Patents Issued in November 22, 2016
  • Patent number: 9499451
    Abstract: Syrup produced in a lignocellulosic biomass fermentation process is used as a binder for soil conditioning materials to make an agricultural composition that is easily handled and applied. The syrup binds powdery soil conditioning materials such as lime and gypsum to form pellets or granules.
    Type: Grant
    Filed: October 9, 2014
    Date of Patent: November 22, 2016
    Assignee: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Steven W Ogle, Stephanie C Vrakas, David William Wood
  • Patent number: 9499452
    Abstract: A primary fuel catalyst used to combust a secondary fuel, the primary fuel comprising the gases produced by water electrolysis. When secondary fuels are combusted by the primary fuel, the by-products include heat, water and other more stable by-product materials. When the secondary fuel is a hazardous waste or a radioactive material and either is bound to thermite before combustion, the by-products are no longer hazardous or have significantly reduced radiation levels after one or more passes. Embodiments of the present invention relate to the method for accelerating the decay of hazardous and/or radioactive waste products, and more particularly they relate to the nuclear transmutation of heavy radioactive elements into lighter ones with shorter half-lives and then finally to stable daughter products. Therefore, the invented process relates to reducing the long-term toxicity of hazardous and/or radioactive waste and to, an economic and effective process facility for doing so.
    Type: Grant
    Filed: October 1, 2014
    Date of Patent: November 22, 2016
    Inventor: Geoffrey Courtright
  • Patent number: 9499453
    Abstract: A catalyst filling apparatus is for a bubble column slurry bed reactor for the FT synthesis reaction. The apparatus includes: a slurry preparation tank installed adjacent to the reactor and configured to prepare a slurry S from a FT synthesis reaction catalyst and a slurry preparation oil; an upper part communication line configured to direct the slurry from the reactor to the slurry preparation tank; a lower part communication line configured to direct the slurry in the slurry preparation tank to the reactor; and a pressure equalizing line configured to communicate the reactor with the slurry preparation tank. The upper part communication line is downwardly inclined from the reactor toward the slurry preparation tank, and the lower part communication line is upwardly inclined from the reactor toward the slurry preparation tank. An inert gas introduction device is provided on the slurry preparation tank.
    Type: Grant
    Filed: March 27, 2013
    Date of Patent: November 22, 2016
    Assignees: Japan Oil, Gas and Metals National Corporation, INPEX CORPORATION, JX Nippon Oil & Energy Corporation, Japan Petroleum Exploration Co., Ltd., COSMO OIL CO., LTD., NIPPON STEEL & SUMKIN ENGINEERING CO., LTD.
    Inventor: Kazuhiko Tasaka
  • Patent number: 9499454
    Abstract: Olefins may be produced by the reductive dehydroxylation of vicinal polyols and/or their respective esters, in an aqueous reaction medium, under a hydrogen atmosphere, under suitable conditions, and in the presence of a halogen-based, preferably iodine-based, catalyst, wherein a solubility enhancing agent is employed to increase the solubility of the iodine-based catalyst in the aqueous reaction medium.
    Type: Grant
    Filed: December 5, 2012
    Date of Patent: November 22, 2016
    Assignee: Dow Global Technologies LLC
    Inventors: Raj Deshpande, Paul Davis, Vandana Pandey, Nitin Kore
  • Patent number: 9499455
    Abstract: The invention concerns a process for the selective dimerization of ethylene to 1-butene employing a catalytic composition comprising at least one alkoxy or aryloxy titanium compound, at least one additive selected from ether type compounds and at least one aluminium compound.
    Type: Grant
    Filed: July 2, 2015
    Date of Patent: November 22, 2016
    Assignee: IFP ENERGIES NOUVELLES
    Inventors: Lionel Magna, Helene Olivier-Bourbigou
  • Patent number: 9499456
    Abstract: A process for the tetramerisation of ethylene under solution phase conditions is carried out in the presence of an activated catalyst at a temperature above 80° C. and up to a temperature of about 115° C. The activated catalyst is provided by combining a source of chromium, a diphosphine ligating compound and optionally a catalyst activator or combination of catalyst activators. The process forms at least 30% 1-octene and a polyethylene co-product that, together with any other reaction products, remains substantially dissolved in the liquid phase. The polyethylene co-product has a weight average molecular weight (Mw) of less than 200 000 g/mol, a number average molecular weight (Mn) of less than 3 000 g/mol, and a melt flow index of more than 20 g/10 minutes.
    Type: Grant
    Filed: May 8, 2013
    Date of Patent: November 22, 2016
    Assignee: SASOL TECHNOLOGY (PROPRIETARY) LIMITED
    Inventors: Matthew James Overett, Elzet Grobler, Stephen John Evans, Kevin Blann
  • Patent number: 9499457
    Abstract: The invention relates to a hydrocarbon conversion process and a reactor configured to carry out the hydrocarbon conversion process. The hydrocarbon conversion process is directed to increasing the overall equilibrium production of ethylene from typical pyrolysis reactions. The hydrocarbon conversion process can be carried out by exposing a hydrocarbon feed to a peak pyrolysis gas temperature in a reaction zone in the range of from 850° C. to 1200° C.
    Type: Grant
    Filed: November 16, 2015
    Date of Patent: November 22, 2016
    Assignee: ExxonMobil Chemical Patents Inc.
    Inventors: Frank Hershkowitz, Paul F. Keusenkothen, Ian J. Laurenzi
  • Patent number: 9499458
    Abstract: Mixed pentenes may be converted to propylene by feeding an alcohol, linear pentenes, and isopentenes to an etherification reactor. The alcohol and isopentenes may be reacted in the etherification reactor to convert isopentenes to tertiary amyl alkyl ether, which may be separated from the linear pentenes, recovered as a linear pentene fraction. The tertiary amyl alkyl ether may be fed to a decomposition reactor to convert at least a portion of the tertiary amyl alkyl ether to alcohol and isopentenes. The alcohol and isopentenes may then be separated to recover an isopentene fraction and an alcohol fraction. The isopentene fraction is then fed to a skeletal isomerization reactor to convert at least a portion of the isopentenes to linear pentenes, the effluent from which may be recycled to the etherification reactor. Ethylene and the linear pentene fraction may then be to a metathesis reactor to produce propylene.
    Type: Grant
    Filed: November 1, 2013
    Date of Patent: November 22, 2016
    Assignee: Lummus Technology Inc.
    Inventors: Bala Ramachandran, Sukwon Choi
  • Patent number: 9499459
    Abstract: The present invention relates to substituted benz[a]anthracene derivatives, to the preparation and use thereof in organic electroluminescent devices, and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as matrix material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.
    Type: Grant
    Filed: July 5, 2010
    Date of Patent: November 22, 2016
    Assignee: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Arne Buesing, Holger Heil, Philipp Stoessel, Michael Holbach
  • Patent number: 9499460
    Abstract: An alcohol production method whereby high quality alcohol can be easily and effectively produced includes a step in which an alcohol solution, which contains sugar and/or sugar alcohol as an impurity and an alcohol other than sugar alcohol as a main component, has the sugar and/or sugar alcohol adsorptively removed therefrom by contacting the alcohol solution with one type or a mixture of two or more types of adsorbents selected from zeolite, an ion-exchange resin, silica alumina, and alumina.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: November 22, 2016
    Assignee: Toray Industries, Inc.
    Inventors: Kenji Kawamura, Masateru Ito, Satoshi Sakami, Katsushige Yamada
  • Patent number: 9499461
    Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: November 22, 2016
    Assignee: NeOnc Technologies, Inc.
    Inventors: Thomas Chen, Daniel Levin, Satish Puppali
  • Patent number: 9499462
    Abstract: Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods for treatment, inhibition, and/or abatement of cognitive decline and/or Alzheimer's disease with a compound or pharmaceutically acceptable salt of the invention are also provided. Also provided are methods of preparing the compounds/compositions of the invention.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: November 22, 2016
    Assignee: Cognition Therapeutics, Inc.
    Inventors: Gilbert M. Rishton, Susan Catalano
  • Patent number: 9499463
    Abstract: The invention relates to mixtures of constitutional isomer bisphosphites of formulae (1a) and (2a), to a method for the production thereof, to the reaction thereof with metals to form mixtures containing complex compounds of the constitutional isomer bisphosphites of formulae (1a) and (2a) and the metal, and to the use thereof as a catalytically active composition in hydroformylation reactions. Said hydroformylactically active compositions comprises, in addition to the complex compounds of metal and the constitutional isomer bisphosphites of formulae (1a) and (2a), non-bound bisphosphites of the constitutional isomer bisphosphites of formulae (1a) and (2a) and at least one additional component.
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: November 22, 2016
    Assignee: Evonik Degussa GmbH
    Inventors: Andrea Christiansen, Robert Franke, Dirk Fridag, Dieter Hess, Katrin Marie Dyballa, Bernd Hannebauer
  • Patent number: 9499464
    Abstract: Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic is visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
    Type: Grant
    Filed: October 19, 2012
    Date of Patent: November 22, 2016
    Assignee: BIKAM PHARMACEUTICALS, INC.
    Inventors: David S. Garvey, Gregory J. Larosa, Jeremy R. Greenwood, Leah L. Frye, Tan Quach, Jamie B. Cote, Judd Berman
  • Patent number: 9499465
    Abstract: Methods for producing bio-terephthalic acid and bio-isophthalic acid are provided. The methods comprise a cycloaddition reaction to produce bio-4-methyl-3-cyclohexene-1-carboxylic acid, and bio-3-methyl-3-cyclohexene-1-carboxylic from bio-isoprene and bio-acrylic acid. An aromatization reaction produces bio-para-toluic acid and bio-meta-toluic acid from the bio-4-methyl-3-cyclohexene-1-carboxylic acid, and bio-3-methyl-3-cyclohexene-1-carboxylic. An oxidation reaction produces the bio-terephthalic acid and iso-phthalic acid from the bio-para-toluic acid and bio-meta-toluic acid.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: November 22, 2016
    Assignee: Board of Trustees of Michigan State University
    Inventor: John W. Frost
  • Patent number: 9499466
    Abstract: The claimed invention provides a novel compound not having been studied before, that is, a diene carboxylate anion that contains a specific structure, and a salt thereof. The claimed invention further provides a diene carboxylate anion and a salt thereof, especially a metal salt thereof, which are easily soluble in general organic solvents, reactive diluents, and resins, may be in a liquid state at normal temperature depending on the structure, and have high polymerizability. Polymerization/curing of these produces a resin to which many ionic bonds and a metal are introduced, providing various properties such as hardness, scratch resistance, anti-fingerprint property, gas-barrier property, water vapor barrier property, oxygen absorption property, ultraviolet protection, infrared protection, color development and coloring, high refractive index, adhesion, various catalytic abilities, fluorescence ability and light-emitting ability, optical amplification, dispersibility, and antistatic properties.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: November 22, 2016
    Assignee: NIPPON SHOKUBAI CO., LTD.
    Inventor: Tomomasa Kaneko
  • Patent number: 9499467
    Abstract: There is provided novel fluoro-substituted compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: November 22, 2016
    Assignee: CALDAN THERAPEUTICS LIMITED
    Inventors: Trond Ulven, Elisabeth Christiansen
  • Patent number: 9499468
    Abstract: Provided is a simple, selective and efficient method for producing 4-alkyl-3-methylenebutyl carboxylates such as 7-methyl-3-methylene-7-octenyl propionate. More specifically provided is a method for producing a 4-alkyl-3-methylenebutyl carboxylate compound, the method comprising a diacyloxylation step of subjecting a 4-halo-2-halomethyl-1-butene compound (6) to diacyloxylation to obtain a 3-acyloxymethyl-3-butenyl carboxylate compound (3), and a coupling step of subjecting the 3-acyloxymethyl-3-butenyl carboxylate compound (3) to a coupling reaction with an organometallic reagent (4) to obtain the 4-alkyl-3-methylenebutyl carboxylate compound (5).
