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1. 发明申请

WO2011153553A2 METHODS AND COMPOSITIONS FOR KINASE INHIBITION 审中-公开
标题翻译：用于激酶抑制的方法和组合物
公开(公告)号：WO2011153553A2
公开(公告)日：2011-12-08
申请号：PCT/US2011/039347
申请日：2011-06-06
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , GARSKE, Adam, L , SHOKAT, Kevan, M.
发明人： GARSKE, Adam, L , SHOKAT, Kevan, M.
CPC分类号： C07D487/04 , C07D239/94 , C07D403/12 , C07D409/12 , C12N9/12
摘要： The present invention sets forth a new chemical genetic approach for engineering kinase enzymes with a cysteine gatekeeper residue as well as for developing electrophilic inhibitors thereto. The present invention also provides a Src proto-oncogenic tyrosine kinase with a cysteine gatekeeper that recapitulates wild type activity and can be irreversibly inhibited both in vitro and in cells. The present invention also provides methods and compositions for modulating kinases and for treating kinase-associated diseases.
摘要翻译：本发明提出了具有半胱氨酸关守残基的工程激酶的新的化学遗传方法以及用于开发亲电抑制剂。本发明还提供了具有半胱氨酸关守的Src原癌基因酪氨酸激酶，其重现野生型活性，并且可以在体外和细胞中不可逆地抑制。本发明还提供了调节激酶和治疗激酶相关疾病的方法和组合物。

2. 发明申请

WO2006068760A2 ANTI-INFLAMMATORY PYRAZOLOPYRIMIDINES 审中-公开
标题翻译：抗炎药吡唑并嘧啶类
公开(公告)号：WO2006068760A2
公开(公告)日：2006-06-29
申请号：PCT/US2005042524
申请日：2005-11-21
申请人： UNIV CALIFORNIA , BIOSEEK INC , SHOKAT KEVAN M , SEPETOV NIKOLAI , ZHANG CHAO , GSCHWEND HIENZ , KUNKEL ERIC J
发明人： SEPETOV NIKOLAI , ZHANG CHAO , GSCHWEND HIENZ , KUNKEL ERIC J
IPC分类号： C07D487/04 , A61K31/505 , A61P29/00 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides anti-inflammatory compounds useful in the treatment of diseases and conditions in which inflammation is involved in disease progression or the manifestation of symptoms of the disease or condition.
摘要翻译：本发明提供了用于治疗其中炎症参与疾病进展或疾病或病症症状的表现的疾病和病症的抗炎化合物。

3. 发明申请

WO2005007085A3 PYRAZOLO PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2005007085A3
公开(公告)日：2005-01-27
申请号：PCT/US2004/019782
申请日：2004-06-21
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , TANAKA, Masahiro , ZHANG, Chao , SHOKAT, Kevan, M. , BURLINGAME, Alma, L. , HANSEN, Kirk , BATEMAN, Raynard, L. , DIMAGNO, Stephen, G.
发明人： TANAKA, Masahiro , ZHANG, Chao , SHOKAT, Kevan, M. , BURLINGAME, Alma, L. , HANSEN, Kirk , BATEMAN, Raynard, L. , DIMAGNO, Stephen, G.
IPC分类号： C07D487/04
摘要： This invention generally relates to pyrazolo pyrimidine derivatives useful as, inter alia, inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. More specifically, the invention relates to pyrazolo pyrimidine derivatives, including derivatives and analogs of SDR inhibitors, pharmaceutical compositions containing derivatives and analogs of SDR inhibitors, methods of making derivatives and analogs of SDR inhibitors and methods of use thereof.

