Patents Examined by Andrew D. Kosar
  • Patent number: 10947239
    Abstract: The present invention relates to a novel [1,2,4]triazolo[1,5-a]pyrimidin-yl derivative as inhibitor of phosphodiesterase 2 (PDE2). The invention is also directed to pharmaceutical compositions comprising the compound, to processes for preparing such compound and compositions, and to the use of such compound and compositions for the prevention and treatment of disorders in which PDE2 is involved, such as neurological and psychiatric disorders.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: March 16, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Petrus Jacobus Johannes Antonius Buijnsters, Henricus Jacobus Maria Gijsen, Wilhelmus Helena Ignatius Maria Drinkenburg, Abdallah Ahnaou
  • Patent number: 10799462
    Abstract: Provided are co-assembled nanoparticles including at least one polypeptide including a polyanion; and at least one amphiphilic peptide capable of forming a ?-sheet structure, a derivative or a salt thereof, the amphiphilic peptide including at least 2 pairs of alternating hydrophobic/hydrophilic amino acid residues in which the hydrophilic amino acid residue is positively charged, and methods of preparation of the nanoparticles. Further provided are pharmaceutical compositions including the co-assembled nanoparticles and a pharmaceutically active ingredient, dissolved, entrapped, encapsulated or attached to the co-assembled nanoparticles. Further provided are therapeutic uses of the pharmaceutical compositions.
    Type: Grant
    Filed: May 13, 2015
    Date of Patent: October 13, 2020
    Assignee: B. G. Negev Technologies and Applications Ltd., at Ben-Gurion University
    Inventors: Hanna Rapaport, Ifat Cohen
  • Patent number: 10632134
    Abstract: Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;
    Type: Grant
    Filed: February 8, 2017
    Date of Patent: April 28, 2020
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Jayant Thatte, Anthony C. Blackburn, Sangdon Han, Robert M. Jones, Jae-Kyu Jung, Antonio Garrido Montalban, Biman B. Pal, Jaimie Karyn Rueter, Sonja Strah-Pleynet, Lars Thoresen, Yifeng Xiong, Dawei Yue, Xiuwen Zhu
  • Patent number: 10589256
    Abstract: The present invention relates to a Ru—Pd bimetallic catalyst for use in hydrogenation of a compound, and more particularly to a catalyst prepared by loading both ruthenium and palladium on a g-C3N4 support and to a selective hydrogenation process of a pyridine group in a reaction system containing both a pyridine group and a benzene group using the catalyst.
    Type: Grant
    Filed: August 22, 2018
    Date of Patent: March 17, 2020
    Assignee: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Ji Hoon Park, Kwan Yong Jeong, Soo Min Kim, Tae Sun Chang, Iljeong Heo
  • Patent number: 10590099
    Abstract: The present invention is directed to processes from producing beta-lactone and beta-lactone derivatives using heterogenous catalysts. In preferred embodiments of the present invention, the processes comprise the steps: passing a feed stream comprising an epoxide reagent and a carbon monoxide reagent to a reaction zone; contacting the epoxide reagent and the carbon monoxide reagent with a heterogenous catalyst to produce a beta-lactone product in the reaction zone; and removing the beta-lactone product from the reaction zone. In preferred embodiments, the heterogenous catalyst comprises a solid support containing a cationic Lewis acid functional group and a metal carbonyl compound comprising at least one of anionic metal carbonyl compound or a neutral metal carbonyl compound. In certain preferred embodiments, the epoxide reagent and carbon monoxide reagent have a biobased content.
    Type: Grant
    Filed: August 10, 2017
    Date of Patent: March 17, 2020
    Assignee: Novomer, Inc.
    Inventor: Sadesh H. Sookraj
  • Patent number: 10583114
    Abstract: The present invention relates to a composition comprising urolithin A, urolithin B, urolithin C, urolithin D, or a combination thereof, for the stimulation of insulin secretion, and to the use of a compound chosen among urolithin A, urolithin B, urolithin C, urolithin D, or a combination thereof, intended for the stimulation of insulin secretion. The present invention also relates to a composition comprising an effective amount of urolithin B, urolithin C, urolithin D, or a combination thereof, for the treatment or the prevention of diabetes mellitus, and in particular for the treatment or the prevention of type 2 diabetes, and to the use of a compound chosen among urolithin B, urolithin C, urolithin D, and a combination thereof, intended for the treatment or the prevention of diabetes mellitus, and in particular of type 2 diabetes.
