Abstract: The invention relates to particular prodrugs of substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the ?-opioid receptor.
Abstract: The present invention provides for the treatment, prevention, and/or reduction of a risk of a disease, disorder, or condition in which aldehyde toxicity is implicated in the pathogenesis, including ocular disorders, skin disorders, conditions associated with injurious effects from blister agents, and autoimmune, inflammatory, neurological and cardiovascular diseases by the use of a primary amine to scavenge toxic aldehydes, such as MDA and HNE.
Type:
Grant
Filed:
March 7, 2022
Date of Patent:
October 3, 2023
Assignee:
Aldeyra Therapeutics, Inc.
Inventors:
Todd Brady, Scott Young, William A. Kinney, Kenneth J. Mandell
Abstract: The present invention discloses a composition containing hesperetin and synergistic hypoglycemic application thereof, and belongs to the technical field of natural active compounds. The composition of the present invention contains the hesperetin and a compound X, and the compound X is galangin or formononetin, where a mass ratio of the hesperetin to the galangin is 30:100, and a mass ratio of the hesperetin to the formononetin is 30:20. The composition of the present invention has an obvious synergistic effect of inhibiting ?-glucosidase, and the effect thereof is better than that of using the flavonoid compound alone, and may reduce a dosage of the use of drugs and occurrence of drug resistance.
Type:
Grant
Filed:
December 15, 2022
Date of Patent:
October 3, 2023
Assignee:
ZHENGZHOU FRUIT RESEARCH INSTITUTE, CHINESE ACADEMY OF AGRICULTURAL SCIENCES
Abstract: Disclosed in the present invention are a naphthalenesulfonamide compound, a preparation method, and an application. The naphthalenesulfonamide compound provided by the present invention can interfere with Keap1-Nrf2 binding and activate Nrf2 to relieve inflammatory damage and improve an inflammatory microenvironment, has a potential anti-inflammatory activity, and can be used for preparing an anti-inflammatory drug for inflammatory damage of various inflammation-related diseases, including chronic obstructive pulmonary disease (COPD), Alzheimer's disease, Parkinson's disease, atherosclerosis, chronic kidney disease (CKD), diabetes, intestinal Inflammations, rheumatoid arthritis, etc.
Type:
Grant
Filed:
April 13, 2020
Date of Patent:
October 3, 2023
Assignee:
CHINA PHARMACEUTICAL UNIVERSITY
Inventors:
Qidong You, Zhengyu Jiang, Yuting Liu, Mengchen Lu, Hongli Shao, Jing Zhao, Xiaoli Xu, Xiaoke Guo, Lei Wang
Abstract: The present disclosure provides the compound having inhibitory property against TNIK having a specific chemical structure or its pharmaceutically acceptable salt. The present disclosure also provides a composition comprising the compound or its pharmaceutically acceptable salt. The present disclosure also provides a medical use of the compound, its salt or the composition comprising the compound or its pharmaceutically acceptable salt for treating or preventing cancer. The present disclosure also provides a method of treatment or prevention of cancer comprising administering the compound, its salt or the composition comprising the compound or its salt to a subject in need of such treatment or prevention.
Type:
Grant
Filed:
September 7, 2022
Date of Patent:
September 26, 2023
Assignees:
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY, INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
Inventors:
Sung Youn Chang, Hyuk Lee, Ki Young Kim, Bum Tae Kim, Sung Soo Kim, Seong Hwan Kim, Hwan Jung Lim, Jung Nyoung Heo, Sang Joon Shin, Sang Youn Park
Abstract: In one aspect, compounds of Formulae (I) and (II), or pharmaceutically acceptable salts thereof, are featured; Formula (I), Formula (II) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formulae (I) and (II) can be as defined anywhere herein.
Type:
Grant
Filed:
April 1, 2022
Date of Patent:
September 19, 2023
Assignee:
Novartis AG
Inventors:
Gary Glick, Shomir Ghosh, William R. Roush
Abstract: The present invention describes a process to isomerize industrial hemp derived Cannabidiol (CBD) to a pure ?8-tetrahydrocannabinol (?8-THC) extract. This procedure will produce ?8-tetrahydrocannabinol that is essentially free from any detectable levels of ?9-tetrahydrocannabinol (?9-THC). Included in this filing are methods and processes to scale the reaction from the lab to process to large scale manufacturing. Additionally, the resulting extract from said methods and processes consists of higher purity than previously reported in the art and greater efficiency compared to prior art.
Abstract: The present disclosure provides methods and compositions for the prevention, amelioration, or alleviation of one or more neurological disorders associated with microbially-induced amyloid formation. Methods of inhibiting, ameliorating, reducing the likelihood, delaying the onset of, treating, or preventing an amyloid disorder are disclosed. Methods of identifying compounds capable of inhibiting the formation of microbially-induced amyloid fibrils are disclosed.
Type:
Grant
Filed:
September 8, 2021
Date of Patent:
September 5, 2023
Assignees:
Axial Therapeutics, Inc., California Institute of Technology
Inventors:
Timothy Sampson, Sarkis Mazmanian, Anthony Stewart Campbell
Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
Type:
Grant
Filed:
November 16, 2020
Date of Patent:
August 29, 2023
Assignee:
THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
Abstract: The present invention relates to the (S) enantiomeric form of certain 6-chromanol derivatives for use as a medicament. Especially, the present invention relates to the (S) enantiomeric form of a 6-chromanol derivative for use as a medicament wherein said 6-chromanol derivative is chosen from the group consisting of (6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)(piperazin-1-yl)methanone; N-(benzyl)-6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxamide; N-(phenyl)-6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxamide; methyl 4-(6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxamido)benzoate; (6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)(morpholino)methanone, and pharmaceutically acceptable salts or bases thereof and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
August 23, 2018
Date of Patent:
August 22, 2023
Assignee:
SULFATEQ B.V.
Inventors:
Robert Henk Henning, Gerrit Jan Willem Euverink, Guido Krenning, Adrianus Cornelis Van der Graaf
Abstract: The present disclosure relates to the selective hydrodeoxygenation (HDO) of bio-based furanic ketones with a bifunctional copper-based catalyst in the presence of a solvent to prepare alkyl furans with high yield, purity, and scalability. The alkyl furans prepared herein are useful in the preparation of surfactants.
Type:
Grant
Filed:
September 25, 2020
Date of Patent:
August 8, 2023
Assignee:
Triad National Security, LLC
Inventors:
Andrew Sutton, Xiaokun Yang, Cameron M. Moore
Abstract: The following invention relates to (R)-4-(1-(1-(4-(trifluoromethyl)benzyl) pyrrodiline-2-carboxamide) cyclopropyl benzoic acid (Compound 1) or a salt thereof. Advantageous methods for obtaining the Compound 1 are also described, as well as pharmaceutical compositions containing it (R)-4-(1-(1-(4-(trifluoromethyl)benzyl)pyrrodiline-2-carboxamide) cyclopropyl benzoic acid (Compound 1) or a pharmaceutically acceptable salt thereof is described for use as an EP4 receptor antagonist in the treatment of a pathology that involves the activities of prostaglandin E2 (PGE2) in its pathogenesis.
Type:
Grant
Filed:
July 4, 2019
Date of Patent:
August 8, 2023
Assignee:
ROTTAPHARM BIOTECH S.R.L.
Inventors:
Sabrina Pucci, Francesco Makovec, Lucio Claudio Rovati
Abstract: The invention relates to a method of preparing titanium dioxide-coated nanostars. Titanium precursors are hydrolyzed into crystalline TiO2 polymorphs at low temperatures, allowing the delicate morphology of the nanostars to be preserved while maintaining their desirable photocatalytic properties.
Type:
Grant
Filed:
April 22, 2020
Date of Patent:
August 1, 2023
Assignee:
RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
Inventors:
Laura Fabris, Fuat E. Celik, Supriya Atta, Ashley M. Pennington
Abstract: A process for carboxylation of a furoate slurry to produce FDCA, especially 2,5-FDCA, includes the steps of: feeding a slurry containing a suspension fluid, furoate, a surfactant and an alkali metal carbonate to a carboxylation reactor; and feeding a flow of CO2 to the carboxylation reactor at flow conditions sufficient to suspend the slurry in the reactor and react the furoate with CO2 to form 2,5-FDCA. A fully integrated process is also disclosed.
Type:
Grant
Filed:
July 16, 2021
Date of Patent:
July 25, 2023
Assignee:
KSE, Inc.
Inventors:
James R. Kittrell, Carl R. Dupre, Keith D. Kittrell, Leonard T. McDonald, Jeffrey A. Kittrell
Abstract: In one embodiment, a continuous process for preparing organic carbonate solvent of Formula (I) as described herein comprises contacting a first reactant (an alcohol) with a reactive carbonyl source (carbonyldiimidazole (CDI) or an alkylchloroformate) in the presence of a catalyst in reaction stream flowing through a continuous flow reactor at temperature 20° C. to about 160° C. and at a flow rate providing a residence time in the range of about 0.1 minute to about 24 hours; collecting a reactor effluent exiting from the continuous flow reactor; recovering a crude product from the reactor effluent; and distilling the crude product to obtain the organic carbonate compound of Formula (I). In another embodiment, the first reactant is an epoxide and the carbonyl source is carbon dioxide.
Abstract: The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B) or a pharmaceutically acceptable salt or hydrate thereof, that inhibit CC chemokine receptor 6 (CCR6), pharmaceutical compositions containing these compounds, and the use of these compounds for treating or preventing diseases, conditions, or disorders ameliorated by inhibition of CCR6.
Type:
Grant
Filed:
March 5, 2021
Date of Patent:
July 25, 2023
Assignee:
Pfizer Inc.
Inventors:
Brian Stephen Gerstenberger, Andrew Christopher Flick, Daniel Wei-Shung Kung, Vincent Michael Lombardo, James John Mousseau, Philippe Marcel Nuhant, Ralph Pelton Robinson, Jr., Daniel Copley Schmitt, Mark Edward Schnute, Atli Thorarensen, John Isidro Trujillo, Rayomand Jal Unwalla, Huixian Wu
Abstract: The present invention provides new methods for preparing compound 5, and pharmaceutically acceptable salts thereof, of structure Compound 5, or a pharmaceutically acceptable salt thereof, is an important intermediate in the synthesis of carfilzomib. The invention further provides methods of making a useful manganese catalyst that may be used in the epoxidation step of the present invention.
Type:
Grant
Filed:
August 3, 2017
Date of Patent:
July 25, 2023
Inventors:
Matthew Beaver, Sheng Cui, Xiangqing Shi
Abstract: The present invention provides for the treatment, prevention, and/or reduction of a risk of a disease, disorder, or condition in which aldehyde toxicity is implicated in the pathogenesis, including ocular disorders, skin disorders, conditions associated with injurious effects from blister agents, and autoimmune, inflammatory, neurological and cardiovascular diseases by the use of a primary amine to scavenge toxic aldehydes, such as MDA and HNE.
Type:
Grant
Filed:
April 12, 2021
Date of Patent:
July 18, 2023
Assignee:
Aldeyra Therapeutics, Inc.
Inventors:
Todd Brady, Scott Young, William A. Kinney, Kenneth J. Mandell
Abstract: Provided herein is a crystalline hydrate of the compound of formula 1: Also provides herein are pharmaceutical compositions comprising such crystalline hydrate, methods of using such crystalline hydrate to treat respiratory diseases, and processes useful for preparing such crystalline hydrate.