Patents Issued in April 19, 2018
  • Publication number: 20180105471
    Abstract: A CMC article may include a CMC substrate defining a major surface and a plurality of CMC reinforcing pins at least partially embedded in the CMC substrate. Each CMC reinforcing pin of the plurality of CMC reinforcing pins defines a respective long axis. The respective long axes may be oriented at an angle substantially perpendicular to the major surface of the CMC substrate. A method may include inserting a plurality of CMC reinforcing pins into a major surface of a ceramic fiber preform. Each CMC reinforcing pin of the plurality of CMC reinforcing pins defines a respective long axis. As the plurality of CMC reinforcing pins are inserted into the major surface, the respective long axes may be oriented at an angle substantially perpendicular to the major surface. The method also includes forming a matrix of material within pores of the ceramic fiber preform to form a CMC article.
    Type: Application
    Filed: September 5, 2017
    Publication date: April 19, 2018
    Inventor: Jun Shi
  • Publication number: 20180105472
    Abstract: The present invention relates to an aerogel composite and a preparation method thereof. The preparation method of the aerogel composite of the present invention comprises the following steps; preparing a hydrophobic gel (step 1); dispersing fiber in a solvent to prepare a solution (step 2); adding the hydrophobic gel above in the solution of step 2 and stirring the mixture to prepare a fiber and hydrophobic gel mixed solution (step 3); separating floc from the mixed solution of step 3 (step 4); and drying the floc (step 5). According to the preparation method of the aerogel composite of the present invention, a high performance aerogel composite having various shapes can be prepared.
    Type: Application
    Filed: May 22, 2017
    Publication date: April 19, 2018
    Inventors: Young-soo AHN, Jin-seok LEE, Chang Guk HONG, Sang Eun LEE, Bong Kwan SONG
  • Publication number: 20180105473
    Abstract: The present invention provides a high temperature and bright red ink-jet ink for ceramic decoration, its preparation method and application thereof. On the base that the existing ink-jet ink production process, ink-jet printing equipment and ink-jet printing process are not made major changes, high temperature bright red ink basic glaze powder composition, basic glaze frit powder composition, solvent composition, basic glaze powder and bright red pigment grinding method and particle size optimization, ink composition and processing methods are adjusted and optimized. Thus the performance of high temperature bright red ink can meet the requirement of the use of ink-jet printing machine, and after high temperature firing (1080° C.˜1230° C.), the surface decoration color of ceramic tile sprayed a single printed high temperature bright red is bright red, colorful, pure red, and at the superposing place with other color ink-jet printing ink, the color is bright, colorful, color gamut broad.
    Type: Application
    Filed: May 18, 2015
    Publication date: April 19, 2018
    Inventors: TONGCAN LIANG, YONGQING WANG, GUOMING YU, JIARUI OU
  • Publication number: 20180105474
    Abstract: The invention is directed to manufacturing fertilizers having commercial levels of nitrogen reacted with organic substances. The process comprises treatment of organics with acid that acidifies and heats a mix causing the hydrolysis of polymers. The acidified organic mix is injected sequentially with a nitrogen base under conditions that result in a partially neutralized melt. The sterilized and liquefied organic matter is disbursed over recycled material for production of granules in a granulator before final drying. The process is green scalable, and safe for the location of community organics processing facilities in locations without generating a nuisance to local communities. Fertilizers also provide a green, dual nitrogen-release profile when applied to crops releasing a bolus of nitrogen over one to two weeks following application followed by a continued slow or enhanced efficiency release of nitrogen over a growing season.
    Type: Application
    Filed: December 14, 2017
    Publication date: April 19, 2018
    Applicant: Anuvia Plant Nutrients Corporation
    Inventors: Jeffrey C. Burnham, Gary L. Dahms, Barry R. Jarrett, Larry S. Murphy
  • Publication number: 20180105475
    Abstract: An alternative salt nutrient mixture for plant growth, wherein one or more of the following nutrients is present as a carbonate: nitrogen (eg ammonium), potassium, calcium, magnesium, iron, manganese, boron, zinc or copper and/or one or more of the following nutrients is present as a nitrate: nitrogen (eg ammonium), potassium, calcium, magnesium, iron, manganese, boron, zinc or copper.
