Patents Assigned to Merck Sharp & Dohme
  • Methods for the treatment and prophylaxis of HIV and AIDS
    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
  • Glycan-based antibody-drug conjugates
    Patent number: 11332544
    Abstract: Genetically engineered antibodies containing non-native N-glycosylated sites, preparation of the antibodies in yeast and fungi, site-specific conjugation of drugs to these antibodies, and methods of treatment utilizing these antibodies are described herein.
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: May 17, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert Davidson, Bing Gong
  • Spiropiperidine allosteric modulators of nicotinic acetylcholine receptors
    Patent number: 11332463
    Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of 7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation (I).
    Type: Grant
    Filed: April 29, 2019
    Date of Patent: May 17, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Brendan M. Crowley, Brian T. Campbell, Harry R. Chobanian, James I. Fells, Deodial G. Guiadeen, Thomas J. Greshock, Kenneth J. Leavitt, Vanessa L. Rada, Ian M. Bell
  • INHIBITORS OF HISTONE DEACETYLASE USEFUL FOR THE TREATMENT OR PREVENTION OF HIV INFECTION
    Publication number: 20220144837
    Abstract: The present invention relates to Compounds of Formula I and Ia and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, X, A and B are as defined herein. The present invention also relates to compositions comprising at least one compound of Formula I or Ia, and methods of using the compounds of Formula I or Ia for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: March 16, 2020
    Publication date: May 12, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Wensheng Yu, Joseph A. Kozlowski, Dane James Clausen, Jian Liu, James Fells
  • PYRROLIDINE OREXIN RECEPTOR AGONISTS
    Publication number: 20220144771
    Abstract: The present invention is directed to pyrrolidine compounds which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: February 11, 2020
    Publication date: May 12, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Stephane L. Bogen, Michael J. Breslin, Dane James Clausen, Anthony Ginnetti, Michael T. Rudd, Shawn J. Stachel, Craig A. Stump, Dexi Yang
  • Blood-based biomarkers of tumor sensitivity to PD-1 antagonists
    Patent number: 11326211
    Abstract: The present disclosure describes baseline and on treatment blood-based gene signature biomarkers that are predictive of tumor sensitivity to therapy with a PD-1 antagonist. The on-treatment biomarkers comprise a PD-L1 gene signature or an interferon gamma gene signature and the baseline gene signature biomarker comprises genes associated with the oxidative phosphorylation pathway. The disclosure also provides methods and kits for testing tumor samples for these biomarkers, as well as methods for treating subjects with a PD-1 antagonist based on the test results.
    Type: Grant
    Filed: April 12, 2016
    Date of Patent: May 10, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark Ayers, Jared Lunceford, Andrey Loboda, Michael Nebozhyn, Terrill K. McClanahan, Heather Hirsch
  • METHODS FOR MAKING POLYSACCHARIDE-PROTEIN CONJUGATES
    Publication number: 20220133874
    Abstract: The present invention provides methods for making polysaccharide-protein conjugates in which polysaccharides, typically from bacteria, are conjugated to a carrier protein by reductive amination under conditions which improve conjugation reaction consistency, increase consumption of protein during conjugation reaction, generate conjugates of higher molecular weight, and/or reduce the levels of free cyanide in the conjugate reaction product. The polysaccharide-protein conjugates obtained using these methods are useful for inclusion in multivalent vaccines.
    Type: Application
    Filed: November 10, 2021
    Publication date: May 5, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jitin Bajaj, Michael Albert Winters, Emily Wen, Jian He
  • Heteroaryl piperidine ether allosteric modulators of the M4 muscarinic acetylcholine receptor
    Patent number: 11319298
    Abstract: The present invention is directed to heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
    Type: Grant
    Filed: December 18, 2017
    Date of Patent: May 3, 2022
    Assignees: Merck Sharp & Dohme Corp., MSD R&D (China) Co., Ltd.
    Inventors: Jianming Bao, Ronald Ferguson, Xiaolei Gao, Scott Harrison, Sandra L. Knowles, Michael Man-Chu Lo, Robert D. Mazzola, Jr., Jeffrey W. Shubert
  • Substituted phenyloxetane and phenyltetrahydrofuran compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
    Patent number: 11319295
    Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Grant
    Filed: October 4, 2018
    Date of Patent: May 3, 2022
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Catherine M. White, Meredeth Ann McGowan, Yongxin Han, Nunzio Sciammetta
  • Substituted cyclobutylbenzene compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
    Patent number: 11319283
    Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Grant
    Filed: October 4, 2018
    Date of Patent: May 3, 2022
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Meredeth Ann McGowan, Abdelghani Achab, Xavier Fradera, Yongxin Han, Derun Li, Jongwon Lim, Kun Liu, Nunzio Sciammetta, Catherine M. White, Wensheng Yu, Hongjun Zhang, Hua Zhou
  • Combinations of PD-1 antagonists and benzo [b] thiophene STING agonists for cancer treatment
    Patent number: 11312772
    Abstract: Therapeutic combinations that comprise at least one antagonist of the Programmed Death 1 receptor (PD-1) and at least one benzo[b]thiophene compound that activates the Stimulator of Interferon Genes (STING) pathway are disclosed herein. Also disclosed is the use of such therapeutic combinations for the treatment of cancers.
