公开(公告)号：US20190106460A1

公开(公告)日：2019-04-11

申请号：US16129700

申请日：2018-09-12

申请人： Mark Bradley ,  Jeffrey George Andrew Walton ,  Sunay Vijaykumar Chankeshwara ,  Mazen Sleiman ,  George S. Baillie ,  Lucien Gibson

发明人： Mark Bradley ,  Jeffrey George Andrew Walton ,  Sunay Vijaykumar Chankeshwara ,  Mazen Sleiman ,  George S. Baillie ,  Lucien Gibson

IPC分类号： C07K14/00 ,  C07K7/08 ,  C07K7/06 ,  C07K7/64 ,  A61K38/08 ,  C12N9/00

摘要： The present invention relates to compounds which bind to Beta Trans-ducin repeat-containing protein (βTrCP), and modulate the activity of βTrCP. In particular, the invention relates to compounds which demonstrate optimised binding to PTrCP. The invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds as medicaments, specifically for the treatment of disorders associated with aberrant protein degradation, such as cancer. The preferred binding inhibitors are peptides derived from the motive DSGXXS, e.g. DEGFWE, DDGFWD and Succinyl-EGFWE.

公开(公告)号：US20140315784A1

公开(公告)日：2014-10-23

申请号：US14127430

申请日：2012-06-27

申请人： Mark Bradley ,  Jeffrey George Andrew Walton ,  Sunay Vijaykumar Chankeshwara ,  Mazen Sleiman ,  George S. Baillie ,  Lucien Gibson

发明人： Mark Bradley ,  Jeffrey George Andrew Walton ,  Sunay Vijaykumar Chankeshwara ,  Mazen Sleiman ,  George S. Baillie ,  Lucien Gibson

IPC分类号： C07K14/00 ,  C07K7/08 ,  C07K7/64 ,  C07K7/06

CPC分类号： C07K14/00 ,  A61K38/00 ,  A61K38/08 ,  C07K7/06 ,  C07K7/08 ,  C07K7/64 ,  C12N9/93 ,  C12Y603/02019 ,  G01N2333/9015 ,  G01N2500/04

摘要： The present invention relates to compounds which bind to Beta Trans-ducin repeat-containing protein (PTrCP), and modulate the activity of 13TrCP. In particular, the invention relates to compounds which demonstrate optimised binding to PTrCP. The invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds as medicaments, specifically for the treatment of disorders associated with aberrant protein degradation, such as cancer. The preferred binding inhibitors are peptides derived from the motive DSGXXS, e.g. DEGFWE, DDGFWD and Succinyl-EGFWE.

摘要翻译： 本发明涉及结合含β反式-Ducin重复蛋白（PTrCP）的化合物，并调节13TrCP的活性。 特别地，本发明涉及证明优化的结合PTrCP的化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物作为药物的用途，特别是用于治疗与异常蛋白质降解相关的疾病例如癌症。 优选的结合抑制剂是衍生自动力学DSGXXS的肽，例如。 DEGFWE，DDGFWD和琥珀酰-EGFWE。