Patents Issued in September 11, 2018
  • Patent number: 10071949
    Abstract: A polymerizable liquid crystal compound represented by Chemical Formula 1: wherein in Chemical Formula 1, groups and variables are the same as defined in the detailed description.
    Type: Grant
    Filed: December 28, 2016
    Date of Patent: September 11, 2018
    Assignee: SAMSUNG ELECTRONICS CO., LTD.
    Inventors: Dmitry Androsov, Joungeun Yoo, Ju Hyun Kim, Eun Sung Lee, Changki Kim, Hyunseok Choi
  • Patent number: 10071950
    Abstract: Method of forming an olefin from a first olefin and a second olefin in a metathesis reaction, comprising step (i): (i) reacting the first olefin with the second olefin in the presence of a silica supported Mo- or W-alkylidene catalyst, wherein the first olefin and the second olefin are different from one another.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: September 11, 2018
    Assignee: XIMO AG
    Inventors: Georg Emil Frater, Jeno Varga, Christophe Coperet, Emmanuel Robe, Victor Mougel
  • Patent number: 10071951
    Abstract: The present application relates to a process for removing an organic compound having one or more positive charges from an aqueous solution, comprising the steps a) provision of the aqueous solution comprising the organic compound and of a hydrophobic organic solution which comprises a liquid cation exchanger, where the liquid cation exchanger is hydrophobic, and where the liquid cation exchanger has one or more negative charges and an overall negative charge, b) contacting the aqueous solution and the organic solution, and c) separating off the organic solution from the aqueous solution.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: September 11, 2018
    Assignee: Evonik Degussa GmbH
    Inventors: Frank Erhardt, Thomas Haas, Martin Roos, Daniel Demicoli, Markus Pötter, Anja Schubert, Jan Christoph Pfeffer, Thomas Tacke, Harald Häger, Andreas Pfennig, Marie-Dominique Przybylski-Freund
  • Patent number: 10071952
    Abstract: Alpha/alpha-prime/alkoxylated glycerol linear carbonic esters have formula (VI): where p is an integer higher than 1, x is an integer equaling 0 or 1 with x not always being zero, and M1 is hydrogen (H). Q1 can be a hydrocarbon aliphatic group, an amino hydrocarbon group or an oxygenated amino hydrocarbon group. G1 can be an ?/??-alkoxylated propyl group of general formula (II?): where R4, R5 and R6 are variously hydrogen (H), an alkyl or an amino-alkyl group having 1 to 5 carbon atoms, or general formula (VII): where R7 is a H or a hydrocarbon group having 1 to 6 carbon atoms, and m is an integer between 0 and 10 inclusive, and X is —O— or —NH—.
    Type: Grant
    Filed: February 23, 2018
    Date of Patent: September 11, 2018
    Assignees: CHRYSO, INSTITUT NATIONAL POLYTECHNIQUE DE TOULOUSE, INSTITUT NATIONAL DE LA RECHERCHE AGRONOMIQUE (INRA)
    Inventors: Frédéric Leising, Zéphirin Mouloungui
  • Patent number: 10071953
    Abstract: The invention includes compositions comprising selective AKR1C3 inhibitors. The invention also includes compositions comprising bifunctional AKR1C3 inhibitors and selective androgen receptor modulators. The invention further includes methods of treatment using the compositions of the invention.
    Type: Grant
    Filed: January 12, 2016
    Date of Patent: September 11, 2018
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Trevor M. Penning, Adegoke O. Adeniji, Michael C. Byrns, Jeffrey Winkler, Barry Twenter
  • Patent number: 10071954
    Abstract: Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of hydrogen peroxide and are therefore selective anti-cancer therapeutics for cancers associated with elevated reactive oxygen species (ROS). Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.
