Abstract: Amide and urea derivatives of the formula I R1—(CH2)n—(Y)q-(Z)r-CO—NH—R2 ??(I) in which R1, n, Y, q, Z, r and R2 have the meanings indicated in claim 1, are potent 5-HT1B/1D antagonists and exhibit 5-HT reuptake-inhibiting actions and are suitable for the treatment and prophylaxis of anxiety states, depressions, schizophrenia, compulsive ideas, tardive dyskinesias, learning disorders, age-dependent memory disorders, for positively affecting obsessive-compulsive behaviour (OCD), and also for the treatment and for the control of the sequelae of cerebral infarcts such as stroke and cerebral ischaemias.
Type:
Application
Filed:
July 2, 2003
Publication date:
August 11, 2005
Applicant:
MERCK PATENT GMBH
Inventors:
Christoph Van Amsterdam, Hartmut Greiner, Henning Boettcher, Gerd Bartoszyk, Juergen Harting, Lisa Matzen, Wilfried Rautenberg
Abstract: Pyridazine derivatives of the formula (I) act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.
Abstract: The present invention relates to compounds 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 angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
Type:
Grant
Filed:
August 26, 2002
Date of Patent:
August 9, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Yuntae Kim, Barbara Hanney, Keith L. Spencer, George D. Hartman, Kenneth L. Arrington
Abstract: A system and method for assessing the performance of a system for delivering a pharmaceutical agent to a portion of a body. A pair of electrodes are applied to the portion of the body. A pharmaceutical agent is infused into the portion of the body and the electrodes are energized by a signal generator, electrically stimulating the portion of the body. The voltage and current delivered to the portion of the body are measured using a data acquisition system thereby generating electrical parameter data. An immune response, gene expression level or other biological response to the pharmaceutical agent is measured and the electrical test data is correlated with the biological response to assess the performance of the system.
Abstract: A sodium salt of Compound A is disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for preventing or treating HIV infection, for delaying the onset of AIDS, and for treating AIDS.
Type:
Grant
Filed:
August 14, 2002
Date of Patent:
August 2, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Wei Xu, John V. Lepore, Amar J. Mahajan
Abstract: A birefringent film comprising at least one birefringent layer of liquid crystal material forming multi domains with a splayed structure may be coated onto a reflective substrate, e.g., with an aluminium surface. The birefringent film is particularly suited for decorative, security, authentification or identification applications.
Type:
Grant
Filed:
February 5, 2003
Date of Patent:
August 2, 2005
Assignee:
Merck Patent GmbH
Inventors:
Robert Hammond-Smith, John Patrick, Donald Gordon Graham
Abstract: Lipid Binding Protein 4 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing Lipid Binding Protein 4 polypeptides and polynucleotides in diagnostic assays.
Abstract: This invention relates to a process for making spiro isobenzofuranone compounds by coupling of an aminopyrazine fragment with a spirolactone piece.
Abstract: The present invention relates to the colored inscription or marking of plastics and surface coatings, including powder coatings, in which a colorant is transferred into the plastic or surface coating by laser radiation with the aid of a laser light-absorbent substance.
Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions related to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of a mammalian species, particularly humans.
Type:
Grant
Filed:
February 10, 2003
Date of Patent:
August 2, 2005
Assignee:
Merck & Co. Inc.
Inventors:
Maria L. Garcia, Gregory J. Kaczorowski, Owen B. McManus
Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful 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 preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
Type:
Grant
Filed:
October 10, 2001
Date of Patent:
July 26, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Robert P. Gomez, Steven D. Young, Melissa Egbertson, John S. Wai, Linghang Zhuang, Mark Embrey, Jeffrey Y. Melamed, H. Marie Langford, James P. Guare, Thorsten E. Fisher, Samson M. Jolly, Michelle S. Kuo, Debra S. Perlow, Jennifer J. Bennett, Timothy W. Funk
Abstract: A microcomponent connection system (1) having an accomodation device for plate-shaped microcomponents (7) has a connection block (2) and a lifting device (6), by means of which the microcomponent (7) and the connection block (2) can be pressed against one another. The connection block (2) has electrical and fluid line connections (8, 9) and optical line connections (16), each of which projects in a sprung or spring-mounted manner on the underside of the connection block (2). In order to connect the microcomponent (7) to the associated line connections (8, 9, 16), the microcomponent (7) is pressed by the lifting device (6) in the direction of the connection block (2) against the electrical line connections (8) or fluid line connections (9) designed as electrically conducting spring tongues or as hollow rams (10), or optical line connections (16).
