Patents Examined by Valerie Rodriguez-Garcia
  • P-chirogenic organophosphorus compounds
    Patent number: 9707553
    Abstract: P-chirogenic organophosphorus compounds of general formula (I), a process for the synthesis of the compounds of formula (I), and intermediate products of general formulae (II), (III) and (IV), as shown below, are involved in the synthesis of compounds (I). Metal complexes comprising compounds (I) as ligands are also described. The compounds and complexes are useful in asymmetric catalysis by transition metal complexes or organocatalysis, especially for asymmetric hydrogenation or allylation. Compounds of general formula (I) may be useful as agrochemical and therapeutic substances, or as reagents or intermediates for fine chemistry.
    Type: Grant
    Filed: October 6, 2015
    Date of Patent: July 18, 2017
    Assignees: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE BOURGOGNE, UNIVERSITE DE STRASBOURG, SYNTHELOR SAS
    Inventors: Sylvain Juge, Jerome Bayardon, Emmanuelle Remond, Hugo Laureano, Jean-Christophe Henry, Frederic Leroux, Francoise Colobert
  • Dibenzo[f,h]quinoxaline derivative, method of synthesizing the same, light-emitting element, light-emitting device, electronic appliance, and lighting device
    Patent number: 9695158
    Abstract: A composition comprising a dibenzo[f,h]quinoxaline derivative in which impurities are reduced and a method of synthesizing dibenzo[f,h]quinoxaline in which impurities are reduced are provided. In addition, a light-emitting element, a light-emitting device, an electronic appliance, or a lighting device with high emission efficiency and high reliability in which dibenzo[f,h]quinoxaline is used as an EL material is provided. In the synthesis method, 2-(chloroaryl)dibenzo[f,h]quinoxaline is used as a synthetic intermediate in a synthetic pathway so that an impurity contained in a final product can be removed easily by purification by sublimation.
    Type: Grant
    Filed: September 12, 2014
    Date of Patent: July 4, 2017
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hideko Inoue, Tomohiro Kubota, Satoshi Seo, Hayato Yamawaki, Yasushi Kitano
  • Drug repositioning: urease inhibitory activity of (2S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid (captopril)
    Patent number: 9688628
    Abstract: This invention provides that (2S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid (captopril) possess potent in vitro urease inhibitory potential with 95.00% inhibition and IC50=16.6±1.52 ?M, when compared to the standard inhibitor i.e. acetohydroxamic acid (IC50=41.5±1.50 ?M).
    Type: Grant
    Filed: February 23, 2016
    Date of Patent: June 27, 2017
    Inventors: Jalaluddin Azam Jalal Khan, Muhammad Iqbal Choudhary, Maryam Abdu Abdullah Al-Ghamdi, Etimad Huwait, Atia-tul Wahab, Samrah Iqbal
  • Extraction solvent control for reducing stable emulsions
    Patent number: 9676800
    Abstract: Disclosed herein are methods for recovering diphosphonite-containing compounds from mixtures comprising organic mononitriles and organic dinitriles, using multistage countercurrent liquid-liquid extraction. Recovery is enhanced with one or more method steps. In a first step, a portion of the heavy phase from the settling section of the first stage is recycled to the settling section of the first stage. In a second step, a portion of the light phase from the settling section of the first stage is recycled to the mixing section of the first stage. In a third step, the first stage takes place in a mixer-settler, a Lewis base is introduced into the settling section of the first stage, and a complex of Lewis acid and Lewis base is formed in this settling section. In a fourth step, a polyamine is added to the first stage.
    Type: Grant
    Filed: December 8, 2015
    Date of Patent: June 13, 2017
    Assignee: INVISTA NORTH AMERICA S.A.R.L.
    Inventors: William J. Tenn, III, Sudhir N. V. K. Aki, Thomas E. Vos, Tseng H. Chao
  • Method for producing a liquid emulsifiable formulation comprising a pyripyropene pesticide
    Patent number: 9668470
    Abstract: The present invention relates to a method for producing a liquid non-aqueous emulsifiable formulation comprising a pyripyropene pesticide of the formula (I) as defined below which is dissolved in an aromatic hydrocarbon or hydrocarbon mixture containing surfactants, which stabilize the emulsion upon dilution with water, which method comprises the steps i) and ii) as described hereinafter: i) dissolving the at least one surfactant and the compound of formula (I) in the organic solvent or solvent mixture to obtain a clear solution of the at least one surfactant and the compound of the formula (I); ii) heating the solution to a temperature of at least 40° C.
