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    • 1. 发明申请
    • HIV VACCINE
    • 艾滋病疫苗
    • WO2012156750A1
    • 2012-11-22
    • PCT/GB2012/051124
    • 2012-05-18
    • ISIS INNOVATION LIMITEDDAVIS, Benjamin GVIJAYAKRISHNAN, BalakumarDOORES, KatieKOEPPE, Julia
    • DAVIS, Benjamin GVIJAYAKRISHNAN, BalakumarDOORES, KatieKOEPPE, Julia
    • A61K47/48A61K39/00C07H3/06A61P31/18
    • A61K39/21A61K39/12A61K47/6415A61K47/643A61K47/646A61K2039/58A61K2039/6037A61K2039/6075A61K2039/6081C07H3/06C12N2740/16134
    • A glycoconjugate for use in treating or preventing an HIV infection or AIDS, wherein the glycoconjugate comprises an oligosaccharide group which is linked to a carrier protein, wherein the oligosaccharide group is of formula (I): wherein: M3 is a modified mannose unit; each M2 is the same or different and represents a mannose unit or a modified mannose unit; - M1 represents a mannose unit or a modified mannose unit, and the oligosaccharide moiety is linked to the carrier protein via M1; p is 0, or 1; q is 0 or 1; S1 is a saccharide unit or a modified saccharide unit; - r, s and t are zero or an integer from 1 to 5, wherein at least two of r, s and t are zero; wherein the or each modified mannose unit or modified saccharide unit is a mannose unit or saccharide unit having one or more modifications, the or each modification being independently selected from modifications A and B, wherein: modification A is replacement of a hydrogen atom of the mannose unit or saccharide unit with a C1 -3 alkyl group optionally substituted with a hydroxyl group; and modification B is replacement of a hydroxyl group of the mannose unit or saccharide unit with a hydrogen atom.
    • 一种用于治疗或预防HIV感染或AIDS的糖缀合物,其中糖缀合物包含与载体蛋白连接的寡糖基团,其中寡糖基团为式(I):其中:M3是修饰的甘露糖单元; 每个M2相同或不同,表示甘露糖单元或修饰的甘露糖单元; M1表示甘露糖单元或修饰的甘露糖单元,寡糖部分通过M1与载体蛋白连接; p为0或1; q为0或1; S1是糖单元或改性糖单元; -r,s和t为零或1至5的整数,其中r,s和t中的至少两个为零; 其中所述或每个修饰的甘露糖单元或修饰的糖单元是具有一个或多个修饰的甘露糖单元或糖单元,所述或每个修饰独立地选自修饰A和B,其中:修饰A是甘露糖的氢原子的取代 具有任选被羟基取代的C1-C3烷基的单元或糖单元; 改性B是用氢原子代替甘露糖单元或糖类单元的羟基。
    • 7. 发明申请
    • SYNTHESIS AND USE OF GLYCODENDRIMER REAGENTS
    • 合成和使用糖苷类试剂
    • WO2006055437A2
    • 2006-05-26
    • PCT/US2005/040989
    • 2005-11-14
    • GENENCOR INTERNATIONAL, INC.ISIS INNOVATION LTDTHE GOVERNING COUNCIL OF THE UNIVERSITY OF TORONTOBOTT, Richard, R.DAVIS, Benjamin G.JONES, John Bryan
    • BOTT, Richard, R.DAVIS, Benjamin G.JONES, John Bryan
    • C07H1/00C07H15/14
    • C08G83/003C07H1/00C07H15/14
    • 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.
    • 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。
    • 8. 发明申请
    • SYNTHESIS AND USE OF GLYCODENDRIMER REAGENTS
    • 合成和使用糖苷类试剂
    • WO02079394A3
    • 2003-07-10
    • PCT/US0210903
    • 2002-04-02
    • GENENCOR INTUNIV TORONTODAVIS BENJAMIN GJONES JOHN BRYANBOTT RICHARD R
    • DAVIS BENJAMIN GJONES JOHN BRYANBOTT RICHARD R
    • A61K47/48C07H5/10C07K14/36C12N1/21C07H1/00A61K31/70A61K38/16C07H17/00
    • B82Y5/00A61K47/51A61K47/665A61K47/6898C07H5/10C07K14/36
    • 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.
    • 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。
    • 9. 发明申请
    • SYNTHESIS AND USE OF GLYCODENDRIMER REAGENTS
    • 合成和使用糖苷类试剂
    • WO2002079394A2
    • 2002-10-10
    • PCT/US2002/010903
    • 2002-04-02
    • GENENCOR INTERNATIONAL, INC.THE GOVERNING COUNCIL OF THE UNIVERSITY OF TORONTODAVIS, Benjamin, G.JONES, John, BryanBOTT, Richard, R.
    • DAVIS, Benjamin, G.JONES, John, BryanBOTT, Richard, R.
    • C12N
    • B82Y5/00A61K47/51A61K47/665A61K47/6898C07H5/10C07K14/36
    • 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.
    • 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。