    Type: Grant
    Filed: July 30, 2018
    Date of Patent: April 26, 2022
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Saso Cemerski, Jared N. Cumming, Johnny E. Kopinja, Samanthi A. Perera, Benjamin Wesley Trotter, Archie Ngai-Chiu Tse
  • 9-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use
    Patent number: 11312719
    Abstract: In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): and pharmaceutically acceptable salts thereof, wherein, ring A, R1 and R2 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
    Type: Grant
    Filed: November 26, 2019
    Date of Patent: April 26, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew A. Larsen, Amjad Ali, Jared Cumming, Duane DeMong, Qiaolin Deng, Thomas H. Graham, Elisabeth Hennessy, Andrew J. Hoover, Ping Liu, Kun Liu, Umar Faruk Mansoor, Jianping Pan, Christopher W. Plummer, Aaron Sather, Uma Swaminathan, Huijun Wang, Yonglian Zhang
  • Oxo-tetrahydro-isoquinoline carboxylic acids as STING inhibitors
    Patent number: 11311528
    Abstract: The instant invention provides compounds of formula I which are STING inhibitors, and as such are useful for the treatment of STING-mediated diseases such as inflammation, asthma, COPD and cancer.
    Type: Grant
    Filed: March 15, 2019
    Date of Patent: April 26, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Matthew L. Childers, James P. Jewell, Charles A. Lesburg, Tony Siu
  • 2-AMINO-N-PHENYL-NICOTINAMIDES AS NAV1.8 INHIBITORS
    Publication number: 20220119363
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
    Type: Application
    Filed: October 28, 2019
    Publication date: April 21, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Christopher James Bungard, Harry R. Chobanian, Kristen L. G. Jones, Mark E. Layton, Jian Liu, James J. Perkins, Jeffrey William Schubert, Shawn J. Stachel, Linda M. Suen-Lai, Zhe Wu
  • SPIROPIPERIDINE ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20220119351
    Abstract: The present disclosure relates to compounds of formula (I) that are useful as modulators of 7? nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
    Type: Application
    Filed: April 27, 2020
    Publication date: April 21, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Brian T. Campbell, Brendan M. Crowley, James Fells, Kenneth J. Leavitt, Anthony J. Roecker, Andrew John Harvey, Belinda C. Huff, Dharam Paul, Christophe Morice, Christophe Joseph, Patrick Bazzini, Jean-Marie Contreras, Fabrice Garrido, Aurelie Witzel
  • AUTOMATED BIOMANUFACTURING SYSTEMS, FACILITIES, AND PROCESSES
    Publication number: 20220119757
    Abstract: Disclosed are a process and an automated facility for manufacturing a purified protein of interest. The protein of interest can be a recombinant or naturally occurring protein and/or a therapeutic or other medically useful protein. For example, the disclosed process and automated facility are useful for manufacturing a purified protein drug substance.
    Type: Application
    Filed: February 16, 2020
    Publication date: April 21, 2022
    Applicants: Just-Evotec Biologics, Inc., Merck Sharp & Dohme Corp.
    Inventors: Michael Wayne Vandiver, Eva Fan Gefroh, Rebecca Eileen McCoy, Robert James Piper, JR., Mark A. Brower, Nuno J. Dos Santos Pinto, William N. Napoli, Rachel Y. Straughn, Lisa A. Connell-Crowley, Megan J. McClure
  • PCSK9 antagonists bicyclo-compounds
    Patent number: 11306125
    Abstract: Disclosed are compounds of Formula I, or a salt thereof cyclic polypeptide of Formula I: Formula I where A, B, E, R4, and R8 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g.
    Type: Grant
    Filed: June 20, 2019
    Date of Patent: April 19, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yusheng Xiong, Thomas Joseph Tucker, Chengwei Wu, Elisabetta Bianchi, Danila Branca, Angela Dawn Kerekes, Abbas M. Walji, Hubert B. Josien, Fa-Xiang Ding, Hyewon Youm, Alessia Santoprete, Raffaele Ingenito
  • Crystalline form of a BACE inhibitor, compositions, and use
    Patent number: 11306080
    Abstract: The present invention provides a novel crystalline form of verubecestat (Crystalline Form II of Verubecestat) and pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an A? pathology and/or a symptom or symptoms thereof. Non-limiting examples of such A? pathologies, including Alzheimer's disease and mild cognitive impairment, are disclosed herein.
    Type: Grant
    Filed: June 8, 2018
    Date of Patent: April 19, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Laura M. Artino, William Morris, Eric Sirota, Richard J. Varsolona
  • PREPARATION OF BENZIMIDAZOLONE DERIVATIVES AS NOVEL DIACYLGLYCERIDE O-ACYLTRANSFERASE 2 INHIBITORS
    Publication number: 20220112182
    Abstract: Invented are compounds of Formula I and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.
    Type: Application
    Filed: October 6, 2021
    Publication date: April 14, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Yeon-Hee Lim, Eric R. Ashley, Jianming Bao, Chen Cheng, James P. Roane, Emma Helen Southgate
  • PREPARATION OF OXINDOLE DERIVATIVES AS NOVEL DIACYLGLYCERIDE O-ACYLTRANSFERASE 2 INHIBITORS
    Publication number: 20220112181
    Abstract: Invented are compounds of formula I and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.
    Type: Application
    Filed: October 6, 2021
    Publication date: April 14, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Yeon-Hee Lim, Jianming Bao, James P. Roane