Patents Assigned to Merck Sharp & Dohme
  • METHODS FOR THE PRODUCTION OF RECOMBINANT PROTEINS WITH IMPROVED SECRETION EFFICIENCIES
    Publication number: 20130011875
    Abstract: The present invention is related to methods and for producing higher titers of recombinant protein in a modified yeast host cell, for example Pichia pastoris, wherein the modified yeast cell lacks vacuolar sorting activity or has decreased vacuolar sorting activity relative to an unmodified yeast host cell of the same species. In particular embodiments vacuolar sorting activity is reduced or eliminated by deletion or disruption of a gene encoding Vps10 or a Vps10 homolog. The invention is also related to the modified yeast cells which are modified in accordance with the methods disclosed herein.
    Type: Application
    Filed: October 25, 2010
    Publication date: January 10, 2013
    Applicant: Merck Sharpe & Dohme Corp
    Inventors: Michael Meehl, Heping Lin, Byung-Kwon Choi
  • Tripyridyl carboxamide orexin receptor antagonists
    Patent number: 8349872
    Abstract: The present invention is directed to tripyridyl carboxamide 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: August 5, 2009
    Date of Patent: January 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker
  • Aryl aminopyridine PDE10 inhibitors
    Patent number: 8349830
    Abstract: The present invention is directed to aryl aminopyridine 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 26, 2010
    Date of Patent: January 8, 2013
    Assignee: Merck Sharp & Dohme
    Inventors: Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem
  • Inhibitors of janus kinases
    Patent number: 8349865
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: September 8, 2008
    Date of Patent: January 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tony Siu, Jonathan Young, Michael Altman, Alan Northrup, Matthew Katcher, Ellalahewage Sathyajith Kumarasinghe, Ekaterina Kozina, Scott Peterson, Matthew Childers
  • Polycyclic guanine derivatives and use thereof
    Patent number: 8349858
    Abstract: The present invention relates to Polycyclic Guanine Derivatives, compositions comprising the Polycyclic Guanine Derivatives and methods of using the Polycyclic Guanine Derivatives to treat pain or an inflammatory disease.
    Type: Grant
    Filed: June 18, 2008
    Date of Patent: January 8, 2013
    Assignee: Merck Sharp & Dohme
    Inventors: Deen Tulshian, William B. Geiss, Gregory S. Martin, Van-Duc Le, James C. Haber, Jr., Julius J. Matasi, Michael F. Czarniecki, Stephanie Nicole Cooke
  • Spirocyclic compounds
    Patent number: 8349825
    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: October 26, 2010
    Date of Patent: January 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dawn M. Mampreian, Joey L. Methot, Thomas Miller, Paul Tempest, Anna A. Zabierek
  • CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT
    Publication number: 20130004518
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: Merck, Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
  • Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
    Patent number: 8343990
    Abstract: Substituted cyclopropyl compounds of formula (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: January 1, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harold B. Wood, Jason W. Szewczyk, Yong Huang, Alan D. Adams
  • IGF-1R specific antibodies useful in the detection and diagnosis of cellular proliferative disorders
    Patent number: 8344112
    Abstract: The present invention relates to mammalian antibodies, designated 12B1 and antigen-binding portions thereof that specifically bind to insulin-like growth factor I receptor (IGF-IR), preferably human IGF-IR. Also included are chimeric, bispecific, derivatized, single chain antibodies derived from the antibodies disclosed herein. Nucleic acid molecules encoding the mammalian antibodies as well as methods of use thereof are also disclosed. Also included are pharmaceutical compositions comprising these antibodies and methods of using the antibodies and compositions thereof for treatment and diagnosis of pathological hyperproliferative oncogenic disorders associated with expression of IGF-1R.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: January 1, 2013
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Liliane Goetsch, David Brooks, Michael Chastain, Zhi-Qiang Zhang, Nathalie Corvaia
  • Antagonists of PCSK9
    Patent number: 8344114
    Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: January 1, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Carl P. Sparrow, Ayesha Sitlani, Shilpa Pandit, Jon H. Condra, Holly A Hammond
