Abstract: A compound of formula I, or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, —SO2Ra, —SO2NRaRb, —CORa, —CO2Ra or —CONRaRb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions including the compound and methods for treating anxiety, convulsions and cognitive disorders are disclosed.
Abstract: The invention relates to a method for selectively dissociating cyclic carboxylic acid anhydrides. According to the inventive method, a chiral amino alcohol with a tertiary amino group that may have a partially or completely bridged structure is used as the chiral auxiliary reagent.
Abstract: The present invention relates to colored pigments based on multicoated platelet-shaped substrates which are distinguished by the fact that they comprise (A) a coating having a refractive index of n>1.8 and a layer thickness of 20-500 nm, (B) a colorless coating having a refractive index of n?1.8 and a layer thickness of 10-100 nm, (C) a colorless coating having a refractive index of n>1.8 and a layer thickness of 20-500 nm, (D) a covering of absorbent pigment particles having a particle size of 1-500 nm, and optionally (E) an outer protective layer, and to their use in paints, coatings, printing inks, plastics, ceramic materials, glasses, for laser marking, in cosmetic formulations and for the production of pigment preparations and dry preparations.
Abstract: Imidazole compounds of the formula I in which R1 and R2, independently of one another, each denote A1, OA1, SA1 or Hal, A1 denotes H, A, alkenyl, cycloalkyl or alkylenecycloalkyl, A denotes alkyl having 1-10 carbon atoms, Hal denotes F, Cl, Br or I, and X denotes O, S, SO or SO2, and their physiologically acceptable salts and/or solvates, as phosphodiesterase VII inhibitors, and their use for the preparation of a medicament.
Type:
Grant
Filed:
October 31, 2000
Date of Patent:
April 26, 2005
Assignee:
Merck Patent Gesellschaft mit Beschrankter Haftung
Inventors:
Hans-Michael Eggenweiler, Rochus Jonas, Michael Wolf, Michael Gassen, Thomas Welge
Abstract: Use of the polypeptide Saratin for the manufacture of a medicament having the capability to significantly decrease platelet adhesion and platelet accumulation after vascular injuries or endarterectomy. The invention furthermore relates to a novel medical use of Saratin as an inhibitor of thrombosis and intimal hyperplasia, wherein the Saratin polypeptide may be used locally as a topical agent or as a coating on, or otherwise incorporated or associated with medical devices.
Type:
Grant
Filed:
August 23, 2001
Date of Patent:
April 19, 2005
Assignee:
Merck GmbH
Inventors:
Christopher Barnes, Matthias Frech, Uwe Hofmann, Johannes Gleitz, Wolfgang Strittmatter
Abstract: Novel polypeptides derived from the C-terminal region of the human and mouse agouti related transcript (ART) proteins are provided. Also provided are DNA sequences encoding the novel C-terminal polypeptides. The novel C-terminal polypeptides can be used to inhibit the binding of melanocyte stimulating hormones to melanocortin receptors. Methods of identifying inhibitors of the binding of ART protein to melanocortin receptors are also provided.
Type:
Grant
Filed:
December 11, 1998
Date of Patent:
April 12, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Tung Ming Fong, Leonardus H. T. Van Der Ploeg, Michael R. Tota
Abstract: The invention relates to a chromatography column for high-pressure liquid chromatography, which can be provided with different connection systems, such as a cartridge retaining device or a reducing screw. The column tube (1, 11) of the inventive chromatography column has an external thread (4,18) at each end and at least one groove (3,14).
Abstract: The invention relates to a liquid crystalline medium, based on a mixture of polar compounds with a positive dielectric anisotropy. Said medium is characterised in that it contains one or more compounds of formula (I) wherein R, A1, A2, Z1, Z2, X1, X2, n and o are defined as per claim 1.
Type:
Grant
Filed:
September 17, 2001
Date of Patent:
April 12, 2005
Assignee:
Merck Patent GmbH
Inventors:
Michael Heckmeier, Martin Engel, Brigitte Schuler, Matthias Bremer, Detlef Pauluth
Abstract: This invention relates to novel formulations of pharmaceutical products, specifically nucleic acid vaccine products. The nucleic acid vaccine products, when introduced directly into muscle cells, induce the production of immune responses which specifically recognize Hepatitis C virus (HCV).
Type:
Application
Filed:
September 17, 2003
Publication date:
April 7, 2005
Applicant:
Merck & Co., Inc.
