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1. 发明申请

WO2007038613A3 SELECTIVE SERINE/THREONINE KINASE INHIBITORS 审中-公开
标题翻译：选择性丝氨酸/螺旋激酶抑制剂
公开(公告)号：WO2007038613A3
公开(公告)日：2007-11-22
申请号：PCT/US2006037699
申请日：2006-09-26
申请人： UNIV CALIFORNIA , TAUNTON JACK , COHEN MICHAEL , SHOKAT KEVAN , ZHANG CHAO
发明人： TAUNTON JACK , COHEN MICHAEL , SHOKAT KEVAN , ZHANG CHAO
IPC分类号： G01N33/00 , G01N33/53
CPC分类号： C07D487/04 , C07D239/42 , C07D403/06 , C07D487/14 , C07D519/00
摘要： Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue.
摘要翻译：在ATP结合位点内具有一个或多个半胱氨酸残基的蛋白激酶的抑制通过使本身或细胞或受试者中的激酶与抑制有效量的具有由两个或更多个的杂环核心结构组成的化合物接触来实现含有至少一个氮环原子的稠合环，以及能够与激酶的ATP结合位点内的半胱氨酸残基反应的亲电取代基。优选的化合物包括具有这样的亲电子取代基的某些吡咯并嘧啶和羟吲哚，以及任选的能够与位于激酶的关守位置的苏氨酸或更小残基相互作用的芳族或杂芳族取代基。缺乏这种半胱氨酸残基的激酶可以被改造或修饰，使得它们能够被这样的化合物抑制，通过用半胱氨酸残基替换ATP结合位点内的缬氨酸或其它氨基酸残基。

2. 发明申请

WO2005000197A3 SELECTIVE SERINE/THREONINE KINASE INHIBITORS 审中-公开
标题翻译：选择性丝氨酸/螺旋激酶抑制剂
公开(公告)号：WO2005000197A3
公开(公告)日：2005-09-01
申请号：PCT/US2004011297
申请日：2004-04-12
申请人： UNIV CALIFORNIA , TAUNTON JACK , COHEN MICHAEL , SHOKAT KEVAN , ZHANG CHAO
发明人： TAUNTON JACK , COHEN MICHAEL , SHOKAT KEVAN , ZHANG CHAO
IPC分类号： A61K20060101 , C07D487/04
CPC分类号： C07D487/04
摘要： Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue.
摘要翻译：在ATP结合位点内具有一个或多个半胱氨酸残基的蛋白激酶的抑制通过使本身或细胞或受试者中的激酶与抑制有效量的具有由两个或更多个的杂环核心结构组成的化合物接触来实现含有至少一个氮环原子的稠合环，以及能够与激酶的ATP结合位点内的半胱氨酸残基反应的亲电取代基。优选的化合物包括具有这样的亲电子取代基的某些吡咯并嘧啶和羟吲哚，以及任选的能够与位于激酶的关守位置的苏氨酸或更小残基相互作用的芳族或杂芳族取代基。缺乏这种半胱氨酸残基的激酶可以被改造或修饰，使得它们能够被这样的化合物抑制，通过用半胱氨酸残基替换ATP结合位点内的缬氨酸或其它氨基酸残基。

3. 发明申请

WO2011047384A9 METHODS OF INHIBITING IRE1 审中-公开
标题翻译：抑制IRE1的方法
公开(公告)号：WO2011047384A9
公开(公告)日：2011-08-25
申请号：PCT/US2010053072
申请日：2010-10-18
申请人： UNIV CALIFORNIA , KORENNYKH ALEXEI , WALTER PETER , LI HAN , DAR ARVIN , SHOKAT KEVAN
发明人： KORENNYKH ALEXEI , WALTER PETER , LI HAN , DAR ARVIN , SHOKAT KEVAN
IPC分类号： A61K31/519 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： A61K31/519

