Patents Issued in September 17, 2020
  • MALEATE SALTS OF (E)-N-(3-CYANO-7-ETHOXY-4-((4-PHENOXYPHENYL)AMINO) QUINOLIN-6-YL)-4-(DIMETHYLAMINO)BUT-2-ENAMIDE AND CRYSTALLINE FORMS THEREOF
    Publication number: 20200290968
    Abstract: The present application relates to maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)aniline]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, crystalline forms thereof, to processes for its preparation, to pharmaceutical compositions comprising it and to its use in the control of disorders.
    Type: Application
    Filed: November 20, 2018
    Publication date: September 17, 2020
    Inventor: Dawei Zhang
  • FUSED PIPERIDINYL BICYCLIC AND RELATED COMPOUNDS AS MODULATORS OF C5A RECEPTOR
    Publication number: 20200290969
    Abstract: The present invention relates to fused piperidinyl bicyclic, meta-substituted piperidinyl and their related compounds that modulate activities of mammalian C5a receptor by directly binding to the C5a receptor. The invention also relates to pharmaceutical compositions containing such compounds and their use in the treatment of a disease or a disorder involving pathogenic activation of C5a receptors.
    Type: Application
    Filed: February 7, 2020
    Publication date: September 17, 2020
    Applicant: InflaRx GmbH
    Inventors: YONG LI, RENFENG GUO, NIELS CHRISTOPH RIEDEMANN
  • INHIBITORS OF MICROBIALLY INDUCED AMYLOID
    Publication number: 20200290970
    Abstract: The present disclosure provides compounds useful for the prevention of amyloid formation and the treatment of amyloid related disorders, including synucleopathies such as Parkinson's Disease.
    Type: Application
    Filed: August 6, 2018
    Publication date: September 17, 2020
    Applicant: Axial Biotherapeutics, Inc.
    Inventors: Anthony Stewart Campbell, Bridget Cole, Alessandra Bartolozzi
  • DEUTERATED CFTR POTENTIATORS
    Publication number: 20200290971
    Abstract: This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.
    Type: Application
    Filed: October 22, 2019
    Publication date: September 17, 2020
    Applicant: Vertex Pharmaceuticals (EUROPE) Limited
    Inventor: Adam J. Morgan
  • PROCESSES FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
    Publication number: 20200290972
    Abstract: The disclosure provides processes for synthesizing compounds for use as CFTR modulators.
    Type: Application
    Filed: November 30, 2018
    Publication date: September 17, 2020
    Inventors: Berenice Lemercier Lewandowski, Robert Lewis, Adam Looker, Adam Morgan, Stefanie Roeper, Michael Ryan, Juan Gabriel Solsona Rocabert, Nathan Wilde
  • FARNESOID X RECEPTOR AGONISTS AND USES THEREOF
    Publication number: 20200290973
    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: May 28, 2020
    Publication date: September 17, 2020
    Inventors: Nicholas D. SMITH, Stephen P. GOVEK, Johnny Y. NAGASAWA
  • FARNESOID X RECEPTOR ANTAGONISTS
    Publication number: 20200290974
    Abstract: Provided herein are Farnesoid X receptor (FXR) antagonists having the structure of formula (I), and pharmaceutical compositions comprising the compound of formula (I) and a pharmaceutically acceptable excipient. Also provided are methods of antagonizing FXR, and methods of treating metabolic disease in a subject in need thereof, comprising administering an effective amount of the FXR antagonists of formula (I) to a subject.
    Type: Application
    Filed: March 30, 2020
    Publication date: September 17, 2020
    Inventors: Barry Forman, Donna Yu
  • ANTICANCER 1,3-DIOXANE-4,6-DIONE DERIVATIVES AND METHOD OF COMBINATORIAL SYNTHESIS THEREOF
    Publication number: 20200290975
    Abstract: Compounds, methods of synthesis, and methods of cancer treatment by arylidene-1,3-dioxane-4,6-diones. A Meldrum's acid-based chemistry and hybrid solid-liquid method. The method includes protection of ketone and aldehyde components and simultaneous immobilization on the solid phase, introduction of substituents, grafts and derivatives compatible with the protection, detachment and restoration of active carbonyl reactivity, reaction of ketone library with malonate, reacting of the products with the aldehyde library in liquid phase and separation of the products by preparative HPLC.
