Patents Issued in December 31, 2015
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Publication number: 20150376095Abstract: A process for converting polyhydric alcohols to monoalcohols in a counter current column reactor with a metal based catalyst supported on a porous membrane coated over a tubular system that delivers hydrogen where a hydrocarbon (low polarity) liquid solvent is fed at the bottom of the column reactor and an aqueous liquid having polyhydric alcohols therein is fed into the top of the reactor such that the aqueous liquid flows countercurrent to the low polarity solvent liquid and further wherein the low polarity solvent liquid is less dense than the aqueous liquid such that the two liquids are subject to phase separation. Monoalcohols are formed by hydrogenolysis reactions of polyhydric alcohols on the metal catalyst. Monoalcohols phase separate from the aqueous phase to the hydrocarbon solvent. Monoalcohols are further separated from the organic solvent.Type: ApplicationFiled: June 25, 2015Publication date: December 31, 2015Applicant: PHILLIPS 66 COMPANYInventors: LOTERO Edgar, FJARE A. Kristi, SUGHRUE L. Edward
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Publication number: 20150376096Abstract: The invention relates to a method for producing butanol through microbial fermentation, in which the butanol product is removed by extraction into a water immiscible organic extractant composition during the fermentation. The invention also relates to a method for producing butanol through microbial fermentation, in which the butanol product is removed during the fermentation by extraction into a water-immiscible extractant composition comprising a first solvent having a butanol partition coefficient of at least 3, and a second solvent having a butanol partition coefficient, wherein the butanol partition coefficient of the first solvent is higher than the butanol partition coefficient of the second solvent. Optionally, the first solvent has a higher concentration of hydrogen bonding sites than the second solvent. The invention further relates to a composition including butanol in the water immiscible organic extractant composition described above.Type: ApplicationFiled: March 14, 2014Publication date: December 31, 2015Applicant: Butamax Advanced Biofuels LLCInventors: Douglas Robert ANTON, John W. HALLAM
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Publication number: 20150376097Abstract: Provided is a methanol plant that can obtain fresh water from sea water by using, in a seawater desalination device, the exhaust heat discharged in a step for producing methanol from natural gas. The methanol plant is provided with: a heat exchanger (4) that recovers into a thermal medium (for example, seawater) the exhaust heat discharged from a step for producing methanol from a feed stock (for example, natural gas); and a seawater desalinization device (6) that obtains freshwater from seawater using the exhaust heat recovered by means of the thermal medium.Type: ApplicationFiled: February 26, 2014Publication date: December 31, 2015Applicant: MITSUBISHI HEAVY INDUSTRIES, LTD.Inventors: Masaki Iijima, Haruaki Hirayama
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Publication number: 20150376098Abstract: A styrenated phenol compound in which a hydrazine or a diaminoalkane compound binds to a styrenated phenol, and a method of preparing the same are provided. The styrenated phenol compound may have improved exterior quality and storage stability of a product by maintaining a hardening stimulation property and plasticity and preventing discoloration when mixed with a hardener for an epoxy paint.Type: ApplicationFiled: June 24, 2015Publication date: December 31, 2015Inventors: Kee Yoon ROH, Jung Hee JANG, Je Young PARK
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Publication number: 20150376099Abstract: The present invention provides 3,3?,5,5?-tetraisopropyl-4,4?-diphenol crystal forms I, II and III, and preparation methods thereof. Crystal form I is superior to crystal form II in terms of stability under high temperature, high humidity, strong light and in water medium. The preparation methods for 3,3?,5,5?-tetraisopropyl-4,4?-diphenol crystal forms I, II and III provided in the invention are simple, easy to operate and suitable for industrial production.Type: ApplicationFiled: January 15, 2014Publication date: December 31, 2015Applicant: XI'AN LIBANG PHARMACEUTICAL CO., LTD.Inventors: Rutao WANG, Tao CHEN, Weijiao WANG
