Abstract: A method for preparing diazoxide includes reacting o-aminobenzenesulfonamide with N-chlorosuccinimide in a chlorine solvent to obtain 2-amino-5-chlorobenzenesulfonamide, mixing the 2-amino-5-chlorobenzenesulfonamide, an imidazole salt and an amide solvent, then heating same for reaction so as to obtain diazoxide; or mixing o-aminobenzenesulfonamide, an imidazole salt and an amide solvent, then heating same for reaction to obtain a compound IV; then reacting the compound IV with N-chlorosuccinimide in a chlorine solvent to obtain diazoxide. The application of imidazole hydrochloride as a catalyst in preparing diazoxide is also disclosed. The present invention avoids the use of highly corrosive and toxic chlorosulfonyl isocyanate, a strong acid (sulfuric acid), and a high reaction temperature (240-250° C.
Abstract: The present invention relates to a phenyl alkyl carbamate compound for use in preventing or treating neurodegenerative diseases. The phenyl alkyl carbamate compound of the present invention, prevented dopaminergic neuron loss, attenuated activation of astrocyte/microglia, repressed phosphorylated alpha-synuclein, and regulated phosphorylation levels of tau and acetylation levels of alpha-tubulin in the Parkinson's disease animal model. In addition, the phenyl alkyl carbamate compound of the present invention reduced the Amyloid-beta precursor protein and Amyloid-beta. Therefore, the phenyl alkyl carbamate compound of the present invention may be effectively used for preventing or treating neurodegenerative diseases.
Abstract: Ethylene oxide purification by quenching and washing ethylene oxide reactor effluent prior to passing the gaseous ethylene oxide-containing stream to an ethylene oxide absorber to form a dilute aqueous ethylene oxide and carbon dioxide solution and thereafter stripping that solution in an EO stripper to produce a gaseous ethylene oxide and carbon dioxide-containing overhead vapor which is then passed to a reabsorber wherein the ethylene oxide and part of the carbon dioxide vapors are absorbed to form an aqueous reabsorbate solution from which carbon dioxide is removed to produce an ethylene oxide-containing solution is improved by passing an impurities-containing liquid bleed stream obtained from the quench wash to a second, small quench bleed stripper where steam and carbon dioxide are added and gaseous overhead from that quench bleed stripper is passed to the reabsorber for recovery of the EO and removal of formaldehyde and other impurities.
Abstract: The present invention relates to compounds which may be useful as inhibitors of PTPN11 for the treatment or prevention of cancer and other PTP-mediated diseases. Disclosed herein are new compounds and compounds based on pyrazolopyrazines and their application as pharmaceuticals for the treatment of disease.
Type:
Grant
Filed:
February 3, 2021
Date of Patent:
March 19, 2024
Assignee:
NAVIRE PHARMA, INC.
Inventors:
Philip Jones, Jason Cross, Jason Burke, Timothy McAfoos, Zhijun Kang
Abstract: Disclosed herein are synthesis methods for coelenterazine and intermediates. Also disclosed are articles including the coelenterazine and coelenterazine derivatives. Representative absorbent articles include disposable diapers and adult incontinence products.
Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
Abstract: A therapeutic method of treating mild cognitive impairment and improving human cognitive function, comprising: orally administering Beta-Caryophyllene (BCP), whereas the BCP improves cognitive function.
Abstract: A process for producing unsaturated nitrile comprising a reaction step of subjecting hydrocarbon to a vapor phase catalytic ammoxidation reaction in a fluidized bed reactor to produce the corresponding unsaturated nitrile, wherein, in the reaction step, a powder is fed to a dense zone in the fluidized bed reactor using a carrier gas, and a ratio of a linear velocity LV1 of the carrier gas at a feed opening to feed the powder to the fluidized bed reactor to a linear velocity LV2 of a gas in the dense zone (LV1/LV2) is not less than 0.01 and not more than 1200.