    Type: Application
    Filed: March 5, 2020
    Publication date: September 17, 2020
    Applicants: National Guard Health Affairs, King Saud bin Abdulaziz University for Health Sciences, King Abdullah International Medical Research Center
    Inventors: Imadul ISLAM, Rabih O. AL-KAYSI, Mohamed BOUDJELAL, Rizwan ALI, Atef NEHDI, Bandar ALGHANEM
  • RADIOLABELED MICROTUBULE IMAGING COMPOUNDS AND USES THEREOF
    Publication number: 20200290976
    Abstract: The present disclosure relates to radiolabeled compounds and methods of uses for diagnosis, monitoring, and treatment of various degenerative neurological disorders, neuropsychiatric disorders, brain injuries, vascular diseases, and cancers. Radiolabled compounds for imaging of microtubules or microtubules and other targets using positron-emission tomography (PET) are specifically disclosed.
    Type: Application
    Filed: October 30, 2018
    Publication date: September 17, 2020
    Inventors: Dileep KUMAR, J. John MANN
  • Inhibitors of Low Molecular Weight Protein Tyrosine Phosphatase and Uses Thereof
    Publication number: 20200290977
    Abstract: Herein are provided, inter alia, compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and methods of using the same. In embodiments, the compound has a structure according to Formula (I-A).
    Type: Application
    Filed: February 18, 2020
    Publication date: September 17, 2020
    Inventors: Nunzio BOTTINI, Jiwen ZOU, Santhi R. GANJI, Stephanie STANFORD, Anthony PINKERTON, Thomas D. Y. CHUNG, Michael HEDRICK, Robert ARDECKY
  • COMPOSITIONS AND METHODS FOR TREATING CANCER
    Publication number: 20200290978
    Abstract: The present disclosure relates to compounds that are capable penetrating to the blood brain barrier to modulate the activity of EGFR tyrosine kinase. The disclosure further relates to methods of treating glioblastoma and other EGFR mediated cancers. The disclosure further relates to methods of treating glioblastoma and other EGFR mediated cancers that have been determined to have altered glucose metabolism in the presence of inhibitors. The present disclosure also provides methods of administering to a subject a glucose metabolism inhibitor and a cytoplasmic p53 stabilizer.
    Type: Application
    Filed: September 26, 2018
    Publication date: September 17, 2020
    Applicant: The Regents of the University of California
    Inventors: David A. Nathanson, Wilson X. Mai, Michael E. Jung, Peter M. Clark, Timothy F. Cloughesy, Gyudong Kim, Jonathan Tsang, Lorenz Urner
  • CHARGED ION CHANNEL BLOCKERS AND METHODS FOR USE
    Publication number: 20200290979
    Abstract: The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, cough, itch, and neurogenic inflammation.
    Type: Application
    Filed: March 11, 2020
    Publication date: September 17, 2020
    Inventors: Bridget McCarthy Cole, James Lamond Ellis
  • POLYCATENAR LIGANDS AND HYBRID NANOPARTICLES MADE THEREFROM
    Publication number: 20200290980
    Abstract: Described herein are polycatenar ligand compounds and their use in the production of hybrid nanoparticles, typically nanocrystals. The present disclosure also relates to films containing the hybrid nanoparticles described herein and their use.
    Type: Application
    Filed: March 17, 2017
    Publication date: September 17, 2020
    Inventors: Bertrand DONNIO, Davit JISHKARIANI, Benjamin DIROLL, Christopher MURRAY, Lawrence Alan HOUGH, Matteo CARGNELLO, Stan NAJMR, Katherine C. ELBERT
  • BENZOTRIAZOLE DERIVATIVE COMPOUND
    Publication number: 20200290981
    Abstract: Provided are benzotriazole derivative compounds of the general formula that are novel compounds capable of strongly absorbing light in the ultraviolet range, particularly 300-330 nm, while strongly absorbing light in the visible light short-wavelength range up to around 450 nm and being used suitably as a light absorber having high light fastness with a light-blocking function over an extended period of time. Preferably, R1 is a hydrogen atom or alkyl group, R2 is a C1-8 alkyl group, R3 is a hydrogen atom, alkyl group, acryloyloxyalkyl group, or methacryloyloxyalkyl group.
    Type: Application
    Filed: June 3, 2020
    Publication date: September 17, 2020
    Applicant: SHIPRO KASEI KAISHA, LTD.
    Inventors: Tomoyuki ISHITANI, Toshiyuki UESAKA, Takuya IWAMOTO
  • METAL/RADIOMETAL-LABELED PSMA INHIBITORS FOR PSMA-TARGETED IMAGING AND RADIOTHERAPY
    Publication number: 20200290982
    Abstract: Low-molecular weight gadolinium (Gd)-based MR contrast agents for PSMA-specific T1-weighted MR imaging are disclosed. The (Gd)-based MR contrast agents exhibit high binding affinity for PSMA and exhibit specific T1 contrast enhancement at PSMA+ cells. The PSMA-targeted Gd-based MR contrast agents can be used for PSMA-targeted imaging in vivo. 86Y-labeled PSMA-binding ureas also are provided, wherein the PSMA-binding ureas also are suitable for use with other radiotherapeutics.
    Type: Application
    Filed: May 29, 2020
    Publication date: September 17, 2020
    Inventors: Sangeeta Ray, Martin G. Pomper, Thomas J. Meade, Ronnie C. Mease, Ying Chen, Xing Yang, Matthew Rotz
  • METHOD FOR PRODUCING CYCLIC ETHER
    Publication number: 20200290983
    Abstract: A method for producing a cyclic ether represented by formula (2) includes reacting a 2-hydroxy cyclic ether, represented by formula (1), with hydrogen in the presence of a catalyst.
    Type: Application
    Filed: December 4, 2018
    Publication date: September 17, 2020
    Applicant: KURARAYCO., LTD.
    Inventors: Ryosuke SHIMIZU, Takahiro HOSONO, Ichihiro ARATANI, Ryo KOUCHI
  • PROCESS FOR PRODUCING 5-HYDROXYMETHYLFURFURAL IN THE PRESENCE OF AN ORGANIC DEHYDRATION CATALYST AND A CHLORIDE SOURCE
    Publication number: 20200290984
    Abstract: The invention relates to a novel process for converting a feedstock comprising at least one sugar into 5-hydroxymethylfurfural, wherein said feedstock is brought into contact with one or more organic dehydration catalysts and one or more chloride sources in the presence of at least one aprotic polar solvent alone or as a mixture, at a temperature of between 30° C. and 200° C., and at a pressure of between 0.1 MPa and 10 MPa.
    Type: Application
    Filed: September 25, 2018
    Publication date: September 17, 2020
    Applicant: IFP Energies nouvelles
    Inventors: Justine DENIS, Marc JACQUIN, Damien DELCROIX
  • COMPOUND, MATERIAL FOR ORGANIC ELECTROLUMINESCENCE DEVICES, ORGANIC ELECTROLUMINESCENCE DEVICE, AND ELECTRONIC DEVICE
    Publication number: 20200290985
    Abstract: A compound represented by formula (A): wherein Ar, R1 to R7, R11 to R14, R21 to R24, R31 to R34, *1, and R41 to R48 are as defined in the description provides organic electroluminescence devices with improved device performance.
