Patents by Inventor Karsten Koppetsch
Karsten Koppetsch 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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Crystalline solids of nicotinic acid mononucleotide and esters thereof and methods of making and use
Patent number: 11952396Abstract: The present disclosure relates to crystalline solids comprising a compound of Formula (I), wherein R is n-propyl, and methods of making compounds of Formula (I) wherein R is C1-C4 alkyl or C2-C4 alkenyl. The present disclosure also relates to crystalline solids comprising a compound of Formula (II), The present disclosure further relates to methods of preparing the crystalline solids, and pharmaceutical preparations of the crystalline solids, and use of such pharmaceutical preparations in treatment of diseases and conditions.Type: GrantFiled: November 22, 2023Date of Patent: April 9, 2024Assignee: Metro International Biotech, LLCInventors: Jonathan N. Kremsky, Bruce Szczepankiewicz, Karsten Koppetsch, Joseph Harris, Mateusz Pitak, Martin Bates -
CRYSTALLINE SOLIDS OF NICOTINIC ACID MONONUCLEOTIDE AND ESTERS THEREOF AND METHODS OF MAKING AND USE
Publication number: 20240109932Abstract: The present disclosure relates to crystalline solids comprising a compound of Formula (I), wherein R is n-propyl, and methods of making compounds of Formula (I) wherein R is C1-C4 alkyl or C2-C4 alkenyl. The present disclosure also relates to crystalline solids comprising a compound of Formula (II), The present disclosure further relates to methods of preparing the crystalline solids, and pharmaceutical preparations of the crystalline solids, and use of such pharmaceutical preparations in treatment of diseases and conditions.Type: ApplicationFiled: November 22, 2023Publication date: April 4, 2024Inventors: Jonathan N. Kremsky, Bruce Szczepankiewicz, Karsten Koppetsch, Joseph Harris, Mateusz Pitak, Martin Bates -
Crystalline solids of nicotinic acid mononucleotide and esters thereof and methods of making and use
Patent number: 11787830Abstract: The present disclosure relates to crystalline solids comprising a compound of Formula (I), wherein R is n-propyl, and methods of making compounds of Formula (I) wherein R is C1-C4 alkyl or C2-C4 alkenyl. The present disclosure also relates to crystalline solids comprising a compound of Formula (II), The present disclosure further relates to methods of preparing the crystalline solids, and pharmaceutical preparations of the crystalline solids, and use of such pharmaceutical preparations in treatment of diseases and conditions.Type: GrantFiled: March 31, 2023Date of Patent: October 17, 2023Assignee: Metro International Biotech, LLCInventors: Jonathan N. Kremsky, Bruce Szczepankiewicz, Karsten Koppetsch, Joseph Harris, Mateusz Pitak, Martin Bates -
CRYSTALLINE SOLIDS OF NICOTINIC ACID MONONUCLEOTIDE AND ESTERS THEREOF AND METHODS OF MAKING AND USE
Publication number: 20230257412Abstract: The present disclosure relates to crystalline solids comprising a compound of Formula (I), wherein R is n-propyl, and methods of making compounds of Formula (I) wherein R is C1-C4 alkyl or C2-C4 alkenyl. The present disclosure also relates to crystalline solids comprising a compound of Formula (II), The present disclosure further relates to methods of preparing the crystalline solids, and pharmaceutical preparations of the crystalline solids, and use of such pharmaceutical preparations in treatment of diseases and conditions.Type: ApplicationFiled: March 31, 2023Publication date: August 17, 2023Inventors: Jonathan N. Kremsky, Bruce Szczepankiewicz, Karsten Koppetsch, Joseph Harris, Mateusz Pitak, Martin Bates -
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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Patent number: 10485814Abstract: Provided herein are stereoisomerically pure ester and carbonate analogues of nicotinamide riboside and nicotinamide riboside hydride, and pharmaceutical compositions and uses thereof. The stereoisomerically pure ester and carbonate analogues of nicotinamide riboside and nicotinamide riboside hydride may be used to treat a disease or disorder that would benefit from increased NAD levels including a mitochondrial disease or disorder, insulin resistance, a metabolic syndrome, diabetes, obesity, for increasing insulin sensitivity in a subject, or to treat or prevent a skin condition. The compounds have general formulas (I) or (II): wherein R1 is —C(?O)—X—(C2-C18 straight chain or branched) alkyl or —C(?O)—X—(C2-C18 straight chain or branched) alkenyl; each R2 is independently selected from hydrogen, and a —C(O)—X—(C1-C18 straight chain or branched) alkyl or a —C(O)—X—(C2-C18 straight chain or branched) alkenyl; and X is a covalent bond or O.Type: GrantFiled: June 5, 2015Date of Patent: November 26, 2019Assignee: GlaxoSmithKline Intellectual Property (No. 2) LimitedInventors: Bruce G. Szczepankiewicz, Frank Preugschat, Karsten Koppetsch, Robert B. Perni