    Type: Application
    Filed: May 10, 2016
    Publication date: April 19, 2018
    Inventor: Peter James Keating
  • Publication number: 20180105476
    Abstract: A compost bin module for aerobic decomposition of organic matter. The module is in the form of a container comprising a free-standing portable structural frame for placement on or above the ground. It further comprises removable sidewalls, and an open top and open bottom. Each of said removable side walls insertable into the structural frame and laterally restrained thereby. The structural frame comprises at least three spaced-apart posts, at least an equal number of structural members spanning between and interconnecting the posts, each of the structural members spanning between two adjacent posts at or near their base.
    Type: Application
    Filed: March 16, 2016
    Publication date: April 19, 2018
    Inventors: Anthony Bruce WALLIS, Richard WALLIS, Grant STEVENS
  • Publication number: 20180105477
    Abstract: The present invention discloses a method for preparing optically active carbonyl compound, comprising the following steps: under the catalysis of chiral amine salt and transition metal catalysts, with hydrogen and catalytic amount of dihydropyridine compound as hydrogen source, use ?, ?-unsaturated aldehydes or ?, ?-unsaturated troponoid compounds to conduct asymmetric catalytic reaction to obtain the optically active carbonyl compound. This method comes in moderate reaction condition, simple operation, and catalytic amount of dihydropyridine compounds usage, the target product is easy to be separated and purified from the reaction system, and the metal catalyst can be recycled, it is economical.
    Type: Application
    Filed: November 29, 2016
    Publication date: April 19, 2018
    Inventors: YOUGUI ZHOU, MING YU, JINTAO YUAN, LEI ZHAO, XIANDONG ZHU, GUANGXIONG YU, WEIWEI SU, WEIKANG SHAO, XINGXING SHI, YIN ZHANG, MING FENG, ZHIRONG CHEN, HAORAN LI, YUHONG ZHANG
  • Publication number: 20180105478
    Abstract: Disclosed herein are catalyst systems containing an alpha-diimine nickel halide complex, a chemically-treated solid oxide, and an optional co-catalyst. These catalyst systems can be used to reduce the light oligomer content of propylene oligomer streams, for instance, by oligomerizing olefin feedstocks containing C6 to C27 propylene oligomers to produce oligomer compositions having higher molecular weights.
    Type: Application
    Filed: October 19, 2016
    Publication date: April 19, 2018
    Inventors: Graham R. Lief, Uriah J. Kilgore, Eric J. Haschke
  • Publication number: 20180105479
    Abstract: The invention relates to a process for producing butadiene from n-butenes which comprises the steps of: A) providing a vaporous n-butenes-comprising input gas stream a1 by evaporating a liquid n-butenes-comprising stream a0; B) introducing the vaporous n-butenes-comprising input gas stream a1 and an at least oxygenous gas into at least one oxidative dehydrogenation zone and oxidatively dehydrogenating n-butenes to butadiene to obtain a product gas stream b comprising butadiene, unconverted n-butenes, steam, oxygen, low-boiling hydrocarbons, high-boiling secondary components, possibly carbon oxides and possibly inert gases, Ca) chilling the product gas stream b by contacting with a cooling medium comprising an organic solvent in at least one chilling zone, the cooling medium being at least partially recycled into the chilling zone, Cb) compressing the chilled product gas stream b which is possibly depleted of high-boiling secondary components in at least one compression stage to obtain at least one aqueous c
    Type: Application
    Filed: March 23, 2016
    Publication date: April 19, 2018
    Inventors: Jan Pablo JOSCH, Ragavendra Prasad BALEGEDDE RAMACHANDRAN, Christian Walsdorff, Regina BENFER, Anton WELLENHOFER, Ulrike WENNING, Heinz BOELT, Hendrik REYNEKE, Christine TOEGEL
  • Publication number: 20180105480
    Abstract: Provided are methods for the production of isophthalic acid (IP A) and derivatives thereof. The methods are based on the addition of beta propiolactone to furfural or a derivative thereof. Provided are cost effective routes to biobased IP A and derivatives thereof, including terephthalic acid.
