Patents Assigned to Merck
  • Publication number: 20120021074
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Application
    Filed: March 15, 2010
    Publication date: January 26, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Craig M. Potteiger
  • Patent number: 8101749
    Abstract: The invention relates to a method for producing onium salts with tetrafluoroborate anion by reacting an onium halide with an oxonium tetrafluoroborate, sulfonium tetrafluoroborate, or triphenylcarbonium tetrafluoroborate.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: January 24, 2012
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Nikolai (Mykola) Ignatyev, Urs Welz-Biermann, Andriy Kucheryna, Helge Willner
  • Patent number: 8101603
    Abstract: The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: July 9, 2007
    Date of Patent: January 24, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher J. Dinsmore, Matthew H. Katcher, Alan B. Northrup
  • Patent number: 8101663
    Abstract: The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: January 24, 2012
    Assignee: Merck HDAC Research, LLC
    Inventors: Thomas A. Miller, Victoria M. Richon
  • Publication number: 20120016011
    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 CTGF gene expression and/or activity, and/or modulate a CTGF gene expression pathway. Specifically, the invention relates to double-stranded 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 CTGF gene expression.
    Type: Application
    Filed: March 17, 2010
    Publication date: January 19, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Victoria Pickering, Jyoti Shah, Walter Strapps
  • Publication number: 20120016010
    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 Bach1 gene expression and/or activity, and/or modulate a Bach1 gene expression pathway. Specifically, the invention relates to double-stranded 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 Bach1 gene expression.
    Type: Application
    Filed: March 17, 2010
    Publication date: January 19, 2012
    Applicant: Merck Sharp & Dohme Corp
    Inventors: Victoria Pickering, Jyoti K. Shah, Walter Strapps
  • Publication number: 20120015976
    Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.
    Type: Application
    Filed: March 9, 2010
    Publication date: January 19, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANK TER HAFTUNG
    Inventors: Melanie Schultz, Kai Schiemann, Wolfgang Staehle
  • Publication number: 20120013831
    Abstract: The invention relates to a process of preparing a multilayer comprising two or more anisotropic layers with different optical axes by using a particle beam etching technique, to a multilayer obtained by said process, to the use of such a multilayer as optical compensator or retarder in optical and electrooptical devices, and to devices comprising such a multilayer.
    Type: Application
    Filed: March 11, 2010
    Publication date: January 19, 2012
    Applicant: MERCK PATENT GMBH
    Inventors: Owain Llyr Parri, Oleg Yaroshchuk, Ruslan Kravchuk
  • Patent number: 8097727
    Abstract: Compounds of the formula (I), in which R1a-R1e, R2a, R2b, R3 and R5 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: October 4, 2005
    Date of Patent: January 17, 2012
    Assignee: Merck patent GmbH
    Inventors: Wolfgang Staehle, Guenter Hoelzemann, Wilfried Rautenberg
  • Publication number: 20120010193
    Abstract: Compounds of Formula (I) (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.
    Type: Application
    Filed: March 8, 2010
    Publication date: January 12, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
  • Publication number: 20120010272
    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 ASK1 gene expression and/or activity, and/or modulate a ASK1 gene expression pathway. Specifically, the invention relates to double-stranded 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 ASK1 gene expression.
    Type: Application
    Filed: March 25, 2010
    Publication date: January 12, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Vasant Jadhav, Victoria Pickering, Walter Strapps
  • Publication number: 20120010186
    Abstract: Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis.
    Type: Application
    Filed: March 18, 2010
    Publication date: January 12, 2012
    Applicant: MERCK FROSST CANADA LTD.
    Inventors: Nicolas Lachance, Serge Leger, Renata M. Oballa, David Powell, Geoffrey K. Tranmer, Evelyn Martins, Yves Gareau
  • Publication number: 20120009393
    Abstract: The present invention relates to curable mixtures for the sealing, encapsulation, bonding or coating of opto-electronic components, such as OLEDs, solar cells, optical sensors and liquid-crystal displays, or for the alignment of liquid crystals.
