Patents Assigned to Merck Sharp
  • Alpha-7 nicotinic acetylcholine receptor modulators and uses thereof
    Patent number: 9994518
    Abstract: Disclosed are compounds of Formula (IVA), or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof: Formula (IVA), wherein “RIa”, “RIb”, “RIc”, “RId”, “RIe”, are defined herein above, which compounds are believed suitable for use in positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7 nAChR) receptors, for example, those found in the cerebral cortex and the hippocampus. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Alzheimer's disease (AD), schizophrenia, and Parkinson's disease (PD), or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.
    Type: Grant
    Filed: June 11, 2015
    Date of Patent: June 12, 2018
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Kenneth Leavitt, Brendan Crowley, Ian M. Bell, Andrew Harvey, Thomas Avery, Dharam Paul, Justin Ripper, Belinda Huff, Rajinder Singh, Laurent Schaeffer, Christophe Joseph, Christophe Morice, Bruno Giethlen, Patrick Bazzini, Aurelie Fromeyer
  • Bridged diazepane orexin receptor antagonists
    Patent number: 9994570
    Abstract: The present invention is directed to bridged 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 12, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Thomas S. Reger, Anthony J. Roecker
  • HIV protease inhibitors
    Patent number: 9994587
    Abstract: The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV 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. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: March 2, 2015
    Date of Patent: June 12, 2018
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: John A. McCauley, David Jonathan Bennett, Christopher J. Bungard, Thomas J. Greshock, M. Katharine Holloway, Peter D. Williams, Christian Beaulieu, Sheldon Crane, Stephanie Lessard, Daniel Mckay, Carmela Molinaro, Oscar Miguel Moradei, Vijayasaradhi Sivalenka, Vouy Linh Truong, Satyanarayana Tummanapalli
  • SUSTAINED RELEASE FORMULATION AND TABLETS PREPARED THEREFROM
    Publication number: 20180154000
    Abstract: Disclosed are formulations and tablets made therefrom comprising the compound of Formula IA or Formula IB which have sustained-release properties, and the dispersion containing the compounds of Formula IA or IB which facilitates such sustained release: Formula IA, Formula IB.
    Type: Application
    Filed: June 21, 2016
    Publication date: June 7, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Pranav Gupta, David Monteith
  • TETRACYCLIC HETEROCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS
    Publication number: 20180155365
    Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula (I). and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: November 30, 2017
    Publication date: June 7, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Thomas H. Graham, Tao Yu, Yonglian Zhang, John A. McCauley
  • 5,5-bicyclic oxazole orexin receptor antagonists
    Patent number: 9987255
    Abstract: The present invention is directed to 5,5-bicyclic oxazole 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: December 14, 2015
    Date of Patent: June 5, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Nigel Liverton, Thomas S. Reger, Jason W. Skudlarek
  • ERK inhibitors
    Patent number: 9988397
    Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting ERK2 in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of Formula (I). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I).
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: June 5, 2018
    Assignees: MERCK SHARP & DOHME CORP., MSD R&D (CHINA) CO., LTD
    Inventors: Phieng Siliphaivanh, David L. Sloman, David Witter, Umar Faruk Mansoor, Joseph Kozlowski, Ziping Liu, Jianmin Fu, Zhilong Wan, Wei Liu, Yimin Qian, Xianhai Huang
  • Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate
    Patent number: 9988406
    Abstract: A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: June 5, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
  • DIHYDROPYRAZOLOPYRIMIDINONE COMPOUNDS AS PDE2 INHIBITORS
    Publication number: 20180148453
    Abstract: The present invention is directed to dihydropyrazolopyrimidinone 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: May 31, 2016
    Publication date: May 31, 2018
    Applicants: Merck Sharp & Dohme Corp., MSD R & D (China) Co. LTD.
    Inventors: Dong-Ming Shen, Michael P. Dwyer, Christopher J. Sinz, Deping Wang, Shawn J. Stachel, Daniel V. Paone, Ashley Forster, Richard Berger, Yili Chen, Yimin Qian, Shimin Xu, Chunmei Hu
  • BLOOD-BASED BIOMARKERS OF TUMOR SENSITIVITY TO PD-1 ANTAGONISTS
    Publication number: 20180148790
    Abstract: The present disclosure describes baseline and on treatment blood-based gene signature biomarkers that are predictive of tumor sensitivity to therapy with a PD-1 antagonist. The on-treatment biomarkers comprise a PD-L1 gene signature or an interferon gamma gene signature and the baseline gene signature biomarker comprises genes associated with the oxidative phosphorylation pathway. The disclosure also provides methods and kits for testing tumor samples for these biomarkers, as well as methods for treating subjects with a PD-1 antagonist based on the test results.