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: November 22, 2016
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Takeshi Kinsho, Naoki Ishibashi, Yusuke Nagae
  • Patent number: 9499469
    Abstract: Provided is a method for producing an industrially useful ketomalonic acid compound such as ketomalinic acid diesters, or a hydrate thereof, by a method more favorable from an economic and environmental standpoint and from a safety standpoint. The present invention relates to a method involving reacting a malonic acid compound represented by general formula (1) (in the formula, The each Rs indicate an alkyl group, a cycloalkyl group, etc.) with chlorine dioxide to produce a ketomalonic acid compound represented by the general formula (2) (in the formula, R has the same meaning as above), or a hydrate thereof.
    Type: Grant
    Filed: July 3, 2014
    Date of Patent: November 22, 2016
    Assignee: IHARA CHEMICAL INDUSTRY CO., LTD.
    Inventors: Shinki Tani, Minekazu Koga, Izumi Matsumoto
  • Patent number: 9499470
    Abstract: Process for preparing methyl acetate by the carbonylation of dimethyl ether with carbon monoxide in the presence of hydrogen and a zeolite catalyst. In a first step, the carbonylation is conducted with a carbon monoxide to hydrogen molar ratio of at least 1 and, in a second and subsequent step, the carbonylation is conducted with a hydrogen to carbon monoxide molar ratio of greater than 1.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: November 22, 2016
    Assignee: BP CHEMICALS LIMITED
    Inventors: Evert Jan Ditzel, Bogdan Costin Gagea, John Glenn Sunley
  • Patent number: 9499471
    Abstract: The present invention relates to a compound of formula (I) as defined herein.
    Type: Grant
    Filed: September 10, 2012
    Date of Patent: November 22, 2016
    Assignee: Medizinische Hochschule Hannover
    Inventors: Dietmar Manstein, Matthias Preller, Marcus Furch, Markus Kalesse, Nina Diaz-Gomez
  • Patent number: 9499472
    Abstract: The compounds of the invention are inhibitors of excitatory amino acid transporters (EAAT) that penetrate the blood-brain barrier to access the central nervous system. The compounds of the invention follow the structural formula: or a salt, ester or prodrug thereof, wherein X is a halogen, such as fluorine, or a radionuclide, such as fluorine-18. The compounds and methods described herein can be used for the treatment of, e.g., neurodegenerative disorders (e.g., amyotrophic lateral sclerosis), ischemia, spinal cord injury, and traumatic brain injury in a patient (e.g., a human). The invention further provides compounds and methods for the synthesis and use of radiographic tracers to diagnose and follow the progression of such disorders.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: November 22, 2016
    Assignee: THE UNIVERSITY OF MONTANA
    Inventors: John M. Gerdes, Richard J. Bridges, Syed K. Ahmed, Sarjubhai Patel
  • Patent number: 9499473
    Abstract: A method for producing nitrous acid ester in which nitric oxide, oxygen, and an alcohol are reacted, thereby generating nitrous acid ester includes a step of generating nitrous acid ester by supplying a bottom liquid from a bottom part of the reaction column, and nitric oxide and/or carbon monoxide, a step of supplying nitrous acid ester to the reaction column; a step of supplying a reaction liquid containing water, nitric acid, and the alcohol to a nitric acid condensing column from the reactor; and a step of separating a low-boiling point component by distillation from the reaction liquid under control of a concentration of the alcohol in a condensed liquid being generated at a bottom part of the nitric acid condensing column to be less than 4.0% by weight so as to introduce the condensed liquid into the reactor from the nitric acid condensing column.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: November 22, 2016
    Assignee: UBE Industries, Ltd.
    Inventors: Syuji Tanaka, Hirofumi Il, Akira Hino, Yuya Fukui, Satoshi Ueda
  • Patent number: 9499474
    Abstract: The invention relates to a process for producing compounds containing at least one arylamino group by means of a coupling reaction of an amino compound with an aryl compound, using a strong base.
    Type: Grant
    Filed: October 19, 2012
    Date of Patent: November 22, 2016
    Assignee: Merck Patent GmbH
    Inventors: Oliver Kaufhold, Hubert Spreitzer, Stefan Riedmueller
  • Patent number: 9499475
    Abstract: Provided is an improved process for the preparation of arformoterol L-(+)-tartrate, and more specifically provided is a novel process for the preparation of arformoterol L-(+)-tartrate via arformoterol D-(?)-tartrate.
