Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting an organic azide and a terminal alkyne with a source of reactive Cu(I) ion for a time sufficient to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole. The source of reactive Cu(I) ion can be, for example, a Cu(I) salt or copper metal. The process is preferably carried out in a solvent, such as an aqueous alcohol. Optionally, the process can be performed in a solvent that comprises a ligand for Cu(I) and an amine.
Type:
Grant
Filed:
July 26, 2010
Date of Patent:
March 6, 2012
Assignee:
The Scripps Research Institute
Inventors:
K. Barry Sharpless, Valery Fokin, Vsevold V. Rostovtsev, Luke Green, Fahmi Himo
Abstract: A reversible thermochromic system comprising a) a compound of the formula (I) or a tautomer thereof (I) wherein R1 is C1-C18alkyl, C2-C18alkenyl, C3-C12cycloalkyl, C3-C12cycloalkyl substituted by 1, 2 or 3 C1-C4alkyl; or C7-C12phenylalkyl; R2 and R3 are hydrogen or R2 and R3 together form a group —CH?CH—CH?CH—; and R4 is hydrogen, —NO2, —SO2—R1 or (4-nitrophenyl)azo; and b) a compound containing a group of the formula (II).
Type:
Grant
Filed:
June 20, 2007
Date of Patent:
February 21, 2012
Assignee:
BASF SE
Inventors:
Walter Fischer, Abdel-Ilah Basbas, Martin Brunner, Rolf Benz, Manuele Vitali
Abstract: Magenta chromophore dyes which are stabilized by adding steric hindering groups to protect the imino carbons; nonlimiting examples of the steric hindering groups being phenyl, methyl, ethyl, isopropyl, fluoride, chloride, bromide and iodide groups.
Type:
Grant
Filed:
September 24, 2008
Date of Patent:
February 21, 2012
Assignee:
Hewlett-Packard Development Company, L.P.
Abstract: Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
Type:
Grant
Filed:
May 2, 2007
Date of Patent:
January 31, 2012
Assignee:
Anacor Pharmaceuticals, Inc.
Inventors:
Ving Lee, Jacob J. Plattner, Stephen J. Benkovic, Stephen J. Baker, Kirk R. Maples, Carolyn Bellinger-Kawahara, Tsutomu Akama, Yong-Kang Zhang, Rajeshwar Singh, Vittorio A. Sauro
Abstract: A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing compounds of Formula I and methods of treating diseases or disorders including metabolic and inflammatory or immune associated diseases or disorders.
Abstract: The invention relates to a compound represented by general formula (I) wherein Z represents N, O or S, and A represents a CH group, a nitrogen atom or an NL+ group wherein L represents a straight-chained or branched C1-C12 alkyl group. The invention also relates to a method for the preparation thereof and the use thereof as an antimitotic.
Type:
Grant
Filed:
May 13, 2005
Date of Patent:
January 31, 2012
Assignees:
Centre National de la Recherche, Universite de Rennes 1
Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
Type:
Grant
Filed:
December 3, 2010
Date of Patent:
January 24, 2012
Assignee:
Aquinox Pharmaceuticals Inc.
Inventors:
Lloyd Mackenzie, Tom MacRury, Curtis Harwig, Jeremy Pettigrew, Noor Aini Bhatti, Sam Place, Paul Bird, Vladimir Khlebnikov, Rudong Shan
Abstract: The present invention relates to novel yellow anionic dyes, a process for their preparation, certain novel intermediates necessary for their preparation and the use of these dyes for dyeing natural or synthetic materials, in particular, paper. The dyes are of formula (14), (15) or (16) in which R1 represents hydrogen, C1-C4alkyl, C1-C4alkoxy or SO3H, R2 represents SO3H or CO2H, R3 represents hydrogen, C1-C4alkyl, halogen, hydroxy, C1-C4alkoxy, carboxy, NH2 or NHC1-C4alkyl, R3a represents hydrogen or NH2 and A1 and A2, independently of the other, is selected from the group consisting of an acetoacetylated amine, a derivative of barbituric acid, a 2,4,6-triaminopyrimidine derivative, a pyridone derivative, an aminopyrazole or a pyrazolone derivative and a benzoic acid derivative, or A1 and A2, each one independently of the other, represent a certain phenol residue.
Type:
Grant
Filed:
March 29, 2010
Date of Patent:
January 24, 2012
Inventors:
Michael Lennartz, Adolf Käser, Sandra Weiss
Abstract: This invention relates to compositions comprising carbon-based diazeniumdiolates that release nitric oxide (NO). The carbon-based diazeniumdiolated molecules release NO spontaneously under physiological conditions without subsequent nitrosamine formation. The present invention also relates to methods of preparing the carbon-based diazeniumdiolated molecules, compositions comprising such molecules, methods of using such compositions, and devices employing such molecule compositions.
