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公开(公告)号:EP1440077B1
公开(公告)日:2013-05-01
申请号:EP02766941.5
申请日:2002-09-06
申请人: Alchemia Limited
发明人: SEIFERT, Joachim , SINGH, Latika , RAMSDALE, Tracie, Elizabeth , WEST, Michael, Leo , DRINNAN, Nicholas, Barry
IPC分类号: C07H3/02 , C07H3/04 , C07H3/06 , A61K31/702 , A61P7/02
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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.
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公开(公告)号:EP1440077A1
公开(公告)日:2004-07-28
申请号:EP02766941.5
申请日:2002-09-06
申请人: Alchemia Limited
发明人: SEIFERT, Joachim , SINGH, Latika , RAMSDALE, Tracie, Elizabeth , WEST, Michael, Leo , DRINNAN, Nicholas, Barry
IPC分类号: C07H3/02 , C07H3/04 , C07H3/06 , A61K31/702 , A61P7/02
CPC分类号: C07H9/00 , C07H3/06 , C07H5/04 , C07H7/033 , C07H11/00 , C07H13/04 , C07H13/08 , C07H15/10 , C07H15/18
摘要: Preparation of synthetic monosaccharides, disaccharides, trisaccharides, tetrasaccharides and pentasaccharides for use in the preparation of synthetic heparinoids.
摘要翻译: 制备用于制备合成类肝素的合成单糖,二糖,三糖,四糖和五糖。
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公开(公告)号:EP1546167A1
公开(公告)日:2005-06-29
申请号:EP03793479.1
申请日:2003-09-05
申请人: Alchemia Limited
发明人: MEUTERMANS, Wim , SCHAFER, Karl , WEST, Michael, Leo , MULDOON, Craig , FOLEY, Fiona , BOULOC, Natalie , TOMETZKI, Gerald
IPC分类号: C07H17/02 , C07H17/08 , A61K31/7056 , A61K31/7076 , A61K31/4184 , A61P9/00 , A61P29/00
CPC分类号: C07H17/02 , A61K31/7056 , A61K31/7076 , A61K31/708 , C07H17/08
摘要: A method of inhibiting or effecting the activity of protein kinase activity which comprises contacting a protein kinase with a compound of formula (I) being a derivative of a furanose or pyranose form of a monosaccharide, or a pharmaceutically acceptable salt thereof.
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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
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.
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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
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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