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  • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    Patent number: 6008212
    Abstract: Compounds of formula I: ##STR1## as well as pharmaceutically acceptable salts thereof are disclosed. R.sup.2 is H and R.sup.3 is C1-3 alkyl, or R.sup.2 and R.sup.3 taken in combination represent C.sub.1-3 alkylidene. Pharmaceutical compositions and methods of treatment are also included. The compounds are useful against methicillin resistant staphylococci (MRSA).
    Type: Grant
    Filed: October 8, 1998
    Date of Patent: December 28, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Ronald W. Ratcliffe, Timothy A. Blizzard
  • Cholecystokinin antagonists
    Patent number: 4530790
    Abstract: The compound having Formula I and several minor related compounds are produced by the aerobic fermentation of Aspergillus alliaceus Thom and Church, ATCC No. 20655 or ATCC No. 20656. ##STR1## The compound of Formula I and the several minor related compounds are antagonists of cholecystokinin (CCK). CCK antagonists are useful in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems of animals, especially humans.
    Type: Grant
    Filed: July 1, 1983
    Date of Patent: July 23, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Richard L. Monaghan, Michael A. Goetz, Raymond S. L. Chang
  • Combination therapy for the treatment of diabetes and obesity
    Patent number: 5908830
    Abstract: The combination of a metabolic rate modifying agent (e.g., a .beta..sub.3 adrenergic receptor agonist) and a feeding behavior modifying agent (e.g., a NPY5 antagonist) is useful in the treatment of obesity and diabetes, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients. Methods of treating obesity and diabetes are also described.
    Type: Grant
    Filed: October 30, 1997
    Date of Patent: June 1, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Roy G. Smith, Margaret A. Cascieri, Euan MacIntyre, Douglas J. MacNeil, John G. Menke
  • Halophenoxy substituted carbapenem antibacterial compounds
    Patent number: 6310055
    Abstract: The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2 -position with a iodophenoxy linked through a group —Z—CH2—; The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: wherein Z represents trans-ethenediyl or ethynediyl. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: May 13, 1999
    Date of Patent: October 30, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Kevin D. Dykstra
  • Carbodiimide phosphors
    Patent number: 9045687
    Abstract: The invention relates to carbodiimide compounds of the general formula (I) EA2-ySi(CN2)4-xOx:Euy where EA stands for one or more elements selected from Mg, Ca, Sr, Ba or Zn and x stands for a value from the range from 0 to 3.9 and Y stands for a value from the range from 0.01 to 0.4, and a process for the preparation of these phosphors and the use thereof as conversion phosphors or in lamps.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: June 2, 2015
    Assignee: MERCK PATENT GMBH
    Inventors: Holger Winkler, Andreas Benker, Ralf Petry, Tim Vosgroene
  • Aryl, alkyl, alkenyl and alkynylmacrolides having immunosuppressive activity
    Patent number: 5550233
    Abstract: Aryl, alkyl, alkenyl and alkynyl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation and alkylation at C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.
    Type: Grant
    Filed: June 21, 1994
    Date of Patent: August 27, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Kathleen M. Rupprecht, Robert K. Baker, Hyun O. Ok, William H. Parsons
  • METHODS OF USING MIR34 AS A BIOMARKER FOR TP53 FUNCTIONAL STATUS
    Publication number: 20110105583
    Abstract: In one aspect, the invention generally relates to use of miR-34 as a biomarker to estimate TP53 function in a cell. In another aspect, the invention generally relates to multiple uses of miR-34 and siRNAs functionally and structurally related to miR-34 for the treatment of cancer.
