Patents Assigned to Merck Sharp
  • Ethyldiamine orexin receptor antagonists
    Patent number: 10011595
    Abstract: The present invention is directed to ethyldiamne compounds which are antagonists of orexin receptors. Such compounds are of the general structural formula I: 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 pharmaceutical 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: Grant
    Filed: December 14, 2015
    Date of Patent: July 3, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Scott D. Kuduk, Nigel Liverton, Gang Zhou
  • Combination therapies for cancer
    Patent number: 10010608
    Abstract: A novel combination comprising a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and a PD-1 antagonist; pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf and/or immune modulation through PD-1 is beneficial, e.g., cancer.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: July 3, 2018
    Assignees: MERCK SHARP & DOHME CORP., NOVARTIS AG
    Inventors: Axel Hoos, Keith W. Orford, Patrick Chun, Venkataraman Sriram, Elaine M. Pinheiro, Scot W. Ebbinghaus
  • Factor XIa inhibitors
    Patent number: 10011585
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Grant
    Filed: July 23, 2015
    Date of Patent: July 3, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Weiguo Liu, Scott D Edmondson, Zhuyan Guo, Alan Hruza, Sung-Sau So, Wanying Sun, Amjad Ali, Rongze Kuang, Ying-Duo Gao, Anthony K Ogawa
  • PROCESS FOR PREPARING SUBSTITUTED TETRACYCLIC HETEROCYCLE COMPOUNDS
    Publication number: 20180179223
    Abstract: The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.
    Type: Application
    Filed: June 3, 2016
    Publication date: June 28, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Jingjun Yin, Tetsuji Itoh, Jianguo Yin, Bangping Xiang, Kevin R. Campos, Alexei Kalinin, Zhuqing Liu, Melodie Deniz Christensen, Kevin M. Belyk, Richard J. Varsolona, Andrew Brunskill
  • Backstop for a Syringe
    Publication number: 20180177949
    Abstract: A backstop for a syringe can include a base having a first surface and an opposing second surface. A skirt can extend outwardly from the second surface of the base. An opening can extend through the base. The opening can be surrounded by the skirt. A first extension can extend generally perpendicularly from the second surface at an outer periphery of the base. A second extension can extend generally perpendicularly from the second surface at the outer periphery of the base. The second extension can be diametrically opposed to the first extension.
    Type: Application
    Filed: June 20, 2016
    Publication date: June 28, 2018
    Applicant: Merck Sharp & Dohme B.V.
    Inventors: Jacobus A. de Waal Malefijt, Dennis Broeke, Sander H. W. de Jong
  • Factor XIa Inhibitors
    Publication number: 20180179180
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Application
    Filed: October 20, 2017
    Publication date: June 28, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ning Shao, Scott D. Edmondson, Santhosh Neelamkavil, Zhuyan Guo, Eric Mertz, Yi Zang, Jiafang He
  • ANTIVIRAL ALIPHATIC ESTER PRODRUGS OF TENOFOVIR
    Publication number: 20180179208
    Abstract: Compounds of 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.
    Type: Application
    Filed: December 20, 2017
    Publication date: June 28, 2018
    Applicants: Merck Sharp & Dohme Corp., Idenix Pharmaceuticals LLC
    Inventors: Jean-Laurent Paparin, Izzat Raheem, Houcine Rahali, Daniel Da Costa, David Dukhan
  • Prodrugs of HIV reverse transcriptase inhibitors
    Patent number: 10004740
    Abstract: Compounds of Formula I are described: wherein R1 and R2 are defined herein. The compounds of Formula I are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV, and the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: June 26, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Jeffrey F. Fritzen, Jaume Balsells, Mehul Patel
  • SYNTHESIS OF CEPHALOSPORIN COMPOUNDS
    Publication number: 20180170949
    Abstract: Described herein are methods for the manufacture of ceftolozane and related compounds, as well as compositions comprising the same.
    Type: Application
    Filed: December 18, 2015
    Publication date: June 21, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Kristos Adrian MOSHOS, Valdas JURKAUSKAS, Giovanni FOGLIATO, Manuel SCANU, Michele BENOTTI
  • CEFTOLOZANE-TAZOBACTAM PHARMACEUTICAL COMPOSITIONS
    Publication number: 20180169106
    Abstract: Pharmaceutical compositions are provided in unit dosage forms comprising ceftolozane and tazobactam in separate unit dosage form containers, ceftolozane prepared in the absence of tazobactam, tazobactam prepared in the absence of ceftolozane, and/or compositions where ceftolozane and tazobactam are first combined within a unit dosage form container.
    Type: Application
    Filed: February 13, 2018
    Publication date: June 21, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph TERRACCIANO, Nicole Miller DAMOUR, Chun JIANG, Giovanni FOGLIATO, Giuseppe Alessandro DONADELLI, DARIO RESEMINI
  • COMBINATION OF A PD-1 ANTAGONIST AND CPG-C TYPE OLIGONUCLEOTIDE FOR TREATING CANCER
    Publication number: 20180169229
    Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a Toll-like receptor 9 (TLR9) agonist that is a CpG-C type oligonucleotide, and the use of the combination therapies for the treatment of cancer.
