Patents Assigned to Merck Sharp
  • COMPOSITIONS AND METHODS FOR SHORT INTERFERING NUCLEIC ACID INHIBITION OF NAV1.8
    Publication number: 20130109739
    Abstract: The invention provides short interfering nucleic acids, either single-stranded or double-stranded, that cause RNAi-induced degradation of mRNA from the Nav1.8 sodium channel gene; to pharmaceutical compositions comprising such short interfering nucleic acids; recombinant vectors comprising such short interfering nucleic acids; a method for inhibiting translation of an mRNA; a method for inhibiting expression of a polypeptide; a method for blocking the membrane potential in a cell; a method for blocking the sodium current in a cell; and a method for inhibiting chronic pain.
    Type: Application
    Filed: October 16, 2012
    Publication date: May 2, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Merck Sharp & Dohme Corp.
  • Ring-annulated dihydropyrrolo[2,1-?]isoquinolines
    Patent number: 8431564
    Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: April 30, 2013
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
  • Inhibitors of janus kinases
    Patent number: 8431569
    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: December 9, 2008
    Date of Patent: April 30, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jonathan R. Young, Jongwon Lim, Michelle R. Machacek, Brandon Mitsuo Taoka, Ryan D. Otte
  • Diaryl substituted alkanes
    Patent number: 8426413
    Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Grant
    Filed: February 23, 2012
    Date of Patent: April 23, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
  • RNA interference mediated inhibition of the FC?R1? gene
    Patent number: 8426581
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of FC?R1? gene expression and/or activity, and/or modulate a FC?R1? gene expression pathway. Specifically, the invention relates to doublestranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against FC?R1? gene expression.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: April 23, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vasant Jadhav, Victoria Pickering, Walter Strapps
  • Heterocyclic-fused pyrazolo[4,3-]pyridin-3-one M1 receptor positive allosteric modulators
    Patent number: 8426438
    Abstract: The present invention is directed to heterocyclic fused pyrazole[4,3-c]pyridine-3-one compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. 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 mediated by the M1 receptor.
    Type: Grant
    Filed: September 20, 2010
    Date of Patent: April 23, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Scott D. Kuduk
  • Monocyte-derived nucleic acids and related compositions and methods
    Patent number: 8426144
    Abstract: Nucleic acids encoding various monocyte-derived proteins and related compositions, including purified proteins and specific antibodies are described. Methods of using such composition are also provided.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: April 23, 2013
    Assignee: Merck & Sharp & Dohme Corp.
    Inventors: Elizabeth Bates, Nathalie Fournier, Lionel Chalus, Pierre Garrone
  • N-heterocyclic M1 receptor positive allosteric modulators
    Patent number: 8426598
    Abstract: The present invention is directed to compounds of formula (I) (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. 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 mediated by the M1 receptor.
    Type: Grant
    Filed: July 31, 2009
    Date of Patent: April 23, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Scott D. Kuduk, Christina Ng Di Marco
  • Nucleic acids encoding TNF?
    Patent number: 8426573
    Abstract: Nucleic acids encoding mammalian, e.g., primate or rodent, genes, 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 provided.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: April 23, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christi L. Parham, Daniel M. Gorman, Hirokazu Kurata, Naoko Arai, Theodore R. Sana, Jeanine D. Mattson, Erin E. Murphy, Chetan Savkoor, Jeffery Grein, Kathleen M. Smith, Terrill K. McClanahan
  • Intermediate compounds for the preparation of -5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1-dibenz[2,3:6,7]-oxepino[4,5-]pyrrole
    Patent number: 8426610
    Abstract: Disclosed are novel amino acid derivatives of formula (I) and (II) processes for the preparation thereof, and their use in the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole.
    Type: Grant
    Filed: May 2, 2011
    Date of Patent: April 23, 2013
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Gerardus Johannes Kemperman, Jacobus Johannes Maria Van Der Linden, Michael R. Reeder
  • POSACONAZOLE INTRAVENOUS SOLUTION FORMULATIONS STABILIZED BY SUBSTITUTED BETA-CYCLODEXTRIN
    Publication number: 20130096053
    Abstract: The present invention relates to aqueous solutions useful as pharmaceutical compositions of posaconazole for intravenous administration. These compositions include a solubilizing agent, such as a modified ?-cyclodextrin in an acidified solution, which can also include a chelating agent such as disodium edetate (EDTA). In clinical trials, a 200 mg posaconazole dose of the selected composition was found to achieve acceptable pharmacokinetic properties.
