Abstract: Compounds described by the chemical structural formula
or a pharmaceutically acceptable salt thereof, are useful in the treatment of pain, migraine, depression, anxiety, schizophrenia, Parkinson's disease, stroke, and in the treatment of neuropathies including postherpetic neuralgia, central pain from spinal cord injury, and phantom limb pain.
Type:
Grant
Filed:
June 25, 2001
Date of Patent:
August 27, 2002
Assignee:
Merck & Co., Inc.
Inventors:
David A. Claremon, John A. McCauley, Nigel J. Liverton, Cory R. Theberge
Abstract: The present invention relates to sulphonylexazolamines of general formula (I), wherein R1, R2 represent independently from each other H, A, —(CH2)n—Ar or alkenyl with 2-6 C atoms, R1 and R2 together also represent a mononuclear saturated heterocycle with 1-2 N, O and/or S atoms, Z is H, A, CF3, NO2, Hal, OH, OA, NH2, NHA or NH2. A represents alkyl with 1-6 C atoms, Ar is Z-monosubstituted or Z-disubstituted phenyl, Hal is F, Cl, Br, or L n is 1 or 2 of the physiologically acceptable salts or solvates thereof. Said sulphonyloxazolamines are used as therapeutic active ingredients. The invention also relates to the use of sulphonyloxazolamines as therapeutic active ingredients and/or to the production of pharmaceutical preparations to combat diseases of the central nervous system. The invention further relates to a pharmaceutical preparation and the production thereof.
Abstract: Polymorphic, amorphous and hydrated forms of the title compound having the following structure:
are disclosed. The compound is a potent and selective cyclooxygenase-2 (COX-2) inhibitor.
Abstract: Combinations of a GABAA alpha 5 inverse agonist and a COX-2 inhibitor, NSAID, estrogen or vitamin E are disclosed for treating neurodegenerative conditions such as Alzheimer's Disease.
Abstract: The invention relates to supertwist liquid-crystal displays (STN-LCDs) having short switching times and good steepnesses and angle dependencies, and to the novel nematic liquid-crystal mixtures used therein, which comprise compounds having a 3,4,5-trifluorophenyl group together with compounds of formula I
wherein
R3 is an alkenyl group with 2 to 7 C atoms,
R4 is an optionally fluorinated alkyl, alkoxy, alkenyl or alkenyloxy group with 1 to 12 C atoms, wherein one or two non-adjacent CH2 groups can be replaced by —O—, —CH═CH—, —CO—, —OCO— or —COO— in such a manner that O atoms are not directly adjacent to one another, or, in case m=1, R4 can also be Q—Y,
Q is CF2, OCF2, CFH, OCFH or a single bond,
Y is F or Cl,
L1 and L2 are each independently H or F, and
m is 0 or 1.
Type:
Grant
Filed:
November 19, 1999
Date of Patent:
August 27, 2002
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Abstract: Methods for identifying compounds which modulate the activity of human neuronal nicotinic acetylcholine receptors are provided. Invention methods employ DNAs encoding alpha and beta subunits of human neuronal nicotinic acetylcholine receptors, and the polypeptides encoded thereby. Test cells useful for conducting invention assays include mammalian and amphibian cells containing said DNA. Various combinations of subunits (i.e., one or more &agr;2, &agr;3, &agr;4, &agr;5, &agr;6 and &agr;7 subunits in combination with &bgr;2, &bgr;3 and/or &bgr;4 subunits) can be employed for the invention assays.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
August 27, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Kathryn J. Elliott, Steven B. Ellis, Michael M. Harpold
Abstract: Composite material for the screening of radiation, comprising a polymer, an additive and the customary stabilizers and processing aids necessary for the particular polymer. The additive is preferably an interference pigment.
Type:
Grant
Filed:
June 20, 1995
Date of Patent:
August 27, 2002
Assignees:
Merck Patent Gesellschaft MIT Beschrankter Haftung, Hyplast N.V.
Inventors:
Manfred Kieser, Gerhard Edler, Tony Leon Filip Daponte, Patrick Corneel Mathilde Verschaeren
Abstract: The present invention relates to the use, for the preparation of drugs to increase the survival rate of transplant patients, including renal and heart transplant patients, of a therapeutically effective amount of an angiotension II receptor antagonist compound, such as the class of substituted imidazoles represented by formula (I) and in particular by losartan potassium, 2-butyl-4-chloro-[(2′-tetrazol-5-yl)biphenyl-4-il]methyl]-5-(hydroxymethyl)imidazole potassium salt.
Abstract: The present invention relates to mixtures of fluoroalkylphosphate salts and polymers, methods of producing same, and their use in electrolytes, batteries, capacitors, supercapacitors and galvanic cells.
Type:
Application
Filed:
November 9, 2001
Publication date:
August 22, 2002
Applicant:
Merck GmbH
Inventors:
Michael Schmidt, Frank Ott, Michael Jungnitz, Nikolai Ignatyev, Andreas Kuehner
Abstract: Immunoregulatory compounds are disclosed of the formula:
as well as the pharmaceutically acceptable salts and hydrates thereof, are disclosed. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection.
