Abstract: Substituted cyclopentanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.
Type:
Grant
Filed:
July 20, 2001
Date of Patent:
June 25, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Marc Labelle, Claudio Sturino, Bruno Roy, Carl Berthelette, Michael Boyd, Nicolas Lachance, John Scheigetz
Abstract: The invention relates to a process for the preparation of organic methanide electrolytes in useable quality for use in electrochemical cells and batteries.
Type:
Grant
Filed:
April 28, 2000
Date of Patent:
June 25, 2002
Assignee:
Merck Patent Gesellschaft mit beschraenkter Haftung
Inventors:
Nikolai Ignatiev, Peter Sartori, Peter Barthen
Abstract: Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.
Type:
Grant
Filed:
February 12, 2001
Date of Patent:
June 25, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Ravi P. Nargund, Zhixiong Ye, Brenda L. Palucki, Raman K. Bakshi, Arthur A. Patchett, Leonardus H. T. Van Der Ploeg
Abstract: The present invention relates to novel nonanoic acid derivatives, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.
Type:
Grant
Filed:
May 31, 2000
Date of Patent:
June 25, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Duggan, George D. Hartman, Robert S. Meissner, James J. Perkins
Abstract: Bacterial polysaccharides which are used to produced vaccines are isolated then precipitated with a long chain detergent. The precipitated polysaccharides are soluble in organic solvents and can be further derivatized and processed to form the vaccine.
Abstract: The invention relates to a fed-batch fermentation process which uses special E. coli host/vector systems for the purpose of efficiently forming recombinant proteins, in particular recombinant antibody molecules, preferably antibody fragments such as miniantibodies. Under the given conditions, the E. coli cells are able to grow at a maximum specific growth rate up to very high cell densities. After the recombinant product formation has been switched on, it is only the formed product which restricts growth; there is no growth restriction due to substrates or metabolic by-products. High space-time yields of recombinant proteins can be achieved in this manner.
Type:
Grant
Filed:
November 16, 1998
Date of Patent:
June 25, 2002
Assignee:
Merck Patent Gesellschaft
Inventors:
Wolfgang Strittmatter, Siegfried Matzku, Dieter Riesenberg, Uwe Horn, Uwe Knüpeer, Marian Kujau, Rolf Wenderoth, Andreas Plückthun, Anke Krebber
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:
June 29, 1999
Date of Patent:
June 25, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Christopher J. Dinsmore, Ian M. Bell, Douglas C. Beshore, Theresa M. Williams
Abstract: Surface-modified conductive pigment obtainable by partial coating of a conductive pigment with an organic modifying agent. The modifying agent is an organometallic compound of the elements silicon, tin, titanium, zirconium or aluminum. The pigment is prepared by dispersing a conductive pigment, subsequently adding the modifying agent, if appropriate as a mixture with a solvent, to the pigment dispersion, and in particular in an amount such that the powder electrical conductance of the partly coated conductive pigment is in the range between 80% of the starting value and 10−7 S, removing the solvent present, if appropriate, with further agitation and heating of the pigment to 100° C. and finally drying the partly coated pigment.
Type:
Grant
Filed:
April 5, 1995
Date of Patent:
June 25, 2002
Assignee:
Merck Patent Gesellschaft mit beschraenkter Haftung
Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by direct compression/dry mix tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.
Type:
Grant
Filed:
October 17, 2000
Date of Patent:
June 18, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Simon R. Bechard, Kenneth A. Kramer, Ashok V. Katdare
Abstract: A novel process is provided for the preparation of imidazolidinone &agr;v&bgr;3/&agr;v&bgr;5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of &agr;v&bgr;3/&agr;v&bgr;5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.
Type:
Grant
Filed:
November 7, 2000
Date of Patent:
June 18, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Mark S Jensen, Michael Palucki, Nelo R. Rivera, Kenneth M. Wells, Yi Xiao, Yaling Wang, Chunhua Yang, Nobuyoshi Yasuda
Abstract: The dog GnRH receptor has been isolated, cloned and sequenced. The dog GnRH receptor may be used to screen and identify compounds which bind to the GnRH receptor. Such identified compounds may be used in the treatment of sex hormone related conditions such as endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasias such as cancers of the prostate, breast and ovary, gonadotrophe pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome and benign prostatic hypertrophy. The receptor proteins and polypeptides, nucleic acids, cells and assays of this invention are useful in drug screening and development, diagnosis and therapeutic applications.