    Type: Grant
    Filed: May 15, 2014
    Date of Patent: November 22, 2016
    Assignee: Glenmark Pharmaceuticals Limited
    Inventors: Shekhar Bhaskar Bhirud, Suresh Mahadev Kadam, Sachin Baban Gavhane, Shailesh Shrirang Pawase, Aniket Ashokrao Deshpande, Anil Subhash Bhujbal
  • Patent number: 9499476
    Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like. Processes for making the compound of formula (I), as well as related intermediates, are disclosed.
    Type: Grant
    Filed: April 22, 2015
    Date of Patent: November 22, 2016
    Assignee: SUNOVION PHARMACEUTICALS INC.
    Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
  • Patent number: 9499477
    Abstract: Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 21, 2015
    Date of Patent: November 22, 2016
    Assignees: TOYAMA CHEMICAL CO., LTD., TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Hajime Takashima, Risa Tsuruta, Tetsuya Yabuuchi, Yusuke Oka, Hiroki Urabe, Yoichiro Suga, Masato Takahashi, Fumito Uneuchi, Hironori Kotsubo, Muneo Shoji, Yasuko Kawaguchi
  • Patent number: 9499478
    Abstract: Provided herein, inter alia, are, methods of using esters of bimatoprost with the Formula (I):
    Type: Grant
    Filed: September 16, 2014
    Date of Patent: November 22, 2016
    Assignee: ALLERGAN, INC.
    Inventors: David F. Woodward, Jenny W. Wang, Neil J. Poloso, Todd S. Gac, Robert M. Burk, Michael E. Garst
  • Patent number: 9499479
    Abstract: This invention provides a compound having the structure: wherein R1 is H, halogen, —NR5R6, —NR5—C(?O)—R6, —NH—C(?O)—OR7, —OR7, —NO2, —CN, —SR7, —SO2R7, —CO2R7, CF3, —SOR7, —POR7, —C(?S)R7, —C(?O)—NR5R6, —CH2—C(?O)—NR5R6, —C(?NR5)R6, —P(?O)(OR5)(OR6), —P(OR5)(OR6), —C(?S)R7, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, heteroaryl, or heterocyclyl, wherein R5, R6, and R7 and are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; m is an integer from 0 to 2; R2 and R3 are each, independently, H, halogen, —NH2, —CX3, —C(?O)OR8, C(?O)R8, —C(?O)NR9R10, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, heteroalkyl, aryl, heteroaryl, or heterocyclyl; wherein X is Cl, Br, or F; R8, R9 and R10 are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; Q is —Ar1—Z— or —Z—Ar1—Z—, wherein Ar1 is aryl or heteroaryl; and each occurrence of Z is independently present or
    Type: Grant
    Filed: October 3, 2012
    Date of Patent: November 22, 2016
    Assignees: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Ronald Breslow, Paul A. Marks
  • Patent number: 9499480
    Abstract: The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease.
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: November 22, 2016
    Assignee: BHI Limited Partnership
    Inventors: Xianqi Kong, Mohamed Atfani, Benoit Bachand, Abderrahim Bouzide, Stephane Ciblat, Sophie Levesque, David Migneault, Isabelle Valade, Xinfu Wu, Daniel Delorme
  • Patent number: 9499481
    Abstract: The invention relates to a method for preparing lactames, according to which a photonitrosation of a cycloalkane is carried out using nitrosyl chloride (NOCI). According to the invention, said photonitrosation is carried out by means of LEDs emitting a monochromatic light. The method according to the invention can also include a step comprising Beckmann transposition/dechlorination of the oxime hydrochloride generated during said phonitrosation, preferably carried out in a glass microreactor.
    Type: Grant
    Filed: April 14, 2014
    Date of Patent: November 22, 2016
    Assignee: ARKEMA FRANCE
    Inventor: Thierry Aubert
  • Patent number: 9499482
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are melanin concentrating hormone receptor-1 (MCHR1) antagonists which may be used as medicaments.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: November 22, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: William N. Washburn, Murugaiah Andappan Murugaiah Subbaiah, Saleem Ahmad
  • Patent number: 9499483
    Abstract: The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (I) [wherein R1 represents a methyl group or a trifluoromethyl group, R2 represents a hydrogen atom or a C1-C3 alkoxy group, and n represents an integer selected from 1 to 3] into its atropisomers, characterized by using an optically active amine having a cinchonine skeletal formula, and a crystal of (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide.
