Patents Assigned to Merck Sharp & Dohme
  • Pegylated interleukin-10
    Patent number: 8697045
    Abstract: Interleukin-10 (IL-10) conjugated via a linker to one or more polyethylene glycol (PEG) molecules at a single amino acid residue of the IL-10, and a method for preparing the same, are provided. The method produces a stable mono-pegylated IL-10, which retains IL-10 activity, where pegylation is selective for the N-terminus on one subunit of IL-10 with little or no formation of monomeric IL-10. The method also provides a substantially homogenous population of mono-PEG-IL-10.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: April 15, 2014
    Assignee: Merck Sharp & Dohme Corporation
    Inventors: Seoju Lee, David C. Wylie, Susan Cannon-Carlson
  • Binding compounds for IL-27
    Patent number: 8691953
    Abstract: Purified genes encoding a cytokine or composite cytokine from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding these molecules are provided. Methods of using said reagents and diagnostic kits are also provided.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jacqueline C. Timans, Stefan Karl-Heinz Pflanz, Robert A. Kastelein, J. Fernando Bazan, Donna Rennick, Rene de Waal Malefyt, Jeanne Cheung
  • Single chemical entities and methods for delivery of oligonucleotides
    Patent number: 8691580
    Abstract: In an embodiment the instant invention discloses a modular composition comprising 1) an oligonucleotide; 2) one or more linkers, which may be the same or different, selected from Table 1, wherein the linkers are attached to the oligonucleotide at any 3? and/or 5? end; 3) one or more peptides, which may be the same or different, selected from SEQ ID NOs: 1-59, wherein the peptides are attached to the linkers; and optionally one or more lipids, solubilizing groups and/or targeting ligands attached to the oligonucleotide.
    Type: Grant
    Filed: April 4, 2011
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jeffrey G. Aaronson, Stanley F. Barnett, René Bartz, Steven L. Colletti, Vasant R. Jadhav, Aaron A. Momose, Anthony W. Shaw, David M. Tellers, Thomas J. Tucker, Weimin Wang, Yu Yuan
  • Heterocyclic aspartyl protease inhibitors
    Patent number: 8691831
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula I are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: April 8, 2014
    Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Drug Discovery, Inc.
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey O. Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
  • Methods of treating multiple sclerosis, rheumatoid arthritis and inflammatory bowel disease using agonists antibodies to PILR-?
    Patent number: 8691227
    Abstract: The present invention provides methods of using PILR? agonists, or PILR? antagonists, to treat immune disorders, such as autoimmune and inflammatory disorders, including CNS, joint and gut inflammation.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Cristina M. Tato, Barbara Joyce-Shaikh, Daniel J. Cua
  • Nucleic acids encoding engineered anti-IL-23R antibodies
    Patent number: 8691532
    Abstract: Antibodies to human IL-23R are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
    Type: Grant
    Filed: November 7, 2012
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Leonard G. Presta
  • Tricyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors
    Patent number: 8691832
    Abstract: The present invention is directed to novel tricyclic heterocycles of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Duane A. Burnett, Zhiqiang Zhao, David Cole, Hubert Josien, Dmitri A. Pissarnitski, Thavalakulamgar Sasikumar, Wen-Lian Wu, Martin Domalski
  • Heterocyclic aspartyl protease inhibitors
    Patent number: 8691833
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: April 8, 2014
    Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Inc.
