Patents by Inventor Charles A. Blum
Charles A. Blum 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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Patent number: 11858919Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.Type: GrantFiled: September 25, 2019Date of Patent: January 2, 2024Assignee: Regenacy Pharmaceuticals, Inc.Inventors: John H. Van Duzer, Ralph Mazitschek, Charles Blum
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Publication number: 20230218632Abstract: The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“TNF”) receptor associated protein 1 (“TRAP1”) modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 (“PINK1”) loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as ?-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g.Type: ApplicationFiled: March 19, 2021Publication date: July 13, 2023Applicant: Amathus Therapeutics, Inc.Inventors: Edward Holson, Charles Blum
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Publication number: 20230174523Abstract: The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“TNF”) receptor associated protein 1 (“TRAP1”) modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 (“PINK1”) loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as ?-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g.Type: ApplicationFiled: March 19, 2021Publication date: June 8, 2023Applicant: Amathus Therapeutics, Inc.Inventors: Edward Holson, Charles Blum
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Publication number: 20230159509Abstract: The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“TNF”) receptor associated protein 1 (“TRAP1”) modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 (“PINK1”) loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as a-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g.Type: ApplicationFiled: March 19, 2021Publication date: May 25, 2023Applicant: Amathus Therapeutics, Inc.Inventors: Edward Holson, Charles Blum
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Publication number: 20220033388Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.Type: ApplicationFiled: September 25, 2019Publication date: February 3, 2022Inventors: John H. VAN DUZER, Ralph MAZITSCHEK, Charles BLUM
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Publication number: 20210332036Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.Type: ApplicationFiled: October 9, 2019Publication date: October 28, 2021Inventors: John H. VAN DUZER, Ralph MAZITSCHEK, Charles BLUM, Matthew B. JARPE
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Patent number: 10590135Abstract: The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: November 19, 2015Date of Patent: March 17, 2020Assignee: GLAXOSMITHKLINE LLCInventors: Charles A. Blum, Richard Dana Caldwell, Rebecca Casaubon, Jeremy S. Disch, Ryan Michael Fox, Karsten Koppetsch, William Henry Miller, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Bruce G. Szczepankiewicz, Brian H. White
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Publication number: 20180044338Abstract: Provided herein are novel substituted bridged urea and related analogs and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: August 4, 2017Publication date: February 15, 2018Inventors: Charles A. BLUM, Richard Dana CALDWELL, Rebecca CASAUBON, Jeremy S. DISCH, Ryan Michael FOX, Karsten KOPPETSCH, Pui Yee NG, Christopher OALMANN, Robert B. PERNI, Bruce G. SZCZEPANKIEWICZ, Brian H. WHITE
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Publication number: 20170355697Abstract: The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: November 19, 2015Publication date: December 14, 2017Inventors: Charles A. BLUM, Richard Dana CALDWELL, Rebecca CASAUBON, Jeremy S. DISCH, Ryan Michael FOX, Karsten KOPPETSCH, William Henry MILLER, Pui Yee NG, Christopher OALMANN, Robert B. PERNI, Bruce G. SZCZEPANKIEWICZ, Brian H. WHITE
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Patent number: 9834558Abstract: The present invention relates to novel substituted bridged urea compounds of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: November 19, 2014Date of Patent: December 5, 2017Assignee: GLAXOSMITHKLINE LLCInventors: Charles A. Blum, Richard Dana Caldwell, Rebecca Casaubon, Jeremy S. Disch, Ryan Michael Fox, Karsten Koppetsch, William Henry Miller, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Bruce G. Szczepankiewicz, Brian White
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Patent number: 9765075Abstract: Provided herein are novel substituted bridged urea and related analogs and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: May 13, 2014Date of Patent: September 19, 2017Assignee: GLAXOSMITHKLINE LLCInventors: Charles A. Blum, Richard Dana Caldwell, Rebecca Casaubon, Jeremy S. Disch, Ryan Michael Fox, Karsten Koppetsch, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Bruce G. Szczepankiewicz, Brian H. White
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Patent number: 9556201Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: October 29, 2010Date of Patent: January 31, 2017Assignee: GLAXOSMITHKLINE LLCInventors: Pui Yee Ng, Charles Blum, Lauren McPherson, Robert B. Perni, Chi B. Vu, Mohammed Mahmood Ahmed, Jeremy S. Disch
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Publication number: 20160083386Abstract: Provided herein are novel substituted bridged urea and related analogs and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: May 13, 2014Publication date: March 24, 2016Inventors: Charles A. BLUM, Richard Dana CALDWELL, Rebecca CASAUBON, Jeremy S. DISCH, Ryan Michael FOX, Karsten KOPPETSCH, Pui Yee NG, Christopher OALMANN, Robet B. PERNI, Bruce G. SZCZEPANKIEWICZ, Brian H. WHITE
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Publication number: 20160002273Abstract: Provided herein are novel substituted thieno[3,2-d]pyrimidine-6-carboxamide sirtuin inhibitors and methods of use thereof. The sirtuin inhibitors may be used for inhibiting a sirtuin-mediated biological process, and, e.g. for treating and/or preventing diseases and disorders including, but not limited to cancer, neurodegenerative disease and inflammation. Also provided herein are pharmaceutical compositions comprising these sirtuin inhibitors and compositions comprising a sirtuin inhibitor in combination with another therapeutic agent.Type: ApplicationFiled: March 7, 2014Publication date: January 7, 2016Inventors: Charles A. BLUM, Jeremy S. DISCH, Ghotas EVINDAR, Robert B. PERNI
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Publication number: 20150152108Abstract: The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: November 19, 2014Publication date: June 4, 2015Inventors: Charles A. BLUM, Richard Dana Caldwell, Rebecca Casaubon, Jeremy S. Disch, Ryan Michael Fox, Karsten Koppetsch, William Henry Miller, Pui Yee NG, Christopher Oalmann, Robert B. Perni, Bruce G. Szczepankiewicz, Brian White
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Publication number: 20150057272Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: August 1, 2014Publication date: February 26, 2015Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Patent number: 8846947Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: July 2, 2009Date of Patent: September 30, 2014Assignee: GlaxoSmithKline LLCInventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Publication number: 20140288052Abstract: Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: October 19, 2012Publication date: September 25, 2014Inventors: Charles A. Blum, Jeremy S. Disch, Stephanie K. Springer
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Publication number: 20140249147Abstract: Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided, are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: October 19, 2012Publication date: September 4, 2014Applicant: GlaxoSmithKline, LLCInventors: Charles A. Blum, Stephanie K. Springer, Chi B. Vu
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Patent number: 8759361Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: GrantFiled: August 22, 2011Date of Patent: June 24, 2014Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum