The catalytic antagonists of this invention thus bind to a target recognized by the targeting moiety (e.g., a receptor) the enzyme component of the chimera then degrades all or part of the target. This typically results in a reduction or loss of activity of the target and release of the chimeric molecule. The chimeric molecule is then free to attack and degrade another target molecule.

3. 发明申请

WO02079394A3 SYNTHESIS AND USE OF GLYCODENDRIMER REAGENTS 审中-公开
标题翻译：合成和使用糖苷类试剂
公开(公告)号：WO02079394A3
公开(公告)日：2003-07-10
申请号：PCT/US0210903
申请日：2002-04-02
申请人： GENENCOR INT , UNIV TORONTO , DAVIS BENJAMIN G , JONES JOHN BRYAN , BOTT RICHARD R
发明人： DAVIS BENJAMIN G , JONES JOHN BRYAN , BOTT RICHARD R
IPC分类号： A61K47/48 , C07H5/10 , C07K14/36 , C12N1/21 , C07H1/00 , A61K31/70 , A61K38/16 , C07H17/00
CPC分类号： B82Y5/00 , A61K47/51 , A61K47/665 , A61K47/6898 , C07H5/10 , C07K14/36
摘要： The present invention relates to a chemically modified mutant protein including a cysteine residue substituted for a residue other than cysteine n a precursor protein, the substituted cysteine residue being subsequently modified by reacting the cysteine residue with a glycosylated thiosulfonate. Also a method of producing the chemically modified mutant protein is provided. The present invention also relates to a glycosylated methanethiosulfonate. Another aspect of the present invention is a method of modifying the functional characteristics of a protein including providing a protein and reacting the protein with a glycosylated methanethiosulfonate reagent under conditions effective to produce a glycoprotein with altered functional characteristics as compared to the protein. In addition, the present invention relates to methods of determining the structure-function relationships of chemically modified mutant proteins. The present invention also relates to synthetic methods for producing thio-glycoses, the thio-glycoses so produced, and to methods for producing glycodendrimer reagents.
摘要翻译：本发明涉及一种化学修饰的突变蛋白，其包含半胱氨酸残基，其取代了半胱氨酸以外的残基而不是前体蛋白，随后通过半胱氨酸残基与糖基化硫代磺酸酯反应来修饰取代的半胱氨酸残基。还提供了一种生产化学修饰的突变蛋白的方法。本发明还涉及糖基化甲磺酸盐。本发明的另一方面是一种改变蛋白质的功能特征的方法，包括提供蛋白质并使蛋白质与糖基化甲磺酸盐试剂在与蛋白质相比产生具有改变的功能特征的糖蛋白的条件下反应。此外，本发明涉及确定化学修饰的突变蛋白的结构 - 功能关系的方法。本发明还涉及用于制备硫代糖糖，如此制备的硫代糖糖的合成方法，以及制备糖苷配基体试剂的方法。

4. 发明申请

WO2006055437A3 SYNTHESIS AND USE OF GLYCODENDRIMER REAGENTS 审中-公开
标题翻译：合成和使用糖苷类试剂
公开(公告)号：WO2006055437A3
公开(公告)日：2006-07-13
申请号：PCT/US2005040989
申请日：2005-11-14
申请人： GENENCOR INT , ISIS INNOVATION , UNIV TORONTO , BOTT RICHARD R , DAVIS BENJAMIN G , JONES JOHN BRYAN
发明人： BOTT RICHARD R , DAVIS BENJAMIN G , JONES JOHN BRYAN
IPC分类号： C07H1/00 , C07H15/14
CPC分类号： C08G83/003 , C07H1/00 , C07H15/14
摘要： The present invention relates to synthetic methods for producing glycodendrimer reagents from disaccharides having a sulhydryl group
摘要翻译：本发明涉及由具有磺酰基的二糖制备糖苷配基试剂的合成方法

