Patents Assigned to Merck
  • Thrombin inhibitors
    Patent number: 6087373
    Abstract: A compound which inhibits human thrombin and which has the general structure ##STR1##
    Type: Grant
    Filed: September 21, 1998
    Date of Patent: July 11, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Craig Coburn, Joseph P. Vacca, Peter D. Williams
  • Method of enhancing cognition with 2-(4-methoxyphenyl)-pyrazolo[4,3-c]quinolin-3-one
    Patent number: 6087372
    Abstract: The present invention provides the use of 2-(4-methoxyphenyl)-pyrazolo[4,3-c]quiniolin-3-one or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for enhancing cognition, particularly in Alzheimer's Disease, a method of enhancing cognition and pharmaceutically acceptable salts such as the hemi camphor sulfonate.
    Type: Grant
    Filed: May 25, 1999
    Date of Patent: July 11, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Gerard Raphael Dawson, Angus Murray MacLeod, Guy Ralph Seabrook
  • Optical coatings of medium refractive index
    Patent number: 6087014
    Abstract: The invention relates-to optical coatings of medium refractive index, having refractive index values of about 1.6 to 1.9, which can be obtained by vapor deposition of vapor-deposition materials having a chemical composition corresponding to the formula IYAl.sub.x O.sub.z Iwhereinx=0.5 to 5, andz=3/2.multidot.(1+x) on optical substrates.
    Type: Grant
    Filed: March 29, 1996
    Date of Patent: July 11, 2000
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventor: Reiner Dombrowski
  • Substituted imidazoles having anti-cancer and cytokine inhibitory activity
    Patent number: 6083949
    Abstract: Compounds represented by formula I: ##STR1## are disclosed. AR represents an aromatic group containing 6-10 atoms; and ##STR2## represents a 4 to 10 membered non-aromatic heterocycle containing at least one N atom, and optionally containing 1-2 additional N atoms and 0-1 O or S atom.A pharmaceutical composition is also included.Methods of treating cancer and cytokine mediated diseases are also included.
    Type: Grant
    Filed: January 26, 1998
    Date of Patent: July 4, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Nigel J. Liverton, Christopher F. Claiborne, David A. Claremon, Harold G. Selnick
  • Liquid-crystalline medium
    Patent number: 6083573
    Abstract: The invention relates to a liquid-crystalline medium based on a mixture of polar compounds having positive dielectric anisotropy, characterized in that it comprises one or more compounds of the general formula I ##STR1## in which R is H, an alkyl or alkenyl radical having 1 to 15 carbon atoms which is unsubstituted, monosubstituted by CN or CF.sub.3 or at least monosubstituted by halogen, it also being possible for one or more CH.sub.2 groups in these radicals to be replaced, in each case independently of one another, by --O--, --S-- ##STR2## --CO--, --CO--O--, --O--CO-- or --O--CO--O--in such a way that O atoms are not linked directly to one another,Y is F, Cl, halogenated alkyl, alkenyl or alkoxy having 1 to 6 carbon atoms, andL.sup.1 is F.
    Type: Grant
    Filed: February 26, 1998
    Date of Patent: July 4, 2000
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Kazuaki Tarumi, Brigitte Schuler, Eike Poetsch
  • Furanyl, tetracyclic triterpene derivatives with immunosuppressant activity
    Patent number: 6083980
    Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
    Type: Grant
    Filed: October 1, 1998
    Date of Patent: July 4, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Jianming Bao, Frank Kayser, Shouwu Miao, William H. Parsons, Kathleen M. Rupprecht
  • Nematic liquid crystal mixtures and a matrix liquid crystal display
    Patent number: 6083423
    Abstract: The invention relates to a nematic liquid crystal mixture having a positive dielectric anisotropy .DELTA..epsilon. of at least +4 and a birefringence .DELTA.n of at least 0.12, characterized in that the mixtures comprises one or more components having the core structure ##STR1## wherein L.sup.1, L.sup.2, Y and Z are each independently of one another H or F, one of Q.sup.1 and Q.sup.2 is 1,4-phenylene, 3-fluoro-1,4-phenylene or 3,5-difluoro-1,4-phenylene and the other residue Q.sup.1 or Q.sup.2 is --CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 -- or -- if at least one of L.sup.1, L.sup.2, Y and Z denotes F-- also a single bond, whereby this core structure can be optionally further fluorinated in the benzene rings.
    Type: Grant
    Filed: March 12, 1997
    Date of Patent: July 4, 2000
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Bernhard Rieger, Volker Reiffenrath, Reinhard Hittich
  • Adenovirus vectors generated from helper viruses and helper-dependent vectors
    Patent number: 6080569
    Abstract: The present invention provides an improved helper-dependent vector system for production of high capacity adenoviral cloning vectors. The invention makes use of the DNA size packaging constraints imposed on a pIX-defective Ad virion that prevent such virions from packaging DNA larger than approximately 35 kb. This constraint can be used to develop helper viruses that do not package their DNA. In one embodiment, the invention combines this methodology with the Cre-loxP helper-dependent system to decrease the quantity of contaminating helper virus in vector preparations. In another embodiment the invention is used for vector growth.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: June 27, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Frank L. Graham, Robin Parks, Liane Chen
  • Process for making phenyl heterocycles useful as COX-2 inhibitors
    Patent number: 6080876
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: September 17, 1998
    Date of Patent: June 27, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Ilias Dorziotis, Ioannis Houpis, Kan K. Eng
  • Biaryl substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
    Patent number: 6080870
    Abstract: The present invention is directed to compounds which inhibit farnesyl-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 farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: October 1, 1998
    Date of Patent: June 27, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, Gerald E. Stokker, John S. Wai, Theresa M. Williams, Wasyl Halczenko, John H. Hutchinson, Steven D. Young, Kelly M. Solinsky
  • STN liquid crystal display
    Patent number: 6080451
    Abstract: Supertwist liquid crystal displays (STN displays) of excellent characteristics are obtained if the nematic liquid crystal mixtures used therein comprise at least one compound of the formula IA ##STR1## and at least one compound of the formula IB ##STR2## in which R.sup.a, R.sup.b, Z, L.sup.a, L.sup.b, L.sup.c, L.sup.d, L.sup.e, L.sup.f, L.sup.g, L.sup.h, R.sup.3, R.sup.4 are as defined below.
