Abstract: DNA encoding human neuronal nicotinic acetylcholine receptor alpha and beta subunits, mammalian and amphibian cells containing said DNA, methods for producing alpha and beta subunits and recombinant (i.e., isolated or substantially pure) alpha subunits (specifically &agr;6) and beta subunits (specifically &bgr;3) are provided. In addition, combinations of a plurality of subunits (i.e., one or more of as &agr;1, &agr;2, &agr;3, &agr;4, &agr;5, &agr;6 and/or &agr;7 subunits in combination with one or more of &bgr;3 subunits are provided.
Abstract: The present invention involves a process for preparing a stable final formulation product of a compound of formula I,
or its pharmaceutically acceptable salt, hydrate or solvate by incorporating a suitable carbon dioxide source to an unstable monosodium adduct of carbapenem antibiotic compound.
Type:
Grant
Filed:
April 27, 2001
Date of Patent:
November 26, 2002
Assignee:
Merck & Co., Inc.
Inventors:
William A. Hunke, Kathleen J. Illig, Anand Kanike, Scott D. Reynolds, Stelios C. Tsinontides, Anthony S. Al-Dehneh, Hiren S. Patel
Abstract: A COX-2 selective inhibiting drug is disclosed as useful in treating or preventing prostate cancer. The compound is used alone or in combination with other drugs.
Type:
Grant
Filed:
January 26, 2001
Date of Patent:
November 26, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Joanne Waldstreicher, Briggs W. Morrison
Abstract: The invention relates to an injectable curable bone cement paste based on bioresorbable hydroxyapatite-like compounds comprising calcium phosphate, which contains a cationic antibiotic in the form of a salt, preferably of its sulfate, the curable biodegradable bone cement releasing the antibiotic in biologically active concentrations with depot-like action over a long period of time. The bone cements according to the invention are suitable for the treatment of infectious inflammations of the bone and of the bone marrow, in particular as a result of bone defects and bone fractures.
Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme.
The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and conditions related to diabetes.
Type:
Grant
Filed:
December 21, 2000
Date of Patent:
November 26, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Yves Leblanc, Claude Dufresne, Jacques Yves Gauthier, Cheuk Kun Lau, Chun Sing Li, Patrick Roy, Michel Therien, John Scheigetz, Zhaoyin Wang
Abstract: Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors.
Type:
Application
Filed:
March 20, 2002
Publication date:
November 21, 2002
Applicant:
Merck Frosst Canada & Co.
Inventors:
Richard Freisen, Yves Ducharme, Bernard Cote, Marc Blouin, Evelyn Martins, Daniel Guay, Pierre Hamel, Mario Girard, Richard Frenette, Sebastien Laliberte
Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
Type:
Grant
Filed:
May 21, 2001
Date of Patent:
November 19, 2002
Assignee:
Merck & Co., Inc.
Inventors:
William K. Hagmann, George A. Doherty, Shrenik Shah
Abstract: Acetonides are obtained in a one-step reaction of a carboxylic acid halide, a 1,2-aminoalcohol, and 2-alkoxypropene or 2,2-dialkoxypropane in an ether solvent and in the presence of an inorganic base. Acetonides are also obtained in a two-step reaction scheme in which an acid halide and 1,2-aminoalcohol are reacted in an ether solvent in the presence of LiOH to form a hydroxyamide, which is then reacted with 2-alkoxypropene or 2,2-dialkoxypropane in the presence of acid to form the acetonide. The acetonides resulting from the one-step and two-step protocols can be further reacted with an allylating agent such as an allyl halide in the presence of a strong base to provide the corresponding allyl acetonide. The acetonides and allyl acetonides can serve as intermediates in the production of certain HIV protease inhibitors which are useful for treating HIV infection and AIDS.
Type:
Grant
Filed:
June 18, 2001
Date of Patent:
November 19, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Steven J. Cianciosi, Gregory L. Tewalt, Eric T. Pisk, Ilia A. Zavialov, Glenn A. Hulvey
Abstract: Arylalkanoylpyridazine derivatives of the formula I
and the physiologically acceptable salts thereof in which R1, R2, R3, R4, Q and B have the meanings given in Claim 1 act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumors, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases and AIDS.
