Patents by Inventor Craig Crews
Craig Crews 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: 20200325130Abstract: 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 comprise a tyrosine kinase inhibitor, a linker and a ubiquitin ligase binder. The methods of the present invention comprise administering to the subject an pharmaceutically effective amount of at least one compound of the invention.Type: ApplicationFiled: April 14, 2020Publication date: October 15, 2020Inventors: Craig CREWS, Momar TOURE, Eunhwa KO, Saul JAIME-FIGUEROA
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Publication number: 20200268897Abstract: The present invention provides bifunctional compounds that efficiently dephosphorylate certain phospho-activated target proteins. Such target proteins can be any protein involved in the pathway of a disease or disorder, such as but not limited to cancer, neurodegeneration, metabolic disease, diabetes, insulin resistance, and so forth.Type: ApplicationFiled: January 8, 2020Publication date: August 27, 2020Inventors: Craig Crews, Samuel W. Gerritz, Kyle J. Eastman, Katherine J. Kayser-Bricker, Jinshan M. Chen, David E. Puleo
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Patent number: 10071164Abstract: 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 10, 2015Date of Patent: September 11, 2018Assignees: Yale University, Arvinas, Inc.Inventors: Andrew Crew, Craig Crews, Hanqing Dong, Eunhwa Ko, Jing Wang
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Publication number: 20180186785Abstract: 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 comprise a tyrosine kinase inhibitor, a linker and a ubiquitin ligase binder. The methods of the present invention comprise administering to the subject an pharmaceutically effective amount of at least one compound of the invention.Type: ApplicationFiled: March 1, 2018Publication date: July 5, 2018Inventors: Craig CREWS, Momar TOURE, Eunhwa KO, Saul JAIME-FIGUEROA
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Patent number: 9938264Abstract: 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 comprise a tyrosine kinase inhibitor, a linker and a ubiquitin ligase binder. The methods of the present invention comprise administering to the subject an pharmaceutically effective amount of at least one compound of the invention.Type: GrantFiled: November 2, 2016Date of Patent: April 10, 2018Assignee: Yale UniversityInventors: Craig Crews, Momar Toure, Eunhwa Ko, Saul Jaime-Figueroa
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Publication number: 20170121321Abstract: 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 comprise a tyrosine kinase inhibitor, a linker and a ubiquitin ligase binder. The methods of the present invention comprise administering to the subject an pharmaceutically effective amount of at least one compound of the invention.Type: ApplicationFiled: November 2, 2016Publication date: May 4, 2017Inventors: Craig CREWS, Momar TOURE, Eunhwa KO, Saul Jaime-Figueroa
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Publication number: 20160058872Abstract: 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: July 6, 2015Publication date: March 3, 2016Inventors: Andrew P. Crew, Craig Crews, Hanqing Dong, Jing Wang, Yimin Qian, Kam Siu, Meizhong Jin
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Publication number: 20160045607Abstract: 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: August 10, 2015Publication date: February 18, 2016Inventors: Andrew Crew, Craig Crews, Hanqing Dong, Eunhwa Ko, Jing Wang
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Publication number: 20150291562Abstract: 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: April 14, 2015Publication date: October 15, 2015Inventors: Andrew P. Crew, Craig Crews, Hanqing Dong, Jing Wang, Yimin Qian, Kam Siu, Caterina Ferraro, Meizhong Jin, Xin Chen
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Publication number: 20150119435Abstract: The present invention includes compounds that act as degraders of a target protein, wherein degradation is independent of the class of the target protein or its localization. In certain embodiments, the invention comprises a compound comprising a protein degradation moiety covalently bound to a linker, wherein the ClogP of the compound is equal to or higher than 1.5. In other embodiments, the target protein contemplated within the invention comprises a posttranslational modified protein or intracellular protein. In yet other embodiments, compounds of the present invention are used to treat disease states wherein protein degradation is a viable therapeutic approach, such as cancer or any sort of oxidative stress disease state.Type: ApplicationFiled: May 10, 2013Publication date: April 30, 2015Inventors: Craig Crews, Jeff Gustafson, Anke Gundula Roth, Hyun Seop Tae, Dennis Buckley, Taavi Neklesa
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Publication number: 20080090785Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsinlike activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.Type: ApplicationFiled: May 9, 2005Publication date: April 17, 2008Applicant: Proteolix, Inc.Inventors: Mark Smyth, Guy Laidig, Ronald Borchardt, Barry Bunin, Craig Crews, John Musser, Kevin Shenk, Peggy Radel
