Patents Issued in April 30, 2020
  • Publication number: 20200131117
    Abstract: Provided is a novel method for producing amide compounds at high stereochemical selectivities. The method according to the present invention for producing amide compounds is provided with an amidation step for reacting, in the presence of a catalyst comprising a metal compound, an amino compound with an aminoester compound represented by general formula (1) to amidate the ester group in the aminoester compound.
    Type: Application
    Filed: April 25, 2018
    Publication date: April 30, 2020
    Inventors: Hisashi YAMAMOTO, Wataru MURAMATSU, Tomohiro HATTORI, Yasushi SHIMODA
  • Publication number: 20200131118
    Abstract: An object of the present invention is to provide a chemical liquid having excellent defect inhibition performance and a chemical liquid storage body. The chemical liquid according to an embodiment of the present invention is a chemical liquid containing an organic solvent that has a conductivity equal to or lower than 10?5 S/m at 25° C., and a compound represented by General Formula (I), in which a content of the compound represented by General Formula (I) with respect to the total mass of the chemical liquid is 0.10 mass ppt to 100,000 mass ppt.
    Type: Application
    Filed: January 2, 2020
    Publication date: April 30, 2020
    Applicant: FUJIFILM Corporation
    Inventor: Tetsuya KAMIMURA
  • Publication number: 20200131119
    Abstract: The invention relates to compounds of Formula (I) and methods for their preparation. Also described are pharmaceutical compositions comprising a compound of Formula (I) and their use in the treatment or prevention of conditions associated with mitochondrial dysfunction.
    Type: Application
    Filed: April 20, 2018
    Publication date: April 30, 2020
    Applicant: UNIVERSITY OF TASMANIA
    Inventors: Nuri GÜVEN, Jason SMITH, Krystel Lee WOOLLEY, Monila NADIKUDI
  • Publication number: 20200131120
    Abstract: The invention relates to a method for preparing an isocyanate by phosgenating the corresponding primary amine in the gas phase, wherein the gaseous reaction product mixture is cooled by being brought into contact with at least one flow stream of a quenching liquid in a quenching zone, wherein the quenching liquid used in total comprises, based on the total mass, organic solvents in a proportion of maximally 50.0% by mass, and the remainder of up to 100% by mass consists of at least the isocyanate to be produced, thereby obtaining a mixture of the reaction product mixture and the quenching liquid. Furthermore, the mixture obtained in this manner of the reaction product mixture and the quenching liquid is separated into a liquid and a gaseous phase in a collection zone, and a liquid solvent intermediate flow comprising more than 50.
    Type: Application
    Filed: June 6, 2018
    Publication date: April 30, 2020
    Inventors: Wolfgang TAUBE, Rainer BRUNS, Artur MAUSBACH
  • Publication number: 20200131121
    Abstract: The application relates to phenyl- or naphthylsulfonamide derivatives of the structural formula (I). The compounds are described as inhibitors of USP30 (ubiquitin specific peptidase 30) useful for the treatment of conditions involving mitochondrial defects including neurodegenerative diseases such as Alzheimer's and Parkinson's or a neoplastic disease such as leukemia.
    Type: Application
    Filed: May 14, 2018
    Publication date: April 30, 2020
    Inventors: Arthur Kluge, Bharat Lagu, Pranab Maiti, Sunil Kumar Panigrahi
  • Publication number: 20200131122
    Abstract: A method for recovering dimethyl sulfoxide, including a step of contacting a recovered resist remover containing at least one compound selected from the group consisting of glycol ether, glycol and triol, and dimethyl sulfoxide with water and performing distillation.
    Type: Application
    Filed: July 31, 2018
    Publication date: April 30, 2020
    Applicant: KURARAY CO., LTD.
    Inventors: Kunio MAYAHARA, Koji TAMURA, Akinobu TAKEDA
  • Publication number: 20200131123
    Abstract: A solid dispersion, a method for preparing same, and a solid preparation comprising the solid dispersion. The solid dispersion contains (R)-4-amino-1-(1-(but-2-ynylacyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazine-7-one or a pharmaceutically acceptable salt thereof, and a carrier material. The carrier material is selected from hydroxypropyl methylcellulose acetate succinate and hydroxypropyl methylcellulose phthalate.
    Type: Application
    Filed: July 5, 2018
    Publication date: April 30, 2020
    Inventors: Dong LIU, Biao LU, Wenjian QIAN, Huaide DONG, Suxing LIU, Rumin ZHANG, Feng HE, Weikang TAO
  • Publication number: 20200131124
    Abstract: Provided is a compound of Chemical Formula 1: and an organic light emitting device including the same.
    Type: Application
    Filed: July 27, 2018
    Publication date: April 30, 2020
    Inventors: Sang Duk SUH, Sung Kil HONG, Seong So KIM
  • Publication number: 20200131125
    Abstract: An aryl-piperidine derivative of formula I, wherein the meaning of R3, X, Cz, and Cy is that specified in the description, for use as inhibitors of T cells.
    Type: Application
    Filed: March 14, 2018
    Publication date: April 30, 2020
    Inventors: Andrés Gagete MATEOS, Damiá Tormo CARULLA, Luc Marti CLAUZEL, Julio Castro PALOMINO
  • Publication number: 20200131126
    Abstract: The subject-matter of the invention is process for the separation of optical isomers of racemic 3-alk-3-carboxylic acid ethyl esters of formula rac-I with the resolving agent (II) (?)-2,3:4,5-di-O-izopropylidene-2-keto-L-gulonic acid (hereinafter: diacetone-L-ketogulonic acid).
    Type: Application
    Filed: March 12, 2018
    Publication date: April 30, 2020
    Inventors: Ferenc FAIGL, Béla MÁTRA VÖLGYI, Ágnes MIZSÁK
  • Publication number: 20200131127
    Abstract: A new intermediate for synthesizing 1-substituted-4-[phenyl(propanoyl)amino]piperidine-4-carbonitrile derivatives is laid open. Specifically set out is a method for use of this intermediate in the preparation of remifentanil. The enclosed shorter process offers a greater yield of products with higher purity as compared to methods reported in the prior art.
    Type: Application
    Filed: October 25, 2019
    Publication date: April 30, 2020
    Applicant: Hameln Pharma Plus GmbH
    Inventors: Pavol Valachovic, Janka Králová, Lubos Slízik, Norbert Varga
  • Publication number: 20200131128
    Abstract: The present invention relates to a method for preparing 2,6-dichloropyridine with product purity greater than or equal to 99.0% by using trifluoromethyl chlorobenzene as a solvent for reaction between pyridine and chlorine gas. The preparation process comprises the following steps: enabling pyridine and chlorine gas to continuously experience chlorination reaction under irradiation of ultraviolet light by using pyridine and chlorine gas as starting materials and using trifluoromethyl chlorobenzene as a solvent, and cooling a chlorination reaction product and the solvent to obtain pyridine chlorination solution. Advantages: firstly, it pioneers the precedent of direct and high-selectivity preparation of 2,6-dichloropyridine through liquid phase photochlorination, and not only can the 2,6-dichloropyridine product with purity greater than or equal to 99.
    Type: Application
    Filed: December 17, 2018
    Publication date: April 30, 2020
    Inventors: HUIYUE LI, KEQIANG JIN, JIAQUAN ZHU
  • Publication number: 20200131129
    Abstract: Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
    Type: Application
    Filed: March 14, 2018
    Publication date: April 30, 2020
    Inventors: Nicholas D. SMITH, Steven P. GOVEK, Johnny Y. NAGASAWA, Andiliy G. LAI
  • Publication number: 20200131130
    Abstract: Disclosed are d-amphetamine compounds and compositions comprising at least one organic acid covalently bound to d-amphetamine, a salt thereof, a derivative thereof, or a combination thereof. Methods of making and using the same are also disclosed.
    Type: Application
    Filed: October 29, 2019
    Publication date: April 30, 2020
    Inventors: Sven Guenther, Guochen Chi, Travis Mickle
  • Publication number: 20200131131
    Abstract: The present invention relates to novel 5-hydroxy pyridine-based compounds useful as P2X1 and P2X3 receptor antagonists and compositions comprising the same. The compounds according to the present invention have an activity of strongly antagonizing P2X1 and P2X3 receptors, and thus can be effectively used as a drug for treating or preventing chronic inflammatory diseases or neuropathic pain diseases caused by P2X1 and P2X3 receptor activity.
    Type: Application
    Filed: March 13, 2018
    Publication date: April 30, 2020
    Inventors: Yong Chul KIM, Young Hwan JUNG
  • Publication number: 20200131132
    Abstract: Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
    Type: Application
    Filed: March 14, 2018
    Publication date: April 30, 2020
    Inventors: Nicholas D. SMITH, Steven P. GOVEK, Johnny Y. NAGASAWA
  • Publication number: 20200131133
    Abstract: The present specification relates to a heterocyclic compound represented by Chemical Formula 1, and an organic light emitting device comprising the same.
    Type: Application
    Filed: December 26, 2018
    Publication date: April 30, 2020
    Applicant: HEESUNG MATERIAL LTD.
    Inventors: Hyun-Ju LA, Seong-Jong PARK, Won-Jang JEONG, Jin-Seok CHOI, Dae-Hyuk CHOI, Joo-Dong LEE
  • Publication number: 20200131134
    Abstract: Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
    Type: Application
    Filed: March 14, 2018
    Publication date: April 30, 2020
    Inventors: Nicholas D. SMITH, Steven P. GOVEK, Johnny Y. NAGASAWA
  • Publication number: 20200131135
    Abstract: Disclosed herein, inter alia, are compositions and methods for modulating Ras and treating cancer.
    Type: Application
    Filed: December 15, 2017
    Publication date: April 30, 2020
    Inventors: Kevan M. Shokat, Daniel Gentile, Steven Moss
  • Publication number: 20200131136
    Abstract: The present disclosure pertains to a process for preparing hydroxyethylethyleneamines, ethyleneamines, or mixtures thereof, and/or ethylene urea derivatives thereof. The process includes reacting diethanolamine with an amine-functional compound that includes at least two —NH— units of which at least one is selected from the group of primary amine groups and cyclic secondary amine groups. The amine-functional compound includes at least one —NH—CH2-CH2-NH— unit wherein one or more —NH—CH2-CH2-NH— units in the amine-functional compound may be present in the form of cyclic ethylene urea moieties, piperazine moieties, or linear ethylene urea moieties, in the presence of a carbon oxide delivering agent.
    Type: Application
    Filed: March 12, 2018
    Publication date: April 30, 2020
    Applicant: NOURYON CHEMICALS INTERNATIONAL B.V.
    Inventors: Antoon Jacob Berend TEN KATE, Michiel Jozef Thomas RAAIJMAKERS, Rens VENEMAN, Karl Fredrik LAKE, Robert Kristoffer BERG, Eike Nicolas KANTZER, Rolf Krister EDVINSSON, Hendrik VAN DAM, Ina EHLERS
  • Publication number: 20200131137
    Abstract: The invention relates to a commercially viable, cost effective and energy efficient process for the preparation of 2-(1H-Imidazol-4-yl)ethanamine or pharmaceutically acceptable salts thereof in high purity and yield via application of continuous flow technology.
    Type: Application
    Filed: January 2, 2020
    Publication date: April 30, 2020
    Applicant: Jubilant Generics Limited
    Inventors: Sanjeev Kumar, Rajesh Kumar, Brijesh Kumar Shukla, Rajendra Singh Shekhawat, Sujay Biswas, Dharam Vir, Nirmal Kumar, Indranil Nandi
  • Publication number: 20200131138
    Abstract: Provided is a fluorene derivative of Chemical Formula 1: and an organic light emitting device comprising the same.
    Type: Application
    Filed: July 23, 2018
    Publication date: April 30, 2020
    Inventors: Miyeon HAN, Dong Hoon LEE, Jungoh HUH, Boonjae JANG, Dong Uk HEO, Junghoon YANG, Heekyung YUN
  • Publication number: 20200131139
    Abstract: The invention relates to compounds of general formula (I): wherein R1, n, R2a, R2b, and R3 are as defined herein. The compounds are inhibitors of Bcl-2-associated death promoter (BAD) phosphorylation and have anti-apoptotic activity and are useful in the treatment of cancer, particularly breast cancer, endometrial cancer, ovarian cancer, liver cancer, colon cancer, prostate cancer or pancreatic cancer.
    Type: Application
    Filed: April 18, 2018
    Publication date: April 30, 2020
    Inventors: Peter Edward Lobie, Vijay Kumar Pandey, Ranpappa Kanchugarakoppal Subbegowda, Bassappa Salundi, Mohan Chakrabhavi Dhananjaya, Shobith Rangappa, Srinivasa Venkatachalaiah
  • Publication number: 20200131140
    Abstract: The present disclosure provides improved methods for controlled cyclization of peptoid dimers to form N,N?-2,5-diketopiperazines (N,N?-2,5-DKPs) with significant selectivity. In at least some examples, selectivity is based on a serendipitous conglomeration of slow exchange of amide rotamers, steric repulsion from the degree of ?-substitution, and the geometric bulk of an amine nucleophile. By varying reaction conditions, the selectivity of the reaction and formation of a particular N,N?-2,5-DKP can be switched. The cyclization works in the presence of a variety of protection groups and diverse functionalities. The teachings herein provide techniques for synthesizing N,N?-2,5-DKPs that can be readily docked with drug candidates for shuttling across the blood brain barrier. This method provides a facile way to produce substituted DKPs containing groups ready for post-modification to include docking drug candidates.
    Type: Application
    Filed: October 30, 2019
    Publication date: April 30, 2020
    Applicant: Triad National Security, LLC
    Inventors: Robert F. Williams, Paul William Peterson, Robert David Gilbertson, Jurgen G. Schmidt, Charlie E. Strauss
  • Publication number: 20200131141
    Abstract: The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein inhibit the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inter alia autoinflammatory and autoimmune diseases and cancers.
    Type: Application
    Filed: March 12, 2018
    Publication date: April 30, 2020
    Inventors: David HARRISON, Alan Paul WATT, Nicolas BOUTARD, Charles-Henry FABRITIUS, Michal GALEZOWSKI, Piotr KOWALCZYK, Oleksandr LEVENETS, Jakub WOYCIECHOWSKI
  • Publication number: 20200131142
    Abstract: Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
    Type: Application
    Filed: March 14, 2018
    Publication date: April 30, 2020
    Inventors: Nicholas D. SMITH, Steven P. GOVEK, Johnny Y. NAGASAWA, Karensa L. Douglas
  • Publication number: 20200131143
    Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.
    Type: Application
    Filed: November 4, 2019
    Publication date: April 30, 2020
    Inventors: Morten JORGENSEN, Peter Hongaard ANDERSEN, Klaus Gjervig JENSEN
  • Publication number: 20200131144
    Abstract: The present invention relates to derivatives of formula (I) which bind to the liver X receptor (LXR? and/or LXR?) and act preferably as inverse agonists of LXR.
    Type: Application
    Filed: July 18, 2018
    Publication date: April 30, 2020
    Applicant: Phenex-FXR GmbH
    Inventors: Christian Gege, Manfred Birkel, Eva Hambruch, Ulrich Deuschle, Claus Kremoser
  • Publication number: 20200131145
    Abstract: The present invention relates to a novel synthetic pathway for alpha-tocopherol. The invention discloses different reactions yielding some new intermediates in a very high yield and stereoselectivity.
    Type: Application
    Filed: July 11, 2018
    Publication date: April 30, 2020
    Inventors: Ulla LETINOIS, Thomas NETSCHER, August RUETTIMANN
  • Publication number: 20200131146
    Abstract: An apparatus and method for removing a compound from a solution are disclosed. The apparatus includes a vessel, a solution heater, and an aeration device, wherein the solution heater and the aeration device are connected to the vessel. The solution is contained in the vessel and heated by the solution heater. The aeration device provides aeration to the heated solution for agitating the heated solution, and the component is thereby removed from the solution.
    Type: Application
    Filed: October 23, 2019
    Publication date: April 30, 2020
    Inventor: GEORGE STANTCHEV
  • Publication number: 20200131147
    Abstract: The present invention discloses a PEGylated thioxanthone photoinitiator and a photosensitive resin composition, the PEGylated thioxanthone compound is eco-friendly and has low toxicity, high initiation efficiency and good thermal stability, meanwhile, as a kind of photoinitiator, the compound has a small amount of fragment residue after cured, and may improve the compatibility of the photoinitiator and photosensitive resin composition system. The photosensitive resin composition provided by the present invention has reasonable allocation of ingredients and content in the components thereof, capable of 3D-printing a hydrogel having a specific structure; the hydrogel has lower cytotoxicity and better biocompatibility, and may applied in bioengineering fields, e.g., 3D cell culture.
    Type: Application
    Filed: December 30, 2019
    Publication date: April 30, 2020
    Inventors: HUI ZHU, MEINA LIN, XUAN ZHAO
  • Publication number: 20200131148
    Abstract: Disclosed herein are compounds of the formulas: as well as analogs thereof, wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used to inhibit ROR? and/or reduce the expression of IL-17. Also provided are methods of administering compounds and composition provided herein to a patient in need thereof, for example, for the treatment or prevention of diseases or disorders associated with inflammation or autoimmune disorders.
    Type: Application
    Filed: December 16, 2017
    Publication date: April 30, 2020
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventors: Xin JIANG, Christopher F. BENDER, Melean VISNICK, Martha R. HOTEMA, Zachary S. SHELDON, Chitase LEE, Bradley William CAPRATHE, Gary BOLTON, Brian KORNBERG
  • Publication number: 20200131149
    Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate are also disclosed.
    Type: Application
    Filed: October 31, 2019
    Publication date: April 30, 2020
    Inventor: Jerry Lee Atwood
  • Publication number: 20200131150
    Abstract: A condensed cyclic compound represented by Formula 1 or Formula 2: wherein ring A1, ring A2, T1, L1, a1, R1 to R9, b1 to b3, and c1 in Formulae 1 and 2 are the same as described in the specification.
    Type: Application
    Filed: October 22, 2019
    Publication date: April 30, 2020
    Inventors: Yongsik JUNG, Eunsuk KWON, Sangmo KIM, Jhunmo SON, Dongseon LEE, Soonok JEON, Yeonsook CHUNG, Jongsoo KIM
  • Publication number: 20200131151
    Abstract: The present invention relates to novel pyridazines, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment and/or prevention of diseases and disorders mediated by Autotaxin.
    Type: Application
    Filed: October 25, 2019
    Publication date: April 30, 2020
    Inventors: Gerald Juergen ROTH, Tom BRETSCHNEIDER, Christian Andreas KUTTRUFF
  • Publication number: 20200131152
    Abstract: A pharmaceutical formulation of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide (compound 1), in particular methanesulfonic acid salt thereof, and methods of using the pharmaceutical formulation for the treatment or prevention of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGFR), such as various cancers, are disclosed.
    Type: Application
    Filed: June 15, 2018
    Publication date: April 30, 2020
    Applicant: Beta Pharma, Inc.
    Inventors: Michael Nicholas Greco, Michael John Costanzo, Michael Alan Green, Jirong Peng, Victoria Lynn Wilde, Don Zhang
  • Publication number: 20200131153
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 25, 2019
    Publication date: April 30, 2020
    Applicant: ASTEX THERAPEUTICS LTD
    Inventors: Gordon SAXTY, Christopher William MURRAY, Valerio BERDINI, Gilbert Ebai BESONG, Christopher Charles Frederick HAMLETT, Christopher Norbert JOHNSON, Steven John WOODHEAD, Michael READER, David Charles REES, Laurence Anne MEVELLEC, Patrick René ANGIBAUD, Eddy Jean Edgard FREYNE, Tom Cornelis Hortense GOVAERTS, Johan Erwin Edmond WEERTS, Timothy Pietro Suren PERERA, Ronaldus Arnodus Hendrika Joseph GILISSEN, Berthold WROBLOWSKI, Jean Fernand Armand LACRAMPE, Alexandra PAPANIKOS, Olivier Alexis Georges QUEROLLE, Elisabeth Thérèse Jeanne PASQUIER, Isabelle Noëlle Constance PILATTE, Pascal Ghislain André BONNET, Werner Constant Johan EMBRECHTS, Rhalid AKKARI, Lieven MEERPOEL
  • Publication number: 20200131154
    Abstract: Compounds having activity as chemotherapeutic agents are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R1a, R1b, R1c, R1d, L, and are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods for treating cancer (e.g., hematological cancers) are also provided.
    Type: Application
    Filed: October 25, 2019
    Publication date: April 30, 2020
    Inventor: Hariprasad Vankayalapati
  • Publication number: 20200131155
    Abstract: The present disclosure reports solid forms of (4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone.
    Type: Application
    Filed: October 29, 2019
    Publication date: April 30, 2020
    Inventors: George P. LUKE, Stephen HUBBS
  • Publication number: 20200131156
    Abstract: The present invention provides novel compounds which activate the Kv3 potassium channels. The compounds have the structure Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and use of the compounds to treat disorders responsive to the activation of Kv3 potassium channels.
    Type: Application
    Filed: October 29, 2019
    Publication date: April 30, 2020
    Inventors: Anette Graven SAMS, Lars Kyhn RASMUSSEN, Wanwan YU, Paul Robert FLEMING
  • Publication number: 20200131157
    Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof. It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses, in particular to modulate CFTR protein or ABC protein activities.
    Type: Application
    Filed: March 14, 2018
    Publication date: April 30, 2020
    Inventors: Tiziano Bandiera, Fabio Bertozzi, Paolo Di Fruscia, Federico Sorana, Emanuela Caci, Loretta Ferrera, Nicoletta Pedemonte, Luis Juan Vicente Galietta
  • Publication number: 20200131158
    Abstract: Disclosed are Type II Topoisomerase Inhibitors, analogs thereof, pharmaceutical compositions thereof and methods of making and using these compounds and compositions. Methods of using the disclosed compounds to treat infections, such as MRSA, MDR P. aeruginosa, and other pathogens are also described.
    Type: Application
    Filed: April 17, 2018
    Publication date: April 30, 2020
    Inventor: Mark MITTON-FRY
  • Publication number: 20200131159
    Abstract: Described are positive allosteric modulators of muscarinic acetylcholine receptor M1 (mAChR M1), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating neurological disorders, psychiatric disorders, or a combination thereof.
    Type: Application
    Filed: October 24, 2019
    Publication date: April 30, 2020
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Darren W. Engers, Aaron M. Bender
  • Publication number: 20200131160
    Abstract: The present disclosure provides compounds of the formula: wherein the variables are defined herein. The present disclosure also provides methods of imaging Zn2+ within granules in cells, such as pancreatic ?-, ?-, and ?-cells. The present disclosure also provides methods of sorting cells comprising the use of the compounds of the present disclosure.
    Type: Application
    Filed: October 28, 2019
    Publication date: April 30, 2020
    Inventors: Wen-Hong LI, Ebrahim GHAZVINI ZADEH
  • Publication number: 20200131161
    Abstract: It is known that foods containing a carbohydrate, e.g., starch, in a large amount produce acrylamide upon heating at high temperatures. Some documents state that acrylamide is formed by the Maillard reaction of an amino acid, e.g., asparagine, with a reducing sugar. The purpose of the present invention is to provide a novel compound which is effective in inhibiting such foods from yielding acrylamide when treated at a high temperature. Specifically, the present invention provides a compound represented by General Formula (I).
