Patents Issued in December 8, 2016
  • Publication number: 20160355451
    Abstract: A process for the preparation of a chemical composition comprising an aromatic compound ? in a concentration B by weight, based on the total weight of the chemical composition, includes: a. providing the following reaction components: i. a chemical composition comprising the following: a) The aromatic compound ? in a concentration A by weight based on the total weight of the chemical composition, and b) An olefin in an amount of about 50 to about 99.99 wt. %, based on the total weight of the chemical composition, and ii. an acid; and b. reacting the components to obtain the chemical composition comprising the aromatic compound ? in a concentration B by weight based on the total weight of the chemical composition; wherein the concentration B is less than the concentration A.
    Type: Application
    Filed: February 5, 2015
    Publication date: December 8, 2016
    Inventors: Roland Schmidt, Shahid Azam
  • Publication number: 20160355452
    Abstract: The present invention relates to a method for obtaining high purity (bromomethyl)cyclopropane and (bromomethyl)cyclobutane, starting respectively with cyclopropylmethanol and cyclobutylmethanol, under synthesis conditions that enable high productivity and high yield.
    Type: Application
    Filed: December 1, 2014
    Publication date: December 8, 2016
    Applicant: MELCHIOR MATERIAL AND LIFE SCIENCE FRANCE
    Inventor: Olivier GUERRET
  • Publication number: 20160355453
    Abstract: In the production of fluorine-containing olefins using a chlorine-containing alkane or a chlorine-containing alkene as a starting material, a process for producing a plurality of useful fluorine-containing olefins with high selectivity using the same raw material, the same equipment, and the same conditions is provided. The present invention provides a process for producing fluorine-containing olefins, the process comprising reacting a chlorine-containing compound represented by a specific formula and anhydrous hydrogen fluoride in the presence of oxidative gas and a fluorination catalyst, wherein the fluorination catalyst is a catalyst in which at least one metal element M selected from the group consisting of Group VIII and Group IX is present together with chromium. This production process can simultaneously produce two or more fluorine-containing olefin compounds, including HFO-1234yf and HFO-1234ze, with high selectivity.
    Type: Application
    Filed: May 27, 2016
    Publication date: December 8, 2016
    Applicant: DAIKIN INDUSTRIES, LTD.
    Inventors: Shun OHKUBO, Daisuke KARUBE
  • Publication number: 20160355454
    Abstract: The invention relates to a method for converting a precatalyst complex to an active catalyst complex, wherein the precatalyst complex and the active catalyst complex comprise a ruthenium atom and an optically active ligand that is insoluble in water, and the active catalyst complex furthermore comprises a monohydride and a water molecule. The method comprises the steps of providing water as an activation solvent system with a pH value equal or below 2, and solving said precatalyst complex, an acid, and hydrogen therein. The invention further relates to a method for manufacturing a catalyst composition, a method for hydrogenating a substrate molecule and a reaction mixture.
    Type: Application
    Filed: August 23, 2016
    Publication date: December 8, 2016
    Applicant: Dexlechem GMBH
    Inventor: Sonja JOST
  • Publication number: 20160355455
    Abstract: This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis.
    Type: Application
    Filed: August 17, 2016
    Publication date: December 8, 2016
    Applicant: United Therapeutics Corporation
    Inventors: Ken Phares, David Mottola
  • Publication number: 20160355456
    Abstract: An object of the present invention is to provide a plant extract which comprises o-diphenol type chlorogenic acids in a high concentration. Also, it is to provide a plant extract excellent in deodorizing property or anti-oxidation property, which does not substantially comprise ferulylquinic acids and caffeine content. The present invention provides a plant extract, which comprises chlorogenic acids comprising an o-diphenol type chlorogenic acid and does not substantially comprise ferulylquinic acid and caffeine, which is excellent in deodorizing property or anti-oxidation property.
    Type: Application
    Filed: August 18, 2016
    Publication date: December 8, 2016
    Applicant: TAKASAGO INTERNATIONAL CORPORATION
    Inventors: Yoshikazu TOYOHARA, Tadahiro HIRAMOTO
  • Publication number: 20160355457
    Abstract: Solid forms comprising a compound useful in the treatment, prevention and management of various conditions and diseases are provided herein. In particular, the invention provides solid forms comprising (?)-O-desmethylvenlafaxine, including salts thereof, having utility for the treatment, prevention and management of conditions and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.
    Type: Application
    Filed: May 25, 2016
    Publication date: December 8, 2016
    Inventors: Michael Sizensky, Harold S. Wilkinson, John R. Snoonian, Norman Kim, Sharon M. Laughlin, Roger P. Bakale, Kevin Plunkett, Patrick Mousaw
  • Publication number: 20160355458
    Abstract: Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods of treating, inhibiting, and/or abatement of cognitive decline and/or Alzheimer's disease with a compound or pharmaceutically acceptable salt of the invention are also provided. Also provided are methods of preparing the compounds/compositions of the invention.
    Type: Application
    Filed: June 13, 2016
    Publication date: December 8, 2016
    Inventors: Gilbert M. Rishton, Susan Catalano
  • Publication number: 20160355459
    Abstract: Compounds that stimulate fibroblast growth factor production, and thus cell growth are provided. Also provided are compositions comprising the compounds and methods of using the compounds. The compounds can be used to treat wounds, to expand cell populations, such as hematopoietic cells, or to grow tissue in vitro, among other uses.
    Type: Application
    Filed: August 22, 2016
    Publication date: December 8, 2016
    Inventors: Billy W. Day, Waikok Michael Tsang, Vasiliy N. Korotchenko
  • Publication number: 20160355460
    Abstract: The present invention provides a method for the production of [18F]-FACBC which has advantages over know such methods. Also provided by the present invention is a system to carry out the method of the invention and a cassette suitable for carrying out the method of the invention on an automated radiosynthesis apparatus.
    Type: Application
    Filed: June 6, 2016
    Publication date: December 8, 2016
    Inventors: Anders Svadberg, Olav Ryan, Roger Smeets
  • Publication number: 20160355461
    Abstract: Provided are a resist and a compound for the resist improving the sensitivity, the resolution and the line edge roughness (LER) in a good balance without spoiling basic properties of a chemical amplification resist such as pattern shape, dry etching resistance, heat resistance and the like. Provided are a method for producing an alicyclic ester compound expressed by general formula (1), an alicyclic ester compound expressed by general formula (1), a (meth)acrylic copolymer obtained by polymerization of the alicyclic ester compound, and a photosensitive resin composition containing the (meth)acrylic copolymer. A method for producing an alicyclic ester compound expressed by general formula (1) includes reacting an adamantane compound expressed by general formula (2) with hydroxyalkylamine expressed by general formula (3) to produce an adamantaneamide compound expressed by general formula (4), and then reacting the adamantaneamide compound expressed by general formula (4) with (meth)acrylic acid.
    Type: Application
    Filed: February 12, 2015
    Publication date: December 8, 2016
    Inventors: Shoichi HAYAKAWA, Hiroshi HORIKOSHI, Kikuo FURUKAWA, Hiroyasu TANAKA, Hiroyuki TANAGI
  • Publication number: 20160355462
    Abstract: Analgesic compounds for treatment of pain or fever, comprising a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering the compounds.
    Type: Application
    Filed: August 17, 2016
    Publication date: December 8, 2016
    Inventor: Kevin Duane Bunker
  • Publication number: 20160355463
    Abstract: Physiological cooling compounds of the structure: where R1 is p-menthyl or 2,3,4-trimethylpent-3-yl group and R2-R8 are hydrogen or alkyl groups. The combination of R2-R8 is such that the N-alkyl group is a branched C5 alkyl or branched or linear C6-C8 alkyl group. The new carboxamides are valuable sensory ingredients which provide long-lasting cooling sensation and freshness in personal care, oral care, cosmetic products, pharmaceutical preparations, confectionary, food and beverages.
    Type: Application
    Filed: June 4, 2015
    Publication date: December 8, 2016
    Inventors: Gennadiy G. Kolomeyer, David J. Sitko, Joe W. Snow
  • Publication number: 20160355464
    Abstract: Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.
    Type: Application
    Filed: June 7, 2015
    Publication date: December 8, 2016
    Inventor: Mark Quang Nguyen
  • Publication number: 20160355465
    Abstract: This invention provides a compound having the structure wherein ?, ?, A, B, and R1-R4 are defined herein. This invention also provides pharmaceutical compositions comprising the above compounds, a method of accelerating the healing of a wound, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.
    Type: Application
    Filed: August 18, 2016
    Publication date: December 8, 2016
    Applicants: THE RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK, CHEM-MASTER INTERNATIONAL, INC.
    Inventors: Lorne M. GOLUB, Hsi-ming LEE, Francis JOHNSON
  • Publication number: 20160355466
    Abstract: The present invention relates to cyclopent(adi)ene compounds of formula I wherein the variables are as defined in the claims and description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
    Type: Application
    Filed: February 3, 2015
    Publication date: December 8, 2016
    Applicant: BASF SE
    Inventors: Pascal BINDSCHAEDLER, Wolfgang VON DEYN, Arun NARINE, Karsten ` KOERBER, Franz-Josef BRAUN
  • Publication number: 20160355467
    Abstract: The present invention provides a titanium-silicalite molecular sieve and a method for preparing the same. The method includes the steps of preparing a mixture of a titanium source, a silicon source, a metal source selected from IIA to IVA elements and a template agent; heating the mixture to form a gel mixture; heating the gel mixture in a water bath; and calcining the gel mixture after the gel mixture in the water bath to form the titanium-silicalite molecular sieve. The present invention further provides a method for preparing cyclohexanone oxime by using the titanium-silicalite molecular sieve as the catalyst which results in high conversion rate, high selectivity and high usage efficiency of hydrogen peroxide.
    Type: Application
    Filed: August 19, 2016
    Publication date: December 8, 2016
    Inventors: Ya-Ping Chen, Cheng-Fa Hsieh, Pin-To Yao, Chien-Chang Chiang
  • Publication number: 20160355468
    Abstract: 4-Amino-5-fluoro-3-chloro-6-(substituted)picolinates are prepared from trifluoroacetic acid, p-methoxyaniline, a C1-C4 alkyl propiolate and a substituted methylene amine by a series of steps.
    Type: Application
    Filed: August 23, 2016
    Publication date: December 8, 2016
    Applicant: Dow AgroSciences LLC
    Inventors: Natalie C. Giampietro, James M. Renga
  • Publication number: 20160355469
    Abstract: The present application relates to compounds and methods for reducing the severity of convulsant activity, or epileptic seizures.
    Type: Application
    Filed: June 6, 2016
    Publication date: December 8, 2016
    Inventors: Michael Poulter, TONY DURST
  • Publication number: 20160355470
    Abstract: There is disclosed a process for producing taurine by the ammonolysis of alkali isethionate in the presence of alkali ditaurinate or alkali tritaurinate, or their mixture, to inhibit the formation of byproducts and to continuously convert the byproducts of the ammonolysis reaction to alkali taurinate. Alkali taurinate is neutralized with isethionic acid to obtain taurine and to regenerate alkali isethionate. The production yield is increased to from 90% to nearly quantitative. The ammonolysis reaction is catalyzed by alkali salts of hydroxide, sulfate, sulfite, phosphate, or carbonate.
    Type: Application
    Filed: August 16, 2016
    Publication date: December 8, 2016
    Inventor: Songzhou Hu
  • Publication number: 20160355471
    Abstract: Methods for preparing intermediates of SGLT2 inhibitors are provided, including crystalline forms and methods of crystallizing intermediates.
    Type: Application
    Filed: August 16, 2016
    Publication date: December 8, 2016
    Inventors: Jacques ROBERGE, Carine VAXELAIRE, Baohu LIU, Ge XU, Jian ZHANG, Xinxing TANG, Baihua XU
  • Publication number: 20160355472
    Abstract: A process for the preparation of mesotrione enolate is provided. The process comprises providing a solution of mesotrione in an organic solvent and contacting the solution with a moderate base in the presence of water at a pH of from 6 to 8, to form an aqueous mesotrione enolate solution. A process for preparing mesotrione from the products of an enol ester rearrangement of 3-oxocyclohex-1-enyl-4-(methylsulfonyl)-2-nitrobenzoate is also provided. The process comprises contacting the products of the rearrangement reaction with an organic solvent to dissolve mesotrione; and contacting the resulting solution with an aqueous solution of an acid.
    Type: Application
    Filed: June 6, 2016
    Publication date: December 8, 2016
    Inventor: James Timothy Bristow
  • Publication number: 20160355473
    Abstract: The present invention relates to the novel compounds represented by Formula (Ia) or (Ib) and to their pharmaceutical preparations for the treatment of atherosclerosis and cholesterol level reduction.
    Type: Application
    Filed: December 16, 2014
    Publication date: December 8, 2016
    Applicant: Rudjer Boskovic Institute
    Inventors: Ivan Habus, Tonko Drazic
  • Publication number: 20160355474
    Abstract: 3,3?-Disubstituted indoline compounds, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: October 6, 2014
    Publication date: December 8, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: JONATHAN E. WILSON, Petr Vachal, Ravi Kurukulasuriya
  • Publication number: 20160355475
    Abstract: The present invention provides a novel indole derivative compound, an isomer thereof, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof. The compound according to the present invention can selectively inhibit histone deacetylase (HDAC), and thus can be used to effectively treat a disease associated with histone deacetylase (HDAC) activity.
    Type: Application
    Filed: January 2, 2015
    Publication date: December 8, 2016
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: Changsik LEE, Hyun-Mo YANG, Dohoon KIM, Miseon BAE, Youngil CHOI, Nina HA
  • Publication number: 20160355476
    Abstract: The present invention relates to compounds of the general formula (I), in which Ra to R6, G and n have the meanings given in the description—and to a process for their preparation and to their use as insecticides and acaricides.
    Type: Application
    Filed: February 13, 2015
    Publication date: December 8, 2016
    Inventors: Markus HEIL, Eike Kevin HEILMANN, Werner HALLENBACH, Kerstin ILG, Ulrich GOERGENS
  • Publication number: 20160355477
    Abstract: A compound of Formula (I) is provided that has been shown to be useful for treating a disease, disorder or syndrome that is mediated by the transportation of essential molecules in the mmpL3 pathway: wherein R1, R2, R3, R4, R5 and R6 are as defined herein.
    Type: Application
    Filed: August 19, 2016
    Publication date: December 8, 2016
    Applicant: NOVARTIS AG
    Inventors: Jan Jiricek, Ravinder Reddy Kondreddi, Paul William Smith
  • Publication number: 20160355478
    Abstract: A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.
    Type: Application
    Filed: May 10, 2016
    Publication date: December 8, 2016
    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Bernard Thomas GOLDING, Christiane RIEDINGER, Roger John GRIFFIN, Ian Robert HARDCASTLE, Eric VALEUR, Anna Frances WATSON, Martin NOBLE
  • Publication number: 20160355479
    Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.
    Type: Application
    Filed: August 19, 2016
    Publication date: December 8, 2016
    Inventors: Anthony B. PINKERTON, Russell DAHL, Nicholas D.P. COSFORD, Jose Luis MILLAN
  • Publication number: 20160355480
    Abstract: The invention discloses compounds of Formula I wherein X, R1, R2, and R3 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
    Type: Application
    Filed: May 25, 2016
    Publication date: December 8, 2016
    Inventors: Robert J. Altenbach, Marlon D. Cowart, Tom Roger Lisette De Munck, Sébastien Jean Jacques Cédric Dropsit Montovert, Gregory A. Gfesser, Hans Kelgtermans, Sébastien Laurent Xavier Martina, Steven Emiel Van der Plas, Xueqing Wang
  • Publication number: 20160355481
    Abstract: Compounds for inhibiting Type 4 Prepilin Peptidases are provided as are methods of using the compounds as an ti-bacterial agents.
    Type: Application
    Filed: February 9, 2015
    Publication date: December 8, 2016
    Inventors: Ronald K. Taylor, Gordon W. Gribble
  • Publication number: 20160355482
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R1, R2, and R3 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by voltage-gated sodium channels, e.g., Nav1.7 and/or Nav1.8. Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
    Type: Application
    Filed: August 17, 2016
    Publication date: December 8, 2016
    Inventors: Andrew Bogdan, Marlon D. Cowart, David A. DeGoey, Tammie K. Jinkerson, John R. Koenig, Michael E. Kort, Bo Liu, Mark A. Matulenko, Derek W. Nelson, Meena V. Patel, Hillary Peltier, Marc J. Scanio, Brian D. Wakefield
  • Publication number: 20160355483
    Abstract: The present invention relates to a compound inhibiting CDK5-mediated PPARG phosphorylation and a pharmaceutical composition for treating PPARG-related diseases containing the same as an active ingredient. A compound represented by formula 1 or an optical isomer thereof according to the present invention that binds to PPARG at a high affinity level, but does not act as an agonist, thereby inducing no gene transcription; blocks CDK5, which is a cause of PPARG phosphorylation, thereby causing no side effects of existing anti-diabetic drugs; can be formulated into drugs due to improved pharmacological properties thereof; and can be favorably used as a pharmaceutical composition for treating PPARG-related diseases due to favorable treatment effects on PPARG-related diseases.
    Type: Application
    Filed: August 23, 2016
    Publication date: December 8, 2016
    Applicant: Hyundai Pharm Co., Ltd.
    Inventors: In Hee LEE, Hee Il CHAE, Se hoan KIM, Soon Young MOON, Tae Young HA, Hyo sun CHOI, Young Seok KIM, Chun hwa KIM, Jae Keol RHEE
  • Publication number: 20160355484
    Abstract: Articles and methods comprising persistent carbenes are provided, as well as related compositions. In some embodiments, a persistent carbene may be associated with a portion of a substrate (e.g., at least a portion of a surface on the substrate). In certain embodiments, the association of persistent carbene with the substrate may be used to affect certain properties of substrate (e.g., surface chemistry, stability). In some cases, a persistent carbene may be functionalized after association with a portion of a substrate. In some embodiments, a persistent carbene and at least one secondary compound may be associated with a portion of a substrate. Articles and methods of the present invention may be useful for applications involving electronics, sensing, microfabrication, nanotechnology, biomimetic, and drug delivery, amongst others.
    Type: Application
    Filed: June 2, 2016
    Publication date: December 8, 2016
    Applicant: Massachusetts Institute of Technology
    Inventors: Jeremiah A. Johnson, Aleksandr V. Zhukhovitskiy
  • Publication number: 20160355485
    Abstract: The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.
    Type: Application
    Filed: September 24, 2014
    Publication date: December 8, 2016
    Inventors: George R. Ehring, Ellen Chao, Herman Ng, Hau Ton, Jia Chian Li, Joseph S. Adorante, Michael E. Garst, Howard B. Rind, Mark R. Hansen, Alfred Arthur Avey, JR., Lloyd Jay Dolby, Shervin Esfandiari, Vivian R. MacKenzie, Jeremiah Andrew Marsden, David Charles Muchmore
  • Publication number: 20160355486
    Abstract: The present invention relates to methods and intermediates useful for the synthesis of protein deacetylase inhibitors.
    Type: Application
    Filed: June 8, 2016
    Publication date: December 8, 2016
    Inventors: Farzaneh Seyedi, John H. van Duzer
  • Publication number: 20160355487
    Abstract: The present invention provides novel phenazine derivatives, such as compounds of Formula (I) and (II), and pharmaceutically acceptable salts thereof. The compounds of the invention are expected to be antimicrobial agents and may act by a microbial warfare strategy (e.g., a reactive oxygen species (ROS)-based competition strategy). The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the compounds of the invention and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium), killing a microorganism (e.g., a bacterium), inhibiting the formation and/or growth of a biofilm, or reducing or clearing a biofilm.