    Type: Grant
    Filed: October 2, 2015
    Date of Patent: September 11, 2018
    Assignee: University of Cincinnati
    Inventors: Edward J. Merino, James Mulloy, Anish K. Vadukoot, Mark Wunderlich, Safnas F. Abdulsalam
  • Patent number: 10071955
    Abstract: The high-yield circular production method of taurine includes the following steps: S1, ethylene oxide reacts with sodium bisulfite solution to generate sodium hydroxyethyl sulfonate; S2, sodium hydroxyethyl sulfonate obtained in S1 is subjected to ammonolysis reaction in ammonia, and ammonia gas is recycled through flash evaporation upon completion of the reaction; S3, a reaction solution obtained after flash evaporation in S2 is sent to pass through an acidic cation exchange resin column, a material liquid containing taurine is collected, the inactivated resin column is subjected to regeneration with sulfur dioxide or carbon dioxide aqueous solution, and an eluent acquired during regeneration can be recycled directly or recycled after treated by sulfur dioxide; S4, the material liquid collected in S3 is subjected to post treatment to acquire taurine.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: September 11, 2018
    Assignee: QIANJIANG YONGAN PHARMACEUTICAL Co., Ltd.
    Inventors: Yong Chen, Xiquan Fang, Shaobo Li
  • Patent number: 10071956
    Abstract: The present invention provides a process for the preparation of dibenzenesulfonimide.
    Type: Grant
    Filed: July 15, 2015
    Date of Patent: September 11, 2018
    Assignee: SRF LIMITED
    Inventors: Thirupathi Arumugam, Mariano Patrick Philips, Dilli Babu, Maheshwaran Chellaiah, Sarathy Iyengar, Rajdeep Anand
  • Patent number: 10071957
    Abstract: The invention provides novel compounds having the general formula (I) and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, ring D, R1, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: July 5, 2013
    Date of Patent: September 11, 2018
    Assignees: GENENTECH, INC., XENON PHARMACEUTICALS INC.
    Inventors: Christoph Martin Dehnhardt, Sultan Chowdhury, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Brian Safina, Daniel P. Sutherlin
  • Patent number: 10071958
    Abstract: According to the present invention, it becomes possible to perform a process for converting into an ?-substituted cysteine represented by general formula (1) or a salt thereof at low cost and on an industrial scale by employing a process that is routed through a compound represented by general formula (3) to a compound represented by general formula (6). Particularly, by employing a process that is routed through a compound represented by general formula (7-2), it becomes possible to detach a tert-butyl protection group in a simple manner and to produce the compound represented by general formula (1) with high purity. Furthermore, by employing a process that is routed through tert-butylthiomethanol or a process that is routed through a compound represented by general formula (9), it becomes possible to produce a compound represented by general formula (2) without generating bischloromethylether that is an oncogenic substance.
    Type: Grant
    Filed: May 1, 2014
    Date of Patent: September 11, 2018
    Assignee: API Corporation
    Inventors: Yuuki Asuma, Hisatoshi Uehara, Tomoko Maeda, Yasuyo Saito, Ryoma Miyake, Hiroshi Kawabata
  • Patent number: 10071959
    Abstract: According to the present invention, a polythiol compound having a total nitrogen content of 50 to 600 ppm inclusive can be provided. According to the present invention, a method for producing the polythiol compound can also be provided, said method being characterized by comprising the steps of: reacting a polyalcohol with thiourea to prepare a thiuronium salt; and adding at least one base selected from the group consisting of hydrazine (hydrate), ammonia and an amine and an inorganic base (that is different from hydrazine (hydrate) or ammonia) to the thiuronium salt in the presence of an organic solvent to hydrolyze the thiuronium salt.
    Type: Grant
    Filed: October 28, 2014
    Date of Patent: September 11, 2018
    Assignee: MITSUBISHI GAS CHEMICAL COMPANY, INC.
    Inventors: Yoshihiko Nishimori, Teruo Kamura, Hiroshi Horikoshi
  • Patent number: 10071960
    Abstract: The present subject matter is directed to an enaminone-grafted trithiocarbonate compound having the structure: and the anticancer and antimicrobial activities exhibited by the compound.
    Type: Grant
    Filed: October 5, 2017
    Date of Patent: September 11, 2018
    Assignee: KING SAUD UNIVERSITY
    Inventors: Yahia Nasser Mabkhot, Jamal Mohammed Ali Khaled, Mujeeb Abdullah Sultan, Fahd Ali Nasr Mohammed, Naiyf Sultan Helial Alaloi Alharbi, Salim Showiman Al-Showiman, Hazem Ahmed Ghabbour
  • Patent number: 10071961
    Abstract: Inhibitors of HBV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein, X, R1 to R7 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.