    Type: Application
    Filed: May 5, 2008
    Publication date: May 5, 2011
    Applicants: MERCK & CO., INC., COLD SPRING HARBOR LABORATORY
    Inventors: Michele A. Cleary, Aimee L. Jackson, Peter S. Linsley, Julja Burchard, Lee P. Lim, Jill F. Magnus, Lin He, Xingyue He, Scott W. Lowe, Gregory J. Hannon
  • Pharmaceutical compositions of tedizolid phosphate
    Patent number: 11452719
    Abstract: Disclosed are pharmaceutical compositions comprising tedizolid phosphate, methods of preparing such pharmaceutical compositions, and methods of treating bacterial infections with such pharmaceutical compositions. Specifically, a pharmaceutical composition comprising tedizolid phosphate, an acid; and a suspending agent; and wherein the pH of the composition upon constitution with water is between about pH 2-4.5, is provided, wherein the acid is not citric acid or malic acid.
    Type: Grant
    Filed: December 10, 2018
    Date of Patent: September 27, 2022
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Lixia Cai, David Dubost, David Harris, Yongjun Li, Majid Mahjour, Dan Zhang
  • Electro-optical liquid-crystal display
    Patent number: 6045878
    Abstract: The invention relates to an electro-optical liquid-crystal display having a realignment layer for realigning the liquid crystals whose field has a significant component parallel to the liquid-crystal layer and which contains a liquid-crystalline medium of positive dielectric anisotropy, where the medium comprises at least one mesogenic compound and at least one alkenyl compound of formula I*.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: April 4, 2000
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Kazuaki Tarumi, Andreas Beyer, Volker Reiffenrath, Eike Poetsch
  • PLASMA KALLIKREIN INHIBITORS
    Publication number: 20240208994
    Abstract: The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age-related macular degeneration, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.
    Type: Application
    Filed: April 18, 2022
    Publication date: June 27, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Alan C. Cheng, Ying-Duo Gao, Song Yang, Mihir Mandal, Jiafang He, Jovan Alexander Lopez, Maoqun Tian
  • Permeable glycosidase inhibitors and uses thereof
    Patent number: 9611275
    Abstract: The present invention is directed to compounds and pharmaceutical formulations comprising these compounds which are useful as O-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus may be useful for the treatment of certain disorders such as Alzheimer's disease including reducing NFTs and/or hyperphosphorylated tau. The invention is also directed to use of the compounds as O-GlcNAcase imaging agents.
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: April 4, 2017
    Assignees: ALECTOS THERAPEUTICS, INC., MERCK SHARP & DOHME CORP.
    Inventors: Harold G. Selnick, Wenping Li, Eric Hostetler, Kun Liu, Ernest J. McEachern, Yuanxi Zhou, Zhongyong Wei, Changwei Mu, Yaode Wang, Jiang Chang
  • Non-Nucleoside Reverse Transcriptase Inhibitors
    Publication number: 20100222322
    Abstract: Indole compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: June 23, 2006
    Publication date: September 2, 2010
    Applicant: MERCK & CO., INC.
    Inventors: Scott E. Wolkenberg, Zhijian Zhao, Craig W. Lindsley
  • Multi-element standard for nuclear magnetic resonance spectroscopy
    Patent number: 10040811
    Abstract: Organic compounds which contain nitrogen, fluorine, and phosphorus atoms together with carbon atoms and hydrogen atoms and which can be used as a multi-element standard for 1H—, 13C—, 15N—, 19F—, and 31P nuclear magnetic resonance spectroscopy. Also, a nuclear magnetic resonance spectroscopy method, preferably a quantitative nuclear magnetic resonance spectroscopy method, using said compounds and a method for qualitatively and/or quantitatively determining an analyte using such a nuclear magnetic resonance spectroscopy method.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: August 7, 2018
    Assignee: Merck Patent GmbH
    Inventor: Bernd Willi Karl-Heinz Diehl
  • Liquid-crystalline material
    Patent number: 5538768
    Abstract: The invention relates to a liquid-crystalline material in the form of an anisotropic gel consisting of a polymerized liquid-crystalline material and a low-molecular weight liquid-crystalline material, wherein the polymerized material (a) forms a permanently oriented network in the low-molecular liquid-crystalline material (b), characterized in that the low-molecular weight liquid-crystalline material (b) exhibits a cholesteric phase, and to a display cell with such a material.
