Patents Issued in May 12, 2016
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Publication number: 20160130210Abstract: A compound represented by formula (I), a resin including a structural unit derived from the compound and a resist composition including the resin: wherein R1 represents a hydrogen atom, a halogen atom or a C1 to C6 alkyl group in which a hydrogen atom may be replaced by a halogen atom, R2 represents a C1 to C6 perfluoroalkyl group or *—CHRf1Rf2, * represents a binding site to a carbonyl group, Rf1 and Rf2 each independently represent a C1 to C4 perfluoroalkyl group or Rf1 and Rf2 may be bonded together with a carbon atom bonded thereto to form a ring, A1 represents a single bond, a C1 to C6 alkanediyl group or **-A3-X1-(A4-X2)a-(A5)b-, ** represents a binding site to an oxygen atom, A2, A3, A4 and A5 each independently represent a C1 to C6 alkanediyl group, X1 and X2 each independently represent —O—, —CO—O— or —O—CO—, a and b each represent 0 or 1, and W1 represents a C5 to C18 divalent alicyclic hydrocarbon group.Type: ApplicationFiled: November 10, 2015Publication date: May 12, 2016Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yukako ANRYU, Shingo FUJITA, Koji ICHIKAWA
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Publication number: 20160130211Abstract: Certain embodiments of the invention provide antioxidant-based diacids and polymers comprising glycol groups as described herein, and methods of use thereof. In certain embodiments the polymers described herein are formulated as microspheres or hydrogels. Described herein is the chemical incorporation of antioxidants, e.g., coumaric acid, ferulic acid, and sinapic acid, into a polymer backbone for use, e.g., in applications for localized release and rapid delivery. As provided, the chemical composition of the linker molecules used (of which hold together two bioactives via ester linkages) may be used to vary the hydrophilicity of the polymer. The bioactive release rate may also be altered for a tunable release delivery system, allowing for increased bioactive release compared to other linkers previously utilized.Type: ApplicationFiled: May 29, 2014Publication date: May 12, 2016Applicant: Rutgers, The State University of New JerseyInventors: Kathryn Uhrich, Michelle Morano
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Publication number: 20160130212Abstract: A compound represented by formula (I), a resin including a structural unit derived from the compound and a resist composition including the resin: wherein R1 represents a hydrogen atom, a halogen atom or a C1 to C6 alkyl group in which a hydrogen atom may be replaced by a halogen atom, R2 represents a C1 to C12 fluorinated saturated hydrocarbon group, A1 represents a single bond, a C1 to C6 alkanediyl group or *-A3-X1-(A4-X2)a-(A5)b-, * represents a binding site to an oxygen atom, A2, A3, A4 and A5 each independently represent a C1 to C6 alkanediyl group, X1 and X2 each independently represent —O—, —CO—O— or —O—CO—, W1 represents a C5 to C18 divalent alicyclic hydrocarbon group, a represents 0 or 1, and b represents 0 or 1.Type: ApplicationFiled: November 10, 2015Publication date: May 12, 2016Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Tatsuro MASUYAMA, Yuichi MUKAI, Koji ICHIKAWA
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Publication number: 20160130213Abstract: In an embodiment, an amine-oxidation inhibitor, such as a free radical scavenger and/or antioxidant, is added to an oxidation-sensitive amine, such as an amine catalyst, to inhibit oxidation of the amine. The inhibitor-treated amine may then be used in an application such as a polyurethane application to reduce the emission of undesired oxidation products from the polyurethane.Type: ApplicationFiled: January 18, 2016Publication date: May 12, 2016Inventors: Bhajendra Narayan Barman, Robert A. Grigsby, JR.
