Patents Issued in December 20, 2018
  • Publication number: 20180362449
    Abstract: A method of altering exocytosis in a plant or animal cell is provided. The method includes exposing the cell to a compound that binds to an EXO70 protein isoform. Also provided is a method of treating diabetes or cancer in a subject in need thereof which includes administering to the subject an effective amount of a compound that binds to an EXO70 protein isoform. In addition, a method of screening for a substance that alters exocytosis in a plant or animal cell is provided, and analogs of compound Endosidin2 are also provided.
    Type: Application
    Filed: September 15, 2016
    Publication date: December 20, 2018
    Applicant: The Regents of the University of California
    Inventors: Natasha V. Raikhel, Glenn R. Hicks, Chunhua Zhang
  • Publication number: 20180362450
    Abstract: Disclosed is a malononitrile oxime ether compound having a novel structure as shown in the general formula I. Respective substituents in the general formula I as defined in the specification. The compound of the general formula I exhibits an excellent microbicidal activity, and can effectively prevent and treat plant diseases caused by bacteria and fungi. Also provided is a use of the compound of the general formula I as a microbicide in the agricultural and other fields.
    Type: Application
    Filed: December 22, 2016
    Publication date: December 20, 2018
    Applicant: Shenyang Sinochem Agrochemicals R&D Co., Ltd.
    Inventors: Xueming CHENG, Lixin ZHANG, Liang CHEN, Qin SUN, Junli LIU, Zhinian LI, Jie ZHAO, Jingbo XU, Hongfei WU
  • Publication number: 20180362451
    Abstract: Compounds of the formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.
    Type: Application
    Filed: December 12, 2016
    Publication date: December 20, 2018
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Matthias Weiss, Julien Daniel Gagnepain, Thomas James Hoffman, Sarah Sulzer-Mosse, Clemens Lamberth
  • Publication number: 20180362452
    Abstract: A shell-and-tube stripper for carbamate decomposition and ammonia recovery from a urea solution comprising a bundle of heated tubes, said tubes being fed with said urea solution and carbon dioxide as stripping medium, the urea solutions forming a liquid falling film on the internal surface of the tubes and the carbon dioxide forming a counter-current gaseous flow; said tubes comprise an external layer made of super austenitic or super duplex stainless steel and an internal layer made of zirconium, said internal layer reaching temperatures higher than 220° C.
    Type: Application
    Filed: December 9, 2016
    Publication date: December 20, 2018
    Applicant: Casale SA
    Inventor: Luca Rugnone
  • Publication number: 20180362453
    Abstract: A process is described for the production of formaldehyde, comprising (a) subjecting methanol to oxidation with air in a formaldehyde production unit thereby producing a formaldehyde-containing stream; (b) separating said formaldehyde-containing stream into a formaldehyde product stream and a formaldehyde vent gas stream; wherein the vent gas stream, optionally after treatment in a vent gas treatment unit, is passed to one or more stages of: (i) synthesis gas generation, (ii) carbon dioxide removal, (iii) methanol synthesis or (iv) urea synthesis.
    Type: Application
    Filed: August 27, 2018
    Publication date: December 20, 2018
    Inventors: Ola Erlandsson, Andreas Magnusson, John David Pach, Daniel Sheldon
  • Publication number: 20180362454
    Abstract: There is provided a novel gelator containing a monourea derivative. A gelator comprising a compound of formula (1): wherein R1 is a linear or branched alkyl group having a carbon atom number of 2 to 20, a cyclic alkyl group having a carbon atom number of 3 to 20, or a linear or branched alkenyl group having a carbon atom number of 12 to 20; and Ar is a C6-18 aryl group unsubstituted or optionally substituted with at least one substituent selected from the group consisting of a C1-10 alkyl group, a C1-10 alkoxy group, a C6-18 aryloxy group, a halogen atom, a nitro group, a phenyl group, a C2-10 alkylcarbonyl group, and a C7-18 aralkyl group.
    Type: Application
    Filed: December 9, 2016
    Publication date: December 20, 2018
    Applicants: NATIONAL UNIVERSITY CORPORATION SHIZUOKA UNIVERSITY, NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Masamichi YAMANAKA, Nobuhide MIYACHI
  • Publication number: 20180362455
    Abstract: Provided herein is a method for preparing a salt including cations of an arene-transition metal sandwich complex and anions of a Brönsted acid.