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Publication number: 20150376100Abstract: An object of the present invention is to provide a method for recovering a fluorine-containing ether capable of recovering a fluorine-containing ether used for producing a fluoropolymer, in higher recovery yield and in a shorter time. The present invention relates to a method for recovering a fluorine-containing ether, including the steps of: producing a wet fluoropolymer by suspension polymerization, solution polymerization, or bulk polymerization in the presence of at least a specific fluorine-containing ether; vaporizing and discharging vaporizable substances including the fluorine-containing ether by heating the wet fluoropolymer in a container; and transferring the vaporizable substances in the vaporized state to a cooling means to cool the vaporizable substances.Type: ApplicationFiled: January 20, 2014Publication date: December 31, 2015Applicant: DAIKIN INDUSTRIES, LTD.Inventors: Yumi ZENKE, Tadaharu ISAKA, Ryouichi FUKAGAWA, Takeshi SHIMONO
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Publication number: 20150376101Abstract: A heterocyclic nitrogen stabilizing agent is employed to reduce the rate of catalyst deactivation in a hydroformylation process.Type: ApplicationFiled: March 7, 2014Publication date: December 31, 2015Inventor: Thomas C. EISENSCHMID
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Publication number: 20150376102Abstract: A method for producing, in a few simple steps, a specific optically active aldehyde represented by the general formula (1), in which * is an asymmetric carbon atom, includes asymmetrically isomerizing a specific allyl alcohol represented by the general formula (2) in the presence of a ruthenium complex and a base.Type: ApplicationFiled: March 6, 2014Publication date: December 31, 2015Applicant: TAKASAGO INTERNATIONAL CORPORATIONInventors: Takeshi OHKUMA, Noriyoshi ARAI, Kazuhiko MATSUMURA
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Publication number: 20150376103Abstract: The present invention concerns a method for synthesising cyclohexenone and cyclohexenol compounds having specific fragrances and remanence properties, said method consisting in condensing a ketone on an ?-methylene-aldehyde in order to obtain, by means of a domino reaction, compounds of formula (I).Type: ApplicationFiled: September 24, 2013Publication date: December 31, 2015Applicant: V. MANE FILSInventors: Jean-Jacques CHANOT, Caroline PLESSIS
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Publication number: 20150376104Abstract: Compositions which inhibit corrosion and alter the physical properties of concrete (admixtures) are prepared from salt mixtures of hydroxycarboxylic acids, carboxylic acids, and nitric acid. The salt mixtures are prepared by neutralizing acid product mixtures from the oxidation of polyols using nitric acid and oxygen as the oxidizing agents. Nitric acid is removed from the hydroxycarboxylic acids by evaporation and diffusion dialysis.Type: ApplicationFiled: September 10, 2015Publication date: December 31, 2015Inventors: Donald E. Kiely, Kirk R. Hash, Kylie Kramer-Presta, Tyler N. Smith
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Publication number: 20150376105Abstract: Processes for the reduction and/or removal of permanganate reducing compounds (PRC'S) formed by the carbonylation of methanol in the presence of a Group VIII metal carbonylation catalyst to produce acetic acid are disclosed. More specifically, processes for reducing and/or removing PRC's or their precursors from intermediate streams during the formation of acetic acid by said carbonylation processes are disclosed. In particular, processes in which a low boiling overhead vapor stream from a light ends column is subjected to a distillation to obtain an overhead that is subjected to an extraction to selectively remove and/or reduce PRC's from the process is disclosed. The processes include steps of recycling one or more return streams derived from the distillation step and/or the extraction step to a light ends column and/or a drying column in order to improve water control in the overall reaction system.Type: ApplicationFiled: September 9, 2015Publication date: December 31, 2015Inventors: Ronald D. Shaver, Mark O. Scates, Raymond J. Zinobile
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Publication number: 20150376106Abstract: This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.Type: ApplicationFiled: September 10, 2015Publication date: December 31, 2015Applicant: United Therapeutics CorporationInventors: Hitesh BATRA, Sudersan M. TULADHAR, Raju PENMASTA, David A. WALSH
