-
公开(公告)号：US20210171470A1
公开(公告)日：2021-06-10
申请号：US16888484
申请日：2020-05-29
Applicant: Arvinas Operations, Inc.
Inventor： Andrew P. Crew , Keith R. Hornberger , Lawrence B. Snyder , Kurt Zimmermann , Jing Wang , Michael Berlin , Craig M. Crews , Hanqing Dong
IPC: C07D233/42 , A61K31/166 , C07D211/76 , C07D241/04 , C07D231/12 , C07D213/72 , C07D205/04 , C07D237/08 , C07D239/24 , C07D221/20 , A61K31/277 , A61K47/10 , A61K31/02 , A61K31/497 , C07D209/48 , C07D401/14 , A61K45/06
Abstract: The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 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 disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.
-
公开(公告)号：US20210040044A1
公开(公告)日：2021-02-11
申请号：US17006193
申请日：2020-08-28
Applicant: Arvinas Operations, Inc.
Inventor： Andrew P. Crew , Keith R. Hornberger , Lawrence B. Snyder , Kurt Zimmermann , Jing Wang , Michael Berlin , Hanqing Dong
IPC: C07D233/42 , C07D221/20 , C07D211/76 , C07D205/04 , C07D239/24 , A61K45/06 , C07D209/48 , C07D237/08 , C07D213/72 , A61K31/02 , C07D401/14 , A61K31/166 , A61K31/277 , C07D231/12 , C07D241/04 , A61K31/497 , A61K47/10
Abstract: The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 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 disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.
-
公开(公告)号：US12264157B2
公开(公告)日：2025-04-01
申请号：US17931814
申请日：2022-09-13
Applicant: Arvinas Operations, Inc. , Yale University
Inventor： 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: C07D521/00 , A61K31/422 , A61K31/437 , A61K31/4439 , A61K31/5377 , A61K45/06 , A61P35/00 , C07D207/16 , C07D207/26 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/12 , C07D471/14 , C07D495/04
Abstract: 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：US11858940B2
公开(公告)日：2024-01-02
申请号：US17207330
申请日：2021-03-19
Applicant: Arvinas Operations, Inc.
Inventor： Erika Araujo , Michael Berlin , Steven M. Sparks , Jing Wang , Wei Zhang
IPC: C07D487/04 , A61K45/06 , C07D519/00
CPC classification number: C07D487/04 , A61K45/06 , C07D519/00
Abstract: Bifunctional compounds, which find utility as modulators of non-receptor Leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
-
公开(公告)号：US20230097358A1
公开(公告)日：2023-03-30
申请号：US17699082
申请日：2022-03-19
Applicant: Arvinas Operations, Inc
Inventor： Erika Marina Vieira Araujo , Michael Berlin , Hanqing Dong , Steven M. Sparks , Jing Wang , Wei Zhang
IPC: C07D498/10 , C07D401/14 , C07D417/14 , C07D413/14 , C07D487/10 , C07D487/08 , C07D471/04 , C07D471/10 , A61K45/06
Abstract: Bifunctional compounds, which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
-
Patent Agency Ranking
公开(公告)号：US11554171B2
公开(公告)日：2023-01-17
申请号：US16912329
申请日：2020-06-25
Applicant: Arvinas Operations, Inc. , Yale University
Inventor： Yimin Qian , Hanqing Dong , Jing Wang , Michael Berlin , Andrew P. Crew , Craig M. Crews
IPC: A61P35/00 , A61K45/06 , C07D519/00 , C07D417/14 , C07D495/14 , A61K47/55
Abstract: 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：US20220323457A1
公开(公告)日：2022-10-13
申请号：US17073135
申请日：2020-10-16
Applicant: Arvinas Operations, Inc.
Inventor： Michael Berlin , Hanqing Dong , Dan Sherman , Lawrence Snyder , Jing Wang , Wei Zhang
IPC: A61K31/551 , A61K31/506 , C07D401/14 , C07D487/08 , A61K31/496 , C07D487/10 , C07D405/14 , C07D413/14 , A61K31/5355 , A61K31/5377 , A61K31/4985 , A61K31/55 , C07D487/04 , C07D417/14 , C07D471/10
Abstract: Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand that 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 bifunctional compounds of the present disclosure exhibit 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：US20200155689A1
公开(公告)日：2020-05-21
申请号：US16751154
申请日：2020-01-23
Applicant: ARVINAS OPERATIONS, INC.
Inventor： ANDREW P. CREW , Craig M. Crews , Hanqing Dong , Keith R. Hornberger , Jing Wang , Yimin Qian , Kurt Zimmermann , Michael Berlin , Lawrence B. Snyder
IPC: A61K47/55 , A61K31/496 , A61K31/506 , A61K31/501 , A61K45/06 , A61K31/551 , A61K31/497 , A61K31/437 , C07D471/04 , C07D401/14 , C07D401/04 , A61P35/00 , A61K47/54
Abstract: 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：US20190300521A1
公开(公告)日：2019-10-03
申请号：US16372345
申请日：2019-04-01
Applicant: Arvinas Operations, Inc. , Genentech, Inc.
Inventor： Andrew P. Crew , Jing Wang , Michael Berlin , Peter Dragovich , Huifen Chen , Leanna Staben
Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau 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：US20240382599A1
公开(公告)日：2024-11-21
申请号：US18623722
申请日：2024-04-01
Applicant: Arvinas Operations, Inc. , Yale University
Inventor： Andrew P. Crew , Kurt Zimmermann , Jing Wang , Michael Berlin , Hanqing Dong , Alexey Ishchenko , Yimin Qian , Saul Jaime-Figueroa , George Burslem , Craig M. Crews
IPC: A61K47/54 , A61K31/427 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/55 , A61K31/551 , A61K38/07 , A61K45/06 , A61K47/55 , C07D471/04
Abstract: The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) TBK1. 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.
-
-
-
-
-
-
-
-
-
Search Results
39
records
(took 0.028 seconds)
