Patents Assigned to Merck
  • Cyclic azapeptides with angiogenic effect
    Patent number: 6534478
    Abstract: Compounds of the formula I cyclo-(aArg-aGly-aAsp-aX-aY)  I in which aArg, aGly, aAsp, aX and aY have the meanings indicated in claim 1, and their salts, can be used as integrin inhibitors, in particular for the prophylaxis and treatment of diseases of the circulation, in thrombosis, cardiac infarct, coronary heart diseases, arteriosclerosis, in pathological processes which are supported or propagated by angiogenesis and in tumour therapy.
    Type: Grant
    Filed: March 23, 2000
    Date of Patent: March 18, 2003
    Assignee: Merck Patent Gesellschaft Mit
    Inventors: Alfred Jonczyk, Simon Goodman, Horst Kessler, Jochen Wermuth, Jörg Schmitt
  • Therapeutic polymorphs of a GABA-A alpha-5 inverse agonist and pamoate formulations of the same
    Patent number: 6534505
    Abstract: There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.
    Type: Grant
    Filed: November 30, 2000
    Date of Patent: March 18, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Michael J. Kaufman, Daniel J. Rush
  • Catalyst system for the Ziegler-Natta polymerization of olefins
    Patent number: 6534606
    Abstract: Described are catalyst systems having aluminium alkyl complexes of the formula (I) described herein applied to magnesium chloride, SiO2 or SiO2 in combination with MgCl2 as support in the presence of titanium halides or vanadium halides and internal and, if desired, external donors act both as cocatalysts and as stereoselectivity promoters in heterogeneous polymerizations of &agr;-olefins. Also described are polymerization methods using these catalyst systems.
    Type: Grant
    Filed: March 8, 2001
    Date of Patent: March 18, 2003
    Assignee: Merck Patent Gesellschaft Mit Beschränkter Haftung
    Inventors: Katrin Köhler, Eike Poetsch, Herbert Schumann, Sebastian Dechert, Walter Kaminsky, Andre Laban, Manfred Arnold, Jana Knorr, Birgit Corinna Wassermann
  • N(CF3)2 anion generation and its use
    Patent number: 6534682
    Abstract: The invention relates to a process of generating N(CF3)2 anions by reacting a metal fluoride of formula MFx with a compound of formula RFSO2N(CF3)2, (CF3)2N(SO2CF2)mSO2N(CF3)2 or RFCON(CF3)2. The invention further relates to the use of the N(CF3)2 anions as a reagent for the introduction of halogen or other organic groups into organic molecules.
    Type: Grant
    Filed: August 1, 2001
    Date of Patent: March 18, 2003
    Assignee: Merck Patent Gesellschaft
    Inventors: Völker Hilarius, Herwig Buchholz, Peter Sartori, Nikolai Ignatiev, Andrei Kucherina, Sergii Datsenko
  • Vaccines comprising synthetic genes
    Patent number: 6534312
    Abstract: Synthetic polynucleotides comprising a DNA sequence encoding a peptide or protein are provided. The DNA sequence of the synthetic polynucleotides comprise codons optimized for expression in a nonhomologous host. The invention is exemplified by synthetic DNA molecules encoding HIV env as well as modifications of HIV env. The codons of the synthetic molecules include the projected host cell's preferred codons. The synthetic molecules provide preferred forms of foreign genetic material. The synthetic molecules may be used as a polynucleotide vaccine which provides immunoprophylaxis against HIV infection through neutralizing antibody and cell-mediated immunity. This invention provides polynucleotides which, when directly introduced into a vertebrate in vivo, including mammals such as primates and humans, induces the expression of encoded proteins within the animal.
    Type: Grant
    Filed: June 28, 1999
    Date of Patent: March 18, 2003
    Assignee: Merck & Co., Inc.
