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公开(公告)号：US20230203030A1
公开(公告)日：2023-06-29
申请号：US17931814
申请日：2022-09-13
发明人： Andrew P. Crew , Craig M. Crews , Xin Chen , Hanqing Dong , Caterina Ferraro , Yimin Qian , Kam Siu , Jing Wang , Meizhong Jin , Michael Berlin , Kurt Zimmermann , Lawrence Snyder
IPC分类号： C07D471/04 , C07D417/14 , A61K45/06 , C07D417/12 , C07D403/06 , C07D403/14 , C07D401/14 , C07D413/14 , C07D405/14 , C07D495/04
CPC分类号： C07D471/04 , A61K45/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D495/04
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：US11512083B2
公开(公告)日：2022-11-29
申请号：US16905641
申请日：2020-06-18
发明人： Andrew P. Crew , Craig M. Crews , Xin Chen , Hanqing Dong , Caterina Ferraro , Yimin Qian , Kam Siu , Jing Wang , Meizhong Jin , Michael Berlin , Kurt Zimmermann
IPC分类号： C07D521/00 , C07D413/14 , C07D471/12 , C07D417/14 , C07D207/16 , C07D207/26 , C07D401/06 , C07D401/10 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/06 , C07D413/12 , A61K31/422 , A61K31/437 , A61K31/4439 , A61K31/5377 , C07D471/04 , A61K45/06 , C07D417/12 , C07D403/14 , C07D401/14 , C07D405/14 , C07D495/04
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：US11427548B2
公开(公告)日：2022-08-30
申请号：US16656526
申请日：2019-10-17
发明人： Andrew P. Crew , Hanqing Dong , Jing Wang , Xin Chen , Yimin Qian , Kurt Zimmermann , Michael Berlin , Lawrence Snyder
IPC分类号： C07D233/86 , C07D417/14 , C07D413/12 , C07D417/12 , A61K45/06 , C07D491/107 , C07D471/10 , C07D235/02 , C07D401/04 , C07D401/08 , C07C255/54 , C07D237/24 , C07C271/24 , C07D241/28 , C07D239/42 , C07D231/14 , C07D213/82 , A61K31/4166 , A61K47/54 , A61K31/4439 , A61K31/4188 , A61K31/435 , A61K31/454 , A61K31/4184 , A61K31/277 , C07D413/14
摘要： The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. 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 Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.
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公开(公告)号：US20200055825A1
公开(公告)日：2020-02-20
申请号：US16656526
申请日：2019-10-17
发明人： Andrew P. Crew , Hanqing Dong , Jing Wang , Xin Chen , Yimin Qian , Kurt Zimmermann , Craig M. Crews , Michael Berlin , Lawrence Snyder
IPC分类号： C07D233/86 , C07D417/14 , C07D413/12 , C07D417/12 , C07D413/14 , A61K45/06 , C07D491/107 , C07D471/10 , C07D235/02 , C07D401/04 , C07D401/08 , C07C255/54 , C07D237/24 , C07C271/24 , C07D241/28 , C07D239/42 , C07D231/14 , C07D213/82 , A61K31/4166 , A61K47/54 , A61K31/4439 , A61K31/4188 , A61K31/435 , A61K31/454 , A61K31/4184 , A61K31/277
摘要： The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. 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 Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.
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公开(公告)号：US10730870B2
公开(公告)日：2020-08-04
申请号：US15074820
申请日：2016-03-18
申请人： Arvinas, Inc. , Yale University
发明人： Andrew P. Crew , Craig M. Crews , Xin Chen , Hanqing Dong , Caterina Ferraro , Yimin Qian , Kam Siu , Jing Wang , Meizhong Jin , Michael Berlin , Kurt Zimmermann , Lawrence Snyder
IPC分类号： C07D521/00 , C07D471/04 , C07D417/14 , A61K45/06 , C07D417/12 , C07D403/06 , C07D403/14 , C07D401/14 , C07D413/14 , C07D405/14 , C07D495/04
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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6.发明申请公开(公告)号：US20160272639A1
公开(公告)日：2016-09-22
申请号：US15074820
申请日：2016-03-18
申请人： Arvinas, Inc. , Yale University
发明人： Andrew P. Crew , Craig M. Crews , Xin Chen , Hanqing Dong , Caterina Ferraro , Yimin Qian , Kam Siu , Jing Wang , Meizhong Jin , Michael Berlin , Kurt Zimmermann , Lawrence Snyder
IPC分类号： C07D471/04 , A61K31/427 , A61K45/06 , C07D417/12 , C07D403/06 , A61K31/4035 , C07D403/14 , A61K31/4155 , C07D401/14 , A61K31/454 , A61K31/4439 , A61K31/5377 , A61K31/437 , C07D413/14 , A61K31/4245 , C07D405/14 , A61K31/422 , A61K31/501 , A61K31/497 , A61K31/53 , C07D417/14
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.
摘要翻译： 本发明涉及双官能化合物，其可用作靶向泛素化的调节剂，特别是根据本发明的双官能化合物降解和/或以其它方式抑制的多种多肽和其它蛋白质的抑制剂。 特别地，本发明涉及化合物，其一端含有与泛素连接酶结合的VHL配体，另一端含有结合靶蛋白的部分，使得靶蛋白置于接近泛素连接酶 以实现该蛋白质的降解（和抑制）。 与靶向多肽的降解/抑制一致，本发明表现出与根据本发明的化合物相关的广泛的药理学活性。
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