Patents Issued in June 13, 2017
  • Patent number: 9676689
    Abstract: A multistage tubular reaction system and method for preparing methylol derivatives of an aldehyde includes a tubular reaction system with a plurality of successive reactor stages comprising a plurality of jacketed reaction tubes provided with a cooling system adapted to control flow of a cooling medium through said jacketed reaction tubes. The cooling medium flow is controlled independently in different stages in response to temperature measurements in the reaction system to regulate temperature. In order to further reduce temperature spikes and byproduct generation, aldehyde is stepwise added to the production stream at a plurality of feed ports proximate to reaction tubes equipped with tube inserts to enhance mixing and heat transfer.
    Type: Grant
    Filed: July 23, 2014
    Date of Patent: June 13, 2017
    Assignee: OXEA BISHOP LLC
    Inventors: Michael J. Stone, Howard W. Brooks, Heinz Strutz, Donald K. Raff, Guido D. Frey, Norman Nowotny, Marcos L. Schroeder, Fred Gaytan, Tracy Kevin Hunt, William E. Slinkard
  • Patent number: 9676690
    Abstract: Described herein are high yield methods for making magnolol derivatives, together with novel intermediates and uses thereof.
    Type: Grant
    Filed: January 23, 2013
    Date of Patent: June 13, 2017
    Assignee: Colgate-Palmolive Company
    Inventors: Basi V. Subba Reddy, Ravi Subramanyam, Shashank Potnis, Jhillu Singh Yadav
  • Patent number: 9676691
    Abstract: A method is described for producing a compound having the formula (I) or an admixture comprising a compound having the formula (I), having the following steps: dissolving an indanone having the formula (II) in a solvent or in an admixture which contains a solvent, the solvent being selected from the group of solvents which form an azeotrope with water, converting the indanone having the formula (II) with an aromatic aldehyde having the formula (III) in the presence of at least one organic base, according to the drawing: where R1 and R2 independently of each other signify hydrogen or a branched or unbranched alkyl group having from 1 to 12 carbon atoms and where R3, R4, R5, R6, R7, R8, R9, R10 and R11 independently of each other signify hydrogen, hydroxy or a branched or unbranched alkyl or alkoxy group having from 1 to 12 carbon atoms and removing water formed from the reaction admixture during the conversion.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: June 13, 2017
    Assignee: SYMRISE AG
    Inventors: Oskar Koch, Dietmar Schatkowski, William Johncock, Christel Jahnke, Karl-Georg Fahlbusch
  • Patent number: 9676692
    Abstract: There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C1-C6 alcohol and an aprotic polar solvent in the presence of a base and water.
    Type: Grant
    Filed: December 29, 2014
    Date of Patent: June 13, 2017
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Manabu Yaosaka, Tomohisa Utsunomiya, Yuji Moriyama, Tomohiro Matsumoto, Kazutaka Matoba
  • Patent number: 9676693
    Abstract: This disclosure provides, molecular metal catalysts supported by sterically bulky ?-diketonate (acac) ligands. Disclosed herein are bulky ?-diketonate ligands, methods of making bulky ?-diketonate ligands, and methods of making metal catalysts supported by sterically bulky ?-diketonate (acac) ligands.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: June 13, 2017
    Inventor: Michael Pesek Marshak
  • Patent number: 9676694
    Abstract: A process for producing acetic acid is disclosed in which the water concentration is controlled in the side stream between two columns. Controlling the water concentration by the liquid light phase recycle controls the hydrogen iodide concentration in the side stream to be less than 50 wppm.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: June 13, 2017
    Assignee: CELANESE INTERNATIONAL CORPORATION
    Inventors: Ronald D. Shaver, Yaw-Hwa Liu, Mark O. Scates
  • Patent number: 9676695
    Abstract: A method is disclosed of coupling and integrating natural gas recovery and separation along with chemical conversion. The method can comprise extracting at least one natural gas component. Non-limiting examples of the extracted component include ethane, propane, butanes, and pentanes. The method can also comprise contacting a natural gas stream with a catalyst under conditions that selectively convert at least one component into at least one product, such as ethylene, acetic acid, polyethylene, vinyl acetate, ethylene vinyl acetate, ethylene oxide, ethylene glycol, and their derivatives, propylene, polypropylene, propylene oxide, propylene glycol, acrylates, acrolein, acrylic acid, butenes, butadiene, methacrolein, methacrylic acid, methacrylates, and their derivatives, which can then be separated from the remaining components.