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Publication number: 20150376107Abstract: The invention pertains to a process for preparing methyl lactate inluding the steps of: bringing an aqueous liquid comprising lactic acid, methanol, and at least 5 wt. % of a dissolved chloride salt selected from magnesium chloride, calcium chloride, and zinc chloride to reaction conditions, thereby obtaining methyl lactate, wherein an extractant is provided to the reaction mixture before, during, and/or after formation of methyl lactate; subjecting the reaction mixture to a liquid-liquid separation step wherein an organic phase comprising methyl lactate and extractant is separated from an aqueous phase comprising dissolved chloride salt. The extractant preferably includes one or more compounds selected from C5+ ketones and C3-C10 ethers, in particular C5-C8 ketones, more in particular methyl isobutyl ketone. It has been found that the process according to the invention makes it possible to manufacture methyl lactate efficiently and in high yield.Type: ApplicationFiled: February 13, 2014Publication date: December 31, 2015Inventors: Jan VAN KRIEKEN, André Banier DE HAAN, Jan VAN BREUGEL
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Publication number: 20150376108Abstract: The invention relates to a method for the synthesis of a branched unsaturated fatty compound, said method comprising the metathesis, in the presence of a metathesis catalyst, of a linear unsaturated fatty compound and a branched olefin. The branched unsaturated fatty compound is used in particular for the production of at least one of the following products: dielectric fluids, specialty surfactants, emulsifiers, frictions agents, antistatic additives, antifogging additives, mould release agents, pigment dispersants, high-performance lubricants, waxes and wax emulsifiers, polymer conversion additives, PVC stabilising agents, inks, resins, paints, varnishes, solvents, lipsticks, creams for the skin, deodorants, particularly stick deodorants, hair dyes, shampoos and other liquid soaps, shaving foam, laundry detergents, cleaning agents, fabric softeners, and mixtures of same.Type: ApplicationFiled: February 10, 2014Publication date: December 31, 2015Applicant: Arkema FranceInventors: Jean-Luc DUBOIS, Jean-Luc COUTURIER
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Publication number: 20150376109Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment and prevention of stroke and the sequelae of stroke. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent to yield more effective treatment tools to treat or prevent stroke and the long term effects of stroke in mammalian subjects.Type: ApplicationFiled: September 3, 2015Publication date: December 31, 2015Inventor: Richard L. Chang
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Publication number: 20150376110Abstract: Disclosed is a fullerene derivative represented by the following formula (1): wherein FLN is a fullerene backbone, R1 is a substituted or non-substituted alkyl group with a carbon number less than or equal to 24, and Ar1 is a substituted or non-substituted aryl group with a carbon number less than or equal to 24.Type: ApplicationFiled: June 26, 2014Publication date: December 31, 2015Inventors: Tienan JIN, Weili SI, Yoshinori YAMAMOTO, Takeshi IGARASHI
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Publication number: 20150376111Abstract: The invention relates to a process for preparing nitroalkanes by reaction of at least one alkane with at least one nitrating agent in the gas phase, wherein the nitration is carried out in a microstructured reaction zone having parallel channels having hydraulic diameters of less than 2.5 mm and a total specific internal surface area of more than 1600 m2/m3 and the alkane and the nitrating agent are conveyed under a pressure of from 1 bar to 20 bar through the reaction zone and reacted at a temperature of from 150° C. to 650° C. and the reaction products are cooled downstream of the reaction zone and discharged and the at least one nitrating agent is introduced over from two to ten introduction points along the reaction zone.Type: ApplicationFiled: April 25, 2014Publication date: December 31, 2015Applicant: BASF SEInventors: Ralf BOEHLING, Michael HAYER, Alwin REHFINGER, Michael SCHELPER, Johann-Peter MELDER, Martin ERNST, Joaquim Henrique TELES
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Publication number: 20150376112Abstract: A photoactivatable caged compound (TPE-C) with AIE characteristics is designed and synthesized. TPE-C is non-emissive either in solution or in aggregated state, but its luminescence can be induced to emit strong cyan emission in aggregated state by UV irradiation. Such property enables TPE-C to be applied in photo-patterning and anti-counterfeiting related areas.Type: ApplicationFiled: June 26, 2015Publication date: December 31, 2015Inventor: Benzhong TANG
