Patents by Inventor Jay A. Grobler

Jay A. Grobler 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).

  • Publication number: 20240287124
    Abstract: The present invention is directed to prodrugs of compound A: which are nucleoside reverse transcriptase translocation inhibitors (NRTTI) and are useful in the inhibition of HIV reverse transcriptase. The present invention also relates to the use of these compounds for prophylaxis of infection by HIV, treatment of infection by HIV, and prophylaxis, treatment, and delay in the onset or progression of AIDS and/or AIDS-related complexes.
    Type: Application
    Filed: January 26, 2024
    Publication date: August 29, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Mark W. Embrey, Jay A. Grobler, Mark E. Layton, Izzat T. Raheem
  • Publication number: 20220331350
    Abstract: The present invention is directed to methods for inhibition of HIV reverse transcriptase, treatment of infection by HIV, prophylaxis of infection by HIV, and the treatment, prophylaxis and/or delay in the onset or progression of AIDS or ARC by administering a compound of structural Formula I or a pharmaceutically acceptable salt or co-crystal thereof, wherein X is —F or —Cl, less frequently than once daily.
    Type: Application
    Filed: April 8, 2022
    Publication date: October 20, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
  • Patent number: 11337991
    Abstract: The present invention is directed to methods for inhibition of HIV reverse transcriptase, treatment of infection by HIV, prophylaxis of infection by HIV, and the treatment, prophylaxis and/or delay in the onset or progression of AIDS or ARC by administering a compound of structural Formula I or a pharmaceutically acceptable salt or co-crystal thereof, wherein X is —F or —Cl, less frequently than once daily.
    Type: Grant
    Filed: December 11, 2019
    Date of Patent: May 24, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
  • Publication number: 20200179273
    Abstract: The present invention relates to long-acting implants useful for the treatment of bacterial infections, particularly mycobacterial infections. The invention also relates to methods of use of such long-acting implants for the treatment of mycobacterial infections such as those caused by Mycobacteria tuberculosis.
    Type: Application
    Filed: June 1, 2018
    Publication date: June 11, 2020
    Applicant: Merck Sharp & DohmeCorp
    Inventors: Stephanie Elizabeth Barrett, Seth P. Forster, Marian E. Gindy, Jay A. Grobler, David Brian Olsen, Ryan Stevenson Teller
  • Patent number: 10624912
    Abstract: The present invention relates to Spirocyclic Pyridotriazine Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Pyridotriazine Derivative, and methods of using the Spirocyclic Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: November 11, 2016
    Date of Patent: April 21, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas H. Graham, Tao Yu, Sherman T. Waddell, John A. McCauley, Andrew Stamford, Wengsheng Liu, Jay A. Grobler, Libo Xu
  • Publication number: 20200101098
    Abstract: The present invention is directed to methods for inhibition of HIV reverse transcriptase, treatment of infection by HIV, prophylaxis of infection by HIV, and the treatment, prophylaxis and/or delay in the onset or progression of AIDS or ARC by administering a compound of structural Formula I or a pharmaceutically acceptable salt or co-crystal thereof, wherein X is —F or —Cl, less frequently than once daily.
    Type: Application
    Filed: December 11, 2019
    Publication date: April 2, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
  • Patent number: 10548910
    Abstract: The present invention relates to Amido-Substituted Pyridotriazine Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein B, X, Y, R, R1, R2 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Pyridotriazine Derivative, and methods of using the Amido-Substituted Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: November 11, 2016
    Date of Patent: February 4, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas H. Graham, Tao Yu, Sherman T. Waddell, John A. McCauley, Andrew Stamford, Wensheng Liu, Jay A. Grobler, Libo Xu
  • Patent number: 10537589
    Abstract: The present invention is directed to methods for inhibition of HIV reverse transcriptase, treatment of infection by HIV, prophylaxis of infection by HIV, and the treatment, prophylaxis and/or delay in the onset or progression of AIDS or ARC by administering a compound of structural Formula I or a pharmaceutically acceptable salt or co-crystal thereof, wherein X is —F or —Cl, less frequently than once daily.
    Type: Grant
    Filed: February 10, 2017
    Date of Patent: January 21, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
  • Publication number: 20190216725
    Abstract: This invention relates to novel implant drug delivery systems for long-acting delivery of integrase inhibitors. These compositions are useful for the treatment or prevention of human immunodeficiency virus (HIV) infection.
    Type: Application
    Filed: September 15, 2017
    Publication date: July 18, 2019
    Applicant: MERCK SHAPR & DOHME CORP.
