Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, and an optionally substituted bicycloalkyl ring system at the 7-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.
Type:
Grant
Filed:
June 26, 2000
Date of Patent:
October 16, 2001
Assignee:
Merck Sharp & Dohme Limited
Inventors:
William Robert Carling, Kevin William Moore, Leslie Joseph Street
Abstract: A process for the preparation of metal sulphides includes reacting corresponding metal oxides at temperatures between 500 and 1500° C. in a stream of gaseous CS2 characterized in that the CS2 is generated from elementary carbon and gaseous H2S by reaction at temperatures between 900 and 1500° C. upstream of the metal oxide. The process furnishes metal sulphides of high purity, thus being of specific usefulness in optical glass materials, for, e.g., fiber optics.
Type:
Grant
Filed:
February 2, 1995
Date of Patent:
October 16, 2001
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Abstract: The present invention is directed to pyrrolidine compounds of the formula I:
(wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
Type:
Grant
Filed:
March 1, 2000
Date of Patent:
October 16, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Jianming Bao, Christopher Forbes, Shouwu Miao, William H. Parsons, Kathleen Rupprecht, Frank Kayser
Abstract: The invention relates to preparations of monodisperse spherical oxide particles in the form of free-flowing powders of agglomerates in which the particles are bonded to one another by a binder. With these preparations, the oxide particles can be homogeneously dispersed in polymer systems with particular ease.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
October 16, 2001
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Ralf Anselmann, Carsten Griessmann, Manuela Loch, Kurt Marquard
Abstract: DNA encoding human neuronal nicotinic acetylcholine receptor alpha and beta subunits, mammalian and amphibian cells containing the DNA, methods for producing &agr; and &bgr; subunits and isolated or substantially pure &agr;4, &agr;7 and &bgr;4 subunits are provided. In addition, cells that expresses these subunits singly or combination with other subunits of nicotinic acetylcholine receptors and methods using the cells are provided.
Type:
Grant
Filed:
December 21, 1998
Date of Patent:
October 16, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Kathryn J. Elliott, Steven B. Ellis, Michael M. Harpold
Abstract: Angiotensin II receptor antagonists are useful for decreasing QT dispersion or inhibiting the progression of QT prolongation in patients. Also disclosed is a method for monitoring the reduction in die risk of experiencing an adverse cardiac event, such as sudden cardiac death, myocardial infarction or arrhythmias, using QT dispersion in patients treated with a therapeutically effective amount of an angiotensin II antagonist.
Type:
Grant
Filed:
August 10, 2000
Date of Patent:
October 9, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Robert Segal, Paul J. Robinson, Lawrence I. Deckelbaum
Abstract: Anti-peptide antibody raised against a portion of human cytochrome P450 3A4 is disclosed. A particular anti-peptide antibody was raised against a 21-amino acid peptide corresponding to residues 253-273 of human cytochrome P450 3A4. High titer antibodies were produced by rabbits immunized with this peptide as judged by ELISA. This anti-peptide antibody is specific for human CYP3A4 and exhibited greater than 90-95% inhibition of testosterone 6&bgr;-hydroxylation, while other cytochrome P450-mediated reactions in human liver microsomes were not inhibited. An inhibitory epitope has been mapped within amino acids 261-267 of human CYP3A4.
Abstract: The present invention relates to a novel stabilized form of carbapenem antibiotics of formula II:
compositions and methods thereof wherein the antibiotics and compositions are stabilized degradation and dimer formation. The compounds can be used in the treatment of infectious diseases, including gram positive and negative, aerobic and anaerobic bacteria. The compounds provide good stability against beta-lactamases, and a favorable duration of action.
The compounds of this invention are represented structural formula I:
or a pharmaceutically acceptable or hydrate thereof.
Type:
Grant
Filed:
April 6, 1999
Date of Patent:
October 2, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Orn Almarsson, Michael J. Kaufman, John D. Stong, John M. Williams
Abstract:
The present invention relates to a process for the preparation of mopholine derivatives of formula (I) which are useful as a therapeutic agents.
Type:
Grant
Filed:
December 15, 2000
Date of Patent:
October 2, 2001
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Ian Frank Cottrell, Ulf H Dolling, David Hands, Robert Darrin Wilson
Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
Type:
Grant
Filed:
December 2, 1999
Date of Patent:
October 2, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Duggan, George D. Hartman, Michael A. Patane
Abstract: Composition for preparing water-repellent coatings on optical substrates, comprising a porous, electrically conductive molding and an organosilicon compound, obtainable by mixing an electrically conductive or semiconductive support material with a binder and subjecting the mixture to compression molding to form a compression molding, sintering the compression molding at preferably 1100 to 1500° C. in air to form a porous molding, impregnating the molding with the organosilicon compound, and ageing the impregnated molding by storage in air for at least 3 days.
Abstract: The present invention is directed to compounds which inhibit a prenyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting a prenyl-protein transferase and the prenylation of the oncogene protein Ras.
Type:
Grant
Filed:
October 6, 1998
Date of Patent:
October 2, 2001
Assignee:
Merck & Co., Inc.
Inventors:
S. Jane deSolms, John H. Hutchinson, Anthony W. Shaw, Samuel L. Graham, Terrence M. Ciccarone
Abstract: A compound of formula I, or a salt or prodrug thereof:
wherein:
Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl or di(C1-6)alkylamino, any of which groups may be optionally substituted;
R1 represents an optionally substituted five-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or
R1 represents an optionally substituted six-membered heteroaromatic ring selected from pyrazine, pyrimidine and pyridazine; and
R2 represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alky, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.
Type:
Grant
Filed:
November 12, 1998
Date of Patent:
October 2, 2001
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Tamara Ladduwahetty, Kevin John Merchant, Francine Sternfeld, Leslie Joseph Street
Abstract: The present invention relates to methods of inhibiting bone resorption comprising administering a therapeutically effective amount of a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor.
Abstract: The present invention relates to pigment mixtures containing at least two components, component A being Al2O3 flakes coated with one or more metals, metal oxides and/or metal sulfides and component B being one or more functional pigments, such as electrically conductive pigments, magnetic pigments, IR-reflective pigments or lasermarkable pigments, and to their use in varnishes, paints, printing inks, plastics and powder coatings.
Type:
Grant
Filed:
December 23, 1999
Date of Patent:
September 25, 2001
Assignee:
Merck Patent Gesellschaft mit Beschrankter Haftung
Inventors:
Gerhard Pfaff, Sabine Schoen, Kaiman Shimizu
Abstract: Compounds of formula I:
as well as pharmaceutically acceptable salts therefor and compositions useful as carbapenem antibacterial agents are disclosed.
Type:
Grant
Filed:
June 23, 1999
Date of Patent:
September 25, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Timothy A. Blizzard, Robert R. Wilkening, Ronald W. Ratcliffe
Abstract: Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.
Type:
Grant
Filed:
June 10, 1999
Date of Patent:
September 25, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Ravi P. Nargund, Brenda L. Palucki, Zhixiong Ye, Raman K. Bakshi, Arthur A. Patchett, Leonardus H. T. Van Der Ploeg
Abstract: A method for eliciting an &agr;v&bgr;5 or dual &agr;v&bgr;3/&agr;v&bgr;5 antagonizing effect in a mammal which comprises administering to the mammal a therapeutically effective amount of a compound of the formula
which are useful for inhibiting restenosis, angiogenesis, atherosclerosis, diabetic retinopathy, macular degeneration, inflammation or tumor growth.