Patents Assigned to Merck Sharp & Dohme
  • Oxyntomodulin analogs
    Patent number: 9593155
    Abstract: Peptide analogs of oxyntomodulin (OXM, glucagon-37), 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 act as a dual GLP-1/glucagon receptor (GCGR) agonist are described. The peptide analogs are useful for treatment of metabolic disorders such as diabetes and obesity.
    Type: Grant
    Filed: April 14, 2015
    Date of Patent: March 14, 2017
    Assignees: MERCK SHARP & DOHME CORP., MSD ITALIA S.R.L., INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Paul E. Carrington, George J. Eiermann, Donald J. Marsh, Joseph M. Metzger, Alessandro Pocai, Ranabir Sinha Roy, Elisabetta Bianchi, Paolo Ingallinella, Antonello Pessi, Alessia Santoprete, Elena Capito, Richard Dimarchi, Brian Ward
  • ?7 nicotinic acetylcholine receptor modulators and uses thereof-III
    Patent number: 9593096
    Abstract: The present invention relates to chemical compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7 nAChR).
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: March 14, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Andrew Harvey, Belinda Huff, Rajinder Singh, Nathan Kuchel
  • AMIDATION PROCESS
    Publication number: 20170066715
    Abstract: This invention describes an amidation process whereby perfluorinated amino acids can be activated and treated with an amine in the presence of a coupling agent and a pyridine derivative to yield amides, without loss of optical purity.
    Type: Application
    Filed: November 21, 2016
    Publication date: March 9, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Guy Humphrey, Kelvin Yong
  • SOLID PRODRUG FORMS OF 2'-CHLORO-2'-METHYL URIDINE FOR HCV
    Publication number: 20170066795
    Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
    Type: Application
    Filed: March 5, 2015
    Publication date: March 9, 2017
    Applicants: IDENIX PHARMACEUTICALS LLC, Merck Sharp & Dohme Corp.
    Inventors: John Zoltan Sulliva-Bolyai, Benjamin Alexander Mayes, Douglas Lytle Mayers, Xiao-Jian Zhou, Adel M. Moussa, Alistair James Stewart, Sindhura Ganga, Clinton Scott Shultz, Alfred Lee
  • Inhibitors of IRAK4 activity
    Patent number: 9586948
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: March 7, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: W. Michael Seganish, Jennifer Hanisak, Guoqing Li, Rui Zhang, Haiqun Tang
  • Bicycloamine-substituted-N-benzenesulfonamide compounds with selective activity in voltage-gated sodium channels
    Patent number: 9586968
    Abstract: Disclosed are compounds of Formula A-a, or a salt thereof: Where “B1” and “R1” through “R5” are as defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-a or their salts, and methods of treating neuropathic pain disorders using the same.
    Type: Grant
    Filed: November 24, 2014
    Date of Patent: March 7, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark E. Layton, Anthony J. Roecker, Melissa Egbertson, Kristen L. G. Jones, Dansu Li, Xiu Wang, Xuanjia Peng
  • 2-pyridyloxy-4-methyl orexin receptor antagonists
    Patent number: 9586934
    Abstract: The present invention is directed to 2-pyridyloxy-4-methyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-methyl 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 pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: March 7, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • 2-pyridyloxy-3-ester-4-nitrile orexin receptor antagonists
    Patent number: 9586950
    Abstract: The present invention is directed to 2-pyridyloxy-3-ester-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-ester-4-nitrile compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 14, 2013
    Date of Patent: March 7, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Immobilized transaminases and process for making and using immobilized transaminase
    Patent number: 9587229
    Abstract: The invention is directed to immobilized transaminases and methods of making and using them.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: March 7, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew D. Truppo, Jacob M. Janey, Gregory Hughes
  • Triazolyl derivatives as Syk inhibitors
    Patent number: 9586931
    Abstract: Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: March 7, 2017
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Michelle R. Machacek, Eric T. Romeo, Solomon D. Kattar, Matthew Christopher, Michael D. Altman, Alan B. Northrup, John Michael Ellis, Brendan O'Boyle, Anthony Donofrio, Jonathan Grimm, Michael H. Reutershan, Kaleen Konrad Childers, Ryan D. Otte, Brandon Cash, Yves Ducharme, Andrew M. Haidle, Kerrie Spencer, Dilrukshi Vitharana, Lingyun Wu, Li Zhang, Peng Zhang, Christian Beaulieu, Daniel Guay
  • METHOD FOR TREATING CANCER
    Publication number: 20170056406
    Abstract: A method for the treatment of cancer by administering a therapeutically effective amount of a cyclin-dependent kinase (CDK) inhibitor with a therapeutically effective amount of a B cell chronic lymphocytic leukemia/lymphoma 2 inhibitor (“B Cell CLL/Lymphoma 2”, or “BCL-2”). Administration of the CDK inhibitor and BCL-2 inhibitor can be simultaneous, successive or separate.
