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1. 发明申请

WO2006081616A1 CLASSES OF COMPOUNDS THAT INTERACT WITH INTEGRINS 审中-公开
标题翻译：与INTEGRINS互动的化合物类
公开(公告)号：WO2006081616A1
公开(公告)日：2006-08-10
申请号：PCT/AU2006/000129
申请日：2006-02-02
申请人： ALCHEMIA LIMITED , MEUTERMANS, Wim , WEST, Michael Leo , THANH LE, Giang , HALLIDAY, Judy , CLARK, Christopher
发明人： MEUTERMANS, Wim , WEST, Michael Leo , THANH LE, Giang , HALLIDAY, Judy , CLARK, Christopher
IPC分类号： A61K31/351 , A61P3/10 , A61P11/06 , A61P17/02 , A61P25/28 , A61P35/00 , A61P37/08
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, CH 2 , NH, NR A or hydrogen, in the case where Z is hydrogen then R 1 is not present, R A is selected from the set defined for R 1 to R 5 , X is oxygen or NR A providing that at least one X of General Formula I is NR A , X may also combine independently with one of R 1 to R 5 to form an azide, R1 to R5 are independently selected from the group comprising H, -(CO)R 6 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 R 6 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 XR 2 or XR 3 or XR 4 or XR 5 is not NH 2 , with the further proviso that not more than one of R2 to R5 is hydrogen, where the group X is NR A and R A is not hydrogen, the groups R A and the corresponding group R 2 to R 5 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; Z是硫，氧，CH 2，NH，NR A或氢，在Z是氢的情况下，R 1不存在 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为NR A，X还可以独立地与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 N或烷基，酰基，烯基，炔基，杂烷基，芳基，杂芳基，芳烷基或杂芳基烷基取代基至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，杂烷基， 1至20个原子的芳基，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在取代基中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 A， / SUP>不是氢，基团R A和相应的R 2至R 5可以组合形成一个周期。

2. 发明申请

WO2006037159A1 SELECTIVE INHIBITORS 审中-公开
标题翻译：选择性抑制剂
公开(公告)号：WO2006037159A1
公开(公告)日：2006-04-13
申请号：PCT/AU2005/001510
申请日：2005-10-04
申请人： ALCHEMIA LIMITED , TOMETZKI, Gerald, Bernard , MEUTERMANS, Wim , BECKER, Bernd , ZUEGG, Johannes , PREMRAJ, Rajaratnam , MULDOON, Craig , MCKEVENEY, Declan , CONDIE, Glenn, Christopher
发明人： MEUTERMANS, Wim , BECKER, Bernd , ZUEGG, Johannes , PREMRAJ, Rajaratnam , MULDOON, Craig , MCKEVENEY, Declan , CONDIE, Glenn, Christopher
IPC分类号： G01N33/566
CPC分类号： C07H5/06 , C07H15/26 , C07H17/00 , G01N33/566
摘要： A method of identifying biologically active compounds with defined selectivity profile comprises: (c) designing a library of compounds of formula (1) to scan molecular diversity; and (d) assaying the library of compounds in at least two different biological assays.
摘要翻译：鉴定具有确定的选择性谱的生物活性化合物的方法包括：（c）设计式（1）化合物文库以扫描分子多样性; 和（d）在至少两种不同的生物测定中测定化合物文库。

3. 发明申请

WO2005097142A1 BIOLOGICALLY ACTIVE COMPOUNDS WITH ANTI-ANGIOGENIC PROPERTIES 审中-公开
标题翻译：具有抗生物性质的生物活性化合物
公开(公告)号：WO2005097142A1
公开(公告)日：2005-10-20
申请号：PCT/AU2005/000506
申请日：2005-04-07
申请人： ALCHEMIA LIMITED , HALLIDAY, Judy , MEUTERMANS, Wim , TOMETZKI, Gerald , RAMSDALE, Tracie, Elizabeth , ZUEGG, Johannes , BECKER, Bernd , MULDOON, Craig , MCKEVENEY, Declan , PREMRAJ, Rajaratnam , CONDIE, Glenn
发明人： HALLIDAY, Judy , MEUTERMANS, Wim , TOMETZKI, Gerald , RAMSDALE, Tracie, Elizabeth , ZUEGG, Johannes , BECKER, Bernd , MULDOON, Craig , MCKEVENEY, Declan , PREMRAJ, Rajaratnam , CONDIE, Glenn
IPC分类号： A61K31/7008
CPC分类号： A61K31/7008 , A61K31/70
摘要： A method for inhibiting angiogenesis in a subject comprising administering to the subject at least one compound of General Formula (I), wherein the ring or any chiral center(s) may be of any configuration; Z is sulphur, oxygen, CH2, C(O), C(O)HN, 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 and X' are independently oxygen or nitrogen providing that at least one X of General Formula (I) is nitrogen, X or X' may also combine independently with one of R1 to R5 to form an azide, R1 to R5 are independently selected from the following definition which includes but is not limited to H 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, and R6 and R7 are hydrogen, or may combine to form a carbonyl function.
摘要翻译：一种用于抑制受试者血管发生的方法，其包括向所述受试者施用至少一种通式（I）的化合物，其中所述环或任何手性中心可以是任何构型; Z是硫，氧，CH 2，C（O），C（O）HN，NH，NRA或氢时，在Z是氢的情况下，R1不存在，RA选自为R1至R5定义的集合， X和X'独立地是氧或氮，条件是至少一个通式（I）的X是氮，X或X'也可以独立地与R 1至R 5中的一个组合形成叠氮化物，R 1至R 5独立地选自包括但不限于H或任选取代的1-20个原子的烷基，酰基，烯基，炔基，杂烷基，芳基，杂芳基，芳烷基或杂芳基烷基取代基，并且可以是支链或直链的以下定义，和 R6和R7是氢，或者可以结合形成羰基官能团。

