Abstract: Compounds, compositions and methods for improving the viability and/or function of cells or for the in vitro, ex vivo or in vivo protection of cells, tissue, graft or organs from various damages are described. The reagents and composition are based on activation of the heat shock response and/or the antioxidant response and include for example, HSP90 co-factor inhibitor such as Celastrol or Celastrol analogs used alone or in combination with an adjunct agent (e.g., a NRF-2 activator, antioxidant, etc.). Therapeutic enhancement may also include increase in paracrine effector production and signaling. Methods for improving the resistance of cells, tissue, grafts or organs to damages or stress, such as hypoxic or oxidative stress-induced cell death, and/or for improving the viability and retention of transplanted or transfused cells are also described. Therapeutic treatment or prevention of ischemic injury (e.g.
Abstract: Provided herein are novel ligands and pharmaceutical compositions thereof which modulate IL-17A. Also provided are methods for preparing the IL-17A modulators. Such compounds may be useful in the treatment and/or prevention of, for example, inflammation, cancer or autoimmune disease.
Type:
Grant
Filed:
February 6, 2020
Date of Patent:
September 20, 2022
Assignee:
DICE ALPHA, INC.
Inventors:
Paul R. Fatheree, Martin S. Linsell, John R. Jacobsen, Wouter Van der Linden, Timothy J. Church, Claudio Aquino, Margot Paulick
Abstract: The present invention provides combination therapy that includes an KRASG12C inhibitor, such as or a pharmaceutically acceptable salt thereof, and one or more additional pharmaceutically active agents, particularly for the treatment of cancers. The invention also relates to pharmaceutical compositions that contain an KRASG12C inhibitor and one or more additional pharmaceutically active agents for the treatment of cancers.
Type:
Grant
Filed:
November 18, 2019
Date of Patent:
September 13, 2022
Assignee:
Amgen Inc.
Inventors:
James Russell Lipford, Jude Robert Canon, Anne Y. Saiki, Karen Louise Rex
Abstract: A treatment for a hyperglycemic condition, including diabetes mellitus, includes the step of administering to a human being dimethylformamide (“DMF”), which has the chemical structural formula: DMF can be administered to the human patient in a wide variety of ways, however it is preferable that the administration of DMF be performed orally and the dose of DMF could be combined with numerous inert substances known to the prior art, such as a sugarless fruit juice concentrate. The preferred daily dosage of DMF administered to a person would be about 0.041 mg/kg body weight to about 1.23 mg/kg of body weight of the person.
Type:
Grant
Filed:
December 1, 2019
Date of Patent:
September 13, 2022
Inventors:
Robert D. Kross, Guadalupe Cleva Villanueva Lopez
Abstract: The present invention relates to a pharmaceutical composition for treating colorectal cancer including a material inhibiting the enzyme activity of peroxiredoxin 2 as an active ingredient, and more specifically, to a pharmaceutical composition for treating colorectal cancer, which exhibits the effect of reducing colon polyps via increase of active ?-catenin degradation by inhibiting the activity of peroxiredoxin 2, based on the mechanism that promotes colorectal tumor by the interaction between peroxiredoxin 2 (PrxII) and tankyrase (TNKS) in an APC-mutant cell.
Type:
Grant
Filed:
December 27, 2019
Date of Patent:
September 13, 2022
Assignee:
EWHA UNIVERSITY—INDUSTRY COLLABORATION FOUNDATION
Abstract: Disclosed herein are methods and compounds for treating glioblastoma with iniparib. Also disclosed herein is a method of selecting subjects having a glioblastoma for treatment based on a biomarker panel.
Abstract: Disclosed herein are methods and compounds for treating glioblastoma with iniparib. Also disclosed herein is a method of selecting subjects having a glioblastoma for treatment based on a biomarker panel.
Abstract: Small molecule inhibitors of neutral sphingomyelinase 2 (nSMase2) and their use for treating neurodegenerative diseases, such as, neurodegenerative diseases associated with high levels of ceramide, including, but not limited to Alzheimer's disease (AD), HIV-associated neurocognitive disorder (HAND), multiple sclerosis (MS), and amyotrophic lateral sclerosis (ALS), and, in other aspects, for treating cancer, are provided.
Type:
Grant
Filed:
January 5, 2018
Date of Patent:
August 30, 2022
Assignees:
The Johns Hopkins University, Institute of Organic Chemistry & Biochemistry
Inventors:
Barbara Slusher, Camilo Rojas, Ajit G. Thomas, Radim Nencka, Michal Sala, Hubert Hrebabecky, Norman Haughey
Abstract: Heterocyclic compounds are described that are lysophosphatidic acid receptor ligands that are useful in the treatment of lysophosphatidic acid receptor-dependent diseases and conditions, including but not limited to diseases involving fibrosis, such as fibrosis of the heart, kidney, liver and lung, and scleroderma; inflammatory diseases such as diabetic nephropathy and inflammatory bowel disease; ocular diseases such as diseases involving retinal degeneration; nerve diseases such as pruritus and pain. Non-limiting examples of those compounds include (RS)-3-Cyclopropyl-2-{4-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-benzyloxy}-propionic acid and (R)-1-(4?-{5-[1-(2-Chloro-phenyl)-ethoxycarbonylamino]-4-fluoro-pyrazol-1-yl}-2-fluoro-biphenyl-4-yl)-cyclopropanecarboxylic acid.
Type:
Grant
Filed:
February 7, 2020
Date of Patent:
August 30, 2022
Assignee:
Epigen Biosciences, Inc.
Inventors:
Graham Beaton, Fabio C. Tucci, Satheesh B. Ravula, Chandravadan R. Shah, Hiep Luu
Abstract: The present disclosure relates to inhibitors of herpesvirus nucleic acid metabolism and inhibitors of Hepatitis B virus. Also provided are methods of treatment using these agents.
Type:
Grant
Filed:
June 10, 2016
Date of Patent:
August 23, 2022
Assignees:
Saint Louis University, Research Foundation of the City University of New York
Inventors:
John Edwin Tavis, Lynda Anne Morrison, Ryan P. Murelli
Abstract: Disclosed is a method for preparing adrenochrome by catalytic oxidation using nitrogen-doped carbon nanotubes. The method catalyzes dissolved oxygen in an aqueous solution by the nitrogen-doped carbon nanotubes to rapidly oxidize adrenaline, which is completely transformed into adrenochrome. It is a novel preparation process of adrenochrome, which is simple, and has mild reaction conditions, high product purity, an impurity content less than 10?8%, and low subsequent processing cost, thereby having a great application prospect. The nitrogen-doped carbon tubes after use can be regenerated and recovered, and its reutilization is still able to realize the complete transformation of adrenaline. The high utilization rate of catalytic material conforms to the concept of energy conservation, minimizing the costs.
Abstract: The present invention relates to the enhancement of the efficacy of anticancer agents by a composition comprising an aqueous phase, an oil phase, EPA and DHA for use in the treatment of solid tumors, wherein EPA and DHA are present in an amount of at least 65% based on the total weight of the oil phase wherein the composition comprises EPA and DHA in a weight ratio between 1:2 and 1:4, or wherein the composition comprises EPA and DHA in a weight ratio between 6:1 and 4:1 and wherein the treatment comprises administering the composition and administering at least one anticancer agent.
Type:
Grant
Filed:
October 5, 2017
Date of Patent:
August 9, 2022
Assignee:
Fresenius Kabi Deutschland GmbH
Inventors:
Martin Westphal, Edmundo Brito De La Fuente, Crispulo Gallegos-Montes, Silke Baasner, Stefanie Honndorf, Lida Quinchia
Abstract: The present invention provides a compound of Formula I: wherein X is CH2CH2, CH2CH2CH2, OCH2, or CH2O; and R is ethyl, n-propyl, cyclopropyl, or cyclobutyl; or a pharmaceutically acceptable salt thereof; with the proviso that when X is CH2CH2, then R is other than cyclopropyl; for use as a human PDE inhibitor.
Type:
Grant
Filed:
August 3, 2018
Date of Patent:
August 2, 2022
Assignee:
ELI LILLY AND COMPANY
Inventors:
Michael James Genin, William Glen Holloway, Cynthia Darshini Jesudason, Qing Shi
Abstract: The present invention relates to new compounds of formula (I) that show great affinity and activity towards the subunit ?2? of voltage-gated calcium channels (VGCC), or dual activity towards the subunit ?2? of voltage-gated calcium channels (VGCC) and the noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.
Type:
Grant
Filed:
October 26, 2018
Date of Patent:
August 2, 2022
Assignee:
ESTEVE PHARMACEUTICALS, S.A.
Inventors:
Carmen Almansa-Rosales, Félix Cuevas-Cordobés
Abstract: Provided in the present invention are a pharmaceutical composition of a substituted diphenylaminopyrimidine compound and a use thereof, wherein the compound is the compound as shown in formula (I), or a pharmaceutically acceptable salt, prodrug, hydrate or solvate, crystal form, N-oxide and various diastereomers thereof. The compound of the present invention can be used for treating diseases that can be treated with the JAK2 kinase inhibitor.
Abstract: Provided are methods of preparing 3-R-1,4,2-dioxazol-5-one compounds using convenient and efficient methods. Also provided are 3-R-1,4,2-dioxazol-5-one compounds produced using the methods described.
Type:
Grant
Filed:
June 13, 2019
Date of Patent:
July 12, 2022
Assignees:
PANASONIC HOLDINGS CORPORATION, TESLA, INC.
Inventors:
David S. Hall, Jeffery Raymond Dahn, Toren Hynes
Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Grant
Filed:
May 29, 2018
Date of Patent:
July 12, 2022
Assignee:
Novartis AG
Inventors:
Jan Jiricek, Isabelle K. Lerario, Fang Liang, Xiaodong Liu, Valentina Molteni, Advait Suresh Nagle, Shuyi Pearly Ng, Maxim Ratnikov, Jeffrey M. Smith, Yongping Xie
Abstract: Disclosed herein is a tri-substituted phenyl Btk inhibitors with improved dual selectivity, a method and a composition for inhibiting Btk and treating disease associated with undesirable Btk activity (Btk-related diseases).
Abstract: This invention is directed to novel heterocyclic prolinamide derivatives of Formula (I), and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., (s) controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention.
Type:
Grant
Filed:
June 15, 2017
Date of Patent:
July 5, 2022
Assignee:
ORION OPHTHALMOLOGY LLC
Inventors:
Robert Gomez, Jinyue Ding, Renata Marcella Oballa, David Andrew Powell, Maxim Epifanov