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Publication number: 20160130214Abstract: Compounds of the formula I in which R1, R4, R6, R, X1, X2, X3, X4, q and W have the meanings indicated in claim 1, are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.Type: ApplicationFiled: May 9, 2014Publication date: May 12, 2016Applicant: Merck Patent GmbHInventors: Christos TSAKLAKIDIS, Wolfgang STAEHLE, Birgitta LEUTHNER, Paul CZODROWSKI, Thomas FUCHSS
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Publication number: 20160130215Abstract: The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like.Type: ApplicationFiled: January 25, 2016Publication date: May 12, 2016Inventors: Naoki Tomita, Shigeo Kajii, Douglas Robert Cary, Daisuke Tomita, Shinichi Imamura, Ken Tsuchida, Satoru Matsuda, Ryujiro Hara, Yusuke Tominari
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Publication number: 20160130216Abstract: The present application describes amphiphatic compounds like compound IIa below, compositions and methods for incorporating chemoselective and bio-orthogonal complementary functional groups into liposomes. Such compounds are incorporated in greater numbers in liposome and fused cell surfaces, leading to greater adhesion and conjugation efficiency. The present application also describes various uses of these modified liposomes including for tethering the chemoselective and bioorthogonal complementary functional groups from cell surfaces by liposome delivery toward the goal of rewiring the cell surface.Type: ApplicationFiled: June 11, 2014Publication date: May 12, 2016Inventor: Muhammad YOUSAF
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Publication number: 20160130217Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have anticancer activity. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.Type: ApplicationFiled: November 4, 2015Publication date: May 12, 2016Applicant: The Board of Regents of the University of Texas SystemInventors: Jung-Mo AHN, Ganesh RAJ
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Publication number: 20160130218Abstract: The present invention provides a key new intermediate (a compound of formula III) of 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound), a pharmaceutically acceptable salt thereof and a preparation method thereof. The present invention additionally discloses a method for preparing 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound) from the formula III compound, said method overcoming the shortcomings of current formula IV compound preparation methods, such as low production volumes, low purity, high energy consumption, high costs, and inability to achieve industrialized production, and provides a formula IV compound preparation method which is simple, economical, environmentally-friendly and easy to produce industrially; the reaction solvent of the method is easily recycled and the method can produce the formula IV compound at high production rates and with high purity.Type: ApplicationFiled: June 23, 2014Publication date: May 12, 2016Applicants: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Fuli Zhang, Zhezhou Yang, Rusheng Bao, Pengcheng Qiu, Linyong Jin, Hu Pan, Linyu Pan, Dongming Jiang, Weiwei Xu
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Publication number: 20160130219Abstract: Semi-synthetic oximes derived from metabolites extracted from medicinal plants, Senecio nutans and Xenophyllum poposum, the method of preparation thereof and their use as agents with vasodilator and hypotensive effects are provided.Type: ApplicationFiled: October 6, 2015Publication date: May 12, 2016Inventors: Adrian Guillermo Paredes Poblete, Glauco Segundo Morales Borcosque, Fredi Eduardo Cifuentes Jorquera
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Publication number: 20160130220Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.Type: ApplicationFiled: October 8, 2015Publication date: May 12, 2016Applicant: REATA PHARMACEUTICALS, INC.Inventors: Eric ANDERSON, Gary L. BOLTON, Bradley CAPRATHE, Xin JIANG, Chitase LEE, William H. ROARK, Melean VISNICK
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Publication number: 20160130221Abstract: Disclosed herein is mixed fertilizer according to the process comprising: reacting isobutyraldehyde with an aqueous solution of urea in the presence of a phase transfer catalyst to form isobutylidene diurea, wherein the phase transfer catalyst is a quaternary ammonium salt; and mixing the isobutylidene diurea with at least one of another fertilizer, a secondary nutrient, a trace element, a plant protection agent, a filler, and other fertilizer ingredients, to form the mixed fertilizer. Also disclosed is isobutylidene diurea produced by the process comprising: reacting isobutyraldehyde with an aqueous solution of urea in the presence of a phase transfer catalyst to form isobutylidene diurea; wherein the phase transfer catalyst is a quaternary ammonium salt.Type: ApplicationFiled: January 15, 2016Publication date: May 12, 2016Inventors: Syed Azhar Hashmi, Abdullah Bin-Nafisa
