Patents Assigned to Merck
  • DNA encoding triol polyketide synthase
    Patent number: 6174706
    Abstract: DNA encoding triol polyketide synthase (TPKS) has been isolated, purified and sequenced. Expression vectors comprising TPKS, cells transformed with the expression vectors, and processes employing the transformed cells are provided.
    Type: Grant
    Filed: January 8, 1998
    Date of Patent: January 16, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Victor A. Vinci, Michael J. Conder, Phyllis C. McAda, Christopher D. Reeves, John Rambosek, Charles Ray Davis, Lee E. Hendrickson
  • Asymmetric conjugate addition reaction
    Patent number: 6172235
    Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.
    Type: Grant
    Filed: April 27, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
  • Inhibitors of prenyl-protein transferase
    Patent number: 6172076
    Abstract: The present invention is directed to conformationally constrained compounds which inhibit prenyl-protein transferase 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 prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Mark W. Embrey, John S. Wai, Debra S. Perlow, Jacob M. Hoffman
  • Tolan derivatives, and liquid-crystalline medium
    Patent number: 6171664
    Abstract: The invention relates to tolan derivatives of the formula I in which R1, R2, A, Z, L1, L2, L3, L4, L5, L6, Q, m and n are as defined herein.
    Type: Grant
    Filed: June 17, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Matthias Bremer, Detlef Pauluth, Harald Hirschmann
  • Process for the preparation cis-(1S,2R)-indanediol by direduction of 1,2-indanedione using trichosporon cutaneum
    Patent number: 6171832
    Abstract: A process for preparing cis-(1S,2R)-indanediol is disclosed. The process comprises (A) fermenting a culture medium containing a yeast strain selected from the group consisting of Trichosporon cutaneum MY 1506 (ATCC 74440) and mutants thereof and 1,2-indanedione to form cis-(1S,2R)-indanediol; and (B) recovering cis-(1S,2R)-indanediol from the culture medium. A process for preparing (1S)-amino-(2R)-indanol from the recovered cis-(1S,2R)-indanediol via the Ritter reaction is also disclosed.
    Type: Grant
    Filed: April 27, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Michael M. Chartrain, Norihiro Ikemoto, Anthony O. King
  • 6-azaindole compounds as antagonists of gonadotropin releasing hormone
    Patent number: 6172080
    Abstract: There are disclosed compounds of formula (I) 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 7, 2000
    Date of Patent: January 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Thomas F. Walsh, Feroze Ujjainwalla
  • Oxidation process using periodic acid
    Patent number: 6172231
    Abstract: The present invention relates to a periodic acid oxidation which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula I having a carboxylic acid.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Zhiguo Song, Mangzu Zhao, David M. Tschaen
  • Liquid-crystalline medium
    Patent number: 6171665
    Abstract: The invention relates to a liquid-crystalline medium based on a mixture of polar compounds of positive dielectric anisotropy, containing at least one compound of the general formula I wherein R1-R4 may each, independently of one another, be an alkyl or alkenyl radical having up to 12 carbon atoms which is unsubstituted, monosubstituted by CN or CF3 or at least monosubstituted by halogen, where one or more CH2 groups in these radicals may also, in each case independently of one another, be replaced by —O—, —S—, —CO—, —CO—O—, —O—CO— or —O—CO—O— in such a way that O atoms are not linked directly to one another, and —A— is 1,4-phenylene, in which, in addition, one or two CH groups may be replaced by N, 2,3-difluoro-1,4-phenylene, 2-fluoro-1,4-phenylene, 3-fluoro-1,4-phenylene or a single bond.
    Type: Grant
    Filed: December 14, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck Patent Gesellschaft
    Inventors: Michael Heckmeier, Brigitte Schuler, Volker Reiffenrath
  • End piece for a chromatographic column
    Patent number: 6171502
    Abstract: The present invention provides a column endpiece for a chromatography column. The column endpiece includes a base part, an extension piece for a discharge tube, and a frit. The frit produces a pressure drop per unit length that is at least twice as great as the pressure drop per unit length created in the sorbent packing when the eluent is flowing through.
    Type: Grant
    Filed: September 13, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck PatentGesellschaft
    Inventors: Hans Daniel Jakob Mueller, Axel Delp, Hans-Dieter Harders, Joseph H. Spurk, Peter F. Pelz
  • Spiro-azacyclic derivatives and their use as therapeutic agents
    Patent number: 6172077
    Abstract: The present invention is directed to substituted spiro-azacyclic derivatives of the formula (I): (wherein R1, R2, R3, R4, R5, R6, R9, R10, X, Y, p and q 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: October 22, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Neil Roy Curtis, Jason Matthew Elliott, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
    Patent number: 6169188
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: October 21, 1999
    Date of Patent: January 2, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Michel Belley, Jacques Yves Gauthier, Erich Grimm, Yves LeBlanc, Chun-Sing Li, Michel Therien, Cameron Black, Petpiboon Prasit, Cheuk-Kun Lau, Patrick Roy
  • Cyclic adhesion inhibitors
    Patent number: 6169072
    Abstract: The invention relates to novel cyclopeptides of the formula I cyclo-(Arg-B-Asp-D-E)  I in which B, D, and E have the meanings defined herein, and their salts. These compounds act as interin inhibitors and can be used, in particular, for the prophylaxis and treatment of disorders of the circulation and in tumor therapy.
