Patents by Inventor George Burslem
George Burslem 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: 20240382599Abstract: The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) TBK1. In particular, the present invention is directed to compounds, which contain on one end an E3 ubiquitin ligase binding moiety which binds to an E3 ubiquitin ligase and on the other end a moiety which binds TBK1 such that TBK1 is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of TBK1. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of TBK1.Type: ApplicationFiled: April 1, 2024Publication date: November 21, 2024Inventors: Andrew P. Crew, Kurt Zimmermann, Jing Wang, Michael Berlin, Hanqing Dong, Alexey Ishchenko, Yimin Qian, Saul Jaime-Figueroa, George Burslem, Craig M. Crews
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Publication number: 20240368179Abstract: 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.Type: ApplicationFiled: September 25, 2023Publication date: November 7, 2024Inventors: Craig M. CREWS, George BURSLEM, Philipp M. CROMM, Saul JAIME-FIGUEROA, Momar TOURE
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Patent number: 11834460Abstract: 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.Type: GrantFiled: December 17, 2021Date of Patent: December 5, 2023Assignee: YALE UNIVERSITYInventors: Craig M. Crews, George Burslem, Philipp M. Cromm, Saul Jaime-Figueroa, Momar Toure
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Publication number: 20220112211Abstract: 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.Type: ApplicationFiled: December 17, 2021Publication date: April 14, 2022Inventors: Craig M. CREWS, George BURSLEM, Philipp M. CROMM, Saul JAIME-FIGUEROA, Momar TOURE
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Patent number: 11220515Abstract: 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.Type: GrantFiled: January 26, 2019Date of Patent: January 11, 2022Assignee: Yale UniversityInventors: Craig M. Crews, George Burslem, Philipp M. Cromm, Saul Jaime-Figueroa, Momar Toure
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Publication number: 20210220475Abstract: The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) TBK1. In particular, the present invention is directed to compounds, which contain on one end an E3 ubiquitin ligase binding moiety which binds to an E3 ubiquitin ligase and on the other end a moiety which binds TBK1 such that TBK1 is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of TBK1. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of TBK1.Type: ApplicationFiled: March 4, 2021Publication date: July 22, 2021Inventors: Andrew P. Crew, Kurt Zimmermann, Jing Wang, Craig M. Crews, Saul Jaime-Figueroa, George Burslem
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Patent number: 10994015Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an 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 effectuate ubiquitination, and therefore, degradation (and inhibition) of the 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 22, 2017Date of Patent: May 4, 2021Assignees: ARVINAS OPERATIONS, INC., YALE UNIVERSITYInventors: Andrew P. Crew, Kurt Zimmermann, Jing Wang, Craig M. Crews, Saul Jaime-Figueroa, George Burslem
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Patent number: 10806737Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of FLT3 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein FLT3, 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 the 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 13, 2017Date of Patent: October 20, 2020Assignees: Arvinas Operations, Inc., Yale UniversityInventors: Andrew P. Crew, Keith R. Hornberger, Craig M. Crews, George Burslem
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Publication number: 20200297725Abstract: The present invention includes novel compounds and methods for preventing or treating diseases associated with and/or caused by overexpression and/or uncontrolled activation of a tyrosine kinase in a subject in need thereof. In certain embodiments, the compounds of the present invention include an allosteric tyrosine kinase inhibitor, a linker, and a ubiquitin ligase binder. The methods of the present invention include administering to the subject an pharmaceutically effective amount of at least one compound of the invention.Type: ApplicationFiled: March 20, 2020Publication date: September 24, 2020Inventors: Craig M. CREWS, George BURSLEM
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Publication number: 20190233433Abstract: 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.Type: ApplicationFiled: January 26, 2019Publication date: August 1, 2019Inventors: Craig M. CREWS, George BURSLEM, Philipp M. CROMM, Saul JAIME-FIGUEROA, Momar TOURE
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Publication number: 20180256586Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of FLT3 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein FLT3, 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 the 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: December 13, 2017Publication date: September 13, 2018Inventors: Andrew P. Crew, Keith R. Hornberger, Craig M. Crews, George Burslem
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Publication number: 20180193470Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an 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 effectuate ubiquitination, and therefore, degradation (and inhibition) of the 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: ApplicationFiled: December 22, 2017Publication date: July 12, 2018Inventors: Andrew P. Crew, Kurt Zimmermann, Jing Wang, Michael Berlin, Hanqing Dong, Alexey Ishchenko, Yimin Qian, Craig M. Crews, Saul Jaime-Figueroa, George Burslem