Abstract: The present invention relates to novel enfumafungin derivatives of formula I and pharmaceutically acceptable salts thereof, their synthesis, and their use as inhibitors of (1,3)-?-D-glucan synthase. The present compounds and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the present compounds and pharmaceutically acceptable salts thereof, are useful for treating or preventing antifungal infections and associated diseases and conditions.
Type:
Grant
Filed:
March 29, 2007
Date of Patent:
January 4, 2011
Assignees:
Merck Sharp & Dohme Corp., Scynexis, Inc.
Inventors:
James M. Balkovec, Frances Aileen Bouffard, Bruno Tse, James Dropinski, Dongfang Meng, Mark L. Greenlee, Michael Peel, Weiming Fan, Ahmed Mamai, Hao Liu, Keqaing Li
Abstract: The present invention relates to genetic markers whose expression is correlated with breast cancer. Specifically, the invention provides sets of markers whose expression patterns can be used to differentiate clinical conditions associated with breast cancer, such as the presence or absence of the estrogen receptor ESR1, and BRCA1 and sporadic tumors, and to provide information on the likelihood of tumor distant metastases within five years of initial diagnosis. The invention relates to methods of using these markers to distinguish these conditions. The invention also relates to kits containing ready-to-use microarrays and computer software for data analysis using the statistical methods disclosed herein.
Type:
Grant
Filed:
June 23, 2008
Date of Patent:
January 4, 2011
Assignees:
The Netherlands Cancer Institute, Merck Sharp & Dohme Corp.
Inventors:
HongYue Dai, Yudong He, Peter S. Linsley, Mao Mao, Christopher J. Roberts, Laura Johanna Van't Veer, Marc J. Van de Vijver, Rene Bernards, Augustinus A. M. Hart
Abstract: The present invention describes new types of metal complexes. Such compounds can be used as functional materials in a series of different types of applications which can be classified within the electronics industry in the widest sense. The inventive compounds are described by the formulae (1) and (4).
Type:
Application
Filed:
September 1, 2010
Publication date:
December 30, 2010
Applicant:
Merck Patent GmbH
Inventors:
Rocco Fortte, Philipp Stössel, Anja Gerhard, Horst Vestweber
Abstract: The present invention is directed to a method for treating tumors and cancer cells by administering an immunocytokine following radiation treatment. This combination of treatments can stimulate an immune response at irradiated and non-irradiated sites, which is useful in eradicating cancer cells that have spread from the site of the primary tumor. In addition, immunocytokines can be administered at a dose that is less that the maximum tolerated dose, which reduces the side effects associated with immunocytokine therapy.
Type:
Application
Filed:
October 21, 2009
Publication date:
December 30, 2010
Applicant:
Merck Patent GmbH
Inventors:
Thomas Wickham, Ulrike Gnad-Vogt, Sylvia Holden, Stephan G. Klinz, Karl-Josef Kallen
Abstract: The present invention relates to photovoltaic cells comprising group IV-VI semiconductor nanocrystals as photoactive components. In particular, these nanocrystals are of core-shell or core-alloyed shell configuration, each comprising a core of a first group IV-VI semiconductor material having a selected band gap energy, and either a core-overcoating shell consisting of a second group IV-VI semiconductor material or a core-overcoating alloyed shell consisting of an alloy of said first group IV-VI semiconductor material and a second group IV-VI semiconductor material, respectively.
Abstract: The present invention provides monolithic supports produced from linear aliphatic polyamides. It also provides a method of producing said monolithic supports by dissolution/precipitation of linear aliphatic polyamides. Finally, the invention provides using said supports in chromatography as well as chromatography columns containing said supports.
Type:
Application
Filed:
January 27, 2009
Publication date:
December 30, 2010
Applicant:
MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Abstract: Novel compounds of the Formula (I) in which R1, R2, R3, and R4 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Type 1 and 2, obesity, neuropathy and/or nephropathy.
Type:
Application
Filed:
February 2, 2009
Publication date:
December 30, 2010
Applicant:
Merck Patent GMBH
Inventors:
Lars Burgdorf, Ulrich Emde, Johannes Gleitz, Norbert Beier, Christine Charon
Abstract: The present invention relates to dielectrically positive liquid-crystalline media comprising one or more compounds of the formula I in which the parameters have the meaning indicated in the specification, and optionally one or more compounds selected from the group of the compounds of the formulae II and III in which the parameters have the meaning indicated in the specification, and optionally one or more compounds of the formula IV in which the parameters have the meaning indicated in the specification, and to liquid-crystal displays containing these media, especially to active-matrix displays and in particular to TN, IPS and FFS displays.
