Patents Assigned to Merck Sharp and Dohme
  • 3,4-substituted pyrrolidine beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 8354545
    Abstract: The present invention is directed to 3,4-substituted pyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that 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: December 10, 2008
    Date of Patent: January 15, 2013
    Assignees: Merck, Sharp & Dohme, Corp., Istituto di Ricerche di Biologia Molecolare P Angeletti SPA
    Inventors: Shawn J. Stachel, Thomas Steele, Alessia Petrocchi
  • OXAZOLE DERIVATIVES USEFUL AS MODULATORS OF FAAH
    Publication number: 20130012526
    Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Application
    Filed: April 18, 2011
    Publication date: January 10, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Philippe G. Nantermet, Zhi-Qiang Yang, Constantine Kreatsoulas, Abbas M. Walji, Hong Zhu
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • EUKARYOTIC CELL DISPLAY SYSTEMS
    Publication number: 20120329679
    Abstract: The present invention provides expression vectors and helper display vectors which can be used in various combinations as vector sets for display of polypeptides on the outer surface of eukaryotic host cells. The expression vector of the invention can be used alone for soluble expression without having to change or reengineer the display vectors. The display systems of the invention are particularly useful for displaying a genetically diverse repertoire or library of polypeptides on the surface of yeast cells, and mammalian cells.
    Type: Application
    Filed: March 23, 2012
    Publication date: December 27, 2012
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Kevin Caili Wang, Peter Peizhi Luo, Pingyu Zhong, Jian Wang
  • 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
  • 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
  • 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
  • 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
  • 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
  • IMMUNOLOGICAL METHODS AND COMPOSITIONS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
    Publication number: 20120315321
    Abstract: The present invention relates to immunogenic compositions and peptides comprising residues 4-10 (FRHDSGY) of the amyloid peptide Abeta42. The invention further relates to antibodies that bind to the Abeta(4-10) antigenic determinant. The invention provides methods for treating Alzheimer's disease and for reducing the amyloid load in Alzheimers patients. The invention also relates to methods for designing small molecule inhibitors of amyloid deposition.
    Type: Application
    Filed: March 29, 2012
    Publication date: December 13, 2012
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Peter H. St. George-Hyslop, JoAnne McLaurin