    Type: Grant
    Filed: February 29, 2012
    Date of Patent: June 13, 2017
    Inventors: Mark Allen Nunley, Madan Mohan Bhasin, William George Etzkorn, George Ernest Keller, II, Parvez H. Wadia
  • Patent number: 9676696
    Abstract: Personal care compositions containing an active selected from the group consisting of phlorogine, phlorgine BG, deoxyArbutin, sucrose dilaurate, bakuchiol, pyrenoine, millet, arlatone dioic acid, cinnamic acid, ferulic acid, achromaxyl, methyl nicotinamide, oil soluble licorice extract, folic acid, undecylenic acid, zinc undecylenate, L-tryptophan, thiamine HCl, hexylresorcinol, lipidami red vine, dragosine, methyl gentisate, inositol, symdiol 68, laminaine, their salts, their derivatives, their precursors, and/or combinations thereof. Methods for regulating the condition of mammalian keratinous tissue by topically applying the personal care compositions are also provided.
    Type: Grant
    Filed: January 25, 2010
    Date of Patent: June 13, 2017
    Assignee: The Procter & Gamble Company
    Inventor: Tomohiro Hakozaki
  • Patent number: 9676697
    Abstract: The present invention relates to the field of converting carbohydrates into levulinic acid, a platform chemical for many chemical end products. More specifically the invention relates to a method for converting carbohydrates such as mono-, di- or polysaccharides, obtained from for example biomass production into a suitable levulinic acid ester in the presence of a zeolite or zeotype catalyst and a suitable alcohol, and the ester may be further converted into levulinic acid if desired.
    Type: Grant
    Filed: February 23, 2016
    Date of Patent: June 13, 2017
    Assignee: DANMARKS TEKNISKE UNIVERSITET
    Inventors: Shunmugavel Saravanamurugan, Anders Riisager
  • Patent number: 9676698
    Abstract: The present invention relates to methods of producing ingenol-3-angelate (I) from ingenol (II). Furthermore, the invention relates to intermediates useful for the synthesis of ingenol-3-angelate (I) from ingenol (II) and to methods of producing said intermediates.
    Type: Grant
    Filed: June 9, 2016
    Date of Patent: June 13, 2017
    Assignee: LEO Laboratories Limited
    Inventors: Thomas Hogberg, Gunnar Grue-Sorensen, Xifu Liang, Anne Marie Horneman, Anders Klarskov Petersen
  • Patent number: 9676699
    Abstract: A process for producing methyl methacrylate, the process comprising contacting reactants comprising methacrolein, methanol and an oxygen-containing gas, under reaction conditions in the presence of a solid catalyst comprising palladium, bismuth and at least one third element X, where X is selected from the group consisting of P, S, Sc, V, Ga, Se, Y, Nb, Mo, La, Ce, and Nd, wherein the solid catalyst further comprises a support selected from at least one member of the group consisting of silica, alumina, calcium carbonate, active carbon, zinc oxide, titanium oxide and magnesium oxide.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: June 13, 2017
    Assignee: Rohm and Haas Company
    Inventors: Kirk W. Limbach, Dmitri A. Kraptchetov, Christopher D. Frick
  • Patent number: 9676700
    Abstract: The present invention is directed to methods for preparing a fluorosulfonate ester or a salt thereof, through a reaction of a dissolved sulfonyl fluoride (RFSO2F) with alkoxide anion (RO?) optionally in the presence of an aprotic base (B), where RF is fluorine or a C1-C8 perfluoroalkyl group, and R is a primary alkyl or alkoxyalkyl. Alkoxide anion (RO?) can be generated from a precursor such as an alcohol or silyl ester.
