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).
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Publication number: 20240287124Abstract: 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: ApplicationFiled: January 26, 2024Publication date: August 29, 2024Applicant: Merck Sharp & Dohme LLCInventors: Mark W. Embrey, Jay A. Grobler, Mark E. Layton, Izzat T. Raheem
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Publication number: 20220331350Abstract: 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: ApplicationFiled: April 8, 2022Publication date: October 20, 2022Applicant: Merck Sharp & Dohme Corp.Inventors: Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
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Patent number: 11337991Abstract: 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: GrantFiled: December 11, 2019Date of Patent: May 24, 2022Assignee: Merck Sharp & Dohme Corp.Inventors: Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
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Publication number: 20200179273Abstract: 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: ApplicationFiled: June 1, 2018Publication date: June 11, 2020Applicant: Merck Sharp & DohmeCorpInventors: Stephanie Elizabeth Barrett, Seth P. Forster, Marian E. Gindy, Jay A. Grobler, David Brian Olsen, Ryan Stevenson Teller
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Patent number: 10624912Abstract: 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: GrantFiled: November 11, 2016Date of Patent: April 21, 2020Assignee: 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
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Publication number: 20200101098Abstract: 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: ApplicationFiled: December 11, 2019Publication date: April 2, 2020Applicant: Merck Sharp & Dohme Corp.Inventors: Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
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Patent number: 10548910Abstract: 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: GrantFiled: November 11, 2016Date of Patent: February 4, 2020Assignee: 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
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Patent number: 10537589Abstract: 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: GrantFiled: February 10, 2017Date of Patent: January 21, 2020Assignee: Merck Sharp & Dohme Corp.Inventors: Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
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Publication number: 20190216725Abstract: 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: ApplicationFiled: September 15, 2017Publication date: July 18, 2019Applicant: MERCK SHAPR & DOHME CORP.Inventors: Stephanie E. Barrett, Marian E. Gindy, Steven J. Henry, Seth P. Forster, Ryan S. Teller, Jay A. Grobler
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Publication number: 20180325926Abstract: 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: ApplicationFiled: November 11, 2016Publication date: November 15, 2018Applicant: 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
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Publication number: 20180325927Abstract: 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: ApplicationFiled: November 11, 2016Publication date: November 15, 2018Applicant: 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
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Patent number: 10081647Abstract: 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: GrantFiled: March 25, 2016Date of Patent: September 25, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Tao Yu, Sherman T. Waddell, John A. McCauley, Thomas H. Graham, Hong Li, Izzat Raheem, Jay A. Grobler
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Publication number: 20180055867Abstract: 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: ApplicationFiled: February 10, 2017Publication date: March 1, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Daria Hazuda, Michael D. Miller, Jay A. Grobler, Deborah Anne Nicoll-Griffith
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Publication number: 20180051043Abstract: 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: ApplicationFiled: March 25, 2016Publication date: February 22, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Tao Yu, Sherman T. Waddell, John A. McCauley, Thomas H. Graham, Hong Li, Izzat Raheem, Jay A. Grobler
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Patent number: 7807455Abstract: 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: GrantFiled: February 9, 2004Date of Patent: October 5, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jay Grobler, Osvaldo Flores, Eric J. Markel
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Patent number: 7786287Abstract: 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: GrantFiled: April 11, 2003Date of Patent: August 31, 2010Assignee: Merck & Co., Inc.Inventors: Osvaldo A. Flores, Jay Grobler, Edward M. Murray, Paul D. Zuck
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Publication number: 20100056516Abstract: 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: ApplicationFiled: July 13, 2007Publication date: March 4, 2010Inventors: 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
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Publication number: 20060228697Abstract: 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: ApplicationFiled: February 9, 2004Publication date: October 12, 2006Inventors: Jay Grobler, Osvaldo Flores, Eric Markel
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Publication number: 20050181356Abstract: 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: ApplicationFiled: April 11, 2003Publication date: August 18, 2005Inventors: Osvaldo Flores, Jay Grobler, Edward Murray, Paul Zuck