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公开(公告)号：US12053469B2
公开(公告)日：2024-08-06
申请号：US17207325
申请日：2021-03-19
发明人： Erika Araujo , Michael M. Berlin , Steven M. Sparks , Jing Wang , Wei Zhang
IPC分类号： A61K31/506 , A61K31/496 , A61K31/5377 , A61K45/06 , A61P25/16 , C07D401/14 , C07D413/14 , C07D487/10
CPC分类号： A61K31/506 , A61K31/496 , A61K31/5377 , A61K45/06 , A61P25/16 , C07D401/14 , C07D413/14 , C07D487/10
摘要： 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.
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公开(公告)号：US11981683B2
公开(公告)日：2024-05-14
申请号：US17699082
申请日：2022-03-19
发明人： Erika Marina Vieira Araujo , Michael Berlin , Hanqing Dong , Steven M. Sparks , Jing Wang , Wei Zhang
IPC分类号： C07D401/14 , A61K45/06 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/08 , C07D487/10 , C07D498/10
CPC分类号： C07D498/10 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/08 , C07D487/10
摘要： 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.
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公开(公告)号：US11858940B2
公开(公告)日：2024-01-02
申请号：US17207330
申请日：2021-03-19
发明人： Erika Araujo , Michael Berlin , Steven M. Sparks , Jing Wang , Wei Zhang
IPC分类号： C07D487/04 , A61K45/06 , C07D519/00
CPC分类号： C07D487/04 , A61K45/06 , C07D519/00
摘要： 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.
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公开(公告)号：US20230097358A1
公开(公告)日：2023-03-30
申请号：US17699082
申请日：2022-03-19
发明人： Erika Marina Vieira Araujo , Michael Berlin , Hanqing Dong , Steven M. Sparks , Jing Wang , Wei Zhang
IPC分类号： C07D498/10 , C07D401/14 , C07D417/14 , C07D413/14 , C07D487/10 , C07D487/08 , C07D471/04 , C07D471/10 , A61K45/06
摘要： 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.
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公开(公告)号：US20220323457A1
公开(公告)日：2022-10-13
申请号：US17073135
申请日：2020-10-16
发明人： Michael Berlin , Hanqing Dong , Dan Sherman , Lawrence Snyder , Jing Wang , Wei Zhang
IPC分类号： 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
摘要： 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.
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公开(公告)号：US20240158405A1
公开(公告)日：2024-05-16
申请号：US18511018
申请日：2023-11-16
IPC分类号： C07D487/04 , A61K45/06 , C07D519/00
CPC分类号： C07D487/04 , A61K45/06 , C07D519/00
摘要： 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.
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公开(公告)号：US20220395576A1
公开(公告)日：2022-12-15
申请号：US17721916
申请日：2022-04-15
发明人： Michael Berlin , Hanqing Dong , Dan Sherman , Lawrence B. Snyder , Jing Wang , Wei Zhang
摘要： 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 cereblon 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.
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公开(公告)号：US20240360152A1
公开(公告)日：2024-10-31
申请号：US18659374
申请日：2024-05-09
发明人： Erika Marina Vieira Araujo , Michael Berlin , Hanqing Dong , Steven M. Sparks , Jing Wang , Wei Zhang
IPC分类号： C07D498/10 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/08 , C07D487/10
CPC分类号： C07D498/10 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/08 , C07D487/10
摘要： 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.
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公开(公告)号：US20240325547A1
公开(公告)日：2024-10-03
申请号：US18610001
申请日：2024-03-19
发明人： MICHAEL BERLIN , Hanqing Dong , Dan Sherman , Lawrence B. Snyder , Jing Wang , Wei Zhang
CPC分类号： A61K47/55 , A61K45/06 , A61K47/545 , A61P35/00
摘要： 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 cereblon 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.
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公开(公告)号：US20220064168A1
公开(公告)日：2022-03-03
申请号：US17207330
申请日：2021-03-19
发明人： Erika Araujo , Michael Berlin , Steven M. Sparks , Jing Wang , Wei Zhang
IPC分类号： C07D487/04 , C07D519/00 , A61K45/06
摘要： 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.
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