Patents Assigned to Merck Sharp
  • OXAZOLOBENZIMIDAZOLE DERIVATIVES
    Publication number: 20110178117
    Abstract: The present invention is directed to oxazolobenzimidazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.
    Type: Application
    Filed: September 16, 2009
    Publication date: July 21, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Antonella Converso, Timothy John Hartingh, Sylwia Stachura
  • Phosphorus derivatives as histone deacetylase inhibitors
    Patent number: 7981874
    Abstract: The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also 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: July 16, 2007
    Date of Patent: July 19, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joshua Close, Jonathan Grimm, Richard W. Heidebrecht, Jr., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Scott Peterson, Phieng Siliphaivanh, Paul J. Tempest, Kevin J. Wilson, David J. Witter
  • Triazole derivatives as inhibitors of 11-?-hydroxysteroid dehydrogenase-1
    Patent number: 7981910
    Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
    Type: Grant
    Filed: October 16, 2006
    Date of Patent: July 19, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sherman T. Waddell, James M. Balkovec, Nancy J. Kevin, Xin Gu
  • MONOCYCLIC AMIDE CGRP RECEPTOR ANTAGONISTS
    Publication number: 20110172205
    Abstract: Compounds of formula (I): wherein variables B, m, n, J, R4, Ea, Eb, Ec, Rf, RPG and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 is involved.
    Type: Application
    Filed: August 31, 2009
    Publication date: July 14, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Howard G. Selnick
  • ANTIFUNGAL AGENTS
    Publication number: 20110172225
    Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
    Type: Application
    Filed: September 25, 2008
    Publication date: July 14, 2011
    Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.
    Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
  • Substituted imidazole 4-carboxamides as cholecystokinin-1 receptor modulators
    Patent number: 7977339
    Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: July 12, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Scott Edmondson, Alexa Hansen, Cheng Zhu
  • Optimized expression of HPV 58 L1 in yeast
    Patent number: 7976848
    Abstract: Synthetic DNA molecules encoding the HPV58 L1 protein are provided. Specifically, the present invention provides polynucleotides encoding HPV58 L1 protein, wherein said polynucleotides are codon-optimized for high level expression in a yeast cell. The synthetic molecules may be used to produce HPV58 virus-like particles (VLPs), and to produce vaccines and pharmaceutical compositions comprising the HPV58 VLPs. The vaccines of the present invention provide effective immunoprophylaxis against papillomavirus infection through neutralizing antibody and cell-mediated immunity and are also useful for treatment of existing HPV infections.
    Type: Grant
    Filed: January 26, 2009
    Date of Patent: July 12, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Janine T. Bryan, Michelle K. Brownlow, Loren D. Schultz, Xin-Min Wang, Kathrin U. Jansen
  • Potassium channel inhibitors
    Patent number: 7973059
    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: October 17, 2006
    Date of Patent: July 5, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Wolkenberg, Mark T. Bilodeau, M. Brad Nolt
  • Macrocyclic quinoxaline compounds as HCV NS3 protease inhibitors
    Patent number: 7973040
    Abstract: The present invention relates to macrocyclic a compound of formula (I) and its use as inhibitors of the hepatitis C virus (HCV) NS3 protease, and in treating or preventing HCV infections.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: July 5, 2011
    Assignees: Merck Sharp & Dohme Corp., Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA
    Inventors: Steven Harper, Vincenzo Summa, Nigel J. Liverton, John A. McCauley
  • HIV integrase inhibitors
    Patent number: 7968564
    Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. 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: April 15, 2010
    Date of Patent: June 28, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph P. Vacca, Linda S. Payne, Richard C. A. Isaacs
  • 2,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's Disease
    Patent number: 7968571
    Abstract: The present invention is directed to 2,4,6-substituted pyridyl derivative compounds 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: April 20, 2005
    Date of Patent: June 28, 2011
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: James C. Barrow, Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Shaun R. Stauffer, Joseph P. Vacca, Shawn J. Stachel, Craig A. Coburn, Matthew G. Stanton
  • Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
    Patent number: 7968589
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: June 28, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John E. Stelmach, Emma R. Parmee, James R. Tata, Keith G. Rosauer, Ronald M. Kim, Amy R. Bittner, Jiang Chang, Christopher Joseph Sinz
  • Spirohydantoin tricyclic CGRP receptor antagonists
    Patent number: 7968540
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, R6, T, U, V, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 is involved.