    Type: Grant
    Filed: February 11, 2014
    Date of Patent: June 13, 2017
    Assignee: TRINAPCO, INC.
    Inventor: Martin Reid Johnson
  • Patent number: 9676701
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.
    Type: Grant
    Filed: March 6, 2015
    Date of Patent: June 13, 2017
    Assignee: ORYZON GENOMICS, S.A.
    Inventors: Matthew Colin Thor Fyfe, Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Marc Martinell Pedemonte, Maria de los Angeles Estiarte-Martinez, Nuria Valls Vidal
  • Patent number: 9676702
    Abstract: The invention relates to novel methods for synthesizing a synthon for ?,?-dihydroxyisoleucine 1 (CAS No. 55399-94-5] as building block for the synthesis of amatoxins, and for novel methods for synthesizing amatoxins using such building block.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: June 13, 2017
    Assignee: Heidelberg Pharma GmbH
    Inventors: Christian Lutz, Christoph Mueller, Werner Simon
  • Patent number: 9676703
    Abstract: An object is to provide a novel production method suitable for industrial production of a 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative and a synthetic intermediate for the method.
    Type: Grant
    Filed: August 8, 2014
    Date of Patent: June 13, 2017
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Kazuhiro Kudou, Masato Nagatsuka
  • Patent number: 9676704
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: June 13, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Paul Renee LePlae, Jr., James E. Hunter, Gerald B. Watson, William C. Lo, John Herbert
  • Patent number: 9676705
    Abstract: A compound of the formula SbxFe1Oy (I) in which x varies from 0.4 to 1 inclusive and y varies from 1.6 to 4 inclusive, may be used as a catalyst for catalyzing the ammoxidation reaction of an alcohol of following formula (II) CH2?C(R1)—CH2—OH (II) in which R1 represents a hydrogen atom or a methyl radical, to give nitrile of following formula (III) CH2?C(R1)—C?N (III) in which R1 has the same meaning as in above formula (II), the said reaction being carried out in the gas phase, the said gas phase comprising at least oxygen and ammonia. The present invention also relates to the process for the ammoxidation of an alcohol of formula (II) employing a compound of formula (I) as catalyst.
    Type: Grant
    Filed: April 16, 2014
    Date of Patent: June 13, 2017
    Assignees: ECOLE CENTRALE DE LILLE, UNIVERSITE DES SCIENCES ET TECHNOLOGIES D
    Inventors: Sebastien Paul, Benjamin Katryniok, Franck Dumeignil, Carsten Liebig, Wolfgang Holderich, Cyrille Guillon
  • Patent number: 9676706
    Abstract: The invention provides a process for making compounds according to Formula I: where R1, R1a, R2, R2a, R3 and R3a are defined as set forth in the specification. Formula I compounds are useful as chelants and stabilizers of cations in aqueous media and the invention therefore provides a method for using the compounds in the treatment of subterranean formations, such as in acidizing operations.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: June 13, 2017
    Assignee: Halliburton Energy Services, Inc.
    Inventors: Antonio Recio, III, Enrique Antonio Reyes
  • Patent number: 9676707
    Abstract: A total green, eco-friendly process for the synthesis of new acceptor molecule [6,6]-phenyl-C61-butyric acid pentyl ester (PC61BP) in high yields is carried under aerobic conditions showing better performance as acceptor in organic solar cells. More importantly this process causes the low cost synthesis of PC61BP in good yield without involving harmful and costly catalysts or chemicals.
    Type: Grant
    Filed: February 18, 2016
    Date of Patent: June 13, 2017
    Assignee: Council of Scientific & Industrial Research
    Inventors: Rachana Kumar, Samya Naqvi, Neha Gupta, Suresh Chand
  • Patent number: 9676708
    Abstract: Protected HNO donors designed to undergo non-enzymatic release at neutral pH via an intramolecular cyclization-elimination are disclosed. The rate of cyclization, and therefore HNO release, can be controlled by substituents and chain length. Thus, biologically useful HNO donors having tunable HNO release rates are provided.