    Type: Grant
    Filed: November 8, 2017
    Date of Patent: September 11, 2018
    Assignee: Janssen Sciences Ireland UC
    Inventors: Koen Vandyck, Geerwin Yvonne Paul Haché, Bart Rudolf Romanie Kesteleyn, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 10071962
    Abstract: Compounds having a structure of Structure I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R4, R6, Y1 and Y2 are as defined herein, and wherein at least one of R3 or R4 is a straight-chain C1-C6 haloalkyl, are provided. Uses of such compounds for treatment of various indications, including prostate cancer, as well as methods of treatment involving such compounds are also provided.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: September 11, 2018
    Assignees: British Columbia Cancer Agency Branch, The University of British Columbia
    Inventors: Luping Yan, Raymond J. Andersen, Marianne Dorothy Sadar, Nasrin R. Mawji, Carmen Adriana Banuelos
  • Patent number: 10071963
    Abstract: The present invention relates to a novel polymorphic form of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine hydrochloride.
    Type: Grant
    Filed: July 3, 2015
    Date of Patent: September 11, 2018
    Assignee: H. LUNDBECK A/S
    Inventors: Kristine Birklund Andersen, Michael Harold Rock, Heidi Lopez De Diego, Frans Dennis Therkelsen
  • Patent number: 10071964
    Abstract: This invention relates to new inhibitors of butyrylcholinesterase with general formulas I and II, where substituents are described in patent description. Compounds can be in the form of pure enantiomers or as racemic mixtures, or in the form of pharmaceutically acceptable salts. The present invention relates to the use of these inhibitors for the treatment of Alzheimer's disease and other forms of dementia.
    Type: Grant
    Filed: March 22, 2016
    Date of Patent: September 11, 2018
    Assignee: UNIVERZA V LJUBJIANI
    Inventors: Boris Brus, Urban Kosak, Damijan Knez, Nicolas Coquelle, Jacques-Philippe Colletier, Stanislav Gobec
  • Patent number: 10071965
    Abstract: The present invention provides novel 2-pyridone compounds and 4-pyridone compounds and methods of treating a subject infected with a pathogen of Staphylococcus aureus, Mycobacterium tuberculosis, Francisella tularensis, Burkholderia pseudomallei, Yersinia pestis, Escherichia coli and Proteus mirabilisone.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: September 11, 2018
    Assignee: THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORK
    Inventors: Peter Tonge, Pan Pan
  • Patent number: 10071966
    Abstract: The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: September 11, 2018
    Assignees: LUDWIG-MAXIMALIANS-UNIVERSITAT MUNCHEN, MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DER WISSENSCHAFTEN E.V.
    Inventors: Armin Giese, Uwe Bertsch, Hans Kretzschmar, Matthias Habeck, Thomas Hirschberger, Paul Tavan, Christian Griesinger, Andrei Leonov, Sergey Ryazanov, Petra Frick, Markus Geissen, Martin H. Groschup, Jens Wagner
  • Patent number: 10071967
    Abstract: The present invention relates to fungicidal N-cycloalkyl-N-{[2-(1-substitutedcycloalkyl)phenyl]methylene} carboxamide derivatives and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: September 11, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Pierre Cristau, Philippe Desbordes, Julie Geist, Lionel Nicolas, Philippe Rinolfi, Jan-Peter Schmidt, Tomoki Tsuchiya, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
  • Patent number: 10071968
    Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor and more particularly to methyl-1H-pyrazole alkylamine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: December 15, 2015
    Date of Patent: September 11, 2018
    Assignee: ESTEVE PHARMACEUTICALS S.A.
    Inventors: Antoni Torrens-Jover, Josep Mas-Prio, Carmen Almansa-Rosales, Monica Garcia-Lopez
  • Patent number: 10071969
    Abstract: Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphophoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.
