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公开(公告)号：US20250034096A1
公开(公告)日：2025-01-30
申请号：US18772066
申请日：2024-07-12
Applicant: Arvinas Operations, Inc.
Inventor： Michael BERLIN , Andrew P. CREW , Craig M. CREWS , Hanqing DONG , Keith R. HORNBERGER , Lawrence B. SNYDER , Jing WANG , Kurt ZIMMERMANN
IPC: C07D233/42 , A61K31/02 , A61K31/166 , A61K31/277 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , A61K47/10 , C07D205/04 , C07D209/48 , C07D211/76 , C07D213/72 , C07D221/20 , C07D231/12 , C07D237/08 , C07D239/24 , C07D241/04 , C07D401/04 , C07D401/14
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.
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公开(公告)号：US20210196710A1
公开(公告)日：2021-07-01
申请号：US17126501
申请日：2020-12-18
Applicant: Arvinas Operations, Inc.
Inventor： Lawrence B. SNYDER , Andrew P. CREW , Jing WANG , Hanqing DONG
IPC: A61K31/496 , A61K31/501 , A61K31/497 , A61K31/506 , A61K31/5386 , A61K31/4545 , A61K31/5377 , A61K31/4523 , A61K31/661 , A61K31/337 , A61K38/09 , A61K31/57 , A61K31/167 , A61K31/277 , A61K31/417 , A61K31/663 , A61K31/675 , A61K47/54 , C07D401/12 , C07D401/14 , C07D498/10 , C07D413/12 , C07D413/14
Abstract: This disclosure pertains to compounds, the preparation thereof, and the use of these compounds in the treatment of prostate cancer, including metastatic and/or castrate-resistant prostate cancer, in subjects in need thereof.
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公开(公告)号：US20240059686A1
公开(公告)日：2024-02-22
申请号：US18085500
申请日：2022-12-20
Applicant: Arvinas Operations, Inc.
Inventor： Andrew P. CREW , Hanqing DONG , Jing WANG , Xin CHEN , Yimin QIAN , Craig M. CREWS , Michael BERLIN , Meizhong JIN
IPC: C07D417/14 , C07D413/14 , C07D417/12 , C07D413/12 , C07D233/86 , C07D401/04 , C07D491/107 , C07D471/10 , A61K45/06 , C07K5/078 , A61P35/00 , A61P25/28
CPC classification number: C07D417/14 , C07D413/14 , C07D417/12 , C07D413/12 , C07D233/86 , A61P25/28 , C07D491/107 , C07D471/10 , A61K45/06 , C07K5/06165 , A61P35/00 , C07D401/04
Abstract: The present invention 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：US20230331681A1
公开(公告)日：2023-10-19
申请号：US18213055
申请日：2023-06-22
Applicant: Arvinas Operations, Inc.
Inventor： Michael BERLIN , Andrew P. CREW , Craig M. CREWS , Hanqing DONG , Keith R. HORNBERGER , Lawrence B. SNYDER , Jing WANG , Kurt ZIMMERMANN
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 , A61K31/506 , A61K31/496 , A61K31/501 , C07D401/04
CPC classification number: 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 , A61K31/506 , A61K31/496 , A61K31/501 , C07D401/04
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.
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公开(公告)号：US20230263893A1
公开(公告)日：2023-08-24
申请号：US18052096
申请日：2022-11-02
Applicant: ARVINAS OPERATIONS, INC. , YALE UNIVERISTY
Inventor： Yimin QIAN , Hanqing DONG , Jing WANG , Michael BERLIN , Andrew P. CREW , Craig M. CREWS
IPC: A61K45/06 , C07D519/00 , C07D417/14 , C07D495/14 , A61K47/55
CPC classification number: 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.
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Patent Agency Ranking
公开(公告)号：US20230069491A1
公开(公告)日：2023-03-02
申请号：US17873748
申请日：2022-07-26
Applicant: Arvinas Operations, Inc.
Inventor： Chungpin Herman CHEN , Hanqing DONG
IPC: C07D401/14 , B01J25/02
Abstract: This disclosure pertains to the preparation of bifunctional compounds (e.g., Compound 1), intermediates in the preparation of such compounds, and preparation of such intermediates.
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7.发明申请公开(公告)号：US20220274955A1
公开(公告)日：2022-09-01
申请号：US16932072
申请日：2020-07-17
Applicant: Arvinas Operations, Inc.
Inventor： Andrew P. CREW , Yimin QIAN , Hanqing DONG , Jing WANG
IPC: C07D401/14 , C07D401/04 , C07D471/10 , A61P35/00 , A61K31/4545 , A61K31/4725 , A61K31/519 , C07K5/078 , A61K38/05 , A61K31/454 , A61K31/501 , C07D487/10 , A61K31/551 , A61K38/06 , A61K31/5386 , C07K5/083 , A61K47/54 , A61P15/00 , A61K31/496 , C07D487/04 , A61K45/06 , C07D498/10 , A61K31/497 , C07D471/04 , C07D487/08
Abstract: 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.
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公开(公告)号：US20210009528A1
公开(公告)日：2021-01-14
申请号：US16938864
申请日：2020-07-24
Applicant: Arvinas Operations, Inc.
Inventor： Andrew P. CREW , Keith R. HORNBERGER , Kurt ZIMMERMANN , Jing WANG , Michael BERLIN , Craig M. CREWS , Hanqing DONG , Lawrence B. SNYDER
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 , A61K31/506 , A61K31/496 , A61K31/501
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.
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9.发明公开公开(公告)号：US20240076281A1
公开(公告)日：2024-03-07
申请号：US18070408
申请日：2022-11-28
Applicant: Arvinas Operations, Inc.
Inventor： Yimin QIAN , Hanqing DONG , Jing WANG
IPC: 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 , A61P15/00 , A61P35/00 , C07D401/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D498/10 , C07K5/078 , C07K5/083
CPC classification number: 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 , C07K5/06165 , C07K5/0806 , C07K5/06034
Abstract: 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.
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公开(公告)号：US20230183209A1
公开(公告)日：2023-06-15
申请号：US18079790
申请日：2022-12-12
Applicant: Arvinas Operations, Inc.
Inventor： Andrew P. CREW , Michael BERLIN , Keith R. HORNBERGER , Lawrence B. SNYDER , Jing WANG , Yimin QIAN , Hanqing DONG , Kurt ZIMMERMANN
IPC: C07D401/14 , C07D417/14 , C07D471/04 , A61P35/02 , C07D487/04 , C07D495/14 , C07D498/04 , C07D471/10
CPC classification number: C07D401/14 , C07D417/14 , C07D471/04 , A61P35/02 , C07D487/04 , C07D495/14 , C07D498/04 , C07D471/10
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.
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