Patents Assigned to Merck Sharp & Dohme
  • Formulations for Cathepsin K Inhibitors with Vitamin D
    Publication number: 20160166529
    Abstract: The instant invention relates to pharmaceutical compositions comprising cathespin K inhibitors and Vitamin D.
    Type: Application
    Filed: July 7, 2014
    Publication date: June 16, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Majid MAHJOUR, Decheng MA, Christina Marie BACCI, Julianne Margaret FARABAUGH, Justin MOSER, Lixia CAI, Stephen L. CONWAY
  • SUBSTITUTED AMIDOPYRAZOLE INHIBITORS OF INTERLEUKIN RECEPTOR-ASSOCIATED KINASES (IRAK-4)
    Publication number: 20160166576
    Abstract: This invention relates to amidopyrazole compounds that are inhibitors of Interieukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment of cellular proliferative diseases. Speifically (5-methylpyridin-2-yl)-1 H-pyrazol-5-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamide derivatives are disclosed for use in the method of treating inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease and cancer.
    Type: Application
    Filed: July 7, 2014
    Publication date: June 16, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Jongwon LIM, Michael D. ALTMAN
  • C5, C6 oxacyclic-fused thiazine dioxide compounds as BACE inhibitors, compositions, and their use
    Patent number: 9365589
    Abstract: In its many embodiments, the present invention provides certain C2-ring-substituted iminothiazine compounds, including compounds Formula (I): (structurally represented) or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and, wherein R1, R2, R3, R4, X, 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: June 14, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, David Earl Kaelin, Jr., Jack D. Scott, Wen-Lian Wu, Duane A. Burnett
  • Prolylcarboxypeptidase inhibitors
    Patent number: 9365539
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: June 14, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jeffrey J. Hale, Jinlong Jiang, Dong-Ming Shen, Zhi-Cai Shi, Min Shu, Zhicai Wu, Cangming Yang
  • Soluble guanylate cyclase activators
    Patent number: 9365574
    Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: June 14, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Subharekha Raghavan, John E. Stelmach, Cameron J. Smith, Hong Li, Alan Whitehead, Sherman T. Waddell, Yi-Heng Chen, Shouwu Miao, Olga A. Ornoski, Joie Garfunkle, Xibin Liao, Jiang Chang, Xiaoqing Han, Jian Guo, Jonathan A. Groeper, Linda L. Brockunier, Keith Rosauer, Emma R. Parmee
  • Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
    Patent number: 9364482
    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: June 19, 2014
    Date of Patent: June 14, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xing Dai, Hong Liu, Anandan Palani, Shuwen He, Ravi Nargund, Dong Xiao, Nicolas Zorn, Qun Dang, Casey C. McComas, Xuanjia Peng, Peng Li, Richard Soll
  • Method of treatment of lymphoma with pegylated IL-10
    Patent number: 9364517
    Abstract: Provided are methods of treatment for tumors. In particular, methods are provided for use of a chemically modified IL-10 to treat tumors.
    Type: Grant
    Filed: September 12, 2014
    Date of Patent: June 14, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Martin Oft, Catherine Sheppard, John Brian Mumm, Lingling Wu
  • 1,3 substituted azetidine PDE10 inhibitors
    Patent number: 9365562
    Abstract: The present invention is directed to substituted azetidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). 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: October 1, 2012
    Date of Patent: June 14, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, Douglas C. Beshore, June J. Kim, Scott D. Kuduk, Carol A. McVean, Thomas Reger, Justin T. Sheen
  • Surface, anchored Fc-bait antibody display system
    Patent number: 9365846
    Abstract: The present invention provides, in part, an antibody display system that simultaneously uses a secretion and a display mode. A bait complexed with a monovalent antibody fragment can be expressed on the surface of the host cell wherein the fragment may be assayed for antigen binding while full antibody is simultaneously secreted from the host cell. Methods of using the system for identifying antibodies that bind specifically to an antigen of interest are also provided. Polypeptides, polynucleotides and host cells useful for making the antibody display system are also provided along with methods of use thereof.
    Type: Grant
    Filed: November 29, 2011
    Date of Patent: June 14, 2016
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Hussam Hisham Shaheen, Dongxing Zha
  • Quinoline Carboxamide and Quinoline Carbonitrile Derivatives as mGluR2-Negative Allosteric Modulators, Compositions, and Their Use
    Publication number: 20160159744
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive 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: February 18, 2016
    Publication date: June 9, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
  • Quinoline Carboxamide and Quinoline Carbonitrile Derivatives as mGluR2-Negative Allosteric Modulators, Compositions, and Their Use
    Publication number: 20160158217
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive 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: February 18, 2016
    Publication date: June 9, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
  • CO-CRYSTAL OF THE PAR-1 RECEPTOR ANTAGONISTS VORAPAXAR AND ASPRIN
    Publication number: 20160159779
    Abstract: This invention relates to a co-crystal of vorapaxar and aspirin. The inventive co-crystal antagonizes the PAR-1 receptor. This invention also provides for pharmaceutical compositions comprising the inventive co-crystal as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by antagonizing the PAR-1 receptor.