    Type: Application
    Filed: April 12, 2016
    Publication date: May 31, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mark Ayers, Jared Lunceford, Andrey Loboda, Michael Nebozhyn, Terrill K. McClanahan, Heather Hirsch
  • IMIDAZO-PYRAZINYL DERIVATIVES USEFUL AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS
    Publication number: 20180147208
    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 pharmaceutically acceptable salt thereofs, 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 pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: May 23, 2016
    Publication date: May 31, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joie GARFUNKLE, Olga ORNOSKI, Dann L. PARKER, JR., Subharekha RAGHAVAN, Libo XU
  • Bicyclic ureas and thiadiazolidine-1, 1-dioxides as CETP inhibitors
    Patent number: 9981970
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein X is —C(?O) or —S(O)2—, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: July 28, 2014
    Date of Patent: May 29, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jian Liu, Pengcheng Patrick Shao, Arto K. Krikorian, Petr Vachal
  • Imidazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug
    Patent number: 9981969
    Abstract: The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R1 and R2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.
    Type: Grant
    Filed: June 2, 2014
    Date of Patent: May 29, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Milana Maletic, Yunfu Luo, Zhiqi Qi, Chunsing Li, Tingting Yu, Richard Soll
  • AZACARBAZOLE BTK INHIBITORS
    Publication number: 20180141962
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, wherein CH, R1, R1a, R1b, R2, R3, and the subscripts m1, m2, p, q, and t are as set forth herein. The present invention also provides pharmaceutical compositions comprising these compounds and their use in therapy. In Cparticular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated dis orders.
    Type: Application
    Filed: April 4, 2016
    Publication date: May 24, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: JIAN LIU, JOSEPH KOZLOWSKI, RONALD KIM, XIAOLEI GAO, SOBHANA BABU BOGA, YOUNONG YU, HAO WU, SHILAN LIU, CHUNDAO YANG
  • BICYCLIC HETEROCYCLIC COMPOUNDS AS PDE2 INHIBITORS
    Publication number: 20180141952
    Abstract: The present invention is directed to dihydropyrazolopyrimidinone compounds of formulas (I) and (II) 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 27, 2016
    Publication date: May 24, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Michael P. Dwyer, Christopher J. Sinz, Jonathan E. Wilson, Daniel V. Paone, Yili Chen, Shimin Xu
  • Purine Inhibitors of Human Phosphatidylinositol 3-Kinase Delta
    Publication number: 20180141947
    Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
    Type: Application
    Filed: June 24, 2016
    Publication date: May 24, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Meredith Ann McGowan, Hua Zhou, Jason D. Katz, Lihu Yang, Joey L. Methot, Kathryn Ann Lipford, Shimin Xu, Ning Fu, Guoquan Xu, Deqian Bian, Jianmin Fu, Yabin Li, Kin Chiu Fong
  • SURFACE ANCHORED LIGHT CHAIN BAIT ANTIBODY DISPLAY SYSTEM
    Publication number: 20180142233
    Abstract: The present invention provides, in part, an antibody display system that simultaneously uses a secretion and a display mode. Embodiments of the invention provide a system in which a bait complexed with a monovalent antibody fragment can be captured prior to secretion in a host cell by virtue of surface displaying an antibody light chain and utilizing the covalent interaction of this light chain with the heavy chain of an antibody molecule that is co-expressed in the same host. Polypeptides, polynucleotides and host cells useful for making the antibody display system are also provided along with methods of using the system for identifying antibodies that bind specifically to an antigen of interest.
    Type: Application
    Filed: January 10, 2018
    Publication date: May 24, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Hussam Hisham Shaheen, Dongxing Zha
  • Factor XIa inhibitors
    Patent number: 9975874
    Abstract: The present invention provides a compound of Formula (I) (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: Grant
    Filed: July 23, 2015
    Date of Patent: May 22, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Eric Mertz, Scott D. Edmondson, Alan Hruza, Jiafang He, Sung-Sau So, Amjad Ali, Ying-Duo Gao
  • Aryl linked imidazole and triazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug
    Patent number: 9975888
    Abstract: The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: May 22, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Milana M. Maletic, Yunfu Luo, Zhiqi Qi, Chun Sing Li, Tingting Yu
  • Medical injector pen
    Patent number: D819199
    Type: Grant
    Filed: November 11, 2016
    Date of Patent: May 29, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Angela M. Amend Kwasnik, Benjamin R. Bartfield, Peter Basile, Jeffrey C. Givand, Philip G. Green, Sharad Gupta, Christin L. O'Neill, Steven Carl Persak, Robert Stianchi, Ari Tao Adler, Florian Altmann, Thomas Junk, Florian Kössler, Martin Meier, Scott R. Mackie, Pernilla Danielsson