    Type: Application
    Filed: December 9, 2016
    Publication date: December 20, 2018
    Inventors: Maximilian Hemgesberg, Juergen Frank, Ralf Noerenberg
  • Publication number: 20180362456
    Abstract: The present invention describes new derivatives of S-allylcysteine with antioxidant and antiaging activity. Said derivatives can be used alone or in a combined formulation with other compounds with known activity.
    Type: Application
    Filed: December 6, 2016
    Publication date: December 20, 2018
    Inventors: Giancarlo SANTUS, Silvana MASIERO, Leticia Khater COVESI
  • Publication number: 20180362457
    Abstract: The subject of the invention is a novel process for the preparation of Carboprost tromethamine salt where alkylation the enone of the general formula (II) is carried out in the presence of a chiral auxiliary in aprotic solvent with a Grignard reagent. The methyl ester epimers of formula (VII) are separated by gravity silicagel chromatography and the salt formation is carried out by using solid tromethamine base.
    Type: Application
    Filed: November 10, 2016
    Publication date: December 20, 2018
    Applicant: CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT .
    Inventors: Péter BUZDER-LANTOS, Zsuzsanna KARDOS, Irén HORTOBÁGYI, István LÁSZLÓFI, Imre JUHÁSZ, László FÓNAGY, Csaba VÁRADI, Ágnes NAGYNÉ BORKÓ
  • Publication number: 20180362458
    Abstract: Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
    Type: Application
    Filed: September 30, 2016
    Publication date: December 20, 2018
    Inventors: Pravin L. Kotian, Yarlagadda S. Badu, V. Satish Kumar, Weihe Zhang, Lakshminarayana Vogeti
  • Publication number: 20180362459
    Abstract: A method is provided to conveniently separate racemic (3R,4S)-3-acetamido-4-allyl-N-(tert-butyl)pyrrolidine-3-carboxamide and (3S,4R)-3-acetamido-4-allyl-N-(tert-butyl)pyrrolidine-3-carboxamide using selective crystallization with chiral carboxylic acids.
    Type: Application
    Filed: May 11, 2018
    Publication date: December 20, 2018
    Inventors: Michael C. VAN ZANDT, Jennifer L. SAVOY
  • Publication number: 20180362460
    Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of Cezanne 1 and ubiquitin C-terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of cancer. Compounds of the invention include compounds having the formula (I): pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c, R1d, R1e, R1f and A are as defined herein.
    Type: Application
    Filed: December 21, 2016
    Publication date: December 20, 2018
    Inventors: Mark Ian KEMP, Michael David WOODROW
  • Publication number: 20180362461
    Abstract: The invention relates to a compound of formula (I) wherein R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: August 24, 2018
    Publication date: December 20, 2018
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Wolfgang Haap, Bernd Kuhn, Thomas Luebbers, Jens-Uwe Peters
  • Publication number: 20180362462
    Abstract: The present disclosure provides compounds and nanostructures having one or more quaternary ammonium salts, compositions including the compounds and nanostructures, and methods useful for treating conditions using the compounds, nanostructures, and compositions. In at least one aspect, a compound is represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein: Q is fluoro, chloro, bromo, or iodo; each of s, b, and n is independently an integer from about 10 to about 100; and each of v, j, p, z, q, x and m is independently an integer from 1 to about 20.
    Type: Application
    Filed: December 12, 2017
    Publication date: December 20, 2018
    Inventors: Michael MONTEIRO, Jason W. ARMSTRONG
  • Publication number: 20180362463
    Abstract: An object of the present invention is to provide a bismaleimide (D-BMI) modified product in which an amino group of dimer diamine (DDA) is maleimidized, which has the good heat resistance, and has the sufficiently enhanced processability, and a method for producing the same. There are provided: <1> A bismaleimide (D-BMI) modified product in which an amino group of dimer diamine is maleimidized, the bismaleimide modified product having the following characteristics: 1) An acid value of the D-BMI modified product is 2 mg-KOH/g or less. 2) In 1H-NMR, when quantitative comparison is performed using an integrated value (A) of a peak corresponding to a proton of a methylene group directly bound to a nitrogen atom of a maleimide group and an integrated value (B) of a peak corresponding to a vinyl proton of a maleimide group, A/B is 1.25 or more and 2.00 or less.
