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1. 发明申请

WO2007002433A1 PYRROLO [2, 3-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： PYRROLO [2,3-B]吡啶衍生物作为蛋白激酶抑制剂
公开(公告)号：WO2007002433A1
公开(公告)日：2007-01-04
申请号：PCT/US2006/024524
申请日：2006-06-21
申请人： PLEXXIKON, INC. , IBRAHIM, Prabha, N. , ARTIS, Dean, R. , BREMER, Ryan , HABETS, Gaston , MAMO, Shumeye , NESPI, Marika , ZHANG, Chao , ZHANG, Jiazhong , ZHU, Yong-Liang , ZUCKERMAN, Rebecca , WEST, Brian , SUZUKI, Yoshihisa , TSAI, James , HIRTH, Klaus-Peter , BOLLAG, Gideon , SPEVAK, Wayne , CHO, Hanna , GILLETTE, Samuel, J. , WU, Guoxian , ZHU, Hongyao , SHI, Shenghua
发明人： IBRAHIM, Prabha, N. , ARTIS, Dean, R. , BREMER, Ryan , HABETS, Gaston , MAMO, Shumeye , NESPI, Marika , ZHANG, Chao , ZHANG, Jiazhong , ZHU, Yong-Liang , ZUCKERMAN, Rebecca , WEST, Brian , SUZUKI, Yoshihisa , TSAI, James , HIRTH, Klaus-Peter , BOLLAG, Gideon , SPEVAK, Wayne , CHO, Hanna , GILLETTE, Samuel, J. , WU, Guoxian , ZHU, Hongyao , SHI, Shenghua
IPC分类号： C07D471/04 , A61K31/435 , C07C49/517 , A61P35/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07C37/62 , C07C39/27 , C07C45/00 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07D209/08
摘要： Compounds of formula III which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. (Formula III).
摘要翻译：描述了对蛋白激酶有活性的式III化合物，以及使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。（式III）。

2. 发明申请

WO2007002325A1 PYRROLO[2,3-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：吡咯并[2,3-B]吡啶衍生物作为蛋白激酶抑制剂
公开(公告)号：WO2007002325A1
公开(公告)日：2007-01-04
申请号：PCT/US2006/024361
申请日：2006-06-21
申请人： PLEXXIKON, INC. , IBRAHIM, Prahbha, N. , ARTIS, Dean, R. , BREMER, Ryan , MAMO, Shumeye , NESPI, Marika , ZHANG, Chao , ZHANG, Jiazhong , ZHU, Yong-Liang , TSAI, James , HIRTH, Klaus-Peter , BOLLAG, Gideon , SPEVAK, Wayne , CHO, Hanna , GILLETTE, Samuel, J. , WU, Guoxiam , ZHU, Hongyao , SHI, Shenghua
发明人： IBRAHIM, Prahbha, N. , ARTIS, Dean, R. , BREMER, Ryan , MAMO, Shumeye , NESPI, Marika , ZHANG, Chao , ZHANG, Jiazhong , ZHU, Yong-Liang , TSAI, James , HIRTH, Klaus-Peter , BOLLAG, Gideon , SPEVAK, Wayne , CHO, Hanna , GILLETTE, Samuel, J. , WU, Guoxiam , ZHU, Hongyao , SHI, Shenghua
IPC分类号： C07D471/04 , A61K31/435 , C07C49/517 , A61P35/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07C37/62 , C07C39/27 , C07C45/00 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07D209/08
摘要： Compounds of formula III which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
摘要翻译：描述了对蛋白激酶有活性的式III化合物，以及使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。

3. 发明申请

WO2008080001A2 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 审中-公开
标题翻译：化合物及其调节方法及其适应症
公开(公告)号：WO2008080001A2
公开(公告)日：2008-07-03
申请号：PCT/US2007/088412
申请日：2007-12-20
申请人： PLEXXIKON, INC. , IBRAHIM, Prabha N. , BREMER, Ryan , ZHANG, Chao , ZHANG, Jiazhong , HIRTH, Klaus-Peter , WU, Guoxian , ZHU, Hongyao
发明人： IBRAHIM, Prabha N. , BREMER, Ryan , ZHANG, Chao , ZHANG, Jiazhong , HIRTH, Klaus-Peter , WU, Guoxian , ZHU, Hongyao
IPC分类号： C07D471/04 , A61K31/437 , A61P25/00 , A61P29/00 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
摘要翻译：描述了对蛋白激酶有活性的化合物，以及使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。