    Type: Grant
    Filed: October 9, 2015
    Date of Patent: November 22, 2016
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Masashi Watanabe, Takahiro Okachi, Michiaki Kawahara, Hiroshi Nagasawa, Noritada Sato, Takashi Takita, Gen Hasegawa
  • Patent number: 9499484
    Abstract: The invention provides indole and indoline derivatives and slats thereof, compositions comprising them and uses thereof for the treatment of diseases and disorders.
    Type: Grant
    Filed: April 2, 2013
    Date of Patent: November 22, 2016
    Assignee: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD
    Inventors: Abraham Nudelman, Marta Weinstock-Rosin
  • Patent number: 9499485
    Abstract: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).
    Type: Grant
    Filed: August 5, 2013
    Date of Patent: November 22, 2016
    Assignee: BIOGEN MA INC.
    Inventors: Kevin Guckian, Gnanasambandam Kumaravel, Bin Ma, Lihong Sun, Zhili Xin, Lei Zhang
  • Patent number: 9499486
    Abstract: There is provided a compound of formula I, which compound has anti-inflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: November 22, 2016
    Assignees: Respivert Limited, Topivert Pharma Limited
    Inventor: Matthew Colin Thor Fyfe
  • Patent number: 9499487
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: November 22, 2016
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Patent number: 9499488
    Abstract: This invention features vitamin D receptor agonists, and their use in treating bone disorders, cardiovascular disease, hyperparathyroidism, immune disorders, proliferative disease, renal disease, and thrombosis.
    Type: Grant
    Filed: July 11, 2012
    Date of Patent: November 22, 2016
    Assignees: Beth Israel Deaconess Medical Center, Inc., The General Hospital Corporation
    Inventors: Peter M. Kang, S. Ananth Karumanchi, Santosh Khedkar, Alan Rigby, Ravi I. Thadhani
  • Patent number: 9499489
    Abstract: This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions. Typically, the pharmaceutical composition comprises a compound of formula I: Formula I, or salt, prodrug, or ester thereof wherein X, Y, and R1 and R10 to R13 are described herein.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: November 22, 2016
    Assignees: Emory University, Children's Healthcare of Atlanta, Inc.
    Inventors: Richard K. Plemper, James P. Snyder, Aiming Sun
  • Patent number: 9499490
    Abstract: The present invention provides a compound of the Formula: wherein X is selected from the group consisting of, R is selected from the group consisting of H and CH3; R1 is selected from the group consisting of H, CH3, F, Cl, OCH3, C(O)OH, C(O)NH2 or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 11, 2014
    Date of Patent: November 22, 2016
    Assignee: Eli Lilly and Company
    Inventors: Kevin Kun-Chin Liu, Yinong Xie, Liang Wu, Guoqiang Zhou
  • Patent number: 9499491
    Abstract: A process for the preparation of bromine free telmisartan in one pot starting from 2-cyano-4?-methyl biphenyl. The process uses raw materials which are readily available to yield telmisartan, its salts and derivatives thereof, which are bromine free and potentially less genotoxic, since there is no bromine atom in any of the raw materials. The process can also be carried out in multiple steps by isolation of the intermediate compounds. The intermediate compound 4-chloromethyl-2?-cyanobiphenyl can also be used for the preparation of irbesartan and other sartans.
    Type: Grant
    Filed: February 16, 2015
    Date of Patent: November 22, 2016
    Inventors: U Amarnath, U Suryakiran
  • Patent number: 9499492
    Abstract: The present invention relates to 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: November 11, 2013
    Date of Patent: November 22, 2016
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Ulrich Lücking, Dirk Kosemund, Rolf Bohlmann, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer
  • Patent number: 9499493
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: September 22, 2015
    Date of Patent: November 22, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 9499494
    Abstract: The present invention relates to the identification of inventive pyrimidine-2,4,6-triones (PYT compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the inventive PYT compounds.