    Type: Grant
    Filed: October 30, 2013
    Date of Patent: June 13, 2017
    Assignee: The Johns Hopkins University
    Inventors: John P. Toscano, Art D. Sutton
  • Patent number: 9676709
    Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.
    Type: Grant
    Filed: January 19, 2017
    Date of Patent: June 13, 2017
    Inventor: Thomas P. Daly
  • Patent number: 9676710
    Abstract: Industrial methods for producing arylsulfur pentafluorides are disclosed. Methods include reacting arylsulfur halotetrafluoride with hydrogen fluoride in the absence or presence of one or more additives selected from a group of fluoride salts, non-fluoride salts, and unsaturated organic compounds to form arylsulfur pentafluorides.
    Type: Grant
    Filed: August 24, 2016
    Date of Patent: June 13, 2017
    Assignee: UBE INDUSTRIES, LTD.
    Inventors: Teruo Umemoto, Norimichi Saito
  • Patent number: 9676711
    Abstract: The present invention relates to novel sulfoperoxycarboxylic acid compounds, and methods for making and using them. The sulfoperoxycarboxylic compounds of the invention are storage stable, water soluble and have low to no odor. Further, the compounds of the present invention can be formed from non-petroleum based renewable materials. The compounds of the present invention can be used as antimicrobials, and bleaching agents. The compounds of the present invention are also suitable for use as coupling agents.
    Type: Grant
    Filed: February 19, 2016
    Date of Patent: June 13, 2017
    Assignee: Ecolab USA Inc.
    Inventors: Li Junzhong, Richard Staub, David D. McSherry, Keith G. Lascotte, Steven J. Lange, Frank Everts
  • Patent number: 9676712
    Abstract: Disclosed herein are compounds of formula (I) wherein L1, L2, L3, R1, R4, R5, and R6 are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, osteoporosis, bone fracture, periodontal bone loss, orthopedic implant, alopecia, neuropathic pain, and related disorders. Pharmaceutical compositions and methods of treating conditions or disorders are also described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: June 13, 2017
    Assignee: CAYMAN CHEMICAL COMPANY, INC.
    Inventors: Stephen Douglas Barrett, Bradlee David Germain, Adam Uzieblo, Fred Lawrence Ciske, Gregory William Endres, Andriy Kornilov, Kirk M. Maxey, James Paul O'Malley, Thomas Allen Owen
  • Patent number: 9676713
    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: November 15, 2016
    Date of Patent: June 13, 2017
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Masashi Watanabe, Takahiro Okachi, Michiaki Kawahara, Hiroshi Nagasawa, Noritada Sato, Takashi Takita, Gen Hasegawa
  • Patent number: 9676714
    Abstract: Disclosed are a sulfonylindole derivative useful for the prevention or treatment of peptic ulcer, gastritis or reflux esophagitis, a method of preparing the same, and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: October 2, 2014
    Date of Patent: June 13, 2017
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: Kyung A Yu, Ji Sung Yoon, Deok Ki Eom, Yeon Im Lee, Hye Ryun Shin, Jun Hee Lee, Ha Nee Seo, Ji Duck Kim, Sang Ho Lee, Chun Ho Lee
  • Patent number: 9676715
    Abstract: Novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: June 13, 2017
    Assignee: UNIVERSITE JOSEPH FOURIER
    Inventors: Jean-Noël Denis, Marcelle Claude Jolivalt, Louis Maurin Max Maurin, Matthieu Jeanty
  • Patent number: 9676716
    Abstract: The present invention relates to thermoplastic high-Tg polycarbonates and molding materials which are distinguished by improved thermal properties and improved mechanical properties, in particular by reduced thermal expansion. The present invention furthermore relates to a process for the preparation of these polycarbonates. In particular, this invention relates to polycarbonates which the structural unit which derives from phthalimide of the formula (I) and polycarbonate compositions and molding materials therefrom as well as a process for the preparation of these polycarbonates, and the use thereof, in particular as reflectors and display substrates.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: June 13, 2017
    Assignee: Covestro Deutschland AG
    Inventors: Helmut-Werner Heuer, Rolf Wehrmann
  • Patent number: 9676717
    Abstract: Provided is an organic electroluminescence device including a pair of electrodes composed of an anode and a cathode, a light emitting layer between the electrodes and an organic layer which is adjacent to the light emitting layer between the light emitting layer and the cathode, on a substrate, and the light emitting layer contains at least one compound having a carbazole structure and the organic layer adjacent to the light emitting layer contains at least one hydrocarbon compound having a specific structure.
