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).

  • PD-1/PD-L1 INHIBITORS
    Publication number: 20180305315
    Abstract: Compounds according to formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
    Type: Application
    Filed: April 19, 2018
    Publication date: October 25, 2018
    Inventors: Evangelos Aktoudianakis, Todd Appleby, Aesop Cho, Zhimin Du, Michael Graupe, Juan A. Guerrero, Salman Y. Jabri, Lateshkumar Thakorlal Lad, Paulo A. Machicao Tello, Jonathan William Medley, Samuel E. Metobo, Prasenjit Kumar Mukherjee, Devan Naduthambi, Gregory Notte, Eric Q. Parkhill, Barton W. Phillips, Scott Preston Simonovich, Neil H. Squires, Chandrasekar Venkataramani, Peiyuan Wang, William J. Watkins, Jie Xu, Kin Shing Yang, Christopher Allen Ziebenhaus
  • THERAPEUTIC COMPOUNDS
    Publication number: 20180273508
    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: March 2, 2018
    Publication date: September 27, 2018
    Inventors: Gediminas Brizgys, Eda Canales, Chien-Hung Chou, Michael Graupe, Randall L. Halcomb, 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
  • Therapeutic compounds
    Patent number: 10071985
    Abstract: The present disclosure relates to a compound of formula (Ia), (Ib), (IIa), and (IIb): which are useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Grant
    Filed: August 17, 2017
    Date of Patent: September 11, 2018
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Steven J. Henry, John O. Link, Charles William Rowe, Roland D. Saito, Scott D. Schroeder, Dimitrios Stefanidis, Winston C. Tse, Jennifer R. Zhang
  • Compounds and combinations for the treatment of HIV
    Patent number: 10059697
    Abstract: Provided are compounds, compositions, combinations, kits, uses, and methods for treating HIV in a human being using such compounds or combinations with proteasome inhibitors.
    Type: Grant
    Filed: September 29, 2016
    Date of Patent: August 28, 2018
    Assignee: Gilead Sciences, Inc.
    Inventors: Tomas Cihlar, Michael Graupe, Yunfeng Eric Hu, Jeffrey Patrick Murry, Derek Dean Sloan, George Stepan, Helen Yu
  • Compounds for the treatment of addiction
    Patent number: 9987295
    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: March 31, 2017
    Date of Patent: June 5, 2018
    Assignee: Amygdala Neurosciences, Inc.
    Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G Strickley, Chandrasekar Venkataramani, Jeff Zablocki
  • Antiviral compounds
    Patent number: 9981955
    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: September 28, 2016
    Date of Patent: May 29, 2018
    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
  • Therapeutic compounds
    Patent number: 9951043
    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: Grant
    Filed: February 28, 2014
    Date of Patent: April 24, 2018
    Assignee: Gilead Sciences, Inc.
    Inventors: Gediminas Brizgys, Eda Canales, Chien-hung Chou, Michael Graupe, Randall L. Halcomb, 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
    Patent number: 9920018
    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 7, 2016
    Date of Patent: March 20, 2018
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Yafan Lu, Jeff Zablocki
  • THERAPEUTIC COMPOUNDS
    Publication number: 20180051005
    Abstract: The present disclosure relates to a compound of formula (Ia), (Ib), (IIa), and (IIb): which are useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: August 17, 2017
    Publication date: February 22, 2018
    Inventors: Michael Graupe, Steven J. Henry, John O. Link, Charles William Rowe, Roland D. Saito, Scott D. Schroeder, Dimitrios Stefanidis, Winston C. Tse, Jennifer R. Zhang
  • COMPOUNDS FOR THE TREATMENT OF ADDICTION
    Publication number: 20170266210
    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 31, 2017
    Publication date: September 21, 2017
    Applicant: Amygdala Neurosciences, Inc.
    Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G. Strickley, Chandrasekar Venkataramani, Jeff Zablocki
  • APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS
    Publication number: 20170196844
    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: January 23, 2017
    Publication date: July 13, 2017
    Inventors: MICHAEL GRAUPE, Keith Koch, Britton Kenneth Corkey, Gregory Notte, Lawrence S. Melvin, JR.
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 9695192
    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: February 24, 2015
    Date of Patent: July 4, 2017
    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
    Patent number: 9682998
    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: June 21, 2016
    Date of Patent: June 20, 2017
    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
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 9676760
    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: May 11, 2016
    Date of Patent: June 13, 2017
    Assignee: Gilead Sciences, Inc.
    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
  • COMPOUNDS AND COMBINATIONS FOR THE TREATMENT OF HIV
    Publication number: 20170114048
    Abstract: Provided are compounds, compositions, combinations, kits, uses, and methods for treating HIV in a human being using such compounds or combinations with proteasome inhibitors.
    Type: Application
    Filed: September 29, 2016
    Publication date: April 27, 2017
    Inventors: Tomas Cihlar, Michael Graupe, Yunfeng Eric Hu, Jeffrey Patrick Murry, Derek Dean Sloan, George Stepan, Helen Yu
  • Modulators of toll-like receptor 7
    Patent number: 9611268
    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: February 19, 2015
    Date of Patent: April 4, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Randall L. Halcomb
  • Compounds for the treatment of addiction
    Patent number: 9610299
    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: March 16, 2015
    Date of Patent: April 4, 2017
    Assignee: Gilead Sciences, Inc.
    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: 20170088527
    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 7, 2016
    Publication date: March 30, 2017
    Inventors: Michael Graupe, Yafan Lu, Jeff Zablocki
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 9598435
    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: October 1, 2015
    Date of Patent: March 21, 2017
    Assignee: Gilead Sciences, Inc.
    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
  • Apoptosis signal-regulating kinase inhibitors
    Patent number: 9586932
    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: May 19, 2015
    Date of Patent: March 7, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Keith Koch, Britton K. Corkey, Gregory Notte, Lawrence S. Melvin, Jr.