Patents Assigned to Merck
  • Substituted 5-phenyl-3,6-dihydro-2-oxo-6H-1,3,4-thiadiazines
    Patent number: 7902186
    Abstract: Compounds of the formula (I), in which R1, R2, m, Q and B have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Grant
    Filed: October 25, 2006
    Date of Patent: March 8, 2011
    Assignee: Merck Patent GmbH
    Inventors: Oliver Schadt, Dieter Dorsch, Melanie Schultz, Andree Blaukat
  • NPC1L1 (NPC3) and methods of identifying ligands thereof
    Patent number: 7901893
    Abstract: The present invention provides human, rat and mouse NPCIL1 polypeptides and polynucleotides encoding the polypeptides. Methods for detecting ligands which bind to NPC1L1 and block intestinal cholesterol absorption are provided. Also included is a method of identifying ligands which bind to NPCILI using membranes derived from brush border membrane preparations. Compounds that bind to NPCILI can be used for inhibiting intestinal cholesterol absorption in a subject.
    Type: Grant
    Filed: January 14, 2005
    Date of Patent: March 8, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Maria Margarita Garcia-Calvo
  • Phenyl derivatives as factor XA inhibitors
    Patent number: 7902223
    Abstract: Novel compounds of the formula (I), in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.
    Type: Grant
    Filed: July 12, 2002
    Date of Patent: March 8, 2011
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Bertram Cezanne, Christos Tsaklakidis, Werner Mederski, Johannes Gleitz, Christopher Barnes
  • Process for preparing chiral dipeptidyl peptidase-IV inhibitor intermediates
    Patent number: 7902376
    Abstract: A novel process is provided for the preparation of chiral trans-2,3-disubstituted 5-oxotetrahydropyrans of structural formula (I): wherein Ar is optionally substituted phenyl and P is a primary amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.
    Type: Grant
    Filed: January 22, 2009
    Date of Patent: March 8, 2011
    Assignees: Merck Sharp & Dohme Corp., Banyu Pharmaceutical Co., Ltd.
    Inventors: Feng Xu, Mary M. Kim, Yoshinori Kohmura, Tricia Sladicka, Jonathan D. Rosen, Michael J. Zacuto
  • NANOPARTICLE FORMATION VIA RAPID PRECIPITATION
    Publication number: 20110053927
    Abstract: The invention encompasses a method for making nano-sized particles of water-insoluble pharmaceuticals comprising: (1) dissolving the water-insoluble pharmaceutical in a water-miscible solvent, optionally with water and inactive pharmaceutical ingredients, to make a solution; (2) rapidly mixing the solution with an anti-solvent which creates a high level of supersaturation, wherein the anti-solvent is water with optional inactive pharmaceutical ingredients; (3) simultaneously applying energy to the resulting mixture during the mixing of solution and anti-solvent as nano-sized drug particles precipitate out and form a slurry mixture under supersaturation; and (4) optionally isolating the nano-sized particles of water-insoluble pharmaceuticals from the slurry mixture.
    Type: Application
    Filed: April 20, 2009
    Publication date: March 3, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Hsien-Hsin Tung, Lei Wang, Santipharp Panmai, Michael Riebe
  • Thiophene derivatives, and LC media containing same
    Publication number: 20110049427
    Abstract: The present invention relates to thiophene derivatives, to processes and intermediates for the preparation thereof, to the use thereof for optical, electro-optical and electronic purposes, in particular in liquid-crystal (LC) media and LC displays, and to LC media and LC displays comprising same.
    Type: Application
    Filed: March 30, 2009
    Publication date: March 3, 2011
    Applicant: MERCK PATENT GESELLSCHAFT
    Inventors: Axel Jansen, Detlef Pauluth, Harald Hirschmann, Markus Czanta
  • PROTEIN KINASE INHIBITORS AND USE THEREOF
    Publication number: 20110053906
    Abstract: Disclosed are benzonaphthyridinyl derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to kinase signal transduction inhibition, regulation or modulation.
    Type: Application
    Filed: February 25, 2009
    Publication date: March 3, 2011
    Applicant: MERCK PATENT GMBH
    Inventors: Bayard R. Huck, Xiaoling Chen, Lizbeth Celeste Deselm, Christopher Charles Victor Jones, Srinivasa R. Karra, Yufang Xiao, Andreas Goutopoulos, Amanda E. Sutton
  • ANGIOTENSIN II RECEPTOR BLOCKER DERIVATIVES
    Publication number: 20110052674
    Abstract: New angiotensin II receptor blocker nitroderivatives of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: and their use for treating cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndromes.
    Type: Application
    Filed: February 19, 2009
    Publication date: March 3, 2011
    Applicants: MERCK SHARP & DOHME CORP., NICOX S.A.
    Inventors: Nicoletta Almirante, Alessia Nicotra, Valentino Mandelli, Stefano Biondi, Silvia Stefanini, Iyassu K. Sebhat, Michael Man-Chu Lo
  • LIQUID-CRYSTAL DISPLAY
    Publication number: 20110051049
    Abstract: The present invention relates to polymerisable compounds, to processes and intermediates for the preparation thereof, and to the use thereof for optical, electro-optical and electronic purposes, in particular in liquid-crystal (LC) media and LC displays, especially in LC displays of the PS (polymer-stabilised) and PSA (polymer-sustained alignment) type.
    Type: Application
    Filed: March 4, 2009
    Publication date: March 3, 2011
    Applicant: MERCK PATENT GESELLSCHAFT
    Inventors: Achim Goetz, Erdal Durmaz, Malgorzata Rillich, Andreas Taugerbeck
  • RNA interference mediated inhibition of protein tyrosine phosphatase-1B (PTP-1B) gene expression using short interfering nucleic acid (siNA)
    Patent number: 7897757
    Abstract: This invention relates to compounds, compositions, and methods useful for modulating protein tyrosine phosphatase-1B (PTP-1B) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of PTP-1B gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features 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 and methods used to modulate the expression of PTP-1B genes. Such small nucleic acid molecules are useful, for example, for treating, preventing, inhibiting, or reducing obesity, insulin resistance, diabetes (eg.
