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    Anomeric derivatives of monosaccharides
    1.
    发明授权
    Anomeric derivatives of monosaccharides 有权
    单糖的异聚衍生物

    公开(公告)号：US07737287B2

    公开(公告)日：2010-06-15

    申请号：US10509092

    申请日：2003-03-28

    申请人： Wim Meutermans ,  Michael Leo West ,  Thanh Le Giang ,  George Adamson ,  Karl Schafer ,  Giovanni Abbenante

    发明人： Wim Meutermans ,  Michael Leo West ,  Thanh Le Giang ,  George Adamson ,  Karl Schafer ,  Giovanni Abbenante

    IPC分类号： C07D315/00

    CPC分类号： C07D405/12 ,  C07D309/14 ,  C07F7/1804 ,  C07H15/12

    摘要： This invention relates to combinatorial libraries of potentially biologically active mainly monosaccharide compounds and to methods of preparing same. These compounds are variously functionalized, with a view to varying lipid solubility, size, function and other properties, with the particular aim of discovering a drug or drug-like compound, or compounds with useful properties. The invention provides intermediates, processes and synthetic strategies for the solution or solid phase synthesis of monosaccharides, variously functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of amino acid and peptide side chain units of isosteres thereof.

    摘要翻译： 本发明涉及潜在的生物活性主要单糖化合物的组合文库及其制备方法。 为了改变脂质溶解度，大小，功能和其他性质，这些化合物被各种功能化，特别是发现药物或药物样化合物或具有有用特性的化合物的目的。 本发明提供了关于糖环的各种功能化的单糖的溶液或固相合成的中间体，方法和合成策略，包括添加芳香性和电荷，以及其等同物的氨基酸和肽侧链单元的放置。

    Anomeric derivatives of monosaccharides
    2.
    发明申请
    Anomeric derivatives of monosaccharides 有权

    公开(公告)号：US20050245746A1

    公开(公告)日：2005-11-03

    申请号：US10509092

    申请日：2003-03-28

    申请人： Wim Meutermans ,  Michael Leo West ,  Thanh Giang ,  George Adamson ,  Karl Schafer ,  Giovanni Abbenante

    发明人： Wim Meutermans ,  Michael Leo West ,  Thanh Giang ,  George Adamson ,  Karl Schafer ,  Giovanni Abbenante

    IPC分类号： C07H9/04 ,  C07D309/14 ,  C07D405/12 ,  C07F7/18 ,  C07H15/12 ,  C07H15/18 ,  C07H15/20 ,  G01N33/53 ,  C07H5/04 ,  C07D211/36 ,  C07D39/14 ,  C07D39/10

    CPC分类号： C07D405/12 ,  C07D309/14 ,  C07F7/1804 ,  C07H15/12

    摘要： A compound of formula (I), wherein, n is 0 or 1; R6 and R7 are hydrogen, or together form a carbonyl oxygen; R1 is selected from the group consisting of hydrogen; —N(Z)Y and —C(Z)Y wherein; when R1 is —N(Z)Y, then: Y is selected from hydrogen, or the following, where G denotes the point of connection to the nitrogen atom in N(Y)Z (i-v); Z is selected from hydrogen or X1; Q is selected from hydrogen or W; the groups W are independently selected from the group consisting of alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, arylalkyl and heteroarylalkyl of 1 to 20 atoms, the groups X1 are independently selected from the group consisting of alkyl, alkenyl, alkynyl, heteroalkyl, acyl, arylacyl, heteroarylacyl, aryl, heteroaryl, arylalkyl and heteroarylalkyl of 1 to 20 atoms, when R1 is —C(Z)Y, then: Y is selected from the group consisting of two hydrogen atoms, a double bonded oxygen to form a carbonyl, and a triple bonded nitrogen to form a nitrile, Z is absent, or is selected from hydrogen or U, wherein U is selected from the group consisting of alkyl, alkenyl, alkynyl, heteroalkyl, aminoalkyl, aminoaryl, aryloxy, alkoxy, heteroaryloxy, aminoaryl, aminoheteroaryl, thioalkyl, thioaryl or thioheteroaryl, acyl, arylacyl, heteroarylacyl, aryl, heteroaryl, arylalkyl and heteroarylalkyl of 1 to 20 atoms, when R1 is H, at least two of the groups R2, R3, R4 and R5 are selected from the group consisting of —OX2 or —N(T)Y, and the others are independently selected from hydrogen, —OH, —OX2, —N(T)Y, wherein Y is as defined above, T is selected from hydrogen or X2; and X2 is independently selected from alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl of 1 to 20 atoms, When R1 is N(Z)Y or C(Z)Y, at least one of the groups R2, R3, R4 and R5 are selected from the group consisting of —OX2 or —N(T)Y, and the others are independently selected from hydrogen, —OH, —OX2, —N(T)Y, wherein Y is as defined above, T is selected from hydrogen or X2; and X2 is independently selected from alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl of 1 to 20 atoms.