Abstract: A process for preparation of eletriptan hydrobromide having ?-form of formula (I) is described that includes reducing 3-((R)-1-methylpyrrolidin-2-yl)methyl)-5-((E)-2-(phenylsulfonyl)vinyl)-1H-indole of formula (II) in presence of a metal catalyst to the product of formula (III) and then converting to hydrobromide salt having ?-form of formula (I).
Abstract: A method for producing 5-(aminomethyl)-2-chlorothiazole, which comprises the step of mixing a compound represented by formula (2): a mineral acid and a nitrite salt together.
Abstract: A quaternary ammonium salt of the formula (1), a composition containing the quaternary ammonium salt and an organic solvent, and an electrochemical device using the salt wherein R1 and R2 are both methyl and X? is BF4? or N(CF3SO2)2?.
Type:
Grant
Filed:
September 13, 2012
Date of Patent:
June 10, 2014
Assignees:
Otsuka Chemical Co., Ltd., Stella Chemifa Corporation
Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of the compounds or their pharmaceutical compositions, to a mammal in need thereof.
Abstract: This invention is directed to methods of preparing certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
Type:
Grant
Filed:
September 14, 2012
Date of Patent:
June 3, 2014
Assignee:
Xenon Pharmaceuticals Inc.
Inventors:
Jean-Jacques Cadieux, Mikhail Chafeev, Sultan Chowdhury, Jianmin Fu, Qi Jia, Stefanie Abel, Emad El-Sayed, Elke Huthmann, Thomas Isarno
Abstract: The present invention relates to pharmaceutically acceptable crystalline and amorphous salts of D-isoglutamyl-D-tryptophan as well as processes for their manufacture, pharmaceutical compositions comprising them, and their uses in the preparation of pharmaceutical compositions for the treatment of various conditions and/or diseases. In particular, the present invention relates to D-isoglutamyl-D-tryptophan potassium salt (1:1), D-isoglutamyl-D-tryptophan lithium salt (1:1), D-isoglutamyl-D-tryptophan calcium salt (2:1), D-isoglutamyl-D-tryptophan magnesium salt (2:1), and D-isoglutamyl-D-tryptophan organic ammonium salts (1:1).
Type:
Grant
Filed:
March 19, 2012
Date of Patent:
May 27, 2014
Assignee:
Apotex Technologies inc.
Inventors:
Tim Fat Tam, Blaise N'Zemba, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao, Lily Yu
Abstract: The present invention provides a production method of optically active 3-substituted-3-formyl-2-hydroxypropanoic acid compound (4), which includes a step of reacting glyoxylic acid compound (1-1) or (1-2) with aldehyde (2) in the presence of optically active pyrrolidine compound (3); wherein each symbol is as defined in the specification.
Abstract: A compound represented by the following general formula (I) (R1 and R2 represent hydrogen atom, an alkyl group, a halogen atom, etc.; R3 and R4 represent hydrogen atom, an alkyl group, an alkoxy group, or an alkenyl group; R5 represents hydrogen atom, an alkyl group, or nitro group, and R6 represents hydrogen atom or an alkyl group), which acts on the transcription process of genes.
Abstract: The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds.
Abstract: Contemplated compounds, compositions, and methods of prokineticin antagonists are presented where a prokineticin antagonist is used in the treatment and prevention of various conditions and disorders, and especially type II diabetes.
Type:
Grant
Filed:
December 16, 2009
Date of Patent:
May 13, 2014
Assignee:
The Regents of the University of California
Abstract: The present invention constitutes new 3-triazolylphenyl-substituted sulphide derivatives of the formula (I) in which A1, A2, B0, B1, B2, B3, X, R1, R2 and n are as defined in the description, to their use as acaricides and insecticides for controlling animal pests, and to processes for preparing them.
Type:
Grant
Filed:
August 19, 2010
Date of Patent:
May 13, 2014
Assignee:
Bayer CropScience AG
Inventors:
Bernd Alig, Stefan Antons, Reiner Fischer, Norbert Lui, Adeline Köhler, Arnd Voerste, Ulrich Görgens
Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.
Type:
Grant
Filed:
May 1, 2012
Date of Patent:
May 6, 2014
Assignee:
Bionomics Limited
Inventors:
Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn, Gabriel Kremmidiotis
Abstract: The invention provides a compound of formula(I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula(I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined in the specification.
Abstract: A family of six 8-amino boron dipyrromethenes having Formulas 1, 2, 3, 4, 6, and 7 has been prepared. The presence of the amine group alters the emission properties of the boron dipyrromethene, such that these compounds are characterized by unexpected blue fluorescence, providing for potential use as lasers. The compound having formula 1 has very high quantum yield. The 8-amino boron dipyrromethenes are prepared in a straightforward, high yield synthesis by substituting an amine group for the thiomethyl group at the 8 position in 8-thiomethyl boron dipyrromethene. The compounds having Formulas 6 and 7 may be used to incorporate peptides and proteins, thus providing biomolecules marked with fluorescent fragments.
Type:
Grant
Filed:
December 10, 2010
Date of Patent:
April 29, 2014
Assignee:
Universidad de Guanajuato
Inventors:
Eduardo Peña Cabrera, César Fernando Azael, Juan Orlando Flores
Abstract: The present invention relates to substituted 2-amino-N-(4-fluoro-3-{1-[1-(alkyl)-1H-indole-3-carbonyl]-piperidin-4-yl}-benzyl)-acetamides (compounds of formula I) compositions thereof, and their use in the treatment of inflammatory diseases.
Abstract: Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.
Type:
Grant
Filed:
August 4, 2011
Date of Patent:
April 29, 2014
Assignee:
Ferrokin Biosciences, Inc.
Inventors:
Amy E. Tapper, Hugh Y. Rienhoff, Jr., Stephan D. Parent, Patricia Andres, Jason A. Hanko, Huamin Zhang
Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
Type:
Grant
Filed:
April 30, 2012
Date of Patent:
April 29, 2014
Assignee:
BASF SE Ludwigshafen
Inventors:
Ulrich Berens, Oliver Dosenbach, Daniel Sprenger
Abstract: An object is to provide an aromatic amine compound with excellent heat resistance. Another object is to provide a light emitting element, a light emitting device, and an electronic device with excellent heat resistance. An aromatic amine compound represented by General Formula (1) is provided. The aromatic amine compound represented by General Formula (1) has a high glass transition point and excellent heat resistance. By using the aromatic amine compound represented by General Formula (1) for a light emitting element, a light emitting device, and an electronic device, a light emitting element, a light emitting device, and an electronic device with excellent heat resistance can be obtained.
Type:
Grant
Filed:
March 20, 2012
Date of Patent:
April 22, 2014
Assignee:
Semiconductor Energy Laboratory Co., Ltd.
Inventors:
Harue Nakashima, Sachiko Kawakami, Satoko Shitagaki, Satoshi Seo
Abstract: A method of catalytic oxidative coupling for the formation of hetero-coupled bis-arenes. The method includes placing a solvent, an arene compound, and a catalyst in a reactor having a oxidant atmosphere such that hetero-coupled bis-arenes are formed.
Type:
Grant
Filed:
April 30, 2009
Date of Patent:
April 22, 2014
Assignee:
Board of Governors for Higher Education, State of Rhode Island and Providence Plantations