    Type: Grant
    Filed: November 23, 2015
    Date of Patent: September 11, 2018
    Assignee: MannKind Corporation
    Inventors: Kelly Sullivan Kraft, John J. Freeman, Paul Serwinski, Vincent Pavia, Otto Phanstiel, Navneet Kaur
  • Patent number: 10071970
    Abstract: This invention provides compounds of the formula I: and their pharmaceutically acceptable salts, useful as sodium channel blockers, compositions containing the same, therapeutic methods and uses for the same and processes for preparing the same.
    Type: Grant
    Filed: March 7, 2017
    Date of Patent: September 11, 2018
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Patent number: 10071971
    Abstract: The present invention relates to compounds of the formula I wherein the variables are defined in the description and claims, their preparation and uses thereof.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: September 11, 2018
    Assignee: BASF SE
    Inventors: Wassilios Grammenos, Ian Robert Craig, Nadege Boudet, Bernd Mueller, Jochen Dietz, Erica May Cambeis, Jan Klaas Lohmann, Thomas Grote, Egon Haden, Ana Escribano Cuesta
  • Patent number: 10071972
    Abstract: This invention relates to a process for the preparation of triazine carbamates by reacting a mixture of an aminotriazine A having at least two amino groups per molecule, an organic carbonate C, and a base B selected from the group consisting of alkoxides, and arylalkoxides of metals M, which may be alkali or earth alkali metals, and a solvent S which is a monohydric alcohol solvent R2OH or a mixture of solvents that comprises a monohydric alcohol R2OH, and a monohydric alcohol R3OH, or a mixture of solvents that comprises a monohydric alcohol R2OH with a further solvent selected from the group consisting of ether, alcohol, and hydrocarbon solvents, and adding to the products of the said reaction, an acid or a solution of an acid in a solvent.
    Type: Grant
    Filed: September 7, 2015
    Date of Patent: September 11, 2018
    Assignee: ALLNEX NETHERLANDS B.V.
    Inventor: Lawrence Flood
  • Patent number: 10071973
    Abstract: This invention pertains to a crystalline compound of Formula (A) as described herein and compositions containing this crystalline compound, as well as methods of using the compound or pharmaceutical compositions comprising it to treat bacterial infections. The compound and compositions are especially useful to treat Gram negative bacterial infections, including multi-drug resistant strains.
    Type: Grant
    Filed: June 12, 2017
    Date of Patent: September 11, 2018
    Assignee: Novartis AG
    Inventors: Jiping Fu, Siyi Jiang, Andreas Kordikowski, Zachary Kevin Sweeney
  • Patent number: 10071974
    Abstract: The invention relates to morpholine and 1,4-oxazepane amide derivatives of general formula (I), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture of the compounds according to the invention.
    Type: Grant
    Filed: November 12, 2015
    Date of Patent: September 11, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Rocco Mazzaferro, Marco Ferrara, Riccardo Giovannini, Iain Lingard, Klaus Rudolf
  • Patent number: 10071975
    Abstract: The present invention relates to macrocyclic amidinourea derivatives of formula 8, methods of preparation and uses thereof, pharmaceutical compositions in particular to be used as chitinase inhibitors in the treatment of a fungal infection.
    Type: Grant
    Filed: June 18, 2014
    Date of Patent: September 11, 2018
    Assignee: CYGNET BIOSCIENCES B.V.
    Inventors: Stefania Sanfilippo, Brunella Posteraro, Maurizio Sanguinetti, Maurizio Botta, Giorgio Maccari, Filomena De Luca, Jean-Denis Docquier, Davide Deodato
  • Patent number: 10071976
    Abstract: Provided herein are small molecule Fatty Acid Synthase Inhibitors, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
    Type: Grant
    Filed: March 5, 2015
    Date of Patent: September 11, 2018
    Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
    Inventors: Nicholas D. P. Cosford, Jeffrey Smith
  • Patent number: 10071977
    Abstract: A process for preparing a batch of highly purified, pharmaceutical grade tasimelteon comprises analyzing a batch of tasimelteon synthesized under GMP conditions for the presence of one or more identified impurities.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: September 11, 2018
    Assignee: VANDA PHARMACEUTICALS INC.
