Patents by Inventor Michael Berlin
Michael Berlin has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Publication number: 20220323457Abstract: 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.Type: ApplicationFiled: October 16, 2020Publication date: October 13, 2022Inventors: Michael Berlin, Hanqing Dong, Dan Sherman, Lawrence Snyder, Jing Wang, Wei Zhang
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Publication number: 20220315575Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.Type: ApplicationFiled: July 17, 2020Publication date: October 6, 2022Inventors: Andrew P. Crew, Michael Berlin, Hanqing Dong, Alexey Ishchenko, Angela M. Cacace, Julian T. Chandler
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Patent number: 11458123Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.Type: GrantFiled: November 1, 2017Date of Patent: October 4, 2022Assignee: ARVINAS OPERATIONS, INC.Inventors: Andrew P. Crew, Michael Berlin, Hanqing Dong, Alexey Ishchenko
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Patent number: 11427548Abstract: The present disclosure 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.Type: GrantFiled: October 17, 2019Date of Patent: August 30, 2022Assignee: ARVINAS OPERATIONS, INC.Inventors: Andrew P. Crew, Hanqing Dong, Jing Wang, Xin Chen, Yimin Qian, Kurt Zimmermann, Michael Berlin, Lawrence Snyder
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Publication number: 20220259154Abstract: 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.Type: ApplicationFiled: December 1, 2021Publication date: August 18, 2022Inventors: Michael BERLIN, Andrew P. CREW, Craig M. CREWS, Hanqing DONG, Keith R. HORNBERGER, Lawrence B. SNYDER, Jing WANG, Kurt ZIMMERMANN
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Publication number: 20220162163Abstract: The description relates to Inhibitors of Apoptosis Proteins (IAPs) 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 invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the IAP 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.Type: ApplicationFiled: January 5, 2022Publication date: May 26, 2022Inventors: Michael Berlin, Andrew P. Crew, Hanqing Dong, Yimin Qian
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Publication number: 20220064168Abstract: 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.Type: ApplicationFiled: March 19, 2021Publication date: March 3, 2022Inventors: Erika Araujo, Michael Berlin, Steven M. Sparks, Jing Wang, Wei Zhang
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Patent number: 11191741Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of enhancer of zeste homolog 2 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand 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.Type: GrantFiled: December 21, 2017Date of Patent: December 7, 2021Assignee: ARVINAS OPERATIONS, INC.Inventors: Andrew P. Crew, Lawrence B. Snyder, Jing Wang, Yimin Qian, Michael Berlin
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Publication number: 20210187108Abstract: 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.Type: ApplicationFiled: June 25, 2020Publication date: June 24, 2021Inventors: Yimin Qian, Hanqing Dong, Jing Wang, Michael Berlin, Andrew P. Crew, Craig M. Crews
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Publication number: 20210171470Abstract: 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.Type: ApplicationFiled: May 29, 2020Publication date: June 10, 2021Inventors: Andrew P. Crew, Keith R. Hornberger, Lawrence B. Snyder, Kurt Zimmermann, Jing Wang, Michael Berlin, Craig M. Crews, Hanqing Dong
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Publication number: 20210053973Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof: wherein: āZā and R1 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.Type: ApplicationFiled: December 10, 2018Publication date: February 25, 2021Applicant: Merck Sharp & Dohme Corp.Inventors: Amjad ALI, Yeon-Hee LIM, Gioconda V. GALLO-ETIENNE, Joseph Michael KELLY, Michael BERLIN, Pauline TING, Jayaram R. TAGAT, Dong XIAO, Rongze KUANG, Heping WU, Hongwu WANG
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Publication number: 20210040044Abstract: 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.Type: ApplicationFiled: August 28, 2020Publication date: February 11, 2021Inventors: Andrew P. Crew, Keith R. Hornberger, Lawrence B. Snyder, Kurt Zimmermann, Jing Wang, Michael Berlin, Hanqing Dong
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Publication number: 20210009528Abstract: 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.Type: ApplicationFiled: July 24, 2020Publication date: January 14, 2021Inventors: Andrew P. CREW, Keith R. HORNBERGER, Kurt ZIMMERMANN, Jing WANG, Michael BERLIN, Craig M. CREWS, Hanqing DONG, Lawrence B. SNYDER
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Publication number: 20200392131Abstract: 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.Type: ApplicationFiled: June 18, 2020Publication date: December 17, 2020Inventors: 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
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Patent number: 10772962Abstract: 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.Type: GrantFiled: August 5, 2016Date of Patent: September 15, 2020Assignees: ARVINAS OPERATIONS, INC., YALE UNIVERSITYInventors: Yimin Qian, Hanqing Dong, Jing Wang, Michael Berlin, Andrew P. Crew, Craig M. Crews
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Patent number: 10730870Abstract: 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.Type: GrantFiled: March 18, 2016Date of Patent: August 4, 2020Assignees: ARVINAS OPERATIONS, INC., YALE UNIVERSITYInventors: 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
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Patent number: 10688082Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof, wherein: āZā, R1 and R2 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.Type: GrantFiled: June 6, 2016Date of Patent: June 23, 2020Assignee: Merck Sharp & Dohme Corp.Inventors: Junying Zheng, Walter Won, Michael Berlin, Pauline Ting, Guoqing Li, Dong Xiao, Hongwu Wang, Robert Aslanian
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Publication number: 20200155689Abstract: 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.Type: ApplicationFiled: January 23, 2020Publication date: May 21, 2020Inventors: ANDREW P. CREW, Craig M. Crews, Hanqing Dong, Keith R. Hornberger, Jing Wang, Yimin Qian, Kurt Zimmermann, Michael Berlin, Lawrence B. Snyder
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Publication number: 20200155690Abstract: 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.Type: ApplicationFiled: January 23, 2020Publication date: May 21, 2020Inventors: Andrew P. Crew, Craig M. Crews, Hanqing Dong, Keith R. Hornberger, Jing Wang, Yimin Qian, Kurt Zimmermann, Michael Berlin, Lawrence B. Snyder
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Publication number: 20200095205Abstract: 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.Type: ApplicationFiled: September 20, 2019Publication date: March 26, 2020Inventors: Andrew P. CREW, Keith R. HORNBERGER, Lawrence B. SNYDER, Kurt ZIMMERMANN, Jing WANG, Michael BERLIN, Craig M. CREWS, Hanqing DONG