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Publication number: 20150376113Abstract: The present invention relates to a method for reducing the production of methane emanating from the digestive activities of a ruminant and/or for improving ruminant animal performance by using, as active compound at least one organic molecule substituted at any position with at least one nitrooxy group, or a salt thereof, which is administrated to the animal together with the feed. The invention also relates to the use of these compounds in feed and feed additives such as premix, concentrates and total mixed ration (TMR) or in the form of a bolus.Type: ApplicationFiled: September 8, 2015Publication date: December 31, 2015Inventors: Stephane DUVAL, Maik KINDERMANN
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Publication number: 20150376114Abstract: A compound for an organic electroluminescent device and an organic electroluminescent device, the compound being represented by the following Formula 1:Type: ApplicationFiled: May 19, 2015Publication date: December 31, 2015Inventor: Naoya SAKAMOTO
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Publication number: 20150376115Abstract: Compounds are provided having the following structure: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6, R7, R8, R9, L1, L2, a, b, c, d and e are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.Type: ApplicationFiled: June 5, 2015Publication date: December 31, 2015Inventors: Steven M. Ansell, Xinyao Du
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Publication number: 20150376116Abstract: The present invention provides novel polymerizable monomers having chelating functionality and processes to make them. In particular, the novel monomers are ethylenically unsaturated aminocarboxylates and are prepared by reacting ethylenediamine triacetic acid or its salt with an ethylenically unsaturated monomer. The ethyleneically unsaturated monomer may be a polymerizable vinyl monomer selected from (o-, p-, m-)DVBMO, allyl glycidyl ether, and glycidyl (meth)acrylate.Type: ApplicationFiled: August 6, 2015Publication date: December 31, 2015Inventors: Scott Backer, Allen Bulick, Joseph Manna, Cynthia Rand, Jia Xie
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Publication number: 20150376117Abstract: Herein described are deuterated catecholamine derivatives of the general Formula (I) wherein R1 is deuterium, R2, and R3 are independently selected from hydrogen and deuterium and wherein at least one of R2 and R3 has a deuterium enrichment in the range from 0.02 mol % to 100 mol % deuterium, and wherein the deuterium enrichment of R2 and R3 is different from each other and that the difference between the deuterium enrichment of R2 and R3 is at least 5 percentage points, R4 is hydrogen, deuterium, C1 to C6-alkyl or C5 to C6-cycloalkyl, deuterated C1 to C6-alkyl or C5 to C6-cycloalkyl, or a group that is easily hydrolytically or enzymatically cleavable under physiological conditions, as well as their physiologically acceptable salts and their stereoisomers, enantiomeres or diastereomers in optically pure form. The compounds can easily be prepared by mixing deuterated and non-deuterated compounds in a predefined ratio. The compounds show anti-Parkinson effect at lower doses and show lower side effects.Type: ApplicationFiled: February 5, 2014Publication date: December 31, 2015Inventors: Rudolf-Giesbert ALKEN, Frank SCHNEIDER
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Publication number: 20150376118Abstract: Fatty amide compositions and their derivatives are disclosed. The fatty amides comprise a reaction product of a metathesis-derived C10-C17 monounsaturated acid, octadecene-1,18-dioic acid, or their ester derivatives with a primary or secondary amine. Derivatives made by reducing, quaternizing, sulfonating, alkoxylating, sulfating, and sulfitating the fatty amide are also included. The amine reactant can be diethylenetriamine or (2-aminoethyl)ethanolamine, which provide imidazoline amides or esters, respectively. In one aspect, the ester derivative of the C10-C17 monounsaturated acid or octadecene-1,18-dioic acid is a lower alkyl ester. In other aspects, the ester derivative is a modified triglyceride made by self-metathesis of a natural oil or an unsaturated triglyceride made by cross-metathesis of a natural oil with an olefin. The compositions are valuable for cleaners, fabric treatment, hair conditioning, personal care, antimicrobial compositions, agricultural uses, and oil field applications.Type: ApplicationFiled: September 8, 2015Publication date: December 31, 2015Inventors: Dave R Allen, Marcos Alonso, Randal J Bernhardt, Aaron Brown, Kelly Buchek, Sangeeta Ganguly-Mink, Brian Holland, Gary Luebke, Renee Luka, Andrew D. Malec, Ronald A Masters, Dennis S Murphy, Irene Shapiro, Patti Skelton, Brian Sook, Michael R Terry, Gregory Wallace, Laura Lee Whitlock, Michael Wiester, Patrick Shane Wolfe, Lena Titievsky