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Publication number: 20160130222Abstract: Provided herein are compounds of the formula (IV) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful as MITF inhibitors, MITF pathway inhibitors and for the treatment of cancer.Type: ApplicationFiled: June 10, 2014Publication date: May 12, 2016Inventors: Patrick FALOON, Warren S. WEINER, Robert A. SMITH, Frank John SCHOENEN, David E. FISHER, Rizwan HAQ
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Publication number: 20160130223Abstract: The invention provides a compound of formula A, B, C or D, methods for making them, intermediates therefor, and their use in making organic biologically active compounds: Wherein: X=F, Cl, Br, I, sulfonate esters, phosphate esters or another leaving group R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 are each individually selected from H, alkyl, aryl, alkynyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, nitro, halogen or amino; or are selected from H, C1-C10 alkyl, aryl, C1-C10 alkynyl, C1-C10 alkenyl, C1-C10 cycloalkyl, C1-C10 cycloalkenyl, C1-C10 alkoxy, nitro, halogen or amino R11=tetrafluoroborate, triflate, halogen, perclorate, sulfates, phosphates or carbonates Excluding the case when: X=F and R1=R2=R3=R4=R5=H and R6=R7=R8=R9=methyl, R10=H and R11=triflate or tetrafluoroborate; or Wherein: X=F, Cl, Br, I, sulfonate esters, phosphate esters or other another leaving group; and R1, R2, R3, R4, R5 are each individually selected from H, alkyl, aryl, alkynyl, alkenyl, cycloalkyl, cycloalkenyl, alkoType: ApplicationFiled: January 20, 2016Publication date: May 12, 2016Applicant: Hovione Inter limitedInventor: Emilia Perpetua Tavares Leitao
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Publication number: 20160130224Abstract: There are provided inter alia novel N-phenyl substituted pyrrole derivativesand theiruse in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections.Type: ApplicationFiled: June 4, 2014Publication date: May 12, 2016Inventors: Peter William ANDREW, Mafalda Pires DAMASO, Mark William DAVIES, Fritz-Frieder FRICKEL, Daniel HAMZA, Simon Christopher HIRST, Rana LONNEN
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Publication number: 20160130225Abstract: A compound is represented by a formula (1) below, in which k is an integer of 0 or more, m is an integer of 1 or more, n is an integer of 2 or more. L is a substituted or unsubstituted aromatic hydrocarbon ring having 6 to 30 ring carbon atoms, CN is a cyano group, and D1 and D2 are each independently represented by one of a formula (2), a formula (3) and formula (3x) below, D1 and D2 being optionally mutually the same or different.Type: ApplicationFiled: June 26, 2014Publication date: May 12, 2016Applicant: Idemitsu Kosan Co., Ltd.Inventors: Satomi TASAKI, Masahiro KAWAMURA, Toshinari OGIWARA, Hitoshi KUMA, Kei YOSHIDA, Keiji OKINAKA
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Publication number: 20160130226Abstract: The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: June 17, 2014Publication date: May 12, 2016Inventors: Jagannath MADANAHALLI RANGANATH RAO, Madhavan GURRAM RANGA, Shanmugam PACHIYAPPAN
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Publication number: 20160130227Abstract: The invention relates to the compounds of formula II, formula Ia, formula IIa or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula II, formula Ia, formula IIa and methods for treating or preventing atherothrombosis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment or management of ischemia, stroke, cerebral thrombosis, arterial thrombosis, thrombotic cerebrovascular, cardiovascular diseases and blood clots.Type: ApplicationFiled: September 21, 2015Publication date: May 12, 2016Inventor: Mahesh Kandula
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Publication number: 20160130228Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.Type: ApplicationFiled: January 15, 2016Publication date: May 12, 2016Inventors: Shuang Liu, Bryan Cordell Duffy, John Frederick Quinn, May Xiaowu Jiang, Ruifang Wang, Gregory Scott Martin, He Zhao, Bruce Francis Molino, Peter Ronald Young