    Type: Application
    Filed: February 25, 2010
    Publication date: January 12, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Matthias Koehler, Volker Meyer, Edgar Boehm, Michael Junge, Eike Poetsch
  • Publication number: 20120009580
    Abstract: In one aspect, the present invention provides methods for amplifying a microRNA molecule to produce DNA molecules. The methods each include the steps of: (a) using primer extension to make a DNA molecule that is complementary to a target microRNA molecule; and (b) using a universal forward primer and a reverse primer to amplify the DNA molecule to produce amplified DNA molecules. In some embodiments of the method, at least one of the forward primer and the reverse primer comprise at least one locked nucleic acid molecule.
    Type: Application
    Filed: September 22, 2011
    Publication date: January 12, 2012
    Applicant: MERCK SHARP & DOHME CORP.
    Inventor: Christopher K. Raymond
  • Patent number: 8093295
    Abstract: The present invention provides a pharmaceutical composition or crystalline composition with a specific dissolution profile, which comprises suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. The present invention provides a process of producing said crystalline composition or pharmaceutical composition. The present invention also provides compositions with a specific particle size distribution.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: January 10, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jeannie Chow Wong, Benjamin Max Cohen, Aaron S. Cote, Erik A. Dienemann, Kimberly Gallagher, Craig Ikeda, Justin Moser, Pavol Rajniak, Robert A. Reed, Brian Sell, Cindy Starbuck, Hsien-Hsin Tung, Qingxi Wang, Vincent R. Capodanno
  • Patent number: 8093270
    Abstract: The invention relates to a solid pharmaceutical preparation containing (R)-(?)-2-[5-(4-fluorophenyl-3-pyridylmethylaminomethyl]chroman as an active substance and at least one sugar alcohol (e.g. mannitol, sorbitol) as a filler. Also disclosed is the production of said solid pharmaceutical preparation, which is provided with an increased shelf life also at elevated temperatures and can be used for the treatment of dyskinesia associated with Parkinson's disease.
    Type: Grant
    Filed: June 9, 2006
    Date of Patent: January 10, 2012
    Assignee: Merck Patent GmbH
    Inventors: Klaus Kunath, Kirstin Heil, Roland Rupp
  • Patent number: 8093389
    Abstract: The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; R1 and R2 each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; R3 and R4 each represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-C
    Type: Grant
    Filed: January 8, 2008
    Date of Patent: January 10, 2012
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Tomoharu Iino, Hideki Jona, Jun Shibata, Tadashi Shimamura, Takeru Yamakawa, Lihu Yang
  • Patent number: 8093010
    Abstract: The present invention relates to a method for providing molecules that are capable of inhibiting angiogenesis, comprising the steps of providing a range of molecules; testing whether these molecules can prevent interaction between JAM-B and JAM-C; testing the positive molecules for their ability to block angiogenesis in vivo; and selecting molecules that are positive in the angiogenesis test as angiogenesis inhibiting molecules. The method may further comprise the step of isolating or producing the angiogenesis inhibiting molecules. The invention further relates to the angiogenesis inhibiting molecules thus provided and produced, to their use in the treatment of cancer, to therapeutical compositions comprising them. In a particular embodiment the invention relates to monoclonal antibodies, in particular Mab H33, to soluble JAM-C and JAM-B and to small molecules.
    Type: Grant
    Filed: October 29, 2009
    Date of Patent: January 10, 2012
    Assignee: Merck Serono S.A.
    Inventors: Beat A. Imhof, Michel Aurrand-Lions
  • Patent number: 8093240
    Abstract: Novel triazole derivatives are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Grant
    Filed: November 24, 2006
    Date of Patent: January 10, 2012
    Assignee: Merck Patent GmbH
    Inventors: Bertram Cezanne, Christiane Amendt, Hartmut Greiner, Ulrich Graedler, Guenter Hoelzemann
  • Publication number: 20120004281
    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 NGF? gene expression and/or activity, and/or modulate a NGF? gene expression pathway. Specifically, the invention relates to double-stranded 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 NGF? gene expression.
    Type: Application
    Filed: March 25, 2010
    Publication date: January 5, 2012
    Applicant: Merck Sharp & Dohme Corp
    Inventors: Vasant Jadhav, Victoria Pickering, Walter Strapps