Patents Assigned to Merck Sharp
  • Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
    Patent number: 9598405
    Abstract: The invention provides certain thiazole-substituted aminopyridine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Cy, and the subscript 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: December 19, 2013
    Date of Patent: March 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Kaleen Konrad Childers, Maria Emilia Di Francesco, John Michael Ellis, Andrew M. Haidle, Yuan Liu, Alan B. Northrup, Brendan O'Boyle, Ryan D. Otte, Michael H. Reutershan, Dilrukshi Vitharana, Hyun Chong Woo
  • PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS
    Publication number: 20170073354
    Abstract: The present invention is directed to compounds of Formula I 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: March 6, 2015
    Publication date: March 16, 2017
    Applicants: Merck Sharp & Dohme Corp., MSD R&D (China) Co., Ltd.
    Inventors: Peter D. Williams, John A. McCauley, Christopher J. Bungard, David Jonathan Bennett, Sherman T. Waddell, Gregori J. Morriello, Lehua Chang, Michael P. Dwyer, M. Katharine Holloway, Alejandro Crespo, Xin-Jie Chu, Catherine Wiscount, H. Marie Loughran, Jesse J. Manikowski, Jurgen Schulz, Kartik M. Keertikar, Bin Hu, Bin Zhong, Tao Ji
  • 2-PYRAZINE CARBOXAMIDES AS SPLEEN TYROSINE KINASE INHIBITORS
    Publication number: 20170071935
    Abstract: The invention provides certain pyrazine-2-carboxamide compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, and X 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: Application
    Filed: March 9, 2015
    Publication date: March 16, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brandon Cash, John Michael Ellis, Matthew L. Maddess, Alan B. Northrup, Ryan D. Otte, Binyuan Sun
  • TRIAZOLO-PYRAZINYL DERIVATIVES USEFUL AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS
    Publication number: 20170073355
    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 compositions which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 19, 2015
    Publication date: March 16, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Raphaelle Berger, Guizhen Dong, Subharekha Raghavan, Zhiqiang Yang
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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