Abstract: This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease) and traumatic CNS injury, as well as pain.
Type:
Grant
Filed:
December 3, 2018
Date of Patent:
July 27, 2021
Assignee:
Tufts University
Inventors:
Philip G. Haydon, Jinbo Lee, Jinghui Dong, Stephen Moss, Raquel Revilla-Sanchez
Abstract: When using a pharmaceutical composition for preventing or treating malignant hyperthermia, containing NAADP antagonists, of the present invention, malignant hyperthermia can be effectively prevented or treated through the inhibition of an oxygen consumption rate abnormal increase, which is associated with a ryanodine receptor (RYR) of skeletal muscles. In addition, the present invention can be used even after the onset of malignant hyperthermia and can inhibit an oxygen consumption rate abnormal increase even at concentrations lower than those of conventional agents for treating malignant hyperthermia, thereby enabling conventional agents for treating malignant hyperthermia to be replaced, and can be stably used, thereby being effectively usable in relevant industries.
Type:
Grant
Filed:
October 11, 2017
Date of Patent:
July 27, 2021
Assignee:
Industrial Cooperation Foundation Chonbuk National University
Inventors:
Uh Hyun Kim, Dae Ryoung Park, Kwang Hyun Park
Abstract: Inhibitor compounds with biological activity against kinetoplastid parasites, along with methods of use of the compounds, are provided. The compounds can be used to strongly inhibit key drug targets found in protozoan parasites, e.g., the target Trypanosoma cruzi glucokinase. Compounds include derivatives of 3-nitro-2-phenyl-2H-chromene, and monosaccharide amines including D-glucosamine, D-mannosamine, D-galactosamine, and D-fructosamine.
Abstract: The present invention relates to a stevioside M crystal form, a preparation method therefor and a use thereof, and specifically, relates to a naturally extracted high-intensity sweetener, i.e., a stevioside M crystal form A, the preparation method therefor and the user thereof. By means of comprehensive characterization of the new crystal form, the new crystal form is found to have advantages such as a high degree of crystallinity, good stability, and low hygroscopicity, and is applicable to a more comprehensive field of application. The preparation method in the present invention is simple and easy to operate, has high selectivity and good reproducibility, and can stably obtain the target crystal form.
Type:
Grant
Filed:
March 14, 2018
Date of Patent:
July 13, 2021
Assignee:
ZHUCHENG HAOTIAN PHARM CO., LTD.
Inventors:
Liping Zhu, Xuefeng Mei, Ying Huang, Jianrong Wang
Abstract: The present invention provides ergostenol glycoside derivatives, method for preventing, treating, or alleviating dermatitis using the same. The present invention also provides a method for preparing the ergostenol and glycoside derivatives thereof. The ergostenol and the glycoside derivatives thereof according to the present invention suppress the production of chemokines increasing according to the skin inflammation stimulation and inhibit the activity of transcriptional factors controlling the expression of various inflammation mediators in the prevention and treatment of dermatitis.
Type:
Grant
Filed:
July 22, 2019
Date of Patent:
July 13, 2021
Assignee:
ST PHARM CO., LTD.
Inventors:
Hakwon Kim, Tae Hoon Lee, Hoongyu Park, Hyunjeong Oh
Abstract: The present invention relates to novel spirobicyclic analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
Type:
Grant
Filed:
December 6, 2018
Date of Patent:
July 13, 2021
Assignee:
Janssen Pharmaceutica NV
Inventors:
Jonas Verhoeven, Guido Alfons F. Verniest, Johannes Wilhelmus John F. Thuring, Tongfei Wu, Vineet Pande, Lieven Meerpoel, Dirk Brehmer, Weimei Sun, Scott E. Denmark
Abstract: A cyclic dinucleotide compound of Formula (I): wherein X1 is H or F; X2 is H or F; at least one among X1 and X2 is a fluorine atom; Z is OH, OR1, SH or SR1, wherein: R1 is Na or NH4, or R1 is an enzyme-labile group which provides OH or SH in vivo such as pivaloyloxymethyl; B1 and B2 are bases chosen from Adenine, Hypoxanthine or Guanine, and B1 is a different base than B2 and a pharmaceutically acceptable salt thereof. Pharmaceutical compositions including the cyclic dinucleotide, as well as their use in the treatment of a bacterial infection, a viral infection or a cancer are also described.
Abstract: An ?-D-galactopyranose compound of the general formula (1). The ?-D-galactopyranose compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-1 to a ligand in a mammal, such as a human. Furthermore, a method for treatment of a disorder relating to the binding of a galectin, such as galectin-1 to a ligand in a mammal, such as a human.
Abstract: This invention relates to pharmaceutical formulations of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate, a monophosphate derivative of the well-known oncology drug gemcitabine. In particular, the invention relates to formulations which comprise a polar aprotic solvent, preferably dimethyl acetamide (DMA). Formulations comprising these solvent provide therapeutically effective treatments of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. The invention also relates to methods of using said formulations and kits comprising said formulations.
Abstract: The present invention is directed carbocyclic nucleoside reverse transcriptase inhibitors compounds of Formula I and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.
Abstract: The present disclosure discloses carbohydrate derivatives used for surface modification of immune cells, use thereof, and method thereof. The carbohydrate derivatives are 9-carbon monosaccharide sialic acid derivatives modified at C9 position by targeting substituents. The surfaces of the immune cells (T cells, NK cells, macrophages, DC cells, B cells, or granulocytes) is modified by the carbohydrate derivatives to obtain modified immune cells, so that the modified immune cells can be used for treatment of tumors or other diseases to obtain good effects.
Abstract: This invention is directed to compositions for promoting wound healing and regeneration and methods of use thereof. In one aspect, methods for promoting wound healing in a subject are provided, the methods comprising: administering a therapeutically effective amount of a DNA methyl transferase inhibitors (DNMT) to the subject. In another aspect, methods for reducing scarring during healing of a skin wound are provided, the methods comprising: administering a therapeutically effective amount of a DNMT inhibitor.
Type:
Grant
Filed:
July 21, 2015
Date of Patent:
June 15, 2021
Assignee:
THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
Inventors:
George Cotsarelis, Jen-Chih Hsieh, Ying Zheng
Abstract: Compositions containing nicotinamide riboside (NR) are provided. NR containing compositions are used in the care or treatment of skin and skin conditions. In some embodiments, the invention relates to pharmaceutical compositions and cosmetic compositions containing nicotinamide riboside. In further embodiments, the invention relates to methods of using nicotinamide riboside to promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for improving cell and tissue survival. A method of treating signs or symptoms of aging or skin wrinkles in an individual is provided, comprising topically administering to the individual in need of such treatment an effective amount of the compound nicotinamide riboside, or salts thereof.
Abstract: The present disclosure provides compounds of formulas (1)-(3), and compositions and methods of use thereof. The present disclosure also provides methods of preparing a provided compound and composition, and methods of characterizing a provided compound and composition.
Abstract: The present invention provides compounds for use in treating and/or preventing influenza. The compound comprises a first and second domain in which the first domain comprises at least one anchoring group which binds to the surface of influenza viruses and the second domain comprises at least one anionic group. The first and second domains are covalently linked. Also provided are pharmaceutically acceptable salts, solvates, prodrugs or stereoisomer of the compounds.
Type:
Grant
Filed:
May 18, 2018
Date of Patent:
May 18, 2021
Assignee:
Ausvir Therapeutics Pty LTD
Inventors:
Betty Jin, Ee-Ling Seah, Paul Arthur Jones, Peter James Jenkins, Henry Kenneth Windle, Wen Yang Wu
Abstract: The present invention relates to an indoleacetic acid derivative and a preparation method and pharmaceutical use thereof. In particular, the present invention relates to a compound shown in general formula (I), a preparation method thereof, a pharmaceutical composition comprising the same, and a use thereof as a cough suppressant in treating a disease such as a cough. The definition of each substituent in the general formula (I) is the same as the definition in the specification.
Type:
Grant
Filed:
May 15, 2018
Date of Patent:
May 18, 2021
Assignee:
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences
Inventors:
An Liu, Jintang Cheng, Cong Guo, Jun Zhang, Chang Chen
Abstract: Provided are methods for treating Arenaviridae and Coronaviridae virus infections by administering nucleosides and prodrugs thereof, of Formula I: wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Lassa virus and Junin virus infections.
Type:
Grant
Filed:
April 30, 2020
Date of Patent:
May 18, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Michael O' Neil Hanrahan Clarke, Joy Yang Feng, Robert Jordan, Richard L. Mackman, Adrian S. Ray, Dustin Siegel
Abstract: The present disclosure relates generally to compositions and methods for treating cancer with a glucopyranosyl lipid A (GLA) in the absence of antigen.
Type:
Grant
Filed:
May 20, 2019
Date of Patent:
May 4, 2021
Assignee:
Immune Design Corp.
Inventors:
Carlos V. Paya Cuenca, Jan Henrik Ter Meulen
Abstract: The present application belongs to the field of chemical synthesis, and specifically relates to a six-membered ring-containing nucleoside compound and a preparation method thereof. The present application discloses a six-membered ring-containing nucleoside compound. The structural formula of the nucleoside compound 7 is: where R1 is selected from one of where R2 is hydroxyl or alkynyl.
Abstract: A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5? position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides can be represented by the general formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.
Type:
Grant
Filed:
August 23, 2019
Date of Patent:
April 13, 2021
Assignee:
TECHNION RESEARCH & DEVELOPMENT FOUNDATION LIMITED
Inventors:
Timor Baasov, Dana Atia-Glikin, Jeyakumar Kandasamy, Valery Belakhov