    Inventors: Stephanie E. Barrett, Marian E. Gindy, Steven J. Henry, Seth P. Forster, Ryan S. Teller, Jay A. Grobler
  • Publication number: 20180325926
    Abstract: The present invention relates to Spirocyclic Pyridotriazine Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R16 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Pyridotriazine Derivative, and methods of using the Spirocyclic Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: November 11, 2016
    Publication date: November 15, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Thomas H. Graham, Tao Yu, Sherman T. Waddell, John A. McCauley, Andrew Stamford, Wengsheng Liu, Jay A. Grobler, Libo Xu
  • Publication number: 20180325927
    Abstract: The present invention relates to Amido-Substituted Pyridotriazine Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein B, X, Y, R, R1, R2 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Pyridotriazine Derivative, and methods of using the Amido-Substituted Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: November 11, 2016
    Publication date: November 15, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Thomas H. Graham, Tao Yu, Sherman T. Waddell, John A. McCauley, Andrew Stamford, Wengsheng Liu, Jay A. Grobler, Libo Xu
  • Patent number: 10081647
    Abstract: The present invention relates to Phosphate Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Phosphate Substituted Quinolizine Derivative, and methods of using the Phosphate Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: March 25, 2016
    Date of Patent: September 25, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tao Yu, Sherman T. Waddell, John A. McCauley, Thomas H. Graham, Hong Li, Izzat Raheem, Jay A. Grobler
  • Publication number: 20180055867
    Abstract: The present invention is directed to methods for inhibition of HIV reverse transcriptase, treatment of infection by HIV, prophylaxis of infection by HIV, and the treatment, prophylaxis and/or delay in the onset or progression of AIDS or ARC by administering a compound of structural Formula I or a pharmaceutically acceptable salt or co-crystal thereof, wherein X is —F or —Cl, less frequently than once daily.
    Type: Application
    Filed: February 10, 2017
    Publication date: March 1, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
  • Publication number: 20180051043
    Abstract: The present invention relates to Phosphate Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Phosphate Substituted Quinolizine Derivative, and methods of using the Phosphate Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: March 25, 2016
    Publication date: February 22, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Tao Yu, Sherman T. Waddell, John A. McCauley, Thomas H. Graham, Hong Li, Izzat Raheem, Jay A. Grobler
  • Patent number: 7807455
    Abstract: The present invention features methods for producing HCV replicons using HCV encoding sequences from different isolates. The featured methods are based on the discovered importance of NS3 amino acid position 470 in conferring cell culture replication activity to different HCV isolates.
    Type: Grant
    Filed: February 9, 2004
    Date of Patent: October 5, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jay Grobler, Osvaldo Flores, Eric J. Markel
  • Patent number: 7786287
    Abstract: The present invention features assays employing a beta-lactamase reporter system, an HCV replicon enhanced cell, and/or a chimeric HCV replicon containing a 3? UTR based on the HCV-1a 3? UTR. These features can be employed alone or together, and are preferably combined together to measure HCV replicon activity and the affect of compounds on such activity.
    Type: Grant
    Filed: April 11, 2003
    Date of Patent: August 31, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Osvaldo A. Flores, Jay Grobler, Edward M. Murray, Paul D. Zuck
  • Publication number: 20100056516
    Abstract: 1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines.
    Type: Application
    Filed: July 13, 2007
    Publication date: March 4, 2010
    Inventors: Peter D. Williams, Shankar Venkatraman, H. Marie Langford, Boyoung Kim, Theresa M. Booth, Jay A. Grobler, Donnette Staas, Rowena D. Ruzek, Mark W. Embrey, Catherine M. Wiscount, Terry A. Lyle
  • Publication number: 20060228697
    Abstract: The present invention features methods for producing HCV replicons using HCV encoding sequences from different isolates. The featured methods are based on the discovered importance of NS3 amino acid position 470 in conferring cell culture replication activity to different HCV isolates.
    Type: Application
    Filed: February 9, 2004
    Publication date: October 12, 2006
    Inventors: Jay Grobler, Osvaldo Flores, Eric Markel
  • Publication number: 20050181356
    Abstract: The present invention features assays employing a beta-lactamase reporter system, an HCV replicon enhanced cell, and/or a chimeric HCV replicon containing a 3? UTR based on the HCV-1a 3? UTR.
    Type: Application
    Filed: April 11, 2003
    Publication date: August 18, 2005
    Inventors: Osvaldo Flores, Jay Grobler, Edward Murray, Paul Zuck