Abstract: The present invention is directed to pyrrolidine compounds of the formula I:
(wherein R1, R2, R3, R4, R5, R6 and n 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-5 and/or CCR-3.
Type:
Grant
Filed:
April 4, 2000
Date of Patent:
December 24, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Charles G. Caldwell, Kevin T. Chapman, Jeffrey Hale, Dooseop Kim, Christopher Lynch, Malcolm MacCoss, Sander G. Mills, Christopher Willoughby, Scott Berk, Ronald M. Kim
Abstract: The invention relates to nematic liquid-crystal compositions comprising bisalkenyl compounds of the formula Ia.
in which
R1 and R2, are each independently alkenyl having 2 to 8 carbon atoms, and
Z2 is a single bond, —(CH2)2— or trans-CH═CH—.
and to their use in plasma-addressed LCDs.
Type:
Grant
Filed:
July 24, 2000
Date of Patent:
December 24, 2002
Assignee:
Merck Patent GmbH
Inventors:
Harald Hirschmann, Sven Schüpfer, Marcus Reuter
Abstract: Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of protein tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.
Type:
Grant
Filed:
June 26, 2000
Date of Patent:
December 24, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Helen M. Armstrong, Richard Beresis, Joung L. Goulet, Mark A. Holmes, Xingfang Hong, Sander G. Mills, William H. Parsons, Peter J. Sinclair, Mark G. Steiner, Frederick Wong, Dennis M. Zaller
Abstract: The present invention relates to colored pigments based on multicoated platelet-shaped substrates which are distinguished by the fact that they comprise
Abstract: The eosinophil eotaxin receptor has been isolated, cloned and sequenced. This receptor is a human &bgr;-chemokine receptor and has been designated “CC CKR3”. The eosinophil eotaxin receptor may be used to screen and identify compounds that bind to the eosinophil eotaxin receptor. Such compounds would be useful in the treatment and prevention of atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and particularly bronchial asthma.
Type:
Application
Filed:
August 6, 2001
Publication date:
December 19, 2002
Applicant:
Merck & Co., Inc.
Inventors:
Bruce L. Daugherty, Julie A. Demartino, Salvatore J. Siciliano, Martin S. Springer
Abstract: The invention relates to a dry toner for laser printing which comprises at least one viewing angle-dependent (“angle-dependent”), platelet-shaped luster pigment. The luster pigment consists of a multicoated, platelet-shaped, opaque or semi-transparent substrate. The toner is particularly suitable for security printing. The invention furthermore relates to a process for the production of images by electrophotographic methods using the dry toner.
Type:
Application
Filed:
May 20, 2002
Publication date:
December 19, 2002
Applicant:
Merck Patent GmbH
Inventors:
Gunter Brenner, Hans-Dieter Bruckner, Wolfgang Hechler, Burkhard Krietsch, Matthias Kuntz, Michael Schmelz
Abstract: The thienopyrimidines of the formula (I) and their physiologically compatible salts display a phosphodiesterase V inhibiting activity and can be used for treating diseases of the cardiovascular system and for treatment and/or therapy of erectile dysfunction.
Type:
Grant
Filed:
May 16, 2002
Date of Patent:
December 17, 2002
Assignee:
Merck Patent Gesellschaft mit beschraenkter Haftung
Inventors:
Rochus Jonas, Pierre Schelling, Franz-Werner Kluxen, Maria Christadler
Abstract: This invention encompasses a process for making a compound of Formula A
These compounds are intermediates useful in the preparation of certain non-steroidal anti-inflammnatory agents.
Type:
Grant
Filed:
January 17, 2002
Date of Patent:
December 17, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Cheng Yi Chen, Weirong Chen, Paul O'Shea, Lushi Tan, Richard Tillyer, Feng Xu, Philippe Dagneau
Abstract: Compounds of general structural formula I such as that shown in structural formula II
are selective NPY Y5 receptor antagonists, useful in the treatment of obesity and the complications associated therewith.
Type:
Grant
Filed:
June 29, 2001
Date of Patent:
December 17, 2002
Assignees:
Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.
Inventors:
Ying-Duo Gao, Douglas J. MacNeil, Lihu Yang, Nancy R. Morin, Takehiro Fukami, Akio Kanatani, Takahiro Fukuroda, Yasuyuki Ishii, Masaki Ihara
Abstract: 4-substituted cyclohexanes substituted in the 1-position with imidazopyridine either directly or through a C1-C4alkyl, C1-C4alkenyl, C1-C4alkynyl, C1-C4alkoxy, amino, aminoC1-C4alkyl, hydroxyC1-C4alkyl, carbonyl, cycloC3-C6alkyl or aminocarbonyl chain are effective as NMDA NR2B antagonists useful for relieving pain.
