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: 10590135
    Abstract: 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: Grant
    Filed: November 19, 2015
    Date of Patent: March 17, 2020
    Assignee: GLAXOSMITHKLINE LLC
    Inventors: 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: 10485814
    Abstract: 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: Grant
    Filed: June 5, 2015
    Date of Patent: November 26, 2019
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Bruce G. Szczepankiewicz, Frank Preugschat, Karsten Koppetsch, Robert B. Perni
  • Patent number: 10316054
    Abstract: 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: Grant
    Filed: June 2, 2015
    Date of Patent: June 11, 2019
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Bruce G. Szczepankiewicz, Karsten Koppetsch, Robert B. Perni
  • Publication number: 20180044338
    Abstract: 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: Application
    Filed: August 4, 2017
    Publication date: February 15, 2018
    Inventors: 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: 20170355697
    Abstract: 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: Application
    Filed: November 19, 2015
    Publication date: December 14, 2017
    Inventors: 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: 9834558
    Abstract: 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: Grant
    Filed: November 19, 2014
    Date of Patent: December 5, 2017
    Assignee: GLAXOSMITHKLINE LLC
    Inventors: 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: 9765075
    Abstract: 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: Grant
    Filed: May 13, 2014
    Date of Patent: September 19, 2017
    Assignee: GLAXOSMITHKLINE LLC
    Inventors: 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: 20170204131
    Abstract: 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: Application
    Filed: June 2, 2015
    Publication date: July 20, 2017
    Inventors: Bruce G. SZCZEPANKIEWICZ, Karsten KOPPETSCH, Robert B. PERNI
  • Publication number: 20170189433
    Abstract: 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: Application
    Filed: June 5, 2015
    Publication date: July 6, 2017
    Inventors: Bruce G. SZCZEPANKIEWICZ, Frank PREUGSCHAT, Karsten KOPPETSCH, Robert B. PERNI
  • Patent number: 9376461
    Abstract: 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: Grant
    Filed: June 6, 2012
    Date of Patent: June 28, 2016
    Assignee: GlaxoSmithKline LLC
    Inventors: Karsten Koppetsch, Bruce G. Szczepankiewicz, Robert B Perni
  • Publication number: 20160083386
    Abstract: 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: Application
    Filed: May 13, 2014
    Publication date: March 24, 2016
    Inventors: 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: 20150218202
    Abstract: 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: Application
    Filed: June 6, 2012
    Publication date: August 6, 2015
    Inventors: Karsten Koppetsch, Bruce G. Szczepankiewicz, Robert B. Perni
  • Publication number: 20150152108
    Abstract: 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: Application
    Filed: November 19, 2014
    Publication date: June 4, 2015
    Inventors: 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: 8637546
    Abstract: 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: Grant
    Filed: April 3, 2012
    Date of Patent: January 28, 2014
    Assignee: 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: 20130059873
    Abstract: 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: Application
    Filed: April 3, 2012
    Publication date: March 7, 2013
    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
  • Patent number: 8119664
    Abstract: 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: Grant
    Filed: March 19, 2010
    Date of Patent: February 21, 2012
    Assignee: Abbott Laboratories
    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
  • Patent number: 7888374
    Abstract: 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: Grant
    Filed: January 23, 2006
    Date of Patent: February 15, 2011
    Assignee: Abbott Laboratories
    Inventors: Gang Liu, Hing L. Sham, Bruce G. Szczepankiewicz, Zhili Xin, Hongyu Zhao, Michael D. Serby, Bo Liu, Mei Liu
  • Publication number: 20100190822
    Abstract: 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: Application
    Filed: March 19, 2010
    Publication date: July 29, 2010
    Applicant: ABBOTT LABORATORIES
    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
  • Patent number: 7365093
    Abstract: 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: Grant
    Filed: February 23, 2005
    Date of Patent: April 29, 2008
    Assignee: Abbott Laboratories
    Inventors: 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: 7262207
    Abstract: 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: Grant
    Filed: February 27, 2004
    Date of Patent: August 28, 2007
    Assignee: Abbott Laboratories
    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