Patents Issued in June 22, 2017
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Publication number: 20170174597Abstract: A method for preparing a phenolic oligomer antioxidant with a very small residual content of butylated hydroxytoluene (BHT) is provided. Specifically, the method for preparing the phenolic oligomer antioxidant relates to a method which is capable of a BHT-free phenolic oligomer antioxidant or a phenolic oligomer antioxidant containing a trace amount of residual BHT by removing the precursor of BHT as much as possible by performing the concentration under the reduced pressure while injecting an inert gas to an intermediate product and/or removing BHT by performing the concentration under the reduced pressure while injecting an inert gas to the final product.Type: ApplicationFiled: August 4, 2016Publication date: June 22, 2017Inventors: Hyung Jae LEE, Chang Kyo SHIN, Seok Hyun KANG, Kyoung Ho ROW, Ji Hyun HEO
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Publication number: 20170174598Abstract: Various embodiments disclosed relate to methods and apparatus for synthesizing various biphenols. In various embodiments, the present invention provides a method of making a bisphenol including feeding a phenol at or proximate to the first end of a reactor column including a first end and a second end and including a solid catalyst distributed in multiple locations between the first end and the second end of the reactor column. The method includes feeding an oxomethylene compound to the reactor column at a first location that is at or proximate the first end and at one or more additional locations between the first location and the second end of the reactor column, and removing at least some water from the reactor column. The method includes removing a product composition including a diphenolmethylene product at or proximate to the second end of the reactor column.Type: ApplicationFiled: July 14, 2015Publication date: June 22, 2017Applicant: SABIC GLOBAL TECHNOLOGIES B.V.Inventors: Arun Vasant Manchekar, Samir Anapat, Martin Oyevaar
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SYSTEMS AND METHODS FOR MANUFACTURE OF DIMETHYL ETHER (DME) FROM NATURAL GAS AND FLARE GAS FEEDSTOCK
Publication number: 20170174599Abstract: Disclosed is a method that reforms flare gas or other raw natural gas source, using air without steam, to directly produce dimethyl ether (DME), a direct diesel substitute. The method first reforms an air-natural gas mixture at ambient atmospheric pressures, and then compresses the resulting CO-hydrogen-nitrogen gas mixture to 100-2,000 psi, and feeds it through a combined reactor which reacts the gas mixture directly into DME. The nitrogen is returned to the atmosphere. DME is an excellent diesel fuel, and can be used to displace significantly costlier and dirtier petroleum-based diesel fuel, while solving a critical problem with flaring or other wasted natural gas. For example, the roughly 120 billion cubic feet per year that was flared in North Dakota in 2014 could be converted into over 3 million tons of DME using the disclosed method.Type: ApplicationFiled: March 1, 2017Publication date: June 22, 2017Inventors: Robert M. Zubrin, Boris Nizamov, Thomas L. Henshaw, Adam M. Kortan, James Siebarth, Colin Apke, Mark Berggren -
Publication number: 20170174600Abstract: The present disclosure provides phenolic compounds useful in the treatment of neurological conditions such as convulsions and tremors, having the structure of Formula (I): wherein R2, R4, & R5, are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating neurological conditions.Type: ApplicationFiled: February 27, 2017Publication date: June 22, 2017Inventors: Max Baker, Rajesh Kumar Mishra, John J. Talley, Eduardo J. Martinez
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Publication number: 20170174601Abstract: The invention relates to Rh, Ru, Co and Ir complexes comprising bidentate diphosphoramidites as ligands and to the use thereof as catalysts for the hydroformylation of olefins. The invention also relates to a process for preparing an aldehyde from an olefin using the complexes or ligands mentioned.Type: ApplicationFiled: December 16, 2016Publication date: June 22, 2017Applicant: EVONIK DEGUSSA GMBHInventors: Katrin Marie DYBALLA, Robert FRANKE, Dirk FRIDAG, Dieter HESS, Frank GEILEN, Galina Morales TORRES, Detlef SELENT, Armin BÖRNER
