Boron Acids Or Salts Thereof (i.e., Compounds Having -xh, Wherein X Is Chalcogen, Attached Directly To Boron By Nonionic Bonding And Wherein The Hydrogen May Be Replaced By A Group Ia Or Iia Light Metal, Or By Substituted Or Unsubstituted Ammonium) Patents (Class 562/7)
  • Patent number: 9410970
    Abstract: A triple sensor structured for simultaneous measurement of glucose, oxygen, and pH. The sensor components are in thin film states such as sensing films or membranes, with a glucose probe associated with emission of radiation in the blue part of the spectrum, an oxygen probe associated with radiation in red portion of the spectrum, and a pH probe—with a green portion of the spectrum. The optical probes are chemically grafted or immobilized in a suitable polymer matrix, alleviating the leaching of the probes from the matrix, improving the thin film sensing stability, and enabling the repeatable use of the same sensing films.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: August 9, 2016
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
    Inventors: Yanqing Tian, Liqiang Zhang, Fengyu Su, Deirdre Meldrum, Sean Buizer, Clifford L. Anderson, Laimonas Kelbauskas, Kristen Lee
  • Patent number: 9284270
    Abstract: The present application provides methods and catalysts for activation of carboxylic acids for organic reactions.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: March 15, 2016
    Assignees: The Governers of the University of Alberta, Greencentre Canada
    Inventors: Dennis Hall, Nicolas Gernigon, Raed M. Al-Zoubi, Paul D. Thornton
  • Publication number: 20150094468
    Abstract: The present invention relates to a novel diamine compound represented by the general formula (1), a ruthenium-diamine complex, an iridium-diamine complex, and a rhodium-diamine complex having the diamine compound as a ligand. Furthermore, the present invention relates to methods for selectively producing optically active compounds by using any of these complexes as a catalyst. wherein R1, R2, R3, X, Y, and Z are as defined in claim 1.
    Type: Application
    Filed: September 26, 2014
    Publication date: April 2, 2015
    Applicant: TAKASAGO INTERNATIONAL CORPORATION
    Inventor: Taichiro TOUGE
  • Publication number: 20150080341
    Abstract: The inventive boronic acid analogs are potent inhibitors of Arginase I and II activity. These compounds are candidate therapeutics for treating a disease or disorder associated with an imbalance in the activity or concentration of cellular arginase I and arginase II enzymes. The invention also provides pharmaceutical compositions of the inventive compounds and methods for using the compositions for therapy.
    Type: Application
    Filed: March 13, 2013
    Publication date: March 19, 2015
    Inventors: Michael Van Zandt, Gunnar Erik Jagdmann, JR.
  • Publication number: 20150072942
    Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
    Type: Application
    Filed: April 8, 2014
    Publication date: March 12, 2015
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Julian Adams, Yu-Ting Ma, Ross L. Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
  • Publication number: 20140371175
    Abstract: Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, R5, R6, R7, R8, R9, D, M, X, and Y are defined as set forth in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use for treating or preventing a disease or a condition associated with arginase activity.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Michael Van Zandt, Adam Golebiowski, Min Koo Ji, Darren Whitehouse, Todd Ryder, Raymond Paul Beckett
  • Publication number: 20140364396
    Abstract: The present invention provides compounds of Formula (I) as inhibitors of LMP7 for the treatment of autoimmune and inflammatory diseases.
    Type: Application
    Filed: December 21, 2012
    Publication date: December 11, 2014
    Inventors: Dominique Swinnen, Stefano Crosignani, Jeyaprakashnarayanan Seenisamy, Federica Morandi
  • Publication number: 20140343019
    Abstract: The inventive compounds are small molecule therapeutics that are potent inhibitors of Arginase I and II activity. The invention also provides pharmaceutical compositions of the inventive compounds and methods for using the inventive compounds for treating or preventing a disease or a condition associated with arginase activity.
    Type: Application
    Filed: October 18, 2012
    Publication date: November 20, 2014
    Inventors: Michael Van Zandt, Adam Golebiowski, Min Koo Ji, Darren Whitehouse, Todd Ryder, Raymond Paul Beckett
  • Patent number: 8871970
    Abstract: A method for producing an organolithium compound includes the step of reacting an aromatic compound or a halogenated unsaturated aliphatic compound and a lithiating agent in the presence of a coordinating compound containing three or more elements having a coordinating ability in a molecule, at least one thereof being a nitrogen element, or a coordinating compound containing three or more oxygen elements having a coordinating ability in a molecule, at least one of the groups containing the oxygen elements having a coordinating ability being a tertiary alkoxy group, at a temperature of ?40° C. to 40° C.