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Patent number: 10316054Abstract: Provided herein are crystalline beta-D-nicotinamide riboside chloride compositions and methods of preparation and use thereof. Also provided are related pharmaceutical compositions and methods of use thereof. The crystalline beta-D-nicotinamide riboside chloride compositions may be used to treat a disease or disorder that would benefit from increased NAD levels including a mitochondrial disease or disorder, insulin resistance, a metabolic syndrome, diabetes, obesity, or for increasing insulin sensitivity in a subject.Type: GrantFiled: June 2, 2015Date of Patent: June 11, 2019Assignee: GlaxoSmithKline Intellectual Property (No. 2) LimitedInventors: Bruce G. Szczepankiewicz, Karsten Koppetsch, Robert B. Perni
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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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Publication number: 20170204131Abstract: Provided herein are crystalline beta-D-nicotinamide riboside chloride compositions and methods of preparation and use thereof. Also provided are related pharmaceutical compositions and methods of use thereof. The crystalline beta-D-nicotinamide riboside chloride compositions may be used to treat a disease or disorder that would benefit from increased NAD levels including a mitochondrial disease or disorder, insulin resistance, a metabolic syndrome, diabetes, obesity, or for increasing insulin sensitivity in a subject.Type: ApplicationFiled: June 2, 2015Publication date: July 20, 2017Inventors: Bruce G. SZCZEPANKIEWICZ, Karsten KOPPETSCH, Robert B. PERNI
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Publication number: 20170189433Abstract: Provided herein are stereoisomerically pure ester and carbonate analogues of nicotinamide riboside and nicotinamide riboside hydride, and pharmaceutical compositions and uses thereof. The stereoisomerically pure ester and carbonate analogues of nicotinamide riboside and nicotinamide riboside hydride may be used to treat a disease or disorder that would benefit from increased NAD levels including a mitochondrial disease or disorder, insulin resistance, a metabolic syndrome, diabetes, obesity, for increasing insulin sensitivity in a subject, or to treat or prevent a skin condition. The compounds have general formulas (I) or (II): wherein R1 is —C(?O)—X—(C2-C18 straight chain or branched) alkyl or —C(?O)—X—(C2-C18 straight chain or branched) alkenyl; each R2 is independently selected from hydrogen, and a —C(O)—X—(C1-C18 straight chain or branched) alkyl or a —C(O)—X—(C2-C18 straight chain or branched) alkenyl; and X is a covalent bond or O.Type: ApplicationFiled: June 5, 2015Publication date: July 6, 2017Inventors: Bruce G. SZCZEPANKIEWICZ, Frank PREUGSCHAT, Karsten KOPPETSCH, Robert B. PERNI
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Patent number: 9376461Abstract: Provided herein is a simple, one-step, non-enzymatic synthesis of O-Acetyl-ADP-ribose (OAADPR) from NAD and sodium acetate in acetic acid. The extension of this reaction to other carboxylic acids, demonstrates that the reaction between NAD, and NAD analogs produces mixtures of the corresponding 2?- and 3?-carboxylic esters. Included are O-carboxyl-ADP-ribose compounds and corresponding methods of synthesis (e.g., O-propionyl-ADP-ribose, O-succinyl-ADP-ribose, O-malonyl-ADP-ribose), as well as non-adenosine nucleoside compounds.Type: GrantFiled: June 6, 2012Date of Patent: June 28, 2016Assignee: GlaxoSmithKline LLCInventors: Karsten Koppetsch, Bruce G. Szczepankiewicz, Robert B Perni
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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: 20150218202Abstract: Provided herein is a simple, one-step, non-enzymatic synthesis of O-Acetyl-ADP-ribose (OAADPR) from NAD and sodium acetate in acetic acid. The extension of this reaction to other carboxylic acids, demonstrates that the reaction between NAD, and NAD analogs produces mixtures of the corresponding 2?- and 3?-carboxylic esters. Included are O-carboxyl-ADP-ribose compounds and corresponding methods of synthesis (e.g., O-propionyl-ADP-ribose, O-succinyl-ADP-ribose, O-malonyl-ADP-ribose), as well as non-adenosine nucleoside compounds.Type: ApplicationFiled: June 6, 2012Publication date: August 6, 2015Inventors: Karsten Koppetsch, Bruce G. Szczepankiewicz, 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