4. 发明申请

WO2006078228A1 METHODS FOR THE DESIGN OF MOLECULAR SCAFFOLDS AND LIGANDS 审中-公开
标题翻译：分子标记和配体设计方法
公开(公告)号：WO2006078228A1
公开(公告)日：2006-07-27
申请号：PCT/US2003/006477
申请日：2003-03-03
申请人： PLEXXIKON, INC. , HIRTH, Klaus-Peter , MILBURN, Michael, V.
发明人： HIRTH, Klaus-Peter , MILBURN, Michael, V.
IPC分类号： C12Q1/00
CPC分类号： G06F19/16 , G01N33/6803 , G06F19/18 , G06F19/706
摘要： The present invention provides methods of designing ligands that specifically bind to target molecules by testing a set of distinct compounds to identify compound that bind to member of a molecular family of interest. Those compounds that show binding activity can be used as a starting point for ligand design. Unlike previous methods, even compounds that bind with only low affinity are of interest and can be used. Common chemical structures of binding molecules including low affinity binding molecules are identified, thereby providing molecular scaffolds. Co-crystals of the protein and the molecular scaffolds can be formed and analyzed by X-ray crystallography to determine the orientation of the scaffold compounds at the binding site of the molecule. Using the orientation information on a scaffold at the binding site of the molecule, chemically tractable structures of the scaffold are identified that are modified to provide ligands that bind to the target molecule with altered binding affinity or specificity to a target molecule or to members of a molecular family. New and useful ligands can therefore be designed in a rational manner and with a minimum investment of resources using the methods provided.
摘要翻译：本发明提供了通过测试一组不同的化合物来鉴定与感兴趣的分子家族成员结合的化合物来设计与靶分子特异性结合的配体的方法。那些显示结合活性的化合物可以用作配体设计的起点。与以前的方法不同，甚至仅以低亲和力结合的化合物是有意义的并且可以使用。鉴定包括低亲和力结合分子的结合分子的常见化学结构，从而提供分子支架。通过X射线晶体学可以形成和分析蛋白质和分子支架的共晶体，以确定支架化合物在分子结合位点的取向。使用分子的结合位点上的支架上的取向信息，鉴定出支架的化学易溶解结构，其被修饰以提供结合靶分子的配体，其具有改变的对靶分子的结合亲和力或特异性分子家族。因此，新的和有用的配体可以以合理的方式设计，并且使用所提供的方法以最小的资源投入。

5. 发明申请

WO2014194127A1 COMPOUNDS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 审中-公开
标题翻译：用于激酶调节的化合物及其适应症
公开(公告)号：WO2014194127A1
公开(公告)日：2014-12-04
申请号：PCT/US2014/040076
申请日：2014-05-29
申请人： PLEXXIKON INC.
发明人： ZHANG, Chao , HIRTH, Klaus-Peter , IBRAHIM, Prabha N. , NESPI, Marika , SHI, Songyuan , SPEVAK, Wayne , HABETS, Gaston G. , BURTON, Betsy
IPC分类号： C07D213/75 , C07D417/04 , C07D471/04 , C07D487/04 , A61K31/519
CPC分类号： C07D487/04 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K31/5377 , C07D213/75 , C07D417/04 , C07D471/04
摘要： Compounds active on protein kinases and methods for regulating protein kinase pathways are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
摘要翻译：描述了对蛋白激酶有活性的化合物和调节蛋白激酶途径的方法，以及使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。

6. 发明申请

WO2013142427A1 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 审中-公开
标题翻译：化合物及其调节方法及其适应症
公开(公告)号：WO2013142427A1
公开(公告)日：2013-09-26
申请号：PCT/US2013/032835
申请日：2013-03-18
申请人： PLEXXIKON INC.
发明人： BOLLAG, Gideon , HIRTH, Klaus-Peter , IBRAHIM, Prabha N. , LIN, Paul , WEST, Brian
IPC分类号： A61K45/06 , A61K31/436 , A61K31/437 , A61K31/4545 , A61K31/506 , A61P35/00 , A61P19/08 , A61P19/10 , A61P25/28 , A61P25/00 , A61P25/30
CPC分类号： A61K31/444 , A61K9/0053 , A61K31/357 , A61K31/436 , A61K31/437 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K45/06 , A61K2300/00 , C07D471/04
摘要： The present disclosure provides methods of using protein kinase inhibitors for treating diseases and conditions, including diseases and conditions associated with activity of any protein kinase selected from Fms protein kinase including any mutations thereof, Kit protein kinase any mutations thereof, Flt-3 protein kinase any mutations thereof and combinations thereof.
摘要翻译：本公开提供了使用蛋白激酶抑制剂治疗疾病和病症的方法，包括与选自包括其任何突变的Fms蛋白激酶的任何蛋白激酶相关的疾病和病症，Kit蛋白激酶其任何突变，Flt-3蛋白激酶任何其突变及其组合。

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