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Publication number: 20160130229Abstract: Provided herein are compounds that exhibit activity as acetyl-CoA carboxylase modulators (e.g., inhibitors) and are useful, for example, in methods for the control of fungal pathogens in plants.Type: ApplicationFiled: June 13, 2014Publication date: May 12, 2016Applicant: Monsanto Technology LLCInventors: Urszula Slomczynska, Matthew W. Dimmic, William P. Haakenson, JR., Jennifer L. Bennett, Barry J. Shortt, Christina M. Taylor, Deryck Jeremy Williams, Martin Slater
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Publication number: 20160130230Abstract: The present application relates to novel substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: November 16, 2015Publication date: May 12, 2016Applicant: Bayer Intellectual Property GmbHInventors: Alexandros VAKALOPOULOS, Daniel MEIBOM, Peter NELL, Frank SÜßMEIER, Barbara ALBRECHT-KÜPPER, Katja ZIMMERMANN, Joerg KELDENICH, Dirk SCHNEIDER, Ursula KRENZ
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Publication number: 20160130231Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.Type: ApplicationFiled: January 5, 2016Publication date: May 12, 2016Inventors: Anderson Gaweco, Jefferson W. Tilley, John Walker, Samantha Palmer, James Blinn
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Publication number: 20160130232Abstract: There are provided 4-alkynylimidazole derivatives represented by the following general formula (I) or phamaceutically acceptable salts thereof; the derivatives have a superior EP4 receptor antagonistic action and are useful as pharmaceuticals for the treatment of diseases associated with the EP4 receptor, for example, as anti-inflammatory and/or analgesic drugs for inflammatory diseases and diseases that involve various kinds of pains, and further as pharmaceuticals for the treatment of immune diseases that result from inflammations as evoked by tissue destruction due to the activation of Th1 cells and/or Th17 cells:Type: ApplicationFiled: June 12, 2014Publication date: May 12, 2016Applicant: KAKEN PHARMACEUTICAL CO., LTD.Inventors: Satoru IKEGAMI, Atsushi WATANABE, Kimio HIRANO, Tadashi OHYAMA
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Publication number: 20160130233Abstract: The present invention provides a dispersant excellent in the solubility to a solvent, the adsorption power to a coloring material, and the coloring material dispersibility, and reduced in the self-coloring property, a compound and a polymerizable compound for preparing the dispersant, and a toner using the dispersant. The dispersant has a structure in which a structure represented by the following specific formula (3) or a tautomer thereof is bonded with a polymer, and the toner contains the dispersant.Type: ApplicationFiled: January 5, 2016Publication date: May 12, 2016Inventors: Haruko Kubo, Suzuka Ueno, Junko Chizuwa, Tomoya Yamamoto, Hitoshi Itabashi, Yuhei Terui, Yu Yoshida, Yasuaki Murai, Takayuki Toyoda
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Publication number: 20160130234Abstract: The present invention generally relates to silver complexes of formula (I) and (II), having high stability and showing antimicrobial activity. The invention also relies on compositions containing said photochemically stable silver complexes of formula (I) and (II), optionally admixed with at least another antimicrobial agent, thus enhancing their antimicrobic activity.Type: ApplicationFiled: June 6, 2013Publication date: May 12, 2016Inventor: Massimo FERRARI
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Publication number: 20160130235Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.Type: ApplicationFiled: September 4, 2015Publication date: May 12, 2016Applicant: Lantheus Medical Imaging, Inc.Inventors: David S. Casebier, Simon P. Robinson, Ajay Purohit, Heike S. Radeke, Michael T. Azure, Douglas D. Dischino
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Publication number: 20160130236Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: January 15, 2016Publication date: May 12, 2016Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Juswinder Singh
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Publication number: 20160130237Abstract: Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.Type: ApplicationFiled: January 19, 2016Publication date: May 12, 2016Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Dominic Reynolds, Ming-Hong Hao, John Wang, Sudeep Prajapati, Takashi Satoh, Anand Selvaraj
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Publication number: 20160130238Abstract: A chemical process that can form pharmaceutically acceptable medicaments NNRTI's for the treatment of HIV starting from thiotriazole compounds. The chemical process can form thiotetrazoles such as 2-((1-(naphthalen-1-yl)-1H-tetrazol-5-yl) thio)-N-(2-nitrophenyl)actetamide that is, a potent NNRTI with nanomolar activity.Type: ApplicationFiled: August 2, 2013Publication date: May 12, 2016Inventor: Gregory ROSOCHA
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Publication number: 20160130239Abstract: Provided herein are sodium channel modulating Compounds, in particular NaV1.7 modulating compounds of Formula I or compounds of Formula I?: In particular, provided herein are processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions comprising, and therapeutic methods comprising administering such compounds. In particular, provided herein are compounds for the treatment of pain and diabetes.Type: ApplicationFiled: January 13, 2016Publication date: May 12, 2016Applicant: CHROMOCELL CORPORATIONInventors: Olga BABICH, Tina GARYANTES, Robert Z. LUO, David J. PALLING, Srinivasan P. VENKATACHALAN, Yanlin WANG-FISCHER
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Publication number: 20160130240Abstract: The present invention relates to aryl sulfoxide derivatives, to the use thereof as acaricides and insecticides for controlling animal pests and to processes and intermediates for preparation thereof. The aryl sulfide and aryl sulfoxide derivatives have the general structure (I) in which the respective radicals are as defined in the description.Type: ApplicationFiled: June 16, 2014Publication date: May 12, 2016Inventors: Bernd ALIG, Silvia CEREZO-GALVEZ, Reiner FISCHER, Adeline KOEHLER, Julia Johanna HAHN, Angela BECKER, Kerstin ILG, Arnd VOERSTE, Daniela PORTZ
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Publication number: 20160130241Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.Type: ApplicationFiled: January 14, 2016Publication date: May 12, 2016Inventors: Craig C. BEESON, Christopher C. LINDSEY, Yuri K. PETERSON, Baerbel ROHRER
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Publication number: 20160130242Abstract: A process for preparing a divinylarene dioxide including the steps of: (a) feeding one or more feed streams of the following reactants into a reactor system: (i) at least one divinylarene, (ii) at least one oxidizing agent, and (iii) at least one solvent to form a reaction mixture in the reactor system; (b) continuously reacting together the one or more feed streams of the reactants of step (a) in the reaction mixture; and (c) controlling heat removal of the reaction mixture as the reactants of step (b) react together; wherein the heat removal is sufficient to provide a residence time of the reactants in the reaction mixture of less than about 180 minutes residence time of the reactants in the reaction step (b); and an apparatus for preparing a divinylarene dioxide.Type: ApplicationFiled: June 3, 2014Publication date: May 12, 2016Inventors: Kishori Deshpande, David Jean, Jianping Zeng, Ravindra S. Dixit, David H. West
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Publication number: 20160130243Abstract: There is provided an epoxy compound whose melt viscosity is low and which exhibits heat resistance and flame retardancy of a cured product; an epoxy resin which includes the same; curable composition and cured product; and semiconductor sealing material. The epoxy compound has a molecular structure represented by the following Formula (I): in the formula, G represents a glycidyl group, and X represents a structural site represented by the following Structural Formula (x1) or (x2); in Formula (x1) or (x2), k represents an integer of 1 to 3, m represents 1 or 2, Ar represents a structural site represented by the following Structural Formula (Ar1) or (Ar2), and when k or m represents 2 or greater, a plurality of Ar's may be the same as or different from each other: in Formula (3) or (4), G represents a glycidyl group, and p and r each independently represent 1 or 2.Type: ApplicationFiled: February 21, 2014Publication date: May 12, 2016Applicant: DIC CorporationInventors: Yutaka Satou, Ayumi Takahashi