    Type: Grant
    Filed: December 25, 2009
    Date of Patent: October 28, 2014
    Assignee: Nippon Soda Co., Ltd.
    Inventor: Hiroki Inoue
  • Patent number: 8871745
    Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Grant
    Filed: August 12, 2013
    Date of Patent: October 28, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Publication number: 20140315861
    Abstract: Disclosed herein inter alia are Boron containing compounds and methods for treating infections related to antibiotic resistant microorganisms.
    Type: Application
    Filed: April 14, 2014
    Publication date: October 23, 2014
    Applicants: The Regents of the University of California, Universita' Degli Studi di Modena e Reggio Emilia
    Inventors: Brian K. Shoichet, Fabio Prati, Emilia Caselli, Chiara Romagnoli, Oliv Eidam
  • Publication number: 20140274954
    Abstract: The present disclosure provides boron-containing diacylhydrazines having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, and R5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: Sheela K. CHELLAPPAN, Robert E. Hormann, Inna Shulman
  • Patent number: 8822720
    Abstract: The present disclosure describes operationally simple methods for the low temperature, catalytic activation of carboxylic acids for organic reactions, in particular for direct amidation reactions with amines. The methods involve the use of orthosubstituted arylboromc acids of the formula (I), wherein the groups R1 to R5 are as defined herein. In preferred embodiments R1 is halogen. The arylboromc acids catalyze nucleophilic 1,2-addition reactions, conjugate 1,4-addition reactions, and cycloaddition reactions, including Diels-Alder reactions involving ?,?-unsaturated carboxylic acids.
    Type: Grant
    Filed: September 5, 2008
    Date of Patent: September 2, 2014
    Assignee: The Governors of the University of Alberta
    Inventors: Dennis Hall, Olivier Marion, Raed Al-Zoubi
  • Publication number: 20140235580
    Abstract: Provided herein are compounds which mediate the activity of monoacyglycerol lipase (MAGL). Also provided are pharmaceutical compositions comprising a compound provided herein, and methods for treating, preventing and/or managing a MAGL mediated condition using a compound or pharmaceutical composition as provided herein.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 21, 2014
    Inventors: Alfredo C. Castro, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Publication number: 20140221631
    Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
    Type: Application
    Filed: March 7, 2014
    Publication date: August 7, 2014
    Applicant: Anacor Pharmaceuticals, Inc.
    Inventors: Stephen J. BAKER, Tsutomu Akama, Michael Richard Kevin Alley, Stephen J. Benkovic, Michael Dipierro, Vincent S. Hernandez, Karin M. Hold, Isaac Kennedy, Igor Likhotvorik, Weimin Mao, Kirk Maples, Jacob J. Plattner, Fernando Rock, Virginia Sanders, Aaron M. Stemphoski, George Petros Yiannikouros, Siead Zagar, Yong-Kang Zhang, Huchen Zhou
  • Patent number: 8785529
    Abstract: Described herein are novel metal salts capable as nucleating agents for polyolefins. The present invention relates to such salts synthesized by reacting potassium hydroxide with carboxylic acids and further, to the achievement of high crystallization temperatures in polypropylene compositions upon dispersal therein of formulations containing one or more of the said metal salts.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: July 22, 2014
    Assignee: Reliance Industries Limited
    Inventors: Gandham Satya Srinivasa Rao, S. Muthukumaru Pillai, Virendra Kumar Gupta
  • Publication number: 20140194386
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Application
    Filed: January 10, 2014
    Publication date: July 10, 2014
    Inventors: Christopher J. BURNS, Denis DAIGLE, Bin LIU, Daniel McGARRY, Daniel C. PEVEAR, Robert E. Lee TROUT, Randy W. JACKSON
  • Publication number: 20140194387
    Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Application
    Filed: January 13, 2014
    Publication date: July 10, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Jing Li
  • Patent number: 8772536
    Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Grant
    Filed: August 12, 2013
    Date of Patent: July 8, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Patent number: 8735582
    Abstract: When phthalic acid is heated in heptane under azeotropic reflux conditions in the presence of a catalytic amount of an arylboronic acid compound (such as 2,6-(diisopropylaminomethyl)phenylboronic acid or 2,6-bis(diisopropylaminomethyl)phenylboronic acid), phthalic anhydride is obtained in high yield.
