Patents by Inventor Bruce G. Szczepankiewicz
Bruce G. Szczepankiewicz 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).
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
Patent number: 8637546Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: GrantFiled: April 3, 2012Date of Patent: January 28, 2014Assignee: AbbVie Inc.Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
-
Publication number: 20130059873Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: ApplicationFiled: April 3, 2012Publication date: March 7, 2013Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
-
Patent number: 8119664Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: GrantFiled: March 19, 2010Date of Patent: February 21, 2012Assignee: Abbott LaboratoriesInventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
-
Patent number: 7888374Abstract: The present invention relates to compounds that are inhibitors of c-jun N-terminal kinase 1, 2, or 3 (JNK1, JNK2, or JNK3), compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the activation of JNK1, JNK2 and JNK3.Type: GrantFiled: January 23, 2006Date of Patent: February 15, 2011Assignee: Abbott LaboratoriesInventors: Gang Liu, Hing L. Sham, Bruce G. Szczepankiewicz, Zhili Xin, Hongyu Zhao, Michael D. Serby, Bo Liu, Mei Liu
-
Publication number: 20100190822Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: ApplicationFiled: March 19, 2010Publication date: July 29, 2010Applicant: ABBOTT LABORATORIESInventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
-
Patent number: 7365093Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.Type: GrantFiled: February 23, 2005Date of Patent: April 29, 2008Assignee: Abbott LaboratoriesInventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen, Bruce G. Szczepankiewicz, Kenneth J. Henry, Gang Liu, Steven J. Wittenberger, Steven A. King
-
Patent number: 7262207Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: GrantFiled: February 27, 2004Date of Patent: August 28, 2007Assignee: Abbott LaboratoriesInventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong