Patents Issued in September 21, 2017
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Publication number: 20170267621Abstract: A plant (1) for recovering acrylic acid, which includes: a absorption column (201); a dissociation column (205); a first line (101) connected to the dissociation column (205); a second line (102) connecting the absorption column (201) and the dissociation column (205); a third line (103) feeding a substream of the mother acid obtained in the crystallization into the dissociation column (205); a fourth line (104) connecting the crystallization apparatus and the absorption column (201); and a fifth line (105) connecting the dissociation column (205) and the absorption column (201).Type: ApplicationFiled: June 7, 2017Publication date: September 21, 2017Applicant: BASF SEInventors: Ulrich HAMMON, Thomas WALTER, Markus OTTENBACHER, Frank HUETTEN
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Publication number: 20170267622Abstract: The present invention concerns a process for the obtention of a halogenated carboxylic halide having a reduced content of impurities, a fraction of the halogenated carboxylic halide having a reduced content of impurities, and its use in the manufacture of agriculturally and pharmaceutically active compounds.Type: ApplicationFiled: August 13, 2015Publication date: September 21, 2017Applicant: Solvay SAInventor: Max Josef BRAUN
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Publication number: 20170267623Abstract: Embodiments are directed to adamantane-intercalated layered double-hydroxide (LDH) particles and the methods of producing adamantane-intercalated LDH particles. The method comprises adding to an aqueous solution a first precursor and a second precursor to form an initial mixture, where the first precursor is Al(OH)3 or Al2O3, the second precursor is a hydroxide M(OH)2 or an oxide MO, where M is a metal of oxidation state +2; and the initial mixture has a M/Al molar ratio of from 1 to 5. The method also comprises adding to the initial mixture an amount of adamantane to form a reaction mixture having an Al/adamantane molar ratio of from 0.5 to 2; and heating the reaction mixture to produce adamantane-intercalated LDH particles, where the adamantane-intercalated LDH particles have aspect ratios greater than 100.Type: ApplicationFiled: March 3, 2017Publication date: September 21, 2017Applicants: Saudi Arabian Oil Company, Durham UniversityInventors: Manohara Gudiyor Veerabhadrappa, Hugh Christopher Greenwell, Gasan Selman Alabedi, John Adrian Hall, Abdullah A. Al-Shahrani, Andrew Whiting
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Publication number: 20170267624Abstract: The present invention relates to a method for producing a C4-C10 alkyl (meth)acrylate, by direct esterification of (meth)acrylic acid by the corresponding alcohol, the reaction water being removed in the form of an azeotrope with the esterification alcohol from a distillation column mounted over the esterification reactor comprising a cationic resin as a catalyst. Said method is characterized in that the molar ratio of alcohol to acid at the inlet of the reactor is between 1.4 and 3, and in that the crude reaction mixture circulates in a recirculation loop joining the reactor and the water removal column, at a recirculation rate of between 6 and 25, expressed by the mass ratio between the flow fed into the loop and the flow sent to a purification treatment.Type: ApplicationFiled: June 22, 2015Publication date: September 21, 2017Applicant: Arkema FranceInventors: Anne MORELIERE, Gilles FRIMOUR, Jean-Michel PAUL, Stephane DENIS
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Publication number: 20170267625Abstract: There is provided a method for producing ethyl 4-methyloctanoate at a lower cost, by fewer steps, and in higher yield. More specifically, there is provided a method for producing ethyl 4-methyloctanoate comprising the steps of: reacting 1-chloro-2-methylhexane through malonic ester synthesis to obtain diethyl 2-methylhexylmalonate, and subjecting the diethyl 2-methylhexylmalonate to a Krapcho reaction to obtain ethyl 4-methyloctanoate.Type: ApplicationFiled: March 8, 2017Publication date: September 21, 2017Inventors: Yuki MIYAKE, Yusuke NAGAE, Takeshi KINSHO
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Publication number: 20170267626Abstract: An object of the present invention is to provide a process for producing ?-fluoroacrylic acid esters at a high starting material conversion and a high yield. The present invention provides, as a means to achieve the object, a process for producing a compound represented by formula (1): wherein R2 and R2 are the same or different and each represent alkyl, fluoroalkyl, aryl optionally substituted with at least one substituent, halogen, or hydrogen; and R3 represents alkyl, fluoroalkyl, or aryl optionally substituted with at least one substituent, the process comprising step A of reacting a compound represented by formula (2): wherein the symbols are as defined above, with carbon monoxide and an alcohol represented by formula (3): R3—OH??(3) wherein the symbol is as defined above, in the presence of a transition metal complex catalyst containing at least one bidentate phosphine ligand and a base to thereby obtain the compound represented by formula (1).Type: ApplicationFiled: June 6, 2017Publication date: September 21, 2017Applicant: DAIKIN INDUSTRIES, LTD.Inventors: Akihiro GOTOU, Manaho MIYAZAKI, Sumi ISHIHARA, Takashi NAMIKAWA, Tatsuya OHTSUKA, Yosuke KISHIKAWA
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Publication number: 20170267627Abstract: In a process for workup of a crude ester comprising esterification catalyst hydrolysis product in suspended particulate form, a) the crude ester is admixed in an emulsifying tank with 1% to 10% by weight of water and the water is emulsified in the crude ester to obtain a suspoemulsion, b) the suspoemulsion from the emulsifying tank is transferred to an agglomerating tank containing an initial charge of water-undersaturated crude ester, such that a water content below the solubility limit of water in the crude ester is established in the mixture of the suspoemulsion and the initial charge of crude ester, as a result of which the suspended particulate esterification catalyst hydrolysis products form stable agglomerates, and c) the agglomerates formed are filtered off.Type: ApplicationFiled: July 29, 2015Publication date: September 21, 2017Inventors: Piotr MAKARCZYK, Boris BREITSCHEIDEL, Beatrice RÖSSLER-FEIGEL, Kerstin MÜHLHEIMS
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Publication number: 20170267628Abstract: [6,6]-Phenyl C71 butyric acid derivatives (C70-PCBR3) having a selectivity of greater than 95 wt % of the ?-isomer are provided by reacting fullerene C70 with a dialkyl sulfonium tetrafluoroborate having the formula:Type: ApplicationFiled: December 23, 2016Publication date: September 21, 2017Inventors: Edward A. JACKSON, Henning RICHTER
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Publication number: 20170267629Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.Type: ApplicationFiled: June 5, 2017Publication date: September 21, 2017Applicant: Dow AgroSciences LLCInventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
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Publication number: 20170267630Abstract: HDAC inhibitors of the general formula (I) and (II) and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase/deacetylase activity as described herein (e.g., cancer). In certain embodiments, the compounds of the invention selectively target either a class or isoform of the HDAC family. Another aspect of the invention provides an assay for determining the inhibitory effect of a test compound on an HDAC protein comprising: incubating the HDAC protein with a substrate of general formula (IIIc) in the presence of a test compound; and determining the activity of the HDAC protein.Type: ApplicationFiled: January 5, 2017Publication date: September 21, 2017Applicants: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.Inventors: Ralph Mazitschek, James E. Bradner
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Publication number: 20170267631Abstract: What is described is a compound of formula I wherein R1 is a linear alkyl, alkenyl, or alkynyl of 2 to 12 carbons, or a branched alkyl with 12 to 20 carbons, R2 is a branched alkyl with 12 to 20 carbons, L1 and L2 are independently a linear alkylene with 1-18 carbons or alkenylene with 2-18 carbons, X is S or O, L3 is a bond or an alkylene with 1 to 6 carbons, R3 is an alkylene with 1 to 6 carbons, and R4 and R5 are the same or different, each a linear or branched alkyl with 1 to 6 carbons.Type: ApplicationFiled: June 5, 2017Publication date: September 21, 2017Inventors: Joseph E. Payne, Padmanabh Chivukula
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Publication number: 20170267632Abstract: Provided are methionine analogs which may be useful for inhibiting protein synthesis, inhibiting microbial growth and/or treating infectious diseases. In some instances, the analogs exhibit bactericidal, antibacterial, anti-infective, antimicrobial, sporicidal, disinfectant, antifungal and/or antiviral properties. Also provided are methods of treatment and methods of preparation, as well as kits and unit dosages.Type: ApplicationFiled: June 1, 2017Publication date: September 21, 2017Inventors: Mansour BASSIRI, Afsaneh RAHIMI-LARIJANI
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Publication number: 20170267633Abstract: The present invention provides novel crystal forms of arylalkylamine compounds. Specifically, the novel crystal forms of 4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1-yl)phenylacetic acid have excellent stability and therefore are useful as pharmaceutical ingredients. The present invention also provides industrially advantageous processes for producing the arylalkylamine compounds.Type: ApplicationFiled: March 30, 2017Publication date: September 21, 2017Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Hiroshi MIYAZAKI, Takao KOMASAKA, Joji TSURUMOTO, Takeshi UEMURA, Yuuji MORITA
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Publication number: 20170267634Abstract: The compounds of Formula (I) which can be used as CRTH2 receptor antagonists are provided. The compounds of Formula (I) can be used in the treatment and prevention of asthma, allergic rhinitis and atopic dermatitis, as well as other diseases mediated by prostaglandin D2 (PGD2) at the CRTH2 receptor.Type: ApplicationFiled: September 11, 2015Publication date: September 21, 2017Applicant: SUNSHINE LAKE PHARMA CO., LTD.Inventors: Yingjun ZHANG, Tianzhu YU, Bing LIU, Xiangyu ZHANG, Shiguo ZHANG, Changchung CHENG, Jiancun ZHANG
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Publication number: 20170267635Abstract: The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to new anticancer miliusane lactam compounds. The present invention also includes its preparation and application method for treating cancer.Type: ApplicationFiled: June 1, 2017Publication date: September 21, 2017Inventor: Hongjie Zhang
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Publication number: 20170267636Abstract: The present invention discloses a process for synthesis of piperidine alkaloids selected from fagomine, 4-epi-fagomine and nojirimycin from tri-O-benzyl-D-glucal or tri-O-benzyl-D-galactal.Type: ApplicationFiled: May 5, 2015Publication date: September 21, 2017Inventors: Asish Kumar Bhattacharya, Hemender Rami Chand
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Publication number: 20170267637Abstract: Provided herein are modified amino acids comprising an azido group, polypeptides, antibodies and conjugates comprising the modified amino acids, and methods of producing the polypeptides, antibodies and conjugates comprising the modified amino acids. The polypeptides, antibodies and conjugates are useful in methods of treatment and prevention, methods of detection and methods of diagnosis.Type: ApplicationFiled: May 24, 2017Publication date: September 21, 2017Inventors: Ryan STAFFORD, Christopher D. THANOS, Wenjin YANG
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Publication number: 20170267638Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: April 6, 2017Publication date: September 21, 2017Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
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Publication number: 20170267639Abstract: The invention provides a method for the synthesis of dehydrogenated lactam drugs of Formula I:Type: ApplicationFiled: April 10, 2017Publication date: September 21, 2017Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
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Publication number: 20170267640Abstract: The present invention relates to a process for the preparation of synthetic intermediates which may be used in the preparation of tetrahydroquinoline derivatives, which derivatives have an inhibitory activity against cholesteryl transfer protein (CETP), show effects of increasing HDL cholesterol level and decreasing LDL cholesterol level, and can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, hyperlipidemia, dyslipidemia and the like.Type: ApplicationFiled: July 29, 2015Publication date: September 21, 2017Applicant: DEZIMA PHARMA B.V.Inventors: John FORD, Johannes Paulus Gerardus SEERDEN, Amandine LEDRU
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Publication number: 20170267641Abstract: The present invention relates to methods and compounds for regulating or enhancing ethropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.Type: ApplicationFiled: April 17, 2017Publication date: September 21, 2017Inventors: Stephen J. Klaus, Christopher J. Molineaux, Thomas B. Neff, Volkmar Guenzler-Pukall, Robert C. Stephenson, Todd W. Seeley, Ingrid Langsetmo Parobok
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Publication number: 20170267642Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.Type: ApplicationFiled: February 1, 2017Publication date: September 21, 2017Applicant: Epizyme, Inc.Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kerren Kalai Swinger
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Publication number: 20170267643Abstract: The invention provides pyrazolyl guanidine compounds that inhibit F1Fo-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.Type: ApplicationFiled: February 1, 2017Publication date: September 21, 2017Inventors: Gary D. Glick, Alexander R. Hurd, Clarke B. Taylor, Chad A. VanHuis
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Publication number: 20170267644Abstract: An electrically conducting organic oligomer comprising 4-nitro-1H-pyrazole-3-yl-amine, 4-trifluoromethyl-1H-pyrazol-3-yl-amine, 4-trichloromethyl-1H-pyrazol-3-yl-amine, 4-tribromomethyl-1H-pyrazol-3-yl-amine, 4-ammonium-1H-pyrazol-3-yl-amine, 4-trimethylammonium-1H-pyrazol-3-yl-amine, 4-triethylammonium-1H-pyrazol-3-yl-amine, or 4-tripropylammonium-1H-pyrazol-3-yl-amine. An electrically conducting organic oligomer made from the steps of preparing an acidic aqueous solution with a monomer, preparing the acidic aqueous solution by mixing water with a monomer (3-amino-1H-pyrazole-4-carbonitrile), forming a solution preparing a second aqueous solution, mixing the acidic aqueous solution with the second aqueous solution, and allowing a reaction to proceed at about 40° C.Type: ApplicationFiled: May 31, 2017Publication date: September 21, 2017Applicant: The Government of the United States of America, as represented by the Secretary of the NavyInventors: Brett D. Martin, Scott A. Trammell, Jeffrey R. Deschamps, Jawad Naciri, Jeffrey DePriest
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Publication number: 20170267645Abstract: The present application relates to crystalline and amorphous forms of Enzalutamide. The present application further relates to amorphous solid dispersions of Enzalutamide with pharmaceutically acceptable carriers. The present application also relates to a process for the preparation of Form R1 of Enzalutamide.Type: ApplicationFiled: June 1, 2017Publication date: September 21, 2017Inventors: Vishweshwar PEDDY, Rajesham BOGE, Lokeswara Rao MADIVADA
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Publication number: 20170267646Abstract: Provided is a preparation method for revaprazan hydrochloride, the method comprising: (1) the preparation of 4-hydroxyl-2-(4-fluoroaniline)-5,6-dimethylpyrimidine; (2) the preparation of 4-chloro-2-(4-fluoroaniline)-5,6-dimethylpyrimidine; (3) the preparation of revaprazan hydrochloride. The method has advantages such as simple operations, high product purity, good yield and suitability for industrial production.Type: ApplicationFiled: November 12, 2015Publication date: September 21, 2017Inventors: Wenzheng Liu, Guocheng Wang, Qingwei Hou, Qiaoping Cui, Zhanyuan Zhu, Jinping Liu, Mingbo Yang, Hongguang Meng
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Publication number: 20170267647Abstract: Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.Type: ApplicationFiled: June 7, 2017Publication date: September 21, 2017Inventors: Mercedes Delgado, Jan Elsner, Paul Erdman, Robert Hilgraf, Laurie Ann LeBrun, Meg McCarrick, Mark A. Nagy, Stephen Norris, David A. Paisner, Yoshitaka Satoh, Marianne Sloss, Jayashree Tikhe, Won Hyung Yoon
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Publication number: 20170267648Abstract: The present application relates to novel substituted uracil derivatives, to a method for the production thereof, to the use thereof either alone or in combination for treating and/or preventing diseases, and to the use thereof for producing pharmaceuticals for the treatment and/or prevention of diseases.Type: ApplicationFiled: June 1, 2017Publication date: September 21, 2017Applicant: Bayer Pharma AktiengesellschaftInventors: Chantal FÜRSTNER, Jens ACKERSTAFF, Alexander STRAUB, Heinrich MEIER, Hanna TINEL, Katja ZIMMERMANN, Dmitry ZUBOV, Jens SCHAMBERGER
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Publication number: 20170267649Abstract: A very stable, selective and renally safe sodium channel blocker represented by the formula: The invention also includes a variety of compositions, combinations and methods of treatment using this inventive sodium channel blocker.Type: ApplicationFiled: January 30, 2017Publication date: September 21, 2017Applicant: PARION SCIENCES, INC.Inventor: Michael R. JOHNSON
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Publication number: 20170267650Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: October 27, 2016Publication date: September 21, 2017Applicant: Parion Sciences, Inc.Inventor: Michael R. Johnson
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Publication number: 20170267651Abstract: Provided are methods of treating and/or preventing dermatological disorders. Provided are methods of reducing skin inflammation, reducing pain, and/or reducing itch in a subject in need thereof. The methods may include administering to the subject an effective amount of a TRPA1 and/or TRPV4 inhibitor. Further provided are compositions including a TRPA1 and/or TRPV4 inhibitor compound in combination with a carrier, vehicle, or diluent that is suitable for topical application.Type: ApplicationFiled: August 22, 2014Publication date: September 21, 2017Inventors: Wolfgang LIEDTKE, Martin STEINHOFF, Farshid GUILAK
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Publication number: 20170267652Abstract: A process for the purification of diaminophenothiazinium compounds, and particularly of methylene blue, is described. The process provides for simple and effective purification by reduction of the post-synthesis or commercially available diaminophenothiazinium compound to form a reduced complex thereof. This can then be purified in a more straightforward manner than the original compound by, for example, recrystallization before being allowed to oxidise back to the diaminophenothiazinium compound.Type: ApplicationFiled: June 6, 2017Publication date: September 21, 2017Inventor: Malvin Eutick
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Publication number: 20170267653Abstract: The present application relates to compounds of any one of Formulae I, Ia, Ib, Ic, Id, Ie, and If. Compounds of Formula (I) have the structure: wherein A, B, W, Y, Z, R2, R4, R5, R6, Rq and q are as defined herein. The compounds can be used as inhibitors of Bcl-3 and can be used for the treatment of cancer, particularly metastatic cancer.Type: ApplicationFiled: July 31, 2015Publication date: September 21, 2017Applicant: University College Cardiff Consultants LimitedInventors: Andrew David WESTWELL, Andrea BRANCALE, Richard William Ernest CLARKSON
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Publication number: 20170267654Abstract: Provided herein are methods of producing dialkylfurans, such as 2,5-dimethylfuran, and other alkyl furans, such as 2-methylfuran. For example, 2,5-dimethylfuran may be produced by hydrogenation of (5-methylfuran-2-yl) methanol or 2-(chloromethyl)-5-methylfuran in the presence of a solid supported metal catalyst having an excess of either basic or acidic sites (as determined by chemisorption of CO2 or NH3). The process could further include a urea reagent (TMU, DMPU, TMI) and an alkyl benzene.Type: ApplicationFiled: August 14, 2015Publication date: September 21, 2017Applicant: Micromidas, Inc.Inventors: Dennis A. HUCUL, Dimitri A. HIRSCH-WEIL, Makoto Nathanael MASUNO, John Albert BISSELL, II, Alex B. WOOD, Robert Joseph ARAIZA, Daniel R. HENTON, Shawn M. BROWNING, Ryan L. SMITH
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Publication number: 20170267655Abstract: Provided herein are novel, commercially viable and industrially advantageous processes for the preparation of benzofuran-2-carboxamide derivatives and their intermediates, or a pharmaceutically acceptable salt thereof, in high yield and purity. Provided particularly herein are novel, commercially viable and industrially advantageous processes for the preparation of vilazodone or a pharmaceutically acceptable salt thereof in high yield and purity. Provided also herein is an improved and commercially viable process for the preparation of 3-(4-hydroxybutyl)-1H-indole-5-carbonitrile, in high yield and purity, using novel intermediate compound 3-(4-hydroxybutyryl)-1H-indole-5-carbonitrile.Type: ApplicationFiled: May 17, 2017Publication date: September 21, 2017Inventors: Mohan Rao DODDA, Jithender AADEPU
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Publication number: 20170267656Abstract: There are provided inter alia pyrazolyl-substituted pyridone compounds, which exhibit biological activity, e.g., inhibitory action, against serine proteases, including thrombin and various kallikreins. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of serine proteases, including thrombin and various kallikreins.Type: ApplicationFiled: September 17, 2015Publication date: September 21, 2017Inventors: Kevin Michael SHORT, David Ben KITA, Maria de los Angeles ESTIARTE-MARTINEZ, Son Minh PHAM
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Publication number: 20170267657Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: ApplicationFiled: June 2, 2017Publication date: September 21, 2017Applicant: Dow AgroSciences LLCInventors: Ann M. Buysse, Noormohamed M. Niyaz, David A. Demeter, Yu Zhang, Martin J. Walsh, Asako Kubota, Ricky Hunter, Tony K. Trullinger, Christian T. Lowe, Daniel I. Knueppel, Akshay Patny, Negar Garizi, Paul R. LePlae, JR., Frank J. Wessels, Ronald Ross, JR., Carl DeAmicis, Peter Borromeo
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Publication number: 20170267658Abstract: Provided are processes for the preparation of isotopologues of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 2, 2017Publication date: September 21, 2017Inventor: John Fitzgerald TRAVERSE
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Publication number: 20170267659Abstract: To provide a method for producing a compound represented by the formula (1) which is a 2-pyridone compound useful as a pharmaceutical or an intermediate for a pharmaceutical, etc. at a high yield.Type: ApplicationFiled: May 11, 2015Publication date: September 21, 2017Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Hironobu YOSHINO, Yasuhiro UMEDA, Jun TAKEOKA, Akihiro NAGAYA, Yudai SUGAWARA, Madoka YOSHINO
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Publication number: 20170267660Abstract: Disclosed are compounds of Formula I(b): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Ring A, Ring HD, J, each T, R3, R4, R5, each R7, and m are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.Type: ApplicationFiled: March 15, 2017Publication date: September 21, 2017Inventors: Jack Lin, Prabha N. Ibrahim, Aaron Albers, John Buell, Zuojun Guo, Phuongly Pham, Hannah Powers, Songyuan Shi, Wayne Spevak, Guoxian Wu, Jiazhong Zhang, Ying Zhang
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Publication number: 20170267661Abstract: Described herein are compounds that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.Type: ApplicationFiled: March 17, 2017Publication date: September 21, 2017Inventors: Joseph L. Kim, Douglas J. Kevin, Jason D. Brubaker
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Publication number: 20170267662Abstract: The invention provides a compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification. The invention also provides a method for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like in a mammal by administering the compound or pharmaceutically acceptable salt thereof or solvate thereof to the mammal.Type: ApplicationFiled: October 28, 2016Publication date: September 21, 2017Applicant: Japan Tobacco Inc.Inventors: Teruhiko INOUE, Tetsudo KAYA, Shinichi KIKUCHI, Koji MATSUMURA, Ritsuki MASUO, Motoya SUZUKI, Michihide MAEKAWA
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Publication number: 20170267663Abstract: Disclosed herein are protein kinase inhibitors, more particularly novel quinazoline derivatives and pharmaceutical compositions thereof, and method of use thereof.Type: ApplicationFiled: June 5, 2017Publication date: September 21, 2017Inventors: Weibo Wang, Xingdong Zhao, Tongshuang Li, Qiang Tian, Ling Chen, Zuwen Zhou, Zhifu Li, Xianlong Wang, Yue Rong, Lihua Jiang, Yanxin Liu, Jing Sun, Fanxin Zeng
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Publication number: 20170267664Abstract: The present invention provides Quinazolin-THF-amines as PDE I inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.Type: ApplicationFiled: June 5, 2017Publication date: September 21, 2017Applicant: H. Lundbeck A/SInventors: Jan Kehler, Lars Kyhn Rasmussen, Morten Langgård
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Publication number: 20170267665Abstract: The present invention relates to the compound (2R,2?R)-bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) 1,1?-adipoylbis(pyrrolidine-2-carboxylate), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.Type: ApplicationFiled: June 1, 2017Publication date: September 21, 2017Inventors: Alexis DENIS, Olivier MIRGUET, Jérôme TOUM
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Publication number: 20170267666Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.Type: ApplicationFiled: June 8, 2017Publication date: September 21, 2017Inventors: Wei Meng, Guohua Zhao
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ALKENYLDIARYLMETHANES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS FOR ANTI-HIV-1 CHEMOTHERAPY
Publication number: 20170267667Abstract: The invention disclosed herein pertains to compounds of alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of patients with acquired-immune deficiency syndrome (AIDS). Also described are methods for treating AIDS patients using the described alkenyldiarylmethane compounds.Type: ApplicationFiled: March 15, 2017Publication date: September 21, 2017Applicant: Purdue Research FoundationInventors: Mark S. Cushman, Takeshi Sakamoto -
Publication number: 20170267668Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula (I): wherein X1 is selected from C and N; X3 and X5 may be the same or different and each is independently selected from C, N, O and S; Y is selected from N and O; Z is selected from C, N and O; each bond represented by a dotted line may independently be a double bond or a single bond, provided that valencies at each ring atom are maintained and provided that the ring Q contains at least one double bond and provided that the atom N has a double bond; R3 and R5 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R3 groups present is such that the valency of X3 is maintained, and the number of R5 groups present is such that the valency of X5 is maintained; each R11 and R12 may be present or absent and may be the samType: ApplicationFiled: August 13, 2015Publication date: September 21, 2017Applicant: IOmet Pharma Ltd.Inventors: Phillip M. COWLEY, Alan WISE, Margaret Huggett
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Publication number: 20170267669Abstract: The present invention relates to an environmentally friendly process for preparing rivaroxaban. The present invention provides a process for preparing rivaroxaban of formula I, the process comprising: reacting a compound of formula VI with a base in the presence of a solvent to form a compound of formula VII; and condensing the compound of formula VII with a compound of formula VIII or a compound of formula IX in the presence of a solvent to prepare rivaroxaban of formula I, wherein the solvent used in both steps comprises water.Type: ApplicationFiled: August 24, 2015Publication date: September 21, 2017Inventors: Dharmaraj Ramachandra RAO, Geena MALHOTRA, Venkata Srinivas PULLELA, Manohar Raghunath SURVE, Hemant Sanjeevan DORLE, Kiran Balasaheb JADHAV
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Publication number: 20170267670Abstract: Anti-angiogenic treatments, treatments of hyperpermeability disorders, treatments of neuropathic and neurodegenerative disorders, pain treatments, methods of reducing the risk of pre-eclampsia and compounds for use in such methods are described.Type: ApplicationFiled: May 31, 2017Publication date: September 21, 2017Inventors: David Bates, Jonathan Morris