    Type: Application
    Filed: March 16, 2018
    Publication date: April 30, 2020
    Applicants: THE KITASATO INSTITUTE, BF AGRO CO., LTD.
    Inventors: Satoshi OMURA, Yoko TAKAHASHI, Takuji NAKASHIMA, Hirotaka MATSUO, Kenichi NONAKA, Hisako SAKATO
  • Publication number: 20200131162
    Abstract: The invention provides 20-nor-salvinorin A, an analog of the kappa-opioid agonist salvinorin A. The 20-nor-salvinorin A is an active kappa-opioid modulator and can be used for treatment of medical conditions wherein modulation of the kappa-opioid receptor is medically indicated, such as pain, pruritis, depression, or inflammation, or conditions implicating perception and consciousness. 20-nor-salvinorin A can be less additive when used in treatment compared to a mu-opioid receptor agonist, and 20-nor-salvinorin A is more stable in vivo than is parent compound salvinorin A. The invention further provides synthetic intermediates and procedures for preparation of 20-nor-salvinorin A.
    Type: Application
    Filed: June 7, 2018
    Publication date: April 30, 2020
    Inventors: Ryan Shenvi, Jeremy Roach, Yusuke Sasano, Laura Bohn, Cullen Schmid
  • Publication number: 20200131163
    Abstract: The present invention relates to process for the preparation of Empagliflozin or its co-crystals, solvates and/or polymorphs thereof. The present invention also relates to novel intermediates used therein, and process for the preparation thereof. The present invention further relates to process for preparation of amorphous and crystalline form of Empagliflozin.
    Type: Application
    Filed: June 5, 2018
    Publication date: April 30, 2020
    Inventors: Uma Maheswar Rao VASIREDDI, Sanjay Kumar DEHURY, Nagaraju MEKALA, Jahangeer Baba SHAIK, Srinivas LAGADAPATI
  • Publication number: 20200131164
    Abstract: Crystalline 2-hydroxy-N,N-dimethylethanaminium 1-(2-(5-(tert-butyl)-thiophene-2-carboxamido)-3-(4-(5-(4?-ethyl-[1,1?-bi(cyclohexan)]-3-en-4-yl)pyrimidin-2-yl)phenyl)propanoyl)azetidine-3-carboxylate salt, and methods related to synthesis and therapeutic use of the same.
    Type: Application
    Filed: September 29, 2017
    Publication date: April 30, 2020
    Inventors: Ephraim Vidal, Roger Bakale, Philip Turnbull, David Moser, Andrew Robbins, Craig Grant
  • Publication number: 20200131165
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicycloheteroaryl-heteroaryl-benzoic acid compounds of the following formula (for convenience, collectively referred to herein as “BHBA compounds”), which, inter alia, are (selective) retinoic acid receptor beta (RAR?) (e.g., RAR?2) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RAR? (e.g., RAR?2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RAR? (e.g., RAR?2), that are ameliorated by the activation of RAR? (e.g., RAR?2), etc., including, e.g., neurological injuries such as spinal cord injuries.
    Type: Application
    Filed: August 9, 2019
    Publication date: April 30, 2020
    Inventors: Alan David Borthwick, Mark Trevor Mills, Jane Theresa Brown, Jonathan Patrick Thomas Corcoran, Maria Beatriz De Castro Vasconcelos Goncalves, Sarkis Barret Kalindjian
  • Publication number: 20200131166
    Abstract: The present invention relates to novel fatty acid esters of the reversible Iloperidone metabolite P-88-8991, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.
    Type: Application
    Filed: December 26, 2019
    Publication date: April 30, 2020
    Inventors: Joachim Nozulak, Hans Kalkman