    Inventors: John W. Shiver, Mary Ellen Davies, Daniel C. Freed, Margaret A. Liu, Helen C. Perry
  • Inhibitors of prenyl-protein transferase
    Patent number: 6534506
    Abstract: The present invention is directed to peptidomimetic macrocyclic 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: April 6, 2001
    Date of Patent: March 18, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Diem N. Nguyen, Craig A. Stump, Theresa M. Williams
  • Process of preparing discotic liquid crystalline compounds
    Patent number: 6534135
    Abstract: The invention relates to a process of preparing a discotic liquid crystalline compound by intramolecular oxidative cyclisation of a diaryl compound in an organic solvent in the presence of a strong acid, characterized in that an oxidative agent comprising a chrom(VI)oxide derivative is used, to discotic liquid crystalline compounds obtainable from said process, to liquid crystalline media, (co)polymers or polymer networks with columnar phases comprising said discotic liquid crystalline compounds, and to the use of said discotic liquid crystalline compounds, liquid crystalline media or liquid crystalline (co)polymers with columnar phases for liquid crystal displays, optical elements like polarizers, compensators or colour filters, chemical sensors, charge transport materials, optical storage media, nonlinear optics, decorative pigments, adhesive or synthetic resins with anisotropic mechanical properties.
    Type: Grant
    Filed: September 14, 2000
    Date of Patent: March 18, 2003
    Assignee: Merck Patent Gesellschaft
    Inventor: Mohammed Cherkaoui
  • Mono-, oligo- and poly-4- fluorothiophenes and their use as charge transport materials
    Publication number: 20030047720
    Abstract: Mono-, oligo- and polymers comprising one or more identical or different recurring units of formula I
    Type: Application
    Filed: July 25, 2002
    Publication date: March 13, 2003
    Applicant: Merck Patent GmbH
    Inventors: Martin Heeney, Louise Farrand, Mark Giles, Marcus Thompson, Steven Tierney, Maxim Shkunov, David Sparrowe, Iain McCulloch
  • Mono-, oligo- and polydithienopyridines
    Publication number: 20030047719
    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: Application
    Filed: July 9, 2002
    Publication date: March 13, 2003
    Applicant: Merck Patent GmbH
    Inventors: Martin Heeney, Steven Tierney, Marcus Thompson, Mark Giles, Louise Farrand, Maxim Shkunov, David Sparrowe, Iain McCulloch
  • Packaging system for cosmetic formulations
    Publication number: 20030048693
    Abstract: The invention relates to a packaging system for the in-situ preparation of cosmetic formulations which has a micromixer. This micromixer can be connected to one or more stock chambers.
    Type: Application
    Filed: May 23, 2002
    Publication date: March 13, 2003
    Applicant: Merck Patent GmbH
    Inventors: Joachim Buenger, Hansjurgen Driller, Jutta Zur Lange, Annette Wagner
  • Pyrrolidine modulators of CCR5 chemokine receptor activity
    Patent number: 6531484
    Abstract: Pyrrolidine compounds of Formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, j, k, 1, m, and n are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: October 10, 2001
    Date of Patent: March 11, 2003
    Assignee: Merck & co., Inc.
    Inventors: Christopher A. Willoughby, Keith Rosauer, Kevin T. Chapman, Sander G. Mills, Dong-Ming Shen, Min Shu
  • STN liquid-crystal display
    Patent number: 6531194
    Abstract: The invention relates to supertwist liquid-crystal displays (SLCDs) having very short response times and good steepnesses and angular dependences and to the novel nematic liquid-crystal mixtures employed therein, which are distinguished by the fact that they comprise at least one compound of the formula IA and at least one compound of the formula IB and/or at least one compound of the formula IC in which Ra, Rb, Rc, Rd, Re, Y1, Y2, Y3, Y4, q and p are as defined above.
    Type: Grant
    Filed: December 12, 2000
    Date of Patent: March 11, 2003
    Assignee: Merck Patentgesellschaft
    Inventor: Harald Hirschmann
  • Method of treating neurodegenerative diseases
    Patent number: 6531488
    Abstract: The present invention provides a method of treating a neurodegenerative disease, and in particular Alzheimer's disease, Mild Cognitive Impairment or other objective memory impairment which comprises the co-administration of ARICEPT or other cholinesterase inhibitor or cholenergic angonist and an effective amount of a selective COX-2 inhibitor. Although a wide range of COX-2 inhibitors may be employed in combination with ARICEPT, there are preferred choices which are specifically set forth herein.
    Type: Grant
    Filed: February 22, 2001
    Date of Patent: March 11, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Gilbert A. Block, Per Wold-Olsen
  • Benzofurane derivatives
    Patent number: 6531503
    Abstract: Benzofurane derivatives of formula (I), wherein R and R′ have the meanings given in claim no. (1), and salts thereof are suitable for use as intermediate products in the synthesis of medicaments.