    Type: Application
    Filed: June 18, 2018
    Publication date: December 20, 2018
    Applicant: UNITIKA LTD.
    Inventors: Yuki YAMADA, Tatsuya MORIKITA, Takeshi YOSHIDA, Akira SHIGETA, Yoshiaki ECHIGO
  • Publication number: 20180362464
    Abstract: The present invention provides a method for producing a 2-aminonicotinic acid benzyl ester derivative. The method includes, as a step, reacting a 2-aminonicotinic acid derivative represented by the formula [I], wherein R1 represents a hydrogen atom or a C1 to C4 alkyl group and M represents an alkali metal, with a benzyl derivative represented by the formula [II], wherein R2 represents, for example, a hydrogen atom or a halogen atom, A represents, for example, a nitrogen atom, X represents a halogen atom, and Y represents, for example, an oxygen atom, in an aromatic hydrocarbon solvent in the presence of a phase transfer catalyst or a tertiary amine.
    Type: Application
    Filed: November 8, 2016
    Publication date: December 20, 2018
    Applicant: AGRO-KANESHO CO., LTD.
    Inventors: Ryo AIZAWA, Koichi ARAKI
  • Publication number: 20180362465
    Abstract: Disclosed are derivative compounds of ELQ-300 that include an ester at position 4. These compounds have enhanced properties relative to ELQ-300. Also disclosed are pharmaceutical compositions comprising the compounds and methods of treating and preventing malaria infections involving administering the pharmaceutical compositions to the subject.
    Type: Application
    Filed: August 23, 2018
    Publication date: December 20, 2018
    Inventors: Michael Riscoe, Aaron Nilsen, Allison Stickles, Galen Miley, Rolf Winter, Sovitj Pou, Yuexin Li, Jane Xu Kelly, Isaac Forquer, J. Stone Doggett, Igor Bruzual, Lisa Frueh, Rozalia Dodean, Martin Smilkstein, Holland Alday, Dennis Koop, Lisa Bleyle
  • Publication number: 20180362466
    Abstract: Quinoline compounds and salts, hydrates or solvates serving as a selective uric acid reabsorption inhibitor, can be used in the treatment of hyperuricemia and gout by promoting uric acid to excrete from the body and reducing serum uric acid. Such compounds have the effect of reducing the uric acid in the animal body and human body.
    Type: Application
    Filed: December 6, 2016
    Publication date: December 20, 2018
    Inventors: Lei FAN, Wu DU, Xinghai LI, Yuanwei CHEN, Kexin XU, Ke CHEN, Shaohua ZHANG, Tongchuan LUO
  • Publication number: 20180362467
    Abstract: The invention relates to 18-20 member bi-polycyclic compounds, methods of making these compounds, and methods of using them in treating hyperproliferative disorders (e.g., cancer) and non-malignant tumors; promoting muscle formation; inhibiting muscle degeneration or the loss of muscle mass or muscle function; and myofibers ex vivo.
    Type: Application
    Filed: December 6, 2017
    Publication date: December 20, 2018
    Inventors: David Bettoun, Eduardo Martinez, James Gleason, Sylvie Mader, Shuo Xing
  • Publication number: 20180362468
    Abstract: Provided are compounds, including those of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.
    Type: Application
    Filed: August 22, 2018
    Publication date: December 20, 2018
    Inventors: Franco J. Duarte, Neel K. Anand, Pankaj Sharma, Devendrapratap Singh
  • Publication number: 20180362469
    Abstract: The invention relates to dextrorphan-derivatives, pharmaceutical compositions and pharmaceutical dosage forms containing such dextrorphan-derivatives as well as the use of those dextrorphan-derivatives and/or compositions for treating and preventing diseases and conditions in man and mammals.
