Patents Assigned to Merck Sharp
  • ACYCLIC CYANOETHYLPYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
    Publication number: 20160272634
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: March 19, 2014
    Publication date: September 22, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher Dinsmore, Peter Fuller, David Guerin, Jason David Katz, Christopher F. Thompson, Danielle Falcone, Wei Deng, Luis Torres, Hongbo Zeng, Yunfeng Bai, Jianmin Fu, Norman Kong, Yumei Liu, Zhixiang Zheng, Mark E. Scott
  • N-(2-CYANO HETEROCYCLYL) PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
    Publication number: 20160272633
    Abstract: Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.
    Type: Application
    Filed: March 19, 2014
    Publication date: September 22, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher Dinsmore, Peter Fuller, David Guerin, Christopher F. Thompson, Qinglin Pu, Mark E. Scott, Jason David Katz, Ravi Kuruklasuriya, Joshua T. Close, Danielle Falcone, Jason Brubaker, Hongbo Zeng, Yunfeng Bai, Jianmin Fu, Norman Kong, Yumei Liu, Zhixiang Zheng
  • Iminothiadiazine dioxides containing a thioamide, amidine, or amide oxime group as BACE inhibitors, compositions, and their use
    Patent number: 9447085
    Abstract: In its many embodiments, the present invention provides certain C2-ring-substituted iminothiadiazine compounds, or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers. The novel compounds of the invention are 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 9, 2013
    Date of Patent: September 20, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Jack D. Scott, Tesfaye Biftu
  • BTK inhibitors
    Patent number: 9446130
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salts thereof. Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: September 20, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Jian Liu, Hao Wu, Shilan Liu, Chundao Yang, Shuling Zheng
  • Enolase peptide conjugate vaccines against
    Patent number: 9447403
    Abstract: The present invention relates to peptides of the enolase protein from Staphylococcus aureus as well as nucleic acid and nucleic acid sequence homologs encoding the peptides. The present invention also relates to a composition, particularly a S. aureus vaccine, comprising one or more of the enolase peptides described herein or a fragment, derivative or variant thereof capable of generating an immune response that induces a protective antibody response or opsonophagocytic activity of human neutrophils for S. aureus. The present invention also encompasses methods of treating and/or reducing the likelihood of a Staphylococcus infection by administering a composition of the invention.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: September 20, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tessie B. McNeely, Leslie Cope, Sharon Smith, Amita Joshi, Irene Pak, Arthur Fridman
  • Process for the preparation of an intermediate for an orexin receptor antagonist
    Patent number: 9441254
    Abstract: The present invention is directed to processes for preparing an intermediate for a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: September 13, 2016
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Fred Fleitz, Ian Mangion, Jingjun Yin
  • Compounds inhibiting leucine-rich repeat kinase enzyme activity
    Patent number: 9440952
    Abstract: The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: September 13, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Kallol Basu, Duane DeMong, Jack Scott, Hong Liu, Xing Dai, Joel M. Harris, Bernard Neustadt, Andrew Stamford, Marc Poirier, John A. McCauley, Thomas Greshock, Heather Stevenson, John Sanders, Jonathan Kern
  • THIOPHENE-SUBSTITUTED TETRACYCLIC COMPOUNDS AND METHODS OFUSE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20160257697
    Abstract: Thiophene-substituted tetracyclic compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein A, A?, R2, R3, R4 and R5 are as defined herein. The compositions comprising at least one thiophene-substituted tetracyclic compound, and methods of using the thiophene-substituted tetracyclic compounds for treating or preventing HCV infection in a patient are also provided.
    Type: Application
    Filed: December 31, 2013
    Publication date: September 8, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Ling Tong, Wensheng Yu, Joseph A. Kozlowski, Lei Chen, Oleg Selyutin, Seong Heon Kim, Michael Dwyer, Bin Hu, Bin Zhong, Dahai Wang, Jinglai Hao, Changmao Shen, Zhixin Lei, Weijun Wang
  • Inhibitors of the Renal Outer Medullary Potassium Channel
    Publication number: 20160257670
    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 chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Application
    Filed: October 27, 2014
    Publication date: September 8, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Haifeng Tang, Jessica Frie, Ronald Dale Ferguson, Zhiqiang Guo, Zhi-Cai Shi, Brian Cato, Qinghong Fu
  • Factor XIa Inhibitors
    Publication number: 20160257668
    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 6, 2014
    Publication date: September 8, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ning SHAO, Scott D. EDMONDSON, Santhosh NEELAMKAVIL, Zhuyan GUO, Eric MERTZ, Yi ZANG, Jiafang HE
  • PROCESS FOR PREPARING TETRACYCLIC HETEROCYCLE COMPOUNDS
    Publication number: 20160257698
    Abstract: The present invention is directed to a process for preparing Tetracyclic Heterocycle Compounds of formula (I): which are useful as HCV NS5A inhibitors. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Application
    Filed: October 24, 2014
    Publication date: September 8, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Ian Mangion, Cheng-yi Chen, Ingyu Jeon, Yonggang Chen, Hongmei Li, Hoa N. Nguyen, Peter E. Maligres, Artis Klapars, Ilia Zavialov, Nobuyoshi Yasuda
  • Substituted pyridine and pyrimidine derivatives and their use in treating viral infections
    Patent number: 9433621
    Abstract: The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: September 6, 2016
    Assignees: Merck Sharp & Dohme Corp., Southern Research Institute
    Inventors: Ashok Arasappan, F. George Njoroge, Cecil D. Kwong, Subramaniam Ananthan, Frank Bennett, Francisco Velazquez, Vinay M. Girijavallabhan, Yuhua Huang, Hollis S. Kezar, III, Joseph A. Maddry, Robert C. Reynolds, Abhijit Roychowdhury, Anita T. Fowler, John A. Secrist, III, Joseph A. Kozlowski, Bandarpalle B. Shankar, Ling Tong, Seong Heon Kim, Malcolm MacCoss, Srikanth Venkatraman, Vishal Verma
  • THERMOSTABLE RESPIRATORY SYNCTIAL VIRUS (RSV) VACCINE COMPOSITIONS
    Publication number: 20160250319
    Abstract: Methods for improving the drying yield and stability of RSV vaccines comprising a highly thermolabile enveloped live virus and/or one or more RSV protein subunits, are described. Methods for rapid drying of RSV formulations containing between 17.5% and 60% w/w of a non-polymeric sugar and using either conduction or radiation dominant drying mechanisms, are disclosed. The disclosed methods provide for; 1) a dried RSV formulation with improved stability profile; 2) faster drying; and 3) integration of dried RSV into a primary device (such as dual chamber cartridges, foil-pouch devices etc.), pre- as well as post-drying.