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Publication number: 20150376119Abstract: Provided is a compound which thickens or gels a fluid organic material to a desired viscosity, or which uniformly stabilizes the formulation of a composition containing the fluid organic material. The compound according to the present invention is represented by Formula (1): R1—(CONH—R2)n ??(1) where R1 represents an n-valent aromatic hydrocarbon group containing two or more benzene rings; R2 represents an aliphatic hydrocarbon group containing 6 or more carbon atoms; and n represents an integer of 4 or more. The group R1 is preferably a group corresponding to an aromatic hydrocarbon selected from the group consisting of benzophenone, biphenyl, and naphthalene, except for removing hydrogen atoms in a number of n from the aromatic hydrocarbon. A thickening/stabilizing agent according to the present invention includes the compound.Type: ApplicationFiled: February 4, 2014Publication date: December 31, 2015Applicants: YAMAGUCHI UNIVERSITY, DAICEL CORPORATIONInventors: Yuichi SAKANISHI, Takashi SAEKI, Yusuke NARUSAKA, Mami ITOH
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Publication number: 20150376120Abstract: Antibiotically active compounds characterized by general formula (I), wherein X1, BB, BC, BD, BE and X2 are building blocks with D1, D2, D3, D4 or D5 being linkers which include carbon, sulphur, nitrogen, phosphor and/or oxygen atoms and which are covalently connecting the moities BA and BB, BB and BC, BC and BD, BD and BE and BE and BF, respectively, and wherein in particular the building block BC comprises an amino acid derivative. The compounds for use in a method of treatment of diseases, in particular for use in a method of treatment of bacterial infections are also disclosed.Type: ApplicationFiled: February 14, 2014Publication date: December 31, 2015Inventors: Roderich SÜSSMUTH, Julian KRETZ, Vivien SCHUBERT, Alexander PESIC, Manuela HÜGELLAND, Monique ROYER, Stéphane COCIANCICH, Philippe ROTT, Dennis KERWAT, Stefan GRÄTZ
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Publication number: 20150376121Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having 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.Type: ApplicationFiled: June 29, 2015Publication date: December 31, 2015Applicant: REATA PHARMACEUTICALS, INC.Inventors: Eric ANDERSON, Xin JIANG, Melean VISNICK
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Publication number: 20150376122Abstract: The present disclosure concerns synthesis and anion binding features of poly-cyanostilbene macrocycles of Formula (I):Type: ApplicationFiled: February 13, 2014Publication date: December 31, 2015Inventors: Amar H. Flood, Semin Lee, Kevin McDonald
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Publication number: 20150376123Abstract: A biguanide derivative compound with N4-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPK and inhibition of cancer cell proliferation in a low dose, compared with conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.Type: ApplicationFiled: September 8, 2015Publication date: December 31, 2015Inventors: Sung Wuk Kim, Sung Soo Jun, Chang Hee Min, Se Hwan Park, Yong Eun Kim, Duck Kim, Ji Sun Lee, Ju Hoon Oh
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Publication number: 20150376124Abstract: Anti-cancer compositions and methods are described including one or more isothiocyanates and/or isoselenocyanates. Methods of treating a subject are provided according to embodiments of the present invention which include administering a therapeutically effective amount of a composition including an isothiocyanate and/or isoselenocyanate to a subject having a condition characterized by Akt dysregulation. Administering a therapeutically effective amount of a composition including an isothiocyanate and/or isoselenocyanate to a subject detectably increases apoptosis and/or decreases proliferation of cancer cells, particularly cancer cells characterized by Akt dysregulation.Type: ApplicationFiled: June 30, 2015Publication date: December 31, 2015Inventors: Gavin P. Robertson, Arati K. Sharma, Arun K. Sharma, Shantu G. Amin, Dhimant H. Desai
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Publication number: 20150376125Abstract: The present invention provides tromethamine salt of (Z)-7-[3,5-Dihydroxy-2-((E)-3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-hept-5-enoic acid in crystalline Form 1 and amorphous form. This compound is may also be referred to as “tromethamine salt of bimatoprost acid.” The invention crystalline form is useful for solid ocular implant or topical formulations, utilized in the treatment of various ocular conditions, such as, for example, ocular hypertension.Type: ApplicationFiled: June 27, 2014Publication date: December 31, 2015Inventors: Thomas K. Karami, Scott W. Smith, Fiona Dubas-Fisher, Adrian St.Clair Brown
