Abstract: The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.
Type:
Grant
Filed:
October 21, 1999
Date of Patent:
October 16, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Jianming Bao, Andrew Kotliar, Frank Kayser, William H. Parsons, Kathleen M. Rupprecht, Christopher F. Claiborne, David A. Claremon, Nigel Liverton, Wayne J. Thompson
Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, represented by
wherein Z represents cyclobutyl or pyrrolidin-1-yl, 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 28, 2000
Date of Patent:
October 16, 2001
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Timothy Harrison, Andrew Madin, Martin Richard Teall
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 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: The invention relates to acetylene derivatives of the formula I
in which n, m, R1, R2, X1, X2, X3, X4, Z1, Z2, A1, A2, Q, Y1 and Y2 are as defined below, wherein at least one of the groups X1, X2, X3 and X4 is —C≡C—R3, R3 is H, alkyl(C1-C8), Cl, CN, SF5 or CF3.
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: 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: 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: 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:
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 methods of inhibiting bone resorption comprising administering a therapeutically effective amount of a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor.
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.
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: There is disclosed a method for continuously monitoring temperature at multiple locations within a controlled temperature unit (CTU) using RTDs that can be removed and reinserted. The key to the method is the collection of data using an RTD fixed in a phenolic thermowell, which in turn is inserted through a polytetrafluoroethylene-coated sleeve in the wall of the CTU. The temperature information is transmitted from a data module to an interfaced computer system where it may be presented to the operator in a graphical, tabular or text format or stored in memory. The temperature probes are easily removable so as to facilitate calibration without disruption of the contents of the CTU and can be consistently replaced in the same location within the CTU.
Type:
Grant
Filed:
October 26, 1999
Date of Patent:
September 25, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Fred J. Bailey, Mark Pinder, Carl W. Holz
Abstract: This invention is directed to compounds and ligands that bind to peroxisome proliferator activated receptors (PPAR) &ggr;1 and &ggr;2 and which function as antiproliferative, antiviral and antitumour agents. The invention is also directed to the use of PPAR &ggr;1 and &ggr;2 to identify such compounds and methods of using the compounds for medical uses.