    Type: Application
    Filed: June 24, 2011
    Publication date: April 18, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Susan K. Heimbecher, David Monteith
  • Silylated piperidine derivatives
    Patent number: 8420622
    Abstract: Compounds of formula I: I wherein at least one of R4 and R5 comprises Si(R6)3 as a substituent selectively attenuate production of A?(1-42) and hence find use in treatment of Alzheimer's disease and related conditions.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: April 16, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Benito Munoz, Jed Hubbs, Christopher L. Hamblett, Hua Zhou, Michelle Martinez
  • Anti-ADDL monoclonal antibody and use thereof
    Patent number: 8420093
    Abstract: The present invention relates to antibodies that differentially recognize multi-dimensional conformations of A?-derived diffusible ligands, also known as ADDLs. The antibodies of the invention can distinguish between Alzheimer's Disease and control human brain extracts and are useful in methods of detecting ADDLs and diagnosing Alzheimer's Disease. The present antibodies also block binding of ADDLs to neurons, assembly of ADDLS, and tau phosphorylation and are there useful in methods for the preventing and treating diseases associated with soluble oligomers of amyloid ? 1-42.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: April 16, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gene Kinney, William R. Strohl, Zhiqiang An
  • Inhibitors of janus kinases
    Patent number: 8420695
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: April 16, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin Wilson, Gabriela de Almeida, Andrew Haidle, Kaleen Konrad, Michelle Machacek, Ann Zabierek
  • Process for the precipitation and isolation of 6,6-dimethyl-3-aza-bicyclo [3.1.0] hexane-amide compounds by controlled precipitation and pharmaceutical formulations containing same
    Patent number: 8420122
    Abstract: The present invention provides a method of continuous precipitation and isolation of an amorphous solid particulate form of 3-[2-(3-tert-Butyl-ureido)-3,3-dimethyl-butyryl]-6,6-dimethyl-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid (2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide having controlled physical properties. The present invention provides also pharmaceutical formulations comprising the precipitated compound.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: April 16, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dimitrios Zarkadas, Vincenzo Liotta, Christopher Stanley Pridgen, Wing-Kee Philip Cho, Zhihui Qiu
  • METHOD FOR TREATING A DISEASE ASSOCIATED WITH SOLUBLE, OLIGOMERIC SPECIES OF AMYLOID BETA 1-42
    Publication number: 20130089537
    Abstract: This invention is a method and kit for treating a disease associated with, or resulting from, the accumulation of soluble oligomer amyloid beta 1-42 using an antibody, or antibody fragment thereof, that has a higher affinity for amyloid beta 1-42 oligomers than for amyloid beta 1-42 monomer, amyloid beta 1-40 monomer, plaques and amyloid beta fibrils and, optionally, a tau therapeutic or an inhibitor of amyloid beta production or aggregation.
    Type: Application
    Filed: December 4, 2012
    Publication date: April 11, 2013
    Applicants: MERCK SHARP & DOHME CORP., ACUMEN PHARMACEUTICALS, INC.
    Inventors: Acumen Pharmaceuticals, Inc., Merck Sharp & Dohme Corp.
  • Inhibitors of Janus kinases
    Patent number: 8415346
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: July 21, 2009
    Date of Patent: April 9, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Altman, Kevin Wilson
  • Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin
    Patent number: 8414921
    Abstract: Disclosed are pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and metformin, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.
    Type: Grant
    Filed: December 12, 2006
    Date of Patent: April 9, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ashkan Kamali, Laman Alani, Kyle A. Fliszar, Soumojeet Ghosh, Monica Tijerina
  • Amino-quinoxaline and amino-quinoline compounds for use as adenosine Areceptor antagonists
    Patent number: 8415353
    Abstract: Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(?NOH)NH2, —CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: April 9, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
  • Methods of making antibodies specific for cysteine-rich soluble protein C23
    Patent number: 8415460
    Abstract: Nucleic acids encoding a new family of small cysteine rich soluble proteins, from a mammal, reagents related thereto, including specific antibodies, and purified proteins are described. Methods of using said reagents and related diagnostic kits are also provided.
    Type: Grant
    Filed: June 12, 2009
    Date of Patent: April 9, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Karin Franz-Bacon, Daniel M. Gorman, Terrill K. McClanahan