Abstract: This invention relates to compounds, compositions, and methods useful for modulating chemokine receptor (CXCR) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of CXCR gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of CXCR genes such as CXCR4 and CXCR7A.
Abstract: The present invention is related to sulfonamide derivatives of formula (I0 notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.
Type:
Grant
Filed:
September 28, 2000
Date of Patent:
September 6, 2011
Assignee:
Merck Serono SA
Inventors:
Stephen Arkinstall, Serge Halazy, Dennis Church, Montserrat Camps, Thomas Rueckle, Jean Pierre Gotteland, Marco Biamonte
Abstract: The present invention relates to heteroleptic electroluminescent metal complexes and to their preparation and use in electroluminescent devices, particularly to electroluminescent compounds having the general chemical formula:
Type:
Grant
Filed:
February 10, 2005
Date of Patent:
September 6, 2011
Assignee:
Merck Patent GmbH
Inventors:
Poopathy Kathirgamanathan, Subramaniam Ganeshamurugan, Gnanamoly Paramaswara, Muthulingham Kumaraverl, Arumugam Partheepan, Selvadurai Selvaranjan, Juan Antipan-Lara, Richard Price, Sivagnanasundram Surendrakumar
Abstract: This invention relates to compounds, compositions, and methods useful for modulating matrix metalloproteinase (e.g., MMP13) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of MMP13 gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of MMP13 genes.
Abstract: The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the following structure of formula (I): wherein A and B represents either a nitrogen atom or a CH group with the proviso that they cannot both simultaneously be CH, Q can represent a nitrogen or a carbon atom, and Y and Z are either a nitrogen atom, a N(O) group or a C(R5) group. Pharmaceutical compositions comprising the derivatives of formula (I) are also included.
Type:
Grant
Filed:
May 15, 2006
Date of Patent:
September 6, 2011
Assignee:
Merck Canada Inc.
Inventors:
Michel Belley, Jason Burch, John Colucci, Julie Farand, Mario Girard, Yongxin Han
Abstract: The invention relates to a pharmaceutical preparation comprising levothyroxine sodium, gelatine and fillers, which is free of organic solvent residues.
Abstract: The present invention relates to benzsulfonamide derivatives of formula I and methods of use thereof. The benzsulfonamide derivatives of the present invention are efficient modulators of the JNK pathway. In particular the benzsulfonamide derivatives of the present invention are selective inhibitors of JNK 2 and 3.
Type:
Grant
Filed:
June 19, 2008
Date of Patent:
August 30, 2011
Assignee:
Merck Serono SA
Inventors:
Serge Halazy, Dennis Church, Stephen J. Arkinstall, Marco Biamonte, Montserrat Camps, Jean-Pierre Gotteland, Thomas Rueckle
Abstract: This invention relates to compounds, compositions, and methods useful for modulating human immunodeficiency virus (HIV) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of human immunodeficiency virus (HIV) gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of HIV genes. The small nucleic acid molecules are useful in the treatment of HIV infection, AIDS, and/or disease and conditions related to HIV infection and/or AIDS in a subject or organism.
Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises an indole-sulfonamide moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
Type:
Grant
Filed:
October 26, 2009
Date of Patent:
August 30, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christopher J. Dinsmore, Douglas C. Beshore, Jeffrey M. Bergman, Craig W. Lindsley
Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
Type:
Grant
Filed:
May 3, 2010
Date of Patent:
August 30, 2011
Assignee:
Merck, Sharp & Dohme Corp.
Inventors:
Philippe G. Nantermet, Hemaka Anthony Rajapakse, Harold G. Selnick
Abstract: The present invention relates to the use of a compound that specifically binds to JAM-C or JAM-B for the treatment of gliomas. More specifically the invention relates to the use of an antagonist of JAM-B or JAM-C for the treatment of glioma, in particular astrocytoma.
Type:
Grant
Filed:
September 28, 2007
Date of Patent:
August 30, 2011
Assignee:
Merck Serono S.A.
Inventors:
Pierre-Yves Dietrich, Mirna Tenan, Michel Aurrand-Lions, Beat Albert Imhof
Abstract: The present invention relates to the use of end groups Y, where Y stands for CF3O— or F5S—, as hydrophobic end group in surface-active compounds, corresponding novel compounds, and processes for the preparation of these compounds.
Type:
Grant
Filed:
December 22, 2005
Date of Patent:
August 30, 2011
Assignee:
Merck Patent GmbH
Inventors:
Peer Kirsch, Klaus-Dieter Franz, Andreas Ruhl
Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Type:
Grant
Filed:
June 7, 2006
Date of Patent:
August 30, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Donna J. Armstrong, Essa H. Hu, Michael J. Kelly, III, Mark E. Layton, Yiwei Li, Jun Liang, Kevin J. Rodzinak, Michael J. Rossi, Philip E. Sanderson, Jiabing Wang
Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
Abstract: The invention relates to a method for detecting and analyzing clinical pictures and the causes thereof and determining appropriate therapy proposals. The invention is a system for detecting and analyzing clinical pictures and the causes thereof and for determining proposals for appropriate therapy, which can lead to a diagnosis and a corresponding therapy proposal even in the case of complex clinical causes and pictures, said proposal involving a maximum diagnostic certainty and minimum risk for the patient.
Type:
Grant
Filed:
June 14, 2003
Date of Patent:
August 30, 2011
Assignee:
Merck Patent Gesellschaft Mit Berschrankter Haftung
Inventors:
Martin Schulte, Marion Norden, Joachim Ganzer
Abstract: Compounds of the formula (I), in which X1, X2, X3, X4, R1, R2, R3 and R4 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:
September 24, 2009
Publication date:
August 25, 2011
Applicant:
MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Abstract: Disclosed are novel amino acid derivatives of formula (I) and (II) processes for the preparation thereof, and their use in the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole.
Type:
Application
Filed:
May 2, 2011
Publication date:
August 25, 2011
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Gerardus Johannes Kemperman, Jacobus Johannes Maria Van Der Linden, Michael R. Reeder
Abstract: The present invention relates to the use of IL-6 or a fragment, variant, fusion protein, functional derivative or salt thereof in microvascular complications.
Type:
Grant
Filed:
August 30, 2005
Date of Patent:
August 23, 2011
Assignee:
Merck Serono SA
Inventors:
Michel Dreano, Pierre-Alain Vitte, Norman Cameron, Mary A. Cotter
Abstract: Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabiniod inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.
Type:
Grant
Filed:
April 17, 2009
Date of Patent:
August 23, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Craig McKelvey, Sarah Geers, Justin Moser, Bhagwant Rege, Dina Zhang, Sutthilug Sotthivirat