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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：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：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：US20230183209A1
公开(公告)日：2023-06-15
申请号：US18079790
申请日：2022-12-12
发明人： Andrew P. CREW , Michael BERLIN , Keith R. HORNBERGER , Lawrence B. SNYDER , Jing WANG , Yimin QIAN , Hanqing DONG , Kurt ZIMMERMANN
IPC分类号： C07D401/14 , C07D417/14 , C07D471/04 , A61P35/02 , C07D487/04 , C07D495/14 , C07D498/04 , C07D471/10
CPC分类号： C07D401/14 , C07D417/14 , C07D471/04 , A61P35/02 , C07D487/04 , C07D495/14 , C07D498/04 , C07D471/10
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：US20220259154A1
公开(公告)日：2022-08-18
申请号：US17539679
申请日：2021-12-01
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
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：US20240180900A1
公开(公告)日：2024-06-06
申请号：US18493773
申请日：2023-10-24
发明人： Ronald PECK , Sarah Deborah CHIRNOMAS , Edward CHAN , Richard Walter GEDRICH , Elmer J. BERGHORN, Jr. , Jeanette Toni ALICEA , Lawrence B. SNYDER , SangHyun LEE , Taavi NEKLESA
IPC分类号： A61K31/496 , A61K31/573 , A61K31/58 , A61P35/00
CPC分类号： A61K31/496 , A61K31/573 , A61K31/58 , A61P35/00
摘要： This disclosure pertains to methods of treating prostate cancer in a subject, including prostate cancer comprising at least one somatic AR tumor mutation, such as metastatic prostate cancer, castrate-resistant prostate cancer, metastatic castrate-resistant prostate cancer, progressive metastatic castrate-resistant prostate cancer, castrate-sensitive prostate cancer, metastatic castrate-sensitive prostate cancer, prostate cancer naïve to novel hormonal agents (NHAs), metastatic prostate cancer naïve NHAs, castrate-resistant prostate cancer naïve to NHAs, castrate-sensitive prostate cancer naïve to NHAs, metastatic castrate-resistant prostate cancer naïve to NHAs, and metastatic castrate-sensitive prostate cancer naïve to NHAs, wherein the method comprises administering to a subject in need thereof a therapeutically effective amount of Compound A, or a pharmaceutically acceptable salt thereof.
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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：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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