Abstract: The invention relates to a process for the preparation of cyclic carboxylic acid orthoester fluorides in which a) at least one bis(alkylthio)carbenium salt is reacted with at least one organic compound containing at least two hydroxyl groups in the presence of at least one base, b) and subsequently, preferably in situ, the resultant thioorthoester is subjected to oxidative fluorodesulfurisation using a fluorinating agent and an oxidant to give the cyclic carboxylic acid orthoester fluoride.
Abstract: The invention relates to 2,4?-substituted 6-cyclohexyl-trans-decalins of the general formula I in which R1, R2 and Z are as defined in Claim 1, to the use thereof as components of liquid-crystalline media, and to a liquid-crystal display element and an electro-optical display element.
Type:
Grant
Filed:
March 22, 2002
Date of Patent:
July 12, 2005
Assignee:
Merck Patent GmbH
Inventors:
Matthias Bremer, Detlef Pauluth, Georg Lüssem
Abstract: The present invention relates to cyclic urea derivatives, their synthesis, and their use as ?v integrinreceptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ?v?3 and/or ?v?5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, tumor growth and metastasis.
Abstract: A class of imidazo[1,2-?]pyrazine analogues substituted in the 3-position by a substituted phenyl ring, being selective ligands for GABAA receptors which interact more favourably with the ?2 and/or ?3 subunit than with the ?1 subunit, are accordingly of benefit in the treatment and/or prevention of a variety of disorders of the central nervous system, including anxiety and convulsions, with a reduced propensity to cause sedation.
Type:
Grant
Filed:
July 18, 2001
Date of Patent:
July 5, 2005
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Simon Charles Goodacre, David James Hallett, Leslie Joseph Street
Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
Type:
Grant
Filed:
February 10, 2003
Date of Patent:
July 5, 2005
Assignee:
Merck & Co. Inc.
Inventors:
Maria L. Garcia, Gregory J. Kaczorowski, Owen B. McManus
Abstract: A class of 3-phenylimidazo[1,2-c]pyrimidine derivatives, of the formula I: (wherein R1, X, Y, and Z are defined herein) are selective ligands for GABA-A receptors and are useful in the treatment or prevention of adverse conditions of the central nervous system, including anxiety and convulsions.
Type:
Grant
Filed:
November 8, 2001
Date of Patent:
July 5, 2005
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
David James Hallett, Michael Geoffrey Neil Russell, Leslie Joseph Street
Abstract: The invention relates to new reactive mesogenic benzodithiophene derivatives, their use as semiconductors or charge transport materials, in optical, electro-optical or electronic devices like for example liquid crystal displays, optical films, organic field effect transistors (FET or OFET) for thin film transistor liquid crystal displays and integrated circuit devices such as RFID tags, electroluminescent devices in flat panel displays, and in photovoltaic and sensor devices, and to a field effect transistor, light emitting device or ID tag comprising the reactive mesogenic benzodithiophenes.
Type:
Grant
Filed:
April 24, 2003
Date of Patent:
July 5, 2005
Assignee:
Merck Patent GmbH
Inventors:
Louise Farrand, Martin Heeney, Steven Tierney, Mark Giles, Marcus Thompson, Maxim Shkunov, David Sparrowe, Iain McCulloch
Abstract: Scramblase 2 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing scramblase 2 polypeptides and polynucleotides in diagnostic assays.
Type:
Grant
Filed:
June 11, 2001
Date of Patent:
July 5, 2005
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Silke Brandt, Johannes Gleitz, Klaus Duecker
Abstract: The present invention relates to imidazo[2,1-f]triazin-4-one analogues which are substituted in the 7-position by a substituted phenyl ring, being ligands for GABAA receptors and accordingly of benefit in the therapy of deleterious neurological disorders.
Abstract: A process is provided for the preparation of 2,5-di-(3?-aminopropyl)pyridine which is useful in the synthesis of ?v?3 integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
Abstract: The invention relates to an optical compensator for liquid crystal displays comprising: at least one O plate retarder (3, 3?), and at least one twisted A plate retarder (6, 6?) with a twist angle ? of more than 90°, and further relates to a liquid crystal display comprising such a compensator, a liquid crystal cell (1) and polarizers (2, 2?).
