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公开(公告)号：EP3559002A1
公开(公告)日：2019-10-30
申请号：EP17884473.4
申请日：2017-12-22
发明人： GREW, Andrew, P. , ZIMMERMANN, Kurt , WANG, Jing , BERLIN, Michael , DONG, Hanqing , ISHCHENKO, Alexey , QIAN, Yimin , CREWS, Craig, M. , JAIME-FIGUEROA, Saul , BURSLEM, George
IPC分类号： C07D487/04 , C07D417/04 , C07D403/14 , A61K31/519 , A61P35/00 , A61P29/00
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2.发明公开
公开(公告)号：EP3558994A1
公开(公告)日：2019-10-30
申请号：EP17882647.5
申请日：2017-12-22
发明人： CREW, Andrew, P. , HORNBERGER, Keith, R. , WANG, Jing , DONG, Hanqing , QIAN, Yimin , CREWS, Craig, M. , JAIME-FIGUEROA, Saul
IPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D417/12 , C07D417/14 , A61K31/437 , A61K31/4375
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公开(公告)号：EP3559006A1
公开(公告)日：2019-10-30
申请号：EP17882731.7
申请日：2017-12-13
IPC分类号： C07D495/04 , C07D513/14 , C07D209/32 , A61K31/519
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4.发明公开
公开(公告)号：EP3548483A1
公开(公告)日：2019-10-09
申请号：EP17875354.7
申请日：2017-12-01
发明人： CREW, Andrew, P. , QIAN, Yimin , DONG, Hanqing , WANG, Jing , HORNBERGER, Keith, R. , CREWS, Craig, M.
IPC分类号： C07D417/14 , C07D401/14 , C07D403/14 , A61K31/4725
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5.发明公开COMPOUNDS&METHODS FOR THE ENHANCED DEGRADATION OF TARGETED PROTEINS&OTHER POLYPEPTIDES BY AN E3 UBIQUITIN LIGASE 审中-公开化合物和方法BY E3泛素连接酶特异性蛋白质和其它多肽的提高的移除
公开(公告)号：EP2802608A2
公开(公告)日：2014-11-19
申请号：EP13736209.1
申请日：2013-01-11
申请人： Yale University , GlaxoSmithKline Intellectual Property Development Limited , Cambridge Enterprise Limited University of Cambridge
发明人： CREWS, Craig, M. , BUCKLEY, Dennis , CIULLI, Alessio , JORGENSEN, William , GAREISS, Peter, C. , MOLLE, Inge, Van , GUSTAFSON, Jeffrey , TAE, Hyun-Seop , MICHEL, Julien , HOYER, Dentin, Wade , ROTH, Anke, G. , HARLING, John, David , SMITH, Ian Edward, David , MIAH, Afjal, Hussain , CAMPOS, Sebastien, Andre , LE, Joelle
IPC分类号： C07K19/00 , C07D413/12 , C07D413/14 , C07D207/26 , C07J9/00
CPC分类号： C07D413/14 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K38/05 , A61K38/06 , A61K45/06 , A61K47/545 , A61K47/64 , C07D207/16 , C07D207/26 , C07D401/06 , C07D401/10 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/06 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07J43/003 , C12N9/93
摘要： The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
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公开(公告)号：EP3337476A1
公开(公告)日：2018-06-27
申请号：EP16837498.1
申请日：2016-08-05
申请人： Arvinas, Inc. , Yale University
发明人： QIAN, Yimin , DONG, Hanqing , WANG, Jing , BERLIN, Michael , SIU, Kam , CREW, Andrew, P. , CREWS, Craig, M.
IPC分类号： A61K31/4025 , A61K31/5517 , C07K5/08 , C07D519/00
CPC分类号： A61K45/06 , A61K47/55 , C07D417/14 , C07D495/14 , C07D519/00
摘要： The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
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7.发明公开SMALL-MOLECULE HYDROPHOBIC TAGGING OF FUSION PROTEINS AND INDUCED DEGRADATION OF SAME 审中-公开融合蛋白的疏水性小分子标记及诱导其降解
公开(公告)号：EP2649099A2
公开(公告)日：2013-10-16
申请号：EP11846166.4
申请日：2011-12-06
申请人： Yale University
发明人： CREWS, Craig, M. , TAE, Hyun, Seop , SCHNEEKLOTH, Ashley, R. , NEKLESA, Taavi , SUNDBERG, Thomas
IPC分类号： C07K17/02 , A61K31/708 , A61K31/7076 , A61K31/66 , A61P31/00
CPC分类号： G01N33/573 , A61K47/48015 , A61K47/52 , C07K1/13 , C07K2319/20 , C07K2319/95 , C12N9/14 , G01N33/5008 , G01N2500/10
摘要： The present invention includes compounds that are useful in perturbing or disrupting the function of a transmembrane or intracellular protein, whereby binding of a compound to the transmembrane or intracellular protein induces proteasomal degradation of the transmembrane or intracellular protein. The present invention further includes a method of inducing proteasomal degradation of a transmembrane or intracellular protein. The present invention further includes a method of identifying or validating a protein of interest as a therapeutic target for treatment of a disease state or condition.
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公开(公告)号：EP1814539A2
公开(公告)日：2007-08-08
申请号：EP05856964.1
申请日：2005-11-15
申请人： Yale University
IPC分类号： A61K31/366 , A61P13/12
CPC分类号： A61K31/366
摘要： In certain aspects, the invention relates to use of PKD2 agonists, such as triptolide and triptolide derivatives, to regulate calcium release. In other aspects, the invention relates to use of PKD2 agonists to treat or aid in the treatment of any condition in which a calcium channel, such as the gene product of PKD 1 and/or PKD2, is mutated; calcium signaling is abnormal; or both, such as polycystic kidney disease.
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