Type:
Application
Filed:
February 10, 2003
Publication date:
July 21, 2005
Applicant:
Merck Patent GmbH
Inventors:
Renate Bender, Gunter Brenner, Thomas Greve, Matthias Joehnck, Bernd Stanislawski, Michael Schmelz, Sigrid Sturmfels
Abstract: N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
Type:
Grant
Filed:
January 30, 2003
Date of Patent:
July 19, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Michael R. Wood, Neville J. Anthony, Mark G. Bock, Dong-Mei Feng, Scott D. Kuduk, Dai-Shi Su, Jenny Miu-chun Wai
Abstract: Aqueous coating solution having a pH of from 3 to 8, comprising 0.5-5.0% by weight of [SiOx(OH)y]n particles, where 0<y<4 and 0<x<2, having a particle size of from 10 nm to 60 nm with a tolerance of ±10%, and from 0.005 to 0.5% by weight, based on the coating solution, of a surfactant mixture obtainable by hydrolytic polycondensation of tetraalkoxysilanes in an aqueous-alcoholic-ammoniacal medium at temperatures between 35° C. and 80° C., with subsequent removal of ammonia and alcohol from the resultant dispersion by steam distillation and subsequent addition of a surfactant mixture comprising 15-30% by weight of anionic surfactants, 5-15% by weight of nonionic surfactants and less than 5% by weight of amphoteric surfactants.
Abstract: The invention relates to modified recombinant allergen mutants which can be obtained from recombinant allergens which are derived from allergens which can be obtained by extraction from natural raw materials such as pollen of the species Phleum pratense. While these modified recombinant allergens stimulate lymphocytes from patients who are allergic to pollent to proliferate and synthesize cytokines, they exhibit a markedly diminished ability to bind to the IgE antibodies which are present in the serum of the T lymphocyte donors and to grass pollen allergen-specific IgEs and can therefore be used for a specific, made-to-release allergy therapy.
Type:
Grant
Filed:
March 16, 1998
Date of Patent:
July 19, 2005
Assignee:
Merck Patent Gesellschaft mit
Inventors:
Helga Kahlert, Hans-Thomas Stüwe, Helmut Fiebig, Oliver Cromwell, Wolf-Meinhard Becker, Albrecht Bufe, Gabriele Schramm, Lothar Jäger, Wolf-Dieter Müller
Abstract: 8-arylquinolines of formula (I) wherein the aryl group at the 8-position contains a meta two atom bridge to an optionally substituted phenyl or pyridyl group, are PDE4 inhibitors useful to treat asthma, chronic bronchitis, chronic obstructive pulmonary disease, arthritis, respiratory distress syndrome, allergic rhinitis, neurogenic inflammation, pain, rheumatoid arthritis, and other diseases. R1-R7 and Ar are as in claim 1.
Type:
Grant
Filed:
June 26, 2002
Date of Patent:
July 19, 2005
Assignee:
Merck Frosst Canada & Co.
Inventors:
Daniel Dube, Yves Girard, Dwight MacDonald, Anthony Mastracchio, Michel Gallant, Patrick Lacombe, Denis Deschenes
Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful 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 preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
Type:
Grant
Filed:
October 9, 2001
Date of Patent:
July 19, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Robert P. Gomez, Steven D. Young, Melissa S. Egbertson, John S. Wai, Jennifer J. Bennett
Abstract: Coumermycin analogs of general formula I: wherein X, a linking group, is selected from the group consisting of alkyl, aryl, diaryl, substituted alkyl, substituted aryl, alkyl with hereroatoms in the chain, heteroaryl, cyclic and bicyclic alkyl, and a combination of alkyl, aryl and heteroaryl substituents. The compounds are suitable for use as chemical dimerizers of chimeric proteins.
Type:
Grant
Filed:
April 23, 2001
Date of Patent:
July 12, 2005
Assignee:
Merck & Co. Inc.
Inventors:
Michael A. Farrar, Steven H. Olson, Roger M. Perlmutter, Llnon H. Slossberg