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1. 发明授权

US08222381B2 Derivatives of monosaccharides for drug discovery 有权
标题翻译：用于药物发现的单糖衍生物
公开(公告)号：US08222381B2
公开(公告)日：2012-07-17
申请号：US10524048
申请日：2003-08-08
申请人： Michael West , Peter Andrews , Tracie Elizabeth Ramsdale , Wim Meutermans , Giang Thanh Le , Chris Clark , Giovanni Abbenante , Ligong Liu
发明人： Michael West , Peter Andrews , Tracie Elizabeth Ramsdale , Wim Meutermans , Giang Thanh Le , Chris Clark , Giovanni Abbenante , Ligong Liu
IPC分类号： C07H15/04 , C07H15/10 , C07H15/14 , C07H15/20 , C07H5/06 , C07H17/00
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, .
摘要翻译：用于制备潜在生物活性化合物的组合文库的新化合物和方法基于式I的单糖，其为呋喃糖或吡喃糖形式的单糖。

2. 发明申请

US20060167237A1 Derivatives of monosaccharides for drug discovery 有权
标题翻译：用于药物发现的单糖衍生物
公开(公告)号：US20060167237A1
公开(公告)日：2006-07-27
申请号：US10524048
申请日：2003-08-08
申请人： Michael West , Peter Andrews , Tracie Ramsdale , Wim Meutermans , Giang Thanh Le , Chris Clark , Giovanni Abbenante , Ligong Liu
发明人： Michael West , Peter Andrews , Tracie Ramsdale , Wim Meutermans , Giang Thanh Le , Chris Clark , Giovanni Abbenante , Ligong Liu
IPC分类号： C07H5/04
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,
摘要翻译：用于制备潜在生物活性化合物的组合文库的新化合物和方法基于式I的单糖，其为呋喃糖或吡喃糖形式的单糖衍生物，

3. 发明授权

US07875707B2 Disaccharides for drug discovery 有权
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
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 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.

4. 发明申请

US20060121530A1 Disaccharides for drug discovery 有权
标题翻译：用于药物发现的二糖
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
IPC分类号： C40B40/02 , C07H15/04 , C07H11/04
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 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。

5. 发明申请

US20110201794A1 Disaccharides for drug discovery 审中-公开
标题翻译：用于药物发现的二糖
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
IPC分类号： C07H15/26 , C07H1/00 , C07H5/06 , C07H17/02
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 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。

6. 发明授权

US07989422B2 Antibacterial agents 有权
标题翻译：抗菌剂
公开(公告)号：US07989422B2
公开(公告)日：2011-08-02
申请号：US12096771
申请日：2006-12-20
申请人： Wim Meutermans , Declan McKeveney , Johannes Zuegg , Rajaratnam Premraj , Craig Muldoon , Giang Thanh Le
发明人： Wim Meutermans , Declan McKeveney , Johannes Zuegg , Rajaratnam Premraj , Craig Muldoon , Giang Thanh Le
IPC分类号： A61K31/7052 , A61K31/7056 , A61K31/706 , A61K31/416 , C07D235/18 , C07H5/04
CPC分类号： A61K31/34 , A61K31/351 , A61K31/70 , C07D235/30 , C07D235/32 , C07D249/06 , Y02A50/473
摘要： The present invention, in one aspect, provides a method of inhibiting bacterial growth by contacting bacteria with an effective amount of at least one monosaccharide compound of formula (1) as described herein:
摘要翻译：本发明在一个方面提供了通过使细菌与有效量的至少一种如本文所述的式（1）单糖化合物接触来抑制细菌生长的方法：

7. 发明申请

US20090023669A1 Antibacterial Agents 有权
标题翻译：抗菌剂
公开(公告)号：US20090023669A1
公开(公告)日：2009-01-22
申请号：US12096771
申请日：2006-12-20
申请人： Wim Meutermans , Declan McKeveney , Johannes Zuegg , Rajaratnam Premraj , Craig Muldoon , Giang Thanh Le
发明人： Wim Meutermans , Declan McKeveney , Johannes Zuegg , Rajaratnam Premraj , Craig Muldoon , Giang Thanh Le
IPC分类号： A61K31/70 , A61K31/7056 , A61P31/04
CPC分类号： A61K31/34 , A61K31/351 , A61K31/70 , C07D235/30 , C07D235/32 , C07D249/06 , Y02A50/473
摘要： The present invention, in one aspect, provides a method of inhibiting bacterial growth by contacting bacteria with an effective amount of at least one monosaccharide compound of formula (1) as described herein:
摘要翻译：本发明在一个方面提供了通过使细菌与有效量的至少一种如本文所述的式（1）单糖化合物接触来抑制细菌生长的方法：