    Type: Grant
    Filed: February 25, 2010
    Date of Patent: March 1, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Leonid Beigelman, James McSwiggen
  • RNA interference mediated inhibition of NOGO and NOGO receptor gene expression using short interfering nucleic acid (siNA)
    Patent number: 7897756
    Abstract: This invention relates to compounds, compositions, and methods useful for modulating NOGO and/or NOGO receptor gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of NOGO and/or NOGO receptor gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features 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 and methods used to modulate the expression of NOGO and/or NOGO receptor genes, such as NOGO-A, NOGO-B, NOGO-C, NOGO-66 receptor, NI-35, NI-220, NI-250, myelin-associated glycoprotein, tenascin-R, and NG-2.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: March 1, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James McSwiggen, Leonid Beigelman
  • Use of 4-oxobutanoic acid derivatives in the treatment of inflammation
    Patent number: 7897644
    Abstract: The present invention relates to the use of a 4-oxobutanoic acid derivative for the preparation of a pharmaceutical composition for treating inflammation.
    Type: Grant
    Filed: November 6, 2002
    Date of Patent: March 1, 2011
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Gérard Moinet, Dominique Marais, Philippe Maizeray
  • Arylpyrazinone derivatives insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes
    Publication number: 20110046159
    Abstract: The present invention relates to arylpyrazinone derivatives of formula (I), wherein R1, R2, R3 and A are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
    Type: Application
    Filed: March 31, 2009
    Publication date: February 24, 2011
    Applicant: Merck Patent Gesellschaft
    Inventors: Gérard Botton, Eric Valeur, Christine Charon, Micheline Kergoat, Samer Elbawab
  • Reactive ionic liquids
    Publication number: 20110045359
    Abstract: The invention relates to reactive ionic liquids containing organic cations with groups or substituents which are susceptible to electrochemical reduction and anions obtained from fluoroalkyl phosphates, fluoroalkyl phosphinates, fluoroalkyl phosphonates, acetates, triflates, imides, methides, borates, phosphates and/or aluminates, for use in electrochemical cells, such as lithium ion batteries and double-layer capacitors.
    Type: Application
    Filed: March 31, 2009
    Publication date: February 24, 2011
    Applicant: MERCK PATENT GESELLSCHAFT
    Inventors: Michael Schmidt, Nikolai (Mykola Ignatyev, William-Robert Pitner
  • LIQUID-CRYSTAL MEDIUM
    Publication number: 20110042615
    Abstract: The invention relates to a liquid-crystalline medium based on a mixture of polar compounds of positive dielectric anisotropy, characterised in that it comprises one or more compounds of the formula I and one or more compounds selected from the compounds of the formulae IA and IB in which R1, R2, L1-4, X1 and X2 have the meanings indicated in claim 1.
    Type: Application
    Filed: December 23, 2008
    Publication date: February 24, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Georg Luessem, Christian Hock, Brigitte Schuler, Eike Poetsch
  • Quinolizidinone M1 Receptor Positive Allosteric Modulators
    Publication number: 20110046145
    Abstract: The present invention is directed to 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: Application
    Filed: March 11, 2009
    Publication date: February 24, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
  • BENZO[F]CHROME ANY PYRANO[3,2-F]CHROME DERIVATIVES FOR USE IN LIQUID CRYSTAL MEDIA
    Publication number: 20110043746
    Abstract: The present invention relates to benzo[f]chromene and pyrano[3,2-f]-chromene derivatives of the formula I in which L1, L2, R1, R2, A1, A2, Z1, Z2, m and n are as defined in claim 1, to the preparation thereof, to the use thereof as components in liquid-crystalline media, and to electro-optical display elements which contain the liquid-crystalline media according to the invention.
    Type: Application
    Filed: November 3, 2008
    Publication date: February 24, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Axel Jansen, Melanie Klasen-Memmer
  • Interactive product selection system
    Patent number: 7891488
    Abstract: The present invention involves an interactive selection system for a consumer product that improves the consumer's ability to quickly sort through numerous criteria in a complex decision making process and determine whether that particular consumer product is appropriate for his or her purchase and use.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: February 22, 2011
    Assignees: McNeil-PPC, Inc., Merck Sharp & Dohme Corp.
    Inventors: Lisa Berry, Frank Gualtieri, Jerry B. Hansen, Robert Hasselman
  • Tyrosine kinase inhibitors
    Patent number: 7893081
    Abstract: This invention relates to salt forms of the compound N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N?-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfamide, an inhibitor of tyrosine kinases, in particular the receptor tyrosine kinase MET, that are useful in the treatment of cellular proliferative diseases, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation. In particular, the invention relates to the sodium salt of N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N?-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfamide.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: February 22, 2011
    Assignee: Merck & Co., Inc.
    Inventors: Paolo Avalle, Jennifer R. Foley, Peter Mullens, Yaling Wang, Peter Yehl
  • Substituted tetrahydroquinolines
    Patent number: 7893082
    Abstract: Disclosed are compounds of formula (I), wherein W, R, R1, R2, R3, R4, R5, R6, and R7 have the meanings indicated in claim 1. Said compounds can be used for the treatment of tumors, among other things.
    Type: Grant
    Filed: May 17, 2006
    Date of Patent: February 22, 2011
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, Ulrich Emde, Dirk Finsinger, Christiane Amendt, Nina Heiss, Frank Zenke