4. 发明申请

WO0107659A3 METHODS FOR IDENTIFYING INHIBITORS OF SIGNALING MOLECULES 审中-公开
标题翻译：识别信号分子抑制剂的方法
公开(公告)号：WO0107659A3
公开(公告)日：2001-03-22
申请号：PCT/US0019912
申请日：2000-07-21
申请人： UNIV PRINCETON , SHOKAT KEVAN M , BISHOP ANTHONY
发明人： SHOKAT KEVAN M , BISHOP ANTHONY
IPC分类号： G01N33/53 , C07D487/04 , C12Q1/02 , C12Q1/48 , G01N37/00 , G01N33/50
CPC分类号： C07D487/04 , C12Q1/485
摘要： The present invention provides a method for the identification of a pattern of changes in cellular responses induced by the selective inhibition of a signaling molecule, by determining the specific effects of a selective inhibitor on a mutant form of a signaling molecule on cellular responses. The pattern of alterations in cellular responses resulting from the inhibition by a selective mutant inhibitor of the mutant signaling molecule are characteristic of the cellular response alterations that a specific inhibitor of the wild-type signaling molecule will produce. After determining the pattern of cellular responses of the mutant cells with the mutant molecule, compounds may be identified capable of inhibiting the wild-type molecule by producing a pattern of cellular responses in wild-type cells matching or having similarity to that of the inhibition of the mutant molecule.
摘要翻译：本发明提供了通过确定选择性抑制剂对细胞反应的信号分子的突变形式的特异性作用来鉴定通过选择性抑制信号分子诱导的细胞反应变化模式的方法。由突变型信号分子的选择性突变抑制剂的抑制引起的细胞反应改变的模式是野生型信号分子的特异性抑制剂将产生的细胞应答改变的特征。在用突变分子确定突变细胞的细胞反应模式之后，可以鉴定能够通过在野生型细胞中匹配或与抑制相似的野生型细胞中产生细胞反应模式来鉴定能够抑制野生型分子的化合物突变分子。

5. 发明申请

WO2011153553A3 METHODS AND COMPOSITIONS FOR KINASE INHIBITION 审中-公开
标题翻译：用于激酶抑制的方法和组合物
公开(公告)号：WO2011153553A3
公开(公告)日：2012-03-29
申请号：PCT/US2011039347
申请日：2011-06-06
申请人： UNIV CALIFORNIA , GARSKE ADAM L , SHOKAT KEVAN M
发明人： GARSKE ADAM L , SHOKAT KEVAN M
IPC分类号： A61K31/495 , A61K31/50
CPC分类号： C07D487/04 , C07D239/94 , C07D403/12 , C07D409/12 , C12N9/12
摘要： The present invention sets forth a new chemical genetic approach for engineering kinase enzymes with a cysteine gatekeeper residue as well as for developing electrophilic inhibitors thereto. The present invention also provides a Src proto-oncogenic tyrosine kinase with a cysteine gatekeeper that recapitulates wild type activity and can be irreversibly inhibited both in vitro and in cells. The present invention also provides methods and compositions for modulating kinases and for treating kinase-associated diseases.
摘要翻译：本发明提出了具有半胱氨酸关守残基的工程激酶的新的化学遗传方法以及用于开发亲电抑制剂。本发明还提供了具有半胱氨酸关守的Src原癌基因酪氨酸激酶，其重现野生型活性，并且可以在体外和细胞中不可逆地抑制。本发明还提供了调节激酶和治疗激酶相关疾病的方法和组合物。

6. 发明申请

WO2010045542A3 FUSED RING HETEROARYL KINASE INHIBITORS 审中-公开
标题翻译：融合环杂合激酶抑制剂
公开(公告)号：WO2010045542A3
公开(公告)日：2010-08-19
申请号：PCT/US2009060985
申请日：2009-10-16
申请人： UNIV CALIFORNIA , DAR ARVIN , SHOKAT KEVAN M
发明人： DAR ARVIN , SHOKAT KEVAN M
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , C07D487/02
CPC分类号： C07D487/04 , A61K31/519
摘要： Provided herein are fused ring heteroaryl compounds useful in a variety of methods, including reducing the activity of certain kinases and treating certain disease states.
摘要翻译：本文提供了用于多种方法的稠合环杂芳基化合物，包括降低某些激酶的活性和治疗某些疾病状态。