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Publication number: 20170174602Abstract: Cyclohexenone and cyclohexenol compounds are provided having specific fragrances and remanence properties, along with methods for synthesizing these compounds, including obtaining the compound by condensing a ketone on an ?-methylene-aldehyde in order to obtain, by means of a domino reaction, compounds of formula (II) as follows:Type: ApplicationFiled: March 8, 2017Publication date: June 22, 2017Inventors: Jean-Jacques CHANOT, Caroline PLESSIS
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Publication number: 20170174603Abstract: The present invention relates to a process for reacting chemical compounds comprising the step of reacting a compound of formula (IV) wherein Hal is independently selected from CI or Br, and X? is a monovalent anion, in the presence of an inorganic acid, wherein the aqueous inorganic acid has a concentration of at least about 60%, at a temperature of about 140° C. to Cabout 250° C., to obtain a compound of formula (V) wherein Hal is as defined above.Type: ApplicationFiled: May 18, 2015Publication date: June 22, 2017Inventors: Andreas PLETSCH, Nicole HOLUB, Thomas ULRICH, Petr KVITA, Laurent CAVIN
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Publication number: 20170174604Abstract: A process for recovering (meth)acrylic acid includes distilling a mixture comprising (meth)acrylic acid in a finishing column at less than atmospheric pressure to produce a finishing column overhead stream and a finishing column bottoms stream. An overhead aspirating direct contact condenser system at least partially condenses the finishing column overhead stream to form a finishing column overhead condensate and an overhead non-condensables vent stream. A finishing column vapor-phase side draw may also be recovered. An aspirating direct contact condenser system may be used to at least partially condense the vapor-phase side draw.Type: ApplicationFiled: February 12, 2015Publication date: June 22, 2017Inventor: Michael S. DECOURCY
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Publication number: 20170174605Abstract: Process for the recovery of carboxylic acid, in particular acetic acid containing carboxylic anhydride in particular acetic anhydride and other impurities, which comprises: (a) treating a fraction, in particular a fraction originating from a wood treatment process, containing carboxylic acid and impurities with a metal salt in the presence of water, (b) treating at least part of the fraction obtained from step (a) to remove metal salt and, (c) treating at least part of the fraction obtained from step (b) by distillation, stripping or membrane separation to recover at least a purified carboxylic acid fraction.Type: ApplicationFiled: May 6, 2015Publication date: June 22, 2017Applicant: SOLVAY ACETOW GmbHInventors: Thomas KRUMREY, Andreas HUMMEL
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Publication number: 20170174606Abstract: Methods, compositions, and systems related to preparing gaseous 18F-compounds for use in radiolabeling positron emission tomography (PET) tracer precursor compounds are disclosed. [18F]fluoride ions produced by conventional methods are converted by reaction with an acid anhydride having the formula: to a gaseous 18F-compound having the formula: wherein each R is independently a substituted or unsubstituted, straight chain or branched CrC4 alkyl group. The resulting gaseous 18F-compounds can be produced and stored in close proximity to the production location of the [18F]fluoride ions (such as within a cyclotron vault), or easily and efficiently transported long distances with minimal loss of-radioactivity.Type: ApplicationFiled: March 18, 2015Publication date: June 22, 2017Inventors: TIMOTHY R. DEGRADO, Huailel Jiang
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Publication number: 20170174607Abstract: Copper(II) bromide mediated oxidation of acylated enol and use of the reaction in the synthesis of ?,?-unsaturated or ?-bromo ketones or aldehydes are disclosed. The method provides an efficient and practical process for manufacturing dehydrohedione (DHH) and many other versatile ?,?-unsaturated or ?-bromo ketones or aldehydes in large scales to avoid using precious metal compounds.Type: ApplicationFiled: December 19, 2016Publication date: June 22, 2017Inventors: Ian R. Baxendale, James S. Sharley, Amadeo Fernández Miranda, Ana Maria Collado Pérez
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Publication number: 20170174608Abstract: The invention relates to a method of alkene metathesis. In the method, at least one monoalkene is subjected to ethenolysis in the presence of a diene. The invention also relates to the use of a diene to promote an ethenolysis reaction conducted on a monoalkene.Type: ApplicationFiled: January 28, 2015Publication date: June 22, 2017Inventors: Jennifer Julis, Stuart Bartlett, David John Cole-Hamilton
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Publication number: 20170174609Abstract: The invention relates to a process for doubly carbonylating allyl ethers to the corresponding diesters, wherein a linear or branched allyl ether is reacted with a linear or branched alkanol (alcohol) with supply of CO and in the presence of a catalytic system composed of a palladium complex and at least one organic phosphorus ligand and in the presence of a hydrogen halide selected from HCl, HBr and HI.Type: ApplicationFiled: December 14, 2016Publication date: June 22, 2017Applicant: EVONIK DEGUSSA GMBHInventors: Jie LUI, Li HAOQUAN, Matthias BELLER, Ralf JACKSTELL, Robert FRANKE, Katrin Marie DYBALLA
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Publication number: 20170174610Abstract: The invention relates to a process for doubly carbonylating allyl alcohols to the corresponding diesters, wherein a linear or branched allyl alcohol is reacted with a linear or branched alkanol (alcohol) with supply of CO and in the presence of a catalytic system composed of a palladium complex and at least one organic phosphorus ligand and in the presence of a hydrogen halide selected from HCl, HBr and HI.Type: ApplicationFiled: December 14, 2016Publication date: June 22, 2017Applicant: EVONIK DEGUSSA GMBHInventors: Li HAOQUAN, Jie LUI, Matthias BELLER, Ralf JACKSTELL, Robert FRANKE, Katrin Marie DYBALLA
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Publication number: 20170174611Abstract: A compound of Formula I or pharmaceutically acceptable salt thereof and its preparation method and applications, the new structure of the compound of formula I has not been reported in literature. It is isolated from Isodon forrestii var. forrestii and can be a compound served as Trx1 selective inhibitor. The present invention further discloses a pharmaceutical composition, preparation of the compound of Formula I and its applications in preparing medicines for preventing or treating cancer. Iso A of the present invention has the advantages of low toxicity, high safety and strong pharmacological effect, which suggests a potential prospect in pharmaceutical applications.Type: ApplicationFiled: February 14, 2017Publication date: June 22, 2017Inventors: PENG CAO, Jianxin PU, Xiaoyan SUN, Handong SUN, Weiguang WANG, Jiao CHEN, Xueting CAI, Xue DU
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Publication number: 20170174612Abstract: The present invention relates to a process for the continuous production of nitrobenzene by the nitration of benzene with nitric acid and sulphuric acid under adiabatic conditions, not the entire production plant being shut down during a production stop, but the production plant being entirely or at least partly operated in recirculation mode. The invention further relates to a plant for producing nitrobenzene and to a method for operating a plant for producing nitrobenzene.Type: ApplicationFiled: June 22, 2015Publication date: June 22, 2017Inventors: Thomas Knauf, Peter Drinda
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Publication number: 20170174613Abstract: Methods of preparing a fenfluramine active pharmaceutical ingredient are provided. Aspects of the method include (a) hydrolyzing a 2-(3-(trifluoromethyl)phenyl)acetonitrile composition to produce a 2-(3-(trifluoromethyl)phenyl)acetic acid composition; (b) reacting the 2-(3-(trifluoromethyl)phenyl)acetic acid composition with acetic anhydride and a catalyst to produce a 1-(3-(trifluoromethyl)phenyl)propan-2-one composition; and (c) reductively aminating the 1-(3-(trifluoromethyl)phenyl)propan-2-one composition with ethylamine using a borohydride reducing agent to produce a fenfluramine composition. Also provided are compositions and pharmaceutical ingredients prepared according to the subject methods including a pharmaceutically acceptable salt of fenfluramine and having less than 0.2% by weight in total of trifluoromethyl regioisomers.Type: ApplicationFiled: December 20, 2016Publication date: June 22, 2017Applicant: ZOGENIX INTERNATIONAL LIMITEDInventors: Derek J. LONDESBROUGH, Marc W. ANDERSEN