    Type: Grant
    Filed: November 14, 2006
    Date of Patent: June 28, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman
  • SPIROAZAINDOLES
    Publication number: 20110152304
    Abstract: The present invention relates to spiroazaindole compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Application
    Filed: April 28, 2009
    Publication date: June 23, 2011
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Joan M. Pierce (nee Fletcher), Jeffrey J. Hale, Shouwu Miao, Petr Vachal
  • Pharmaceutical phenylquinoline and chromen-2-one triazole compounds
    Patent number: 7960409
    Abstract: The instant invention provides compounds of Formula I which are leukotriene biosynthesis inhibitors. Compounds of Formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Grant
    Filed: February 1, 2008
    Date of Patent: June 14, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Erich L. Grimm, Yves Ducharme, Richard Frenette, Richard Friesen, Marc Gagnon, Helene Juteau, Sebastien Laliberte, Bruce MacKay, Yves Gareau
  • Method of designing siRNAs for gene silencing
    Patent number: 7962316
    Abstract: The present invention provides a method for identifying siRNA target motifs in a transcript using a position-specific score matrix approach. The invention also provides a method for identifying off-target genes of an siRNA using a position-specific score matrix approach. The invention further provides a method for designing siRNAs with higher silencing efficacy and specificity. The invention also provides a library of siRNAs comprising siRNAs with high silencing efficacy and specificity.
    Type: Grant
    Filed: October 27, 2004
    Date of Patent: June 14, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Aimee L. Jackson, Steven R. Bartz, Julja Burchard, Peter S. Linsley, Wei Ge, Guy L. Cavet
  • Benzazole potentiators of metabotropic glutamate receptors
    Patent number: 7960417
    Abstract: The present invention is directed to benzazole compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: February 17, 2006
    Date of Patent: June 14, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Steven P. Govek, Jean-Michel Vernier, Theodore Kamenecka, John H. Hutchinson, Richard Pracitto
  • METHOD OF TREATING MEN WITH TESTOSTERONE SUPPLEMENT AND 5ALPHA-REDUCTASE INHIBITOR
    Publication number: 20110136769
    Abstract: A method of treating Alzheimer's disease, Parkinson's disease, sexual dysfunction or erectile dysfunction in a man by administration of a 5alpha reductase inhibitor together with a testosterone supplement is described. The method is also concerned with the use of the 5alpha reductase inhibiting compound and the testosterone supplement together with another agent useful for treating erectile dysfunction, including PDE V inhibitors; AGE (advanced glycation end-product) breakers; alpha 1 blockers; alpha 1A antagonists; alpha 2 antagonists; dopamine agonists; dopamine D4 agonists; melanocortin agonists; oxytocin agonists; prostaglandin; radical scavengers; rotamase inhibitors; aviptadil; nitroglycerine; and GPCR agonists for treating male sexual dysfunction or erectile dysfunction.
    Type: Application
    Filed: February 17, 2011
    Publication date: June 9, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Alan Meehan
  • Bicyclic pyrimidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 7956061
    Abstract: The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) 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: January 18, 2006
    Date of Patent: June 7, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wallace T. Ashton, Charles G. Caldwell, Hong Dong, Ying-Duo Gao, Giovanna Scapin, Ann E. Weber
  • Constrained spirocyclic compounds as CGRP receptor antagonists
    Patent number: 7951795
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, G1, G2, G3, J, m, n, p, R1, R2, R3, R4 and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 is involved.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: May 31, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Harold G. Selnick