4. 发明申请

US20130172210A1 METHOD OF DRUG DESIGN 有权
标题翻译：药物设计方法
公开(公告)号：US20130172210A1
公开(公告)日：2013-07-04
申请号：US13772222
申请日：2013-02-20
申请人： Alchemia Limited
发明人： Gerald B. TOMETZKI , Wim F. MEUTERMANS , Johannes ZUEGG
IPC分类号： G01N33/68
CPC分类号： G01N33/68 , C07H3/02 , C07H15/18 , G01N33/566 , G01N2333/726 , G01N2500/04
摘要： The invention provides a method of identifying biologically active compounds comprising: (a) designing a first library of compounds of formula (1) to scan molecular diversity wherein each compound of the library has at least two pharmacophoric groups R1 to R5 as defined below and wherein compound of the library has same number of pharmacophoric groups; (b) assaying the first library of compounds in one or more biological assay(s); and (c) designing a second library wherein each compound of the second library contains one or more additional pharmacophoric group with respect to the first library; such that the/each component of the first and second library is a compound of formula (1).
摘要翻译：本发明提供了鉴定生物活性化合物的方法，包括：（a）设计式（1）化合物的第一文库以扫描分子多样性，其中文库的每种化合物具有如下定义的至少两个药用基团R 1至R 5，并且其中文库化合物具有相同数量的药效团; （b）在一个或多个生物测定中测定化合物的第一文库; 和（c）设计第二文库，其中第二文库的每种化合物相对于第一文库含有一个或多个另外的药物亲和基团; 使得第一和第二文库的每个组分是式（1）的化合物。

5. 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。

6. 发明授权

US07291623B2 Compounds that interact with kinases 有权
标题翻译：与激酶相互作用的化合物
公开(公告)号：US07291623B2
公开(公告)日：2007-11-06
申请号：US10526388
申请日：2003-09-05
申请人： Wim Meutermans , Karl Schafer , Michael L. West , Craig Muldoon , Fiona Foley , Natalie Bouloc , Gerald Tometzki
发明人： Wim Meutermans , Karl Schafer , Michael L. West , Craig Muldoon , Fiona Foley , Natalie Bouloc , Gerald Tometzki
IPC分类号： A61K31/52 , A61K31/417 , A61K31/4166 , A61K31/4184 , C07D257/04 , C07D473/32
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.
摘要翻译：一种抑制或影响蛋白激酶活性活性的方法，其包括使蛋白激酶与式（I）化合物接触，所述式（I）化合物是呋喃糖或吡喃糖形式的单糖衍生物或其药学上可接受的盐。

7. 发明授权

US08426345B2 Method of drug design 有权
标题翻译：药物设计方法
公开(公告)号：US08426345B2
公开(公告)日：2013-04-23
申请号：US12063920
申请日：2006-10-03
申请人： Wim Meutermans , Johannes Zuegg , Michael L. West
发明人： Gerald B. Tometzki , Wim Meutermans , Johannes Zuegg
IPC分类号： C30B30/06 , C40B50/00 , C40B40/12
CPC分类号： G01N33/68 , C07H3/02 , C07H15/18 , G01N33/566 , G01N2333/726 , G01N2500/04
摘要： The invention provides a method of identifying biologically active compounds comprising: (a) designing a first library of compounds of formula (1) to scan molecular diversity wherein each compound of the library has at least two pharmacophoric groups R1 to R5 as defined below and wherein compound of the library has same number of pharmacophoric groups; (b) assaying the first library of compounds in one or more biological assay(s); and (c) designing a second library wherein each compound of the second library contains one or more additional pharmacophoric group with respect to the first library; such that the/each component of the first and second library is a compound of formula (1).
摘要翻译：本发明提供了鉴定生物活性化合物的方法，包括：（a）设计式（1）化合物的第一文库以扫描分子多样性，其中文库的每种化合物具有如下定义的至少两个药用基团R 1至R 5，并且其中文库化合物具有相同数量的药效团; （b）在一个或多个生物测定中测定化合物的第一文库; 和（c）设计第二文库，其中第二文库的每种化合物相对于第一文库含有一个或多个另外的药物亲和基团; 使得第一和第二文库的每个组分是式（1）的化合物。

8. 发明授权

US08114970B2 Synthetic heparin monosaccharides 有权
标题翻译：合成肝素单糖
公开(公告)号：US08114970B2
公开(公告)日：2012-02-14
申请号：US12354643
申请日：2009-01-15
申请人： Joachim Seifert , Latika Singh , Tracie E. Ramsdale , Michael L. West , Nicholas B. Drinnan
发明人： Joachim Seifert , Latika Singh , Tracie E. Ramsdale , Michael L. West , Nicholas B. Drinnan
IPC分类号： C07H15/18 , C07H15/203
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, for use in the preparation of synthetic heparinoids.
摘要翻译：合成单糖的制备，用于合成类肝素的制备。

9. 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。

10. 发明授权

US07700577B2 Carbohydrate based anti-bacterials 有权
标题翻译：基于碳水化合物的抗菌剂
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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