    Inventors: Deepak Phadke, Natalie M Platt, Ravi K Pandrapragada
  • Patent number: 10071978
    Abstract: The invention discloses novel processes for production, enrichment and/or isolation of alpha-tocotrienol from source material comprising at least one non-alpha-tocotrienol, such as natural extracts comprising mixed tocotrienols.
    Type: Grant
    Filed: March 11, 2016
    Date of Patent: September 11, 2018
    Assignee: BIOELECTRON TECHNOLOGY CORPORATION
    Inventors: Kieron W. Wesson, Andrew W. Hinman, Orion D. Jankowski
  • Patent number: 10071979
    Abstract: The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), useful for treating CFTR mediated diseases such as cystic fibrosis.
    Type: Grant
    Filed: April 15, 2015
    Date of Patent: September 11, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Gerald J. Tanoury, Cristian Harrison, Benjamin Joseph Littler, Peter Jamison Rose, Robert Michael Hughes, Young Chun Jung, David Andrew Siesel, Elaine Chungmin Lee, Daniel T. Belmont, William A. Nugent
  • Patent number: 10071980
    Abstract: A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ?4?1, ?5?1, ?4?7, ?v?3 and ?L?2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.
    Type: Grant
    Filed: June 26, 2015
    Date of Patent: September 11, 2018
    Assignee: TEXAS HEART INSTITUTE
    Inventors: Ronald J. Biediger, Robert V. Market
  • Patent number: 10071981
    Abstract: A method of reducing cellular damage to a plant by treating the plant with a compound containing an NO-releasing moiety and an H2S-releasing moiety covalently bonded to an aspirin derived core or a NOSH compound is claimed. The compounds may also be used in a method of priming a plant against abiotic stress factors and a method of promoting plant growth.
    Type: Grant
    Filed: February 11, 2015
    Date of Patent: September 11, 2018
    Assignees: RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK, CYPRUS UNIVERSITY OF TECHNOLOGY
    Inventors: Khosrow Kashfi, Vasileios Fotopoulos
  • Patent number: 10071982
    Abstract: Provided are methods for using bis-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: September 11, 2018
    Assignees: University of Kentucky Research Foundation, University of Utah
    Inventors: Joseph R Holtman, Peter Anthony Crooks, Linda P Dwoskin, J Michael McIntosh, Elzbieta Pogonowska Wala
  • Patent number: 10071983
    Abstract: Novel fluorogenic compounds designed such that upon a chemical event, compounds capable of emitting NIR light are generated, are disclosed. The compounds comprise two or more acceptor-containing moieties and a cleavable donor-containing moiety, being in complete pi-electrons conjugation and being such that no delocalization of pi-electrons is enabled. Also disclosed are fluorescent compounds generated upon subjecting the fluorogenic compounds to a chemical event (e.g., deprotonation). Also disclosed are uses of the fluorogenic compounds as NIR probed with a Turn-ON mechanism in monitoring presence and/or level of various analytes.
    Type: Grant
    Filed: April 18, 2016
    Date of Patent: September 11, 2018
    Assignee: Ramot at Tel-Aviv University Ltd.
    Inventors: Doron Shabat, Ronit Satchi-Fainaro
  • Patent number: 10071984
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as pancreatic cancer, prostate cancer, breast cancer, bladder cancer, lung cancer, gastric cancer, leukemia and/or melanoma and the like.
