Abstract: The present invention is directed to benzazole compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
Type:
Grant
Filed:
February 17, 2006
Date of Patent:
June 14, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Steven P. Govek, Jean-Michel Vernier, Theodore Kamenecka, John H. Hutchinson, Richard Pracitto
Abstract: The present invention provides a method for identifying siRNA target motifs in a transcript using a position-specific score matrix approach. The invention also provides a method for identifying off-target genes of an siRNA using a position-specific score matrix approach. The invention further provides a method for designing siRNAs with higher silencing efficacy and specificity. The invention also provides a library of siRNAs comprising siRNAs with high silencing efficacy and specificity.
Type:
Grant
Filed:
October 27, 2004
Date of Patent:
June 14, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Aimee L. Jackson, Steven R. Bartz, Julja Burchard, Peter S. Linsley, Wei Ge, Guy L. Cavet
Abstract: The invention relates to solid forms of antibodies against the EGF receptor, in particular precipitates and crystals of monoclonal antibodies against the EGF receptor, particularly preferably of Mab C225 (cetuximab) and Mab h425 (EMD 72000), which result in biologically active antibody protein through dissolution or suspension in aqueous medium, obtainable by precipitation of the antibody and/or one of its variants and/or fragments dissolved or suspended in aqueous medium by means of a precipitation reagent. The invention furthermore relates to pharmaceutical preparations comprising at least one solid form of above-mentioned antibodies in precipitated non-crystalline, precipitated crystalline or in soluble or suspended form, and optionally excipients and/or adjuvants and/or further pharmaceutical active ingredients, and to a process for the preparation of solid forms of anti-EGFR antibodies according to the invention.
Abstract: The invention is directed to a fusion protein which includes a first portion including an immunoglobulin (Ig) chain and a second portion including interleukin-7 (IL-7).
Abstract: Compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R3, R4, R5 and R6 have the meanings indicated in Claim 1, are suitable as ligands of 5 HT receptors.
Type:
Grant
Filed:
March 8, 2004
Date of Patent:
June 14, 2011
Assignee:
Merck Patent GmbH
Inventors:
Oliver Schadt, Kai Schiemann, Christoph Van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
Abstract: The instant invention provides compounds of Formula I which are leukotriene biosynthesis inhibitors. Compounds of Formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
Type:
Grant
Filed:
February 1, 2008
Date of Patent:
June 14, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Erich L. Grimm, Yves Ducharme, Richard Frenette, Richard Friesen, Marc Gagnon, Helene Juteau, Sebastien Laliberte, Bruce MacKay, Yves Gareau
Abstract: A method of treating Alzheimer's disease, Parkinson's disease, sexual dysfunction or erectile dysfunction in a man by administration of a 5alpha reductase inhibitor together with a testosterone supplement is described. The method is also concerned with the use of the 5alpha reductase inhibiting compound and the testosterone supplement together with another agent useful for treating erectile dysfunction, including PDE V inhibitors; AGE (advanced glycation end-product) breakers; alpha 1 blockers; alpha 1A antagonists; alpha 2 antagonists; dopamine agonists; dopamine D4 agonists; melanocortin agonists; oxytocin agonists; prostaglandin; radical scavengers; rotamase inhibitors; aviptadil; nitroglycerine; and GPCR agonists for treating male sexual dysfunction or erectile dysfunction.
Abstract: Compounds of the formula I, in which R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
Type:
Application
Filed:
July 18, 2008
Publication date:
June 9, 2011
Applicant:
MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG
Inventors:
Dieter Dorsch, Oliver Schadt, Andree Blaukat, Frank Stieber
Abstract: The invention relates to a modified separating material having improved properties, to the preparation thereof, and to the use thereof for the separation of charged biopolymers from liquids.
Type:
Application
Filed:
July 8, 2009
Publication date:
June 9, 2011
Applicant:
MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Abstract: The invention relates to the determination of the degree of membrane receptor binding by specific monoclonal antibodies. This method is notably beneficial for monoclonal antibodies that are used in targeted therapies in order to define a target effective dose (TED). Especially the invention relates to the determination of the saturation degree of receptor binding effected by an anti-EGFR antibody of interest.
Abstract: FSH mutant with increased glycosylation and longer half-life is described. The use of this FSH mutant for inducing folliculogenesis in human patients is also described.
