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1.发明申请CYCLIZED PEPTIDOMIMETIC SMALL MOLECULE INHIBITORS OF THE WDR5 AND MLL1 INTERACTION 有权WDR5和MLL1相互作用的环化小分子抑制剂公开(公告)号：US20130150309A1
公开(公告)日：2013-06-13
申请号：US13686475
申请日：2012-11-27
Applicant: The Regents of the University of Michigan
Inventor： Shaomeng Wang , Hacer Karatas , Yali Dou , Elizabeth Townsend , Denzil Bernard , Fang Cao
IPC: C07K5/12 , A61N5/10 , C07D255/02 , A61K38/12 , A61K45/00
CPC classification number: C07K5/126 , A61K38/12 , A61K45/00 , A61K45/06 , A61N5/10 , A61N2005/1098 , C07D255/02 , C07K5/0207 , C07K5/021 , C07K5/0215 , C07K5/06034 , C07K5/0815 , C07K5/101 , C07K5/1019 , C07K5/123 , A61K2300/00
Abstract: Cyclic peptidomimetics that inhibit the interaction between MLL1 and WDR5 are disclosed. Methods of inhibiting MLL1 activity and methods of treating cancers also are disclosed.
Abstract translation: 公开了抑制MLL1和WDR5之间相互作用的循环肽模拟物。 还公开了抑制MLL1活性的方法和治疗癌症的方法。
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公开(公告)号：US20210130401A1
公开(公告)日：2021-05-06
申请号：US16605057
申请日：2018-05-15
Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Inventor： Shaomeng Wang , Yangbing Li , Hacer Karatas , Liu Liu , Jeanne Stuckey , Yali Dou , Liyue Huang , Atsunori Kaneshige
Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3a, R3b, R4a, R4b, R5a and R5b are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition, disease, or disorder responsive to inhibition of the WDR5 interaction with its binding partners including, but not limited to, the WDR5-MLL protein-protein interaction.
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3.发明授权Cyclized peptidomimetic small molecule inhibitors of the WDR5 and MLL1 interaction 有权环化的拟肽小分子抑制剂WDR5和MLL1相互作用公开(公告)号：US08980838B2
公开(公告)日：2015-03-17
申请号：US13686475
申请日：2012-11-27
Applicant: The Regents of the University of Michigan
Inventor： Shaomeng Wang , Hacer Karatas , Yali Dou , Elizabeth Townsend , Denzil Bernard , Fang Cao
IPC: A61K38/12 , A61P35/00 , C07K5/12 , A61K45/00 , A61N5/10 , C07D255/02 , C07K5/02 , C07K5/09 , C07K5/103 , C07K5/11 , C07K5/062 , A61K45/06
CPC classification number: C07K5/126 , A61K38/12 , A61K45/00 , A61K45/06 , A61N5/10 , A61N2005/1098 , C07D255/02 , C07K5/0207 , C07K5/021 , C07K5/0215 , C07K5/06034 , C07K5/0815 , C07K5/101 , C07K5/1019 , C07K5/123 , A61K2300/00
Abstract: Cyclic peptidomimetics that inhibit the interaction between MLL1 and WDR5 are disclosed. Methods of inhibiting MLL1 activity and methods of treating cancers also are disclosed.
Abstract translation: 公开了抑制MLL1和WDR5之间相互作用的循环肽模拟物。 还公开了抑制MLL1活性的方法和治疗癌症的方法。
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