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1. 发明公开

EP1539780A1 DERIVATIVES OF MONOSACCHARIDES FOR DRUG DISCOVERY 审中-公开
标题翻译：单糖药物的发现
公开(公告)号：EP1539780A1
公开(公告)日：2005-06-15
申请号：EP03783843.0
申请日：2003-08-08
申请人： Alchemia Limited
发明人： WEST, Michael, Leo , ANDREWS, Peter , RAMSDALE, Tracie, Elizabeth , MEUTERMANS, Wim , THANH LE, Giang , CLARK, Chris , ABBENANTE, Giovani , LIU, Ligong
IPC分类号： C07H15/18 , C07H5/06 , C07H23/00
CPC分类号： C07H23/00 , C07H5/06 , C07H15/18
摘要： New compounds and methods for the preparation of combinatorial libraries of potentially biologically active compounds are based on monosaccharides of formula (I) being a derivative of a furanose or pyranose form of a monosaccharide.

2. 发明公开

EP1487812A1 ANOMERIC DERIVATIVES OF MONOSACCHARIDES 审中-公开
标题翻译：单糖异头
公开(公告)号：EP1487812A1
公开(公告)日：2004-12-22
申请号：EP03745223.2
申请日：2003-03-28
申请人： Alchemia Limited
发明人： MEUTERMANS, Wim , WEST, Michael, Leo , THANH LE, Giang , ADAMSON, George , SCHAFER, Karl , ABBENANTE, Giovani
IPC分类号： C07D307/20 , C07D307/22 , C07D307/24 , C07D309/08 , C07D309/10 , C07D309/14 , C07H5/04 , C07H7/02 , C07H7/04
CPC分类号： C07D405/12 , C07D309/14 , C07F7/1856 , C07H15/12
摘要： A compound of formula (I), wherein, n is 0 or 1; R6 and R7 are h ydrogen, 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 (=O) 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.

3. 发明公开

EP1501844A1 DISACCHARIDES FOR DRUG DISCOVERY 审中-公开
标题翻译：二糖的药物开发
公开(公告)号：EP1501844A1
公开(公告)日：2005-02-02
申请号：EP03714557.0
申请日：2003-04-24
申请人： Alchemia Limited
发明人： MEUTERMANS, Wim , WEST, Michael, Leo , ADAMSON, George , THANH LE, Giang , DRINNAN, Nicholas, Barry , ABBENANTE, Giovani , BECKER, Bernd , GRATHWOHL, Matthias , RAJARATNAM, Premraj , TOMETZKI, Gerald
IPC分类号： C07H3/04 , C07H3/02 , C07D307/18 , C07D309/10 , C07D309/14
CPC分类号： C07H3/04 , C07H3/02 , C40B40/12 , C40B50/14
摘要： Methods are described for the preparation of combinatorial libraries of potentially biologically active disaccharide compounds. These compounds are variously functionalized, with a view to varying lipid solubility size, function and other properties, with the particular aim of discovering novel drug or drug-like compounds, or compounds with useful properties. The invention provides intermediates, processes and synthetic strategies for the solution or solid phase synthesis of disaccharides, variously functionalised about the sugar ring, including the addition of aromaticity and charge, and the placement of pharmaceutically useful groups and isosteres.

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