Pharmaceutical compositions and methods of use are included.
Type:
Grant
Filed:
August 30, 2001
Date of Patent:
August 20, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Suzanne Mandala, James Bergstrom, Richard Hajdu, Hugh Rosen, William Parsons, Deborah J. Card, Malcolm Maccoss, Rupprecht Kathleen
Abstract: Compounds represented by formula I:
as well as pharmaceutically acceptable salts and hydrates thereof are disclosed as useful for treating or preventing diseases and conditions mediated by PDE-IV.
Pharmaceutical compositions and methods of treatment are also included.
Type:
Grant
Filed:
March 1, 2001
Date of Patent:
August 20, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Marc Labelle, Claudio Sturino, Nicolas Lachance, Dwight Macdonald
Abstract: Arylhydantoin derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
Type:
Grant
Filed:
September 27, 2000
Date of Patent:
August 20, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Jacob M. Hoffman, Mark G. Bock, Robert M. DiPardo, Linda S. Payne, Michael A. Patane
Abstract: Human papillomavirus virus-like particles (VLPs) are subjected to various maturation conditions, including incubation at higher temperatures, exposure to soluble metals or thios-oxidation. The resultant matured VLPs are more stable, and can be used to make a vaccine formulation with increased shelf life and higher potency.
Type:
Grant
Filed:
October 6, 2000
Date of Patent:
August 20, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Qinjian Zhao, Shilu Wu, Walter Manger, Shishir Gadam
Abstract: The present invention relates to the field of chemistry and more particularly to that of therapeutic chemistry.
The subject of the present invention is more precisely new 5-phenoxyalkyl-2,4-thiazolidinediones of general formula I:
in which
A represents a linear or branched alkylene group comprising from 2 to 16 carbon atoms
D represents a homo- or heterocarbon mono-, di- or tricyclic aromatic structure which may include one or more heteroatoms
X represents the substituent of the aromatic structure and is as defined in Claim 1
n is an integer ranging from 1 to 3
with the proviso that if A represents a butyl radical,
does not represent the 4-chlorophenyl group.
The invention also relates to the tautomeric forms, to the enantiomers, diastereoisomers and epimers of the compounds of general formula I, in free or salified form.
Type:
Grant
Filed:
December 7, 1998
Date of Patent:
August 20, 2002
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Abstract: Disclosed is a method for controlling phytopathogenic fungi using pure strains of Rosellinia subiculata ATCC 74386 and fungus ATCC 74387. Further, methods of producing a sordarin compound are disclosed. The method includes cultivating each strain separately in a nutrient medium containing assimilable sources of carbon and nitrogen and recovering the compound. A sordarin compound of formula I is also disclosed. Also an antifungal composition containing a sordarin compound is also disclosed.
Type:
Grant
Filed:
June 23, 1999
Date of Patent:
August 20, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Gerald F. Bills, Anne W. Dombrowski, Wendy S. Horn, Richard K. Jansson, Mark Rattray, Dennis Schmatz, Robert E. Schwartz
Abstract: A cosmetic preparation having butylmethoxydibenzoyhmethane as a protection filter and insoluble inorganic particles which are titanium dioxide particles doped with cerium or iron ions which absorb in the UVA region and are added to improve the photostability of the cosmetic preparation.
Type:
Grant
Filed:
May 8, 2000
Date of Patent:
August 20, 2002
Assignee:
Merck Patent Gesellschaft mit beschraenkter Haftung
Abstract: The invention relates to a liquid-crystalline medium based on a mixture of polar compounds of positive dielectric anisotropy, comprising one or more compounds of the general formula I
and simultaneously one or more compounds of the general formula II
in which R is H or an alkyl or alkoxy radical having 1 to 15 carbon atoms, Y is F, OCF3 or OCHF2, and simultaneously one or more compounds of the formula II in which R′, independently of the radical selected in the formula I, is as defined for R, and L is H or F.
Type:
Grant
Filed:
May 2, 2000
Date of Patent:
August 20, 2002
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Abstract: Reactive systems for polymerizing ethylenically unsaturated compounds comprising a first component, comprised of ethylenically unsaturated compounds capable of polymerization, and a second component of a hardener system comprised of organoboron compounds which are stabilized with suitable oligomers. An organic peroxide (perester, hydroperoxide, perether and/or peranhydride)is admixed with the compounds. These components are mixed to form a polymer. The reactive system reaches full strength in reduced time with the use of the organic peroxide and are suitable for joining hard body materials in human or animal tissue, in particular in the surgical and/or dental sector, in the production of body-absorbable or body-resistant adhesives, cements, and/or filling compounds and for forming synthetic material moldings.
Type:
Grant
Filed:
September 10, 1999
Date of Patent:
August 20, 2002
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Wolfgang Ritter, Robert Wenz, Peter Pokinskyj