Patents Assigned to ARVINAS OPERATIONS, INC.
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Patent number: 11964945Abstract: 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: GrantFiled: May 29, 2020Date of Patent: April 23, 2024Assignee: Arvinas Operations, Inc.Inventors: Andrew P. Crew, Keith R. Hornberger, Lawrence B. Snyder, Kurt Zimmermann, Jing Wang, Hanqing Dong
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Patent number: 11957759Abstract: Provided herein are bifunctional compounds having the chemical structure I: PTM-L-CLM??(I): or pharmaceutically acceptable salts thereof, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (Raf, such as c-Raf, A-Raf, and/or B-RAF) and are useful in the treatment of a variety of Raf mediated conditions or diseases, such as cancer, specifically lung cancer, skin cancer, or colorectal cancer.Type: GrantFiled: September 7, 2023Date of Patent: April 16, 2024Assignee: Arvinas Operations, Inc.Inventor: Keith R. Hornberger
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Patent number: 11952347Abstract: 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: GrantFiled: December 1, 2021Date of Patent: April 9, 2024Assignee: Arvinas Operations, Inc.Inventors: Andrew P. Crew, Lawrence B. Snyder, Jing Wang
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Publication number: 20240076281Abstract: 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.Type: ApplicationFiled: November 28, 2022Publication date: March 7, 2024Applicant: Arvinas Operations, Inc.Inventors: Yimin QIAN, Hanqing DONG, Jing WANG
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Patent number: 11912699Abstract: 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: July 17, 2020Date of Patent: February 27, 2024Assignee: ARVINAS OPERATIONS, INC.Inventors: Andrew P. Crew, Michael Berlin, Angela M. Cacace, Julian T. Chandler
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Publication number: 20240059686Abstract: 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.Type: ApplicationFiled: December 20, 2022Publication date: February 22, 2024Applicant: Arvinas Operations, Inc.Inventors: Andrew P. CREW, Hanqing DONG, Jing WANG, Xin CHEN, Yimin QIAN, Craig M. CREWS, Michael BERLIN, Meizhong JIN
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Patent number: 11883393Abstract: 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.Type: GrantFiled: December 18, 2020Date of Patent: January 30, 2024Assignee: Arvinas Operations, Inc.Inventors: Lawrence B. Snyder, Hanqing Dong
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Patent number: 11857519Abstract: 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: June 22, 2021Date of Patent: January 2, 2024Assignee: Arvinas Operations, Inc.Inventors: Andrew P. Crew, Lawrence B. Snyder, Jing Wang, Hanqing Dong, Yimin Qian, Michael Berlin
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Patent number: 11858940Abstract: 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: GrantFiled: March 19, 2021Date of Patent: January 2, 2024Assignee: Arvinas Operations, Inc.Inventors: Erika Araujo, Michael Berlin, Steven M. Sparks, Jing Wang, Wei Zhang
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Patent number: 11707452Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of ?-synuclein (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: August 20, 2019Date of Patent: July 25, 2023Assignee: Arvinas Operations, Inc.Inventors: Andrew P. Crew, Hanqing Dong, Michael Berlin, Steven M. Sparks
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Publication number: 20230183209Abstract: 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: December 12, 2022Publication date: June 15, 2023Applicant: Arvinas Operations, Inc.Inventors: Andrew P. CREW, Michael BERLIN, Keith R. HORNBERGER, Lawrence B. SNYDER, Jing WANG, Yimin QIAN, Hanqing DONG, Kurt ZIMMERMANN
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Publication number: 20230128132Abstract: 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.Type: ApplicationFiled: December 21, 2022Publication date: April 27, 2023Applicant: Arvinas Operations, Inc.Inventors: Andrew P. CREW, Lawrence B. SNYDER, Jing WANG, Royal J. HASKELL, III, Marcia Dougan MOORE
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Patent number: 11597720Abstract: 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.Type: GrantFiled: July 17, 2020Date of Patent: March 7, 2023Assignee: Arvinas Operations, Inc.Inventors: Yimin Qian, Hanqing Dong, Jing Wang
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Patent number: 11584743Abstract: The present disclosure relates to compounds and a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing the compounds, and processes for their preparation. The disclosure also relates to the use of the compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.Type: GrantFiled: October 28, 2020Date of Patent: February 21, 2023Assignee: Arvinas Operations, Inc.Inventors: Andrew P. Crew, Yimin Qian, Hanging Dong, Jing Wang
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Patent number: 11554171Abstract: 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: June 25, 2020Date of Patent: January 17, 2023Assignees: Arvinas Operations, Inc., Yale UniversityInventors: Yimin Qian, Hanqing Dong, Jing Wang, Michael Berlin, Andrew P. Crew, Craig M. Crews
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Publication number: 20230012321Abstract: The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A: The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.Type: ApplicationFiled: May 6, 2021Publication date: January 12, 2023Applicant: Arvinas Operations, Inc.Inventors: Laura E.N. ALLAN, Chungpin Herman CHEN, Hanqing DONG, Robert J. DUGUID, John A. GROSSO, Royal J. HASKELL, III, Casey Keith JAGER, Venkata A. KATTUBOINA, Aditya Mohan KAUSHAL, Samuel Elliott KENNEDY, Rhys LLOYD, Miranda Annell NEESER, Yuping QIU, Hayley REECE, Maxwell Marco REEVE, Joseph P. REO, Jerod ROBERTSON, Mohammad Mehdi ZAHEDI
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Patent number: 11512083Abstract: 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: June 18, 2020Date of Patent: November 29, 2022Assignees: 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
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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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Patent number: 11384063Abstract: 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 a cereblon, Von Hippel-Lindau ligase-binding moiety, 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: March 5, 2020Date of Patent: July 12, 2022Assignee: ARVINAS OPERATIONS, INC.Inventors: Andrew P. Crew, Hanqing Dong, Jing Wang, Yimin Qian