7. 发明申请

WO2006012624A3 MECHANISM-BASED CROSSLINKERS 审中-公开
标题翻译：基于机制的交通工具
公开(公告)号：WO2006012624A3
公开(公告)日：2009-05-14
申请号：PCT/US2005026359
申请日：2005-07-21
申请人： UNIV CALIFORNIA , MALY DUSTIN , SHOKAT KEVAN M
发明人： MALY DUSTIN , SHOKAT KEVAN M
IPC分类号： A61K31/7076 , A01N43/50 , C07D239/24 , C07D403/12 , C07H19/167
CPC分类号： C07D403/12 , C07D473/34 , C07H19/16 , C12Q1/485
摘要： The present invention provides novel mechanism-based crosslinkers useful in covalently linking a kinase and an interactor.
摘要翻译：本发明提供了用于共价连接激酶和相互作用剂的新的基于机理的交联剂。

8. 发明申请

WO2008127226A2 P13 KINASE ANTAGONISTS 审中-公开
标题翻译： P13激酶拮抗剂
公开(公告)号：WO2008127226A2
公开(公告)日：2008-10-23
申请号：PCT/US2007008355
申请日：2007-04-04
申请人： UNIV CALIFORNIA , KNIGHT ZACHARY A , SHOKAT KEVAN M , WILLIAMS OLESEGUN
发明人： KNIGHT ZACHARY A , SHOKAT KEVAN M , WILLIAMS OLESEGUN
IPC分类号： A61K31/519 , A61P35/00 , A61P35/02 , C07D487/02 , C12N9/99
CPC分类号： C07D487/04
摘要： The present invention provides novel PB -Kinase antagonists and methods of use thereof.
摘要翻译：本发明提供了新的PB-激酶拮抗剂及其使用方法。

9. 发明申请

WO2013077921A2 SUBSTITUTED PYRAZOLO[3,4-D]PYRIMIDINES AND USES THEREOF 审中-公开
标题翻译：取代的吡唑并[3,4-D]吡嗪并及其用途
公开(公告)号：WO2013077921A2
公开(公告)日：2013-05-30
申请号：PCT/US2012053542
申请日：2012-08-31
申请人： UNIV CALIFORNIA , SINAI SCHOOL MEDICINE , DAR ARVIN C , DAS TIRTHA K , SOS MARTIN , BIVONA TREVER G , SHOKAT KEVAN M , CAGAN ROSS L
发明人： DAR ARVIN C , DAS TIRTHA K , SOS MARTIN , BIVONA TREVER G , SHOKAT KEVAN M , CAGAN ROSS L
CPC分类号： A61K31/519 , A61K45/06 , C07D487/04
摘要： Presented herein are novel therapeutic compounds and methods of using the same for the treatment of cancers.
摘要翻译：本文提出的是新的治疗化合物及其用于治疗癌症的方法。

10. 发明申请

WO2010031056A3 METHODS AND COMPOSITIONS FOR MODULATING IRE1, SRC, AND ABL ACTIVITY 审中-公开
标题翻译：调节IRE1，SRC和ABL活性的方法和组合物
公开(公告)号：WO2010031056A3
公开(公告)日：2010-08-05
申请号：PCT/US2009056993
申请日：2009-09-15
申请人： UNIV CALIFORNIA , WALTER PETER , KORENNYKH ALEXEI , SHOKAT KEVAN M , ZHANG CHAO , FINER-MORE JANET , STROUD ROBERT , EGEA PASCAL , KOROSTELEV ANDREI , DAR ARVIN
发明人： WALTER PETER , KORENNYKH ALEXEI , SHOKAT KEVAN M , ZHANG CHAO , FINER-MORE JANET , STROUD ROBERT , EGEA PASCAL , KOROSTELEV ANDREI , DAR ARVIN
IPC分类号： C07D403/14 , A61K31/497 , A61P25/28 , C07D401/12 , C07D401/14 , C07D403/12
CPC分类号： C07D403/12 , A61K31/4155 , A61K31/497 , C07D401/14 , C07D403/14
摘要： Disclosed herein are, inter alia, compositions for modulating Ire1, Src, or Abl, methods for identifying modulating activity in test compounds, and methods for treating diseases caused by the activity or inactivity of Ire1, Src, or Abl.
摘要翻译：本文公开的是用于调节Ire1，Src或Ab1的组合物，用于鉴定测试化合物中调节活性的方法，以及用于治疗由Ire1，Src或Abl的活性或不活动引起的疾病的方法。

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