    Type: Grant
    Filed: March 3, 2010
    Date of Patent: May 27, 2014
    Assignee: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Akira Sakakura
  • Publication number: 20140142322
    Abstract: The present application provides methods and catalysts for activation of carboxylic acids for organic reactions.
    Type: Application
    Filed: February 14, 2012
    Publication date: May 22, 2014
    Inventors: Dennis Hall, Nicolas Gernigon, Raed Al-Zoubi, Paul D. Thornton
  • Publication number: 20140131283
    Abstract: A method for treating in an industrial water treatment system for at least two of metal corrosion inhibition, scale inhibition, suspended matter dispersion, biocide efficacy, or biofilm removal/biofilm dispersion is taught by the use of at least one compound which is a salt derived from a thioamine or an oxyamine and an acid.
    Type: Application
    Filed: March 28, 2013
    Publication date: May 15, 2014
    Applicant: AMSA, INC.
    Inventors: Attila G Relenyi, Anthony P Haag
  • Patent number: 8722917
    Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: May 13, 2014
    Assignee: Anacor Pharmaceuticals, Inc.
    Inventors: Stephen J. Baker, Tsutomu Akama, Michael Richard Kevin Alley, Stephen J. Benkovic, Michael Dipierro, Vincent S. Hernandez, Karin M. Hold, Isaac Kennedy, Igor Likhotvorik, Weimin Mao, Kirk Maples, Jacob J. Plattner, Fernando Rock, Virginia Sanders, Aaron M. Stemphoski, George Petros Yiannikouros, Siead Zagar, Yong-Kang Zhang, Huchen Zhou
  • Publication number: 20140127137
    Abstract: Small Molecule Metabolite Reporters (SMMRs) for use as in vivo glucose biosensors, sensor compositions, and methods of use, are described. The SMMRs include boronic acid-containing xanthene, coumarin, carbostyril and phenalene-based small molecules which are used for monitoring glucose in vivo, advantageously on the skin.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 8, 2014
    Applicant: Cercacor Laboratories, Inc
    Inventors: Emile M. Bellott, Dongsheng Bu, James J. Childs, Christopher Lambert, Hubert A. Nienaber, Shirley J. Shi, Zhaolin Wang, Jerome J. Workman, Alex R. Zelenchuk
  • Publication number: 20140121183
    Abstract: The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.
    Type: Application
    Filed: December 20, 2013
    Publication date: May 1, 2014
    Applicant: INFINITY PHARMACEUTICALS, INC.
    Inventors: Julian ADAMS, Mark L. Behnke, Alfredo C. Castro, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Tao Liu, Daniel A. Snyder, Thomas T. Tibbitts
  • Publication number: 20140121182
    Abstract: The invention provides boronic esters of Formula (I) wherein R is H or methyl, and methods for the preparation and purification thereof.
    Type: Application
    Filed: June 21, 2012
    Publication date: May 1, 2014
    Applicant: Cephalon, Inc.
    Inventors: Roger P. Bakale, John P. Mallamo, Renee Caroline Roemmele
  • Publication number: 20140080787
    Abstract: The present invention relates to compositions and methods for the treatment, prevention, and diagnosis of neuropathies due to PMP22 mis-expression in a subject having Charcot-Marie-Tooth disease, especially Charcot-Marie-Tooth 1A disease. The present invention incorporates the use of small molecule proteasome inhibitors such as, but not limited to, Bortezomib to inhibit or reduce the overexpression of the PMP2 gene.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 20, 2014
    Inventors: James Inglese, John Peter Svaren, Sung-Wook Jang, Mark Albert Scheideler, Lars Jacob Stray Knutsen
  • Publication number: 20140073603
    Abstract: The present invention relates to a specific phenylboronic acid compound having anti-cancer, anti-inflammatory, and anti-microbial activity, in addition to a pharmaceutical composition comprising the same. The present invention also discloses a process for preparing said compound.