Abstract: Phenothiazine compounds of Formula (I) are described herein. These compounds are useful as highly reducing organic photoredox catalysts. Suitable substrates for use with the compounds of Formula (I) include acrylates, styrene, acrylamides, acrylonitrile, vinyl chloride, methylacrylonitrile, vinyl acetate, and acrylic acid.
Type:
Grant
Filed:
January 8, 2021
Date of Patent:
February 20, 2024
Assignees:
THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE, COLORADO STATE UNIVERSITY RESEARCH FOUNDATION
Inventors:
Steven Sartor, Niels Damrauer, Garet Miyake, Cameron Chrisman, Ryan Pearson
Abstract: The present invention relates to reagents comprising a substituted acyl borate or a substituted hydroxylamine, to a method of synthesizing a carrier-linked prodrug using said reagents and to carrier-linked prodrugs obtainable by said method.
Type:
Grant
Filed:
July 12, 2017
Date of Patent:
February 13, 2024
Assignee:
ASCENDIS PHARMA A/S
Inventors:
Nicola Bisek, Samuel Weisbrod, Kornelia Bigott
Abstract: This disclosure relates to JAK1 pathway inhibitors and the use thereof in treating chronic lung allograft dysfunction such as, e.g., bronchiolitis obliterans syndrome.
Abstract: Sultam compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with the KEAP1-Nrf2 interaction, such as inflammatory bowel disease, including Crohn's disease and ulcerative colitis.
Type:
Grant
Filed:
December 18, 2020
Date of Patent:
February 13, 2024
Assignee:
Janssen Pharmaceutica NV
Inventors:
J. Kent Barbay, Wenying Chai, Gavin C. Hirst, Kevin D. Kreutter, David A. Kummer, Kelly J. McClure, Rachel T. Nishimura, Amy Y. Shih, Jennifer D. Venable, Hariharan Venkatesan, Jianmei Wei
Abstract: Compounds of the present application or pharmaceutically acceptable salts thereof are capable of interacting with and attenuating the activity of a stimulator of interferon genes (STING) protein. In an embodiment of the invention, antagonist compounds bind to STING protein and attenuate STING downstream signaling. Pharmaceutical compositions and methods involving such compounds as STING modulators are additionally provided herein.
Abstract: A treatment regime for use in the treatment or prevention of dermatitis and inflammatory skin conditions, said regime comprising the administration of: a) between 50 mg and 3000 mg of a topical liquid or gel composition comprising between 1% w/w and 15% w/w cannabinoid, wherein the cannabinoid is dissolved in the liquid or gel composition.
Abstract: Certain embodiments are directed to methods and compositions for treating or preventing seizures in a subject using a therapeutic agent comprising one or more Transient Receptor Potential-Canonical 4/5 channel antagonists sufficient to regulate excitability of neurons in the brain of a subject.
Type:
Grant
Filed:
February 25, 2021
Date of Patent:
January 23, 2024
Assignee:
Board of Regents, The University of Texas System
Abstract: The invention relates to compounds of Formula (I), (Ia), (Ib), (II) or (III), salts thereof, pharmaceutical compositions thereof, as well as therapeutic methods of treatment and prevention.
Type:
Grant
Filed:
August 6, 2021
Date of Patent:
January 16, 2024
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Abstract: Disclosed herein are methods for treating a subject afflicted with a cancer having an activating RET alteration by administering an effective amount of a selective RET inhibitor, e.g., Compound 1 or pharmaceutically acceptable salts thereof, including, e.g., administering an amount of 60 mg to 400 mg of the selective RET inhibitor once daily.
Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.
Type:
Grant
Filed:
November 16, 2020
Date of Patent:
January 9, 2024
Assignee:
Incyte Corporation
Inventors:
Joshua Hummel, Oleg Vechorkin, Alexander Sokolsky, Qinda Ye, Kai Liu, Wenqing Yao