-
公开(公告)号：US20180237418A1
公开(公告)日：2018-08-23
申请号：US15881318
申请日：2018-01-26
申请人： Arvinas, Inc.
发明人： Andrew P. Crew , Keith R. Hornberger , Hanqing Dong , Jing Wang , Yimin Qian , Craig M. Crews
IPC分类号： C07D401/14 , C07D471/04 , C07D409/12 , C07D403/06 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/12 , C07D417/14 , A61P35/00
CPC分类号： C07D401/14 , A61P35/00 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
-
公开(公告)号：US20180193470A1
公开(公告)日：2018-07-12
申请号：US15852854
申请日：2017-12-22
申请人： Arvinas, Inc. , Yale University
发明人： Andrew P. Crew , Kurt Zimmermann , Jing Wang , Michael Berlin , Hanqing Dong , Alexey Ishchenko , Yimin Qian , Craig M. Crews , Saul Jaime-Figueroa , George Burslem
IPC分类号： A61K47/54 , A61K47/55 , A61K31/519 , A61K31/427 , A61K31/454 , A61K31/517 , A61K31/506 , A61K31/496 , A61K31/551 , A61K45/06 , A61K38/07 , A61K31/52 , A61K31/55
摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an E3 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 effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
-
公开(公告)号：US20170327469A1
公开(公告)日：2017-11-16
申请号：US15663273
申请日：2017-07-28
申请人： Arvinas, Inc.
发明人： Andrew P. Crew , Hanqing Dong , Jing Wang , Caterina Ferraro , Xin Chen , Yimin Qian
IPC分类号： C07D233/86 , C07D471/10 , C07D401/08 , C07D401/04 , C07D241/28 , C07D239/42 , C07D237/24 , C07D235/02 , C07D231/14 , C07D213/82 , C07C271/24 , C07C255/54 , A61K45/06 , A61K31/454 , A61K31/4439 , A61K31/435 , A61K31/4188 , A61K31/4184 , A61K31/4166 , A61K31/277 , A61K47/54 , C07D491/107 , C07C2601/04
CPC分类号： C07D233/86 , A61K31/277 , A61K31/4166 , A61K31/4184 , A61K31/4188 , A61K31/435 , A61K31/4439 , A61K31/454 , A61K45/06 , A61K47/545 , C07C255/54 , C07C271/24 , C07C2601/04 , C07D213/82 , C07D231/14 , C07D235/02 , C07D237/24 , C07D239/42 , C07D241/28 , C07D401/04 , C07D401/08 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D491/107
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.
-
4.发明授权公开(公告)号：US10723717B2
公开(公告)日：2020-07-28
申请号：US15853166
申请日：2017-12-22
申请人： Arvinas, Inc. , Yale University
发明人： Andrew P. Crew , Keith R. Hornberger , Jing Wang , Hanqing Dong , Yimin Qian , Craig M. Crews , Saul Jaime-Figueroa
IPC分类号： C07D519/00 , C07D401/14 , C07D401/04 , A61K31/4439 , C07D417/14 , A61K31/4545 , C07D487/04 , A61P9/00 , C07D471/04 , A61K31/437 , A61K45/06 , A61P35/00 , A61P43/00 , A61P25/00 , A61K31/4188 , A61K47/54 , A61K47/55
摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
-
5.发明申请公开(公告)号：US20180155322A1
公开(公告)日：2018-06-07
申请号：US15829541
申请日：2017-12-01
申请人： Arvinas, Inc.
