Patents Assigned to Merck Sharp
  • ANTIVIRAL ARYL-AMIDE PHOSPHODIAMIDE COMPOUNDS
    Publication number: 20190262365
    Abstract: Compounds of Formula (I): (Formula (I)) and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 20, 2017
    Publication date: August 29, 2019
    Applicants: Merck Sharp & Dohme Corp., Idenix Pharmaceuticals LLC.
    Inventors: Jean-Laurent Paparin, Houcine Rahali, Aurélien Salanson, Daniel Da Costa, David Dukhan, Timothy J. Hartingh, Izzat Raheem, John Schreier
  • SYNTHESIS OF CEPHALOSPORIN COMPOUNDS
    Publication number: 20190263831
    Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.
    Type: Application
    Filed: November 6, 2018
    Publication date: August 29, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: David Waller, Gregory Gazda, Zachary Minden, Lisa Barton, Clifton Leigh
  • COMBINATION OF A PD-1 ANTAGONIST AND ERIBULIN FOR TREATING UROTHELIAL CANCER
    Publication number: 20190263927
    Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and eribulin or a pharmaceutically acceptable salt thereof, and the use of the combination therapies for the treatment of urothelial cancer.
    Type: Application
    Filed: October 13, 2017
    Publication date: August 29, 2019
    Applicants: Merck Sharp & Dohme Corp., Eisai R&D Management Co., Ltd.
    Inventor: Martin S. OLIVO
  • Processes for making substituted quinazoline compounds using hydrogen bonding catalysts
    Patent number: 10392353
    Abstract: Disclosed herein is a novel process for preparing substituted quinazoline compounds of formula (I) using a hydrogen bonding catalyst.
    Type: Grant
    Filed: November 18, 2016
    Date of Patent: August 27, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Cheol K. Chung, Guy R. Humphrey, Zhijian Liu, Mark McLaughlin, Yingju Xu, Younong Yu
  • PHARMACEUTICAL COMPOSITIONS CONTAINING DORAVIRINE, TENOFOVIR DISOPROXIL FUMARATE AND LAMIVUDINE
    Publication number: 20190254977
    Abstract: The instant invention relates to pharmaceutical compositions comprising doravirine, tenofovir disoproxil fumarate and lamivudine. These compositions are useful for the treatment of HIV infection. Also disclosed are processes for making said pharmaceutical compositions.
    Type: Application
    Filed: November 29, 2016
    Publication date: August 22, 2019
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Santipharp Panmai, Aditya Tatavarti, Andrew M. Farrington, Varsha Biyyala, Leonardo R. Allain, Marcela Nefliu, Gerard R. Klinzing, Jie Ren, Matthew Lamm
  • Tricyclic gyrase inhibitors
    Patent number: 10385055
    Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
    Type: Grant
    Filed: September 10, 2014
    Date of Patent: August 20, 2019
    Assignees: MERCK SHARP & DOHME CORP., LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
    Inventors: John Finn, Leslie William Tari, Zhiyong Chen, Junhu Zhang, Douglas Phillipson, Suk Joong Lee, Michael Trzoss, Daniel Bensen, Xiaoming Li, Min Teng, Voon Ong, Allen John Borchardt, Thanh To Lam, Felice C. Lightstone, Sergio E. Wong, Toan B. Nguyen
  • CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20190247374
    Abstract: The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild congnitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 23, 2019
    Publication date: August 15, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Iyassu K. Sebhat, Ashok Arasappan, Scott B. Hoyt, Robert R. Wilkening, Duane DeMong
  • Tetrahydronaphthyridine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease
    Patent number: 10377768
    Abstract: The invention provides tetrahydronaphthyridine and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydronaphthyridine and related compounds.
    Type: Grant
    Filed: May 5, 2017
    Date of Patent: August 13, 2019
    Assignees: Lycera Corporation, Merck Sharp & Dohme Corp.
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Blair T. Lapointe, Vladimir Simov, Karin A. Stein, William D. Thomas, Peter L. Toogood, Chad A. Van Huis, Catherine M. White
  • Substituted quinolinones as PDE9 inhibitors
    Patent number: 10376504
    Abstract: The present invention is directed to azacyanoquinolinone compounds of the general structural formula: (wherein R5 and R6 are defined herein) which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: August 13, 2019
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Antonella Converso, Kevin Rodzinak
  • Treating infections with ceftolozane/tazobactam in subjects having impaired renal function
    Patent number: 10376496
    Abstract: Disclosed are methods of administering cephalosporin/tazobactam to human patients with end stage renal disease undergoing hemodialysis and suffering from a complicated intra-abdominal infection or a complicated urinary tract infection.
    Type: Grant
    Filed: September 9, 2014
    Date of Patent: August 13, 2019
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Gopal Krishna, Gurudatt Chandorkar, Elham Hershberger, Benjamin Miller, Alan Xiao
  • ILT3 LIGAND
    Publication number: 20190241655
    Abstract: The present invention provides antibodies and antigen-binding fragments thereof that bind ILT3, ILT3 ligand (i.e., PI16) or a complex between ILT3 and the ILT3 ligand. Methods for determining whether ILT3 and the ILT3 ligand bind together or whether a substance agonizes or antagonizes such binding are also provided.