Type:
Grant
Filed:
May 21, 2001
Date of Patent:
December 17, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Wayne J. Thompson, David A. Claremon, Peter M. Munson, John A. McCauley
Abstract: The invention describes biodegradable calcium phosphate cements, in particular mixtures of calcium phosphate-containing powders of different stoichiometric composition, the precipitated hydroxylapatite present being a cation-deficient hydroxylapatite of the formula 1, with the result that the mixtures have improved properties with regard to compressive strength.
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:
March 15, 2000
Date of Patent:
December 17, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Tong M. Fong, Jie Liu, Leonardus H. T. Van Der Ploeg
Abstract: The invention relates to a method for classifying and identifying by means of energy dispersion X-ray fluorescence analysis chemical substances whose X-ray fluorescence lines cannot be detected and which therefore cannot be classified by energy dispersion X-ray fluorescence analysis alone. Said method is characterized in that the sample to be analyzed is analyzed in its original packaging or natural state without prior processing in a sample vessel. According to the method the sample is: a) positioned in front of the measuring aperture in a sample chamber of an X-ray fluorescence apparatus; b) measured; and c) classified and identified by application of multivariate, statistical techniques to the measurement signals obtained, i.e., to the Compton and Rayleigh scattering.
Type:
Grant
Filed:
July 20, 2001
Date of Patent:
December 17, 2002
Assignee:
Merck Patentgesellschaft mit Beschrankter Haftung
Inventors:
Alexander Henrich, Hans-Helmut Itzel, Peter Hoffmann, Hugo Ortner
Abstract: The invention relates to chiral compounds of formula I
wherein R1, R2, X, Y1 and Y2 have the meanings defined herein, as well as to liquid crystalline mixtures comprising at least one chiral compound of formula I.
Abstract: Thienopyrimidines of the formula I
and their physiologically acceptable salts,
in which
R1, R2 and X have the meanings given in claim 1, inhibit phosphodiesterase V and can be employed for the treatment of illnesses of the cardiovascular system and for the treatment and/or therapy of impaired potency.
Type:
Grant
Filed:
March 23, 2001
Date of Patent:
December 17, 2002
Assignee:
Merck Patent Gesellschaft mit beschraenkter Haftung
Inventors:
Rochus Jonas, Pierre Schelling, Franz-Werner Kluxen, Maria Christadler
Abstract: The present invention relates to novel pharmaceutical tablets useful for administering pharmaceutical active ingredients, such as bisphosphonates. These tablets have improved surface properties which can aid esophageal transit, thereby reducing the potential for adverse gesture intestinal effects. The present invention also relates to processes for making said novel pharmaceutical tablets.
Type:
Application
Filed:
March 15, 2002
Publication date:
December 12, 2002
Applicant:
Merck & Co., Inc.
Inventors:
Tzyy-Show H. Chen, Thomas G. Nyairo, Ashok V. Katdare
Abstract: The invention relates to a pharmaceutical preparation comprising levothyroxine sodium, potassium iodide, microcrystalline cellulose and binding agent, which is free of antioxidants or further auxiliaries, and processes for its production.
Abstract: The invention relates e.g. to the use of aldehydes and/or ketones for improving the stability of cosmetic formulations containing butylmethoxydibenzoylmethane as organic light protection filters in conjunction with inorganic light protection filters.
Abstract: Novel compounds of the formula I
in which
X, Y, R1, R2 and R3 are as defined in Patent Claim 1
are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.
Abstract:
The invention relates to novel compounds of formula (I), wherein R, R1, R2, R3, n and p have the meaning defined in claim 1. Compounds are inhibitors of clotting factor Xa and can be used for the prophylaxis and/or therapy of thrombo-embolic disorders.
Type:
Grant
Filed:
December 13, 2001
Date of Patent:
December 10, 2002
Assignee:
Merck Patent GmbH
Inventors:
Werner Mederski, Horst Juraszyk, Hanns Wurziger, Joachim Gante, Dieter Dorsch, Hans-Peter Buchstaller, Sabine Bernotat-Danielowski, Guido Melzer, Soheila Anzali