    Type: Application
    Filed: December 2, 2016
    Publication date: December 20, 2018
    Inventors: Eckhard Lammert, Alena Welters, Silke Otter, Jan Marquard, Thomas Meissner, Diran Herebian, Ertan Mayatepek
  • Publication number: 20180362470
    Abstract: A compound represented by Formula (I), or a salt or N-oxide compound thereof is provided. In Formula (I), A1 to A4 each independently represents a carbon atom or nitrogen atom, X1 represents a C1-6 alkyl group or the like, n represents the number of X1 groups, R1 represents a C1-6 alkylthio group or the like, and D is a group represented by Formula (D-1) or (D-2), and in Formula (D-1) and (D-2), * represents a binding position, Q represents a C1-6 alkyl group or the like, B1 and B2 each independently represents a nitrogen atom or the like, R2 represents a C1-6 alkyl group or the like that is bound to one of the nitrogen atoms in Formula (D-1), B3 and B4 each independently represents a nitrogen atom or carbon atom, R4 represents a C1-6 alkyl group or the like, and m represents the number of R4 groups.
    Type: Application
    Filed: December 15, 2016
    Publication date: December 20, 2018
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Hikaru AOYAMA, Keita SAKANISHI, Takao IWASA, Tomomi KOBAYASHI
  • Publication number: 20180362471
    Abstract: The present invention provides substituted heterocyclyl derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.
    Type: Application
    Filed: June 3, 2016
    Publication date: December 20, 2018
    Applicant: Aurigene Discovery Technologies Limited
    Inventors: Susanta Samajdar, Ramulu Poddutoori, Chetan Pandit, Subhendu Mukherjee, Rajeev Goswami
  • Publication number: 20180362472
    Abstract: Disclosed herein are compounds of formula (I), and methods of inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I).
    Type: Application
    Filed: June 15, 2018
    Publication date: December 20, 2018
    Inventors: Vincent Jacques, James R. Rusche
  • Publication number: 20180362473
    Abstract: The invention provides a new bioorthogonal deprotection method for preparing heterocyclic compounds by bond cleavage using palladium. The methods have general application in the field of biological synthetic chemistry. Compounds, such as prodrugs, which are useful in such methods are also provided.
    Type: Application
    Filed: May 11, 2018
    Publication date: December 20, 2018
    Inventors: Asier UNCITI-BROCETA, Jason WEISS
  • Publication number: 20180362474
    Abstract: The present invention relates to LpxC antibacterial compounds of Formula (IA): corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation, treatment methods and uses for bacterial infections, especially those caused by gram-negative bacteria.
    Type: Application
    Filed: December 8, 2016
    Publication date: December 20, 2018
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Qi JIN, Denise Teotico POHLHAUS, Jared T. SPLETSTOSER
  • Publication number: 20180362475
    Abstract: The present invention relates to spiropyrazine compounds which are inhibitors of non-apoptotic regulated cell death, and to pharmaceutical compositions containing such compounds. Furthermore, the present invention relates to the use of such compounds and pharmaceutical compositions in therapy, in particular in the treatment of a condition, disorder or disease that is characterised by non-apoptotic regulated cell-death or where non-apoptotic regulated cell-death is likely to play or plays a substantial role.
    Type: Application
    Filed: November 10, 2015
    Publication date: December 20, 2018
    Inventors: Marcus Conrad, Joel Schick, Bettina Proneth, Peter Sennhenn
  • Publication number: 20180362476
    Abstract: The present invention relates to new class of functionalized macrocycles capable of chelating paramagnetic metal ions, their chelated complexes with metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.
    Type: Application
    Filed: December 12, 2016
    Publication date: December 20, 2018
    Applicant: BRACCO IMAGING S.P.A.
    Inventors: Luciano LATTUADA, Roberta NAPOLITANO, Valeria BOI, Massimo VISIGALLI, Silvio AIME, Giovanni Battista GIOVENZANA, Alberto FRINGUELLO MINGO
  • Publication number: 20180362477
    Abstract: The present invention provides an oxazine compound having a specific structure, which contains a group having an aromatic ring structure and a plurality of specified carbon-carbon triple bond structure. The present invention further provides a composition containing the oxazine compound having a specific structure of the present invention, a cured product containing the composition, and a laminate having a layer of the cured product. The present invention further still provides a composition for a heat-resistant material and a composition for an electronic material, which contain the composition containing the oxazine compound of the present invention.
    Type: Application
    Filed: November 24, 2016
    Publication date: December 20, 2018
    Inventors: Tomohiro Shimono, Junji Yamaguchi, Masato Otsu, Kazuo Arita
  • Publication number: 20180362478
    Abstract: The present invention provides an oxazine compound having a specific structure, which contains a group having an aromatic ring structure and a plurality of specified carbon-carbon triple bond structure. The present invention further provides a composition containing the oxazine compound having a specific structure of the present invention, a cured product containing the composition, and a laminate having the layer of the cured product. The present invention further still provides a composition for a heat-resistant material and a composition for an electronic material, which contain the composition containing the oxazine compound of the present invention.
    Type: Application
    Filed: November 24, 2016
    Publication date: December 20, 2018
    Inventors: Tomohiro SHIMONO, Kazuo ARITA, Junji YAMAGUCHI, Masato OTSU
  • Publication number: 20180362479
    Abstract: The present invention provides an oxazine compound which contains a group having an aromatic ring structure and a plurality of specified carbon-carbon double bond structure so as to achieve an object. The present invention further provides a composition containing the oxazine compound of the present invention, a cured product containing the composition, and a laminate having a layer of the cured product. The present invention further still provides a composition for a heat-resistant material and a composition for an electronic material, which contain the composition containing the oxazine compound of the present invention so as to achieve the object.
    Type: Application
    Filed: November 8, 2016
    Publication date: December 20, 2018
    Inventors: Masato Otsu, Tomohiro Shimono, Kazuo Arita, Junji Yamaguchi
  • Publication number: 20180362480
    Abstract: The present invention provides an oxazine compound having a specific structure, which contains a group having an aromatic ring structure and a plurality of specified carbon-carbon triple bond structure. The present invention further provides a composition containing the oxazine compound having a specific structure of the present invention, a cured product containing the composition, and a laminate having a layer of the cured product. The present invention further still provides a composition for a heat-resistant material and a composition for an electronic material, which contain the composition containing the oxazine compound of the present invention.
    Type: Application
    Filed: November 24, 2016
    Publication date: December 20, 2018
    Applicant: DIC Corporation
    Inventors: Kazuo ARITA, Tomohiro SHIMONO, Masato OTSU, Junji YAMAGUCHI, Etsuko SUZUKI
  • Publication number: 20180362481
    Abstract: The present invention relates to medicine and includes a method for preventing and treating diseases caused by RNA- and DNA-containing viruses, and concomitant diseases, wherein the method comprises the use of an effective amount of compounds of general formula I or pharmaceutically acceptable salts thereof. The invention also relates to methods for preparing said compounds, pharmaceutical compositions for the prevention or treatment of diseases caused by RNA- and DNA-containing viruses, said compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 17, 2018
    Publication date: December 20, 2018
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
  • Publication number: 20180362482
    Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Application
    Filed: December 12, 2016
    Publication date: December 20, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Yongxin Han, Abdelghani Achab, Purakkattle Biju, Yongqi Deng, Xavier Fradera, Liangqin Guo, Shuwen He, Joseph Kozlowski, Ravi Kurukulasuriya, Kun Liu, Meredeth Ann McGowan, Qinglin Pu, Nunzio Sciammetta, Hongjun Zhang, Hua Zhou
  • Publication number: 20180362483
    Abstract: The present invention provides novel compounds of Formulae (I?), (I), (II?), and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.
    Type: Application
    Filed: September 9, 2016
    Publication date: December 20, 2018
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Tinghu Zhandg, Nicholas Paul Kwiatkowski, Mingfeng Hao
  • Publication number: 20180362484
    Abstract: 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 reducing (5-methylfuran-2-yl)methanol or 2-(chloromethyl)-5-methylfuran.
    Type: Application
    Filed: January 12, 2018
    Publication date: December 20, 2018
    Applicant: MICROMIDAS, INC.
    Inventors: Dimitri A. Hirsch-Weil, Makoto N. Masuno, John Bissell, Dennis A. Hucul, Alex B. Wood, Robert Joseph Araiza, Daniel R. Henton
  • Publication number: 20180362485
    Abstract: Compounds of Formulas (I) and (II): and salts thereof; methods of making and using the same, including use for inhibiting BMP1, TLL1 and/or TLL2 and in treatment of diseases associated with BMP1, TLL1 and/or TLL2 activity.
    Type: Application
    Filed: July 8, 2016
    Publication date: December 20, 2018
    Inventors: Carla A. DONATELLI, Sarah E. DOWDELL, Mark ELBAN, Mark A. HILFIKER, Tram H. HOANG, Dennis Alan HOLT, Sharada MANNS, Andrew MARCUS, Craig POTTEIGER, Raynold SHENJE, David G. WASHBURN
  • Publication number: 20180362486
    Abstract: The present invention relates to a process for the production of 2,5-furandicarboxylic acid (FDCA) via oxidation of 5-hydroxymethyl-2-furfural (HMF), said HMF being present in a solution in a high-boiling polar solvent and water. The process is characterized by the combination of—a first oxidation step wherein the HMF is at least partly oxidized in said solution to yield a first reaction mixture comprising at least one monoacid selected from the group consisting of -hydroxymethylfuran-2-carboxylic acid (HMFA), 5-formylfuran-2-carboxylic acid (FFCA) and, optionally, FDCA—an extraction step after the first oxidation step wherein said high-boiling polar solvent is extracted from said first reaction mixture by means of an extraction solvent, wherein said at least one monoacid remains in an aqueous phase,—a second oxidation step wherein said at least one monoacid is oxidized to FDCA.
    Type: Application
    Filed: December 7, 2016
    Publication date: December 20, 2018
    Inventors: Gunter TEKAUTZ, Dirk KIRSCHNECK, Walter LINHART
  • Publication number: 20180362487
    Abstract: Disclosed is a configurational stereoisomer, named enantiomer E3, of bromadiolone having, by chromatographic analysis of a bromadiolone composition including four configurational stereoisomers of bromadiolone performed under the conditions described hereinbelow, a retention time t3 having a value such that t1<t2<t3<t4; t1, t2 and t4 being the retention times of the configurational stereoisomers of bromadiolone different from the enantiomer E3, the analysis being performed at a temperature of 27.3° C.
    Type: Application
    Filed: December 6, 2016
    Publication date: December 20, 2018
    Inventors: Hervé CARUEL, Etienne BENOIT, Isabelle FOUREL, Virginie LATTARD
  • Publication number: 20180362488
    Abstract: Disclosed is a configurational stereoisomer, referred to as enantiomer E2, of flocoumafen, the enantiomer E2 having, as determined by the chromatographic analysis of a flocoumafen composition including four configurational stereoisomers of flocoumafen, carried out under conditions described hereinafter, a retention time t2 with a value such that t1<t2<t3<t4; t1, t3 and t4 representing the retention times of the configurational stereoisomers of flocoumafen different from the enantiomer E2, the chromatographic analysis being carried out at a temperature of 23.5° C.
    Type: Application
    Filed: December 6, 2016
    Publication date: December 20, 2018
    Inventors: Hervé CARUEL, Etienne BENOIT, Isabelle FOUREL, Virginie LATTARD
  • Publication number: 20180362489
    Abstract: Disclosed is a composition including flocoumafen and an amount of a configurational stereoisomer of flocoumafen, named enantiomer E4, such that the ratio of this amount to the amount of flocoumafen in the composition is less than 10%, the enantiomer E4 being present with the exclusion of a racemic mixture, the enantiomer E4 having, by chromatographic analysis of flocoumafen, a retention time t4 having a value such that t1<t2<t3<t4; t1, t2 and t3 representing the retention times of the configurational stereoisomers of flocoumafen different from the enantiomer E4, the chromatographic analysis being performed at a temperature of 23.5° C.
    Type: Application
    Filed: December 6, 2016
    Publication date: December 20, 2018
    Inventors: Hervé CARUEL, Etienne BENOIT, Isabelle FOUREL, Virginie LATTARD
  • Publication number: 20180362490
    Abstract: Disclosed is a configurational stereoisomer, named enantiomer E1, of bromadiolone having, by chromatographic analysis of bromadiolone including four configurational stereoisomers of bromadiolone performed under the conditions described below, a retention time t1 having a value such that t1<t2<t3<t4; t2, t3 and t4 being the retention times of the configurational stereoisomers of bromadiolone different from the enantiomer E1, the analysis being performed at a temperature of 27.3° C.