    Type: Application
    Filed: May 1, 2020
    Publication date: September 17, 2020
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Yu KUDO, Tasuku Haketa, Hirokatsu Ito
  • MONO AMINE DERIVATIVES AND ORGANIC ELECTROLUMINESCENT DEVICE INCLUDING THE SAME
    Publication number: 20200290986
    Abstract: An organic electroluminescent device includes a monoamine derivative represented by Formula 1: In Formula 1, Ar1 may be represented by Formula 2; Ar2 may be a substituted or unsubstituted aryl group having 6 to 30 carbon atoms for forming a ring, wherein the substituent of Ar2 is an unsubstituted aryl group having 6 to 30 carbon atoms for forming a ring; Ar1 and Ar2 may be different from each other; m may be an integer from 0 to 4; and R1 may be a substituted or unsubstituted aryl group having 6 to 30 carbon atoms for forming a ring, and when m is 2 or more, a plurality of R1 may combine to form a ring:
    Type: Application
    Filed: June 2, 2020
    Publication date: September 17, 2020
    Inventor: Hideo Miyake
  • SALTS OF A HETEROCYCLIC COMPOUND AND CRYSTALLINE FORMS, PROCESSES FOR PREPARING, THERAPEUTIC USES, AND PHARMACEUTICAL COMPOSITIONS THEREOF
    Publication number: 20200290987
    Abstract: The present disclosure relates to salts of (R)-1-(8-fluoroisochroman-1-yl)-N-methylmethanamine, crystalline forms thereof, and methods of preparation thereof, which are useful in the treatment of CNS disorders.
    Type: Application
    Filed: March 13, 2020
    Publication date: September 17, 2020
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Nandkumar Nivritti BHOGLE, Takahiko HASHIZUKA, Robert Joseph PRYTKO, John R. SNOONIAN, Harold Scott WILKINSON, Haitao ZHANG
  • GAS PHASE METHODS TO DECARBOXYLATE CANNABINOIDS
    Publication number: 20200290988
    Abstract: Various aspects of this disclosure relate to gas phase methods to decarboxylate cannabinoid carboxylic acids.
    Type: Application
    Filed: June 1, 2020
    Publication date: September 17, 2020
    Inventors: C. Russell Thomas, Mathew M. Depalo
  • CALIXCROWNS AND USES THEREOF
    Publication number: 20200290989
    Abstract: Provided herein are novel calixcrowns, such as those of Formula I, which are useful for coating a solid substrate such as a protein chip, diagnostic kit or protein separation pack. Also provided herein are methods detecting protein-protein interactions with a solid substrate coated with the calixcrown herein and an immobilized protein.
    Type: Application
    Filed: March 16, 2020
    Publication date: September 17, 2020
    Inventors: Incheol KANG, Nari LEE
  • METHODS FOR TREATING PROTOZOAN INFECTIONS
    Publication number: 20200290990
    Abstract: The invention provides compounds of Formula (I), and their use in methods for treating or preventing a protozoan infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a protozoan infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a protozoan infection in a subject and to a medical device comprising the composition of the invention.
    Type: Application
    Filed: June 4, 2020
    Publication date: September 17, 2020
    Inventors: Stephen Page, Andrew Stevens, Adam McCluskey, Martine Keenan, Rebecca Abraham
  • ESTER SUBSTITUTED ION CHANNEL BLOCKERS AND METHODS FOR USE
    Publication number: 20200290991
    Abstract: The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.
    Type: Application
    Filed: March 11, 2020
    Publication date: September 17, 2020
    Inventors: Bridget McCarthy Cole, James Lamond Ellis
  • Deuterium-Substituted Pyridin- And Pyrimidin-2-yl-Methylamine Compounds
    Publication number: 20200290992
    Abstract: Described are deuterium-substituted pyridin- and pyrimidin-2-yl-methylamine compounds of structural Formula (I), which are agonists of 5-hydroxytryptamine receptors. Also described are pharmaceutical compositions comprising the deuterium-substituted pyridin- and pyrimidin-2-yl-methylamine compounds, and methods of use thereof.