发明人： Andrew P. Crew , Yimin Qian , Hanqing Dong , Jing Wang , Keith R. Hornberger , Craig M. Crews
IPC分类号： C07D401/14 , C07K5/083 , A61K38/06 , C07D401/04 , C07D487/08 , A61K31/4725 , A61K31/454 , C07D487/10 , A61K31/4545 , A61K31/551 , A61K31/497 , C07D498/10 , A61K31/5386 , A61K31/501 , C07D471/04 , C07D471/10 , C07D487/04 , A61K31/519 , A61K45/06 , A61K31/496 , C07K5/078 , A61K38/05 , A61P35/00 , A61P15/00
CPC分类号： C07D401/14 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/519 , A61K31/5386 , A61K31/551 , A61K38/05 , A61K38/06 , A61K45/06 , A61K47/54 , A61K47/545 , A61P15/00 , A61P35/00 , C07D401/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D498/10 , C07K5/06034 , C07K5/06165 , C07K5/0806
摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
-
公开(公告)号：US20180147202A1
公开(公告)日：2018-05-31
申请号：US15574770
申请日：2016-06-06
申请人： Arvinas, Inc.
发明人： Andrew P. Crew , Jing Wang , Hanqing Dong , Yimin Qian , Craig M Crews
IPC分类号： A61K31/506 , C07K5/062 , C07D417/04 , A61K47/66 , C07D413/04 , A61K45/06
CPC分类号： A61K31/506 , A61K45/06 , A61K47/665 , A61K2300/00 , C07D413/04 , C07D417/04 , C07K5/06034
摘要： The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) TBK 1. In particular, the present invention is directed to compounds, which contain on one end an E3 ubiquitin ligase binding moiety which binds to an E3 ubiquitin ligase and on the other end a moiety which binds TBK1 such that TBK1 is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of TBK1. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of TBK1.
-
公开(公告)号：US10772962B2
公开(公告)日：2020-09-15
申请号：US15230354
申请日：2016-08-05
申请人： Arvinas, Inc. , Yale University
发明人： Yimin Qian , Hanqing Dong , Jing Wang , Michael Berlin , Andrew P. Crew , Craig M. Crews
IPC分类号： C07D521/00 , A61K45/06 , C07D519/00 , C07D417/14 , C07D495/14 , A61K47/55
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.
-
公开(公告)号：US20180228907A1
公开(公告)日：2018-08-16
申请号：US15953108
申请日：2018-04-13
申请人： Arvinas, Inc.
发明人： Andrew P. Crew , Craig M. Crews , Hanqing Dong , Keith R. Hornberger , Jing Wang , Yimin Qian , Kurt Zimmermann , Michael Berlin , Lawrence B. Snyder
IPC分类号： A61K47/55 , C07D401/04 , C07D401/14 , C07D471/04 , A61K31/437 , A61K31/496 , A61K31/551 , A61K45/06 , A61K31/501 , A61K31/506 , A61K31/497
CPC分类号： A61K47/55 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/551 , A61K45/06 , A61K47/545 , A61P35/00 , C07D401/04 , C07D401/14 , C07D471/04
摘要： The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, 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 disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 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. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
-
公开(公告)号：US20180215731A1
公开(公告)日：2018-08-02
申请号：US15885671
申请日：2018-01-31
申请人： Arvinas, Inc.
发明人： Andrew P. Crew , Michael Berlin , Hanqing Dong , Keith R. Homberger , Yimin Qian , Lawrence B. Snyder , Jing Wang , Kurt Zimmermann
IPC分类号： C07D401/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D495/14 , C07D498/04 , A61P35/02
CPC分类号： C07D401/14 , A61P35/02 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D495/14 , C07D498/04
摘要： The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, 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 disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 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. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
-
公开(公告)号：US20180072711A1
公开(公告)日：2018-03-15
申请号：US15706064
申请日：2017-09-15
申请人： Arvinas, Inc.
发明人： Andrew P. Crew , Yimin Qian , Hanqing Dong , Jing Wang , Craig M. Crews
IPC分类号： C07D417/14 , C07D413/14 , C07D403/14 , C07D403/12
CPC分类号： C07D417/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07K5/06034 , C07K5/06052
摘要： The present disclosure relates to compounds and a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing the compounds, and processes for their preparation. The disclosure also relates to the use of the compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
-
-
-
-
-
-
-
-
-
搜索结果
24 条记录 (耗时 0.039 秒)