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Publication number: 20150376126Abstract: A method is described for the synthesis of 4-piperidin-4-yl-benzene-1,3-diol of the following formula (I): and the pharmaceutically acceptable salts thereof.Type: ApplicationFiled: February 14, 2014Publication date: December 31, 2015Applicant: Galderma Research & DevelopmentInventors: Jean-Guy BOITEAU, Branislav MUSICKI
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Publication number: 20150376127Abstract: A process for preparing a compound represented by the following general formula (I) or a salt thereof, which comprises reacting lysine or a protective product thereof or a salt thereof with allysine or a protective product thereof in the presence of a specific trifluoromethane sulfonate to obtain a compound having pyridine ring or a salt thereof. (wherein, in the above-described general formula (I), one of R1 and R2 is —CH2CH2CH2CH(NH2)COOH group, and the other is hydrogen atom. And wherein, in the above-described general formula (I), one, or two or more of hydrogen atom, one, or two or more of carbon atom, or one, or two or more of nitrogen atom may be substituted with their isotope.Type: ApplicationFiled: January 24, 2014Publication date: December 31, 2015Inventor: Toyonobu USUKI
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Publication number: 20150376128Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X 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 processes and intermediates for preparing such compounds.Type: ApplicationFiled: June 25, 2015Publication date: December 31, 2015Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
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Publication number: 20150376129Abstract: The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them.Type: ApplicationFiled: February 7, 2014Publication date: December 31, 2015Applicant: DRACONIS PHARMA, S.L.Inventors: Marina VIRGILI BERNADO, Elena CARCELLER GONZALEZ, Jordi SALAS SOLANA
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Publication number: 20150376130Abstract: Compounds of formula I, wherein A, B, X, Z and R1-R6, are as defined in the claims, exhibit TRPA 1 activity and are thus useful as TRPA1 modulators.Type: ApplicationFiled: September 30, 2013Publication date: December 31, 2015Applicant: Orlon CorporationInventors: Riina ARVELA, Terhi HEIKKINEN, Patrik HOLM, Peteris PRUSIS, Mattias ROSLUND, Harri SALO
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Publication number: 20150376131Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: September 2, 2015Publication date: December 31, 2015Inventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
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Publication number: 20150376132Abstract: The present disclosure relates to quinoline sulfonyl compounds, compositions comprising these compounds and their use, in particular for the treatment of cancer.Type: ApplicationFiled: February 18, 2014Publication date: December 31, 2015Inventors: Hoyun Lee, Viswas Raja Solomon, Sheetal Pundir
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Publication number: 20150376133Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: September 8, 2015Publication date: December 31, 2015Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
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Publication number: 20150376134Abstract: The present invention provides process for the preparation of ivacaftor and solvates thereof.Type: ApplicationFiled: January 30, 2014Publication date: December 31, 2015Applicant: Glenmark Pharmaceuticals LimitedInventors: Shekhar Bhaskar BHIRUD, Samir NAIK, Sachin SRIVASTAVA, Ramesh Santosh BADGUJAR, Sachin LAD, Sukumar SINHA, Mohammad Amjed KHAN
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Publication number: 20150376135Abstract: The present invention relates to a process for the preparation of bisdihaloalkyl pyrazoles of formula (V) starting from diketones and acylhalides reacted with a Lewis acid, and a subsequent reaction with a substituted hydrazine.Type: ApplicationFiled: February 7, 2014Publication date: December 31, 2015Applicant: Syngenta Participations AGInventors: Anup JAWALEKAR, Helmars SMITS, Laura QUARANTA, Sitaram PAL, David Anthony JACKSON