Type:
Grant
Filed:
July 2, 2009
Date of Patent:
January 24, 2012
Assignee:
Noxilizer, Inc.
Inventors:
Ernst V. Arnold, Blaine G. Doletski, Robert E. Raulli
Abstract: Nitroderivatives of prostaglandins having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
Type:
Grant
Filed:
May 11, 2009
Date of Patent:
January 24, 2012
Assignee:
Nicox S.A.
Inventors:
Francesca Benedini, Stefano Biondi, Valerio Chiroli, Wesley Kwan Mung Chong, Liming Dong, Achim Hans-Peter Krauss, Fabio Nicoli, Ganesh Prasanna, William Francois Vernier, Yi Yang
Abstract: Compounds effective for preventing, treatment or improving diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1, R2, R3, L1, L2, L3, X and Y are defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
Abstract: A method for producing special supramolecular assemblies of colorants, in particular cyanine dyes, called J aggregates consists in depositing a monolayer of dendrimers on a support and subsequently in deposing cyanines in solution for forming the organized monolayer of J aggregates. The method can be used for producing a secondary light source for injecting light into a waveguide from a light energy received from a primary light source emitting at different wavelength. The secondary source, which consists of the J aggregates incorporating energy acceptors, can also be integrated into an optical device incorporating the waveguide.
Type:
Grant
Filed:
November 10, 2006
Date of Patent:
January 3, 2012
Assignee:
CSEM Centre Suisse d'Electronique et de Microtechnique SA - Recherche et Developpment
Inventors:
Myriam Losson, Raphaël Pugin, Rolf Steiger, Véronique Monnier, Rino E. Kunz, Stanley Ross
Abstract: A novel class of pyridazine compositions and related methods of use.
Type:
Grant
Filed:
July 7, 2010
Date of Patent:
January 3, 2012
Assignees:
Northwestern University, Universite de Strasbourg, Centre National de la Recherche Scientifique, A Scientific Research Centre
Inventors:
Daniel Martin Watterson, Anu R. Sawkar, Thomas J. Lukas, Salida Mirzoeva, Linda J. Van Eldik, Marcel Hibert, Anastasia Velentza, Magdalena Zasadzki, Jacques Haiech, Jean-Jacques Bourguignon
Abstract: Disclosed is a group of azo quencher compositions useful as fluorescence quenchers having the general structure of formula 1, methods of making or using the compositions, and kits comprising the composition.
Type:
Grant
Filed:
October 16, 2008
Date of Patent:
December 27, 2011
Assignee:
Integrated DNA Technologies, Inc.
Inventors:
Andrei Laikhter, Mark Aaron Behlke, Joseph Walder, Kevin William Roberts, Yawfui Yong
Abstract: A method for manufacturing a charge control agent comprising steps of: an initiative chelating step by reacting with a monoazo compound represented by the following chemical formula [1] (in the chemical formula [1], —Ar1— and —Ar2— are aromatic groups) and a metal chelating agent to prepare an azo-type metal complex salt intermediate; a subsequent ion-exchanging step by reacting with the azo-type metal complex salt intermediate and an ammonium counter ion forming agent including an inorganic ammonium salt and aqueous ammonia to prepare an azo-type metal complex salt having an ammonium ion of a counter ion represented by the following chemical formula [2] (in the chemical formula [2], —Ar1— and —Ar2— are the same as the chemical formula [1]; M is a trivalent metal; B+ is a cation except an ammonium ion; n is from 0.70 to 1.00).
Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof:
Type:
Grant
Filed:
August 16, 2007
Date of Patent:
December 6, 2011
Assignees:
The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone, University Of Maryland, Baltimore
Inventors:
Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
Abstract: Anti-cancer compounds and manufacturing methods thereof are disclosed. The anti-cancer compounds are 1,8-diamidoanthraquinone derivatives with amino compounds. The manufacturing method includes the steps of: add 1,8-bis(chloroacetamido)anthraquinone or 1,8-bis(3-chloropropionamido)-anthraquinone with amino compounds, catalysts, and dehydrated dimethylformamide (DMF) to form a mixture and react with one another. Then by purification and recrystallization, the anti-cancer compounds are obtained. The anti-cancer compounds of the present invention are compounds with whole new structure that overcome serious cardiac toxicity of the conventional anti-cancer drug-doxorubincin.
Abstract: The invention is concerned with novel piperidine-amide derivatives of formula (I) wherein R1, R2, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and may be used to treat diseases associated with L-CPT1.
Type:
Grant
Filed:
May 23, 2008
Date of Patent:
October 18, 2011
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Mirjana Andjelkovic, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.
Type:
Grant
Filed:
April 19, 2011
Date of Patent:
September 20, 2011
Assignee:
Pliva Hrvatska D.O.O.
Inventors:
Edislav Leksic, Helena Ceric, Tina Mundorfer, Irena Zrinski Antonac, Zrinka Mastelic Samardzic