5. 发明申请

WO2006055644A2 SYNTHESIS AND USE OF GLYCODENDRIMER REAGENTS 审中-公开
标题翻译：甘油二酯试剂的合成和使用
公开(公告)号：WO2006055644A2
公开(公告)日：2006-05-26
申请号：PCT/US2005041549
申请日：2005-11-14
申请人： GENENCOR INT , ISIS INNOVATION , UNIV TORONTO , BOTT RICHARD R , DAVIS BENJAMIN G , JONES JOHN BRYAN
发明人： BOTT RICHARD R , DAVIS BENJAMIN G , JONES JOHN BRYAN
CPC分类号： C07H5/10
摘要： The present invention relates to a chemically modified mutant protein including a cysteine residue substituted for a residue other than cysteine n a precursor protein, the substituted cysteine residue being subsequently modified by reacting the cysteine residue with a glycosylated thiosulfonate. Also a method of producing the chemically modified mutant protein is provided. The present invention also relates to a glycosylated methanethiosulfonate. Another aspect of the present invention is a method of modifying the functional characteristics of a protein including providing a protein and reacting the protein with a glycosylated methanethiosulfonate reagent under conditions effective to produce a glycoprotein with altered functional characteristics as compared to the protein. In addition, the present invention relates to methods of determining the structure-function relationships of chemically modified mutant proteins. The present invention also relates to synthetic methods for producing thio-glycoses, the thio-glycoses so produced, and to methods for producing glycodendrimer reagents.
摘要翻译：本发明涉及化学修饰的突变蛋白质，其包含半胱氨酸残基取代除半胱氨酸之外的残基前体蛋白质，随后通过使半胱氨酸残基与糖基化硫代磺酸盐反应来修饰取代的半胱氨酸残基。还提供了生产化学修饰的突变蛋白的方法。本发明还涉及糖基化的甲硫代磺酸盐。本发明的另一个方面是改变蛋白质的功能特征的方法，包括提供蛋白质并且使蛋白质与糖基化甲硫代磺酸盐试剂在有效产生与蛋白质相比具有改变的功能特性的糖蛋白的条件下反应。另外，本发明涉及确定化学修饰的突变蛋白的结构 - 功能关系的方法。本发明还涉及用于产生硫代糖的合成方法，由此产生的硫代糖，并且涉及用于生产糖代码二聚体试剂的方法。

6. 发明申请

WO2004093787A2 USE OF GLYCODENDRIMER REAGENTS FOR INHIBITING ADHESION BY MICROORGANISMS 审中-公开
标题翻译：谷氨酰胆碱试剂用于抑制微生物粘附的用途
公开(公告)号：WO2004093787A2
公开(公告)日：2004-11-04
申请号：PCT/US2004011605
申请日：2004-04-14
申请人： GENENCOR INT , UNIV TORONTO , UNIV OXFORD , BOTT RICHARD R , COWAN M M , DAVIS BENJAMIN G , JONES JOHN BRYAN
发明人： BOTT RICHARD R , COWAN M M , DAVIS BENJAMIN G , JONES JOHN BRYAN
IPC分类号： A61K20060101 , A61K38/48 , C07H5/10 , C07K14/36 , C12N1/21 , C12N9/48 , A61K
CPC分类号： C07H5/10 , A61K38/43 , A61K38/48 , A61K38/482 , B82Y5/00 , C07K14/36
摘要： The present invention is directed to glyodendrimeric proteases, composition with glycodendrimeric proteases and methods for inhibiting adhesion binding in microorganisms by contacting microorganisms with a glycodendrimeric protease or a composition with a glycodendrimeric protease. The invention may be used to treat patients in need of treatment.

7. 发明申请

WO0001712A2 CHEMICALLY MODIFIED PROTEINS WITH A CARBOHYDRATE MOIETY 审中-公开
公开(公告)号：WO0001712A2
公开(公告)日：2000-01-13
申请号：PCT/US9915138
申请日：1999-07-02
申请人： GENENCOR INT
发明人： JONES J BRYAN , DAVIS BENJAMIN G
IPC分类号： C12N15/09 , C07K14/00 , C12N9/54 , C12N9/96 , C12Q1/25 , C12Q1/37 , C07K
CPC分类号： B82Y5/00 , C12N9/54
摘要： The present invention relates to a chemically modified mutant protein including a cysteine residue substituted for a residue other than cysteine in a precursor protein, the substituted cysteine residue being subsequently modified by reacting the cysteine residue with a glycosylated thiosulfonate. Also, a method of producing the chemically modified mutant protein is provided. The present invention also relates to a glycosylated methanethiosulfonate. Another aspect of the present invention is a method of modifying the functional characteristics of a protein including providing a protein and reacting the protein with a glycosylated methanethiosulfonate reagent under conditions effective to produce a glycoprotein with altered functional characteristics as compared to the protein. In addition, the present invention relates to methods of determining the structure-function relationships of chemically modified mutant proteins.

