Abstract: Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors.
Type:
Grant
Filed:
March 20, 2002
Date of Patent:
January 11, 2005
Assignee:
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: The invention relates to new conjugated mono-, oligo- and polydithienopyridines, their use as semiconductors or charge transport materials in optical, electrooptical or electronic devices including field effect transistors, electroluminescent, photovoltaics, sensors and electrophotographic recording devices, and to a field effect transistor as a component of integrated circuitry, as a thin fim transistor in flat panel display applications or for RFID tags, or a semiconducting component in organic light-emitting diode applications, comprising the new mono-, oligo and polydithienopyridines.
Type:
Grant
Filed:
July 9, 2002
Date of Patent:
January 11, 2005
Assignee:
Merck Patent Gesellschaft Mit Beschraenkter
Inventors:
Martin Heeney, Steven Tierney, Marcus Thompson, Mark Giles, Louise Farrand, Maxim Shkunov, David Sparrowe, Iain McCulloch
Abstract: Compounds of the formula I in which R1, R2, R4 and R5 have the meanings indicated in claim 1, are potent 5-HT2A antagonists and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkingson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia, nervous anorexia, premenstrual syndrome and/or for positively affecting compulsive behavior (obsessive-compulsive disorder, OCD).
Abstract: The present invention is directed to the radioligand compound, [35S]-radiolabeled (+)-N-[1?-(6-cyano-1,2,3,4-tetrahydro-2(R)-naphthalenyl)-3,4-dihydro-4(R)-hydoxyspiro[2H-1-benzopyran-2,4?-piperidin]-6-yl]methanesulfonamide. Also within the scope of this invention is a method for identifying compounds that bind to the IKr channel, and may have antiarrhythmic activity.
Type:
Grant
Filed:
July 12, 2001
Date of Patent:
January 4, 2005
Assignee:
Merck & Co., Inc.
Inventors:
John W. Butcher, David A. Claremon, Thomas M. Connolly, Jerzy Karczewski, Kenneth S. Koblan, Matthew J. Kostura, Nigel J. Liverton, Dennis C. Dean, David G. Melillo
Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
Type:
Grant
Filed:
May 6, 2002
Date of Patent:
January 4, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Timothy Allen Blizzard, Milton Lloyd Hammond, Jerry Dwain Morgan, Ralph Troy Mosley
Abstract: The invention includes mouse serotonin 5-HT2c receptor isoforms having amino acid replacements at one or more positions of the natural mouse serotonin 5-HT2c receptor polypeptide sequence, specifically at one or more of positions 157, 159 and 161. The polypeptides are useful for identifying ligands which bind with the serotonin 5-HT2c receptor and modulators of the serotonin 5-HT2c, and for identifying drugs with affinity for 5-HT2 receptors which are used to treat schizophrenia, Parkinsonism, and anxiety disorders.
Type:
Grant
Filed:
December 17, 2002
Date of Patent:
December 28, 2004
Assignee:
Merck & Company, Inc.
Inventors:
Tong M. Fong, Jie Liu, Leonardus H.T. Van Der Ploeg
Abstract: Iodohydroxylated olefins can be prepared by treating an olefin with an aqueous solution of an iodine monohalide selected from iodine monochloride and iodine monobromide.
Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Type:
Grant
Filed:
August 23, 2002
Date of Patent:
December 28, 2004
Assignees:
Merck Frosst Canada & Co., Banyu Pharmaceutical Co., Ltd., Axys Pharmaceuticals, Inc.
Abstract: The present invention relates to a system for the processing of order transactions with a data memory, a recording device which is provided to record order data from a purchaser, a processing unit for the storage of recorded order data in the data memory. Furthermore, the present invention relates to a method for the processing of order transactions between a supplier and a purchaser, which has the steps of the recording of order data which consist of individual data fields, and transmission by the purchaser to the supplier, the creation of a file which contains data fields which represent at least some of the order data and the transmission of the file to the purchaser.
Abstract: The invention relates to a liquid-crystalline medium based on a mixture of polar compounds of positive dielectric anisotropy, characterized in that it comprises one or more compounds of the formula I
in which R1, L1 and L2 are as defined in claim 1.
Type:
Grant
Filed:
May 27, 2003
Date of Patent:
December 7, 2004
Assignee:
Merck Patent GmbH
Inventors:
Michael Heckmeier, Brigitte Schuler, Izumi Saito, Volker Reiffenrath, Georg Luessem, Christian Hock
Abstract: The invention relates to a liquid-crystalline medium with positive dielectric anisotropy and high optical anisotropy, characterized in that it contains one or more biphenyl derivatives comprising a terminal alkenyl group, and its use in electrooptical displays and projection systems, in particular reflective displays and displays based on a birefringence effect, such as OCB displays.