8. 发明申请

US20080176936A1 Classes of Compounds that Interact with Integrins 审中-公开
标题翻译：与整合素相互作用的化合物类
公开(公告)号：US20080176936A1
公开(公告)日：2008-07-24
申请号：US11813737
申请日：2006-02-02
申请人： Wim Meutermans , Michael L. West , Giang Thanh Le , Judy Halliday , Christopher Clark
发明人： Wim Meutermans , Michael L. West , Giang Thanh Le , Judy Halliday , Christopher Clark
IPC分类号： A61K31/351 , C07D315/00 , A61P3/10
CPC分类号： A61K31/351 , A61K31/70
摘要： A method of inhibiting or effecting the activity of an integral receptor which comprises contacting an integrin with a compound of formula I, or a pharmaceutically acceptable salt thereof; General Formula I Wherein the ring may be of any configuration; Z is sulphur, oxygen, CH2, NH, NRA or hydrogen, in the case where Z is hydrogen then R1 is not present, RA is selected from the set defined for R1 to R5, X is oxygen or NRA providing that at least one X of General Formula I is NRA, X may also combine independently with one of R1 to R5 to form an azide, R1 to R5 are independently selected from the group comprising H, —(CO)R6 or an alkyl, acyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl substituent of 1 to 20 atoms, which is optionally substituted, and can be branched or linear wherein substituents may optionally be further substituted, wherein R6 is selected from the group comprising an alkyl, acyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl substituent of 1 to 20 atoms, which is optionally substituted, and can be branched or linear wherein substituents may optionally be further substituted, with the proviso that XR2 or XR3 or XR4 or XR5 is not NH2, with the further proviso that not more than one of R2 to R5 is hydrogen, where the group X is NRA and RA is not hydrogen, the groups RA and the corresponding group R2 to R5 may combine to form a cycle.
摘要翻译：一种抑制或影响整体受体活性的方法，其包括使整联蛋白与式I化合物或其药学上可接受的盐接触; 通式I其中环可以是任何配置; 在Z是氢的情况下，Z是硫，氧，CH 2，NH，NR A或氢，则不存在R 1 R A选自从R 1至R 5定义的集合，X是氧或NR A，条件是通式I的至少一个X是NR A，X也可以独立地与R 1至R 5中的一个结合形成叠氮化物，R 1至R 5独立地选自H， - （CO）R 6或烷基，酰基，烯基，炔基，杂烷基，芳基，杂芳基，芳基烷基或杂芳基烷基取代基 1至20个原子，其任选被取代，并且可以是支链或直链的，其中取代基可任选被进一步取代，其中R 6选自烷基，酰基，烯基，炔基， 1至20个原子的杂烷基，芳基，杂芳基，芳基烷基或杂芳基烷基取代基，其任选被取代，并且可以是支链或直链的取代基可以任选地被进一步取代，条件是XR 2或XR 3或XR 4或XR 5 不是NH 2，另外条件是R 2至R 5中不超过一个是氢，其中基团X是NR A和R O， A 不是氢，基团R A和相应的基团R 2至R 5可以结合形成一个循环。

9. 发明授权

US07994140B2 Classes of compounds that interact with GPCRs 有权
标题翻译：与GPCR相互作用的化合物类
公开(公告)号：US07994140B2
公开(公告)日：2011-08-09
申请号：US10530851
申请日：2003-10-10
申请人： Wim Meutermans , Glang Le Thanh , Giovanni Abbenante , Gerald Tometzki , Judy Halliday , Johannes Zuegg
发明人： Wim Meutermans , Glang Le Thanh , Giovanni Abbenante , Gerald Tometzki , Judy Halliday , Johannes Zuegg
IPC分类号： A61K31/70 , A01N43/04 , C07H5/04 , C07H5/06 , C07G3/00 , C08B37/00
CPC分类号： A61K31/7008 , A61K31/7034 , A61K31/7036 , A61K31/7052
摘要： The present invention relates to a method of identifying a candidate therapeutic agent. The method comprises contacting a G-Protein Coupled Receptor (GPCR) with a compound of General Formula (I), or a pharmaceutically acceptable salt thereof determining whether the compound inhibits or effects signal transduction activity of the GPCR, wherein a compound that inhibits or effects the activity of the GPCR is a candidate therapeutic agent.
摘要翻译：本发明涉及鉴定候选治疗剂的方法。该方法包括使G-蛋白偶联受体（GPCR）与通式（I）的化合物或其药学上可接受的盐接触，确定该化合物是否抑制或影响GPCR的信号转导活性，其中抑制或影响的化合物 GPCR的活性是候选治疗剂。

10. 发明授权

US07737287B2 Anomeric derivatives of monosaccharides 有权
标题翻译：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。

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