    Type: Grant
    Filed: October 5, 1998
    Date of Patent: June 27, 2000
    Assignee: Merck Patent Gesellschaft Mit
    Inventors: Harald Hirschmann, Sven Schupfer, Volker Reiffenrath, Sabine Schoen
  • Fused tricyclic heteroaromatic derivatives as dopamine receptor subtype ligands
    Patent number: 6080745
    Abstract: A class of fused tricyclic heteroaromatic compounds of formula (I) as defined in claim 1 or a salt thereof or a prodrug thereof, containing a fused pyrazole, oxazole or pyrimidine ring are ligands for dopamine receptor subtypes within the body and are therefore of use in the treatment and/or prevention of disorders of the dopamine system, such as schizophrenia.
    Type: Grant
    Filed: March 12, 1996
    Date of Patent: June 27, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventors: William Barnaby Davey, Paul David Leeson, Michael Rowley
  • Spiro-ketal derivatives and their use as therapeutic agents
    Patent number: 6080740
    Abstract: The present invention is directed to spiro-ketal derivatives of the formula (I): ##STR1## (wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9a, R.sup.9b, m and n are defined herein) which are tachykinin antagonists and are useful, for example, in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: August 13, 1998
    Date of Patent: June 27, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jonathan David Moseley, Christopher John Swain
  • Process for synthesizing carbapenem intermediates
    Patent number: 6080854
    Abstract: A process of synthesizing a compound of formula I is described: ##STR1## wherein P and P' independently represent H or a protecting group, R.sub.1 represents H or C.sub.1-4 alkyl, and Hal represents a halogen characterized by reacting a compound of formula 2: ##STR2## with R.sub.2 OH, wherein R.sub.2 is C.sub.1-4 alkyl, C.sub.6-10 aryl or C.sub.5-10 heteroaryl in the presence of an acid catalyst or carbodiimide reagent to produce a compound of formula 3: ##STR3## and reacting a compound of formula 3 in the presence of a base and a haloalkylating agent to produce a compound of formula 1.
    Type: Grant
    Filed: July 27, 1998
    Date of Patent: June 27, 2000
    Assignee: Merck & Co., Inc.
    Inventors: John Y. Chung, Nobuyoshi Yasuda, Johnnie L. Leazer, Jr.
  • Electro-optical liquid-crystal display
    Patent number: 6080452
    Abstract: The invention relates to an electro-optical liquid-crystal display having a realignment layer for realigning the liquid crystals whose field has a significant component parallel to the liquid-crystal layer and which contains a liquid-crystalline medium of positive dielectric anisotropy, where the medium comprises at least one mesogenic compound of the formula II ##STR1## in which R.sup.1 is H, an alkyl or alkenyl radical having 1 to 15 carbon atoms which is unsubstituted or monosubstituted or polysubstituted by halogen and in which one or more CH.sub.2 groups may each, independently of one another, be replaced by --O--, --S--, --CO--, --COO--, --OCO-- or --OCO--O-- in such a way that O atoms are not linked directly to one another.
    Type: Grant
    Filed: May 27, 1999
    Date of Patent: June 27, 2000
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Kazuaki Tarumi, Andreas Beyer, Eike Poetsch
  • Alpha 1A adrenergic receptor antagonists
    Patent number: 6080760
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds 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 are achieved.
    Type: Grant
    Filed: June 17, 1998
    Date of Patent: June 27, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Michael A. Patane, Mark G. Bock
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6077853
    Abstract: The present invention is directed to compounds which inhibit farnesyl-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 farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: April 28, 1999
    Date of Patent: June 20, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Samuel L. Graham, Steven D. Young
  • Antidiabetic agents
    Patent number: 6077849
    Abstract: Compounds of formula I: ##STR1## as well as tautomers, pharmaceutically acceptable salts, hydrates, prodrugs and reduced forms are disclosed. The compounds are useful for the treatment and prevention of diabetes mellitus, and in particular, for the treatment or prevention of hyperglycemia in diabetic patients.
    Type: Grant
    Filed: March 29, 1999
    Date of Patent: June 20, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Kun Liu, Harold B. Wood, Anthony B. Jones, Bei Zhang
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6077847
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: March 25, 1999
    Date of Patent: June 20, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6077858
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: September 21, 1999
    Date of Patent: June 20, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Feroze Ujjainwalla, Thomas F. Walsh, Matthew J. Wyvratt, Jr., Jonathan R. Young, Lin Chu