4. 发明申请

WO0185664A8 COMPOUNDS AND METHODS FOR REGULATING BACTERIAL GROWTH AND PATHOGENESIS 审中-公开
标题翻译：化合物和调节细菌生长和致病的方法
公开(公告)号：WO0185664A8
公开(公告)日：2003-11-20
申请号：PCT/US0115221
申请日：2001-05-10
申请人： UNIV PRINCETON , QUOREX PHARMACEUTICALS INC , UNIV TECHNOLOGIES INT , BASSLER BONNIE L , DAMMEL CAROL S , SCHAUDER STEPHAN , SHOKAT KEVAN , STEIN JEFFREY , SURETTE MICHAEL G
发明人： BASSLER BONNIE L , DAMMEL CAROL S , SCHAUDER STEPHAN , SHOKAT KEVAN , STEIN JEFFREY , SURETTE MICHAEL G
IPC分类号： G01N33/50 , A61K31/00 , A61K31/12 , A61K31/121 , A61K31/122 , A61K31/201 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/385 , A61K31/40 , A61K31/42 , A61K31/43 , A61K31/496 , A61K38/00 , A61K39/00 , A61K45/00 , A61K45/06 , A61P31/04 , A61P43/00 , C07C49/395 , C07C49/597 , C07C49/647 , C07C69/145 , C07D215/56 , C07D261/16 , C07D307/12 , C07D307/20 , C07D307/32 , C07D307/33 , C07D307/58 , C07D307/60 , C07D309/10 , C07D317/20 , C07D317/34 , C07D333/32 , C07D499/68 , C07K14/28 , C12N1/20 , C12P7/26 , C12Q1/02 , C12Q1/18 , C12R1/63 , G01N33/15 , A61K319/34 , C12Q1/04
CPC分类号： C12Q1/18 , A61K31/00 , A61K31/34 , A61K31/365 , A61K31/38 , A61K31/385 , A61K31/40 , A61K39/00 , A61K45/06 , C07K14/28 , A61K2300/00
摘要： The invention provides autoinducer-2 analogs that regulate the activity of autoinducer-2 and methods of using such analogs for regulating bacterial growth and pathogenesis.
摘要翻译：本发明提供了调节自体诱导剂-2的活性的自动诱导剂-2类似物和使用这种类似物调节细菌生长和发病机理的方法。

5. 发明申请

WO0185664A3 COMPOUNDS AND METHODS FOR REGULATING BACTERIAL GROWTH AND PATHOGENESIS 审中-公开
标题翻译：化合物和调节细菌生长和致病的方法
公开(公告)号：WO0185664A3
公开(公告)日：2002-08-08
申请号：PCT/US0115221
申请日：2001-05-10
申请人： UNIV PRINCETON , QUOREX PHARMACEUTICALS INC , UNIV TECHNOLOGIES INT , BASSLER BONNIE L , DAMMEL CAROL S , SCHAUDER STEPHAN , SHOKAT KEVAN , STEIN JEFFREY , SURETTE MICHAEL G
发明人： BASSLER BONNIE L , DAMMEL CAROL S , SCHAUDER STEPHAN , SHOKAT KEVAN , STEIN JEFFREY , SURETTE MICHAEL G
IPC分类号： G01N33/50 , A61K31/00 , A61K31/12 , A61K31/121 , A61K31/122 , A61K31/201 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/385 , A61K31/40 , A61K31/42 , A61K31/43 , A61K31/496 , A61K38/00 , A61K39/00 , A61K45/00 , A61K45/06 , A61P31/04 , A61P43/00 , C07C49/395 , C07C49/597 , C07C49/647 , C07C69/145 , C07D215/56 , C07D261/16 , C07D307/12 , C07D307/20 , C07D307/32 , C07D307/33 , C07D307/58 , C07D307/60 , C07D309/10 , C07D317/20 , C07D317/34 , C07D333/32 , C07D499/68 , C07K14/28 , C12N1/20 , C12P7/26 , C12Q1/02 , C12Q1/18 , C12R1/63 , G01N33/15 , A61K319/34 , C12Q1/04
CPC分类号： C12Q1/18 , A61K31/00 , A61K31/34 , A61K31/365 , A61K31/38 , A61K31/385 , A61K31/40 , A61K39/00 , A61K45/06 , C07K14/28 , A61K2300/00
摘要： The invention provides autoinducer-2 analogs that regulate the activity of autoinducer-2 and methods of using such analogs for regulating bacterial growth and pathogenesis.
摘要翻译：本发明提供了调节自体诱导剂-2的活性的自动诱导剂-2类似物和使用这种类似物调节细菌生长和发病机理的方法。

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