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1. 发明申请

US20050287596A9 Novel ligands and libraries of ligands 审中-公开
标题翻译：配体的新配体和文库
公开(公告)号：US20050287596A9
公开(公告)日：2005-12-29
申请号：US10143455
申请日：2002-05-10
申请人： Andrew Braisted , Daniel Erlanson , Jeffrey Jacobs
发明人： Andrew Braisted , Daniel Erlanson , Jeffrey Jacobs
IPC分类号： C07C321/00 , C07C323/00 , C07C333/00 , C07C381/00 , C12Q1/00 , G01N33/53 , G01N33/543
CPC分类号： C07D207/46 , C07D333/38 , C07D333/70 , C07D401/04 , C07D405/12 , C40B20/08 , C40B30/04 , C40B40/04 , G01N33/6845
摘要： The present invention provides compounds and libraries of compounds having formula (I): wherein L, n, S and A are defined generally and subsets herein. These compounds and libraries of compounds are useful generally in the drug discovery process.
摘要翻译：本发明提供具有式（I）的化合物的化合物和文库：其中L，n，S和A通常定义并在本文中定义。这些化合物和化合物文库通常用于药物发现过程。

2. 发明申请

US20050186630A1 Extended tethering approach for rapid identification of ligands 审中-公开
公开(公告)号：US20050186630A1
公开(公告)日：2005-08-25
申请号：US11107658
申请日：2005-04-15
申请人： Daniel Erlanson , Andrew Braisted , Robert McDowell , John Prescott
发明人： Daniel Erlanson , Andrew Braisted , Robert McDowell , John Prescott
IPC分类号： C07B61/00 , C07D333/38 , C07D333/70 , C07D401/04 , C07D405/12 , C40B30/04 , G01N33/68 , C12Q1/68 , G01N33/53
CPC分类号： C07D333/38 , C07B2200/11 , C07D333/70 , C07D401/04 , C07D405/12 , C40B30/04 , G01N33/6845 , G01N2500/04
摘要： The invention concerns a method for rapid identification and characterization of binding partners for a target molecule, and for providing binding partners with improved binding affinity. More specifically, the invention concerns an improved tethering method for the rapid identification of at least two binding partners that bind near one another to a target molecule.

3. 发明申请

US20070026451A1 Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules 审中-公开
标题翻译：用于快速鉴定结合生物靶分子的小有机分子配体的方法
公开(公告)号：US20070026451A1
公开(公告)日：2007-02-01
申请号：US11540883
申请日：2006-09-28
申请人： Jim Wells , Dan Erlanson , Andrew Braisted
发明人： Jim Wells , Dan Erlanson , Andrew Braisted
IPC分类号： C40B30/06 , C40B40/08 , C40B40/10
CPC分类号： G01N33/566 , G01N33/53 , Y10T436/24
摘要： The present invention is directed to novel methods for rapidly and unambiguously identifying small organic molecule ligands for binding to biological target molecules. Small organic molecule ligands identified according to the methods of the present invention may find use, for example, as novel therapeutic drug lead compounds, enzyme inhibitors, labeling compounds, diagnostic reagents, affinity reagents for protein purification, and the like. Also presented are novel methods for identifying high affinity binding ligands for a biological target molecule of interest, wherein those methods comprise linking two or more small organic molecule ligands previously identified as being capable of binding to the biological target molecule of interest. Biological target molecules include, for example, polypeptides, nucleic acids, carbohydrates, nucleoproteins, glycoproteins, glycolipids and lipoproteins.
摘要翻译：本发明涉及用于快速且明确地鉴定用于结合生物靶分子的小有机分子配体的新方法。根据本发明方法鉴定的小有机分子配体可用于例如新型治疗药物铅化合物，酶抑制剂，标记化合物，诊断试剂，用于蛋白质纯化的亲和试剂等。还提出了用于鉴定感兴趣的生物靶分子的高亲和力结合配体的新方法，其中这些方法包括将先前鉴定为能够结合目的生物靶标分子的两个或更多个小有机分子配体连接。生物靶分子包括例如多肽，核酸，碳水化合物，核蛋白，糖蛋白，糖脂和脂蛋白。

4. 发明授权

US07202033B2 Identification of kinase inhibitors 有权
标题翻译：鉴定激酶抑制剂
公开(公告)号：US07202033B2
公开(公告)日：2007-04-10
申请号：US10394322
申请日：2003-03-20
申请人： John C. Prescott , Andrew Braisted
发明人： John C. Prescott , Andrew Braisted
IPC分类号： C12Q1/68
CPC分类号： C40B30/04 , C12Q1/485 , G01N2500/00
摘要： The invention concerns the identification of protein kinase inhibitors that preferentially bind to the inactive conformation of a target protein kinase. The inhibitors are identified by locking the target protein kinase in an inactive conformation, and using a covalent tethering approach to identify inhibitors preferentially targeting the inactive conformation.
摘要翻译：本发明涉及优先结合靶蛋白激酶的无活性构象的蛋白激酶抑制剂的鉴定。通过将靶蛋白激酶锁定在无活性构象中，并使用共价连接方法鉴定优先靶向非活性构象的抑制物来鉴定抑制剂。

5. 发明申请

US20050142614A1 Methods for ligand discovery 审中-公开
标题翻译：配体发现方法
公开(公告)号：US20050142614A1
公开(公告)日：2005-06-30
申请号：US11054754
申请日：2005-02-09
申请人： Jim Wells , Dan Erlanson , Andrew Braisted
发明人： Jim Wells , Dan Erlanson , Andrew Braisted
IPC分类号： G01N33/531 , C07B61/00 , C07C323/39 , C07C335/04 , C07D207/46 , C07D333/38 , C07D333/70 , C07D401/04 , C07D405/12 , C07K14/00 , C07K14/435 , C12Q1/00 , C12Q1/68 , C12Q1/70 , C40B20/08 , C40B30/04 , C40B40/04 , G01N33/00 , G01N33/53
CPC分类号： C40B40/04 , C07D207/46 , C07D333/38 , C07D333/70 , C07D401/04 , C07D405/12 , C40B20/08 , C40B30/04 , G01N33/6845
摘要： The present invention provides novel methods for ligand discovery. The inventive methods rely on a process termed “tethering” where potential ligands are covalently bonded or “tethered” to a target and subsequently identified.
摘要翻译：本发明提供了配体发现的新方法。本发明的方法依赖于称为“系链”的过程，其中潜在的配体共价键合或“连接”到靶并随后鉴定。

6. 发明申请

US20050084905A1 Identification of kinase inhibitors 审中-公开
标题翻译：鉴定激酶抑制剂
公开(公告)号：US20050084905A1
公开(公告)日：2005-04-21
申请号：US10666927
申请日：2003-09-17
申请人： John Prescott , Andrew Braisted , Joelle Morrow
发明人： John Prescott , Andrew Braisted , Joelle Morrow
IPC分类号： C12Q1/48 , C40B30/04 , G01N33/68 , G01N33/53
CPC分类号： C40B30/04 , C12Q1/485 , G01N2500/00
摘要： The invention concerns the identification of protein kinase inhibitors that preferentially bind to the inactive conformation of a target protein kinase. The inhibitors are identified by locking the target protein kinase in an inactive conformation, and using Tethering to identify inhibitors preferentially targeting the inactive conformation.
摘要翻译：本发明涉及优先结合靶蛋白激酶的无活性构象的蛋白激酶抑制剂的鉴定。通过将靶蛋白激酶锁定在无活性构象中，并使用Tethering鉴定优先靶向非活性构象的抑制物来鉴定抑制剂。

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