Abstract: The present invention relates to compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Type:
Grant
Filed:
May 15, 2006
Date of Patent:
April 27, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Andreas Termin, Dean Wilson, Lev T. D. Fanning, Paul Krenitsky, Pramod Joshi
Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
Abstract: A catalyst and a process for preparing carboxylic acid esters from an aldehyde and an alcohol in the presence of molecular oxygen are disclosed. The catalyst comprises metals supported on a silica-containing support, wherein the metals consist essentially of palladium, lead, an alkali or alkaline earth metal, and at least one of niobium and zirconium. The process for preparing a carboxylic acid ester comprises reacting an aldehyde with an alcohol in the presence of molecular oxygen and the aforementioned catalyst.
Type:
Grant
Filed:
July 6, 2005
Date of Patent:
April 13, 2010
Assignee:
Lee Chang Yung Chemical Industry Corporation
Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.
Abstract: The invention relates to 5-diazacycloalkylpyrazole derivatives of the formula (I) or salts thereof a process for their preparation, to compositions thereof and to their use for the control of pests, including arthropods and helminths
Type:
Grant
Filed:
June 7, 2007
Date of Patent:
March 16, 2010
Assignee:
Merial Limited
Inventors:
Stefan Schnatterer, Michael Maier, Friederike Petry, Werner Knauf, Karl Seeger
Abstract: Novel hybrid monomers containing both the aryltrifluorovyinyloxyether-group (TFVE-group) and the cyanato-group, their synthesis, and the synthesis of polymers made from these new hybrid monomers are disclosed.
Type:
Grant
Filed:
May 24, 2006
Date of Patent:
March 9, 2010
Assignees:
Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V., Clemson University
Inventors:
Christian Dreyer, Monika Bauer, Suresh S. Iyer, Dennis W. Smith
Abstract: The invention relates to tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents.
Type:
Grant
Filed:
October 12, 2004
Date of Patent:
February 16, 2010
Assignee:
Bayer Schering Pharma AG
Inventors:
Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
Abstract: The invention relates to bis-5-pyrazolyl derivatives of formula (I) or salts thereof: wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).
Type:
Grant
Filed:
December 22, 2006
Date of Patent:
February 16, 2010
Assignee:
Merial Limited
Inventors:
Stefan Schnatterer, Michael Maier, Friederike Lochhaas, Werner Knauf, Karl Seeger
Abstract: The present invention relates to polymorphic forms of (1-{3-[3-(4-cyano-3-methoxy-phenyl)ureido]-phenyl}-ethyl)-carbamic acid-2-cyano-1-ethyl-ethyl ester, processes therein, pharmaceutical compositions thereof, and uses therewith.
Abstract: The present application discloses methods for the production of organic compounds comprising a linear series of five fused carbon rings. Such compounds are useful in the production of electronic components, devices and materials. For example the methods disclosed permit the production of 2,9- and 2,10-disubstituted pentacene compounds that present particularly advantageous properties for the manufacture of semiconductor materials, and may be used in devices such as for example thin film transistors and solar cells. Also disclosed are compounds that are excellent candidates for use in the manufacture of semiconductor materials, and other components of electronic systems, by virtue of their solubility, crystal packing geometries, and electronic properties.
Type:
Grant
Filed:
May 17, 2005
Date of Patent:
February 2, 2010
Assignee:
University of Ottawa
Inventors:
Alexander Graham Fallis, Matthew Allen Heuft, Christophe Bénard
Abstract: A thienopyrimidine compound of the formula: wherein R1, R2, R3, and R4 are as defined herein, and methods of use of such compounds for the treatment of melanocortin receptor-associated disorders.
Abstract: Crystalline aripiprazole Type II can be formed without solid state heat treatment. Instead a liquid is used such as in crystallizing from a solvent, especially 2-propanol, dimethyl sulfoxide, or a combination thereof with ethyl acetate, or in a solvent mediated solid-solid transformation, typically in ethyl acetate.