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Publication number: 20170174614Abstract: Metabolism-resistant fenfluramine analogs are provided. The subject fenfluramine analogs find use in the treatment of a variety of diseases. For example, methods of treating epilepsy by administering a fenfluramine analog to a subject in need thereof are provided. Also provided are methods of suppressing appetite in a subject in need thereof. Pharmaceutical compositions for use in practicing the subject methods are also provided.Type: ApplicationFiled: December 20, 2016Publication date: June 22, 2017Applicant: ZOGENIX INTERNATIONAL LIMITEDInventors: Stephen J. FARR, Brooks M. BOYD
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Publication number: 20170174615Abstract: A compound represented by the formula: wherein R is selected from the group consisting of (i) substituted or unsubstituted alkyl with C=0 to 12 inclusive; (ii) substituted or unsubstituted aryl; and (iii) substituted and unsubstituted alkylaryl; wherein X1, X2, X3 and X4 are each selected from the group consisting of alkyl, aryl, alkylaryl groups and hydrogen; wherein R1, R2, R3, and R4 are each selected from the group consisting of alkyl, aryl, alkylaryl groups and hydrogen and R2 and R3 may optionally be bridged by a polymethylene group; wherein when C=0 in R, the combined group R1 R2 is the same as the combined group R3 R4; and wherein when C=1 in R, each of R1, R2, R3, and R4 are hydrogen.Type: ApplicationFiled: December 7, 2016Publication date: June 22, 2017Applicant: Eastman Chemical CompanyInventors: MATTHEW ALLEN BOONE, Donald L. Fields, JR., Frederick lgnatz-Hoover
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Publication number: 20170174616Abstract: Systems and method are provided for reducing the water content from approximately 0.15%-0.19% by weight to approximately 0.01-0.03% by weight in an ethanolamine product stream in a non-reactive distillation column. The reduced water content can be achieved by increasing the processing conditions at the drying column by approximately 5% to approximately 20%, more preferably to approximately 10%. The increased processing conditions at the drying column can result in an increased bottom stream flow rate and an increased reboiler duty. The reboiler duty of the drying column can be increased by up to 2% to achieve said level of water content. The bottom stream flow rate can be increased by up to approximately 12% to achieve said level of water content.Type: ApplicationFiled: April 2, 2015Publication date: June 22, 2017Inventor: Naeem AL-HAZMI
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Publication number: 20170174617Abstract: Isolated metabolites of (1R-trans)-N-[[2-(2,3-dihydro-4-benzofuranyl)cyclopropyl]-methyl]propanamide, methods for their use, and compositions containing the metabolites.Type: ApplicationFiled: March 2, 2017Publication date: June 22, 2017Inventors: Marlene Michelle Dressman, Deepak Phadke
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Publication number: 20170174618Abstract: The present invention relates generally to an eco-friendly methodology for the conversion of alcohols and aldehydes to amines and amides using an integrated enzyme cascade system with metal- and organocatalysis. More specifically, the present invention relates to synthesis of capsaicinoids starting from vanillin alcohol and using a combination of an enzyme cascade system and catalysts. Furthermore, the method also relates to synthesis of capsaicinoids derivatives starting from vanillin alcohol derivatives and using a combination of an enzyme cascade system and catalysts.Type: ApplicationFiled: March 27, 2015Publication date: June 22, 2017Inventors: Armando CÓRDOVA, Per BERGLUND, Mattias ANDERSON, Samson AFEWERKI
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Publication number: 20170174619Abstract: The instant invention describes hydrazide-containing compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdifferentiation.Type: ApplicationFiled: March 30, 2015Publication date: June 22, 2017Inventors: Daiqing Liao, William R. Roush, Ryan L Stowe
