Glycan conjugates and methods of use thereof

    公开(公告)号:US10342858B2

    公开(公告)日:2019-07-09

    申请号:US14832993

    申请日:2015-08-21

    Abstract: The present disclosure is directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA3/SSEA4/GloboH associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globo-series glycosphingolipid synthesis. The present disclosure relates to methods and compositions which can modulate the globo-series glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globo-series glycosphingolipid SSEA3/SSEA4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globo-series synthetic pathway. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions.

    Chlorination of sucrose-6-esters
    4.
    发明授权

    公开(公告)号:US10081651B2

    公开(公告)日:2018-09-25

    申请号:US15502372

    申请日:2015-06-16

    CPC classification number: C07H5/02 C07H13/04

    Abstract: There is provided a method for the chlorination of a sucrose-6-acylate to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate, wherein said method comprises the following steps (i) to (v): (i) providing a first component comprising sucrose-6-acylate; (ii) providing a second component comprising a chlorinating agent; (iii) combining said first component and said second component to afford a mixture; (iv) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1′ and 6′ positions thereof; (v) quenching said mixture to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate; wherein at least one of said first component and said second component comprises a reaction vehicle, and said reaction vehicle comprises a tertiary amide; and wherein said mixture comprises a cosolvent during a least a portion of the heating period of step (iv), wherein said cosolvent comprises dimethylacetamide (DMAc).

    Purification of tertiary formamide contaminated with tertiary acetamide
    9.
    发明授权
    Purification of tertiary formamide contaminated with tertiary acetamide 有权
    用叔乙酰胺污染的叔甲酰胺的纯化

    公开(公告)号:US08981079B2

    公开(公告)日:2015-03-17

    申请号:US13378531

    申请日:2010-06-18

    CPC classification number: C07C231/24 C07H1/06 C07H5/02 C07C233/03

    Abstract: A chlorinating agent such as a chloroiminium species is used to remove or neutralize tertiary acetamide present as a contaminant in a tertiary formamide solvent. Tertiary formamide solvent purified or treated in this manner can be used as a reaction vehicle for the chlorination of sucrose-6-acylates, thereby improving the yields of the desired sucralose-6-acylate (an intermediate in the production of sucralose).

    Abstract translation: 使用氯化剂如氯亚胺鎓物质来除去或中和作为叔甲酰胺溶剂中的污染物存在的叔乙酰胺。 以这种方式纯化或处理的叔甲酰胺溶剂可用作蔗糖-6-酰化物氯化反应载体,从而提高所需三氯半乳蔗糖-6-酰化物(三氯蔗糖生产中的中间体)的产率。

Patent Agency Ranking