Patents Assigned to Merck Sharp & Dohme
  • Intravaginal ring drug delivery system
    Patent number: 10413504
    Abstract: Described herein is an intra-vaginal drug delivery system comprising (i) a core comprising a first thermoplastic polymer and a first therapeutic agent, wherein the first therapeutic agent is dissolved in the first thermoplastic polymer, and (ii) a skin surrounding the core comprising a second thermoplastic polymer, wherein the first therapeutic agent is less permeable in the second thermoplastic polymer than the first thermoplastic polymer, and a second therapeutic agent in solid form, wherein the second therapeutic agent is loaded in a portion of the skin.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: September 17, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wouter de Graaff, Willy J. H. Verhoeven
  • Co-agonists of the glucagon and GLP-1 receptors
    Patent number: 10413593
    Abstract: Described are peptide analogs of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have relatively balanced agonist activity at the glucagon-like peptide 1 (GLP-1) receptor and the glucagon (GCG) receptor, and the use of such GLP-1 receptor/GCG receptor co-agonists for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: September 17, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Elisabetta Bianchi, Paul E. Carrington, Qiaolin Deng, Ravi Nargund, Federica Orvieto, Anandan Palani, Antonello Pessi, Thomas Joseph Tucker, Chengwei Wu
  • PIPERIDINONE CARBOXAMIDE AZAINDANE CGRP RECEPTOR ANTAGONISTS
    Publication number: 20190275024
    Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Application
    Filed: April 26, 2019
    Publication date: September 12, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
  • INDOLE DERIVATIVES USEFUL AS INHIBITORS OF DIACYLGLYCERIDE O-ACYLTRANSFERASE 2
    Publication number: 20190276443
    Abstract: The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
    Type: Application
    Filed: November 13, 2017
    Publication date: September 12, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Thomas H. Graham, Jinlong Jiang, Fa-Xiang Ding, Clare Tudge
  • Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections
    Patent number: 10407421
    Abstract: The present invention relates to bicyclic aryl monobactam compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein A1, L, M, W, X, Y, Z, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a bicyclic aryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of one or more beta-lactamase inhibitor compounds.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: September 10, 2019
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Weiguo Liu, Fa-Xiang Ding, Wanying Sun, Reynalda Keh Dejesus, Haifeng Tang, Xianhai Huang, Jinlong Jiang, Yan Guo, Hongwu Wang
  • Purifying insulin using cation exchange and reverse phase chromatography in the presence of an organic modifier and elevated temperature
    Patent number: 10407483
    Abstract: A process is described for purifying insulin and insulin analogs that comprises high-pressure liquid chromatography with an acidic cation exchange medium performed in the presence of a water miscible organic modifier and at an elevated temperature followed by reverse phase chromatography performed in the presence of a water miscible organic modifier and at an elevated temperature.
    Type: Grant
    Filed: March 11, 2015
    Date of Patent: September 10, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Allison D. Ortigosa, Michael P. Coleman, Shibu T. George, Michael A. Rauscher, Mark C. Sleevi, Kartoa Chow
  • Biocatalytic transamination process
    Patent number: 10407702
    Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: employing dynamic kinetic resolution (DKR). The DKR process involves an enzymatic enantioselective amination reaction catalyzed by transaminases. The process can be used to manufacture key intermediates in the preparation of poly (ADP-ribose) polymerase (PARP) inhibitors which may be useful for the treatment of cancer.
    Type: Grant
    Filed: August 1, 2017
    Date of Patent: September 10, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul Gerard Bulger, Birgit Kosjek, Nelo Rivera
  • HYDROXY ISOXAZOLE COMPOUNDS USEFUL AS GPR120 AGONISTS
    Publication number: 20190269679
    Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: December 11, 2017
    Publication date: September 5, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: John S. Debenham, Jason M. Cox, Ping Lan, Zhongxiang Sun, Zhe Feng, Chunrui Sun, Michael W. Seganish, Zhong Lai, Cheng Zhu, Thomas Bara, Murali Rajagopalan, Qun Dang, Hyunjin M. Kim, Bin Hu, Jinglai Hao
  • TREATING CANCER WITH A COMBINATION OF A PD-1 ANTAGONIST AND AN IL-27 ANTAGONIST
    Publication number: 20190270802
    Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and an antagonist of IL-27, and the use of the combination therapies for the treatment of cancer. In certain embodiments, the PD-1 antagonist is an anti-human PD-1 antibody, or antigen binding fragment thereof. In further embodiments, the anti-PD-1 antibody is pembrolizumab. In certain embodiments the antagonist of IL-27 is an anti-IL-27 antibody, or antigen binding fragment thereof, an anti-p28 antibody, or antigen binding fragment thereof, or an anti-EBI-3 antibody, or antigen binding fragment thereof. Also provided are medicaments, compositions, and kits comprising a PD-1 antagonist and an IL-27 antagonist for use in treating cancer.
    Type: Application
    Filed: October 19, 2017
    Publication date: September 5, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Nataliya Tovbis Shifrin, Rene de Waal Malefyt
  • Manually-Actuated Injection Device for High-Viscosity Drugs
    Publication number: 20190269857
    Abstract: A manually actuated drug-injecting device is configured such that the grip strength of the entire hand (i.e., majority of fingers closing toward the palm or heel of the hand) is employed to discharge medication through a hypodermic needle and into a patient's body. The device is well suited for delivering medications with high viscosity and/or by patients (e.g., elderly patients) with reduced finger strength and dexterity. The device includes a grip member, a push member (which causes the medication to be injected), and a force-transfer mechanism that couples the grip member to the push member. Suitably, the device is configured to be held transverse to the palm of the medication-administering hand, with a discharge port located by the outer, blade edge of the administering hand, when the device is being gripped to administer medication.
    Type: Application
    Filed: November 20, 2017
    Publication date: September 5, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Peter A. BASILE, Henry J. MACK, Jr., Oliver SHA, Steven G. MIGGELS
  • Tricyclic compounds as inhibitors of mutant IDH enzymes
    Patent number: 10399972
    Abstract: The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes 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 cancers.
    Type: Grant
    Filed: October 25, 2016
    Date of Patent: September 3, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: David J. Witter, Tesfaye Biftu, Purakkattle Biju, Stephane L. Bogen, Qingmei Hong, Chunhui Huang, Xianhai Huang, Bing Li, Min K. Park, David L. Sloman
  • Anti-GITR antibodies
    Patent number: 10400040
    Abstract: Antibodies to human GITR are provided, as well as uses thereof, e.g., in treatment of proliferative and immune disorders.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: September 3, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xiao Min Schebye, Grigori P. Ermakov, Douglas J. Hodges, Leonard G. Presta
  • 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
  • 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
  • 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
  • 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
  • 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