    Type: Application
    Filed: December 23, 2014
    Publication date: December 8, 2016
    Applicant: University of Florida Research Foundation, Incorporated
    Inventors: Robert William Huigens, III, Shouguang Jin
  • Publication number: 20160355488
    Abstract: The invention relates to triazole compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as modulators of demyelinating diseases: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention, methods of using the compositions and kits thereof in the treatment of various demyelinating and neurodegenerative diseases, including multiple sclerosis.
    Type: Application
    Filed: June 3, 2016
    Publication date: December 8, 2016
    Inventors: Robert J. Davies, Jingrong Cao, Meghan Elise Cockerill, Philip Noel Collier, Elisabeth Doyle, James Daniel Frantz, Huai Gao, Brian Anthony Goldman, Ronald Lee Grey, Jr., Anne-Laure Grillot, Wenxin Gu, James A. Henderson, Raul Eduardo Krauss Irarrazaval, Adrianne Lynn Kolpak, Yusheng Liao, Sanjay Shivayogi Magavi, David Messersmith, Albert Charles Pierce, Emanuele Perola, Elizabeth Jin-Sun Ryu, Joshua Syken, Jian Wang, Michael Paul DeNinno, Francois Maltais
  • Publication number: 20160355489
    Abstract: Compounds of formula (I), wherein Z=cyclopentyl. cyclopropylmethyl, —CH3; R?=—CH3, CHF2, X=formula (II) (III) (IV) (V) Y=—CO; —C?O(CH2), —CH(OH)—CH2, —CH2—C?O, —CH2—CH2—C?O; —CH2—CH(OH)—CH2, —CH2—CH(OCOR1)—CH2 NR2=—N(CH2—CH2OH)2, formula (VI) (VII) (VIII) (IX) (X) (XI) R1=optionally substituted C1-C8 alkyl, optionally substituted aryl; optionally substituted aralkyl, preferably C1-C3 alkyl, more preferably CH3; and enantiomers, diastereoisomers and pharmaceutically acceptable salts thereof; these compounds have a PDE4D inhibiting activity and can be used as a medicament for treating dementia, in particular Alzheimer disease, and for improving memory.
    Type: Application
    Filed: February 10, 2015
    Publication date: December 8, 2016
    Inventors: Olga BRUNO, Chiara BRULLO, Alessia ROMUSSI, Ernesto FEDELE, Roberta RICCIARELLI, Ottavio ARANCIO, Jos PRICKAERTS
  • Publication number: 20160355490
    Abstract: The present invention provides a process for forming vinyl-containing compounds including the steps of: a) reacting in a nitrogen atmosphere a dicarboxylic acid and/or anhydride and a functional mono or polyfunctional alcohol to provide a hydroxyl-containing polyester; b) reacting the hydroxyl-containing polyester with a vinyl-containing organic acid in the presence of an esterification catalyst, a polymerization inhibitor and an azeotropic agent; and c) reacting the vinyl functional esterified intermediate, residual esterification catalyst and residual vinyl-containing organic acid with an epoxy to provide the vinyl-containing compound.
    Type: Application
    Filed: August 10, 2016
    Publication date: December 8, 2016
    Inventors: Hildeberto Nava, Yongning Li
  • Publication number: 20160355491
    Abstract: An object of the present invention is to provide high-purity gamma-butyrolactone (GBL) capable of preventing occurrence of reaction other than the object at the time of use, which reaction is caused due to a high acidity of GBL, and the present invention relates to a gamma-butyrolactone composition containing gamma-butyrolactone and a nitrogen-containing compound, wherein a content of the gamma-butyrolactone is 99.0% by mass or more, and a total content of the nitrogen-containing compound is 0.1 ppm by mass to 1,000 ppm by mass as converted to a nitrogen atom.
    Type: Application
    Filed: August 17, 2016
    Publication date: December 8, 2016
    Applicant: MITSUBISHI CHEMICAL CORPORATION
    Inventors: Shohei Taniguchi, Yusuke Izawa, Masaru Utsunomiya
  • Publication number: 20160355492
    Abstract: This disclosure relates to sulfurized derivatives made from functionalized monomers. The disclosure relates to lubricants, functional fluids, fuels, dispersants, detergents and functional compositions (e.g., cleaning solutions, food compositions, etc.
