Patents by Inventor Michael Graupe

Michael Graupe 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).

  • FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
    Publication number: 20160362421
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: June 21, 2016
    Publication date: December 15, 2016
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Michael Graupe, Juan Guerrero, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Chandrasekar Venkataramani, Jeff Zablocki
  • Antiviral compounds
    Patent number: 9511056
    Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: May 16, 2014
    Date of Patent: December 6, 2016
    Assignee: Gilead Pharmasset LLC
    Inventors: Elizabeth M. Bacon, Eda Canales, Aesop Cho, Jeromy J. Cottell, Manoj C. Desai, Michael Graupe, Hongyan Guo, Randall L. Halcomb, Darryl Kato, Choung U. Kim, Thorsten A. Kirschberg, Evan S. Krygowski, Scott E. Lazerwith, John O. Link, Hongtao Liu, Qi Liu, Richard L. Mackman, Michael L. Mitchell, Jay P. Parrish, Hyung-Jung Pyun, Joseph H. Saugier, Scott D. Schroeder, Jianyu Sun, James G. Taylor, James D. Trenkle, Winston C. Tse, Randall W. Vivian, William J. Watkins, Lianhong Xu
  • FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
    Publication number: 20160347744
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: May 11, 2016
    Publication date: December 1, 2016
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Michael Graupe, Juan Guerrero, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Chandrasekar Venkataramani, Jeff Zablocki
  • FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
    Publication number: 20160317504
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein X, Y, Z, R2, R3, R4, p and q are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: July 7, 2016
    Publication date: November 3, 2016
    Inventors: Michael Graupe, Yafan Lu, Jeff Zablocki
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 9416115
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein X, Y, Z, R2, R3, R4, p and q are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: December 3, 2014
    Date of Patent: August 16, 2016
    Assignee: Gilead Scineces, Inc.
    Inventors: Michael Graupe, Yafan Lu, Jeff A. Zablocki
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 9403782
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: August 2, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Michael Graupe, Juan Guerrero, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Chandrasekar Venkataramani, Jeff Zablocki
  • APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS
    Publication number: 20160130251
    Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
    Type: Application
    Filed: May 19, 2015
    Publication date: May 12, 2016
    Inventors: Michael Graupe, Keith Koch, Britton K. Corkey, Gregory Notte, Lawrence S. Melvin, JR.
  • THERAPEUTIC COMPOUNDS
    Publication number: 20160108030
    Abstract: Compounds of formula (I) or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: February 28, 2014
    Publication date: April 21, 2016
    Inventors: Gediminas Brizgys, Eda Canales, Chien-Hung Chou, Michael Graupe, Yunfeng Eric Hu, Scott E. Lazerwith, John O. Link, Qi Liu, Yafan Lu, Roland D. Saito, Scott D. Schroeder, John R. Somoza, Winston C. Tse, Jennifer R. Zhang
  • FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
    Publication number: 20160096846
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: October 1, 2015
    Publication date: April 7, 2016
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Michael Graupe, Juan Guerrero, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Chandrasekar Venkataramani, Jeff Zablocki
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 9193694
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: September 26, 2013
    Date of Patent: November 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
    Publication number: 20150329558
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: July 24, 2015
    Publication date: November 19, 2015
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Michael Graupe, Juan Guerrero, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Chandrasekar Venkataramani, Jeff Zablocki
  • COMPOUNDS FOR THE TREATMENT OF ADDICTION
    Publication number: 20150250805
    Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
    Type: Application
    Filed: March 16, 2015
    Publication date: September 10, 2015
    Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G. Strickley, Chandrasekar Venkataramani, Jeff Zablocki
  • FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
    Publication number: 20150239904
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: February 24, 2015
    Publication date: August 27, 2015
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • MODULATORS OF TOLL-LIKE RECEPTOR 7
    Publication number: 20150239888
    Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
    Type: Application
    Filed: February 19, 2015
    Publication date: August 27, 2015
    Inventors: Michael Graupe, Randall L. Halcomb
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 9115096
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: May 8, 2012
    Date of Patent: August 25, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Apoptosis signal-regulating kinase inhibitors
    Patent number: 9067933
    Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
    Type: Grant
    Filed: July 2, 2013
    Date of Patent: June 30, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, Jr., Gregory Notte
  • FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
    Publication number: 20150175560
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein X, Y, Z, R2, R3, R4, p and q are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: December 3, 2014
    Publication date: June 25, 2015
    Inventors: Michael Graupe, Yafan Lu, Jeff A. Zablocki
  • Compounds for the treatment of addiction
    Patent number: 9000015
    Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
    Type: Grant
    Filed: August 13, 2013
    Date of Patent: April 7, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G. Strickley, Chandrasekar Venkataramani, Jeff Zablocki
  • Modulators of toll-like receptor 7
    Patent number: 8993755
    Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: March 31, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Randall L. Halcomb
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 8962610
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero