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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
发明人： Yimin QIAN , Hanqing DONG , Jing WANG , Michael BERLIN , Andrew P. CREW , Craig M. CREWS
IPC分类号： A61K45/06 , C07D519/00 , C07D417/14 , C07D495/14 , A61K47/55
CPC分类号： 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.
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2.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
发明人： Andrew P. CREW , Yimin QIAN , Hanqing DONG , Jing WANG
IPC分类号： 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
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.
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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
发明人： Andrew P. CREW , Keith R. HORNBERGER , Kurt ZIMMERMANN , Jing WANG , Michael BERLIN , Craig M. CREWS , Hanqing DONG , Lawrence B. SNYDER
IPC分类号： 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
摘要： 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：US20230128132A1
公开(公告)日：2023-04-27
申请号：US18085869
申请日：2022-12-21
IPC分类号： A61K31/501 , A61P35/00 , A61K9/00
摘要： The present application relates to treating and/or preventing prostate cancer, including metastatic and/or castrate-resistant prostate cancer, in a subject in need of treatment, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph, isotopic derivative, or prodrug thereof, wherein R1, R2, R3, X1, X2, X3, X4, and n are defined herein.
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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
发明人： Lawrence B. SNYDER , Andrew P. CREW , Jing WANG , Hanqing DONG
IPC分类号： 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
摘要： 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：US20230082997A1
公开(公告)日：2023-03-16
申请号：US17571018
申请日：2022-01-07
发明人： Michael BERLIN , Andrew P. CREW , Craig M. CREWS , Hanqing DONG , Keith R. HORNBERGER , Yimin QIAN , Lawrence B. SNYDER , Jing WANG , Kurt ZIMMERMANN
IPC分类号： A61K47/55 , C07D401/04 , C07D401/14 , C07D471/04 , A61K31/437 , A61K31/497 , A61K31/551 , A61K45/06 , A61K31/501 , A61K31/506 , A61K31/496 , A61K47/54 , A61P35/00
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.
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公开(公告)号：US20220089570A1
公开(公告)日：2022-03-24
申请号：US17484628
申请日：2021-09-24
发明人： Andrew P. CREW , Craig M. CREWS , Hanqing DONG , Meizhong JIN , Yimin QIAN , Jing WANG
IPC分类号： C07D401/14 , C12N9/12 , C12N9/18 , A61K45/06 , C12Q1/25 , A61K31/4439 , A61K31/519 , A61K31/513 , A61K47/54 , A61K47/66
摘要： The description relates to imide-based 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 invention. 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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公开(公告)号：US20210113557A1
公开(公告)日：2021-04-22
申请号：US17075808
申请日：2020-10-21
IPC分类号： A61K31/501 , A61P35/00 , A61K9/00
摘要： The present application relates to treating and/or preventing prostate cancer, including metastatic and/or castrate-resistant prostate cancer, in a subject in need of treatment, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph, isotopic derivative, or prodrug thereof, wherein R1, R2, R3, X1, X2, X3, X4 and n are defined herein.
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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
发明人： Andrew P. CREW , Hanqing DONG , Jing WANG , Xin CHEN , Yimin QIAN , Craig M. CREWS , Michael BERLIN , Meizhong JIN
IPC分类号： 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分类号： C07D417/14 , C07D413/14 , C07D417/12 , C07D413/12 , C07D233/86 , A61P25/28 , C07D491/107 , C07D471/10 , A61K45/06 , C07K5/06165 , A61P35/00 , C07D401/04
摘要： 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
发明人： Michael BERLIN , Andrew P. CREW , Craig M. CREWS , Hanqing DONG , Keith R. HORNBERGER , Lawrence B. SNYDER , Jing WANG , Kurt ZIMMERMANN
IPC分类号： 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分类号： 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
摘要： 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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