    Type: Grant
    Filed: December 28, 2010
    Date of Patent: June 13, 2017
    Assignee: UDC Ireland Limited
    Inventors: Tetsu Kitamura, Toru Watanabe, Toshihiro Ise
  • Patent number: 9676718
    Abstract: Piperidine compounds and pharmaceutically useful salts thereof, a pharmaceutical composition including an effective amount of the racemic or enantiomerically enriched piperidine compounds to treat gastrointestinal diseases, and a method of treating gastrointestinal diseases in a mammal are provided.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: June 13, 2017
    Assignee: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Coo-Min Chung, Hyung-Jin Jun, Jin-Sung Kim, Hiu-Ho Kim, Hye-Kyung Min, Yong-Gil Kim, Jong-Gil Choi, Hongwook Kim
  • Patent number: 9676719
    Abstract: An object of the present invention is to provide a compound having strong human S1P2 antagonistic activity in order to develop a useful medicament for therapy of a S1P2-mediated disease such as a disease resulting from vascular constriction, fibrosis and respiratory disease. The compound represented by the general formula (I), wherein all the symbols have the same meanings as described in the specification, has a halogen atom or a haloalkyl group and a phenoxy group at certain substitution sites, and thus has strong human S1P2 antagonistic activity. Therefore, the compound can be a therapeutic agent for a S1P2-mediated disease, such as a disease resulting from vascular constriction, fibrosis and respiratory disease.
    Type: Grant
    Filed: March 25, 2014
    Date of Patent: June 13, 2017
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kensuke Kusumi, Atsushi Naganawa, Kazuhiro Otsuki, Tetsuya Sekiguchi, Koji Shinozaki, Hiroshi Yamamoto, Yasuko Yamamoto
  • Patent number: 9676720
    Abstract: The present invention provides a substituted biaryl compound of general formula (I): wherein, R1, W, R2, and Z are as defined in the claims and the description, or a pharmacologically acceptable salt thereof. The compound according to the present invention has an excellent inhibition effect of pulmonary fibroblast proliferation, and is therefore useful as a therapeutic agent and/or a prophylactic agent for interstitial pneumonia and pulmonary fibrosis.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: June 13, 2017
    Assignee: UBE INDUSTRIES, LTD.
    Inventors: Nobuhiko Shibakawa, Kenji Yoneda, Tetsushi Katsube, Tomoko Kanda, Koji Ito, Kiyoshi Yamamoto, Noriaki Iwase, Shigeru Ushiyama
  • Patent number: 9676721
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: June 13, 2017
    Assignee: FORMA TM, LLC
    Inventors: Kenneth W. Bair, Alexandre J. Buckmelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
  • Patent number: 9676722
    Abstract: The present invention relates to an improved process for the preparation of Ivacaftor intermediates. The present invention is also provides industrial applicable, commercially and eco-friendly viable process for the preparation of Ivacaftor.
    Type: Grant
    Filed: August 24, 2016
    Date of Patent: June 13, 2017
    Assignee: Optimus Drugs Private Limited
    Inventors: Srinivas Reddy Desi Reddy, Dnyandev Ragho Rane, Venkata Srinivasa Rao Velivela
  • Patent number: 9676723
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: June 13, 2017
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Santhosh F. Neelamkavil, Scott D. Edmondson, Zhuyan Guo, Alan W. Hruza, Zahid Hussain, Remond Moningka, Nancy Jo Kevin
  • Patent number: 9676724
    Abstract: Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.