Type:
Grant
Filed:
September 13, 2000
Date of Patent:
June 28, 2005
Assignee:
Merck Patent GmbH
Inventors:
David Coates, Owain Llyr Parri, Mark Verrall, Peter Le Masurier
Abstract: A tamper-evident label suitable for placement onto a container and cap assembly. The label may be characterized as a planar sheet having a tear strip that divides upper and lower panels. The lower panel of the label attaches to the container, while the upper panel, defined by at least one tab, and preferably two tabs, is attached to the cap. To open the container and cap assembly, the tear strip is pulled across the label to separate the two panels of the label. Thereafter, the cap may be removed from the container to reveal the contents of the container.
Type:
Grant
Filed:
August 15, 2002
Date of Patent:
June 21, 2005
Assignee:
Laboratories Merck Sharp and Dohme-Chibret, SNC
Abstract: 2-Quinoxalinone derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
Abstract: In one aspect, the present invention is directed to a one pot method of preparing intermediates of Formula V, which are useful in making inhibitors of phosphodiesterase-4: The present invention is also directed to a method of preparing phosphodiesterase inhibitors comprising the Formula
Type:
Grant
Filed:
October 21, 2003
Date of Patent:
June 21, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Jennifer Albaneze-Walker, Scott Ceglia, Jerry Anthony Murry, Arash Soheili
Abstract: The invention relates to liquid-crystalline compounds of the formula I and to a liquid-crystalline medium based on a mixture of polar compounds, characterized in that it comprises one or more compounds of the general formula I in which R1, L1, L2, L3, L4, L5, L6, Z1, Z2, X, v and u are as defined in claim 1.
Type:
Grant
Filed:
September 30, 2003
Date of Patent:
June 21, 2005
Assignee:
Merck Patent GmbH
Inventors:
Peer Kirsch, Marc Lenges, Michael Heckmeier
Abstract: Compounds of Formula I and the pharmaceutically acceptable salts and esters thereof, wherein Z is selected from the group consisting of: (a) Formula Ia ?and (b) Formula Ib are novel LXR agonists and are useful in the treatment of dyslipidemic conditions particularly depressed levels of HDL cholesterol.
Type:
Grant
Filed:
May 30, 2002
Date of Patent:
June 21, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Alan D. Adams, Aileen Bouffard, James F. Dropinski, Clare E. Gutteridge, A. Brian Jones, Weiguo Lui, John George Ondeyka, Ali Shiafee, Sheo Bux Singh
Abstract: The invention relates to a novel purified recombinant ?V?3 adhesion receptor which shows an unimpaired ligand binding activity, and a process for preparing said soluble non-membrane bound receptor in excellent yields by recombinant techniques using a baculovirus-insect cell expression system. The so-synthesized soluble receptor may be used very easily as screening tool for new therapeutic compounds which may inhibit the natural ?v?3 adhesion receptor. Such therapeutic compounds which can be discovered very easily, fast and without health risk by means of the souluble receptors according to the invention may be, for example, RGD peptides or non-peptidic compounds mimicking the natural ligand epitopes. The invention relates, furthermore, to a corresponding process for preparing recombinant full-length ?V?3 adhesion receptor in excellent yields, additionally using detergents to dissolve the membrane bound receptor from the surface of the host cell.
Type:
Application
Filed:
October 31, 2003
Publication date:
June 16, 2005
Applicant:
Merck Patent GmbH
Inventors:
Simon Goodman, Beate Dieffenbach, Detlef Gussow, Raj Mehta, Eilish Cullen, Alex Brown
Abstract: Compounds of the formula (1), in which R1, R2?, R2?, R2??, R3 and n are as defined in claim 1, are effectors of the nicotinic and/or muscarinic acetylcholine receprot and are suitable for the prophylaxis or treatment of schizophrenia, depression, anxiety states, dementia, Alzheimer's disease, Lewy bodies dementia, neurodegenerative diseases, Parkinson's disease, Huntington's disease, Tourette's syndrome, learning and memory impairments, age-related memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds.
Type:
Application
Filed:
December 17, 2002
Publication date:
June 16, 2005
Applicant:
Merck Patent GmbH
Inventors:
Gunter Holzemann, Helmut Prucher, Kai Schiemann, Joachim Leibrock, Hartmut Greiner, Christa Burger, laurie von Melchner
Abstract: A liquid-crystalline medium comprises one or more compounds of the general formula (I) CF3O-a-b-c-F??(I) in which a, b, c may each denote, independently of one another, and further liquid-crystalline compounds.