    Type: Grant
    Filed: October 15, 2014
    Date of Patent: March 10, 2020
    Assignees: Centre National de la Recherche Scientifique (CNRS), Universite de Montpellier, University of Parma, Ecole Nationale Superieure de Chimie, Centre National de la Recherche Scientifique, Universite de Montpellier
    Inventors: Gerard Cros, Alan Crozier, Margherita Dall'asta, Daniele Del Rio, Richard Magous, Catherine Oiry
  • Patent number: 10570111
    Abstract: A method of purifying a cyclic ester, the method including: granulating a crude cyclic ester, an average particle size of resulting granules being 0.05-1.00 mm; adding the granules to 0-4° C. water to yield a mixture, a mass ratio of the water to the granules being (0.5-2):1; stirring the mixture, and performing solid-liquid separation on the mixture; repeating the stirring and solid-liquid separation for 1-4 times, to yield a purified cyclic ester; drying the purified cyclic ester at 0-4° C. and at an absolute pressure of less than or equal to 10 pascal for 4-6 hours, and continually drying the purified cyclic ester at 40-60° C. and at an absolute pressure of less than or equal to 5 pascal for 1-2 hours.
    Type: Grant
    Filed: January 17, 2019
    Date of Patent: February 25, 2020
    Assignee: NANJING UNIVERSITY
    Inventors: Hong Li, Quanxing Zhang, Jiaye Sheng, Na Cheng, Wei Huang, Wei Jiang, Aimin Li
  • Patent number: 10561661
    Abstract: A method for treatment of disease by reduction in macrophages-mediated bacterial killing, including administration to patients in need a compound of formula (I): wherein A is N or CH; B is NO, or S; R1 is H, (C1-C4)alkyl group, methyl(C1-C6)cycloalkyl group or (C1-C6)cycloalkyl group; R2 is an aryl, arylmethyl group or methylheteroaryl group as methylpyridine and methylthiophene; R3 is absent when B is O or S, or is H or (C1-C4)alkyl group when B is N; R4 is (C1-C5)alkyl group or (C1-C4)cycloalkyl group, groups bearing a carboxylic acid group, and (C1-C5)alkyl group or (C1-C4)cycloalkyl substituted by hydroxyl group, halogen group or methoxy group, when B is N, R3 and R4 can together form a 5- or 6-membered heterocycle substituted by carboxylic acid group, substituted by a halogen atom, hydroxyl group, methoxy group or hydroxymethyl group, or pharmaceutically acceptable salt. Also provided are new compounds relating to this use.
    Type: Grant
    Filed: February 17, 2015
    Date of Patent: February 18, 2020
    Assignees: MANROS THERAPEUTICS, UNIVERSITY OF CHICAGO
    Inventors: Laurent Meijer, Nassima Oumata, Hervé Galons, Aida Gabdoulkhakova, Vladimir Riazanski, Deborah Nelson
  • Patent number: 10562882
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, in which R1, R2, R3, R4 and R5 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: November 26, 2014
    Date of Patent: February 18, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Anne Goldby, Kerry Jenkins, Martin Teall
  • Patent number: 10561633
    Abstract: The invention relates to compounds of formula (I) or the salts thereof, said compounds of formula (I) being selected from among the group consisting of homoeriodictyol (1), eriodictyol (2), hesperetin (3) and sterubin (4), for use in the treatment of an ailment which can be alleviated or prevented by influencing the serotonin level and the concentration of free fatty acids in the blood.
    Type: Grant
    Filed: July 26, 2015
    Date of Patent: February 18, 2020
    Assignee: SYMRISE AG
    Inventors: Veronika Somoza, Barbara Rohm, Kathrin Liszt, Marc Pignitter, Christina Hochkogler, Jakob Ley, Sabine Widder, Gerhard Krammer
  • Patent number: 10556910
    Abstract: The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: February 11, 2020
    Assignee: President and Fellows of Harvard College
    Inventors: Yoshito Kishi, Atsushi Ueda, Akihiko Yamamoto, Daisuke Kato
  • Patent number: 10556890
    Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: February 11, 2020
    Assignees: Sunovion Pharmaceuticals Inc., PGI DRUG DISCOVERY LLC
    Inventors: John Emmerson Campbell, Una Campbell, Taleen G. Hanania, Liming Shao
  • Patent number: 10556876
    Abstract: The invention relates to process for the preparation of gamma valerolactone (GVL) from levulinic acid (LA), said process comprising a) subjecting LA to a hydrogenation reaction comprising hydrogen and a solid catalyst system comprising a metal and a support in the liquid phase, to yield a first reaction mixture comprising GVL, hydroxypentanoic acid (4HPA), and water; b) removing water from said first reaction mixture; and c) subjecting the mixture obtained in step b) to a further reaction under conditions suitable to convert said 4-HPA to GVL, to yield a further reaction mixture. Steps b) and c) can be integrated. Optionally, water can be removed from the further reaction mixture. The process may include recycling the—optionally at least partially dewatered—further reaction mixture back to step (b). This is particularly advantageous when the first reaction mixture is low in, or even free of levulinic acid.
    Type: Grant
    Filed: February 16, 2016
    Date of Patent: February 11, 2020
    Assignee: DSM IP ASSETS B.V.
    Inventors: Rudolf Philippus Maria Guit, Alejandro Varela Fernández
  • Patent number: 10559764
    Abstract: A fused polycyclic heteroaromatic compound represented by Chemical Formula 1A or 1B that has a compact planar structure in which eight or more rings are fused together.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: February 11, 2020
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Jeong Il Park, Eigo Miyazaki, Eun Kyung Lee, Ajeong Choi
  • Patent number: 10550113
    Abstract: A compound of formula (I?) or (I?) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of mammalian kinase enzyme activity, including ROR1 tyrosine kinase activity and may be used in the treatment of disorders associated with such activity.
    Type: Grant
    Filed: February 1, 2016
    Date of Patent: February 4, 2020
    Assignee: KANCERA AB
    Inventors: Hakan Mellstedt, Styrbjorn Bystrom, Jan Vagberg, Elisabeth Olsson
  • Patent number: 10531664
    Abstract: A method of stabilizing aqueous solutions of antimicrobial silanol quaternary ammonium compounds (SQACs) from premature polymerization where the stabilizing agent is selected from a list of antimicrobial, naturally occurring, renewable, volatile, liquid phytochemical essential oils that easily form crystal clear microemulsions when water is added to the concentrated SQAC/essential oil mixture. These non-foaming oil-in-water microemulsions have excellent long term storage stability, remain very low in viscosity and do not phase or precipitate for many months. Many essential oils found to be useful in this process are non-toxic food additives having pleasant scents, have low flammability yet are volatile enough to evaporate upon cure down of the SQAC, resulting in a higher concentration of SQAC in the cured, antimicrobial film.
    Type: Grant
    Filed: March 28, 2018
    Date of Patent: January 14, 2020
    Assignee: Indusco, Ltd.
    Inventors: Joseph E. Mason, Dennis Victor Neigel
  • Patent number: 10533034
    Abstract: Glycosphingolipids (GSLs) compositions and methods for iNKT-independent induction of chemokines are disclosed.
    Type: Grant
    Filed: January 9, 2018
    Date of Patent: January 14, 2020
    Assignee: ACADEMIA SINICA
    Inventors: Chi-Huey Wong, Alice L. Yu, Kun-Hsien Lin, Tai-Na Wu
  • Patent number: 10526349
    Abstract: The disclosure includes high purity compounds having CCR5 and/or CCR2 antagonism, or a salt thereof, and processes for synthesizing the same.
    Type: Grant
    Filed: December 23, 2015
    Date of Patent: January 7, 2020
    Assignee: Tobira Therapeutics, Inc.
    Inventor: Nicholas Morra
  • Patent number: 10519124
    Abstract: Disclosed herein are methods for synthesizing 1,2,5,6-hexanetetrol (HTO), 1,6 hexanediol (HDO) and other reduced polyols from C5 and C6 sugar alcohols or R glycosides. The methods include contacting the sugar alcohol or R-glycoside with a copper catalyst, most desirably a Raney copper catalyst with hydrogen for a time, temperature and pressure sufficient to form reduced polyols having 2 to 3 fewer hydoxy groups than the starting material. When the starting compound is a C6 sugar alcohol such as sorbitol or R-glycoside of a C6 sugar such as methyl glucoside, the predominant product is HTO. The same catalyst can be used to further reduce the HTO to HDO.
    Type: Grant
    Filed: April 25, 2018
    Date of Patent: December 31, 2019
    Assignee: ARCHER DANIELS MIDLAND COMPANY
    Inventors: Kenneth Stensrud, Chi-Cheng Ma, Kevin Martin
  • Patent number: 10519147
    Abstract: Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: December 31, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas J. Greshock, James Mulhearn, Liangqin Guo, Ting Zhang, Deping Wang, Ronald M. Kim, Mark E. Layton, Michael J. Kelly, III, Rajan Anand, Philippe Nantermet, Tianying Jian, Anthony J. Roecker, Walter Won, Gang Zhou