    Type: Grant
    Filed: October 4, 2013
    Date of Patent: November 22, 2016
    Assignee: Northwestern University
    Inventors: Donald R. Kirsch, Radhia Benmohamed, Anthony C. Arvanites, Richard I. Morimoto, Guoyao Xia, Richard B. Silverman
  • Patent number: 9499495
    Abstract: The present application provides novel quinazolines and azaquinazolines and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in for co-regulating RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways by administering a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, T and R4, and R6 to R8? are defined herein, to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment/the disease is cancer.
    Type: Grant
    Filed: April 11, 2014
    Date of Patent: November 22, 2016
    Assignee: Asana Biosciences, LLC
    Inventors: Scott K. Thompson, Roger A. Smith, Sanjeeva Reddy, Tyler M. John, Vijay Kumar Nyavanandi, Hosahalli Subramanya, Vijay Potluri, Sunil Kumar Panigrahi, Prabhakara Rao Nadipalli, Saumitra Sengupta
  • Patent number: 9499496
    Abstract: Described herein are compounds, pharmaceutical compositions and methods for treating a respiratory syncytial virus infection in a subject, or for inhibiting replication of respiratory syncytial virus.
    Type: Grant
    Filed: June 5, 2013
    Date of Patent: November 22, 2016
    Assignees: University of Kansas, Southern Research Institute
    Inventors: Jennifer E. Golden, Jeffrey Aube, Denise S. Simpson, Daniel P. Flaherty, Daljit S. Matharu, William E. Severson, Lynn Rasmussen
  • Patent number: 9499497
    Abstract: The present invention relates to compounds useful as inhibitors of indoleamine 2,3-dioxygenase (IDO). The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications. The compounds of this invention have formula I-A: wherein the variables are as defined herein.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: November 22, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Boyall, Christopher Davis, James Dodd, Simon Everitt, Andrew Miller, Peter Weber, James Westcott, Stephen Young, Luca Settimo
  • Patent number: 9499498
    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 which is preferably an acyclic carbonate, and a mixture B of bases comprising at least two basic metal compounds B1 and B2 individually selected from the group consisting of hydrides, amides, alkoxides, and arylalkoxides of metals, wherein the metal in B1 is not the same as the metal in B2.
    Type: Grant
    Filed: February 28, 2014
    Date of Patent: November 22, 2016
    Assignee: ALLNEX IP S.À.R.L.
    Inventors: William Jacobs, III, Lawrence A. Flood
  • Patent number: 9499499
    Abstract: The invention relates to new salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: November 22, 2016
    Assignee: Novartis AG
    Inventors: Erwin Marti, Hans Rudolf Oswald, Peter Buehlmayer, Wolfgang Marterer
  • Patent number: 9499501
    Abstract: The present invention belongs to the technical field of agricultural fungicides and discloses a 2-mercaptobenzothiazole manganese zinc, preparation method therefor and application thereof. The chemical structure of the 2-mercaptobenzothiazole manganese zinc is shown as the above formula. Wherein m, n and n? are positive integers, m=2(n+n?), n?n?, n:n?=1:1˜9:1. Materials are prepared according to the stoichiometric ratio of the target products; 2-mercaptobenzothiazole is dissolved in sodium hydroxide solution. The aqueous solution of water-soluble manganese salts and water-soluble zinc salts solution are successively added to 2-mercaptobenzothiazole sodium solution under stirring, followed by stirring for mixing well, then the solution being allowed to stand, filtered and washed with water to obtain filter cake, and then dried in vacuum to obtain 2-mercaptobenzothiazole manganese zinc. The present 2-mercaptobenzothiazole manganese zinc may be used as an agricultural fungicide.
    Type: Grant
    Filed: November 30, 2013
    Date of Patent: November 22, 2016
    Assignee: HENAN XINXIANG ACADEMY OF AGRICULTURE SCIENCES
    Inventors: Zhenjun Wang, Xu Zhang, Limin Wang, Hongyan Liu, Senxiang Cheng, Mengjiao Li