Abstract: A class of substituted 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-methoxy moiety at the 6-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
Type:
Grant
Filed:
June 17, 2003
Date of Patent:
December 7, 2004
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
William Robert Carling, Jose Luis Castro Pineiro, Ian James Collins, Alexander Richard Guiblin, Timothy Harrison, Andrew Madin, Kevin William Moore, Michael Geoffrey Russell, Gayle Scott, Leslie Joseph Street
Abstract: The invention relates to new mono-, oligo- and poly-difluorovinyl(hetero)arylenes comprising one or more identical or different recurring units of formula I
wherein D, D′, Ar, a and b have the meanings as defined in herein. Furthermore the inventions relates to their synthesis, their use as semiconductors or charge transport materials and their different applications.
Type:
Grant
Filed:
July 24, 2002
Date of Patent:
November 30, 2004
Assignee:
Merck Patent Gesellschaft mit beschrank Haftung
Inventors:
Martin Heeney, Louise Farrand, Mark Giles, Marcus Thompson, Steven Tierney, Maxim Shkunov, David Sparrowe, Iain McCulloch
Abstract: In accordance with the present invention, there are provided nucleic acids encoding human NMDA receptor protein subunits and the proteins encoded thereby. The NMDA receptor subunits of the invention comprise components of NMDA receptors that have cation-selective channels and bind glutamate and NMDA. In one aspect of the invention, the nucleic acids encode NMDAR1 and NMDAR2 subunits of human NMDA receptors. In a preferred embodiment, the invention nucleic acids encode NMDAR1, NMDAR2A, NMDAR2B, NMDAR2C and NMDAR2D subunits of human NMDA receptors. In addition to being useful for the production of NMDA receptor subunit proteins, these nucleic acids are also useful as probes, thus enabling those skilled in the art, without undue experimentation, to identify and isolate related human receptor subunits.
Abstract: The invention relates to a liquid-crystalline medium of positive dielectric anisotropy, characterized in that it comprises in each case one or more compounds of the general formulae I, II and IV
in which the parameters are as defined in the text, and to the use thereof as a constituent of a multibottle system and in electro-optical displays, and to multibottle systems of this type and displays which contain this medium.
Abstract: Process for the preparation of the cyclic pentapeptide
cyclo(Arg-Gly-Asp-DPhe-NMeVal)
by cyclization of a linear pentapeptide selected from the group consisting of
H-Arg(Pbf)-Gly-Asp(OBzl)-DPhe-NMeVal-OH,
H-Gly-Asp(OBzl)-DPhe-NMeVal-Arg(Pbf)-OH,
H-Asp(OBzl)-DPhe-NMeVal-Arg(Pbf)-Gly-OH,
H-DPhe-NMeVal-Arg(Pbf)-Gly-Asp(OBzl)-OH or
H-NMeVal-Arg(Pbf)-Gly-Asp (OBzl)-DPhe-OH,
subsequent protective group removal and, if appropriate, further conversion into its physiologically acceptable salts.
Abstract: A liquid-crystalline mixture that contains one or more compounds of each of the formulae IA, IB and IC
and to the use thereof in TN, STN and IPS displays.
Type:
Grant
Filed:
July 26, 2002
Date of Patent:
November 23, 2004
Assignee:
Merck Patent GmbH
Inventors:
Harald Hirschmann, Volker Reiffenrath, Marcus Reuter, Sabine Schoen, Sven Schüpfer, Clarissa Weller
Abstract: The invention relates to a method and an apparatus for the on-line analysis of liquid substance mixtures by means of NIRS. For evaluation by spectral data comparison, merely the binary mixtures of the possible components in quantitative graduations are used as calibration spectra. In order to accelerate the evaluation, all data points of a spectrum are summated, and each spectrum is characterized by only one characteristic number.
Type:
Grant
Filed:
October 16, 2002
Date of Patent:
November 16, 2004
Assignee:
Merck Patent GmbH
Inventors:
Hans Frickel, Hanshelmut Itzel, Joachim Born
Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
Type:
Grant
Filed:
February 3, 2003
Date of Patent:
November 16, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Feroze Ujjainwalla, Lin Chu, Mark T. Goulet, Bonnie Louridas, Matthew J. Wyvratt, Daniel Warner