Type:
Grant
Filed:
March 15, 2000
Date of Patent:
November 12, 2002
Assignee:
Merck Patent Gesellschaft Mit Beschraenkter Haftung
Inventors:
Jonas Rochus, Norbert Beier, Franz-Werner Kluxen, Michael Wolf
Abstract: Compounds according to Formula (I) or a salt thereof are selective antagonists of the human 5-HT2A receptor useful for treatment of adverse conditions of the central nervous system:
Type:
Grant
Filed:
January 12, 2001
Date of Patent:
November 12, 2002
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Christopher Richard Moyes, Michael Rowley
Abstract: The present invention is directed to certain novel compounds represented by structural formula I:
or a pharmaceutically acceptable salt thereof, wherein R3, R5, R6, R7, R8, R11, R12, R13, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.
Type:
Grant
Filed:
September 21, 2001
Date of Patent:
November 12, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Paul E. Finke, Laura C. Meurer, Sander G. Mills, Malcolm MacCoss, Hongbo Qi
Abstract: Substituted or 6,7-ring fused 1,2,3-triazolo[4,5-b]pyridine derivatives are selective ligands for GABAA receptors useful in the treatment of disorders of the central nervous system.
Type:
Grant
Filed:
November 7, 2000
Date of Patent:
November 12, 2002
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Howard Barff Broughton, Jose Luis Castro Pineiro, Ian James Collins, Leslie Joseph Street
Abstract: Michael addition conducted in the presence of a zinc-amine complex and additional amounts of the amine component results in product with high diastereomeric excess.
Type:
Grant
Filed:
April 7, 2000
Date of Patent:
November 12, 2002
Assignees:
Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd,
Inventors:
Ioannis Houpis, Ralph P. Volante, Fengrui Lang, Ilias Dorziotis, David Tschaen, Shinji Kato, Toshiaki Mase
Abstract: The invention concerns a method for the immunological determination of an analyte in a sample using magnetic particles coated with the analyte to be determined or analyte-specific bonding partners and directly detectable non-magnetic particles coated with analyte-specific bonding partners or the analyte to be determined or using a non-magnetic substance which is indirectly detectable, and incubation of the reaction mixture. The method is characterized in that the magnetic particles are subsequently separated from the reaction mixture using a magnetic test strip and the analyte concentration is determined directly.
Abstract: Crystalline 2S-cis-3-[[(4-mercapto-2-pyrrolidinyl)carbonyl]-amino]benzoic acid and salts and solvates thereof are disclosed. A crystalline type is described.
Type:
Grant
Filed:
February 28, 2001
Date of Patent:
November 12, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Karel J. M. Brands, Karen M. Conrad, John M. Williams
Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
Type:
Grant
Filed:
October 17, 2000
Date of Patent:
November 12, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Fraley, Scott R. Hambaugh, Randall W. Hungate
Abstract: The invention relates to methods for separating biological contaminants (viruses, nucleic acids and/or endotoxins) from biological products, or for reducing the content of such biological contaminants in said biological products. The sample (biological product) to be purified is treated with an anion exchanger membrane. Said anion exchanger membrane is obtained by reacting a polyamide with an aminoreactive compound which is capable of polymerisation. This is followed by polymerisation with monomers which contain cationic groups or into which cationic groups can be introduced in a reaction analogous to polymerisation.
Abstract: The invention relates to a method for disubstituting carboxylic acid amides on a geminal carbonyl-C-atom using a Grignard reagent in the presence of an organotitanate.
Type:
Grant
Filed:
March 23, 2001
Date of Patent:
November 12, 2002
Assignee:
Merck Patent Gesellschaft
Inventors:
Herwig Buchholz, Urs Welz-Biermann, Armin Meijere, Vladimir Chaplinski
Abstract: The present invention relates compounds of the formula (I):
wherein
Z is —CR9R10CH2— or —CH2CR9R10—;
and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
Type:
Grant
Filed:
April 1, 2002
Date of Patent:
November 12, 2002
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Ian Thomas Huscroft, Janusz Jozef Kulagowski, Piotr Antoni Raubo