Type:
Grant
Filed:
March 17, 2006
Date of Patent:
February 2, 2010
Assignee:
Synthon BV
Inventors:
Gerrit J. B. Ettema, Raymond J. H. Westheim, Faysal Kalmoua
Abstract: The present invention relates to a process for preparing 3-cyano-3,5,5-trimethylcyclohexanone (isophoronenitrile) by reacting isophorone with hydrogen cyanide in the presence of a base as a catalyst to obtain a crude isophoronenitrile product, and subsequently distilling the crude isophoronenitrile product, with the addition before distillation of at least one specific sulfonic acid or specific carboxylic acid. In addition, the present invention relates to the use of a specific sulfonic acid or of a specific carboxylic acid as a neutralizing agent before distillation of a crude isophoronenitrile product which has been obtained by reacting isophorone with hydrogen cyanide in the presence of a base as a catalyst, in order to avoid precipitates in the neutralization of the base used as a catalyst with an acid.
Abstract: Method for oxygen treatment of liquid unsaturated carbon compounds with carbon number between 6 and 26 wherein the material is placed in a reaction chamber (11), a mixture ozone and oxygen is passed through the material, and by controlling the flow rate of the gas mixture through the material the temperature of the reaction is controlled to remain below a predetermined maximum value being 100° C. As a result of the reaction a novel material is obtained which has an epoxy-structure, has a higher density and smaller viscosity than the starting material, it has excellent burning properties and can be used as a limited rate source of oxygen. The apparatus for carrying of the method comprises an oxygen source, and ozonizer (6), a reaction chamber (11) for containing the liquid starting material, a gas pump (13) for removing the gas from the reaction chamber, and a temperature control system.
Type:
Grant
Filed:
December 4, 2002
Date of Patent:
January 19, 2010
Inventors:
Andras Bertha, Mihaly Lantos, Peter Kolta, Peter Kolta, legal representative, Gergely Kolta
Abstract: There is provided a process for stereoselectively producing E-form of 3-acyloxyacrylonitrile compound (3) or Z-form which comprises reacting 3-oxopropionitrile compound (1) with an acid chloride (2), characterized in that the reaction is conducted with removal of hydrogen chloride, or by using an organic base or an inorganic base, to thereby regulate the stereostructure of the product; a process for producing the compound (1) characterized by reacting acetonitrile compound (5) with an aromatic ester compound (6) by use of an alkali metal alkoxide in a hydrocarbon solvent while removing alcohol formed as a by-product by azeotropic distillation in a separating tank; and a process for isomerizing E-form of 3-acyloxyacrylonitrile compound to Z-form thereof by use of an organic base.
Abstract: A compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein the symbols have meaning as defined, which are antagonists of CCR-1 and which find use pharmaceutically for treatment of diseases and conditions in which CCR-1 is implicated, e.g. inflammatory diseases.
Type:
Grant
Filed:
October 24, 2003
Date of Patent:
January 12, 2010
Assignee:
Novartis AG.
Inventors:
Birgit Bollbuck, Jorg Eder, Richard Heng, Laszio Revesz, Achim Schlapbach, Rudolf Walchli
Abstract: Crystalline aripiprazole Form B can be formed by crystallizing from a solvent selected from 1-propanol, 2-propanol, 1-butanol, ethyl acetate, acetonitrile or a combination thereof.
Type:
Grant
Filed:
November 18, 2005
Date of Patent:
January 5, 2010
Assignee:
Synthon BV
Inventors:
Gerrit Jan Ettema, Raymond Westheim, Faysal Kalmoua
Inventors:
Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
Abstract: The present invention provides a heterocyclic compound having potent tyrosine kinase-inhibiting activity represented by formula: (wherein, R1b is a C6-10 aryl group which has substituent(s), and the like; Ta is a single bond, a C1-6 alkyl group, —CH2O—, and the like; X and Y are the same or different, and each is a nitrogen atom which may have substituent(s), and the like; the broken line is a single bond or a double bond; Za is a nitrogen atom or CH; W is a single bond, an oxygen atom, and the like; Q is a C6-10 aryl group which may have substituent(s) or an aromatic heterocyclic group which may have substituent(s)); or a salt thereof and a pharmaceutical composition comprising thereof.