    Type: Application
    Filed: April 22, 2016
    Publication date: April 19, 2018
    Inventors: Jay J Farmer, Sadesh H. Sookraj
  • Publication number: 20180105481
    Abstract: A novel method for the catalytic selective decarboxylation of a starting material to produce an organic acid is disclosed. According to at least one embodiment, the method may include placing a reaction mixture into a reaction vessel, the reaction mixture including a solvent, a starting material, and a catalyst, subjecting the reaction mixture to a predetermined pressure and temperature, and allowing the reaction to continue for 1-3 hours. The starting material may be at least one of a dicarboxylic acid, a tricarboxylic acid, and an anhydride of a dicarboxylic or tricarboxylic acid. As an exemplary embodiment, itaconic acid may be a starting material and the organic acid may be methacrylic acid. The predetermined temperature may be 250° C. or less, and the reaction pressure may be less than 425 psi. Further, a polymerization inhibitor may be used.
    Type: Application
    Filed: October 3, 2017
    Publication date: April 19, 2018
    Inventors: Bryan R. Moser, James C. Lansing, Rex E. Murray
  • Publication number: 20180105482
    Abstract: The present invention relates to the use of compounds which are capable of attenuating skin irritation when they are applied to the skin. Skin irritation can be caused, inter alia, by ingredients of cosmetic or pharmaceutical compositions and/or environmental irritants. In particular, the present invention relates to compounds having the property of antagonizing the activation of the transient receptor potential (TRP) ankyrin 1 (TRPA1) ion channel and the use of said compounds as soothing agents. Such compounds can be used in many fields, particularly in personal-care products, cosmetics, textile and packaging products, pharmaceutical compositions, medical devices, and foodstuffs. The present invention further relates to products and/or pharmaceutical compositions containing said compounds. The present invention also relates to the use of the compounds described herein for the modulation of the taste of a food product.
    Type: Application
    Filed: August 2, 2016
    Publication date: April 19, 2018
    Applicant: B.R.A.I.N. Biotechnology Research and Information Network AG
    Inventors: Michael KROHN, Dirk SOMBROEK
  • Publication number: 20180105483
    Abstract: A method for producing a (meth) acrylate comprises transesterification reaction of an alcohol and a monofunctional (meth) acrylate with catalysts in combination being cyclic tertiary amines having an azabicyclo structure and compounds containing zinc, separating a solid that contains the catalysts from a reaction product containing a (meth) acrylate, and producing a (meth) acrylate by transesterification reaction of an alcohol and a monofunctional (meth) acrylate, while using the recovered solid catalyst.
    Type: Application
    Filed: March 3, 2016
    Publication date: April 19, 2018
    Applicant: TOAGOSEI CO., LTD.
    Inventor: Naoki HASHIMOTO
  • Publication number: 20180105484
    Abstract: Polyol esters of metathesized fatty acids are generally disclosed herein. Methods of using such compounds, for example, as cleaning agents, solvents, and coalescents for paints and coatings, are also disclosed.
    Type: Application
    Filed: September 21, 2017
    Publication date: April 19, 2018
    Applicant: Elevance Renewable Sciences, Inc.
    Inventor: Paul A. Bertin
  • Publication number: 20180105485
    Abstract: Cyclic vinylogous amides of Formula I are disclosed The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.