    Type: Application
    Filed: September 11, 2012
    Publication date: March 13, 2014
    Inventors: Khaled Mahmood Al-Qaoud, Penelope Ahmad Shihab, Luay Fawzi Abu-Qatouseh, Christopher R. Lowe, Abdel Monem Mohammad Rawashdeh, Yusuf Abdalsalam Alkhayyat, Samer Sami Ratrout, Saleem Muneer Naser
  • Patent number: 8668871
    Abstract: Provided are a sensing device and a biosensor that are capable of achieving stable performance in sensing saccharides or hydroxyl group-containing polymers, and that can be stored for a long time. The biosensor 8 of the present invention uses, as a component for sensing glucose, a sensing device 16 in which a completely synthetic phenylboronic acid compound 21 is bound without using enzymes that have been conventionally used. Consequently, the biosensor 8 can eliminate the problem of protein denaturation to achieve stable performance in sensing glucose, and it is possible to achieve the biosensor 8 can be stored for a long time.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: March 11, 2014
    Assignee: National Institute for Materials Science
    Inventors: Akira Matsumoto, Yuji Miyahara
  • Publication number: 20140014935
    Abstract: A polymer compound is provided having a constitutional unit represented by the following formula (1): wherein: R1 and R2 represent an alkyl group, an aryl group, a mono-valent aromatic heterocyclic group, an alkoxy group or an aryloxy group, and Ar1 represents an arylene group or a di-valent condensed polycyclic aromatic heterocyclic group.
    Type: Application
    Filed: March 16, 2012
    Publication date: January 16, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Daisuke Fukushima, Tomoyasu Yoshida, Yoshihiro Kawada, Takashi Kuragano, Makoto Anryu
  • Publication number: 20140005398
    Abstract: A borate moiety-contained linker and a bio-sensing element containing the same are disclosed. The borate moiety-contained linker can be used to modify a sensing molecule and connect the sensing molecule to a substrate to form the bio-sensing element.
    Type: Application
    Filed: January 8, 2013
    Publication date: January 2, 2014
    Applicant: NATIONAL CHIAO TUNG UNIVERSITY
    Inventors: Yaw-Kuen LI, Mo-Yuan SHEN, Yu-Ju PIEN
  • Publication number: 20130331602
    Abstract: Provided is a process for preparing 4-borono-L-phenylalanine, which has steps of: reacting N-protected (S)-4-halophenylalanine of formula (I), a boronating agent and an organolithium to obtain a reaction mixture, wherein the reaction mixture comprises N-protected (S)-4-boronophenylalanine of formula (II) and the R group represents a protecting group; isolating the N-protected (S)-4-boronophenylalanine from the reaction mixture; deprotecting the R group of the N-protected (S)-4-boronophenylalanine to obtain L-BPA.
    Type: Application
    Filed: June 5, 2013
    Publication date: December 12, 2013
    Inventors: Chia-Cheng Shaw, Kuen-Wang Sheu, Shu-Fen Huang
  • Publication number: 20130331595
    Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Application
    Filed: August 12, 2013
    Publication date: December 12, 2013
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Publication number: 20130316943
    Abstract: Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and their methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent.
    Type: Application
    Filed: February 6, 2012
    Publication date: November 28, 2013
    Applicant: REMPEX PHARMACEUTICALS, INC.
    Inventors: Tomasz Glinka, Robert Higuchi, Scott Hecker, Brian Eastman, Olga Rodny
  • Publication number: 20130310320
    Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
    Type: Application
    Filed: January 11, 2013
    Publication date: November 21, 2013
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Julian Adams, Yu-Ting Ma, Ross L. Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
  • Publication number: 20130296573
    Abstract: A protected organoboronic acid includes a boron having an sp3 hybridization, a conformationally rigid protecting group bonded to the boron, and an organic group bonded to the boron through a boron-carbon bond. A method of performing a chemical reaction includes contacting a protected organoboronic acid with a reagent, the protected organoboronic acid including a boron having an sp3 hybridization, a conformationally rigid protecting group bonded to the boron, and an organic group bonded to the boron through a boron-carbon bond. The organic group is chemically transformed, and the boron is not chemically transformed.