  • Inhibitors of Janus kinases
    Patent number: 8344144
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: January 1, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michelle Machacek, Gabriela de Almeida, Jonathan B. Grimm, Rachel N. MacCoss, Eric Romeo, Tony Siu, Catherine White, Kevin Wilson
  • Tertiary carbinamines having substituted heterocycles which are active as ?-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 8338614
    Abstract: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: December 25, 2012
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Shaun R. Stauffer
  • Method of treatment using fused aromatic compounds having anti-diabetic activity
    Patent number: 8338458
    Abstract: Fused aromatic compounds of Formula I are PPAR gamma agonists or partial agonists and are useful for weekly dosing in the treatment or control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
    Type: Grant
    Filed: May 2, 2008
    Date of Patent: December 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Peter T. Meinke, Andrew Denker, Gary E. Meininger, Naoto Uemura, John A. Wagner, Steven Charnick
  • Isoquinolinone potassium channel inhibitors
    Patent number: 8338449
    Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: April 2, 2010
    Date of Patent: December 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: B. Wesley Trotter, Christopher Claiborne, Gerald S. Ponticello, Charles J. McIntyre, Nigel Liverton, David A. Claremon
  • Hexahydrocyclopentyl[]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor modulators
    Patent number: 8338472
    Abstract: The present invention is directed to hexahydrocyclopentylf]imidazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: February 16, 2009
    Date of Patent: December 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William P. Dankulich, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
  • CETP inhibitors
    Patent number: 8334290
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: October 30, 2006
    Date of Patent: December 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Julianne A. Hunt, Florida Kallashi, Jennifer Kowalchick, Dooseop Kim, Cameron J. Smith, Peter J. Sinclair, Ramzi F. Sweis, Gayle E. Taylor, Christopher F. Thompson, Liya Chen, Nazia Quraishi
  • Renin inhibitors
    Patent number: 8334308
    Abstract: The present invention relates to biphenyl-based renin inhibitor compounds having amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: December 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helene Juteau, Michel Gallant, Daniel Dube, Patrick Roy, Renee Aspiotis, Rejean Fortin, Patrick Lacombe, Daniel McKay, Tom Yao-Hsiang Wu
  • PYRIDONE DERIVATIVES
    Publication number: 20120316200
    Abstract: The present invention is directed to novel phenylpyridone derivative compounds. The compounds act as a melanin concentrating hormone receptor antagonists, and can be useful in preventing, treating or acting as a remedial agent for various circular system diseases, nervous system diseases, metabolic diseases, genital diseases, respiratory diseases and digestive diseases.
    Type: Application
    Filed: April 7, 2011
    Publication date: December 13, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Linus S. Lin, Richard Soll, Jingchao Dong, Hao Wu, Takao Suzuki, Bin Hu, Dejun Liu, Jinglai Hao, Ming Xu
  • Inhibitors of janus kinases and/or 3-phosphoinositide-dependent protein kinase-1
    Patent number: 8329722
    Abstract: The instant invention provides for compounds that inhibit JAK2 tyrosine kinase and/or PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting JAK2 tyrosine kinase activity and/or PDK1 kinase inhibitory activity by administering the compound to a patient in need of treatment or prevention of myeloproliferative disorders or cancer.
    Type: Grant
    Filed: March 10, 2008
    Date of Patent: December 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tony Siu, Jonathan Young, Michael Altman, Alan Northrup, Ekaterina Kozina, Christopher Dinsmore, David J. Guerin, Kevin A. Keenan, Joon O. Jung, Solomon Kattar, Rachel N. MacCoss
  • Imidizo[1,2-A]pyrazines useful as AHCY hydrolase inhibitors
    Patent number: 8329697
    Abstract: The present invention is directed to AHCY inhibitors of formula (I) which are useful in the treatment of diseases characterized by high homocysteine levels, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases characterized by high homocysteine levels.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: December 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert M. Garbaccio, Antonella Converso, Mark E. Fraley, Timothy J. Hartingh