    Type: Application
    Filed: December 6, 2016
    Publication date: December 20, 2018
    Inventors: Hervé CARUEL, Etienne BENOIT, Isabelle FOUREL, Virginie LATTARD
  • Publication number: 20180362491
    Abstract: Disclosed is a configurational stereoisomer, named enantiomer E3, of flocoumafen, the enantiomer E3 having, by chromatographic analysis of flocoumafen performed under particular conditions, a retention time t3 having a value such that t1<t2<t3<t4; t1, t2 and t4 representing the retention times of the configurational stereoisomers of flocoumafen different from the enantiomer E3, the analysis being performed at a temperature of 23.5° C.
    Type: Application
    Filed: December 6, 2016
    Publication date: December 20, 2018
    Inventors: Hervé CARUEL, Etienne BENOIT, Isabelle FOUREL, Virginie LATTARD
  • Publication number: 20180362492
    Abstract: Provided herein are methods for making an alpha-tocotrienol enriched tocol mixture, such as from a plant or plant-derived material. Also provided herein are simulated moving bed purification methods for tocotrienol compounds such as alpha tocotrienol.
    Type: Application
    Filed: December 16, 2016
    Publication date: December 20, 2018
    Inventors: Peter GIANNOUSIS, Paul MOLLARD, Noah M. BENJAMIN, Jeffrey D. BUTLER, Olivier DAPREMONT, James B. FALABELLA
  • Publication number: 20180362493
    Abstract: The present invention generally relates to various dinaphthothiophene compounds and processes for preparing these compounds.
    Type: Application
    Filed: June 20, 2018
    Publication date: December 20, 2018
    Applicant: Saint Louis University
    Inventors: Ryan D. McCulla, John T. Petroff, II, Satyanarayana M. Chintala, John C. Throgmorton
  • Publication number: 20180362494
    Abstract: Disclosed is to a laevorotatory enantiomer of the configurational stereoisomer of difethialone, named hetero-stereoisomer, the formula of which is 3-(4?-bromobiphenyl-4-yl)-1-(4-hydroxythiocoumarin-3-yl)-1,2,3,4-tetrahydronaphthalene, in which carbons 1 and 3 of the 1,2,3,4-tetrahydronaphthalene group have different absolute configurations.
    Type: Application
    Filed: December 6, 2016
    Publication date: December 20, 2018
    Inventors: Hervé CARUEL, Etienne BENOIT, Isabelle FOUREL, Virginie LATTARD
  • Publication number: 20180362495
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, (I) 0 wherein A, X1, X2, X3 and X4 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: December 8, 2016
    Publication date: December 20, 2018
    Inventors: Wenming Zhang, Michael Alan Rossi
  • Publication number: 20180362496
    Abstract: The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.
    Type: Application
    Filed: August 30, 2018
    Publication date: December 20, 2018
    Applicant: NOVARTIS AG
    Inventors: Christine Hiu-Tung Chen, Zhuoliang Chen, Jorge Garcia Fortanet, Denise Grunenfelder, Rajesh Karki, Mitsunori Kato, Matthew J. LaMarche, Lawrence Blas Perez, Travis Matthew Stams, Sarah Williams
  • Publication number: 20180362497
    Abstract: Disclosed herein are compounds, compositions, and methods of their use for the treatment of diabetes.
    Type: Application
    Filed: June 24, 2016
    Publication date: December 20, 2018
    Inventors: Hank Michael James PETRASSI, Murali Mohan Reddy PERAM SURAKATTULA, Kathrin MAEDLER, Amin ARDESTANI, Jason T. ROLAND, Tyler D. BAGULEY, Matthew S. TREMBLAY, Weijun SHEN, Peter G. SCHULTZ, Arnab K. CHATTERJEE
  • Publication number: 20180362498
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of one or both of ERK1 and ERK2.
    Type: Application
    Filed: June 14, 2018
    Publication date: December 20, 2018
    Inventors: Antonio Christian Ferretti, Lianfeng Huang, Ying Li, John Traverse, Jean Xu, Kelvin Hin-Yeong Yong, Daozhong Zou