    Type: Grant
    Filed: May 5, 2017
    Date of Patent: September 11, 2018
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Young K. Chen, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 10071985
    Abstract: The present disclosure relates to a compound of formula (Ia), (Ib), (IIa), and (IIb): which are useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Grant
    Filed: August 17, 2017
    Date of Patent: September 11, 2018
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Steven J. Henry, John O. Link, Charles William Rowe, Roland D. Saito, Scott D. Schroeder, Dimitrios Stefanidis, Winston C. Tse, Jennifer R. Zhang
  • Patent number: 10071986
    Abstract: The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: May 18, 2017
    Date of Patent: September 11, 2018
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maria Gabriella Brasca, Simona Bindi, Marina Caldarelli, Marcella Nesi, Sten Christian Orrenius, Achille Panzeri
  • Patent number: 10071987
    Abstract: A compound having the structure according to formula III wherein: X is NH or S; R1 is H or (1C-4C)alkyl; R2 is (1C-4C)alkyl, phenyl or a monocyclic aromatic ring having one or more N—, O— or S— atoms in the ring, which alkyl, phenyl or aromatic ring is optionally substituted with one or more groups selected from (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, phenyloxy, phenylthio, halogen, or nitro; R3 and R4 are each independently H, (1C-6C)alkyl, (2C-6C) alkenyl, (2C-6C)alkynyl, cyano, (3C-6C)cycloalkyl, phenyl, a monocyclic aromatic ring having one or more N—, O— or S— atoms in the ring, a monocyclic non-aromatic ring having one or more N—, O— or S— atoms in the ring, each optionally substituted with hydroxyl, (1C-4C)alkoxy, phenyl, cycloalkyl, piperidyl, piperazinyl, furyl, thienyl, pirazinyl, pyrrolyl, 2H-pyrrolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyrrolidonyl, pyrrolinyl, imidazolinyl, imidazolyl, a monocyclic aromatic ring having one or more N—, O— or S— atoms in the r
    Type: Grant
    Filed: October 10, 2017
    Date of Patent: September 11, 2018
    Assignees: Compound Handling B.V., Stichting Katholieke Universiteit
    Inventors: Onno Van Hooij, Jacobus Antonius Schalken, Hendrik Engelbertus Vietor, Dennis Patrick Piet, Petrus Emmanuel Marie Maas, Johann Heinrich Tijhuis, Sirik Deerenberg, Nanda Elisabeth Sprenkels, Siu Ha Tang
  • Patent number: 10071988
    Abstract: Substituted 1,2,3-triazoles as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity.
    Type: Grant
    Filed: February 9, 2017
    Date of Patent: September 11, 2018
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Gang Chen, Christa C. Chrovian, Heather R. Coate, Curt A. Dvorak, Christine F. Gelin, Afton Hiscox, Michael A. Letavic, Jason C. Rech, Akinola Soyode-Johnson, Brice Stenne, Jessica L. Wall, Wei Zhang
  • Patent number: 10071989
    Abstract: The present invention relates to substituted cinnamamide derivatives, the method for preparing thereof and the use thereof. Each of said derivatives has a structure of formula (I). The method for preparing the substituted cinnamamides and their derivatives of the present invention is also disclosed. Substituted piperonal derivatives are selected as starting materials to prepare the substituted cinnamamide derivatives of the present invention by Wittig reaction and acid-amine condensation reaction. Further, a use of the present compounds in preventing and treating depressive-type mental diseases is disclosed.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: September 11, 2018
    Assignee: TASLY PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Xiaohui Ma, Yuanpeng Jin, Min Han, Shuiping Zhou, Wangyi Zhou, Xuejun Luo, Guocheng Wang, Lulu Yan, Lanlan Zhang, Yonghong Zhu
  • Patent number: 10071990
    Abstract: A technique is provided to visualize microtubules in live cells that does not require genetic manipulation or microinjection. Moreover, this method also avoids perturbation of the endogenous microtubule network that occurs with taxol treatment. This technique exploits tyrosination and detyrosination of tubulin, a posttranslational modification cycle specific to the C-terminus of ?-tubulin. Specifically, cells are grown in medium supplemented with a tyrosine derivative possessing a reactive functional group. The cellular enzyme tubulin tyrosine ligase attaches the unnatural amino acid to a single site on tubulin. Addition of fresh medium containing a suitably derivatized fluorophore then yields fluorescent tubulin, which incorporate into cellular microtubules. Importantly, the tubulin labeling approach demonstrated here does not detrimentally affect microtubule network or cell morphology. Thus we present a simple, robust labeling technique that allows microscopic analysis of microtubules in live cells.