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Publication number: 20170174620Abstract: Provided are compositions comprising linked diaryl compounds that possess anticancer properties. Methods of use are also disclosed herein. The method comprises administering an effective amount of a compound described herein to an individual in need thereof.Type: ApplicationFiled: July 22, 2015Publication date: June 22, 2017Inventors: Herman O. SINTIM, Shizuka NAKAYAMA, Dimpy KALIA, Jie ZHOU, Min GUO, Jinbing LIU, Changhao WANG, Rena LAPIDUS
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Publication number: 20170174621Abstract: Provided are dental polymerizable monomers that can give cured products having high toughness and high rigidity, dental polymerizable monomer compositions containing the polymerizable monomers, and dental compositions containing the dental polymerizable monomer compositions, and cured products thereof having high mechanical properties. The dental polymerizable monomer (A) which includes a urethane acrylate obtained from an appropriately rigid diisocyanate and an appropriately flexible hydroxyacrylate is used to prepare a dental polymerizable monomer composition containing the dental polymerizable monomer, and a dental composition containing the dental polymerizable monomer composition.Type: ApplicationFiled: March 31, 2015Publication date: June 22, 2017Applicants: MITSUI CHEMICALS, INC., SHOFU INC., SUN MEDICAL CO., LTD.Inventors: Kazuhiko YOSHINAGA, Hiroshi NARUSE, Mitsuji TERAMAE, Kiyomi FUCHIGAMI, Hidefumi FUJIMURA, Masuji TSUCHIKAWA, Hirofumi IMAI
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Publication number: 20170174622Abstract: A tri-carbobenzoxy-arginine represented by the following formula (2): is produced by carbobenzoxylating the arginine or arginine derivative (1) represented by the following formula (1), or a salt thereof: by adding carbobenzoxy chloride and a base in a water/organic solvent bilayer system to an arginine or arginine derivative (1) represented by the formula (1), or a salt thereof.Type: ApplicationFiled: March 23, 2015Publication date: June 22, 2017Applicant: KANEKA CORPORATIONInventors: Koji MACHIDA, Kohei MORI, Narumi KISHIMOTO, Toshihiro TAKEDA
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Publication number: 20170174623Abstract: Organosulfur compounds and compositions are disclosed which can be administered in order to provide protection from the formation of aldehyde-protein adducts, protein aggregates, and the resulting neuroinflammation. Various neurodegenerative diseases which are suitable for treatment using these compositions include Alzheimer's disease, senile dementia, Parkinson's disease, multiple sclerosis, Lewy body disease, peripheral neuropathy, spinal cord injury, traumatic brain injury, stroke and cerebral ischemia.Type: ApplicationFiled: March 1, 2017Publication date: June 22, 2017Inventor: David Michael Ott
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Publication number: 20170174624Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: January 5, 2017Publication date: June 22, 2017Applicant: AbbVie Inc.Inventors: Dominique Bonafoux, Heather M. Davis, Kristine E. Frank, Michael M. Friedman, J. Martin Herold, Michael Z. Hoemann, Raymond Huntley, Augustine Osuma, George Sheppard, Gagandeep K. Somal, Jennifer Van Camp, Stacy A. Van Epps, Anil Vasudevan, Grier A. Wallace, Lu Wang, Lu Wang, Zhi Wang, Noel S. Wilson, Xiangdong Xu
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Publication number: 20170174625Abstract: Disclosed is a preparation method of nintedanib (I), comprising the following steps: carrying out a condensation reaction on 4-(R acetate-2-yl)-3-nitrobenzoate (II) and trimethyl orthobenzoate to obtain (E)-4-[(2-methoxybenzylidene) R acetate-2-yl]-3-nitrobenzoate (III); carrying out a substitution reaction on the compound (EI) and N-(4-aminophenyl)-N-methyl-2-(4-methyl piperazine-1-yl) acetamide (IV) under the action of an acid-binding agent to generate (Z)-4-{[2-(N-methyl-2-(4-methyl piperazine-1-yl) acetamido-aniline) benzylidene] R acetate-2-yl}-3-nitrobenzoate (V); and sequentially carrying out reduction reactions and cyc-lization reactions on the compound (V) to prepare the nintedanib (I). The preparation method has an easily obtained raw material and a simple process, is economical and environmentally friendly, and is suitable for industrial production.Type: ApplicationFiled: March 8, 2017Publication date: June 22, 2017Applicant: SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.Inventor: Xuenong XU