Type:
Grant
Filed:
January 16, 2007
Date of Patent:
June 7, 2011
Assignee:
Merck Serono SA
Inventors:
Marco Muda, Xuliang Jiang, Sean D. McKenna
Abstract: Disclosed herein are methods and compositions for enhancing the immunogenicity of a preselected protein or peptide antigen in a mammal. Immunogenicity is enhanced by fusing the preselected antigen to an immunoglobulin heavy chain constant region to produce an Fc-antigen fusion protein. The Fc-antigen fusion proteins bind Fc receptors on the surface of antigen presenting cells, thereby targeting the antigen to the antigen presenting cells in the mammal. In addition, disclosed is a family of adjuvants, for example, an Fc-adjuvant fusion protein, for use in combination with the Fc-antigen fusion proteins to enhance or modulate a particular immune response against the preselected antigen.
Type:
Grant
Filed:
March 24, 2005
Date of Patent:
June 7, 2011
Assignee:
Merck Patent GmbH
Inventors:
Stephen D. Gillies, Kin-Ming Lo, John S. Wesolowski, Jr.
Abstract: The chroman compounds of the formula I according to the invention R1-(A1-Z1)a—W1—(Z2-A2)b-Z3—W2—(Z4-A3)c-R2 in which R1, A1, A2, A3, W1, W2, Z1, Z2, Z3, Z4, a, b and c have the meanings indicated in claim 1, have two moieties W1 and W2 derived from chroman. The compounds are suitable as components of anisotropic switching media, as used, for example, in liquid-crystal display devices.
Type:
Grant
Filed:
December 11, 2007
Date of Patent:
June 7, 2011
Assignee:
Merck Patent Gesellschaft
Inventors:
Andreas Taugerbeck, Alexander Hahn, Achim Goetz
Abstract: The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Type:
Grant
Filed:
January 18, 2006
Date of Patent:
June 7, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Wallace T. Ashton, Charles G. Caldwell, Hong Dong, Ying-Duo Gao, Giovanna Scapin, Ann E. Weber
Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds (I) pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
Abstract: The present invention relates to a glass composition comprising crystalline phases, and to glass flakes produced therefrom. These glass flakes can be used as base substrate for effect pigments. The glass flakes can furthermore be used in paints, coatings, printing inks, plastics and in cosmetic formulations. The glass flakes are converted into glass-ceramics, and are present in one of the following composition ranges I or II in % by weight: I: 40-50 SiO2, 10-20 B2O3, 10-20 Na2O, 15-30 TiO2; II: 10-60 SiO2, 5-30 B2O3, 5-40 TiO2, 2-20 Nb2O5, 2-20 Fe2O3, 5-40 Na2O+K2O+CaO+SrO+BaO.
Type:
Application
Filed:
May 15, 2009
Publication date:
June 2, 2011
Applicant:
MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Inventors:
Reinhold Rueger, Anke Geisen, Gerald Karn
Abstract: The present invention relates to compounds of formula (I) wherein X, Y, Z, R1, R2, R3 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diabetes, metabolic syndrome, obesity, cancer, inflammation.
Type:
Application
Filed:
May 19, 2009
Publication date:
June 2, 2011
Applicant:
Merck Patent GmbH
Inventors:
Daniel Cravo, Sophie Hallakou-Bozec, Franck Lepifre
Abstract: The invention relates to a process for the preparation of bis(fluoroalkyl)phosphinic acid and/or fluoroalkylphosphonic acid by reaction of, monofluoroalkyltetrafluorophosphorane bis(fluoroalkyl)trifluorophosphorane or tris(fluoroalkyl)difluorophosphorane with water.
Type:
Application
Filed:
July 8, 2009
Publication date:
June 2, 2011
Applicant:
Merck Patent Gesellschaft Mit Beschrankter Haftung
Inventors:
Nikolai Mykola Ignatyev, Dana Bejan, Helge Willner
Abstract: The present invention relates to a hydrophilic crosslinked polymer, preferably in the form of porous particles, and to the preparation and use thereof. The polymer according to the invention is produced by polymerisation from chain-forming hydrophilic vinyl ethers and crosslinking, preferably heterocyclic divinyl ethers.
Abstract: Novel compounds of the formula (I) in which D, E, Q, T, X, Y, Z, Z?, R1, R4 and R4? have the meanings indicated, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.
Type:
Grant
Filed:
November 19, 2004
Date of Patent:
May 31, 2011
Assignee:
Merck Patent GmbH
Inventors:
Bertram Cezanne, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Johannes Gleitz