    Type: Grant
    Filed: June 2, 2014
    Date of Patent: September 11, 2018
    Assignee: The Research Foundation for The State University of New York
    Inventors: Susan Bane Tuttle, Kamalika Mukherjee
  • Patent number: 10071991
    Abstract: The present invention is directed to substituted pyridine derivatives, pharmaceutical compositions containing said derivatives and the use of said derivatives in the treatment of disorders mediated by c-fms kinase. The present invention is further directed to a process for the preparation of said substituted pyridine derivatives.
    Type: Grant
    Filed: February 23, 2017
    Date of Patent: September 11, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Jie Chen, Matthew Donahue, Heng-Keang Lim, Ronghui Lin, Rhys Salter, Jiejun Wu, Yong Gong
  • Patent number: 10071992
    Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
    Type: Grant
    Filed: August 11, 2017
    Date of Patent: September 11, 2018
    Assignee: Pfizer Inc.
    Inventors: Markus Boehm, Shawn Cabral, Matthew S. Dowling, Kentaro Futatsugi, Kim Huard, Esther Cheng Yin Lee, Allyn T. Londregan, Jana Polivkova, David A. Price, Qifang Li
  • Patent number: 10071993
    Abstract: An object is to provide a novel carbazole derivative that has an excellent carrier-transport property and can be suitably used for a transport layer or as a host material of a light-emitting element. Another object is to provide an organic semiconductor material and a light-emitting element material each using the carbazole derivative. As the carbazole derivative that can achieve the above objects, a carbazole derivative in which a carbazolyl group whose either 2- or 3-position of carbazole is substituted by the 4-position of a dibenzothiophene skeleton or a dibenzofuran skeleton is bonded to aromatic hydrocarbon that has 14 to 70 carbon atoms and includes a condensed tricyclic ring, a condensed tetracyclic ring, a condensed pentacyclic ring, a condensed hexacyclic ring, or a condensed heptacyclic ring has been able to be synthesized.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: September 11, 2018
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroki Suzuki, Kyoko Takeda, Sachiko Kawakami, Tsunenori Suzuki, Satoshi Seo, Nobuharu Ohsawa
  • Patent number: 10071994
    Abstract: The invention relates to a homoserine lactone derivative of Formula I, preparation method and use thereof.
    Type: Grant
    Filed: May 25, 2015
    Date of Patent: September 11, 2018
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Song Li, Junhai Xiao, Qi Sun, Wu Zhong, Lili Wang, Zhibing Zheng, Yunde Xie, Xingzhou Li, Xinbo Zhou, Xiaokui Wang, Ruiyuan Cao
  • Patent number: 10071995
    Abstract: The invention relates to substituted oxopyridine derivatives and to processes for preparation thereof, and also to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
    Type: Grant
    Filed: September 22, 2015
    Date of Patent: September 11, 2018
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Susanne Röhrig, Eloisa Jimenez Núnez, Karl-Heinz Schlemmer, Adrian Tersteegen, Henrik Teller, Alexander Hillisch, Stefan Heitmeier, Martina Victoria Schmidt, Jan Stampfuß
  • Patent number: 10071996
    Abstract: The present invention provides: a novel compound which is characterized by being capable of increasing the number of heart beats or a blood pressure mildly to improve hemodynamics, and which is useful as a therapeutic or prophylactic agent for atrial fibrillation and heart failure; and a pharmaceutical composition which contains the compound. The present invention relates to: an optical isomer of a 1,4-benzothiazepine-1-oxide derivative represented by general formula [II] (wherein R represents a hydrogen atom or a hydroxy group; and * indicates the presence of an optical isomer) or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition which contains the optical isomer or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 17, 2015
    Date of Patent: September 11, 2018
    Assignees: AETAS PHARMA CO., LTD.
    Inventor: Noboru Kaneko
  • Patent number: 10071997
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: November 24, 2015
    Date of Patent: September 11, 2018
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Michel Muehlebach, Andrew Edmunds, Andre Jeanguenat, Pierre Joseph Marcel Jung, Peter Renold, Ottmar Franz Hueter
  • Patent number: 10071998
    Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, ring A, RA, m, ring B, RB, and n are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: September 11, 2018
    Inventors: Wen-Lian Wu, Shuwen He, Shawn P. Walsh, Jared N. Cumming