Abstract: The present invention is concerned with novel processes for the preparation of (2S)-phenyl-3-piperidone. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
Abstract: The present invention is directed to compounds which inhibit prenyl-protein transferases, farnesyl-protein transferase and geranylgeranyl-protein transferase type I, and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and geranylgeranyl-protein transferase type I and the prenylation of the oncogene protein RAS.
Type:
Grant
Filed:
February 1, 2000
Date of Patent:
May 14, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Christopher J Dinsmore, John H. Hutchinson, Theresa M. Williams
Abstract: The present invention is directed to a pesticidal composition of a water-soluble pesticide and processes for its manufacture. More specifically, the invention relates to a soluble granule (SG) pesticidal formulation comprising a water-soluble pesticide and a water-soluble filler. The present invention provides a pesticidal formulation with efficacy equal to the corresponding liquid formulation, yet with improved handler safety, such as lower eye irritation.
Type:
Grant
Filed:
May 25, 1999
Date of Patent:
May 14, 2002
Assignee:
Merck & Co., Inc.
Inventors:
John Misselbrook, Robert F. Peterson, Jr.
Abstract: Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are 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:
May 14, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Ben E. Evans, Jacob M. Hoffman, Kevin F. Gilbert, Kenneth E. Rittle
Abstract: The invention relates to polymer beads comprising an anisotropic polymer material with helically twisted structure, to their use in reflective films, spraying or printing inks or as pigments, for optical or electrooptical, decorative or security applications, to a reflective film comprising one or more polymer beads in a transmissive binder, and to a security marking or security device comprising one or more polymer beads or comprising a reflective film.
Type:
Application
Filed:
September 18, 2001
Publication date:
May 9, 2002
Applicant:
MERCK PATENTGESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Inventors:
Mathias Kuntz, David Coates, Simon Greenfield, John Patrick
Abstract: The invention relates to a process for preparing electrically conductive pigments based on F−- and/or PO43−-doped tin mixed oxides applied as an electrically conductive layer to a substrate, in which, first of all, SnO2-coated substrates are prepared by precipitation and subsequent calcining and then, in further process steps, this SnO2 layer is converted into a tin mixed oxide layer doped with F− and/or PO43−. The invention further relates to electrically conductive pigments prepared by the process of the invention, to the use of these pigments for pigmenting lacquers, printing inks, plastics systems or coatings, and to lacquers, printing inks, plastics systems or coatings pigmented with an electrically conductive pigment prepared by the process of the invention.
Type:
Application
Filed:
October 19, 2001
Publication date:
May 9, 2002
Applicant:
MERCK PATENTGESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by direct compression/dry mix tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.
Type:
Application
Filed:
October 19, 2001
Publication date:
May 9, 2002
Applicant:
MERCK & Co., Inc.
Inventors:
Simon R. Bechard, Kenneth A. Kramer, Ashok V. Katdare
Abstract: Genes encoding Mycobacterium tuberculosis (M.tb) proteins were cloned into eukaryotic expression vectors to express the encoded proteins in mammalian muscle cells in vivo. Animals were immunized by injection of these DNA constructs, termed polynucleotide vaccines or PNV, into their muscles. Immune antisera was produced against M.tb antigens. Specific T-cell responses were detected in spleen cells of vaccinated mice and the profile of cytokine secretion in response to antigen 85 was indicative of a Th1 type of helper T-cell response (i.e., high IL-2 and IFN-&ggr;). Protective efficacy of an M.tb DNA vaccine was demonstrated in mice after challenge with M.bovis BCG, as measured by a reduction in mycobacterial multiplication in the spleens and lungs of M.tb DNA-vaccinated mice compared to control DNA-vaccinated mice or primary infection in naive mice.
Type:
Grant
Filed:
January 22, 1998
Date of Patent:
May 7, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Jean Content, Kris Huygen, Margaret A. Liu, Donna Montgomery, Jeffrey Ulmer
Abstract: The present invention relates to an azlactone-derivatized polyamide shaped article made by reacting at least one polyamide with a solution comprising an aza-bicyclo compound and a vinylazlactone derivative of the formula I
wherein R1, R2, R3, R4, and R5 are defined herein.
Type:
Grant
Filed:
January 6, 1999
Date of Patent:
May 7, 2002
Assignee:
Merck Patent Geselleschaft mit beschrankter
Abstract: The invention relates to a process for the preparation of monohalogenated 2-oxo-1,3-dioxolanes of the general formula
C3H3XO3 (I)
in which
X is Cl or Br,
characterized in that the monohalogenation is carried out starting from ethylene carbonate with sulfuryl dihalides under UV irradiation and in the absence of solvents.
Type:
Grant
Filed:
May 3, 2001
Date of Patent:
May 7, 2002
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Abstract: The invention relates to a process for the preparation of mineralized collagen fibrils, where the fibril formation and mineralization take place in one process step, and to the use thereof as bone substitute material. The collagen is recombinant collagen.
Abstract: cis-aminochromanols are obtained in high yield and with high selectivity over their trans counterparts by hydrogenating the corresponding oximes in the presence of a catalyst and an acid selected from HBr, HCl, and organic sulfonic acid. The cis-aminochromanols can be employed as intermediates in the production of HIV protease inhibitors which are useful for treating HIV infection and AIDS.
Type:
Grant
Filed:
May 11, 2001
Date of Patent:
May 7, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Ian Davies, Karl Hansen, Paul N. Devine, Louis Matty, Jr., Yuan Cheng, Philippe M. Rabbat
Abstract: The invention relates to a process for the preparation of mineralized collagen fibrils, where the fibril formation and mineralization take place in one process step, and to the use thereof as bone substitute material. The collagen is natural collagen.
Abstract: The invention describes a process for the production of a human cartilage implant from chondrocytes cultured in vitro, which come as close as possible to the original with respect to their biochemical composition and biomechanical properties. Up to 20% by vol. of human serum are used as medium addition in the process. The chondrocytes can be kept in monolayer culture until the 12th passage in order firstly to be re-differentiated, incubated under a reduced oxygen partial pressure, and subsequently stimulated to form a three-dimensional cartilage tissue due to aggregation under an oxygen partial pressure of 21%.
Abstract: Substituted 5-aryl-2,4-thiazolidinediones and oxazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr; and/or &ggr; mediated diseases, disorders and conditions.
Type:
Grant
Filed:
June 16, 2000
Date of Patent:
April 30, 2002
Assignee:
Merck & Co. Inc.
Inventors:
Ranjit C. Desai, Soumya P. Sahoo, Jeffrey P. Bergman, Victoria K. Lombardo, Edward J. Metzger, Hiroo Koyama
Abstract: In the present invention, viruses, plasmids or both are constructed which contain viral DNA and lox sites positioned such that site-specific recombination between lox sites in separate plasmids results in generation of infectious viral DNA at high-efficiency in cotransfected host cells that have been engineered to express the Cre recombinase. Because of the high-efficiency and specificity of the Cre enzyme, suitably engineered plasmids can be readily recombined to produce infectious virus at high-efficiency in cotransfected 293 cells, without, at the same time, producing wild-type adenovirus, with the attendant problems for removal thereof. Use of recombinases besides Cre and recombinase recognition sites besides lox sites, and use of cells other than 293 cells are also disclosed and enabled, as are kits incorporating the site-specific vector system, as well as compositions and methods for using such compositions as vaccines or in gene therapeutic applications.
Type:
Grant
Filed:
March 5, 1999
Date of Patent:
April 30, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Frank L. Graham, Robin J. Parks, Philip Ng