    Type: Grant
    Filed: January 9, 2002
    Date of Patent: March 11, 2003
    Assignee: Merck Patent GmbH
    Inventors: Andreas Bathe, Bernd Helfert, Henning Böttcher
  • Process for preparing hydroxychomanones and cis-aminochromanols
    Patent number: 6531617
    Abstract: Enantiomerically enriched hydroxychromanones are obtained by the AlCl3-catalyzed intramolecular Friedel-Crafts acylation of the corresponding 3-phenoxy-2-alkylcarbonyloxy-propionic acid followed by cleavage of the carboxylate in the presence of an alkali metal peroxide or hydroperoxide. Enantiomerically enriched cis-aminochromanols can then be prepared by treating the hydroxychromanones with a hydroxylamine and hydrogenating the resulting oxime. 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: October 24, 2001
    Date of Patent: March 11, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Karl Hansen, Paul Devine, Philippe M. Rabbat
  • Isoxazole derivatives to be used as phosphodiesterase VII inhibitors
    Patent number: 6531498
    Abstract: The invention relates to compounds of formula I and to their physiologically acceptable salts and solvates which act as phosphodiesterse VII inhibitors and are thus useful for the treatment of allergic disorders, asthma, chronic bronchitis, atopic dermatitis, psoriasis and other skin disorders, inflammatory disorders, autoimmune diseases, rheumatoid arthritis, multiple sclerosis, Crohn's disease, diabetes mellitus or ulcerative colitis, osteoporosis, transplant rejection reactions, cachexia, tumor growth, tumor metastases, sepsis, memory disturbances, atherosclerosis and AIDS.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: March 11, 2003
    Assignee: Merck Patentgesellschaft
    Inventors: Hans-Michael Eggenweiler, Rochus Jonas, Michael Wolf, Michael Gassen, Thomas Welge
  • Transport drum for liquids
    Patent number: 6530497
    Abstract: A plastic transporting container for liquids, in particular high-purity liquids, has a submersion tube (1) which extends from a top wall (2) of the container to the container base (3) and is integrally formed in the transporting container. At its end which opens out in the top wall (2) of the container, the submersion tube is provided with a screw-connection device (6).
    Type: Grant
    Filed: May 26, 2000
    Date of Patent: March 11, 2003
    Assignee: Merck Patent GmbH
    Inventors: Joachim Horn, Martin Benzinger, Thomas Schwortschik
  • Growth hormone secretagogue receptor family
    Patent number: 6531314
    Abstract: Human, swine and rat growth hormone secretagogue receptors have been isolated, cloned and sequenced. Growth hormone secretagogue receptors are new members of the G-protein family of receptors. The growth hormone secretagogue receptors may be used to screen and identify compounds which bind to the growth hormone secretagogue receptor. Such compounds may be used in the treatment of conditions which occur when there is a shortage of growth hormone, such as observed in growth hormone deficient children, elderly patients with musculoskeletal impairment and recovering from hip fracture and osteoporosis.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: March 11, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Joseph P. Arena, Doris F. Cully, Scott D. Feighner, Andrew D. Howard, Paul A. Liberator, James M. Schaeffer, Leonardus H. T. Van Der Ploeg
  • Method of treatment using arylalkylpyridazinones
    Patent number: 6531473
    Abstract: Aralkylpyridazinone derivatives of the formula I and their physiologically acceptable salts in which R1, R2, R3, R4, R5 and Q have the meanings indicated in claim 1, show inhibition of phosphodiesterase IV and can be employed for the treatment of inflammatory processes and of allergies, asthma and autoimmune disorders.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: March 11, 2003
    Assignee: Merck Patent GmbH
    Inventors: Rochus Jonas, Michael Wolf, Norbert Beier
  • Capillary column including porous silica gel having continuous throughpores and mesopores
    Patent number: 6531060
    Abstract: A capillary column comprising a capillary of which the inner diameter is less than 1000 &mgr;m and a continuous porous silica gel which uniformly fills the capillary, said silica gel containing both continuous through pores having diameters ranging from 0.5-5 &mgr;m and mesopores having diameters ranging from 2-50 nm.
    Type: Grant
    Filed: September 25, 2000
    Date of Patent: March 11, 2003
    Assignee: Merck Patent Gesellschaft
    Inventors: Kazuki Nakanishi, Naohiro Soga, Hiroyoshi Minakuchi