    Type: Application
    Filed: May 26, 2016
    Publication date: June 21, 2018
    Applicants: MERCK SHARP & DOHME CORP., DYNAVAX TECHNOLOGIES CORPORATION
    Inventors: Ying YU, Andrew Evan DENKER, Svetlana SADEKOVA, Uyen Truong PHAN, Robert A. KASTELEIN, David Ross KAUFMAN, Robert L. COFFMAN, Cristiana GUIDUCCI, Robert S. JANSSEN
  • Inhibitors of HIF prolyl hydroxylase
    Patent number: 10000501
    Abstract: The present invention concerns a compound of formula I or a pharmaceutically acceptable salt thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
    Type: Grant
    Filed: September 23, 2015
    Date of Patent: June 19, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiaqiang Cai, Vincent Colandrea, Alejandro Crespo, John Debenham, Xiaoxing Du, Deodialsingh Guiadeen, Ping Liu, Rongqiang Liu, Christina B. Madsen-Duggan, Joshua G. McCoy, Weiguo Quan, Christopher Sinz, Liping Wang
  • Salt forms of ceftolozane
    Patent number: 10000510
    Abstract: This disclosure relates to salt forms of ceftolozane, processes for making these salt forms, and compositions comprising the same. Also disclosed are stabilized compositions of ceftolozane. Provided herein are salt forms of ceftolozane, processes for making these salt forms and compositions comprising the same. The salt forms provided herein include ceftolozane bromide, ceftolozane edisylate, ceftolozane mesylate, ceftolozane chloride, ceftolozane sulfate, ceftolozane maleate, ceftolozane phosphate, and ceftolozane ketoglutarate.
    Type: Grant
    Filed: August 17, 2015
    Date of Patent: June 19, 2018
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Jian-Qiao Gu, Valdas Jurkauskas, Carlos Lopez, Kristos Adrian Moshos, Pradip M. Pathare, Sudhakar Garad, You Seok Hwang
  • Antidiabetic tricyclic compounds
    Patent number: 10000454
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: May 19, 2015
    Date of Patent: June 19, 2018
    Assignee: Merck Sharp & Dohme
    Inventors: Tesfaye Biftu, Purakkattle Biju, Timothy A. Blizzard, Zhengxia Chen, Matthew J. Clements, Mingxiang Cui, Jessica L. Frie, William K. Hagmann, Bin Hu, Hubert Josien, Anilkumar G. Nair, Christopher W. Plummer, Cheng Zhu
  • Inhibitors of the renal outer medullary potassim channel
    Patent number: 10000484
    Abstract: The present invention provides compounds of Formula (I) (Formula (I)) including 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 chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: June 19, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Barbara Pio, Yan Guo, Fa-Xiang Ding, Shuzhi Dong, Shawn P. Walsh, Jinlong Jiang, Dooseop Kim
  • Methyl diazepane orexin receptor antagonists
    Patent number: 10000499
    Abstract: The present invention is directed to methyl diazepane compounds which are antagonists 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: Grant
    Filed: November 20, 2015
    Date of Patent: June 19, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Thomas S. Reger, Jason W. Skudlarek
  • CELLULAR EXPRESSION MODEL OF TAU AGGREGATION
    Publication number: 20180164288
    Abstract: The invention relates to novel methods and compositions for detecting tau hyperphosphorylation and aggregation.
    Type: Application
    Filed: December 14, 2016
    Publication date: June 14, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joel Schachter, John Majercak, Mali Liu Cosden
  • COMBINATION OF AN ANTI-IL-10 ANTIBODY AND A CPG-C TYPE OLIGONUCLEOTIDE FOR TREATING CANCER
    Publication number: 20180161427
    Abstract: The present disclosure describes combination therapies comprising an anti-IL-10 antibody or antigen-binding fragment thereof and a CpG-C type oligonucleotide, and the use of the combination therapies for the treatment of cancer.
    Type: Application
    Filed: May 26, 2016
    Publication date: June 14, 2018
    Applicants: MERCK SHARP & DOHME CORP., DYNAVAX TECHNOLOGIES CORPORATION
    Inventors: Ying YU, Elliot Keith CHARTASH, Svetlana SADEKOVA, Uyen Truong PHAN, Robert A. KASTELEIN, Robert L. COFFMAN, Cristiana GUIDUCCI, Robert S. JANSSEN
  • SUBSTITUTED PYRAZOLO/IMIDAZOLO BICYCLIC COMPOUNDS AS PDE2 INHIBITORS
    Publication number: 20180162874
    Abstract: The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: June 20, 2016
    Publication date: June 14, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Gregori J. Morriello, Michael P. Dwyer, Lehua Chang, Yili Chen, Ming Wang, Ashley Forster, Richard Berger, Kausik k Nanda, Jaime L Bunda, William D Shipe
  • Anti-pembrolizumab antibodies
    Patent number: 9995753
    Abstract: The present invention provides antibodies and antigen-binding fragments thereof that bind to the antibody pembrolizumab (pembrolizumab). These antibodies are useful, for example, for use as positive controls in assays for detecting the presence of anti-drug antibodies in a sample, e.g., the blood of a patient who has been administered pembrolizumab.
    Type: Grant
    Filed: September 23, 2016
    Date of Patent: June 12, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: LiNa Loo, Shuangping Shi