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Publication number: 20160130244Abstract: Disclosed is a process to produce a dry purified carboxylic acid product comprising furan-2,5-dicarboxylic acid (FDCA). The process comprises oxidizing at least one oxidizable compound selected from the following group: 5-(hydroxymethyl)furfural (5-HMF), 5-HMF esters (5-R(CO)OCH2-furfural where R=alkyl, cycloalkyl and aryl), 5-HMF ethers (5-R?OCH2-furfural, where R?=alkyl, cycloalkyl and aryl), 5-alkyl furfurals (5-R?-furfural, where R?=alkyl, cycloalkyl and aryl), mixed feed-stocks of 5-HMF and 5-HMF esters and mixed feed-stocks of 5-HMF and 5-HMF ethers and mixed feed-stocks of 5-HMF and 5-alkyl furfurals to generate a crude carboxylic acid slurry comprising FDCA, removing impurities from a crude carboxylic acid slurry in a liquid displacement zone to form a low impurity slurry stream. The low impurity slurry stream is further treated in a secondary oxidation zone to produce a secondary oxidation slurry stream which is routed to a crystallization zone to form a crystallized slurry stream.Type: ApplicationFiled: January 14, 2016Publication date: May 12, 2016Applicant: Eastman Chemical CompanyInventors: Mesfin Ejerssa Janka, Kenny Randolph Parker, Paula Moody, Ashfaq Shahanawaz Shaikh, Lee Reynolds Partin, Bradford Russell Bowers, Michael Charles Morrow
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Publication number: 20160130245Abstract: Disclosed in the present invention are a 6,8-substituted naringenin derivative as shown in formula (I): in which A6 and A8 in formula (I) are respectively selected from H, halogen, hydroxyl, an alkyl group with 1-3 carbon atoms, and a straight-chain alkenyl, alcohol group, aldehyde group, or carboxylic acid group containing 2-3 carbon atoms, obtained by modifying naringenin as lead compound, or a pharmaceutically acceptable salt thereof, a preparation method therefor and use thereof in preparation of drugs for improving the function of the respiratory system and relieving cough.Type: ApplicationFiled: January 18, 2013Publication date: May 12, 2016Applicant: SUN YAT-SEN UNIVERSITYInventors: Weiwei SU, Yonggang WANG, Zhong WU
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Publication number: 20160130246Abstract: A compound useful as a Sirt2 or Sirt5 inhibitor having the formula (1) wherein: R1 is a hydrocarbon group having at least two carbon atoms connected by carbon-carbon bonds, wherein said hydrocarbon group is optionally endcapped by a neutral or anionic oxygen-containing group; R2a, R2b, and R2c are independently selected from hydrogen atom and hydrocarbon groups; X0, X1, X2, and X3 are independently selected from —(CH2)n—, —NR5—, —O—, —S—, and a bond, wherein n represents 1, 2, or 3, provided that at least one of X0-X3 is —(CH2)n—; and R3 and R4 are independently selected from the group consisting of hydrogen atom, hydrocarbon groups, biological groups, and protecting groups. Also described are pharmaceutical compositions of the inhibiting compounds, and methods of treatment by administration of the inhibiting compounds.Type: ApplicationFiled: June 6, 2014Publication date: May 12, 2016Inventor: Hening LIN
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Publication number: 20160130247Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.Type: ApplicationFiled: January 5, 2016Publication date: May 12, 2016Inventors: Young K. CHEN, Toufike KANOUNI, Stephen W. KALDOR, Jeffrey Alan STAFFORD, James Marvin VEAL
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Publication number: 20160130248Abstract: Provided is (+)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione or a salt thereof. Also provided is a drug containing as the active ingredient (+)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione or a salt thereof.Type: ApplicationFiled: June 6, 2014Publication date: May 12, 2016Applicant: KAKEN PHARMACEUTICAL CO., LTD.Inventors: Noriyuki KAMEI, Daigo KAMIMURA, Yoshitake SUMIKAWA, Shota TOKUOKA
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Publication number: 20160130249Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidin-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.Type: ApplicationFiled: May 22, 2015Publication date: May 12, 2016Applicant: ASTRAZENECA ABInventors: Andrew Peter Thomas, Elaine Sophie Elizabeth Stokes, Laurent Francois Andre Hennequin
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Publication number: 20160130250Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: January 19, 2016Publication date: May 12, 2016Inventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
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Publication number: 20160130251Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: ApplicationFiled: May 19, 2015Publication date: May 12, 2016Inventors: Michael Graupe, Keith Koch, Britton K. Corkey, Gregory Notte, Lawrence S. Melvin, JR.