    Type: Application
    Filed: December 14, 2017
    Publication date: April 19, 2018
    Applicant: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI
    Inventors: Ming-Ming ZHOU, Michael OHLMEYER, Adam VINCEK, Nilesh ZAWARE
  • Publication number: 20180105486
    Abstract: Process for making a chelating agent according to the general formula (I), R1—CH(COOX1)—N(CH2COOX1)2 wherein R1 is selected from hydrogen, C1-C4-alkyl, phenyl, benzyl, CH2OH, and CH2CH2COOX1, X1 is (M?H1-?), M being selected from alkali metal, x is in the range of from 0.6 to 1, said process comprising the following steps: (a) providing a solid, a slurry or a solution of a compound according to general formula (II a) R1—CH(COOX2)—N(CH2CN)2 wherein X2 is (MyH1-y), M being selected from alkali metal, y is in the range of from zero to 1, (b) contacting said solid or slurry or solution with an aqueous solution of alkali metal hydroxide, wherein the molar ratio of alkali metal ions to nitrile groups is in the range of from 0.6:1 to 0.95:1, (c) reacting said compound according to general formula (II a) with said alkali metal hydroxide.
    Type: Application
    Filed: May 3, 2016
    Publication date: April 19, 2018
    Applicant: BASF SE
    Inventors: Armin STAMM, Thomas SCHMIDT, Christopher ORR, Jeremy MANNING
  • Publication number: 20180105487
    Abstract: The present invention relates to a process for preparing Lomitapide or its pharmaceutically acceptable salt thereof having high purity with acceptable levels of impurities.
    Type: Application
    Filed: November 4, 2015
    Publication date: April 19, 2018
    Inventors: BANDI PARTHASARADHI REDDY, KURA RATHNAKAR REDDY, BANDI VAMSI KRISHNA, JAMBULA MUKUNDA REDDY
  • Publication number: 20180105488
    Abstract: The present invention provides a novel cyanate ester compound which has excellent solvent solubility and from which a hardened product having a low coefficiency of thermal expansion and excellent flame retardancy and heat resistance is obtained. The present invention is a cyanate ester compound obtained by cyanating a naphthol-dihydroxynaphthalene aralkyl resin or a dihydroxynaphthalene aralkyl resin.
    Type: Application
    Filed: February 19, 2016
    Publication date: April 19, 2018
    Applicant: MITSUBISHI GAS CHEMICAL COMPANY, INC.
    Inventors: Masayuki KATAGIRI, Tatsuya SHIMA, Keita TOKUZUMI
  • Publication number: 20180105489
    Abstract: Disclosed is a method for separating, with a multi-stage distillation column, a mixture containing an active hydrogen-containing compound (A) and a compound (B) that reversibly reacts with the active hydrogen containing compound (A), the method comprising distillation-separating the active hydrogen-containing compound (A) and the compound (B) with the multi-stage distillation column in the presence of an intermediate-boiling-point inactive compound (C) that has a normal boiling point between a normal boiling point of the active hydrogen-containing compound (A) and a normal boiling point of the compound (B) and is chemically inactive for both of the (A) and the compound (B).
    Type: Application
    Filed: December 13, 2017
    Publication date: April 19, 2018
    Applicant: Asahi Kasei Kabushiki Kaisha
    Inventors: Masaaki Shinohata, Nobuhisa Miyake
  • Publication number: 20180105490
    Abstract: Disclosed is a process for preparing unsaturated malonates and/or their isomers. The process includes the step of reacting an aldehyde and a dialkyl malonate in the presence of a Lewis acid and a carboxylic acid thereby forming an unsaturated malonate.
    Type: Application
    Filed: March 11, 2016
    Publication date: April 19, 2018
    Inventors: Michael CHESKIS, Yigal BECKER
  • Publication number: 20180105491
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.
    Type: Application
    Filed: October 16, 2017
    Publication date: April 19, 2018
    Inventors: Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
  • Publication number: 20180105492
    Abstract: The invention relates to the methods for producing derivatives of 3-alkylamino-1H-indole acrylate (I) with transcription factor Nrf2-inducing activity, free radical scavenging activity and neuroprotective ability. The invention also relates to the use of the derivatives according to the invention for the treatment of diseases, the pathogenesis of which involves oxidative stress, or diseases involving the deregulation of the activity of phase II genes activated by the factor Nrf2, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, multiple sclerosis, ictus or amyotrophic lateral sclerosis.
    Type: Application
    Filed: October 15, 2015
    Publication date: April 19, 2018
    Inventors: Rafael LEON MARTINEZ, Izaskun BUENDIA ABAITUA, Elisa NAVARRO GONZALEZ DE MESA, Patrycja MICHALSKA, Isabel GAMEIRO ROS, Alicia LOPEZ VIVO, Javier EGEA MAIQUEZ, Manuela GARCIA LOPEZ, Antonio GARCIA GARCIA
  • Publication number: 20180105493
    Abstract: The present invention provides a cationic lipid which can be used for nucleic acid delivery to a cytoplasm and which is possible to solve the problem of physical stability of a lipid complex. This cationic lipid is a compound represented by the general formula (3) or a pharmaceutically acceptable salt thereof: wherein, L is an alkyl having 7-12 carbon atoms or an alkenyl having 7-12 carbon atoms, R is an alkyl having 1-2 carbon atoms, and n1 and n2 are independently an integer of 1-3.
    Type: Application
    Filed: December 14, 2017
    Publication date: April 19, 2018
    Applicants: Eisai R&D Management Co., Ltd., Sogo Pharmaceutical Co., Ltd.
    Inventors: Yuta Suzuki, Kenji Hyodo, Yohei Tanaka
  • Publication number: 20180105494
    Abstract: The present invention provides an N1-cyclic amine-N5-substituted biguanide derivative compound represented by Formula 1, a method of preparing the same and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient. The biguanide derivatives have an effect of inhibiting cancer cell proliferation, cancer metastasis and cancer recurrence by activation of AMPK, even when administered in a small dose compared with conventional drugs.
    Type: Application
    Filed: December 14, 2017
    Publication date: April 19, 2018
    Inventors: Chang Hee MIN, Yong Eun KIM, Byung Kyu OH, Ji Sun LEE, Hye Jin HEO, Ju Hoon OH, Woong CHO
  • Publication number: 20180105495
    Abstract: A new azo-type quaternary pyridinium salt (Azo-QPS) shows enhanced activity at acidic conditions (e.g., pH=5); in neutral or basic conditions, this new Azo-QPS shows a much lower level (2-50 times less) anti-bacterial activity. The use of such a “stimulus-enhance” antibiotic can response to the proliferation of bacteria directly. It helps reduce or prevent the build-up of potent antibacterial agents in the oral environment. The antibacterial properties of Azo-QPS are “activated” when the environmental pH becomes acidic; this acidic pH may be indicative of the accumulation of Streptococcus mutans, or the initiation of tooth decay.
    Type: Application
    Filed: October 3, 2017
    Publication date: April 19, 2018
    Applicant: ADA Foundation
    Inventor: Jirun Sun
  • Publication number: 20180105496
    Abstract: The invention relates to compounds of formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.
    Type: Application
    Filed: December 19, 2017
    Publication date: April 19, 2018
    Applicant: IDORSIA PHARMACEUTICALS LTD
    Inventors: Romain SIEGRIST, Bibia HEIDMANN, Simon STAMM, John GATFIELD, Olivier BEZENCON
  • Publication number: 20180105497
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: August 11, 2017
    Publication date: April 19, 2018
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kevin Wayne Kuntz
  • Publication number: 20180105498
    Abstract: Methods and compounds useful for reducing, treating, preventing, or sustaining the reduction of a metabolic disease or disorder are provided herein. Also provided herein are compositions and kits for practicing any of the methods described herein.
    Type: Application
    Filed: September 26, 2017
    Publication date: April 19, 2018
    Inventors: Michael Zemel, Antje Bruckbauer
  • Publication number: 20180105499
    Abstract: An alkyl ester of 4-(5-(bis(2-hydroxyethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butyric acid, such as ethyl 4-(5-(bis(2-hydroxyethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoate, is obtained by reacting an alkyl ester of 4-(5-amino-1-methyl-1H-benzo[d]imidazol-2-yl)butyric acid with 2-hydroxyacetaldehyde under reducing conditions.