    Type: Application
    Filed: February 23, 2015
    Publication date: March 2, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Peter Strack, Robert Booher
  • C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use
    Patent number: 9580396
    Abstract: In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: February 28, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Jack D. Scott, Jr., Andrew W. Stamford, Ulrich Iserloh, Santhosh Francis Neelamkavil, Pengcheng Patrick Shao, Jonathan E. Wilson
  • Regioselective N-2 arylation of indazoles
    Patent number: 9580407
    Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.
    Type: Grant
    Filed: December 3, 2013
    Date of Patent: February 28, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Cheol K. Chung, Mark E. Scott, Paul Gerard Bulger, Kevin Michael Belyk, John Limanto, Guy R. Humphrey
  • Method for preparation of aluminum hydroxyphosphate adjuvant
    Patent number: 9573811
    Abstract: The present invention relates to methods for preparing amorphous aluminum hydroxyphosphate. An aluminum salt and a phosphate solution are co-mixed at a constant ratio in the presence of a buffer. Preferably, an excess of the phosphate solution is used to act as a buffer. Due to the presence of a buffer, the pH is maintained constant during reaction (after initial rapid equilibration) without active adjustment. The methods are particularly applicable for the large scale manufacturing of aluminum phosphate adjuvant. Aluminum phosphate is used as an adjuvant in vaccine formulations, particularly those including a protein or saccharide antigen.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: February 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: David S. Thiriot, Patrick L. Ahl, Jayme Cannon, Gabriel M. Lobel
  • Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
    Patent number: 9573939
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: February 21, 2017
    Assignees: Merck Sharp & Dohme Corp., MSD Italia SRL
    Inventors: Casey C. McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Qun Dang
  • Inhibitors of the renal outer medullary potassium channel
    Patent number: 9573961
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: February 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Reynalda Keh DeJesus, Jessica L. Frie, Barbara Pio, Haifeng Tang, Shawn P. Walsh
  • Cathepsin cysteine protease inhibitors
    Patent number: 9573913
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Grant
    Filed: October 3, 2014
    Date of Patent: February 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn Stachel, Daniel V. Paone, Jing Li, Anthony Ginnetti, John Lim, Jianmin Fu, Shimin Xu
  • PHARMACEUTICAL SALTS OF AN OREXIN RECEPTOR ANTAGONIST
    Publication number: 20170044149
    Abstract: The invention is directed to pharmaceutically acceptable salts of suvorexant, which is an antagonist of orexin receptors. The pharmaceutically acceptable salts of suvorexant are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is further directed to pharmaceutical compositions comprising pharmaceutically acceptable salts of suvorexant.
    Type: Application
    Filed: April 16, 2015
    Publication date: February 16, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Michael MCNEVIN, Sachin LOHANI
  • CYCLIC DI-NUCLEOTIDE COMPOUNDS AS STING AGONISTS
    Publication number: 20170044206
    Abstract: A class of polycyclic compounds of general formula (I), of general formula (I?), or of general formula (I?), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.
    Type: Application
    Filed: August 11, 2016
    Publication date: February 16, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brian Michael Andresen, Wonsuk Chang, Matthew Lloyd Childers, Jared N. Cumming, Andrew Marc Haidle, Timothy J. Henderson, James P. Jewell, Rui Liang, Jongwon Lim, Hong Liu, Min Lu, Alan B. Northrup, Ryan D. Otte, Tony Siu, Benjamin Wesley Trotter, Quang T. Truong, Shawn P. Walsh, Kake Zhao
  • Autoinjector pen
    Patent number: D780909
    Type: Grant
    Filed: April 10, 2014
    Date of Patent: March 7, 2017
    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