    Type: Application
    Filed: April 20, 2020
    Publication date: September 17, 2020
    Inventor: Chengzhi ZHANG
  • TLR INHIBITORS
    Publication number: 20200290993
    Abstract: A method for inhibiting TLR7 and/or TLR8 receptors includes contacting the receptor with compound of general formula (I): wherein the meanings of the variables are explained in the specification, or a stereoisomeric form or a mixture of stereoisomeric forms, or pharmaceutically acceptable salts thereof. A pharmaceutical composition can include compounds of the invention, which can be used in a method for inhibiting TLR7 receptors and/or TLR8 receptors. The method can be performed by administering the compound to a subject to inhibit TLR7, TLR8, or TLR7/8 activity, which can be used to treat a disease or disorder associated with the receptors.
    Type: Application
    Filed: April 28, 2020
    Publication date: September 17, 2020
    Inventors: Aleksandrs Zavoronkovs, Vladimir Aladinskiy, Aleksandr Aliper
  • TLR 9 INHIBITORS
    Publication number: 20200290994
    Abstract: A method for inhibiting TLR9 includes contacting the TLR9 with compound of general formula (I): wherein the meanings of the variables are explained in the specification, or a stereoisomeric form or a mixture of stereoisomeric forms, or pharmaceutically acceptable salts thereof. A pharmaceutical composition can include compounds of the invention, which can be used in a method for inhibiting TLR9 activity in vitro or in vivo. The method can be performed by administering the compound to a subject to inhibit TLR9 activity, which can be used to treat a disease or disorder associated with TLR9.
    Type: Application
    Filed: June 1, 2020
    Publication date: September 17, 2020
    Inventors: Aleksandrs Zavoronkovs, Vladimir Aladinskiy, Aleksandr Aliper
  • Process for the Preparation of Crystalline Ridinilazole Using Acid Addition Salts
    Publication number: 20200290995
    Abstract: The invention relates to acid addition salts of ridinilazole and processes for the preparation of ridinilazole using these acid addition salts. In addition, the present invention relates to processes for the preparation of ridinilazole in pure form using acid addition salts of ridinilazole as process intermediates.
    Type: Application
    Filed: July 27, 2018
    Publication date: September 17, 2020
    Applicant: Sandoz AG
    Inventors: Erwin Schreiner, Sven Nerdinger, Gerhard Laus
  • NOVEL SUBSTITUTED CYCLOBUTYLPYRIDINE AND CYCLOBUTYLPYRIMIDINE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS
    Publication number: 20200290996
    Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Application
    Filed: October 4, 2018
    Publication date: September 17, 2020
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Catherine M. White, Abdelghani Achab, Indu T. Bharathan, Xavier Fradera, Yongxin Han, Derun Li, Jongwon Lim, Kun Liu, Meredeth Ann McGowan, Nunzio Sciammetta, Wensheng Yu, Hongjun Zhang, Hua Zhou
  • BTK INHIBITOR COMPOUNDS
    Publication number: 20200290997
    Abstract: The invention provides BTK Inhibitor compounds, pharmaceutically acceptable salts, pharmaceutical compositions thereof, and methods of using these compounds, salts, or compositions to treat autoimmune diseases such as Rheumatoid Arthritis.
    Type: Application
    Filed: October 30, 2018
    Publication date: September 17, 2020
    Inventors: Kenneth James Henry, Jr., Albert Khilevich, Steven Lee Kuklish, Katherine Marie Partridge, Steven James Quimby
  • NOVEL IMIDAZOLE-PYRAZOLE DERIVATIVES
    Publication number: 20200290998
    Abstract: The disclosure provides novel imidazole pyrazole derivatives having the general formula (I), and pharmaceutically acceptable salts thereof, wherein X1, RA and R3 to R7 are as described herein: Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
    Type: Application
    Filed: March 6, 2020
    Publication date: September 17, 2020
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Jean-Baptiste Blanc, Christian Kramer, Christian Lerner, Matthias Nettekoven, Philippe Pflieger, Bernd Puellmann, Thomas Ryckmans, Sébastien Schmitt, Min Wang, Song Yang, Chengang Zhou
  • Stable solutions of multicyclic antidepressants
    Publication number: 20200290999
    Abstract: The invention relates to the field of medicine, specifically the field of atypical antipsychotics. New compositions are provided that provide drug solutions of high stability.