    Type: Application
    Filed: October 18, 2012
    Publication date: November 7, 2013
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Martin D. Burke, Eric P. Gillis, Suk Joong Lee, David M. Knapp, Kaitlyn C. Gray
  • Publication number: 20130274160
    Abstract: The disclosed technology relates to a dispersant composition comprising the reaction product of a polyolefin acylating agent and an amine terminated or hydroxyl terminated polyether. In addition, the technology relates to lubricating compositions containing the dispersant composition and an optional synergistic amount of another dispersant, as well as methods of employing the dispersant composition in an engine and engine oils.
    Type: Application
    Filed: April 8, 2013
    Publication date: October 17, 2013
    Applicant: THE LUBRIZOL CORPORATION
    Inventors: Ewan E. Delbridge, Renee A. Eveland, Joanne L. Jones, John K. Pudelski, Nicolas Proust
  • Patent number: 8546607
    Abstract: Embodiments of the invention provide methods and materials for chemical cross-coupling reactions that utilize unconventional phenol derivatives as cross-coupling partners. Embodiments of the invention can be used to synthesize a variety of useful organic compounds, for example the anti-inflammatory drug flurbiprofen.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: October 1, 2013
    Assignee: The Regents of the University of California
    Inventors: Neil K. Garg, Kyle W. Quasdorf, Xia Tian
  • Patent number: 8546608
    Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.
    Type: Grant
    Filed: September 30, 2011
    Date of Patent: October 1, 2013
    Assignee: Cephalon, Inc.
    Inventors: Raffaella Bernardini, Alberto Bernareggi, Paolo G. Cassara, Sankar Chatterjee, Germano D'Arasmo, Sergio De Munari, Edmondo Ferretti, Mohamed Iqbal, Ernesto Menta, Patricia A. Messina McLaughlin, Ambrogio Oliva
  • Publication number: 20130243670
    Abstract: Provided are methods for purifying N-methyliminodiacetic acid (MIDA) boronates from solution. Also provided are methods for deprotection of boronic acids from their MIDA ligands. The purification and deprotection methods can be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chemical compounds of interest. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated synthesis of small molecules using iterative cycles of deprotection, coupling, and purification in accordance with methods of the invention.
    Type: Application
    Filed: July 22, 2011
    Publication date: September 19, 2013
    Inventors: Martin D. Burke, Eric P. Gillis
  • Patent number: 8530694
    Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Grant
    Filed: August 15, 2011
    Date of Patent: September 10, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Publication number: 20130184484
    Abstract: The present invention relates to the process for preparing a boronic acid or ester chemically, in which an aromatic compound is reacted with a boronating agent, in the presence of magnesium metal (Mg0). The invention also relates to the boronic acids or esters that can be obtained by means of this process and to the use thereof for example as a synthesis intermediate, in the Suzuki reaction, in the pharmaceutical or alternatively electronics field.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 18, 2013
    Applicant: Universite De Nice Sophia Antipolis
    Inventor: Universite De Nice Sophia Antipolis
  • Publication number: 20130172566
    Abstract: Methods of producing methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate. One method comprises adding methyl isobutyl ketone to an aqueous solution comprising 4-chloro-2-fluoro-3-methoxyphenyl-boronic acid to form an organic phase comprising the 4-chloro-2-fluoro-3-methoxyphenylboronic acid and an aqueous phase. The organic phase and the aqueous phase are separated. The 4-chloro-2-fluoro-3-methoxyphenylboronic acid is reacted with methyl 4-(acetylamino)-3,6-dichloropyridine-2-carboxylate in methyl isobutyl ketone to produce methyl 4-(acetylamino)-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate, which is deacetylated to produce methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 4, 2013
    Applicant: Dow AgroSciences LLC
    Inventor: Dow AgroSciences LLC
  • Publication number: 20130172567
    Abstract: Methods of isolating a 4-chloro-2-fluoro-3-substituted-phenylboronate include adding carbon dioxide gas or carbon dioxide solid (dry ice) to a solution comprising a 4-chloro-2-fluoro-3-substituted-phenylboronate, an inert organic solvent, and at least one lithium salt to react the at least one lithium salt with the carbon dioxide gas or carbon dioxide solid (dry ice) and form a mixture comprising the 4-chloro-2-fluoro-3-substituted-phenylboronate, the inert organic solvent, and a precipitated solid. The precipitated solid may be removed from the mixture. Methods of using 4-chloro-2-fluoro-3-substituted-phenylboronates to produce methyl-4-amino-3-chloro-6-(4-chloro-2-fluoro-3-substituted-phenyl)pyridine-2-carboxylates are also disclosed.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 4, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventor: Dow AgroSciences LLC
  • Publication number: 20130150292
    Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.