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Publication number: 20150376136Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formulae (Ia), (Ib) and (Ic), and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.Type: ApplicationFiled: February 19, 2014Publication date: December 31, 2015Inventors: Lyudmyla Chumakova, Andrew Patron, Chad Priest, Donald Karanewsky, Rachel Kimmich, Brant Clayton Boren, Jeffrey Robert Hammaker, Volodymyr Chumakov, Wen Zhao, Alain Noncovich, Jane Ung
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Publication number: 20150376137Abstract: A production method of the present invention is a method for producing a halohydantoin compound in which method a composition including a halohydantoin compound and an impurity is treated, the method including the step of adding the composition to a mixed solvent of water and an organic solvent and washing the composition.Type: ApplicationFiled: November 15, 2013Publication date: December 31, 2015Inventors: Naoki Fujiwara, Keisuke Takahashi
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Publication number: 20150376138Abstract: The present invention provides a process for producing a compound of the formula (1) wherein X represents a hydrogen atom, etc., and Y represents a hydrogen atom, etc., which comprises step 1 of reacting a compound of the formula (2) and a compound of the formula (3) in the presence of a Lewis acid wherein R represents a hydrogen atom, etc., to obtain an adduct, and step 2 of reacting the adduct obtained in the step 1 and hydrazine to obtain the compound of the formula (1).Type: ApplicationFiled: February 18, 2014Publication date: December 31, 2015Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yasuyuki NAKAE, Akio MANABE, Takashi MIYAMOTO
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Publication number: 20150376139Abstract: Disclosed are compounds that modulate the physiological action of the proprotein convertase subtilisin kexin type 9 (PCSK9), and methods of using these modulators to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease (CVD), including treatment of hypercholesterolemia.Type: ApplicationFiled: March 11, 2014Publication date: December 31, 2015Inventors: Sherin Salaheldin Abdel-Meguid, Magid Abou-Gharbia, Benjamin Blass, Wayne Childers, Nabil Elshourbagy, Victor Ghidu, Rogelio Martinez, Harold Meyers, Shaker A. Mousa
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Publication number: 20150376140Abstract: This invention relates to 2-aminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.Type: ApplicationFiled: February 20, 2014Publication date: December 31, 2015Applicant: Janssen Infections Diseases BVBA,Inventors: David Craig Mc Gowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers
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Publication number: 20150376141Abstract: The present invention encompasses compounds of general formula (1) wherein A, B, X, R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: September 4, 2015Publication date: December 31, 2015Inventors: Heinz STADTMUELLER, Ioannis SAPOUNTZIS
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Publication number: 20150376142Abstract: Processes for the preparation of 4-amino-1((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-hydroxymethyl-cyclopent-2-enyl)-1H-pyrimidin-2-one (13, RX-3117) and its intermediates are described.Type: ApplicationFiled: September 4, 2015Publication date: December 31, 2015Inventors: Haifeng Yin, Deog Joong Kim, Eliezer Falb, Leigh Andre Pearcey, Jonathan Cummins, Petra Dieterich, Jean-Francois Carniaux, Yi Wang, Vikram Chandrakant Purohit
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Publication number: 20150376143Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.Type: ApplicationFiled: June 30, 2015Publication date: December 31, 2015Inventors: Laura Cook Blumberg, Julius F. Remenar, Orn Almarsson, Tarek A. Zeidan
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Publication number: 20150376144Abstract: Provided, in part, is a composition comprising one or more chemical entities of formula I, each of which is a compound of formula I: a pharmaceutically acceptable salt thereof, a solvate thereof, or a solvate of a pharmaceutically acceptable salt thereof, the composition characterized in that greater than a first threshold amount of the total amount of chemical entities of formula I in the composition: are chemical entities of formula I.a, wherein the first threshold amount is 50%; or are chemical entities of formula I.b.1, wherein the first threshold amount is 25%; or are chemical entities of formula I.b.2, wherein the first threshold amount is 25%, wherein the chemical entities of formula I.a, I.b.1, and I.b.2, are described herein, and methods of using such compositions, for example, for the delivery of a polynucleotide in vivo.Type: ApplicationFiled: June 24, 2015Publication date: December 31, 2015Inventors: Frank DeRosa, Shrirang Karve, Michael Heartlein