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey O. Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoiang Liu, Tao Guo, Thuy X.E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
  • Inhibitors of AKT activity
    Patent number: 8691825
    Abstract: The instant invention provides for substituted fused pyrimidine compounds of Formula A that inhibit Akt activity: In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qi Chen, Mingxiang Cui, Bin Hu, Shuangxi Hu, Zhifa Pu, Philip E. Sanderson, Richard Soll, Xue Tang, Jiabing Wang, Yongjin Yan, Jinfeng Yao, Hongjie Zhang
  • Amino tetrahydro-pyridopyrimidine PDE10 inhibitors
    Patent number: 8691827
    Abstract: The present invention is directed to amino tetrahydro-pyridopyrimidine 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: August 5, 2010
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, John D. Schreier
  • Mono- and di-PEG IL-10 production; and uses
    Patent number: 8691205
    Abstract: Provided are methods of producing a mixture of mono- and di-pegylated IL-10.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corporation
    Inventors: Steven J. Blaisdell, Collette M. Cutler, Brittany C. Paporello, Alexandre Ambrogelly
  • MAMMALIAN CYTOKINES; RECEPTORS; RELATED REAGENTS AND METHODS
    Publication number: 20140093875
    Abstract: Nucleic acids encoding mammalian cytokine receptor, e.g., for cytokine IL-B50, purified proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described.
    Type: Application
    Filed: December 2, 2013
    Publication date: April 3, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Pedro A. Reche-Gallardo, Vassili Soumelis, Yong-Jun Liu, Rene de Waal Malefyt, J. Fernando Bazan, Robert A. Kastelein
  • PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS WITH SIMVASTATIN
    Publication number: 20140093564
    Abstract: The present invention is directed to novel pharmaceutical compositions comprising fixed dose combinations of a dipeptidyl peptidase-4 inhibitor (DPP-4 inhibitor), or a pharmaceutically acceptable salt thereof, and simvastatin, or pharmaceutically acceptable salt thereof, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes and hypercholesterolemia with such pharmaceutical compositions. In particular, the invention is directed to pharmaceutical compositions comprising fixed-dose combinations of sitagliptin phosphate and simvastatin.
    Type: Application
    Filed: June 8, 2012
    Publication date: April 3, 2014
    Applicants: MERCK SHARP & DOHME LTD., Merck Sharp & Dohme Corp
    Inventors: Kathryn Bradley, Richard Elkes, Shaun Fitzpatrick, Robert Saklatvala, Mustafa Mohamed, Richard Kendall
  • Diazepan orexin receptor antagonists
    Patent number: 8685961
    Abstract: The present invention is directed to diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
    Type: Grant
    Filed: March 27, 2007
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Karen M. Brashear, Paul J. Coleman, Christopher D. Cox, Anthony M. Smith, David B. Whitman
  • Substituted triazolopyridines and analogs thereof
    Patent number: 8685967
    Abstract: The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.
    Type: Grant
    Filed: April 5, 2010
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ginny D. Ho, Elizabeth M. Smith, Eugenia Y. Kiselgof, Kallol Basu, Zheng Tan, Brian McKittrick, Deen Tulshian
  • Beta carboline sulphonylurea derivatives as EP4 receptor antagonists
    Patent number: 8685999
    Abstract: The invention is directed to ?-carboline sulphonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, inflammation, osteoarthritis, and rheumatoid arthritis. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Carl Berthelette, Michael Boyd, Jason Burch, Claude Dufresne, Julie Farand, Yongxin Han, Claudio F. Sturino
  • Pyrimidine derivatives for treatment of alzheimer's disease
    Patent number: 8685972
    Abstract: The invention encompasses pyrimidine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.
    Type: Grant
    Filed: July 31, 2009
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexey A. Rivkin, Sean P. Ahearn, Stephanie M. Chichetti
  • CGRP receptor antagonists
    Patent number: 8685965
    Abstract: Compounds of Formula (I), (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, L, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG, W, Y and Z are as described herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. 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 CGRP receptors are involved.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Donnette D. Staas, Ian M. Bell, Harold G. Selnick
  • Process for preparing N-substituted hydroxypyrimidinone carboxamides
    Patent number: 8686141
    Abstract: Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)-2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed.
    Type: Grant
    Filed: December 22, 2008
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Guy R. Humphrey, Ross A. Miller, Peter E. Maligres, Steven Weissman
  • Spirocyclic compounds
    Patent number: 8686020
    Abstract: The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher Hamblett, Joey L. Methot, Thomas Miller, David L. Sloman, Matthew G. Stanton, Paul Tempest, Anna A. Zabierek