    Type: Application
    Filed: August 19, 2016
    Publication date: December 8, 2016
    Applicant: Elevance Renewable Sciences, Inc.
    Inventors: Stephen A. Di Biase, Syed Q. A. Rizvi, Georgeta Hategan
  • Publication number: 20160355493
    Abstract: The present invention develops a series of methyl caffeate derivatives having biological activity in anti-angiogenesis. The present invention suggests that the compounds of the invention possess inhibiting angiogenesis through regulation of VEGF/VEGFR-2 and its downstream signaling cascades in the vascular endothelial cells (VECs).
    Type: Application
    Filed: June 4, 2015
    Publication date: December 8, 2016
    Inventors: Chieh-Hsi Wu, Yueh-Hsiung Kuo, Chun-Hsu Pan
  • Publication number: 20160355494
    Abstract: A fused heterocyclic compound having an enteropeptidase inhibitory action and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided. Specifically, a compound represented by the following formula (I): wherein each symbol is as defined herein, or a salt thereof and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided.
    Type: Application
    Filed: February 12, 2015
    Publication date: December 8, 2016
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Minoru SASAKI, Keiko KAKEGAWA, Fumiaki KIKUCHI, Zenichi IKEDA, Yoichi NISHIKAWA
  • Publication number: 20160355495
    Abstract: An organocatalytic kinetic resolution of racemic secondary nitroallylic alcohols via Michael/acetalization sequence to give fully substituted tetrahydropyranols is described. The process affords the products with high to excellent stereoselectivities. The highly enantioenriched, less reactive (S)-nitroallylic alcohols were isolated with good to high chemical yields. The synthetic application of the resolved substrate is shown toward the synthesis of enantioenriched (+)-(2S,3R)-3-amino-2-hydroxy-4-phenylbutyric acid.
    Type: Application
    Filed: October 1, 2015
    Publication date: December 8, 2016
    Inventors: Kwunmin Chen, Ramani Gurubrahamam, You-Song Cheng
  • Publication number: 20160355496
    Abstract: Compounds of formula (IIc); wherein X3 and X4 independently from each other are N or CR8 wherein R8 may be same or different; Y1, Y2, Y3 and Y4 independently from each other are N or CR9 wherein R9 may be same or different and wherein up to 3 of the group Y1, Y2, Y3 and Y4 may be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.
    Type: Application
    Filed: May 19, 2016
    Publication date: December 8, 2016
    Inventors: Michael BOUTROS, Rajendra-Prasad MASKEY, Corinna KOCH, Florian FUCHS, Sandra STEINBRINK, Daniel GILBERT
  • Publication number: 20160355497
    Abstract: There is provided a production method of a thiopyranose compound represented by the following Formula (2) by reacting a compound represented by the following Formula (1) with a sulfur compound. X represents a leaving group. A represents an oxygen atom or a sulfur atom. Further, each of R1A to R4B, R1B to R4B, and R5 represents a hydrogen atom or a specific substituent.
    Type: Application
    Filed: August 17, 2016
    Publication date: December 8, 2016
    Applicant: FUJIFILM Corporation
    Inventors: Akira TAKEDA, Toru WATANABE, Taiji KATSUMATA, Takayuki ITO, Toshihiko SAWADA
  • Publication number: 20160355498
    Abstract: Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are described, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Application
    Filed: June 3, 2016
    Publication date: December 8, 2016
    Inventors: Wei Chen, Zhaozhong J. Jia, William D. Thomas
  • Publication number: 20160355499
    Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.
    Type: Application
    Filed: June 10, 2016
    Publication date: December 8, 2016
    Inventor: Laykea TAFESSE
  • Publication number: 20160355500
    Abstract: The present invention relates to a process for the preparation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylene-1-piperidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol (Efinaconazole) and intermediates used in such process.
    Type: Application
    Filed: March 2, 2015
    Publication date: December 8, 2016
    Applicant: MAPI PHARMA LTD.
    Inventors: Anna GOPIN, Shai RUBNOV, Galina ZATS, Ehud MAROM