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Publication number: 20170174626Abstract: The present invention provides a new amorphous form of apremilast, pharmaceutical compositions comprising same, methods for preparation and use thereof in treating conditions mediated by inhibition of TNF-? production or inhibition of phosphodiesterase 4 (PDE4), e.g., psoriatic arthritis and other chronic inflammatory diseases.Type: ApplicationFiled: July 20, 2014Publication date: June 22, 2017Applicant: MAPI PHARMA LTD.Inventors: Shai RUBNOV, Ehud MAROM
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Publication number: 20170174627Abstract: The present invention relates to processes for preparing ?-aminosulfone compounds. The provided compounds are useful intermediates in the preparation of sulfone group containing isoindoline-based compounds, in particular apremilast.Type: ApplicationFiled: May 27, 2015Publication date: June 22, 2017Applicant: Lek Pharmaceuticals d.d.Inventors: Gaj Stavber, Jerome Cluzeau
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Publication number: 20170174628Abstract: Disclosed are a method for preparing a series of novel pyridine derivatives and a use thereof. Such derivatives can be used in the treatment of related diseases caused by mycobacteria, in particular diseases caused by pathogenic mycobacteria, such as Mycobacterium tuberculosis, Mycobacterium bovis, Mycobacterium avium and Mycobacterium marinum.Type: ApplicationFiled: July 9, 2015Publication date: June 22, 2017Inventors: Zhaozhong DING, Shuhui CHEN, Zhigang HUANG, Wei LUO, Zhe CAI, Yepeng WANG, Dongdong TANG
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Publication number: 20170174629Abstract: The present disclosure provides novel compounds, including compounds that bind to potassium channels, methods for their manufacture, and methods for their use, including their use to diagnose and/or assess traumatic brain injury and use to treat dymeylinating diseases, and/or in vivo imaging of the central neverous system, and to diagnose and/or assess the progression of MS or other diseases.Type: ApplicationFiled: March 7, 2017Publication date: June 22, 2017Inventors: Pedro Brugarolas, Brian Popko, Daniel Appelbaum, Chin-Tu Chen
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Publication number: 20170174630Abstract: Cure accelerators for anaerobic curable compositions, such as adhesives and sealants, are provided, and which are defined with reference to the compounds shown in structure I where A is CH2 or benzyl, R is C1-10 alkyl, R? is H or C1-10 alkyl, or R and R? taken together may form a four to seven membered ring fused to the benzene ring, R? is optional, but when R? is present, R? is halogen, alkyl, alkenyl, cycloalkyl, hydroxyalkyl, hydroxyalkenyl, alkoxy, amino, alkylene- or alkenylene-ether, alkylene (meth)acrylate, carbonyl, carboxyl, nitroso, sulfonate, hydroxyl or haloalkyl, and EWG is as shown, an electron withdrawing group, such as nitro, nitrile, carboxylate or trihaloalkyl.Type: ApplicationFiled: March 8, 2017Publication date: June 22, 2017Inventor: Philip T. Klemarczyk
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Publication number: 20170174631Abstract: A compound expressed by any one of Structural Formulas (1) to (13), a method for producing the same, and a compound-containing composition, an anti-cancer agent, and an anti-Helicobacter pylori agent each containing the above compound.Type: ApplicationFiled: March 1, 2017Publication date: June 22, 2017Inventors: Manabu KAWADA, Hikaru ABE, Takumi WATANABE, Hiroyuki INOUE, Shun-ichi OHBA, Chigusa HAYASHI, Masayuki IGARASHI