Type:
Grant
Filed:
May 31, 2000
Date of Patent:
June 18, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Jisong Cui, Jane-Ling Lo, George R. Mount
Abstract: The present invention relates to a process for the preparation of morpholine derivatives of formula (I) which are useful as a therapeutic agents.
Type:
Grant
Filed:
September 10, 2001
Date of Patent:
June 18, 2002
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Ian Frank Cottrell, Ulf H Dolling, David Hands, Robert Darrin Wilson
Abstract: The present invention is a cloned human BK-2 bradykinin receptor cloned from a human lung fibroblast cell line. A cDNA clone, also part of the instant invention, encodes a novel 364 amino acid protein (the BK-2 receptor) that has the characteristics of a seven transmembrane domain G-protein coupled receptor. The invention is used to express a BK-2 bradykinin receptor in a host mammalian cell to screen for pharmaceutical antagonists or agonists which bind to or interact with the BK-2 bradykinin receptor protein.
Type:
Grant
Filed:
November 8, 1993
Date of Patent:
June 18, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Joseph A. Borkowski, John W. Hess, Catherine D. Strader, Richard W. Ransom
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
in which R, Y and L1 are as defined in claim 1.
Type:
Grant
Filed:
July 26, 2000
Date of Patent:
June 18, 2002
Assignee:
Merck Patents Gesellschaft mit beschraenkter Haftung
Abstract: The present invention is concerned with novel processes for the preparation of (2R-cis)-2-[[1-[3.5-bis(trifluoromethyl)phenyl]ethenyl]oxy]-3-(4-fluorophenyl)-4-(phenylmethyl) mopholine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
Abstract: The present invention provides novel liquid and lyophilized formulations of vaccines against rotavirus infection and methods of their preparation. The formulations include buffering agents appropriate for oral administration of rotavirus vaccines. The formulations also include compounds to stabilize of the vaccine compositions against loss of potency.
Abstract: The present invention relates to a compound of the tantomeric formula Ia or Ib
and/or of a physiologically acceptable salt of the compound of the formula Ia or Ib and/or of a sterio-isomeric form of the compound of the formula Ia or Ib. R1 can be:
a) a hydrogen atom or
b) C1-C4)-alkyl.
R2 can be:
a) a hydrogen atom,
b) —COOH,
c)
d)
in which R5 is
1) a hydrogen atom,
2) (C1-C4)-alkyl
3) an amino acid radical,
4) a dipeptide radical or
5) a tripeptide radical.
R3 and R4 independently of one another can be:
a) a hydrogen atom or
b) —OH, and
n is the number 1, 2 or 3.
Type:
Grant
Filed:
April 16, 2001
Date of Patent:
June 11, 2002
Assignee:
Merck Patent Gesellschaft mit beschrankter
Abstract: A device and a method arc disclosed for indicating the reaching of a temperature within a predetermined temperature range by heated food. The device includes a transparent sealed container including a first compartment containing a first substance and a second compartment containing a second substance. The first compartment is separated from the second compartment by a meltable sealant having a melting point within the predetermined temperature range. The device is partially or fully immersed in the heated food and on reaching a temperature within the predetermined temperature range, the meltable sealant melts enabling the first substance to contact the second substance. The contact between the first substance and the second substance results in a detectable change such as a color change of at least one of the first substance and the second substance. The color change is visibly detectable through the transparent sealed container.
Type:
Grant
Filed:
September 17, 2001
Date of Patent:
June 11, 2002
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Abstract: The instant invention involves a combination therapy and pharmaceutical compositions comprised of a therapeutically effective amount of a cholesterol reducing agent such as an HMG-CoA reductase inhibitor in combination with a platelet aggregation inhibitor which is useful for inhibiting platelet aggregation, for inhibiting the formation of thrombotic occlusions, and for treating, preventing and reducing the risk of occurrence of cardiovascular and cerebrovascular events and related vaso-occlusive disorders.
Type:
Grant
Filed:
January 18, 2001
Date of Patent:
June 11, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Robert J. Gould, Steven A. Nichtberger, Patricia A. Rhymer, Lars Olofsson