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公开(公告)号:US07875707B2
公开(公告)日:2011-01-25
申请号:US10513286
申请日:2003-04-24
申请人: Wim Meutermans , Michael West , George Adamson , Giang Thanh Le , Nicholas B. Drinnan , Giovanni Abbenante , Bernd Becker , Matthias Grathwohl , Premraj Rajaratnam , Gerald Tometzki
发明人: Wim Meutermans , Michael West , George Adamson , Giang Thanh Le , Nicholas B. Drinnan , Giovanni Abbenante , Bernd Becker , Matthias Grathwohl , Premraj Rajaratnam , Gerald Tometzki
IPC分类号: C07H1/00 , C07H15/00 , C07H17/00 , C07H5/04 , C07H5/06 , C07G3/00 , C07G11/00 , C08B37/00 , C13K5/00 , C13K7/00
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 an 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 functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of pharmaceutically useful groups and isosteres.
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公开(公告)号:US20110201794A1
公开(公告)日:2011-08-18
申请号:US12926913
申请日:2010-12-17
申请人: Wim Meutermans , Michael L. West , George Adamson , Giang Thanh Le , Nicholas B. Drinnan , Giovani Abbenante , Bernd Becker , Matthias Grathwohl , Premraj Rajaratnam , Gerald Tometzki
发明人: Wim Meutermans , Michael L. West , George Adamson , Giang Thanh Le , Nicholas B. Drinnan , Giovani Abbenante , Bernd Becker , Matthias Grathwohl , Premraj Rajaratnam , Gerald Tometzki
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 an 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 functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of pharmaceutically useful groups and isosteres.
摘要翻译: 描述了用于制备潜在的生物活性二糖化合物的组合文库的方法。 为了改变脂质溶解度大小,这些化合物被多种功能化,起到其它特性的作用,特别是发现新的药物或药物样化合物或具有有用特性的化合物。 本发明提供了关于糖环的各种功能化的二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,以及放置药学上有用的基团和等体积体。
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公开(公告)号:US20060121530A1
公开(公告)日:2006-06-08
申请号:US10513286
申请日:2003-04-24
申请人: Wim Meutermans , Michael West , George Adamson , Giang Thanh Le , Nicholas Drinnan , Giovani Abbenante , Bernd Becker , Matthias Grathwohl , Premraj Rajaratnam , Gerald Tometzki
发明人: Wim Meutermans , Michael West , George Adamson , Giang Thanh Le , Nicholas Drinnan , Giovani Abbenante , Bernd Becker , Matthias Grathwohl , Premraj Rajaratnam , Gerald Tometzki
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 an 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 functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of pharmaceutically useful groups and isosteres.
摘要翻译: 描述了用于制备潜在的生物活性二糖化合物的组合文库的方法。 为了改变脂质溶解度大小,这些化合物被多种功能化,起到其它特性的作用,特别是发现新的药物或药物样化合物或具有有用特性的化合物。 本发明提供了关于糖环的各种功能化的二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,以及放置药学上有用的基团和等体积体。
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公开(公告)号:US07700577B2
公开(公告)日:2010-04-20
申请号:US10531303
申请日:2003-10-16
申请人: Wim Meutermans , Giang Le Thanh , Giovani Abbenante , Gerald Tometzki , George Adamson , Bernd Becker , Matthias Grathwohl , Premraj Rajaratnam
发明人: Wim Meutermans , Giang Le Thanh , Giovani Abbenante , Gerald Tometzki , George Adamson , Bernd Becker , Matthias Grathwohl , Premraj Rajaratnam
IPC分类号: A61K31/715 , C07H1/00 , A01N25/34
CPC分类号: A61K31/7016 , Y02A50/473
摘要: A method of inhibiting bacterial growth by contacting a bacteria with at least one disaccharide compound of General Formula I,
摘要翻译: 通过使细菌与至少一种通式I的二糖化合物接触来抑制细菌生长的方法,
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公开(公告)号:US20060142217A1
公开(公告)日:2006-06-29
申请号:US10531303
申请日:2003-10-16
申请人: Wim Meutermans , Giang Le Thanh , Giovani Abbenante , Gerald Tometzki , George Adamson , Bernd Becker , Matthias Grathwohl , Premraj Rajaratnam
发明人: Wim Meutermans , Giang Le Thanh , Giovani Abbenante , Gerald Tometzki , George Adamson , Bernd Becker , Matthias Grathwohl , Premraj Rajaratnam
IPC分类号: A61K31/7012
CPC分类号: A61K31/7016 , Y02A50/473
摘要: A method of inhibiting bacterial growth by contacting a bacteria with at least one disaccharide compound of General Formula I,
摘要翻译: 通过使细菌与至少一种通式I的二糖化合物接触来抑制细菌生长的方法,
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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。
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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.
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公开(公告)号:US20100184607A1
公开(公告)日:2010-07-22
申请号:US12184473
申请日:2008-08-01
摘要: A monosaccharide compound of formula I as shown in the specification. Processes for the preparation of the compound of formula I and methods of screening for antibacterial or antibiotic compounds involving the compound of formula I.
摘要翻译: 如说明书所示的式I的单糖化合物。 用于制备式I化合物的方法和涉及式I化合物的抗细菌剂或抗生素化合物的筛选方法。
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公开(公告)号:US08093227B2
公开(公告)日:2012-01-10
申请号:US12184473
申请日:2008-08-01
摘要: A monosaccharide compound of formula I as shown in the specification. Processes for the preparation of the compound of formula I and methods of screening for antibacterial or antibiotic compounds involving the compound of formula I.
摘要翻译: 如说明书所示的式I的单糖化合物。 用于制备式I化合物的方法和涉及式I化合物的抗细菌剂或抗生素化合物的筛选方法。
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公开(公告)号:US07417129B2
公开(公告)日:2008-08-26
申请号:US10419070
申请日:2003-04-17
IPC分类号: C07H15/00
摘要: A monosaccharide compound of formula I as shown in the specification. Processes for the preparation of the compound of formula I and methods of screening for antibacterial or antibiotic compounds involving the compound of formula I.
摘要翻译: 如说明书所示的式I的单糖化合物。 用于制备式I化合物的方法和涉及式I化合物的抗细菌剂或抗生素化合物的筛选方法。
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