    Type: Application
    Filed: October 13, 2014
    Publication date: September 1, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Akhilesh Bhambhani, Robert K. Evans, Lynne A. Isopi
  • GLUCOSE-RESPONSIVE INSULIN CONJUGATES
    Publication number: 20160251407
    Abstract: Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.
    Type: Application
    Filed: October 2, 2014
    Publication date: September 1, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Lin Yan, Ahmet Kekec, Yuping Zhu, David N. Hunter, Pei Huo, Danqing Feng, Ravi P. Nargund, Christopher R. Moyes, Zhiqiang Zhao, Brenda Pipik, Dmitri Pissarnitski, Joseph L. Duffy, Erin Guidry
  • COMPLIMENTARY TRADE DRUG DELIVERY SYSTEM
    Publication number: 20160253475
    Abstract: A complimentary trade drug delivery system comprising (a) an electronic health record platform for storing patient health record data and generating electronic prescriptions, and (b) an eligibility verification system for identifying and verifying eligible programs, patients and health care providers for complimentary trade drug programs. The eligibility verification system automatically verifies that patients and prescribing health care providers are eligible to participate in existing complimentary trade drug programs and sends orders to program pharmacy computer systems that cause a program pharmacy computer system to deliver complimentary trade drugs to a patient.
    Type: Application
    Filed: October 30, 2014
    Publication date: September 1, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventor: Kevin Scott PARIS
  • METHODS AND INTERMEDIATES FOR PREPARING MACROLACTAMS
    Publication number: 20160251375
    Abstract: The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.
    Type: Application
    Filed: October 14, 2014
    Publication date: September 1, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Feng XU, Richard DESMOND, Guy R. HUMPHREY, Hongming LI, Ji QI, Rebecca T. RUCK, Zhiguo Jake SONG, Tao WANG, Yong-Li ZHONG, Jeonghan PARK, Laura Marie ARTINO, Richard John VARSOLONA
  • GLUCAGON RECEPTOR ANTAGONIST COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE
    Publication number: 20160250184
    Abstract: Glucagon receptor antagonist compounds are disclosed which are of long duration of action. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: October 30, 2014
    Publication date: September 1, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: SONGNIAN LIN, Libo Xu, Emma R. Parmee, Xibin Liao
  • METHOD OF MICROWAVE VACUUM DRYING SPHERICAL-SHAPED PELLETS OF BIOLOGICAL MATERIALS
    Publication number: 20160252300
    Abstract: Methods for preparing dried pellets of biological materials are described. The pellets can have a substantially spherical shape and are prepared by freezing droplets of a liquid composition of a desired biological material on a solid surface followed by microwave vacuum drying the frozen droplets. These methods are useful for preparing dried pellets having a high concentration of a desired biological material, in particular a therapeutic protein or vaccine, and which have a faster reconstitution time than lyophilized powder cakes prepared in vials.
    Type: Application
    Filed: October 13, 2014
    Publication date: September 1, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Akhilesh Bhambhani, Robert K. Evans, Jessica Sinacola, Rebecca Lizzano
  • -imino--oxo-iminothiadiazine compounds as BACE inhibitors, compositions, and their use
    Patent number: 9428476
    Abstract: In its many embodiments, the present invention provides provides certain S-imino-S-oxo iminothiadiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein RN, R1, R2, R3, R4, ring A, RA, m, L1, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful 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: March 11, 2014
    Date of Patent: August 30, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tanweer A. Khan, Jack D. Scott, Jared N. Cumming
  • Methods for increasing N-glycan occupancy and reducing production of hybrid N-glycans in pichia pastoris strains lacking ALG3 expression
    Patent number: 9428784
    Abstract: Methods for increasing the yield and N-glycosylation site occupancy of paucimannose or complex N-glycans of recombinant glycoproteins produced in a recombinant host cell lacking dolichyl-P-Man:Man5GlcNAc2-PP-dolichyl alpha-1,3 mannosyltransferase (Alg3p) activity are disclosed. In particular, recombinant host cells are provided that comprise a disruption of the expression of an OS-9 family gene in the host cell. These recombinant host cells may then be used for producing recombinant glycoproteins. In further embodiments, the recombinant host cells further overexpress at least one heterologous single-subunit oligosaccharyltransferase, which in particular embodiments is capable of functionally suppressing the lethal phenotype of a mutation of at least one essential protein of the yeast oligosaccharyltransferase (OTase) complex.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: August 30, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Byung-Kwon Choi, Stephen R. Hamilton, Natarajan Sethuraman