OLIGOSACCHARIDES AND OLIGOSACCHARIDE-PROTEIN CONJUGATES DERIVED FROM CLOSTRIDIUM DIFFICILE POLYSACCHARIDE PS-II, METHODS OF SYNTHESIS AND USES THEREOF, IN PARTICULAR AS A VACCINE
    2.
    发明申请
    OLIGOSACCHARIDES AND OLIGOSACCHARIDE-PROTEIN CONJUGATES DERIVED FROM CLOSTRIDIUM DIFFICILE POLYSACCHARIDE PS-II, METHODS OF SYNTHESIS AND USES THEREOF, IN PARTICULAR AS A VACCINE 审中-公开
    寡聚糖苷和寡糖苷 - 蛋白质结合物衍生自离子多糖多糖PS-II,其合成方法及其用途,特别是作为疫苗

    公开(公告)号:US20130344104A1

    公开(公告)日:2013-12-26

    申请号:US14003801

    申请日:2012-03-07

    摘要: The present invention provides an oligosaccharide-protein conjugate comprising an oligosaccharide, in particular synthetic oligosaccharide, derived from the repeating unit of the Clostridium difficile glycopolymer PS-II and a protein carrier. More specifically, the oligosaccharide is the hexasaccharide having the following formula (I) wherein R is a linker or spacer group. In a specific embodiment of the invention, R is (CH2)nNH2, with n being an integer from 2 to 50. The present invention also provides the use of said oligosaccharide and said oligosaccharide-protein conjugate for the treatment or prevention of a disease caused by the pathogen Clostridium difficile. In still further aspects, the present invention also provides a favourable method for preparing said oligosaccharide and said oligosaccharide-protein conjugate.

    摘要翻译: 本发明提供一种寡糖 - 蛋白质结合物,其包含衍生自艰难梭菌聚糖聚合物PS-II的重复单元的寡糖,特别是合成寡糖和蛋白质载体。 更具体地,寡糖是具有下式(I)的六糖,其中R是连接基或间隔基。 在本发明的一个具体实施方案中,R为(CH 2)n NH 2,n为2至50的整数。本发明还提供所述寡糖和所述寡糖 - 蛋白质缀合物用于治疗或预防疾病的用途 由病原体艰难梭菌。 在另外的方面,本发明还提供了制备所述寡糖和所述寡糖 - 蛋白质缀合物的有利方法。

    Linkers for synthesis of oligosaccharides on solid supports
    9.
    发明授权
    Linkers for synthesis of oligosaccharides on solid supports 失效
    用于在固体支持物上合成寡糖的接头

    公开(公告)号:US06579725B1

    公开(公告)日:2003-06-17

    申请号:US09518102

    申请日:2000-03-03

    IPC分类号: G01N33543

    摘要: The present invention relates to versatile linkers for tethering a molecule to a solid support, e.g., for tethering a monomer, oligomer or polymer to a solid support, which are stable to a wide range of reaction conditions, but can be cleaved under well-defined conditions, thereby liberating the molecule from the solid support. Preferably, the linkers are used to tether to the solid support unprotected, partially-protected or fully-protected monosaccharides or oligosaccharides, or unprotected, partially-protected or fully-protected glycoconjugates. The linkers of the present invention may be used to tether to solid supports building blocks useful in the assembly of libraries of other types of small molecules. The present invention also relates to a molecule or plurality of molecules tethered to the solid support via a linker or linkers of the present invention. The present invention also relates to processes for synthesizing molecules, e.g., monomers, oligomers or polymers, on a solid support, wherein a starting material in the synthesis of the molecule, intermediates in the synthesis of the molecule, and the molecule itself are tethered to the solid support during the process via one of the linkers of the present invention. In certain processes of the present invention, the molecule is liberated from the solid support by cleavage of the linker of the present invention.

    摘要翻译: 本发明涉及用于将分子连接到固体支持物的多功能连接体,例如用于将单体,低聚物或聚合物束缚到固体支持物,其在宽范围的反应条件下是稳定的,但可以在明确定义的条件下裂解 从而从固体支持物释放分子。 优选地,接头用于连接到固体支持物未保护的,部分保护的或完全保护的单糖或寡糖,或未保护的,部分保护的或完全保护的糖缀合物。 本发明的接头可用于连接到用于组装其他类型的小分子的文库的固体支持物构建块。 本发明还涉及通过本发明的接头或接头连接到固体支持物上的分子或多个分子。 本发明还涉及在固体支持物上合成分子例如单体,低聚物或聚合物的方法,其中分子合成中的原料,分子合成中的中间体和分子本身被束缚于 在本过程中通过本发明的接头之一的固体支持物。 在本发明的某些方法中,通过切割本发明的接头,分子从固体支持物中释放出来。

    Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries
    10.
    发明授权
    Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries 失效
    用于合成多糖,天然产物和组合文库的保护基团

    公开(公告)号:US06426421B1

    公开(公告)日:2002-07-30

    申请号:US09717197

    申请日:2000-11-21

    IPC分类号: C07D30910

    摘要: One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.

    摘要翻译: 本发明的一个方面涉及任选取代的卤代苄基卤化物等。 这些化合物可用作各种官能团的卤代苄基醚基保护基。 本发明的另一方面涉及所述保护基团在正交保护基团策略中用于合成包含多个合适官能团的复合分子的用途。 本发明的另一方面涉及带有本发明的各种保护基阵列的糖类。 本发明的另一方面涉及寡糖或糖缀合物的合成方法,其包括以下步骤:使用具有本发明的至少一个保护基团的糖糖基化第二分子以得到包含所述糖的产物; 并从所述产品中除去本发明的保护基团。