    Type: Grant
    Filed: January 15, 2014
    Date of Patent: June 6, 2017
    Assignee: BASF SE
    Inventors: Wen Xu, Ralph Paulini, Michael Krapp, Kara Benton
  • Furanyl compounds and the use thereof
    Patent number: 9663483
    Abstract: Provided herein are substituted furanyl compounds of formula (I), pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate eIF4E activity. In one embodiment, the compounds provided herein modulate the Hedgehog pathway activity. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders.
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: May 30, 2017
    Assignee: NovoMedix, LLC
    Inventors: Leah M. Fung, Kyle W. H. Chan, Cathy A. Swindlehurst
  • Substituted piperazinyl acetohydrazide procaspase-activating compounds
    Patent number: 9663482
    Abstract: The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds are of Formula I The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: May 30, 2017
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Howard S. Roth
  • Benzamide-containing compounds and their use in the treatment of pain
    Patent number: 9649308
    Abstract: The present invention is directed to benzamide-containing compounds of formula I or pharmaceutically acceptable salts thereof which inhibit the P2X7 receptor, and their use in the treatment of pain.
    Type: Grant
    Filed: June 19, 2015
    Date of Patent: May 16, 2017
    Assignee: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohamed Eldemenky, Bin Chen, Yu Jiang, Allen T. Hopper
  • Diarylamine-based fluorogenic probes for detection of peroxynitrite
    Patent number: 9651528
    Abstract: Provided herein are improved fluorogenic compounds and probes that can be used as reagents for measuring, detecting and/or screening peroxynitrite. The fluorogenic compounds of the invention can produce fluorescence colors, such as green, yellow, red, or far-red. Also provided herein are fluorogenic compounds for selectively staining peroxynitrite in the mitochondria of living cells. Provided also herein are methods that can be used to measure, directly or indirectly, the presence and/or amount of peroxynitrite in chemical samples and biological samples such as cells and tissues in living organisms. Also provided are high-throughput screening methods for detecting or screening peroxynitrite or compounds that can increase or decrease the level of peroxynitrite in chemical and biological samples.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: May 16, 2017
    Assignee: THE UNIVERSITY OF HONG KONG
    Inventors: Dan Yang, Tao Peng, Jiangang Shen, Xingmiao Chen
  • Membrane-supported catalyst removal in the epoxidation of cyclic unsaturated C12 compounds, for example cyclododecene (CDEN)
    Patent number: 9643153
    Abstract: A homogeneous catalyst system is removed from a reaction mixture of two liquid phases by separating the two liquid phases with a membrane having at least one separation-active layer in such a way that the homogeneous catalyst system is at least partially concentrated in a membrane retentate; wherein the reaction mixture contains at least one partially epoxidized cyclic unsaturated compound having twelve carbon atoms; and wherein the membrane separation-active layer contains crosslinked a silicone acrylate and/or polydimethylsiloxane and/or polyimide.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: May 9, 2017
    Assignee: EVONIK DEGUSSA GmbH
    Inventors: Ralf Meier, Kévin Micoine, Peter Kreis, Frederik Gluth, Markus Priske
  • Crystalline 4-(3S-(1R-(1-napthyl)ethylamino)pyrrolidin-1-yl)phenylacetic acid
    Patent number: 9643920
    Abstract: The present invention provides crystal forms A and B of 4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1-yl)phenylacetic acid having excellent stability and use as pharmaceutical ingredients. The present invention also provides industrially advantageous processes for producing these crystalline compounds.
    Type: Grant
    Filed: September 5, 2014
    Date of Patent: May 9, 2017
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Hiroshi Miyazaki, Takao Komasaka, Joji Tsurumoto, Takeshi Uemura, Yuuji Morita
  • Methods for the synthesis of sphingomyelins and dihydrosphingomyelins
    Patent number: 9643915
    Abstract: The present invention includes methods for the synthesis of sphingomyelins and dihydrosphingomyelins. The present invention also includes methods for the synthesis of sphingosines and dihydrosphingosines. The present invention further includes methods for the synthesis of ceramides and dihydroceramides.
    Type: Grant
    Filed: April 22, 2015
    Date of Patent: May 9, 2017
    Assignee: Cerenis Therapeutics Holding SA
    Inventors: Daniela Carmen Oniciu, Stefan Heckhoff, Benoit Oswald, Peter Rebmann, Andreas Peer, Miguel Gonzalez, Patrik Sauter
  • Method for preparing IDO inhibitor epacadostat
    Patent number: 9624185
    Abstract: The present disclosure provides a new method for preparing IDO inhibitor epacadostat. The whole reaction route is simple, easy to control and has high yield.
    Type: Grant
    Filed: January 20, 2016
    Date of Patent: April 18, 2017
    Inventor: Yong Xu
  • Nucleoside kinase bypass compositions and methods
    Patent number: 9624249
    Abstract: The present invention relates to disulfide masked prodrug compounds of Formula (I), nucleoside kinase bypass compositions thereof and methods that are amenable to bioactivation by a reducing agent such as glutathione: Such disulfide based compounds, compositions, and methods can be useful, for example, in providing prodrugs for use as therapeutics.
    Type: Grant
    Filed: December 2, 2013
    Date of Patent: April 18, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Gabor Butora
  • Synthesis of coumalic acid
    Patent number: 9617236
    Abstract: A method to prepare coumalic acid comprising (a) heating a solution in dichloroethane of malic acid and sulfuric acid or a solution in dichloroethane of malic acid and a perfluorosulfonic acid or (b) adding an acid comprising sulfuric acid or a perfluorosulfonic acid to a solution of malic acid in dichloroethane to yield a solution that is heated for a period of time so as to convert the malic acid into a major amount of coumalic acid and, optionally, a minor amount of fumaric acid.
    Type: Grant
    Filed: May 20, 2014
    Date of Patent: April 11, 2017
    Assignee: Iowa State University Research Foundation, Inc.
    Inventor: George A. Kraus
  • Preparation method for azoxystrobin
    Patent number: 9611226
    Abstract: Disclosed in the present invention is a preparation method of azoxystrobin having a structure as shown by formula (1), the method comprising: a) performing an etherification reaction by reacting the compound having a structure shown by formula (2) with 2-cyanophenol and/or a salt thereof under the catalysis of an azabicyclo tertiary amine compound and/or a salt thereof as the catalyst in a butyl acetate medium to obtain a butyl acetate solution containing azoxystrobin; and b) cooling the butyl acetate solution containing azoxystrobin to precipitate Azoxystrobin having a structure as shown by formula (1) from the butyl acetate solution. Using the method provided by the present invention to prepare azoxystrobin can significantly improve the yield of azoxystrobin, and can obtain azoxystrobin products having high purity.
    Type: Grant
    Filed: March 20, 2014
    Date of Patent: April 4, 2017
    Assignees: Nutrichem Company Limited, Shanqyu Nutrichem Co., Ltd.
    Inventors: Wenjun Wang, Jianwei Chen, Jianhong Chi, Yongchang Zhao, Xufang Deng, Long Wang, Hua'nan You
  • Oxazolidinone and imidazolidinone compounds
    Patent number: 9611232
    Abstract: The invention provides compounds having the general formula I wherein n, R1, R2a, R2b, R3a and R3b are as herein defined, composition comprising the compounds and methods of using the compounds.
    Type: Grant
    Filed: April 29, 2015
    Date of Patent: April 4, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luke Green, Haiyan Wang
  • Nucleophile-reactive sulfonated compounds for the (radio)labelling of (bio) molecules; precursors and conjugates thereof
    Patent number: 9611215
    Abstract: Nucleophile-reactive sulfonated compounds used as precursors to (radio)labelled (bio)molecules are produced by pre-introduction of a nucleophilic compound R* through an unusual nucleophile-induced ring-opening reaction of the sultone moiety of the precursor. The precursors and compounds conform to respective formulae (Ip) and (I): Also disclosed are methods for producing these precursors and compounds, as well as for conjugation of these compounds with (bio)molecules, and to the drugs obtained by this method.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: April 4, 2017
    Assignee: Advanced Accelerator Applications SA
    Inventors: Thomas Priem, Cedric Bouteiller, Davide Camporese, Anthony Romieu, Pierre-Yves Renard
  • Bicyclic thiophenylamide compounds
    Patent number: 9604977
    Abstract: Compounds having the formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A, E and n are as described herein, compositions including the compounds and methods of using the compounds as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors for the treatment or prophylaxis of type 2 diabetes, atherosclerosis, chronic kidney diseases, non-alcoholic steatohepatitis and cancer.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: March 28, 2017
    Assignee: Hoffman-La Roche Inc.
    Inventors: Bernd Buettelmann, Simona M. Ceccarelli, Holger Kuehne, Bernd Kuhn, Werner Neidhart, Ulrike Obst Sander, Hans Richter
  • Derivatives of hemin with antibacterial and antiviral activity
    Patent number: 9605013
    Abstract: The invention relates to hemin derivatives of general formula (I), preparing and use thereof as antibacterial and/or antiviral agents, including, as a component in a pharmaceutical compositions. Advantages of the antibacterial and antiviral agents based on the hemin derivatives are in their biocompatibility, biodegradability, a high efficacy against resistant bacteria and widespread viruses which are dangerous to humans, and the lack of toxicity.
    Type: Grant
    Filed: November 15, 2012
    Date of Patent: March 28, 2017
    Assignee: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”
    Inventors: Vladimir Evgenievich Nebolsin, Galina Alexandrovna Zheltukhina, Sergei Alexandrovich Okorochenkov