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Publication number: 20080063601Abstract: Described herein are therapeutic strategies (methods and compositions) useful for treating conditions in which cilia are affected and which manifest with cysts and/or fibrosis, such as conditions in which the kidney, pancreas, liver and/or spleen are affected and contain cysts. Particular embodiments described herein are therapeutic strategies in which PC-2 agonists, particularly agonists (calcium channel agonists) that target PC-2 directly and/or selectively, are administered to individuals with mutations in PKD1, in order to alter the course of polycystic kidney disease, particularly ADPKD. In specific embodiments, the invention relates to use of PC-2 agonists triptolide and triptolide derivatives to regulate calcium release. In other aspects, the invention relates to use of PC-2 agonists to treat or aid in the treatment of any condition in which a calcium channel, such as the gene product of PKD1 and/or PKD2, is mutated; calcium signaling is abnormal; or both.Type: ApplicationFiled: March 12, 2007Publication date: March 13, 2008Applicant: Yale UniversityInventors: Stefan Somlo, Craig Crews, Stephanie Quinn, Dayne Okuhara
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Publication number: 20070191284Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.Type: ApplicationFiled: April 11, 2007Publication date: August 16, 2007Applicant: Proteolix, Inc.Inventors: Mark Smyth, Guy Laidig, Ronald Borchardt, Barry Bunin, Craig Crews, John Musser
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Patent number: 7208157Abstract: The present invention is based on the discovery of a composition that provides targeted ubiquitination. Specifically the composition contains a ubiquitin pathway protein binding moiety which recognizes a ubiquitin pathway protein and a targeting moiety which recognizes a target protein. In addition, the present invention provides libraries of compositions, where each composition contains a ubiquitin pathway protein binding moiety and a member of a molecular library. The libraries of the present invention can be used to identify proteins involved in a predetermined function of cells.Type: GrantFiled: November 18, 2002Date of Patent: April 24, 2007Assignees: California Institute of Technology, Yale University, The Regents of the University of CaliforniaInventors: Raymond J. Dashaies, Craig Crews, Kathleen M. Sakamoto
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Patent number: 7041298Abstract: The present invention is based on the discovery of a composition that provides targeted ubiquitination. Specifically the composition contains an ubiquitin pathway protein binding moiety which recognizes an ubiquitin pathway protein and a targeting moiety which recognizes a target protein. In addition, the present invention provides libraries of compositions, where each composition contains an ubiquitin pathway protein binding moiety and a member of a molecular library. The libraries of the present invention can be used to identify proteins involved in a predetermined function of cells.Type: GrantFiled: September 10, 2001Date of Patent: May 9, 2006Assignees: California Institute of Technology, Yale School of Medicine, The Regents of the University of CaliforniaInventors: Raymond J. Deshaies, Craig Crews, Kathleen M. Sakamoto
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Publication number: 20050245435Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.Type: ApplicationFiled: April 14, 2005Publication date: November 3, 2005Applicant: Proteolix, Inc.Inventors: Mark Smyth, Guy Laidig, Ronald Borchardt, Barry Bunin, Craig Crews, John Musser, John Schneekloth, John Chabala
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Publication number: 20040038358Abstract: The present invention is based on the discovery of a composition that provides targeted ubiquitination. Specifically the composition contains a ubiquitin pathway protein binding moiety which recognizes a ubiquitin pathway protein and a targeting moiety which recognizes a target protein. In addition, the present invention provides libraries of compositions, where each composition contains a ubiquitin pathway protein binding moiety and a member of a molecular library. The libraries of the present invention can be used to identify proteins involved in a predetermined function of cells.Type: ApplicationFiled: November 18, 2002Publication date: February 26, 2004Inventors: Raymond J. Dashaies, Craig Crews, Kathleen M. Sakamoto
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Publication number: 20020068063Abstract: The present invention is based on the discovery of a composition that provides targeted ubiquitination. Specifically the composition contains an ubiquitin pathway protein binding moiety which recognizes an ubiquitin pathway protein and a targeting moiety which recognizes a target protein. In addition, the present invention provides libraries of compositions, where each composition contains an ubiquitin pathway protein binding moiety and a member of a molecular library. The libraries of the present invention can be used to identify proteins involved in a predetermined function of cells.Type: ApplicationFiled: September 10, 2001Publication date: June 6, 2002Inventors: Raymond J. Deshaies, Craig Crews, Kathleen M. Sakamoto