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22 条记录 (耗时 0.028 秒)

    SPIROHETEROCYCLIC GLYCOSIDES AND MEHTODS OF USE
    9.
    发明申请
    SPIROHETEROCYCLIC GLYCOSIDES AND MEHTODS OF USE 有权
    螺旋藻糖苷和使用的MEHTODS

    公开(公告)号：US20080182802A1

    公开(公告)日：2008-07-31

    申请号：US11964493

    申请日：2007-12-26

    申请人： Michael J. Hadd ,  Yuanwei Chen ,  Yan Feng ,  Sengen Sen ,  Brian Seed

    发明人： Michael J. Hadd ,  Yuanwei Chen ,  Yan Feng ,  Sengen Sen ,  Brian Seed

    IPC分类号： A61K31/7048 ,  C07H17/04 ,  A61P3/10 ,  A61P3/04

    CPC分类号： C07H17/04

    摘要： Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

    摘要翻译： 提供对钠依赖性葡萄糖转运蛋白SGLT具有抑制作用的化合物。 本发明还提供药物组合物，制备化合物的方法，合成中间体，以及独立地或与其它治疗剂组合使用化合物治疗受SGLT抑制影响的疾病和病症的方法。

    Disulfone reagents and methods of preparing and using same
    10.
    发明授权
    Disulfone reagents and methods of preparing and using same 失效
    二砜试剂及其制备及使用方法

    公开(公告)号：US06812365B2

    公开(公告)日：2004-11-02

    申请号：US10287760

    申请日：2002-11-05

    申请人： Jacqueline Gervay-Hague ,  Michael J. Hadd

    发明人： Jacqueline Gervay-Hague ,  Michael J. Hadd

    IPC分类号： C07F902

    CPC分类号： C07F9/65502 ,  C07F9/4006

    摘要： The present invention provides novel disulfone compounds and methods of preparing and using those compounds to further prepare biologically relevant gem-disulfone analogs of natural enzyme substrates. Methods of using a variety of disulfone compounds as reagents capable of forming symmetrical and non-symmetrical &agr;, &bgr; unsaturated gem-disulfones are also provided. There is also provided a disulfone reagent which reacts with both aromatic and aliphatic aldehydes in good to moderate yield to give exclusively the trans isomer. In accordance with further aspects of the present invention, a methodology for stereospecifically preparing potential gem-disulfone enzyme inhibitors is provided. A synthetic design which allows easy substitution of functional groups so that a number of substrate analogs can be synthesized readily is also provided. In addition, there is provided a new class of compounds which are potential glycosyl transferase inhibitors having characteristics which can inhibit the incorporation of sialic acid and/or fucose into glycoconjugates present at the surface of certain cancer cells. Additionally, a class of potent disulfone-linked catechol-based enzyme inhibitors, such as HIV-1 integrase inhibitors, is provided.

    摘要翻译： 本发明提供了新的二砜化合物以及制备和使用这些化合物以进一步制备天然酶底物的生物学相关的宝石 - 二砜类似物的方法。 还提供了使用各种二砜化合物作为能够形成对称和非对称的α，β不饱和Gem-disulfones的试剂的方法。 还提供了一种二砜试剂，其以良好至中等的产率与芳族和脂族醛反应，仅产生反式异构体。 根据本发明的另外的方面，提供了立体选择性制备潜在的宝石 - 二砜酶抑制剂的方法。 还提供了容易地代替官能团以便容易地合成许多底物类似物的合成设计。 此外，提供了一类新的具有潜在的糖基转移酶抑制剂的化合物，其具有可抑制唾液酸和/或岩藻糖掺入存在于某些癌细胞表面的糖缀合物的特征。 另外，提供一类有效的基于二硫键的儿茶酚基酶抑制剂，如HIV-1整合酶抑制剂。