Abstract: Disclosed herein is a method for preparing a 2-arylmalonic acid derivative. In this method, a cyclohexadiene compound is used as a raw material, and sequentially undergoes an isomerization reaction, a halogenation reaction in the presence of a halogenating agent and a dehydrohalogenation-aromatization reaction to obtain a 2-arylmalonic acid derivative (3). An intermediate for preparing the 2-arylmalonic acid derivative (3) and use of the intermediate are also disclosed.
Abstract: The present disclosure provides compounds having the general formula P-L-U, or pharmaceutically acceptable salts thereof, wherein P is a FOXO1 fusion protein binding moiety, L is a bivalent linker, and U is an ubiquitin ligase binding moiety. Also provided are pharmaceutical compositions containing such compounds and methods of using such compounds.
Type:
Grant
Filed:
September 16, 2022
Date of Patent:
April 23, 2024
Assignees:
Massachusetts Institute of Technology, Universität Zürich
Inventors:
Angela Nicole Koehler, Shelby Doyle, Becky Leifer, Madeleine Henley, Beat W. Schaefer, Marco Wachtel
Abstract: Composition for use in the prevention and/or treatment of a mitochondrial dysfunction-related neurodegenerative diseases, the composition comprising an active agent, said active agent containing the amino acids leucine, isoleucine, valine, threonine, lysine and citric acid, succinic acid, malic acid.
Abstract: Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo. Also disclosed are pharmaceutical compositions comprising a Cbl-b inhibitor and a cancer vaccine, as well as methods for treating cancer using a Cbl-b inhibitor and a cancer vaccine; and pharmaceutical compositions comprising a Cbl-b inhibitor and an oncolytic virus, as well as methods for treating cancer using a Cbl-b inhibitor and an oncolytic virus.
Type:
Grant
Filed:
July 13, 2022
Date of Patent:
April 9, 2024
Assignee:
NURIX THERAPEUTICS, INC.
Inventors:
Arthur T. Sands, Neil F. Bence, Christoph W. Zapf, Frederick Cohen, Chenbo Wang, Thomas Cummins, Hiroko Tanaka, Hunter Shunatona, Mario Cardozo, Dahlia Weiss, Jennifa Gosling
Abstract: Described herein are synthetic progestogens, such as 6?,7?:15?,16?-Dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.
Type:
Grant
Filed:
August 4, 2023
Date of Patent:
April 9, 2024
Assignee:
LABORATORIOS LEON FARMA SA
Inventors:
Philippe Perrin, Jose Luis Velada, Dominique Drouin
Abstract: Disclosed are conjugate molecules formed from an active agent which is linked to a cannabinoid moiety through a specified linker having ester and amide end groups. The active agent can be a COX-2 inhibitor moiety, and the cannabinoid moiety can be a cannabidiol moiety. These conjugate molecules are contemplated to potentially be effective in the treatment of medical conditions.
Type:
Grant
Filed:
April 21, 2023
Date of Patent:
April 2, 2024
Assignee:
AKOS BIOSCIENCES, INC.
Inventors:
Paul M. Hershberger, Yinghui Liu, Kirk William Hering, James Bernard Kramer, Ramanathan S. Lalgudi
Abstract: Disclosed herein are 5-Substituted 4-amino-1H-benzo[c][1,2,6]thiadiazine 2,2-dioxide compounds useful as sweet flavor modifiers. Also disclosed herein are ingestible compositions that include one or more of these compounds in combination with a natural or artificial sweetener.
Type:
Grant
Filed:
August 6, 2019
Date of Patent:
April 2, 2024
Assignee:
FIRMENICH INCORPORATED
Inventors:
Joseph R. Fotsing, Catherine Tachdjian, Guy Servant, Brett Weylan Ching, Timothy Davis
Abstract: The present invention relates to compounds of Formula I, pharmaceutically acceptable salts, solvates or formulations thereof. Compounds of Formula I increase significantly low density lipoprotein receptor and are useful for preventing and treating of elevated cholesterol.
Type:
Grant
Filed:
May 23, 2022
Date of Patent:
March 19, 2024
Assignee:
Montréal Heart Institute
Inventors:
Steve Poirier, Brent Richard Stranix, Gaétan Mayer
Abstract: The present disclosure relates to a JAK inhibitor upadacitinib intermediate and a preparation method therefor, and to a preparation method for a JAK inhibitor upadacitinib. The upadacitinib intermediate of the present application is as shown in Formula (II) or Formula (III), wherein, R is a protective group of nitrogen atoms, and R1 is an open-chain or cyclic amine group. Compared with the prior art, the method for the synthesis of upadacitinib of the present application, significantly reduces cost, is environmentally-friendly. And the quality of the final product is well controlled.
Abstract: The invention provides for bifunctional molecules comprising an Rpn11 binding partner and a target protein binding partner. A bifunctional molecule according to the invention binds to Rpn11 and to the target protein, thereby facilitating degradation of the target protein bound to the target protein binding partner. The invention also provides for use of a bifunctional molecule for preventing or treating disease.
Type:
Grant
Filed:
June 13, 2019
Date of Patent:
March 12, 2024
Assignee:
AMPHISTA THERAPEUTICS LIMITED
Inventors:
Alessio Ciulli, Andrea Testa, Scott Hughes, Steven Peter Butcher
Abstract: This invention relates to new crystalline forms of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile(lorlatinib) maleate. The invention also relates to pharmaceutical compositions comprising lorlatinib maleate, and to methods of using lorlatinib maleate and compositions comprising it in the treatment of abnormal cell growth, such as cancer, in mammals.
Abstract: The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.
Type:
Grant
Filed:
March 4, 2022
Date of Patent:
March 5, 2024
Assignee:
Praxis Precision Medicines, Inc.
Inventors:
Kiran Reddy, Gabriel Martinez Botella, Andrew Mark Griffin, Brian Edward Marron
Abstract: The present invention enables provision of a production method for 1,2,3,5,6-pentathiepane, the method comprising, in the following order, step A for reacting a trithiocarbonate, sulfur, and a methane dihalide together using a phase-transfer catalyst in a multilayer system having a water layer and an organic layer, step B for separating the water layer from the organic layer, and step C for stopping the reaction using an acid.
Abstract: The invention provides 5-deuterium-enriched 2,4-thiazolidinediones (e.g., 5-[4-[2-(5-ethyl-2-pyridyl)-2-oxoethoxy]benzyl]-5-deutero-thiazolidine-2,4-dione), deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
Type:
Grant
Filed:
August 13, 2021
Date of Patent:
March 5, 2024
Assignee:
Poxel SA
Inventors:
Sheila DeWitt, Vincent Jacques, Leonardus van der Ploeg
Abstract: Described herein are neurotrophic and nootropic compositions and methods for treating subjects with such compositions. In one aspect the composition comprises one or more tryptamines or in pure form or extracts from psilocybin containing mushrooms, or combinations thereof optionally combined with one or more phenethylamines or amphetamines in pure form or extracts from a plant or mushroom, or combinations thereof, optionally one or more erinacines or hericenones in pure form, extracts from Hericium mushroom species (e.g., H. erinaceus, H. coralloides, H. ramosum) or combinations thereof, optionally one or more cannabinoids in pure form or extracts from Cannabis sativa, Cannabis sativa, Cannabis indica, or Cannabis ruderalis, optionally, one or more adversive compounds, and optionally one or more pharmaceutically acceptable excipients.
Abstract: The present invention relates to a phosphine precursor for the preparation of a quantum dot, and a quantum dot prepared therefrom. Using the phosphine precursor for the preparation of a quantum dot of the present invention, a quantum dot with improved luminous efficiency and higher luminous color purity can be provided.
Type:
Grant
Filed:
March 2, 2018
Date of Patent:
February 27, 2024
Assignee:
SK Chemicals Co., Ltd.
Inventors:
Hee Il Chae, Jeong Ho Park, Kyung Sil Yoon, Ju-Sik Kang, Yu Mi Chang, Nam-Choul Yang, Jae Kyun Park, Song Lee
Abstract: A solid oral nicotine formulation is disclosed, the formulation comprises a nicotine-ion exchange resin combination, and a salt comprising inorganic divalent cations, wherein the salt has a water-solubility of at least 5 grams per 100 mL of water measured at 25 degrees Celsius, atmospheric pressure and pH 7.0.
Abstract: The coumarin compounds are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against gram-positive and gram-negative bacteria, as well tuberculosis mycobacteria. They also showed potent activity against drug-resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.
Abstract: A method of synthesizing a pharmacological compound substance by attaching a psychoactive base substance to an amino acid and creating a prodrug with modified pharmacological behavior. A prodrug made by the method. A pharmaceutical composition comprising a prodrug of a psychoactive base substance attached to an amino acid and a pharmaceutically acceptable salt.
Type:
Grant
Filed:
August 23, 2022
Date of Patent:
February 13, 2024
Assignee:
Mind Medicine, Inc.
Inventors:
Daniel Trachsel, Matthias Emanuel Liechti, Felix Lustenberger