    Type: Grant
    Filed: October 1, 1998
    Date of Patent: January 2, 2001
    Assignee: Merck Patent Gesellschaft Mit
    Inventors: Alfred Jonczyk, G{umlaut over (u)}nter Hölzemann, Brunhilde Felding-Habermann, Friedrich Rippmann, Beate Diefenbach, Horst Kessler, Roland Haubner, Jochen Wermuth
  • Polyol composition
    Patent number: 6165511
    Abstract: A polyol composition useful for the production of tablets for consumption. The polyol is obtained by co-spray drying or co-fluidized bed granulating at least two polyols, one of which is a non-hygroscopic polyol, and the non-hygroscopic polyol is present in an amount of at least 80% by weight. An optional binder may be present. An active medicament may be present.
    Type: Grant
    Filed: October 21, 1998
    Date of Patent: December 26, 2000
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Eugen Schwarz, Gernot Moschl, Karin Maul
  • TN cell having improved display of grey shades
    Patent number: 6166798
    Abstract: The invention relates to a TN cell which contains a nematic liquid crystal having positive dielectric anisotropy and a twist angle of essentially 90.degree., between two substrates provided with electrode and alignment layers, where the product of the separation between the substrate plates d and the optical anisotropy d.multidot..DELTA.n [sic] of the liquid crystal is between 0.15 and 0.70 .mu.m, characterised in that the liquid crystal contains a doping component in order to improve the grey shade capacity, so that the cell has a value for the undisturbed quotient of the separation between the substrate plates d and the pitch of the liquid crystal p of 0.1.ltoreq.d/p.ltoreq.0.5.
    Type: Grant
    Filed: April 7, 1998
    Date of Patent: December 26, 2000
    Assignee: Merck KGaA
    Inventors: Herbert Plach, Paulus Adrianus Breddels
  • Pyrrolidine and piperidine modulators of chemokine receptor activity
    Patent number: 6166037
    Abstract: The present invention is directed to pyrrolidine and piperidine compounds of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.4d, R.sup.4e, R.sup.4f, R.sup.4g, R.sup.4h, m, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: August 27, 1998
    Date of Patent: December 26, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Richard J. Budhu, Edward Holson, Jeffrey J. Hale, Christopher Lynch, Malcolm Maccoss, Scott C. Berk, Sander G. Mills, Christopher A. Willoughby
  • Human adenosine receptors
    Patent number: 6166181
    Abstract: The invention concerns recombinant human adenosine receptors A1, A2a, A2b and A3 which have been prepared by cDNA cloning and polymerase chain reaction techniques. The invention also concerns expression systems for these receptors and an assay using the expression systems. The recombinant adenosine receptors comprising the invention can be utililized in an assay to identify and evaluate entities that bind to or enhance binding to adenosine receptors.
    Type: Grant
    Filed: May 18, 1998
    Date of Patent: December 26, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Marlene A. Jacobson, Christopher J. Luneau, Robert G. Johnson, Christopher A. Salvatore
  • High-strength degradable materials and molded articles for implantation into human and animal organisms
    Patent number: 6166159
    Abstract: Described are high-strength materials which are degradable and resorbable in the human and animal organisms and shaped articles manufactured therefrom, such as implants, based on cured (meth)acrylic acid esters of polyfunctionally hydroxyl-terminated oligomers of lower hydroxycarboxylic acids {polyfunctional (meth)acrylic acid esters}. The invention is characterized in that said materials and/or shaped articles have been three-dimensionally cross-linked by radiation-curing and/or any other, however boron-free, free radical-initiated polymerization of the polyfunctional (meth)acrylic acid esters and exhibit a tensile strength under standard conditions of at least 10 N/mm.sup.2.
    Type: Grant
    Filed: May 26, 1993
    Date of Patent: December 26, 2000
    Assignee: Merck Patent GmbH
    Inventor: Wolfgang Ritter
  • Omeprazole process and compositions thereof
    Patent number: 6166213
    Abstract: The present invention describes an improved process for the preparation, isolation, and purification of the anti-ulcer agent omeprazole whereby the sulfide precursor pyrmetazole is reacted subsurfacely with exactly one molar equivalent of meta-chloroperoxybenzoic acid in methylene chloride or toluene solution; residual organic solvent is removed from the aqueous layer by vacuum distillation; crude product is obtained by reactive crystallization with an alkyl formate and seeding; and pure product is isolated by recrystallization in methanol-water containing aqueous NaOH by subsurface addition of aqueous acetic acid to pH 9.0, seeding, filtration, washing, and drying. Compositions of omeprazole containing no chromatographically detectable levels of residual non-alcoholic organic reaction solvent are also described.
    Type: Grant
    Filed: October 9, 1998
    Date of Patent: December 26, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Nick Anousis, James W. McManus, Benjamin Newton Banks, Lingwen Zhou, Hui Liu
  • Tyrosine kinase inhibitors
    Patent number: 6162804
    Abstract: The present invention relates to benzinidazole compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tyrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.
    Type: Grant
    Filed: March 11, 1999
    Date of Patent: December 19, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, April M. Cunningham, Randall W. Hungate, Timothy J. Koester
  • Use of an NK-1 receptor antagonist and an SSRI for treating obesity
    Patent number: 6162805
    Abstract: The present invention relates to the use of an NK-1 receptor antagonist and a selective serotonin reuptake inhibitor for the treatment or prevention of obesity.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: December 19, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Franz Fridolin Hefti