Abstract: The present invention provides a novel ?-sulfonimide compound having at least one imide group and at least one sulfonyl group and a method for preparing the same.
Abstract: A compound having the structure useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
Type:
Grant
Filed:
March 5, 2012
Date of Patent:
January 29, 2013
Assignee:
Merck Sharp & Dohme Corp
Inventors:
Amjad Ali, Michael Man-Chu Lo, Zhiqiang Guo, Brent Whitehead, Timothy J. Henderson, Lin Yan, Shrenik K. Shah
Abstract: A series of mono- and binuclear 4-arylazo-3,5-diamino-pyrazoles which are useful for inhibition of cyclin-dependent kinases (preferably CDK9). Hence they can be used as antimitotic-, pro-apoptotic and antiinflammatory drugs, in particular, in chemotherapy of cancer and asthma, therapy of psoriasis and parasitoses as those caused by fungi or protists, treatment of Alzheimer's disease or as antineurodegenerative drugs, or to suppress immunostimulation. These compounds are useful in a variety of utilities, including as intermediates in the preparation of flame-retardants, diagnostic reagents and therapeutics, including antivirals and immunosuppressors.
Type:
Grant
Filed:
September 1, 2005
Date of Patent:
January 22, 2013
Assignee:
Univerzita Palackeho V Olomouci
Inventors:
Petr Cankar, Iveta Frysova, Vladimir Krystof, Rene Lenobel, Jan Slouka, Miroslav Strnad, Peter Martin Fischer
Abstract: A compound having the structure (I) wherein R is selected from the group consisting of 1) and 2), or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
Type:
Grant
Filed:
October 22, 2010
Date of Patent:
January 15, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Amjad Ali, Christopher Franklin, Ravi Nargund, Michael Man-Chu Lo, Lin Yan, Pei Huo
Abstract: A method for making diazo-compounds, diazonium salts thereof and other protected forms of these compounds. Diaz-compounds are prepared by reaction of a tertiary phosphine reagent carrying a reactive carbonyl group with an azide. The reaction can also generate an acyl triazene which can be converted thermally or by addition of base to form the diazo-compound or the acyl triazene can be isolated. The method is particularly useful for conversion of azides carrying one or more electron withdrawing groups to diazo-compounds. The method can be carried out in aqueous medium under mild conditions and is particularly useful for conversion of azido sugars to diazo-compound and diazonium salts thereof under physiological conditions. Tertiary phosphine reagents, particularly those that are water-soluble, and precursors for preparation of the reagents are provided.
Type:
Grant
Filed:
November 17, 2009
Date of Patent:
January 8, 2013
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Ronald Thaddeus Raines, Eddie Leonard Myers
Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
Type:
Grant
Filed:
December 20, 2010
Date of Patent:
January 8, 2013
Assignee:
Astrazeneca AB
Inventors:
Timothy Jon Luker, Rukhsana Tanseem Mohammed, Mark Dickinson, Stephen Thom
Abstract: An objective of this invention is to extend the range of choosing organic dye compounds as radiation-absorbing agents in a variety of fields by providing a novel organic dye compound which absorbs short-wavelength visible radiation and exhibits a superior in optical resistance, solubility in solvents, and heat characteristics required in a novel field in which the organic dye compound is applied: The objective is attainable by providing a cyanine dye which has a specific structure and exhibits a major adsorption maximum at a wavelength longer than 400 nm in a solution.
Abstract: The invention encompasses fluorescent cyanine dyes and methods of using such dyes. In particular, the invention encompasses near infrared polymethine cyanine dyes.
Type:
Grant
Filed:
August 15, 2008
Date of Patent:
January 1, 2013
Assignee:
Washington University
Inventors:
Samuel Achilefu, Hyeran Lee, John Christian Mason, Hyeran Lee, legal representative
Abstract: The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, as disclosed herein. The present invention also relates to pharmaceutical compositions comprising said compounds and to methods of using said compounds and compositions for modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
Type:
Grant
Filed:
January 23, 2007
Date of Patent:
December 25, 2012
Assignee:
Allergan, Inc.
Inventors:
Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
Abstract: The invention relates to a process for preparing naphthalen-2-yl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.
Type:
Grant
Filed:
April 24, 2009
Date of Patent:
December 11, 2012
Assignee:
Laboratorios del Dr. Esteve, S.A.
Inventors:
Antoni Torrens Jover, Jordi Corbera Arjona, Maria Rosa Cuberes-Altisent
Abstract: The present invention relates to a method for producing cyanoacrylic acid esters. The method is based substantially on a transesterification reaction, wherein the transesterification reaction is performed in the presence of at least one transition metal catalyst that is formed by reacting at least one hydroxyl group-containing support material with at least one transition metal alkoxide.