    Type: Application
    Filed: July 17, 2014
    Publication date: June 9, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott Trzaska, Alicia V. Duran-Capece, Matthew Lamm
  • PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS
    Publication number: 20160159752
    Abstract: The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
    Type: Application
    Filed: July 29, 2014
    Publication date: June 9, 2016
    Applicants: Merck Sharp & Dohme Corp., MSD R&D (CHINA) CO., LTD.
    Inventors: Peter D. Williams, John A. McCauley, David Jonathan Bennett, Christopher J. Bungard, Lehua Chang, Michael P. Dwyer, M. Katharine Holloway, Kartik M. Keertikar, H. Marie Loughran, Jessie J. Manikowski, Gregori J. Morriello, Dong-Ming Shen, Edward C. Sherer, Jurgen Schultz, Sherman T. Waddell, Catherine M. Wiscount, Nicolas Zorn, Xin-Jie Chu, Satyanarayana Tummanapalli, Vijayasaradhi Sivalenka, Bin Hu, Tao Ji, Bin Zhong
  • Posaconazole intravenous solution formulations stabilized by substituted ?-cyclodextrin
    Patent number: 9358297
    Abstract: The present invention relates to aqueous solutions useful as pharmaceutical compositions of posaconazole for intravenous administration. These compositions include a solubilizing agent, such as a modified ?-cyclodextrin in an acidified solution, which can also include a chelating agent such as disodium edetate (EDTA). In clinical trials, a 200 mg posaconazole dose of the selected composition was found to achieve acceptable pharmacokinetic properties.
    Type: Grant
    Filed: March 25, 2015
    Date of Patent: June 7, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Susan K. Heimbecher, David Monteith, James D. Pipkin
  • Cyclopropyl imidazopyridine PDE10 inhibitors
    Patent number: 9359348
    Abstract: The present invention is directed to substituted cyclopropyl imidazopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). 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: November 11, 2013
    Date of Patent: June 7, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Thomas S. Reger
  • Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
    Patent number: 9359339
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: August 5, 2014
    Date of Patent: June 7, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Fengqi Zhang, Emma R. Parmee, Sunita V. Dewnani
  • DENGUE VIRUS VACCINE COMPOSITIONS AND METHODS OF USE THEREOF
    Publication number: 20160151477
    Abstract: The present invention relates to dengue virus vaccine compositions comprising a first and a second dengue vaccine, wherein the first dengue vaccine is a live, attenuated dengue vaccine and the second dengue vaccine is a recombinant dengue subunit vaccine or an inactivated dengue vaccine; wherein the live attenuated dengue vaccine comprises at least one live, attenuated dengue virus or at least one live attenuated chimeric flavivirus. The dengue virus vaccine compositions of the invention may further comprise one or more adjuvants. In preferred embodiments of the invention, the first and the second dengue vaccine are tetravalent. The invention also relates to methods of using the dengue virus vaccine compositions of the invention to treat or prevent dengue infection, or to prevent, ameliorate, or delay the onset or progression of the clinical manifestations thereof.
    Type: Application
    Filed: June 17, 2014
    Publication date: June 2, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Andrew Bett, Beth-Ann Griswold Coller, Govindarajan Dhanasekaran, Ramesh V. Chintala
  • Substituted phenyl-Spleen Tyrosine Kinase (Syk) inhibitors
    Patent number: 9353066
    Abstract: The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: May 31, 2016
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Andrew M. Haidle, Jason Burch, Daniel Guay, Jacques Yves Gauthier, Joel Robichaud, Jean Francois Fournier, John Michael Ellis, Matthew Christopher, Solomon D. Kattar, Graham F. Smith, Alan B. Northrup
  • Cyclic amine substituted heterocyclic CETP inhibitors
    Patent number: 9353101
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: May 31, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John J. Acton, III, Feng Ye, Petr Vachal, Deyou Sha, James F. Dropinski, Lin Chu, Debra Ondeyka, Alexander J. Kim, Vincent J. Colandrea, Yi Zang, Fengqi Zhang, Guizhen Dong
  • Indazole derivatives useful as ERK inhibitors
    Patent number: 9351965
    Abstract: The present invention provides a compound of the Formula I, or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, m and are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions that comprise the above compounds, and methods of treating cancer using the same.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: May 31, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gerald W. Shipps, Jr., Xiaohua Huang, Yongqi Deng, Liang Zhu, Alan B. Cooper, Binyuan Sun, Abdelghani Achab, Sie-Mun Lo