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Publication number: 20160130252Abstract: Crystalline Forms R5, R5a, R5b and R6 of nilotinib hydrochloride and processes for their preparation.Type: ApplicationFiled: April 23, 2014Publication date: May 12, 2016Inventors: Vishweshwar PEDDY, Ramanaiah CHENNURU, Srividya RAMAKRISHNAN
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Publication number: 20160130253Abstract: The invention provides for novel MAP kinase inhibitors and compositions comprising the same. In some embodiments, the MAP kinase inhibitors are p38? MAP kinase inhibitors. The invention further provides for methods for treatment of diseases comprising administration of MAP kinase inhibitors or compositions comprising MAP kinase inhibitors. In some embodiments, the disease is Alzheimer's Disease, ALS, Huntington's Disease or Parkinson's Disease.Type: ApplicationFiled: September 15, 2015Publication date: May 12, 2016Inventors: Ottavio ARANCIO, Daniel Martin WATTERSON, Jeffrey Claude PELLETIER, Saktimayee Mitra ROY
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Publication number: 20160130254Abstract: Compounds of formula (I) wherein R1 to R8, A, B, Z1, and Z2 are as defined in the claims and pharmaceutically acceptable salts and esters thereof are disclosed. The compounds of formula (I) possess utility as androgen receptor antagonists (inhibitors) and/or cytochrome P450 monooxygenase 17?-hydroxylase/17,20-lyase (CYP17) inhibitors. The compounds are useful as medicaments in the treatment of cancer, particularly prostate cancer, and other androgen dependent conditions and diseases where androgen antagonism is desired.Type: ApplicationFiled: June 10, 2014Publication date: May 12, 2016Inventors: Gerd WOHLFAHRT, Petteri RUMMAKKO, Arja KARJALAINEN, Mikko PASSINIEMI, Pekka PIETIKÄINEN, Anssi HAIKARAINEN, Emilia VÄISÄNEN, Eija TIAINEN
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Publication number: 20160130255Abstract: The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).Type: ApplicationFiled: January 8, 2016Publication date: May 12, 2016Applicant: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Rainer E. Martin, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20160130256Abstract: There are provided inter alia compounds of formula (I) wherein R1, R2a, R2b, R3, R4, L, X, R5 and R6 are as defined in the description for use in the treatment of inflammatory diseases.Type: ApplicationFiled: January 18, 2016Publication date: May 12, 2016Applicant: Respivert LimitedInventors: John King-Underwood, George Hardy, Peter John Murray, Jonathan Gareth Williams, Stuart Thomas Onions
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Publication number: 20160130257Abstract: Compositions are provided for selectively inhibiting bacterial proteasome. Also provided are methods for assaying the compositions, methods for treating bacterial infection, and methods for inducing apoptosis in tumor cells using the compositions.Type: ApplicationFiled: November 9, 2015Publication date: May 12, 2016Applicant: BROWN UNIVERSITYInventor: Jason K. Sello
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Publication number: 20160130258Abstract: Described herein are compounds and compositions for the treatment of a fibrotic disease.Type: ApplicationFiled: June 5, 2014Publication date: May 12, 2016Inventors: Luke LAIRSON, Michael BOLLONG, Peter G. SCHULTZ, Arnab K. CHATTERJEE, Baiyuan YANG, Puneet KUMAR, Kaveri URKALAN
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Publication number: 20160130259Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: June 19, 2014Publication date: May 12, 2016Applicant: Merck Sharp & Dohme Corp.Inventors: Hong Liu, Xing Dai, Anandan Palani, Shuwen He, Ravi Nargund, Dong Xiao, Qun Dang, Xuanjia Peng, Peng Li