    Type: Grant
    Filed: October 12, 2015
    Date of Patent: June 13, 2017
    Assignee: Tianjin Hemay Oncology Pharmaceutical Co., Ltd.
    Inventors: Hesheng Zhang, Yingwei Chen, Qingchao He
  • Patent number: 9676725
    Abstract: Disclosed are a new S crystal form of ivabradine hydrochloride, and preparation method and pharmaceutical composition thereof. The S crystal form of ivabradine hydrochloride has a powder diffraction pattern having characteristic peaks at degrees two-theta positions of 8.5±0.2, 11.5±0.2, 14.6±0.2, 15.3±0.2, 16.1±0.2, 17.1±0.2, 17.4±0.2, 17.8±0.2, 18.6±0.2, 19.3±0.2, 21.6±0.2, 21.9±0.2, 27.2±0.2, and, by DSC measurement, has an endothermic crystal transformation peak as a characteristic peak at 111.6° C. and an exothermic crystal transformation peak as a characteristic peak at 136.9° C., and a melting decomposition peak as a characteristic peak at 194.9° C. The S crystal form products are easy to dry, have high purity and stability, and are convenient for long-term storage without particular temperature and humidity requirements. The preparation method thereof facilitates industrial production, and has great application value and market value.
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: June 13, 2017
    Assignee: Beijing Lunarsun Pharmaceutical Co., LTD.
    Inventors: Xiaobo Zhang, Dongdong Cui, Tianxiang Zhang
  • Patent number: 9676726
    Abstract: A process is described for the synthesis of pyrazoles having general formula (I) which comprises the steps of mixing a compound having general formula (II) and a 1,2-disubstituted hydrazine having general formula (III) to form a reaction intermediate having general formula (IV) and the reaction mixture obtained in step i), in an acid environment, cyclizes to form a pyrazole having general formula (I), according to reaction scheme 1
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: June 13, 2017
    Assignee: ISAGRO S.P.A.
    Inventors: Giovanni Meazza, Laura Sillani, Pierangelo Mereghetti, Daniele Forgia
  • Patent number: 9676727
    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: or salt, prodrug, or ester thereof wherein X, Y, and R1 and R10 to R13 are described herein.
    Type: Grant
    Filed: July 7, 2016
    Date of Patent: June 13, 2017
    Assignees: Emory University, Children's Healthcare of Atlanta, Inc.
    Inventors: Richard K. Plemper, James P. Snyder, Aiming Sun
  • Patent number: 9676728
    Abstract: The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: October 29, 2014
    Date of Patent: June 13, 2017
    Assignee: Novartis AG
    Inventors: Christopher Adams, Takeru Ehara, Keith Jendza, Nan Ji, Rajeshri Ganesh Karki, Toshio Kawanami, Nello Mainolfi, James Powers, Michael Serrano-Wu, Chun Zhang
  • Patent number: 9676729
    Abstract: The present invention relates to oxygen-comprising amine salts of HMG-CoA reductase inhibitors, to a method of producing said amine salts and to the use of said amine salts in the production of pharmaceutically acceptable salts of HMG-CoA reductase inhibitors.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: June 13, 2017
    Assignee: DSM Sinochem Pharmaceuticals Netherlands B.V.
    Inventors: Ben De Lange, Erik De Vroom
  • Patent number: 9676730
    Abstract: The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.
    Type: Grant
    Filed: July 7, 2016
    Date of Patent: June 13, 2017
    Assignees: Array BioPharma Inc., Genentech, Inc.
    Inventors: David Askin, Chong Han, Jonathan W. Lane, Travis Remarchuk, Sagar Shakya, C. Gregory Sowell, Keith L. Spencer, Peter J. Stengel
  • Patent number: 9676731
    Abstract: The present invention relates to a new synthetic intermediate, namely the compound of formula I-2 or a salt thereof. Said compound of formula I-2 or its salt can be used to prepare the compound of formula I-3 which is an important synthetic intermediate used in the preparation of macitentan.