8. 发明申请

WO0037658A3 CHEMICALLY MODIFIED ENZYMES WITH MULTIPLE CHARGED VARIANTS 审中-公开
标题翻译：具有多种带电变体的化学修饰的酶
公开(公告)号：WO0037658A3
公开(公告)日：2000-11-09
申请号：PCT/US9930362
申请日：1999-12-20
申请人： GENENCOR INT
发明人： DAVIS BENJAMIN G , JONES JOHN BRYAN , BOTT RICHARD R
IPC分类号： G01N33/483 , C11D3/386 , C12N9/50 , C12N9/54 , C12N9/64 , C12N15/55 , C12Q1/34 , C12R1/07 , C12N15/57 , C12Q1/37
CPC分类号： C12N9/6408 , C12N9/50 , C12N9/54 , C12N2310/334
摘要： This invention provides modified enzymes comprising one or more amino acid residues replaced by cysteine residues, where the cysteine residues are modified by replacing the thiol hydrogen in the cysteine residues with a substituent group providing a thiol side chain comprising a multiply charged moiety. The enzymes show improved interaction and/or specificity and/or activity with charged substrates.
摘要翻译：本发明提供了包含一个或多个氨基酸残基被半胱氨酸残基取代的修饰酶，其中半胱氨酸残基通过用提供包含多电荷部分的硫醇侧链的取代基取代半胱氨酸残基中的巯基氢而被修饰。这些酶与带电底物显示改善的相互作用和/或特异性和/或活性。

9. 发明申请

WO0001712A9 CHEMICALLY MODIFIED PROTEINS WITH A CARBOHYDRATE MOIETY 审中-公开
标题翻译：具有碳水化合物晶体的化学修饰的蛋白质
公开(公告)号：WO0001712A9
公开(公告)日：2000-06-22
申请号：PCT/US9915138
申请日：1999-07-02
申请人： GENENCOR INT
发明人： JONES J BRYAN , DAVIS BENJAMIN G
IPC分类号： C12N15/09 , C07K14/00 , C12N9/54 , C12N9/96 , C12Q1/25 , C12Q1/37 , C07K1/107 , C12N9/00 , C12N15/00 , C12N15/52 , C12N15/57
CPC分类号： B82Y5/00 , C12N9/54
摘要： The present invention relates to a chemically modified mutant protein including a cysteine residue substituted for a residue other than cysteine in a precursor protein, the substituted cysteine residue being subsequently modified by reacting the cysteine residue with a glycosylated thiosulfonate. Also, a method of producing the chemically modified mutant protein is provided. The present invention also relates to a glycosylated methanethiosulfonate. Another aspect of the present invention is a method of modifying the functional characteristics of a protein including providing a protein and reacting the protein with a glycosylated methanethiosulfonate reagent under conditions effective to produce a glycoprotein with altered functional characteristics as compared to the protein. In addition, the present invention relates to methods of determining the structure-function relationships of chemically modified mutant proteins.
摘要翻译：本发明涉及化学修饰的突变蛋白质，其包含取代前体蛋白质中半胱氨酸以外的残基的半胱氨酸残基，随后通过使半胱氨酸残基与糖基化硫代磺酸盐反应来修饰取代的半胱氨酸残基。而且，提供了生产化学修饰的突变蛋白的方法。本发明还涉及糖基化的甲硫代磺酸盐。本发明的另一个方面是改变蛋白质的功能特征的方法，包括提供蛋白质并且使蛋白质与糖基化甲硫代磺酸盐试剂在有效产生与蛋白质相比具有改变的功能特性的糖蛋白的条件下反应。另外，本发明涉及确定化学修饰的突变蛋白的结构 - 功能关系的方法。

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