    Type: Grant
    Filed: July 1, 1994
    Date of Patent: July 23, 1996
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Shirley A. Marden, David Coates
  • Triazolo-pyrimidine as ligands for GABA receptors
    Patent number: 6337331
    Abstract: Substituted or 6,7-ring fused 1,2,3-triazolo[1,5-&agr;]-pyrimidine derivatives are selective ligands for GABAA receptors useful in the treatment of disorders of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: November 8, 2000
    Date of Patent: January 8, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Howard Barff Broughton, Jose Luis Castro Pineiro, Ian James Collins, Karl Richard Gibson, Michael Rowley, Leslie Joseph Street
  • 5-AZAINDAZOLE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS
    Publication number: 20210361669
    Abstract: The present invention relates to novel 5-azaindazole derivatives of formula (I), as described and defined herein, and pharmaceutically acceptable salts, solvates and prodrug thereof, as well as pharmaceutical compositions comprising such compounds. The 5-azaindazole derivatives according to the invention have been found to be highly effective dual A2A/A2B adenosine receptor antagonists, and can thus be used as therapeutic agents, particularly in the treatment or prevention of hyperproliferative or infectious diseases or disorders.
    Type: Application
    Filed: October 22, 2019
    Publication date: November 25, 2021
    Applicant: MERCK PATENT GMBH
    Inventors: Anne-Laure BLAYO, Bapriste MANTEAU, Camille AMALRIC, Stanislas MAYER, Stehan SCHANN, Mickaël FER
  • C-8A-Oxo-avermectin and milbemycin derivatives, pharmaceutical compositions and method of use
    Patent number: 4547491
    Abstract: There are disclosed novel avermectin and milbemycin compounds wherein the 8a position is oxidized to a ketone group. The 8a-oxo compounds are prepared by oxidizing an avermectin or milbemycin compound. The avermectin and milbemycin 8a-oxo compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests.
    Type: Grant
    Filed: July 18, 1984
    Date of Patent: October 15, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Helmut H. Mrozik, Frank S. Waksmunski
  • Hypocholesteremic fermentation products and process of preparation
    Patent number: 4231938
    Abstract: Substances isolated after cultivation of a microorganism belonging to the genus Aspergillus in a culture medium comprise a compound designated MSD803 which has the lactone structure: ##STR1## as well as its free hydroxy acid form. Together with salts and esters of the free acid form, these compounds form a class of highly active hypocholesteremic and hypolipemic medicaments.
    Type: Grant
    Filed: June 15, 1979
    Date of Patent: November 4, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Richard L. Monaghan, Alfred W. Alberts, Carl H. Hoffman, George Albers-Schonberg
  • Variants of the major allergen Phl p 1 from timothy grass
    Patent number: 7731970
    Abstract: The invention relates to pharmaceutically important variants of the major allergen Phl p 1 from timothy grass, characterized in that a preparation, hitherto not possible, of monomeric molecules which are soluble and stable in physiological media can be carried out with the aid of prokaryotic expression systems and subsequent purification thereof.
    Type: Grant
    Filed: July 31, 2003
    Date of Patent: June 8, 2010
    Assignee: Merck Patent GmbH
    Inventors: Roland Suck, Helmut Fiebig, Oliver Cromwell
  • Muscarine agonists
    Patent number: 5718912
    Abstract: This invention is concerned with novel 1-?cycloalkylpioeridin-4-yl!-2H benzimidazolones, their compositions and method of use. The novel compounds are selective muscarinic agonists of the m2 subtype with low activity at the m3 subtype. The compounds are effective for the treatment of glaucoma with fewer side effects than the pilocarpine therapy.
    Type: Grant
    Filed: October 28, 1996
    Date of Patent: February 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Wayne J. Thomspon, Pierre Mallorga, Richard W. Ransom, Ian M. Bell, Michael F. Sugrue, Peter M. Munson
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