    Type: Application
    Filed: November 6, 2017
    Publication date: August 8, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Daniel Cua, Holly Cherwinski, Adele Wang, Yi Chen, Barbara Joyce-Shaikh
  • Oxy-cyanoquinolinone PDE9 inhibitors
    Patent number: 10370337
    Abstract: The present invention is directed to oxycyanoquinolinone compounds which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: August 6, 2019
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Antonella Converso, Mildred L. Kaufman, Kevin Rodzinak
  • Thermostable respiratory synctial virus (RSV) vaccine compositions
    Patent number: 10369213
    Abstract: Methods for improving the drying yield and stability of RSV vaccines comprising a highly thermolabile enveloped live virus and/or one or more RSV protein subunits, are described. Methods for rapid drying of RSV formulations containing between 17.5% and 60% w/w of a non-polymeric sugar and using either conduction or radiation dominant drying mechanisms, are disclosed. The disclosed methods provide for; 1) a dried RSV formulation with improved stability profile; 2) faster drying; and 3) integration of dried RSV into a primary device (such as dual chamber cartridges, foil-pouch devices etc.), pre- as well as post-drying.
    Type: Grant
    Filed: October 13, 2014
    Date of Patent: August 6, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Akhilesh Bhambhani, Robert K. Evans, Lynne A. Isopi
  • Phenyl-cyanoquinolinone PDE9 inhibitors
    Patent number: 10370336
    Abstract: The present invention is directed to phenylcyanoquinolinone compounds which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: August 6, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Victoria Cofre, Antonella Converso, Kevin Rodzinak
  • Aryl acylsulfonamides as BLT1 antagonists
    Patent number: 10370368
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.
    Type: Grant
    Filed: November 28, 2016
    Date of Patent: August 6, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yongxin Han, Satyanarayana Tummanapalli, Phieng Siliphaivanh, Kerrie Spencer
  • Micro-titration vessel
    Patent number: 10369571
    Abstract: A micro-titration vessel may include a plurality of fins protruding outward from an exterior wall of a cup and flush with the bottom of the cup to provide stability to the vessel. Interior walls of the cup are angled inward at multiple points along the body of the cup, resulting in a small surface area at the bottom of the cup where titration occurs.
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: August 6, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Tinh Nguyen-DeMary
  • CYCLIC PHOSPHATE SUBSTITUTED NUCLEOSIDE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20190233463
    Abstract: The present invention relates to Cyclic Phosphate Substituted Nucleoside Compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein in A, B, R1, R2, R3, Q and V are as defined herein. The present invention also relates to compositions comprising a Cyclic Phosphate Substituted Nucleoside Compound, and methods of using the Cyclic Phosphate Substituted Nucleoside Compounds for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: June 20, 2017
    Publication date: August 1, 2019
    Applicants: MERCK SHARP & DOHME CORP., IDENIX PHARMACEUTICALS LLC
    Inventors: Stephane BOGEN, David DUKHAN, Guillaume BRANDT, Claire Pierra ROUVIERE, Cyril B. DOUSSON, Francois-Rene ALEXANDRE
  • Process for Preparing Beta-Lactamase Inhibitor Hydroxylurea Intermediates
    Publication number: 20190233421
    Abstract: The present invention relates to processes for the preparation of N-protected (2S,5R)-6-hydroxy-7-oxo-N-piperidin-4-yl-1,6-diazabicyclo[3.2.1]octane-2-carboxamide intermediates. Such compounds have application in the preparation of beta-lactamase inhibitors such as 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamides and esters, in particular, the beta lactamase inhibitor, (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also encompasses intermediates useful in the disclosed processes and methods for their preparation.
    Type: Application
    Filed: September 14, 2017
    Publication date: August 1, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jianguo Yin, Zhijian Liu, Nobuyoshi Yasuda, Mark Weisel
  • HIGH DRUG LOAD POLYMERIC NANOPARTICLE FORMULATIONS AND METHODS OF MAKING AND USING SAME
    Publication number: 20190231705
    Abstract: Described herein are polymeric nanoparticles that comprise {[(1R,25)-1-({[(1aR,5S,8S,10R,22aR)-5-tert-butyl-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]-dioxadiazacyclo-nonadecino[11,12-b]quinoxalin-8-yl]carbonyl}amino)-2-vinylcylopropyl]carbonyl}(cyclopropylsulfonyl)azanide, (i.e., grazoprevir), or a pharmaceutically acceptable salt thereof, and methods of making and using such nanoparticles.
    Type: Application
    Filed: January 23, 2019
    Publication date: August 1, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph Della Rocca, Angela M. Wagner, Wei Xu, W. Peter Wuelfing
  • Autoinjector device
    Patent number: D857192
    Type: Grant
    Filed: December 13, 2016
    Date of Patent: August 20, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Greg Burkett, Shu Kuen Chang, Angie Kim, Jin Ko, Scott Mackie, Philip G. Green, Sharad Gupta, Angela M. Amend Kwasnik, Christin L. O'Neill, Robert Stianchi, Witold Swiatek