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Publication number: 20170174632Abstract: The present invention is directed to new compounds selectively binding the cannabinoid 2 receptor. In addition, the invention relates to the use of said compounds for determining cannabinoid receptor 2 (CB2)-selective receptor localization and density, preferably in the central nervous system (CNS), the peripheral nervous system (PNS), heart, liver, gastrointestinal tract, spleen, pancreas, kidney, testis, ovary and/or the prostate. Moreover, the invention pertains to the use of said compounds in the diagnosis, prophylaxis and/or therapy of CB2 receptor-related diseases.Type: ApplicationFiled: July 8, 2015Publication date: June 22, 2017Inventors: Simon M. Ametamey, Roger Slavik, Linjing Mu
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Publication number: 20170174633Abstract: This invention relates generally to the discovery of pyrazole compounds selective for the neurotensin receptor 2 (NTR2) and uses thereof.Type: ApplicationFiled: March 24, 2015Publication date: June 22, 2017Inventors: James B. THOMAS, Brian P. GILMOUR, Angela M. GIDDINGS, Robert W. WIETHE, Keith R. WARNER, Srinivas OLEPU
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Publication number: 20170174634Abstract: The present invention relates to novel pyrazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for controlling harmful microorganisms in crop protection and in the protection of materials. Further, the present invention also relates to certain intermediates useful for producing said novel pyrazole derivatives.Type: ApplicationFiled: July 21, 2015Publication date: June 22, 2017Inventors: JOACHIM TELSER, PETER DAHMEN, ULRIKE WACHENDORFF-NEUMANN, PIERRE CRISTAU, PHILIPPE RINOLFI
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Publication number: 20170174635Abstract: The present invention provides a process for the preparation of enzalutamide.Type: ApplicationFiled: January 30, 2015Publication date: June 22, 2017Inventors: Ramendra Singh RATHORE, Venugopal Venkatarama DURVASULA, Amit SHARMA, Ram Chander ARYAN
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Publication number: 20170174636Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.Type: ApplicationFiled: December 16, 2016Publication date: June 22, 2017Inventors: Craig BATES, David P. REED
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Publication number: 20170174637Abstract: The present application relates to methods of preparing Compound A: or a salt thereof, and a polymorph of Compound A dihydrochloride salt:Type: ApplicationFiled: December 16, 2016Publication date: June 22, 2017Inventors: Craig BATES, Jianmin MAO, David P. REED
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Publication number: 20170174638Abstract: A compound of Formula II, is provided. R1, R2 and R3 are independently either hydrogen, alkyl, aryl, halogen, alkoxy, nitro, amino or hydroxyl. X is either F, Cl, Br, I or CN. Y is either N or CH. Compositions that include Formula II can be used to inhibit vacuolar H+ ATPase.Type: ApplicationFiled: December 19, 2016Publication date: June 22, 2017Applicant: University of Southern CaliforniaInventors: Chao ZHANG, Ying-Chu CHEN
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Publication number: 20170174639Abstract: Provided herein are novel small-molecules that have use in the inhibition of Eis, which mediates kanamycin resistance in Mycobacterium tuberculosis. The presently-disclosed subject matter further includes a pharmaceutical composition including a small molecule inhibitor, as described herein, and a suitable pharmaceutical carrier. Methods of treating tuberculosis comprising administering to an individual an effective amount of the disclosed small molecule inhibitors to mediate kanamycin A resistance and treat tuberculosis are also provided.Type: ApplicationFiled: December 16, 2016Publication date: June 22, 2017Inventors: Sylvie Garneau-Tsodikova, Oleg V. Tsodikov, James E. Posey
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Publication number: 20170174640Abstract: This invention pertains generally to compounds of Formula I and compositions containing such compounds, as well as methods of using such compounds to treat bacterial infections. In certain aspects, the invention pertains to methods and compositions for treating infections caused by Gram-negative bacteria.Type: ApplicationFiled: March 9, 2017Publication date: June 22, 2017Inventors: Jiping FU, Xianming JIN, Subramanian KARUR, Guillaume LAPOINTE, Patrick LEE, Zachary Kevin SWEENEY
