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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。

5. 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。

6. 发明申请

US20050245746A1 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.

7. 发明申请

US20060223764A1 Classes of compounds that interact with gpcrs 有权
标题翻译：与gpcrs相互作用的化合物类
公开(公告)号：US20060223764A1
公开(公告)日：2006-10-05
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： A61K31/7008 , C07H5/04
CPC分类号： A61K31/7008 , A61K31/7034 , A61K31/7036 , A61K31/7052
摘要： A method of inhibiting or effecting the activity of a GPCR which comprises contacting a GPCR with a compound of general formula 1, or a pharmaceutically acceptable salt thereof
摘要翻译：一种抑制或影响GPCR活性的方法，包括使GPCR与通式1的化合物或其药学上可接受的盐接触

8. 发明申请

US20070249526A1 PROCESS FOR THE PREPARATION OF CYCLIC PEPTIDES 审中-公开
标题翻译：制备循环肽的方法
公开(公告)号：US20070249526A1
公开(公告)日：2007-10-25
申请号：US11736517
申请日：2007-04-17
申请人： Giovanni Abbenante , David Fairlie , Robert Reid
发明人： Giovanni Abbenante , David Fairlie , Robert Reid
IPC分类号： A61K38/08 , C07K7/00
CPC分类号： C07K7/56 , A61K38/00
摘要： The present invention relates to a process for the preparation of cyclic peptides, in particular the preparation of Ac-Phe[Orn-Pro-D-Cha-Trp-Arg] known as 3D53 or PMX53 which is a macrocyclic peptidomimetic of the human plasma protein C5a and displays excellent anti-inflammatory activity.
摘要翻译：本发明涉及制备环肽的方法，特别是制备称为3D53的Ac-Phe [Orn-Pro-D-Cha-Trp-Arg]或PMX53，其是人血浆蛋白的大环肽模拟物 C5a并显示出优异的抗炎活性。

9. 发明申请

US20050119167A1 Process for the preparation of cyclic peptides 审中-公开
标题翻译：制备环肽的方法
公开(公告)号：US20050119167A1
公开(公告)日：2005-06-02
申请号：US10839760
申请日：2004-05-05
申请人： Giovanni Abbenante , David Fairlie , Robert Reid , Hua Williams
发明人： Giovanni Abbenante , David Fairlie , Robert Reid , Hua Williams
IPC分类号： A61K38/00 , C07K7/56 , A61K38/12 , C07K5/12
CPC分类号： C07K7/56 , A61K38/00
摘要： The present invention relates to a process for the preparation of cyclic peptides, in particular the preparation of Ac-Phe[Orn-Pro-D-Cha-Trp-Arg] known as 3D53 or PMX53 which is a macrocyclic peptidomimetic of the human plasma protein C5a and displays excellent anti-inflammatory activity.
摘要翻译：本发明涉及制备环肽的方法，特别是制备称为3D53的Ac-Phe [Orn-Pro-D-Cha-Trp-Arg]或PMX53，其是人血浆蛋白的大环肽模拟物 C5a并显示出优异的抗炎活性。

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