Type:
Grant
Filed:
January 3, 2012
Date of Patent:
December 11, 2012
Assignee:
Henkel AG & Co. KGaA
Inventors:
Carsten Friese, Andreas Kirschning, Ludovic Coutable
Abstract: The present invention relates to a process for the preparation of alkyl esters of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid, which are intermediates useful in the synthesis of (S)—N-(1-cyanocyclopropyl)-5-cyclopropyl-4,4-difluoro-2-((S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethylamino)pentanamide and related compounds, which are compounds that are cysteine protease inhibitors.
Type:
Grant
Filed:
August 16, 2010
Date of Patent:
December 4, 2012
Assignee:
ViroBay, Inc.
Inventors:
Barry Hart, Jeff Dener, Michael Green, Michael Standen, Oldrich Kocian
Abstract: The present invention relates to screens for compounds that can induce stem cell differentiation. In addition, isoxazoles and sulfonyl hydrazones are identified as general classes of compounds that can induce differentiation of stem cells into cells of neuronal and cardiac fate, respectively.
Type:
Grant
Filed:
May 26, 2011
Date of Patent:
November 27, 2012
Assignee:
The Board of Regents of the University of Texas System
Inventors:
Eric N. Olson, Douglas Frantz, Jenny Hsieh, Steven L. McKnight, Jay Schneider
Abstract: Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes.
Type:
Grant
Filed:
April 26, 2011
Date of Patent:
November 20, 2012
Assignee:
Biocon Limited
Inventors:
Jennifer A. Riggs-Sauthier, Nnochiri N. Ekwuribe
Abstract: A linker system is provided where a small molecule reactive group, e.g., an activity based probe which binds to certain enzymes at the active site, is linked through an aryl diazo linker to an affinity molecule such as biotin. The reactive group may comprise a number of functionalities known to react with a specific target to be studied. This enables the probe to be exposed to analytes, such as proteins and bind specifically to them to form a complex having an affinity molecule allowing immobilization of the bound analyte on an affinity column or other support, e.g. with streptavidin. Then, the linker is cleaved without causing removal of the affinity group or dissociation of the probe from the analyte. The linker is cleaved under mild reducing conditions, e.g., dithionite. The probe is synthesized along with the linker on a solid support.
Type:
Grant
Filed:
August 1, 2007
Date of Patent:
November 20, 2012
Assignee:
The Board of Trustees of the Leland Stanford Junior University
Inventors:
Matthew S. Bogyo, Steven H. L. Verhelst, Marko Fonovic
Abstract: The present invention relates to a labeling reagent of formula: in which: R1 represents at least one detectable label, L and A are each a linker arm, n is an integer equal to 1, and u is an integer between 0 and 2. The present invention also describes a method of synthesizing said markers and also applications for the labeling of biological molecules, more particularly nucleic acids, with a labeling reagent bearing diazo and nitro functions. The invention is particularly suitable for use in the diagnostics field.
Type:
Grant
Filed:
June 9, 2008
Date of Patent:
November 13, 2012
Assignees:
Biomerieux, CNRS, Universite de Strasbourg
Inventors:
Alain Laurent, Ali Laayoun, Mitsuharu Kotera
Abstract: The present invention provides an azo pigment comprising a group represented by the general formula (1) below, an electrophotographic photosensitive member comprising an intermediate layer comprising the azo pigment, and a process cartridge and an electrophotographic apparatus that comprise the electrophotographic photosensitive member.
Abstract: The present invention is directed to an isomerized alpha olefin sulfonate and a method of making the same wherein the isomerized alpha olefin sulfonate is derived from sulfonating an isomerized alpha olefin with sulfur trioxide in the presence of air thereby producing an isomerized alpha olefin sulfonic acid, wherein the isomerized alpha olefin is derived from the isomerization of C12-C40 normal alpha olefins; and neutralizing the isomerized alpha olefin sulfonic acid with a source of a mono-valent cation.
Type:
Grant
Filed:
July 29, 2011
Date of Patent:
October 30, 2012
Assignee:
Chevron Oronite Company LLC
Inventors:
Curtis Bay Campbell, Theresa Ann Denslow
Abstract: Disclosed is a method for producing a compound represented by Formula (4), the method including Step I of adding a solution in which hydrogen chloride is dissolved in an alcohol, to a mixture containing an organic solvent and a compound represented by Formula (1), and Step II of mixing a compound obtained in Step I, represented by Formula (3), with water.
Abstract: The present invention relates to a novel reactive dyestuff with a N-alkylamino group, represented by the following formula (I): wherein A1, A2, R1, R2, R3, R4, (R5)0-2, (R6)0-2, (Z1)0-1, (Z2)0-1, X1, X2 and n are defined the same as the specification. The reactive dyestuff of the present invention is suitable for exhaust dyeing, cold batch-up dyeing, continuous dyeing, printing and digital spray printing materials that contain hydroxyl group or amino group fibers.