    Type: Grant
    Filed: July 14, 2016
    Date of Patent: June 13, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Stefan Abele, Jacques-Alexis Funel, Ivan Schindelholz
  • Patent number: 9676732
    Abstract: It has been surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4), useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: June 13, 2017
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Antonio Ricci, Daniel Rueher, Eric Vieira
  • Patent number: 9676733
    Abstract: A method for obtaining solutions that contain 1,2,4-triazole-5-one (OTA) in concentrated sulphuric acid, includes using 3-amino-1,2,4-triazole (ATA) as a precursor of OTA. There is also provided a method for preparing 3-nitro-1,2,4-triazole-5-one (4) (ONTA) from the solutions.
    Type: Grant
    Filed: April 4, 2014
    Date of Patent: June 13, 2017
    Assignees: HERAKLES, EURENCO
    Inventors: Grégoire Herve, Guy Jacob, Guy Cagnon, Jean-Marc Bouchez
  • Patent number: 9676734
    Abstract: Thiol derivatives of general formula (II) have antiviral activity, particularly against influenza virus. In particular, the compound (4-(2-chloro-4-nitrophenyl)piperazin-1-yl)(4-(2-fluoro-6-methoxyphenyl)-1-methyl-1H-1,2,3-triazol-5-yl)methanone is provided. Methods of preparing the compounds are also described.
    Type: Grant
    Filed: June 6, 2016
    Date of Patent: June 13, 2017
    Assignee: VIRONOVA INFLUENZA AB
    Inventors: Mohammed Homman, Ngarita Kingi, Jan Bergman, Robert Berg
  • Patent number: 9676735
    Abstract: The invention relates to a process for the preparation of Efavirenz via an efficient transition metal catalyzed cyclization, to a device suitable to perform such process as well as to novel intermediates.
    Type: Grant
    Filed: August 27, 2015
    Date of Patent: June 13, 2017
    Assignee: Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.
    Inventors: Camille A. Correia, Kerry Gilmore, David Tyler McQuade, Peter H. Seeberger
  • Patent number: 9676736
    Abstract: A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof.
    Type: Grant
    Filed: April 15, 2013
    Date of Patent: June 13, 2017
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Fuli Zhang, Chonghao Liu, Pengcheng Qiu, Jian Chai, Qingfeng Cai
  • Patent number: 9676737
    Abstract: The present invention concerns a process for converting biomass into useful organic building blocks for the chemical industry. The process involves the use of molybdenum catalysts of the formula Aa+a(MovXxR1yR2zR3e)a*3?, which may be readily prepared from industrial molybdenum compounds.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: June 13, 2017
    Assignee: Danmarks Tekniska Universitet
    Inventors: Johannes Rytter Dethlefsen, Peter Fristrup
  • Patent number: 9676738
    Abstract: A compound, or a pharmaceutically acceptable salt thereof, having a structure of wherein Z is aryl or substituted aryl, heteroaryl, or substituted heteroaryl; X is —S—, —S(O)—, or S(O)2—; R20 and R21 are each independently H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, or halogenated alkyl; one of R22, R23, and R24 is —O— and the others of R22, R23 and R24 are independently —CH2—, or —C(R13)— wherein R13 is alkyl, alkenyl, alkynyl, trialkylsilyl group, or —(CH2)mOR15, wherein R15 is alkyl or an aryl and m is an integer in the range of 1 to 10; and R25 is H, alkyl, substituted alkyl, halogen, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, C1-C3 alkoxy, aryloxy, or —(CH2)qOR17, wherein R17 is alkyl an aryl and q is an integer in the range of 1 to 10.
    Type: Grant
    Filed: October 13, 2016
    Date of Patent: June 13, 2017
    Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, MUSC Foundation for Research Development
    Inventors: Peter Wipf, Carol A. Feghali-Bostwick