Inventors:
John Donnelly, Margaret Liu, John Shiver, Tong-Ming Fu
Abstract: The present invention relates to compounds having the formula I: which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions. The compounds of the present invention are useful in treating angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
Abstract: The invention relates to bis(alkylthio)carbenium salts of the formula I with the stated definitions for R1, R2, R3 and Y?, and to a process for the preparation thereof. The compounds according to the invention are advantageously suitable as electrophilic reagents for the transfer of fluorinated alkyl and acyl radicals onto nucleophilic compounds.
Type:
Grant
Filed:
February 11, 2002
Date of Patent:
April 5, 2005
Assignee:
Merck Patent GmbH
Inventors:
Peer Kirsch, Andreas Ruhl, Gerd-Volker Röschenthaler, Dmitrii Sevenard
Abstract: PHPIP-120 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed, also disclosed are methods for utilizing PHPIP-120 polypeptides and polynucleotides in diagnostic assays.
Type:
Application
Filed:
January 25, 2002
Publication date:
March 31, 2005
Applicant:
Merck Patent GmbH
Inventors:
Bjorn Hock, Klaus Ducker, Roland Kellner
Abstract: The present invention relates to a device at mixing devices for mixing pulverulent and liquid substances with each other for the manufacture of medical products, wherein a displaceable piston means (17) has at least one groove (22) extending around said piston means (17) and at least one sealing ring (23) is located in said groove (22). At least one connecting passage (22e) is provided for preventing a liquid substance (21) from generating or building up such a pressure in an inner space (22d) in the groove (22) within or behind the sealing ring (23) that said pressure presses the sealing ring (23) in a direction outwards (F) relative to the groove (22) towards a surrounding wall (1a) of the mixing device (1) and prevents or counteracts flow of the liquid substance (21) past the piston means (17) when said piston means (17) is displaced.
Abstract: Heparanase-2 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing heparanese-2 polypeptides and polynucleotides and diagnostic assays.
Abstract: A class of substituted pyrazolo[1,5-d][1,2,4]triazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 7-position, an alkyl group at the 4-position, and a substituted alkoxy moiety at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?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:
April 4, 2001
Date of Patent:
March 29, 2005
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
William Robert Carling, Andrew Mitchinson, Michael Geoffrey Russell, Leslie Joseph Street
Abstract: The present invention relates to active polymorphs of 4-[2-(5-cyano-thiazol-2-ylamino)-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angio-genesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, retinal ischemia, macular edema, inflammatory diseases, and the like in mammals.
Abstract: A class of 3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH-linkage, are selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?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:
May 23, 2002
Date of Patent:
March 29, 2005
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
James Michael Crawforth, Simon Charles Goodacre, Timothy Harrison, David James Hallett, Andrew Pate Owens, Michael Rowley, Martin Richard Teall
Abstract: The present invention is concerned with a process for the preparation of trifluorophenylacetic acids using a Grignard reagent and an allylating agent, such as allyl bromide.
Abstract: This invention provides isolated polynucleotides that encode the MurE protein of Pseudomonas aeruginosa. Purified and isolated MurE recombinant proteins are also provided. Nucleic acid sequences which encode functionally active MurE proteins are described. Assays for the identification of modulators of the of expression of murE and inhibitors of the activity of MurE, are also provided.
Type:
Grant
Filed:
September 11, 2000
Date of Patent:
March 22, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Mohamend El-Sherbeini, Barbara Azzolina
Abstract: The present invention concerns certain isoquinolinone compounds and their utility as inhibitors of voltage-dependent potassium channels or currents, such as Kv1.5 and IKur, that could serve as targets for the treatment of cardiac arrhythmias especially atrial arrhythmias. The present invention also provide a method for treating or preventing conditions which respond to the inhibition of potassium channels or currents, such as cardiac arrhythmias and more especially atrial arrhythmias. The present invention further includes pharmaceutical formulations and a process of making a pharmaceutical composition comprising a compound of certain isoquinolinone or its pharmaceutically acceptable salts, hydrates, solvates, crystal forms, and stereoisomers thereof, and a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
September 17, 2001
Date of Patent:
March 22, 2005
Assignee:
Merck & Co., Inc.
Inventors:
David A. Claremon, Charles J. McIntyre, Nigel J. Liverton