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    • 5. 发明申请
    • SUGAR CHAIN CONTAINING 4-POSITION HALOGENATED GALACTOSE AND APPLICATION THEREOF
    • 含有4-位羟基糖的糖链及其应用
    • US20090018327A1
    • 2009-01-15
    • US11815329
    • 2006-02-14
    • Shin-Ichiro NishimuraNoriko NagahoriTomoki HamamotoKiyoshi OkuyamaToshitada Noguchi
    • Shin-Ichiro NishimuraNoriko NagahoriTomoki HamamotoKiyoshi OkuyamaToshitada Noguchi
    • C07H5/02C12P19/30
    • C12P19/32C07H15/08
    • The present invention is directed to, for example, an oligosaccharide having at an end thereof a 4-position halogenated galactose residue represented by formula (I): (wherein X represents a halogen atom, and R represents a monosaccharide, an oligosaccharide, or a carrier), a transferase inhibitor containing the oligosaccharide, and a method for inhibiting sugar chain elongation reaction in the presence of glycosyltransferase, the method including employing the inhibitor.The invention also provides a method for producing a 4-position halogenated galactose sugar nucleotide represented by formula (II): (wherein each of R1 to R3 represents a hydroxyl group, an acetyl group, a halogen atom, or a hydrogen atom; X represents a halogen atom; and M represents a hydrogen ion or a metal ion), wherein the method employs bacterium-derived galactokinase and bacterium-derived hexose-1-phosphate uridylyltransferase.The invention is also directed to a sugar chain containing 4-position halogenated galactose envisaged to be employed as drugs and other materials, and to applications of the compound.
    • 本发明涉及例如末端具有由式(I)表示的4-位卤代半乳糖残基的寡糖:(其中,X表示卤素原子,R表示单糖,寡糖,或 载体),含有寡糖的转移酶抑制剂,以及在糖基转移酶存在下抑制糖链延长反应的方法,该方法包括使用该抑制剂。 本发明还提供了由式(II)表示的4-位卤代半乳糖糖核苷酸的制备方法:(式中,R 1〜R 3各自表示羟基,乙酰基,卤素原子或氢原子; X表示 卤素原子; M表示氢离子或金属离子),其中该方法采用细菌来源的半乳糖激酶和细菌来源的己糖-1-磷酸尿苷酰转移酶。 本发明还涉及设想用作药物和其它材料的4-位卤代半乳糖的糖链以及该化合物的应用。
    • 9. 发明授权
    • Sugar chain containing 4-position halogenated galactose and application thereof
    • 含有4-位卤代半乳糖的糖链及其应用
    • US08148112B2
    • 2012-04-03
    • US11815329
    • 2006-02-14
    • Shin-Ichiro NishimuraNoriko NagahoriTomoki HamamotoKiyoshi OkuyamaToshitada Noguchi
    • Shin-Ichiro NishimuraNoriko NagahoriTomoki HamamotoKiyoshi OkuyamaToshitada Noguchi
    • C12P19/50C12P19/52C12P19/26C07H15/00C07H5/04C07H5/06C08B37/00
    • C12P19/32C07H15/08
    • The present invention is directed to, for example, an oligosaccharide having at an end thereof a 4-position halogenated galactose residue represented by formula (I): (wherein X represents a halogen atom, and R represents a monosaccharide, an oligosaccharide, or a carrier), a transferase inhibitor containing the oligosaccharide, and a method for inhibiting sugar chain elongation reaction in the presence of glycosyltransferase, the method including employing the inhibitor. The invention also provides a method for producing a 4-position halogenated galactose sugar nucleotide represented by formula (II): (wherein each of R1 to R3 represents a hydroxyl group, an acetyl group, a halogen atom, or a hydrogen atom; X represents a halogen atom; and M represents a hydrogen ion or a metal ion), wherein the method employs bacterium-derived galactokinase and bacterium-derived hexose-1-phosphate uridylyltransferase. The invention is also directed to a sugar chain containing 4-position halogenated galactose envisaged to be employed as drugs and other materials, and to applications of the compound.
    • 本发明涉及例如末端具有由式(I)表示的4位卤代半乳糖残基的寡糖:(其中X表示卤素原子,R表示单糖,寡糖或 载体),含有寡糖的转移酶抑制剂,以及在糖基转移酶存在下抑制糖链延长反应的方法,该方法包括使用该抑制剂。 本发明还提供了由式(II)表示的4-位卤代半乳糖糖核苷酸的制备方法:(式中,R 1〜R 3各自表示羟基,乙酰基,卤素原子或氢原子; X表示 卤素原子; M表示氢离子或金属离子),其中该方法采用细菌来源的半乳糖激酶和细菌来源的己糖-1-磷酸尿苷酰转移酶。 本发明还涉及设想用作药物和其它材料的4-位卤代半乳糖的糖链以及该化合物的应用。
    • 10. 发明授权
    • Method of producing uridine 5′-diphospho-N-acetylgalactosamine
    • 尿苷5'-二磷酸-N-乙酰半乳糖胺的制备方法
    • US07901912B1
    • 2011-03-08
    • US11576837
    • 2005-10-18
    • Kiyoshi OkuyamaToshitada Noguchi
    • Kiyoshi OkuyamaToshitada Noguchi
    • C12P19/00C12P19/26C12P19/30C12P21/06C12N9/10C12N9/12C12N9/00C07H21/04C08B37/00
    • C12P19/305C12N9/1241
    • The present invention provides a method for enzymatically producing uridine 5′-diphospho-N-acetylgalactosamine (UDP-GalNAc) (which is an important substrate for oligosaccharide synthesis) from uridine 5′-triphosphate (UTP) and N-acetylgalactosamine 1-phosphate (GalNAc 1-P), the method including using, as an enzyme, uridine 5′-diphospho-N-acetylglucosamine pyrophosphorylase (UDP-GlcNAc pyrophosphorylase) derived from a microorganism (exclusive of a pathogenic microorganism). The GalNAc 1-P employed can be prepared from N-acetylgalactosamine and a phosphate donor in a reaction system by use of N-acetylgalactosamine kinase. According to the present invention, uridine 5′-diphospho-N-acetylgalactosamine can be efficiently produced by use of a relatively inexpensive substrate.
    • 本发明提供了一种从尿苷5'-三磷酸(UTP)和N-乙酰半乳糖胺-1-磷酸酯(UTP)酶促产生尿苷5'-二磷酸-N-乙酰半乳糖胺(UDP-GalNAc)(其是寡糖合成的重要底物) GalNAc 1-P),该方法包括使用来自微生物(不包括病原微生物)的尿苷5'-二磷酸-N-乙酰葡糖胺焦磷酸化酶(UDP-GlcNAc焦磷酸化酶)作为酶。 使用的GalNAc 1-P可以通过使用N-乙酰半乳糖胺激酶在反应体系中由N-乙酰半乳糖胺和磷酸供体制备。 根据本发明,可以通过使用相对便宜的底物有效地制备尿苷5'-二磷酸-N-乙酰半乳糖胺。