Type:
Application
Filed:
January 27, 2009
Publication date:
December 30, 2010
Applicant:
Merck Patent GmbH
Inventors:
Markus Czanta, Harald Hirschmann, Michael Wittek, Volker Reiffenrath, Renate Bender, Christian Hock, Brigitte Schuler
Abstract: In OLEDs, improved efficiency is obtained by novel compounds which can form inter alia electron injection layers of the formula (I) wherein R1 is a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with one or more C1-C4 alkyl, alkoxy or cyano; R2 and R3 together form a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with C1-C4 alkyl, alkoxy or cyano; R4 is hydrogen, C1-C4 alkyl or aryl; and Ar is monocyclic, bicyclic or tricyclic aryl or heteroaryl which is optionally substituted with one or more C1-C4-alkyl or alkoxy groups, or an oligomer thereof.
Abstract: The invention relates to a porous polymeric monolith based on a polymerised high internal phase emulsion (polyHIPE) which is hypercrosslinked, and to the preparation and use thereof, preferably as gas storage material.
Type:
Application
Filed:
January 14, 2009
Publication date:
December 30, 2010
Applicant:
Merck Patent GmbH
Inventors:
Gerhard Jonschker, Matthias Koch, Joerg Pahnke, Matthias Schwab
Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R2?, R2?, R3, R4, R5, R6, R7 and R8 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.
Type:
Application
Filed:
December 23, 2008
Publication date:
December 30, 2010
Applicant:
Merck Patent Gesellschaft Mit Beschrankter Haftung
Inventors:
Stefan Bender, Lars Thore Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
Abstract: The present invention relates to the compounds of the formula (1) and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as host material in the emitting layer and/or as electron-transport material.
Type:
Application
Filed:
February 13, 2009
Publication date:
December 30, 2010
Applicant:
Merck Patent GmbH
Inventors:
Arne Buesing, Holger Heil, Philipp Stoessel
Abstract: The present invention discloses peptides isolated from the extracellular domain of OX40 Ligand (OX40L) capable of binding OX40 Receptor (OX40R) and inhibiting OX40R-OX40L interaction. Such peptides, fusion proteins comprising them, as well as peptides and other molecules designed on their sequences, can be used as OX40R binding agents competing with natural OX40L for blocking OX40R-mediated cell signaling in the prophylaxis and/or treatment of diseases related to activated T cells.
Abstract: The present invention relates to compounds, compositions, and methods useful for modulating the expression of genes associated with respiratory and pulmonary disease, such as cholinergic muscarinic receptor genes, using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of cholinergic muscarinic receptor genes, or other genes involved in pathways of cholinergic muscarinic receptor 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 M3 muscarinic acetylcholine receptor or cholinergic receptor muscarinic 3 (CHRM3).
Abstract: The invention relates to a method and reagent mixture for the staining and thus visualization of amino acids, peptides and similar compounds, in particular after separation by means of thin-layer chromatography. The staining is carried out using ninhydrin for the detection of amino acids, peptides or proteins in combination with at least one ionic liquid.
Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.
Type:
Grant
Filed:
April 10, 2007
Date of Patent:
December 28, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Richard Berger, Scott Edmondson, Alexa Hansen, Cheng Zhu
Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R3, R4 have the meaning cited in the claims, to methods for the production thereof, agents containing said compounds and to their use for the functionalisation of matrices, in particular their use as skin and/or hair-binding UV filters.
Abstract: The invention provides a method for qualitatively and quantitatively detecting methyl malonic acid in a clinical sample that also may contain succinic acid and homocysteine, said method involving a liquid chromatography separation step followed by a mass spectroscopy detection step, said method comprising the steps of: a) providing a sample that may contain methyl malonic acid and/or succinic acid and optionally homocysteine; b) injecting said sample in a mobile phase comprising a high amount of water-miscible organic solvent; c) eluting said mobile phase containing said sample through a liquid chromatography column containing zwitterionic groups covalently bound to carriers as a stationary phase; d) detecting the possible presence of methyl malonic acid and succinic acid and optionally homocysteine by mass spectroscopy detection; and e) determining the presence and optionally the amounts of said organic molecules using calibration data.
Abstract: Compounds of Formula I: I (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. 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 CGRP receptors are involved.
Abstract: The present invention is directed to compounds of formula (I) (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
Type:
Application
Filed:
February 3, 2009
Publication date:
December 23, 2010
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco