Patents Issued in June 25, 2019
  • Patent number: 10329226
    Abstract: The present invention provides processes for the production of chlorinated methanes via the direct chlorination of methane. The processes include a dehydrochlorination and/or chlorination step that converts up to 100% of the higher chlorinated alkanes in a process stream from the methane chlorination reaction into more highly chlorinated alkanes. These more highly chlorinated alkanes can be easily removed from the process stream. The use of a cost effective feedstream of crude methane is thus rendered possible, without additional capital expenditure for the sophisticated separation equipment required to separate ethane and other hydrocarbon components from the methane feed.
    Type: Grant
    Filed: September 22, 2016
    Date of Patent: June 25, 2019
    Assignee: Blue Cube IP LLC
    Inventors: John D. Myers, Matthew L. Grandbois
  • Patent number: 10329227
    Abstract: The present invention provides a process for preparing 2,3,3,3-tetrafluoropropene from 1,1,1,2,3-pentachloropropane and/or 1,1,2,2,3-pentachloropropane, comprising the following steps: (a) catalytic reaction of 1,1,1,2,3-pentachloropropane and/or 1,1,2,2,3-pentachloropropane with HF into a reaction mixture comprising HCl, 2-chloro-3,3,3-trifluoropropene, 2,3,3,3-tetrafluoropropene, unreacted HF, and optionally 1,1,1,2,2-pentafluoropropane; (b) separating the reaction mixture into a first stream comprising HCl and 2,3,3,3-tetrafluoropropene and a second stream comprising HF, 2-chloro-3,3,3-trifluoropropene and optionally 1,1,1,2,2-pentafluoropropane; (c) catalytic reaction of the second stream into a reaction mixture comprising 2,3,3,3-tetrafluoropropene, HCl, unreacted 2-chloro-3,3,3-trifluoropropene, unreacted HF and optionally 1,1,1,2,2-pentafluoropropane and (d) feeding the reaction mixture of step (c) directly without separation to step (a).
    Type: Grant
    Filed: July 19, 2018
    Date of Patent: June 25, 2019
    Assignee: ARKEMA FRANCE
    Inventors: Dominique Deur-Bert, Bertrand Collier, Laurent Wendlinger
  • Patent number: 10329228
    Abstract: A process for the production of saturated or unsaturated aliphatic alcohols and/or hydrocarbons includes condensing acetone and/or alcohol(s) to form one or more carbonyl compounds, and hydrogenating and/or hydrodeoxygenating at least one of the one or more carbonyl compounds to form the saturated or unsaturated alcohol(s) and/or hydrocarbons. In some embodiments, the condensation of acetone and/or alcohol(s) may be carried out in the presence of a solid acid catalyst and a transition metal catalyst. The saturated or unsaturated aliphatic alcohols and/or hydrocarbons may include one or more saturated linear C9 alcohols, C9 alkanes and/or one or more mono-unsaturated C9 alkenes.
    Type: Grant
    Filed: April 24, 2017
    Date of Patent: June 25, 2019
    Assignee: Triad National Security, LLC
    Inventors: Andrew Sutton, Cameron Moore, Rhodri Jenkins, Troy A. Semelsberger
  • Patent number: 10329229
    Abstract: The present invention aims at providing a method for producing a high-concentration alcohol from a water-alcohol mixture, in which the overall process is efficient and the present invention relates to a production method of a high-concentration alcohol, including a water adsorption step of adsorbing water of a water-alcohol mixture on an adsorption column to obtain a first concentrated alcohol, a water desorption step of introducing an alcohol to obtain a hydrous alcohol, and a membrane separation step of introducing the hydrous alcohol into a membrane separation unit provided with a membrane composite containing zeolite having an SiO2/Al2O3 molar ratio of 5 to 15 to obtain a second concentrated alcohol.
    Type: Grant
    Filed: March 30, 2017
    Date of Patent: June 25, 2019
    Assignees: MITSUBISHI CHEMICAL CORPORATION, Mitsubishi Chemical Engineering Corporation
    Inventors: Kazuhide Maeda, Koichi Yamazaki, Hiroyuki Kakiuchi, Takeshi Tahara, Takahiko Takewaki
  • Patent number: 10329230
    Abstract: Disclosed is a process for the purification of a mixed diol stream. The mixed diol stream comprising two-, three-, and four-carbon diols is separated into component diols by extraction with a hydrophobic solvent mixture. The diols recovered in the extractant may be removed from the extractant stream by back extraction with water or by distillation with an azeotrope-forming agent present, preferably an azeotroping agent already present in the extractant mixture.
    Type: Grant
    Filed: November 24, 2015
    Date of Patent: June 25, 2019
    Assignee: Eastman Chemical Company
    Inventor: Scott Donald Barnicki
  • Patent number: 10329231
    Abstract: The present invention provides an epoxy compound which is 2,2?,7,7?-tetraglycidyloxy-1,1?-binaphthalene. Also, the present invention provides a method for producing [1,1?-binaphthalene]-2,2?,7,7?-tetraol, the method including a step of bringing a crude product produced by dimerization reaction of naphthalene-2,7-diol or a naphthalene-2,7-diol derivative into contact with an aromatic solvent; a step of separating [1,1?-binaphthalene]-2,2?,7,7?-tetraol dissolved in the aromatic solvent from insoluble substances; and a step of removing the solvent from a solution of [1,1?-binaphthalene]-2,2?,7,7?-tetraol. The present invention also provides a method for producing an epoxy compound, the method including reacting [1,1?-binaphthalene]-2,2?,7,7?-tetraol or [1,1?-binaphthalene]-2,2?,7,7?-tetraol monohydrate with epihalohydrin.
    Type: Grant
    Filed: July 12, 2017
    Date of Patent: June 25, 2019
    Assignee: DIC Corporation
    Inventors: Yasuyo Yoshimoto, Kunihiro Morinaga, Hiroshi Kinoshita, Masamichi Hayashi
  • Patent number: 10329232
    Abstract: A calixarene directly grafted onto the surface of a material, a related grafting process, and certain calixarene intermediates useful for carrying out the grafting process.
    Type: Grant
    Filed: March 28, 2013
    Date of Patent: June 25, 2019
    Assignees: UNIVERSITE LIBRE DE BRUXELLES (ULB), CENTER NATIONAL DE LA RECHERCHE SCIENTIFIQUE—CNRS, UNIVERSITE DE RENNES 1, UNIVERSITE PARIS DESCARTES
    Inventors: Ivan Jabin, Alice Mattiuzzi, Corlnne Lagrost, Philippe Hapiot, Olivia Reinaud
  • Patent number: 10329233
    Abstract: The presently disclosed and/or claimed inventive concept(s) relates generally to the reduction of carbon dioxide by heterogeneous catalysis. More particularly, but not by way of limitation, the presently disclosed and/or claimed inventive concept(s) relates to the reduction of carbon dioxide by heterogeneous catalysis with a heterogeneous hydrogenation catalyst comprising structurally frustrated Lewis pairs, wherein, for example but not by way of limitation, formic acid is produced and hydrocarbons are indirectly produced. In one non-limiting embodiment, the heterogeneous catalyst comprises hexagonal boron nitride (h-BN) having structurally frustrated Lewis pairs therein.
    Type: Grant
    Filed: March 28, 2017
    Date of Patent: June 25, 2019
    Assignee: University of Central Florida Research Foundation, Inc.
    Inventor: Richard G. Blair
  • Patent number: 10329234
    Abstract: The inventive concepts disclosed and/or claimed herein relate generally to catalysts and, more particularly, but not by way of limitation, to a heterogeneous, metal-free hydrogenation catalyst containing frustrated Lewis pairs. In one non-limiting embodiment, the heterogeneous, metal-free catalyst comprises hexagonal boron nitride (h-BN) having frustrated Lewis pairs therein.
    Type: Grant
    Filed: August 7, 2017
    Date of Patent: June 25, 2019
    Assignee: University of Central Florida Research Foundation, Inc.
    Inventor: Richard G. Blair
  • Patent number: 10329235
    Abstract: This invention relates to the continuous production of 1,4-cyclohexane dimethanol (CHDM) and optionally and additionally of 1,4-cyclohexane dicarboxylic acid (CHDA) directly using terephthalic acid (TPA) as the raw material. More specifically, this invention relates to a method and system for continuous production of CHDM and CHDA that features direct use of TPA as feedstock, promotes efficient use of solvent and energy, and provides products with the desired high trans isomer content, by exploiting unexpected features of the thermodynamic phase behavior and the reaction mechanisms.
    Type: Grant
    Filed: August 31, 2017
    Date of Patent: June 25, 2019
    Assignee: ClearWaterBay CHDM Technology Limited
    Inventors: Ketan D. Samant, Drow Lionel O'Young, Yik Chung Chan
  • Patent number: 10329236
    Abstract: Provided is a process for preparing 4-phenyl-1-butyric acid, comprising: reacting 4-phenyl-1-butanol with sodium chlorite, a nitroxyl radical catalyst and sodium hypochlorite in an organic solvent and a phosphate buffer; and quenching the reaction with sodium sulfite to produce 4-phenyl-1-butyric. Also provided is 4-phenyl-1-butyric acid prepared by such a process.
    Type: Grant
    Filed: September 6, 2017
    Date of Patent: June 25, 2019
    Assignee: Horizon Therapeutics, LLC
    Inventors: Huai-Chueh Chang, Steven S. Pfeiffer, Vasilios H. Iskos, Maki Uragami, Steven Weissman, Andrew Thompson
  • Patent number: 10329237
    Abstract: The present invention relates to a method for hydrogenating aromatic compounds with hydrogen in the presence of a catalyst, in which the catalyst comprises ruthenium on a zirconium oxide support material, and also the use of a catalyst comprising ruthenium on a zirconium oxide support material for hydrogenating aromatic compounds.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: June 25, 2019
    Assignee: BASF SE
    Inventors: Bernd Bastian Schaack, Martin Bock, Kirsten Dahmen
  • Patent number: 10329238
    Abstract: A method for isomerizing a starting mixture comprising 2,4-diamino-1-methylcyclohexane, 2,4-MDACH for short, 2,6-diamino-1-methylcyclohexane, 2,6-MDACH for short, or mixtures thereof, wherein the isomerization is carried out in the presence of a supported catalyst with zirconium dioxide as support and ruthenium as active metal.
    Type: Grant
    Filed: November 30, 2016
    Date of Patent: June 25, 2019
    Assignee: BASF SE
    Inventors: Andreas Weickgenannt, Sandra Kramp, Jan-Oliver Weidert, Alexander Panchenko, Artur Kozicki, Ralph Busch
  • Patent number: 10329239
    Abstract: Systems and method are provided for reducing the water content from approximately 0.15%-0.19% by weight to approximately 0.01-0.03% by weight in an ethanolamine product stream in a non-reactive distillation column. The reduced water content can be achieved by increasing the processing conditions at the drying column by approximately 5% to approximately 20%, more preferably to approximately 10%. The increased processing conditions at the drying column can result in an increased bottom stream flow rate and an increased reboiler duty. The reboiler duty of the drying column can be increased by up to 2% to achieve said level of water content. The bottom stream flow rate can be increased by up to approximately 12% to achieve said level of water content.
    Type: Grant
    Filed: April 2, 2015
    Date of Patent: June 25, 2019
    Assignee: SABIC GLOBAL TECHNOLOGIES B.V
    Inventor: Naeem Al-Hazmi
  • Patent number: 10329240
    Abstract: There is disclosed a process for the separation of long chain amino acid and long chain dibasic acid, comprising: (1) recovering alkylamine from an aqueous solution of an alkali hydroxide hydrolysis of the mixed amide derivatives by distilling or by extracting with an extractant solvent; (2) cooling the aqueous solution of step (1) to precipitate a mixed alkali salts of long chain amino acid and dibasic acid; (3) recovering the mixed alkali salts of long chain amino acid and dibasic acid to provide a mother liquor; (4) separating long chain amino acid and dibasic acid by acidification-extraction of long chain dibasic acid with an extractant solvent or by selective dissolution of alkali salt of long chain amino acid in an aqueous solvent; and (4) adding an acid to the mother liquor of step (3) to obtain alkanoic acid.
    Type: Grant
    Filed: July 7, 2017
    Date of Patent: June 25, 2019
    Assignee: VITAWORKS IP, LLC
    Inventor: Songzhou Hu
  • Patent number: 10329241
    Abstract: There is disclosed a process for the separation of long chain amino acid and long chain dibasic acid, comprising: (1) cooling the hydrolysis solution to crystallize and separate alkali salt of long chain dibasic acid to provide an aqueous solvent solution; (2) distilling the aqueous solvent solution of step (1) to recover the solvent and to recover alkylamine; (3) cooling the residual solution of step (2) to precipitate and separate alkali salt of long chain amino acid to provide a mother liquor; (4) adding an acid to the mother liquor of step (3) to yield alkanoic acid; (5) adding an acid to an aqueous solution of the alkali salt of long chain dibasic acid of step (1) to obtain long chain dibasic acid; and (6) neutralizing the alkali salt of long chain amino acid of step (3) with an acid to obtain long chain amino acid.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: June 25, 2019
    Assignee: VITAWORKS IP, LLC
    Inventor: Songzhou Hu
  • Patent number: 10329242
    Abstract: There is disclosed a process for the purification of long chain amino acids by recrystallization in an aqueous solution of organic carboxylic acid in the absence or presence of solvent, comprising: (1) dissolving a long chain amino acid in an aqueous solution of organic carboxylic acid by heating; (2) cooling the solution of step (1) to crystallize the long chain amino acid; and (3) recovering the long chain amino acid of step (2) by means of solid-liquid separation.
    Type: Grant
    Filed: December 14, 2017
    Date of Patent: June 25, 2019
    Assignee: VITAWORKS IP, LLC
    Inventors: Songzhou Hu, William S. Hu
  • Patent number: 10329243
    Abstract: The present invention relates to a biphenyl derivative and use thereof, and the biphenyl derivative has a structure represented by the formula (I) as defined in the specification. The use refers the use of the biphenyl derivative or a pharmaceutically acceptable salt or solvate thereof, or a pharmaceutical composition comprising the biphenyl derivative or a pharmaceutically acceptable salt or solvate thereof in the preparation of a medicament for the treatment and/or prevention of ischemic stroke.
    Type: Grant
    Filed: March 11, 2016
    Date of Patent: June 25, 2019
    Assignee: XI'AN LIBANG PHARMACEUTICAL CO., LTD
    Inventors: Rutao Wang, Tao Chen, Long An, Yi Zhao, Weijiao Wang, Shupan Guo, Sa Xiao, Jinghua Pang, Huijing Hu
  • Patent number: 10329244
    Abstract: The invention relates to novel compounds which are especially suitable for use as writing monomers in holographic media. The invention further provides a photopolymer and a holographic medium comprising the inventive compounds, and an optical display, a security document and a holographic optical element comprising an inventive holographic medium.
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: June 25, 2019
    Assignee: Covestro Deutschland AG
    Inventors: Thomas Fäcke, Friedrich-Karl Bruder, Thomas Rölle, Dennis Hönel
  • Patent number: 10329245
    Abstract: A method for producing a compound of formula (I) or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer, such as compound 1 and compound 2 is disclosed. The method proceeds through an O-allylated tyrosine-based compound, such as compound 3 and preferably comprises [3,3] sigmatropic Claisen rearrangement and olefin cross metathesis reactions. In addition, a pharmaceutical composition comprising a compound of formula (I) a tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL) and a pharmaceutically acceptable carrier or excipient is disclosed.
    Type: Grant
    Filed: March 22, 2018
    Date of Patent: June 25, 2019
    Assignee: King Fahd University of Petroleum and Minerals
    Inventors: Muhammad Mansha, Yasir Abbas, Nisar Ullah
  • Patent number: 10329246
    Abstract: Provide herein are compounds with a general chemical structure of: Substituents R1 and R2 independently are H, Cl, F, Br, CH3, CF3, SH, —N(C1-3alkyl)2, —NHC(O)C1-3alkyl, or —NHC(O)C5-7cycloalkyl, substituent R3 is H or C1-3 alkyl and R4 is a bridged cycloalkene such as a bridged cyclohexene or a bridge-substituted cyclohexene. The compounds are therapeutics to treat a cancer, such as breast cancer, or metastatic cancers, to inhibit RUNX2 activity, such as protein expression, in a cancer cell and to increase survival of a subject with breast cancer.
    Type: Grant
    Filed: September 19, 2017
    Date of Patent: June 25, 2019
    Assignees: University of Maryland, Baltimore, The United States of America as represented by the Department of Veterans Affairs
    Inventors: Antonino Passaniti, MacKerell D. Alexander, Jr.
  • Patent number: 10329247
    Abstract: The present invention relates to: a polymerizable compound represented by a formula (I); a polymerizable composition comprising the polymerizable compound and an initiator; a polymer obtained by polymerizing the polymerizable compound or the polymerizable composition; and an optically anisotropic article comprising the polymer [in the formula, Y1 to Y8 are a chemical single bond, —O—, —O—C(?O)—, —C(?O)—O—, or the like; G1 and G2 are a divalent aliphatic group having 1 to 20 carbon atoms, or the like; Z1 and Z2 are an alkenyl group having 2 to 10 carbon atoms, or the like; A1 is a tetravalent aromatic group, or the like; A2 and A3 are a divalent alicyclic hydrocarbon group having 3 to 30 carbon atoms, or the like; A4 and A5 are a divalent aromatic group having 4 to 30 carbon atoms, or the like; Ax1 and Ax2 are an organic group having 2 to 30 carbon atoms that includes an aromatic ring, or the like; Ay1 and Ay2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; Q1 and Q2 are a hydrogen
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: June 25, 2019
    Assignee: ZEON CORPORATION
    Inventors: Kei Sakamoto, Satoshi Kiriki, Kumi Okuyama
  • Patent number: 10329248
    Abstract: The invention relates to a method for producing 1,5-pentanediisocyanate (PDI) by reacting 1,5-pentanediamine (PDA) with phosgene in the gas phase.
    Type: Grant
    Filed: December 7, 2018
    Date of Patent: June 25, 2019
    Assignee: Covestro Deutschland AG
    Inventors: Josef Sanders, Martin Ehrig, Reinhard Halpaap, Manfred Keller-Killewald, Armin Schymura, Dietmar Wastian
  • Patent number: 10329249
    Abstract: The sulindac derivatives are compounds of the formula: wherein R is one of twenty-five substituted or unsubstituted phenyl substituents; and pharmaceutically acceptable salts thereof. The sulindac derivatives are synthesized by refluxing sulindac hydrazide with appropriately substituted benzaldehydes in the presence of ethanol and catalytic amounts of glacial acetic acid. The sulindac derivatives may be used as active ingredients in pharmaceutical compositions for the treatment of inflammation or inflammatory diseases. The sulindac derivatives may also be used as analgesic and/or gastric sparing agents.
    Type: Grant
    Filed: October 3, 2018
    Date of Patent: June 25, 2019
    Assignee: King Saud University
    Inventors: Mashooq Ahmad Bhat, Mohamed A. Al-Omar, Nawaf Abdulaziz Alsaif, Syed Hidayathulla
  • Patent number: 10329250
    Abstract: According to the present invention, there can be provided a process for producing 7-dehydrocholesterol (7DHC), comprising culturing, in a medium, a 7DHC-producing Labyrinthulea microorganism in which sterol 24-C-methyltransferase activity is reduced or lost as compared to a parent strain, allowing 7DHC to be produced and accumulated in the culture, and collecting the 7DHC from the culture; and a process for producing vitamin D3, comprising irradiating, with ultraviolet light, 7-dehydrocholesterol produced by the production process.
    Type: Grant
    Filed: October 8, 2015
    Date of Patent: June 25, 2019
    Assignee: KYOWA HAKKO BIO CO., LTD.
    Inventors: Tetsuro Ujihara, Satoshi Mitsuhashi
  • Patent number: 10329251
    Abstract: A compound of the formula: CH3—SO2—O—O—SO2OH.
    Type: Grant
    Filed: November 17, 2014
    Date of Patent: June 25, 2019
    Assignee: Grillo-Werke AG
    Inventors: Timo Ott, Ingo Biertümpel
  • Patent number: 10329252
    Abstract: The present invention provides a compound represented by General Formula (I). The compound according to the present invention prevents the liquid crystal composition from being deteriorated due to light, has high compatibility with the liquid crystal composition, and does not impair the storage stability of the liquid crystal composition, thus the compound is useful as a constituent member of a liquid crystal composition. Since the liquid crystal composition and the liquid crystal display element containing the compound of the present invention exhibit UV resistance and have a high VHR, it is possible to obtain a liquid crystal display element with excellent display quality in which display defects such as burn-in and display unevenness do not occur or are suppressed.
    Type: Grant
    Filed: August 23, 2016
    Date of Patent: June 25, 2019
    Assignee: DIC CORPORATION
    Inventors: Yoshio Aoki, Ayaki Hosono
  • Patent number: 10329253
    Abstract: The present invention relates to a process for the synthesis of molecules that have a pyrrole ring bonded to a diol. In particular, the invention relates to the synthesis of molecules that have the pyrrole ring and a diol derived from serinol by means of a process that does not demand the use of solvents or chemical catalysts. The process consists of a first reaction phase that takes place without any solvents and/or organic diluents, giving rise to an intermediate compound, and a second phase in which the intermediate compound is converted into the required compound by heating the reaction mixture to a temperature ranging from 100° to 200° C. for an interval in the range of 1 to 500 minutes, or by adding a carbon allotrope or its derivatives.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: June 25, 2019
    Assignee: Politencnico di Milano
    Inventors: Vincenzina Barbera, Attilio Citterio, Maurizio Stefano Galimberti, Gabriella Leonardi, Roberto Sebastiano, Suresh Udhavrao Shisodia, Antonio Marco Valerio
  • Patent number: 10329254
    Abstract: The invention relates to a novel process for the preparation of rac-6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide (I) in pharmaceutically acceptable polymorphic form, through the conversion of a 3-bromo-2-oxo-cyclohexanecarboxylic acid alkyl ester into 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxylic acid alkyl ester, which in turn is processed to yield the final product.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: June 25, 2019
    Assignee: AOP ORPHAN PHARMACEUTICALS AG
    Inventors: Enrica Diodato, Katia Marcucci, Russell Thomas, Paul Wiedenau, Martin Rettig, Huw Roberts
  • Patent number: 10329255
    Abstract: The present disclosure relates to tosylate salts 1-{[4-(methoxymethyl)-4-({[(1R,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the LSD1-associated or mediated diseases such as cancer.
    Type: Grant
    Filed: August 11, 2016
    Date of Patent: June 25, 2019
    Assignee: Incyte Corporation
    Inventors: Yongchun Pan, Wayne Han, Ganfeng Cao, Zhongjiang Jia, Vaqar Sharief, Jiacheng Zhou
  • Patent number: 10329256
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Grant
    Filed: March 5, 2018
    Date of Patent: June 25, 2019
    Assignee: Oryzon Genomics, S.A.
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Àngeles Estiarte Martinez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Patent number: 10329257
    Abstract: The present invention provides compounds for the treatment of a bacterial infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the treatment of a bacterial infection in a subject.
    Type: Grant
    Filed: August 12, 2016
    Date of Patent: June 25, 2019
    Assignee: The Broad Institute, Inc.
    Inventors: Michael H. Serrano-Wu, Chao Fang
  • Patent number: 10329258
    Abstract: The present invention provides therapeutic strategies for treatment of severe debilitating diseases associated with IFN-I due to cGAS activation. In one aspect, the invention provides compounds of Formula (I): [Formula should be inserted here] and pharmaceutical uses thereof. In another aspect, the invention provides methods for treating an autoimmune disease or a monogenic disorder by administering an effective amount of a compound of Formula (I).
    Type: Grant
    Filed: April 26, 2016
    Date of Patent: June 25, 2019
    Assignee: UNIVERSITY OF WASHINGTON
    Inventors: Keith Elkon, Jie An, Mark Minie, Tomikazu Sasaki, Joshua J. Woodward
  • Patent number: 10329259
    Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X and Y are each independently selected from optionally-substituted aryl, optionally-substituted heteroaryl, optionally-substituted cycloalkyl, optionally-substituted heterocycloalkyl, or optionally-substituted alkyl; Q is H, hydroxyl, or optionally-substituted alkoxy; R1, R2, and R3 are each independently selected from H, optionally-substituted alkyl, optionally-substituted cycloalkyl, halogen, cyano, nitro, hydroxy, optionally-substituted alkoxy, amino, aminocarbonyl, optionally-substituted sulfonyl, optionally-substituted aryl, optionally-substituted heteroaryl, optionally-substituted carboxyl, acyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted phosphonyl, optionally-substituted phosphinyl, aralkyl, optionally-substituted thiol, or R2 and R3 together with Z form an optionally-substituted cycloalkyl ring or an optionally-substituted heterocycloalkyl ring; Z is B
    Type: Grant
    Filed: May 8, 2015
    Date of Patent: June 25, 2019
    Assignee: The United States of America, as represented by the Secretary, Department of Health & Human Services
    Inventors: George Kunos, Malliga Iyer, Resat Cinar, Kenner C. Rice
  • Patent number: 10329260
    Abstract: Disclosed are compounds of formula I as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also disclosed are pharmaceutical compositions comprising at least one such compound, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
    Type: Grant
    Filed: May 11, 2018
    Date of Patent: June 25, 2019
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Pravin L. Kotian, Yarlagadda S. Babu, Minwan Wu, Venkat R. Chintareddy, V. Satish Kumar, Weihe Zhang
  • Patent number: 10329261
    Abstract: A method of preparing 6-chloro-5-nitro-2,4-diaminopyrimidine includes: reacting guanidine hydrochloride with ethyl carbamoylacetate and sodium hypochlorite in the presence of a metal nitrate salt and acetate anhydride in an organic solvent.
    Type: Grant
    Filed: July 18, 2018
    Date of Patent: June 25, 2019
    Assignee: XI'AN TAIKOMED PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Yonghong Tang, Minghui Chang, Chengyuan Liang, Danni Tian, Juan Xia, Kaiqi Shi, Han Li, Xuechuan Wang
  • Patent number: 10329262
    Abstract: A new class of antibiotics effective against methicillin-resistant Staphylococcus aureus (MRSA) is disclosed (Formula V). Compounds of this class can impair cell-wall biosynthesis by binding to both the allosteric and the catalytic domains of penicillin-binding protein (PBP) 2a. This class of antibiotics holds promise in reversing obsolescence of staphylococcal PBPs as important targets for antibiotics. Embodiments of the invention thus provide novel antibacterial compounds that target penicillin-binding proteins and/or other important cellular targets. Methods for inhibiting the growth and/or replication of bacteria using the compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, including drug-resistant strains of Staphylococcus aureus.
    Type: Grant
    Filed: October 2, 2017
    Date of Patent: June 25, 2019
    Assignee: University of Notre Dame du Lac
    Inventors: Mayland Chang, Shahriar Mobashery, Renee Bouley
  • Patent number: 10329263
    Abstract: This invention provides a novel disubstituted 1,2,4-triazine compound or a pharmaceutically acceptable salt thereof, which has an aldosterone synthetase inhibitory activity and is useful for preventing and/or treating various diseases or conditions associated with aldosterone; a method for preparing it; use of it; as well as a pharmaceutical composition comprising it as an active ingredient. A compound of the general formula [I]: wherein RA is, for example, a group of the following formula (A-1): wherein ring A1 is, for example, a cycloalkyl group which may be substituted, and RB is, for example, a monocyclic cycloalkyl group, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 22, 2018
    Date of Patent: June 25, 2019
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Hideki Ushirogochi, Wataru Sasaki, Yuichi Onda, Ryo Sakakibara, Fumihiko Akahoshi
  • Patent number: 10329264
    Abstract: This invention relates to a novel chemical process for the synthesis of N?-benzyl-5-methylisoxazole-3-carbohydrazide (Isocarboxazid) which comprises reacting 5-methyl-3-isoxazole carboxylic acid ester with benzylhydrazine or a salt thereof in an aprotic organic solvent and in the presence of an organic base.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: June 25, 2019
    Assignee: Lundbeck Pharmaceuticals Italy S.P.A.
    Inventors: Carla De Faveri, Florian Anton Martin Huber, Nicola Antolini
  • Patent number: 10329265
    Abstract: Provided are methods of treating and/or preventing dermatological disorders. Provided are methods of reducing skin inflammation, reducing pain, and/or reducing itch in a subject in need thereof. The methods may include administering to the subject an effective amount of a TRPA1 and/or TRPV4 inhibitor. Further provided are compositions including a TRPA1 and/or TRPV4 inhibitor compound in combination with a carrier, vehicle, or diluent that is suitable for topical application.
    Type: Grant
    Filed: August 22, 2014
    Date of Patent: June 25, 2019
    Assignee: Duke University
    Inventors: Wolfgang Liedtke, Farshid Guilak
  • Patent number: 10329266
    Abstract: Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4 alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as oste
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: June 25, 2019
    Assignee: MEDIVIR AB
    Inventors: Lourdes Salvador Oden, Magnus Nilsson, Pia Kahnberg, Bertil Samuelsson, Urszula Grabowska
  • Patent number: 10329267
    Abstract: The invention addresses the problem of providing a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione that is suited to industrial production. The invention provides a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by reacting 3-bromo-3-buten-2-one and 2-hydroxy-1,4-naphthoquinone in the presence of a solvent, then obtaining crystals of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by adding an alcohol-based solvent and/or water to the reaction system, and treating the crystals by using a specific adsorbent in the presence of a solvent.
    Type: Grant
    Filed: July 15, 2016
    Date of Patent: June 25, 2019
    Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventors: Toshikazu Yagi, Satoshi Suzuki, Hiroto Tatamidani, Kazuki Hashimoto
  • Patent number: 10329268
    Abstract: The present invention provides a compound of formula N wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group, wherein N is in the form of the individual R- and S-enantiomer or a mixture of the (R)- and (S)-enantiomer. The present invention also provides a compound of formula MA. The present invention also provides processes for preparing the above compounds, and processes involving their use. The compounds are particularly useful as intermediates in the synthesis of peripherally-selective inhibitors of dopamine-?-hydroxylase.
    Type: Grant
    Filed: September 12, 2014
    Date of Patent: June 25, 2019
    Assignee: Bial-Portela & CA, S.A.
    Inventors: Domenico Russo, Jorge Wahnon, William Maton, Beat T. Weber, Paula Jeronimo, Luisa Sousa, Pedro Barrocas, Rita Pires, Ricardo Lima, Teofilo Vasconcelos
  • Patent number: 10329269
    Abstract: The present invention relates to compounds of formula (I): including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of, for example, cancer.
    Type: Grant
    Filed: August 29, 2018
    Date of Patent: June 25, 2019
    Assignees: Leukogene Therapeutics Incorporated, MUSC Foundation for Research Development
    Inventors: Nathan G. Dolloff, Reeder M. Robinson, Allen B. Reitz, Haiyan Bian
  • Patent number: 10329270
    Abstract: The present invention relates to pyridine, pyrimidine, pyrazine, and pyridazine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
    Type: Grant
    Filed: October 21, 2014
    Date of Patent: June 25, 2019
    Assignee: Merck Patent GmbH
    Inventors: Hui Qiu, Richard D. Caldwell, Constantin Neagu, Igor Mochalkin, Lesley Liu-Bujalski, Reinaldo Jones, Devon Tate, Theresa L. Johnson, Anna Gardberg
  • Patent number: 10329271
    Abstract: The present disclosure generally relates to methods of preparing nicotine and resolving R,S nicotine to enrich the (S)(?) enantiomer. The method may comprise combining N-methyl-2-pyrrolidone or a salt thereof with a nicotinate compound in the presence of a solvent and a strong base to form 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof; and reducing the 1-methyl-3-nicotinoyl-2-pyrrolidone or salt thereof in solution with Na2S2O4 to produce racemic nicotine or salt thereof. Resolving the racemic nicotine (or other enantiomeric mixture) may comprise combining the nicotine with (?)-O,O?-di-p-toluoyl-L-tartaric acid (L-PTTA).
    Type: Grant
    Filed: October 6, 2017
    Date of Patent: June 25, 2019
    Assignee: NJOY, LLC
    Inventors: Bert Willis, Mohammed Moinuddin Ahmed, Wesley Freund, Douglas Sawyer
  • Patent number: 10329272
    Abstract: Compounds of the formula (I), wherein A, Y—X, R1, R2, R3, R4, Rb, Rc, Rd, R5, R6, R7, Ra, m and n are as defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.
    Type: Grant
    Filed: August 8, 2016
    Date of Patent: June 25, 2019
    Assignee: Syngenta Participations AG
    Inventors: Stephan Trah, Farhan Bou Hamdan, Laura Quaranta, Matthis Weiss
  • Patent number: 10329273
    Abstract: The present invention provides compounds of Formula (I): a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, a solvate thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Grant
    Filed: August 30, 2018
    Date of Patent: June 25, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventor: Saleem Ahmad
  • Patent number: 10329274
    Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR4 or N; R1, R2, R3, R4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Grant
    Filed: February 1, 2018
    Date of Patent: June 25, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Qingjie Liu, Scott Hunter Watterson, John E. Macor, Khehyong Ngu, Saleem Ahmad
  • Patent number: 10329275
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An embodiment of the invention is the provision of a compound of Formula IIIA.
    Type: Grant
    Filed: June 14, 2018
    Date of Patent: June 25, 2019
    Assignees: FORMA TM, LLC, Genentech, Inc.
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng, Po-Wai Yuen