    Type: Application
    Filed: December 18, 2017
    Publication date: April 19, 2018
    Inventors: Xing FU, Saroop Singh MATHARU
  • Publication number: 20180105500
    Abstract: The present invention provides novel inhibitors of TAK1 and methods of using such compounds to treat various diseases.
    Type: Application
    Filed: September 29, 2017
    Publication date: April 19, 2018
    Inventors: Emily Derbyshire, Timothy A. J. Haystead
  • Publication number: 20180105501
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A, Z, R1 R2, R3 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: June 1, 2016
    Publication date: April 19, 2018
    Inventors: Nicholas Ryan Deprez, Paula Louise Sharpe, Ravisekhara Pochimireddy Reddy, John Robbins Debergh
  • Publication number: 20180105502
    Abstract: The present application provides a one-pot catalytic process which involves the formation of 1,4-dibenzodiazepines from o-haloaldimines (either pre-formed or formed in situ) of formula (I) and o-haloanilines of formula (II) via a palladium catalyzed Buchwald-Hartwig reaction and a cyclization sequence, to afford the 1,4-dibenzodiazepine products of formula (III). The present application describes the preparation of the 1,4-dibenzodiazepine products of formula (III) from simple commercial raw materials by efficient processes.
    Type: Application
    Filed: June 21, 2016
    Publication date: April 19, 2018
    Inventors: Anthony BURKE, Daniela Alexandra SILVA PEIXOTO
  • Publication number: 20180105503
    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: Application
    Filed: August 29, 2017
    Publication date: April 19, 2018
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Publication number: 20180105504
    Abstract: The invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein the variables X, Y1-Y5, R1, R2, R3, R4, and Het have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Application
    Filed: October 31, 2017
    Publication date: April 19, 2018
    Applicants: GENENTECH, INC., XENON PHARMACEUTICALS INC.
    Inventors: Daniel SUTHERLIN, Steven MCKERRALL, Michael Scott WILSON, Kwong Wah LAI, Philippe BERGERON, Birong ZHANG
  • Publication number: 20180105505
    Abstract: A glutathione-cleavable prodrug is provided herein, as well as methods for its use in treating cancer, including triple negative breast cancer. The prodrug can be cleaved by glutathione under physiological conditions to generate a biologically active agent. The compound described herein is advantageous as the compound is fluorescent and can therefore be monitored within a subject.
    Type: Application
    Filed: May 12, 2016
    Publication date: April 19, 2018
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Milton L. Brown, Yali Kong, Jacqueline Smith, Kan Wang, Shujie Hou
  • Publication number: 20180105506
    Abstract: The subject invention relates to improved tocopheryl quinine derivatives and tocopherol derivatives having improved pharmacokinetics in vivo that can, in some embodiments, be useful in the treatment of Lysosomal Storage Disorder, restoration of normal mitochondrial ATP production, modulation of intracellular calcium ion concentration and other treatments or therapies. The tocopheryl quinone derivatives and tocopherol derivatives have side chains that have terminally halogenated carbon atoms.
    Type: Application
    Filed: May 30, 2017
    Publication date: April 19, 2018
    Inventors: Juan Jose MARUGAN, Wei ZHENG, Jingbo XIAO, John MCKEW
  • Publication number: 20180105507
    Abstract: A compound of formula (I) wherein X is O, C?O or S; Y is N or CH; R2 and R4 are each independently H, —(CH2)pCOOH, —(CH2)pCON(R5)2 or —(CH2)pCOOC1-6alkyl; or R2 and R4 together form a 6-membered phenyl ring fused to the five membered ring; each R1 is independently selected from H, halo (e.g. fluoro or chloro), C6-10aryl, C7-12arylalkyl, C2-12 alkenyl; OC1-12 alkyl, OC2-12 alkenyl or a C1-12 alkyl group; each R5 is H or C1-6 alkyl; each p is 0 to 3; n is 1 to 4; or a salt, ester, solvate, N-oxide, or prodrug thereof, e.g.
    Type: Application
    Filed: October 20, 2017
    Publication date: April 19, 2018
    Inventors: Berit Johansen, Marcel Sanderberg, Inger-Reidun Aukrust, George Kokotos, Efrosini Barbayianni
  • Publication number: 20180105508
    Abstract: The present invention provides compounds pounds of Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, pro-drugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I), (II) or (III) for treating diseases associated with the over-expression of phosphoglycerate dehydrogenase (PHGDH) in a subject, such as proliferative diseases (e.g., cancers (e.g., breast cancer, ER negative breast cancer, melanoma, cervical cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases). Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the activity of PHGDH or inhibit the serine biosynthetic pathway, or both.
    Type: Application
    Filed: January 15, 2016
    Publication date: April 19, 2018
    Applicants: Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Inc.
    Inventors: David M. Sabatini, Michael Pacold, Matthew B. Boxer, Jason M. Rohde, Kyle R. Brimacombe, Min Shen
  • Publication number: 20180105509
    Abstract: The present invention relates to novel aminoindazolyl derivative compounds of Formula (I), the use of said compounds in treating diseases mediated by modulation of voltage-gated sodium channels in particular Nav1.7 AND to compositions containing said derivatives.
    Type: Application
    Filed: April 20, 2016
    Publication date: April 19, 2018
    Inventors: James DUFFY, Mark Stuart CHAMBERS, Alastair RAE, James OSBORNE, Isabelle Anne LEMASSON, Michael Daniel GOLDSMITH, Andrew SHARPE, Silvia FONQUERNA POU
  • Publication number: 20180105510
    Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.
    Type: Application
    Filed: December 18, 2017
    Publication date: April 19, 2018
    Inventors: Geoff G.Z. ZHANG, Michael F. BRADLEY, David M. BARNES, Rodger HENRY
  • Publication number: 20180105511
    Abstract: The present invention is directed to novel synthetic methods for preparing cyclopropyl indolinone compound represented by Structural Formula (A): (A) or its pharmaceutically acceptable salt thereof. Also included are synthetic intermediates described herein.
    Type: Application
    Filed: October 23, 2017
    Publication date: April 19, 2018
    Applicant: University Health Network
    Inventors: Graham Cumming, Narendra Kumar B. Patel, Bryan T. Forrest, Yong Liu, Sze-Wan Li, Peter Brent Sampson, Louise G. Edwards, Heinz W. Pauls
  • Publication number: 20180105512
    Abstract: The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R1, R2, R3, R4, X, and Z? have one of the meanings as defined in the specification, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).
    Type: Application
    Filed: January 7, 2016
    Publication date: April 19, 2018
    Inventors: Armin HECKEL, Dieter HAMPRECHT, Joerg KLEY
  • Publication number: 20180105513
    Abstract: The present invention relates to the technical field of pesticides, particularly relates to a pyrazole compound or a salt thereof, a preparation method therefor, a herbicidal composition and use thereof. A pyrazole compound of formula (I) or a salt thereof: wherein, R1 represents hydrogen or C1-C4 alkyl; R2 represents C1-C3 alkyl; R3 represents C1-C6 linear chain or cyclic group containing one or more heteroatoms selected from O, S, and N; R4 represents C1-C3 alkyl or halogen; R5 represents pyrazole ring or pyrazole ring substituted with one or more groups selected from alkyl, alkoxyl, halogen, halogenated alkyl, amino, and nitro. The pyrazole compound is an excellent herbicide with broad spectrum biological activity and outstanding safety for crops.
    Type: Application
    Filed: March 4, 2016
    Publication date: April 19, 2018
    Inventors: Lei LIAN, Yurong ZHENG, Song LI, Xuegang PENG, Tao JIN, Qi CUI
  • Publication number: 20180105514
    Abstract: Disclosed are compounds having the formula: wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, and R17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
    Type: Application
    Filed: January 3, 2018
    Publication date: April 19, 2018
    Inventors: John F. MEHLMANN, Joseph J. ROMANO
  • Publication number: 20180105515
    Abstract: This invention is directed to compounds, which are useful as protein kinase (PK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, metabolic diseases inflammatory disorders and neurodegenerative disorders.
    Type: Application
    Filed: December 15, 2017
    Publication date: April 19, 2018
    Inventors: Sougato Boral, Thomas C. Malone, Shimiao Wang
  • Publication number: 20180105516
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, X1, X2, X3, X4, Y, Z, A, Het, R1, R2, R3, R4, R5 R6, R7, R8, R9, R10, R11, R12 and R13 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis, muscular sclerosis and psoriasis.
    Type: Application
    Filed: December 19, 2017
    Publication date: April 19, 2018
    Applicant: Genentech, Inc.
    Inventors: Benjamin FAUBER, Emanuela GANCIA, Tammy LADDUWAHETTY, David VESEY, Paul WINSHIP, Olivier RENE
  • Publication number: 20180105517
    Abstract: A process for preparing (3R)-3-[2-Hydroxy(di-2-thienyl)acetoxy]-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide) comprises reacting 2-hydroxy-2,2-dithien-2-ylacetic acid 1-azabicyclo[2.2.2]oct-3(R)yl methyl ester and 3-phenoxypropyl bromide, wherein the reaction takes place in a solvent or mixture of solvents selected from the group of amides and/or the group of solvents with a sulfoxide group. Also provided is a crystalline aclidinium bromide characterized by a powder XRPD pattern having peaks at 7.7±0.2° 2?, 10.4±0.2° 2?, 13.2±0.2° 2?, 13.8±0.2° 2?, 19.9±0.2° 2?, 20.3±0.2° 2?, 20.8±0.2° 2?, 24.2±0.2° 2?, 25.7±0.2° 2?, 26.1±0.2° 2?, 29.2±0.2° 2?, 30.8±0.2° 2?. A pharmaceutical composition comprises aclidinium bromide according to the invention and a pharmaceutically acceptable excipient.
    Type: Application
    Filed: March 30, 2016
    Publication date: April 19, 2018
    Inventors: Zita MENDES, Constança CACELA, Ana Carina CONSTANTINO, Bruno SANTOS
  • Publication number: 20180105518
    Abstract: The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I): which are tropomyos-in-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: April 4, 2016
    Publication date: April 19, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Yi Heng Chen, Ping Liu, Dongfang Meng, Jane Yang Wu, Chun Sing Li, Zhiqi Qi
  • Publication number: 20180105519
    Abstract: A compound which is an isoxazolyl imidazopyridine of formula (I): wherein: R0 and R, which are the same or different, are each H or C alkyl; R9? and R9?, which are the same or different, are each H or F; X is -(alk)n-, -alk-C(?O)—NR—, -alk-NR—C(?O)— or -alk-C(?O)—; R1 is selected from —S(?O)2R? and a 4- to 7-membered heterocyclic group which is unsubstituted or substituted; R2 and R2?, which are the same or different, are each H or C1-6 alkyl; or R2 and R2? form, together with the C atom to which they are attached, a C3-6 cycloalkyl group; R3 and R3?, which are the same or different, are each H, C1-6 alkyl, OH or F; R4 is phenyl or a 5- to 12-membered N-containing heteroaryl group and is unsubstituted or substituted; alk is C1-6 alkylene; R? is C1-6 alkyl; and n is 0 or 1; or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer.
    Type: Application
    Filed: April 20, 2016
    Publication date: April 19, 2018
    Inventors: Neil Anthony PEGG, David Michel Adrien TADDEI, Richard BROWN
  • Publication number: 20180105520
    Abstract: The present invention relates to azaindole acetic acid derivatives of formula (I), wherein R1 and R2 are as described in the description, and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
    Type: Application
    Filed: December 14, 2017
    Publication date: April 19, 2018
    Inventors: Hamed Aissaoui, Christoph Boss, Patrick Bouis, Julien Hazemann, Romain Siegrist