    Type: Application
    Filed: September 14, 2012
    Publication date: June 13, 2013
    Applicant: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-Sen Lai, Wengen Wu
  • Publication number: 20130075704
    Abstract: Provided is a novel heterocyclic compound which can be used in a light-emitting layer of a light-emitting element as a host material in which a light-emitting material is dispersed, i.e., a heterocyclic compound represented by a general formula (G1). Any one of R1 to R10 represents a substituent represented by a general formula (G1-1); another one of R1 to R10 represents hydrogen, an alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted phenyl group, a substituted or unsubstituted biphenyl group, or a substituent represented by a general formula (G1-2); and the others separately represent hydrogen, an alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted phenyl group, or a substituted or unsubstituted biphenyl group.
    Type: Application
    Filed: August 28, 2012
    Publication date: March 28, 2013
    Applicant: SEMICONDUCTOR ENERGY LABORATORY CO., LTD.
    Inventors: Takako Takasu, Harue Osaka, Satoko Shitagaki
  • Patent number: 8394539
    Abstract: Lithium salts with fluorinated chelated orthoborate anions are prepared and used as electrolytes or electrolyte additives in lithium-ion batteries. The lithium salts have two chelate rings formed by the coordination of two bidentate ligands to a single boron atom. In addition, each chelate ring has two oxygen atoms bonded to one boron atom, methylene groups bonded to the two oxygen atoms, and one or more fluorinated carbon atoms bonded to and forming a cyclic bridge between the methylene groups.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: March 12, 2013
    Assignee: GM Global Technology Operations LLC
    Inventors: Olt E. Geiculescu, Ion C. Halalay, Darryl D. Desmarteau, Stephen E. Creager
  • Publication number: 20130030213
    Abstract: Provided herein are methods of isolating a 4-chloro-2-fluoro-3-substituted-phenylboronic acid. The method comprises contacting a mixture of water, a water miscible organic solvent, and a 4-chloro-2-fluoro-3-substituted-phenylboronic acid with a salt to form a water miscible organic solvent layer and a water layer. The 4-chloro-2-fluoro-3-substituted-phenylboronic acid is partitioned into the water miscible organic solvent layer, which is separated from the water layer. Additional methods are disclosed, as is a 4-chloro-2-fluoro-3-substituted-phenylboronic acid produced by one of the methods, wherein the 4-chloro-2-fluoro-3-substituted-phenylboronic acid is obtained at a yield of greater than approximately 90%.
    Type: Application
    Filed: July 26, 2012
    Publication date: January 31, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventor: Jossian Oppenheimer
  • Publication number: 20120322702
    Abstract: Multi-functional additives which impart improved antioxidancy to lubricating oil compositions and frictional properties resulting in improved fuel economy in an internal combustion engine are disclosed. More particularly disclosed is a boron containing salt of an oil soluble hydroxylated amine and a hindered phenolic acid product prepared by: a) reacting an oil soluble hydroxylated amine of the general formula II: wherein A at each occurrence is each independently C2-C6 alkylene group; R is methyl or an alkyl or alkenyl group having C2-C24 carbon atoms; Y is hydrogen, C1-C6 alkyl group or A-OH; x is an integer of 1 or 2; and z is an integer of 0 or 1; with a boron containing compound under reactive conditions; and b) mixing the reaction product of step a) with a hindered phenolic acid.
    Type: Application
    Filed: August 30, 2012
    Publication date: December 20, 2012
    Applicant: Chevron Oronite Company LLC
    Inventors: Yat Fan Suen, John Ward, Trevor Miller
  • Patent number: 8318983
    Abstract: A protected organoboronic acid includes a boron having an sp3 hybridization, a conformationally rigid protecting group bonded to the boron, and an organic group bonded to the boron through a boron-carbon bond. A method of performing a chemical reaction includes contacting a protected organoboronic acid with a reagent, the protected organoboronic acid including a boron having an sp3 hybridization, a conformationally rigid protecting group bonded to the boron, and an organic group bonded to the boron through a boron-carbon bond. The organic group is chemically transformed, and the boron is not chemically transformed.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: November 27, 2012
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Martin D. Burke, Eric P. Gillis