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Publication number: 20170174641Abstract: In general, among other things, compounds of Formula I are provided: in which R11 is e.g., 4-(pyrrolidin-1-yl)piperidin-1-yl, N-methyl-3-(pyrrolidin-1-yl)propan-1-amino, N1,N1,N3-trimethylpropane-1,3-diamino, N,N-dimethylpiperidin-4-amino, 3-(pyrrolidin-1-ylmethyl)azetidin-1-yl, 3-(pyrrolidin-1-ylmethanon)azetidin-1-yl, or 3-(morpholin-1-ylmethyl)azetidin-1-yl; R13 is, e.g., phenyl optionally substituted with one or more substituents; and R12 and R14 are each independently hydrogen or alkyl. Methods of treatment are also provided.Type: ApplicationFiled: February 27, 2015Publication date: June 22, 2017Applicant: Treventis CorporationInventors: Mark A. Reed, Thomas K. Wood, Scott C. Banfield, Christopher J. Barden, Arun Yadav, Erhu Lu, Fan Wu
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Publication number: 20170174642Abstract: The present disclosure relates to a chemical compound having the general formula wherein R1 and R2 are, equal or independently, aryl, heteroaryl; wherein RTA is a 2-1,3-, or 4-1,3- or 5-1,3-thiazole ring and its use in for improving the short term memory and/or the working memory.Type: ApplicationFiled: February 10, 2017Publication date: June 22, 2017Inventors: Johann Leban, Gert Lubec
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Publication number: 20170174643Abstract: The invention relates to a novel choline cocrystal of 5-[(1Z.2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients.Type: ApplicationFiled: March 3, 2017Publication date: June 22, 2017Inventors: Isabel KALOFONOS, G. Patrick STAHLY, William MARTIN-DOYLE, Dimitris KALOFONOS, Travis L. HOUSTON, Jeffrey S. STULTS
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Publication number: 20170174644Abstract: The invention relates to compounds in the treatment or prevention of disorders associated with Lamin A and/or Lamin C depletion or LMNA mutations, such as laminopathy, premature ageing disorders, normal ageing and cancer (such as a cancer characterised by low levels of LMNA expression).Type: ApplicationFiled: April 2, 2015Publication date: June 22, 2017Applicants: CAMBRIDGE ENTERPRISE LIMITED, THE CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Delphine Laurence Daniele LARRIEU, Raphaël Joël RODRIGUEZ, Sébastien Frédéric Stéphane BRITTON, Stephen Philip JACKSON
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Publication number: 20170174645Abstract: The present invention relates to a novel 2-phenylbenzofuran derivative or a pharmaceutically acceptable salt thereof, a production method for the same, and a pharmaceutical composition for preventing or treating an inflammatory disease comprising the same as an active ingredient, and the novel 2-phenylbenzofuran derivative or the pharmaceutically acceptable salt thereof according to the present invention is outstandingly effective in suppressing NO, IL-6, and TNF-alpha induced by macrophages, and therefore can advantageously be used in a pharmaceutical composition for preventing or treating an inflammatory disease.Type: ApplicationFiled: March 3, 2017Publication date: June 22, 2017Applicants: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY, DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATIONInventors: Kyeong LEE, Sei-Ryang OH, Kyung Seop AHN, Ok-Kyoung KWON, Doo-Young KIM, Hyung Won RYU, Jung Hee KIM, Xuezhen XU
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Publication number: 20170174646Abstract: The present invention provides a compound of the following Formula (1) or a pharmaceutically acceptable salt thereof: wherein X is an oxygen atom and the like; Y is —CO—, —SO2— and the like; R1 is an optionally-substituted C1-6 alkyl group, an optionally-substituted C1-6 alkylcarbonyl group and the like; R2 is an optionally-substituted C1-6 alkyl group, an optionally-substituted C1-6 alkoxy group, an optionally-substituted amino group, an optionally-substituted 5- to 12-membered monocyclic or polycyclic saturated heterocyclic group and the like; R3, R4, R5, and R6 are independently a hydrogen atom and the like which exhibits excellent effects in suppressing the proliferation and sphere-forming ability of cancer cells, and can be useful as an antitumor drug or cell growth inhibitor.Type: ApplicationFiled: February 6, 2015Publication date: June 22, 2017Applicant: Boston Biomedical, Inc.Inventors: Toshihiko SONE, Wataru HIROSE, Naoaki SHIMADA, Chiang J. LI, Wei LI, David LEGGETT