    Type: Application
    Filed: October 5, 2018
    Publication date: September 17, 2020
    Applicant: Leyden Technologies B.V.
    Inventors: Hans van der Steen, Karel Jollie, Willem van Rijn
  • DOPAMINE D3 RECEPTOR SELECTIVE ANTAGONISTS/PARTIAL AGONISTS; METHOD OF MAKING; AND USE THEREOF
    Publication number: 20200291000
    Abstract: Disclosed herein novel dopamine D3 receptor selective antagonists/partial agonists compounds with high affinity and metabolic stability useful for the treatment of psychiatric and neurological disorders and as research and diagnostic tools. Also disclosed are methods of making the compounds.
    Type: Application
    Filed: September 21, 2017
    Publication date: September 17, 2020
    Inventors: Amy Hauck NEWMAN, Vivek KUMAR, Anver Basha SHAIK
  • MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)
    Publication number: 20200291001
    Abstract: Disclosed are compounds having the formula: (I) wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, R17, Rx, and Ry are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
    Type: Application
    Filed: October 4, 2018
    Publication date: September 17, 2020
    Inventors: David T. FOSBENNER, Todd L. GRAYBILL, Jianxing KANG, Bryan W. KING, Yunfeng LAN, Lara Kathryn LEISTER, Mukesh K. MAHAJAN, John F. MEHLMANN, Angel I. MORALES-RAMOS, George Scott PESIRIDIS, Joshi M. RAMANJULU, Joseph J. ROMANO, Stuart Paul ROMERIL, Mark J. SCHULZ, Huiqiang ZHOU, Junya QU
  • BENZOFURAN DERIVATIVES FOR THE TREATMENT OF HEPATITIS C
    Publication number: 20200291002
    Abstract: The disclosure provides compounds of formula (I), including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: March 17, 2017
    Publication date: September 17, 2020
    Inventors: Kap-Sun Yeung, John F. Kadow, Rajesh Onkardas Bora, Prakash Anjanappa, Kumaravel Selvakumar, Samayamunthula Venkata Satya Arun Gupta
  • NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS
    Publication number: 20200291003
    Abstract: The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R1 may optionally be substituted; and R2 is a cyclic group substituted at the ?-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
    Type: Application
    Filed: July 4, 2018
    Publication date: September 17, 2020
    Inventors: Matthew COOPER, David MILLER, Angus MACLEOD, Jimmy VAN WILTENBURG, Stephen THOM, Stephen ST-GALLAY, Jonathan SHANNON
  • 5-FLUORO-C-(ARYL OR HETEROCYCLYL)-GLYCOSIDE DERIVATIVES USEFUL AS DUAL SGLT1 / SGLT2 MODULATORS
    Publication number: 20200291004
    Abstract: The present invention is directed to 5-fluoro-C-(aryl or heterocyclyl)-glycoside derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT activity, more particularly dual SGLT1/2 activity.
    Type: Application
    Filed: June 2, 2020
    Publication date: September 17, 2020
    Inventors: Guozhang Xu, Gee-Hong Kuo, Micheal Gaul
  • COMPOSITIONS AND METHODS FOR INHIBITING ACSS2
    Publication number: 20200291005
    Abstract: The present invention provides compositions and methods for inhibiting ACSS2 for modulating histone acetylation or for treating or preventing a neurological disease or disorder.
    Type: Application
    Filed: September 26, 2018
    Publication date: September 17, 2020
    Inventors: Philipp MEWS, Shelley L. BERGER, Jeffrey D. WINKLER, Andrew GLASS, Simon David Peter Baugh
  • ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
    Publication number: 20200291006
    Abstract: Transition metal compounds having naphthalene imide moiety having enhanced electron withdrawing property and more metal-ligand charge transfer (MLCT) based excited state are disclosed. The disclosed compounds will improve the photoluminescent quantum yield (PLQY) and produce phosphorescent emission in red to near IR region which has many desired applications.
    Type: Application
    Filed: February 25, 2020
    Publication date: September 17, 2020
    Applicant: Universal Display Corporation
    Inventors: Zhiqiang JI, Pierre-Luc T. BOUDREAULT
  • BENZIMIDAZOLE DERIVATIVES, AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF
    Publication number: 20200291007
    Abstract: Provided herein are benzimidazole derivatives, for example, of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.
    Type: Application
    Filed: May 5, 2020
    Publication date: September 17, 2020
    Inventor: Yun Long
  • MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE
    Publication number: 20200291008
    Abstract: Provided are IDO1 inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.
    Type: Application
    Filed: November 28, 2018
    Publication date: September 17, 2020
    Inventors: Wieslaw M. KAZMIERSKI, John G. CATALANO, Pek Y. CHONG
  • 2,3-DIHYDROBENZOFURANS AS BROMODOMAIN INHIBITORS
    Publication number: 20200291009
    Abstract: The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
    Type: Application
    Filed: October 4, 2018
    Publication date: September 17, 2020
    Inventors: Stephen John ATKINSON, Emmanuel Hubert DEMONT, Lee Andrew HARRISON, Simon Christopher Cranko LUCAS, Alexander G. PRESTON, Jonathan Thomas SEAL, Ian David WALL, Robert J. WATSON, James Michael WOOLVEN
  • HETEROAROMATIC MDOULATORS OF THE RETINOID-RELATED ORPHAN RECEPTOR GAMMA
    Publication number: 20200291010
    Abstract: The present invention relates to a compound according to general formula (I) wherein X represents N or CH; R1 is —CN, (C1-C6)alkyl, (C3-C7)cycloalkyl, (3-7 membered)heterocycloalkyl, (5-6 membered)heteroaryl, (C3-C7)cycloalkyl(C1-C4)alkyl, (3-7 membered)heterocycloalkyl-(C1-C4)alkyl or (5-6 membered)heteroaryl-(C1-C4)alkyl; R2 is halogen, cyano, (C1-C4)alkyl or (C3-C7)cycloalkyl; R3 is halogen, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl or (C3-C7)cycloalkyl; R4 is (C1-C4)alkyl or (C1-C4)haloalkyl; R5 is (C1-C6)alkyl, (C3-C7)cycloalkyl, (C1-C6)alkyl-(C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, (3-7 membered)heterocycloalkyl, phenyl, (5-6 membered)heteroaryl or —ORa. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds and to intermediates for preparation of said compounds.
    Type: Application
    Filed: May 15, 2020
    Publication date: September 17, 2020
    Inventors: Alan Stuart JESSIMAN, Patrick Stephen JOHNSON, Kristoffer MAANSSON, Morten Dahl SØRENSEN
  • COUMARIN DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND USES THEREOF FOR THE TREATMENT OF CANCER
    Publication number: 20200291011
    Abstract: The invention provides novel coumarin derivatives as specific mitochondrial RNA polymerase inhibitors for the treatment of cancer.
    Type: Application
    Filed: September 20, 2018
    Publication date: September 17, 2020
    Inventors: Raffaella Di Lucrezia, Tim Bergbrede, Peter Nussbaumer, Uwe Koch, Bert Klebl, Axel Choidas, Anke Unger, Nils-Göran Larsson, Maria Falkenberg-Gustafsson, Claes M. Gustafsson
  • CRYSTALLINE SULFAMIDE COMPOUND
    Publication number: 20200291012
    Abstract: The present application relates to a crystalline sulfamide compound, and in particular relates to a crystalline (S)-N-((S)-1-(2-chlorphenyl)-2-((3,3-difluorocyclobutyl)amido)-2oxoethyl)-2-(4-cyanopyridin-2-base)-N-(3-fluorophenyl)-isothiazolidine-3-formamide 1,1-dioxide, and a preparation method therefor, a crystalline composition, a pharmaceutical composition and uses thereof. An X-ray powder diffraction spectrum of a crystalline hydrate of formula II of the present application has diffraction peaks at positions of about 14.40°, 20.28°, 20.94°, 22.02°, and 24.46°, represented by 2?. The crystalline hydrate of formula II of the present application has good IDH1 inhibitory activity and performs high stability, and therefore has advantages in physical property, safety and metabolic stability, and has high medicine value.
    Type: Application
    Filed: September 21, 2018
    Publication date: September 17, 2020
    Applicants: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD., CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Xiquan ZHANG, Wenwei XU, Mingming LI, Minmin KONG, Shufeng WU, Aiming ZHANG
  • ALKOXY BIS-HETEROARYL DERIVATIVES AS MODULATORS OF PROTEIN AGGREGATION
    Publication number: 20200291013
    Abstract: The present invention relates to certain bis-heteroaryl compounds, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto-temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer including melanoma.
    Type: Application
    Filed: January 23, 2018
    Publication date: September 17, 2020
    Applicant: UCB Biopharma SPRL
    Inventors: Adrian HALL, Malcolm MACCOSS
  • RAD51 INHIBITORS
    Publication number: 20200291014
    Abstract: This application is directed to inhibitors of RAD51 represented by the following structural formula, and methods for their use, such as to treat cancer, autoimmune diseases, immune deficiencies, or neurodegenerative diseases.
    Type: Application
    Filed: March 12, 2020
    Publication date: September 17, 2020
    Inventors: Jean-Marc LAPIERRE, Casey Cameron MCCOMAS, Joseph VACCA
  • TRIAZOLOPYRIDINE INHIBITORS OF MYELOPEROXIDASE
    Publication number: 20200291015
    Abstract: The present invention provides compounds of Formula (I). wherein A and Z are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and may be useful for the treatment and/or prophylaxis of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.
    Type: Application
    Filed: March 10, 2017
    Publication date: September 17, 2020
    Inventors: Joanne M. Smallheer, Carol Hui HU, Meriah Neissel Valente, Scott A. Shaw, Benjamin P. Vokits, Oz Scott Halpern
  • TRIAZOLOPYRIDINE INHIBITORS OF MYELOPEROXIDASE AND/OR EPX
    Publication number: 20200291016
    Abstract: The present invention provides compounds of Formula (I); wherein the substituents are each as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, and may be useful for the treatment and/or prophylaxis of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.
    Type: Application
    Filed: March 16, 2017
    Publication date: September 17, 2020
    Inventors: Ellen K. Kick, Joanne M. Smalheer, Scott A. Shaw, Benjiman P. Vokits, Andrew K. Dilger, Charles G. Clark, Meriah Neissel Valente, Sutjano Jusuf, Nicholas R. Wurtz
  • CITRATE SALT OF THE COMPOUND (S)-4-((S)-3-FLUORO-3-(2-(5,6,7,8-TETRAHYDRO-1,8-NAPHTHYDRIN-2-YL)ETHYL)PYRROLIDIN-1-YL)-3-(3-(2-METHOXYETHOXY)PHENYL) BUTANOIC ACID
    Publication number: 20200291017
    Abstract: The invention relates to a compound which is (S)-4-((S)-3-Fluoro-3-(2-(5,6,7,8-tetrahydro-1, 8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)-3-(3-(2-methoxyethoxy)phenyl) butanoic acid (1:1) citrate salt, pharmaceutical compositions including such compound, and to the use of such compound in therapy, including in the treatment of a disease or condition for which an ?vJ36 integrin antagonist is indicated, and in particular idiopathic pulmonary fibrosis.
    Type: Application
    Filed: March 16, 2017
    Publication date: September 17, 2020
    Inventors: Tim BARRETT, Richard Jonathan Daniel HATLEY, Simon John Fawcett MACDONALD, Paula SAKLATVALA, Sing Yuen Eric TSE