Abstract: The present disclosure provides compounds and nanostructures having one or more quaternary ammonium salts, compositions including the compounds and nanostructures, and methods useful for treating conditions using the compounds, nanostructures, and compositions. In at least one aspect, a compound is represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein: Q is fluoro, chloro, bromo, or iodo; each of s, b, and n is independently an integer from about 10 to about 100; and each of v, j, p, z, q, x and m is independently an integer from 1 to about 20.
Abstract: Polymorphic forms of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73) and a metabolite of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73) are disclosed and characterized. Compositions and method for treatment of Alzheimer's disease that includes the polymorphic forms and metabolite of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73).
Type:
Grant
Filed:
April 5, 2021
Date of Patent:
May 30, 2023
Assignee:
ANAVEX LIFE SCIENCES CORP.
Inventors:
Linda Sharon Daintree, Daniel Mark Ledger, Lucy Anne Leonard, Peter York, Alani Selvey
Abstract: Dioxetane compounds represented by Formula I below, and methods of using the dioxetane compounds in the detection of presence or absence, quantification, and identification of microorganisms including bacteria, bacterial fragments (e.g., LPS, endotoxin), viruses, and fungi by means of chemiluminescence.
Type:
Grant
Filed:
May 24, 2019
Date of Patent:
May 16, 2023
Assignees:
Ramot at Tel-Aviv University Ltd., NEMIS Technologies AG
Inventors:
Doron Shabat, Michal Eli Roth-Konforti, Nir Hananya, Ori Green, Urs Spitz, Lukas Wick, Julian Ihssen, Raffael Vorberg, Riccardo Cribiu, Zuzana Babjakovà, Chunyan Yao
Abstract: The present invention refers to a crystalline salt comprising 5-methyl-(6S)-tetrahydrofolic acid and 4-(2-hydroxyethyl)-morpholine wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to 4-(2-hydroxyethyl)-morpholine is from 1:0.3 to 1:2.0 (in mol/mol) and/or hydrates and/or solvates thereof as well as to a process of obtaining the same.
Type:
Grant
Filed:
July 2, 2019
Date of Patent:
April 25, 2023
Assignee:
MERCK PATENT GMBH
Inventors:
Rudolf Moser, Viola Groehn, Ruth Boehni Stamm, Fritz Blatter, Martin Szelagiewicz
Abstract: This disclosure features chemical entities of formula I (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
Type:
Grant
Filed:
July 2, 2019
Date of Patent:
April 4, 2023
Assignee:
IFM Due, Inc.
Inventors:
William R. Roush, Shankar Venkatraman, Gary Glick, Hans Martin Seidel
Abstract: The present disclosure provides a method for preparing diselenide compound. A polar solvent is added to a dihydroflavonol compound, heated to 80° C.˜100° C., kept for 40˜50 minutes, then the base in the amount of 0.4˜1.0 times the amount of the dihydroflavonol compound is added and reacted at 80° C.˜100° C. for 5˜60 minutes, then selenium dioxide in the amount of 0.6˜1.2 times the amount of dihydroflavonol compounds at 80° C.˜100° C. The diselenide compound of the dihydroflavonol compound is obtained by reacting at a temperature of 80° C.˜100° C. for 30˜150 minutes. The method of the present disclosure has mild reaction, low pollution, does not require an anhydrous and oxygen-free environment, and is suitable for large-scale industrial production.
Abstract: According to the present invention a process is provided for producing glycolide which comprises contacting glycolaldehyde dimer with an oxidizing agent to produce a glycolide product. Preferably, the process is carried out in an aprotic environment, such as in a reaction mixture comprising the glycolaldehyde dimer, the oxidizing agent, the glycolide product and an aprotic solvent.
Type:
Grant
Filed:
November 29, 2019
Date of Patent:
March 14, 2023
Assignee:
HALDOR TOPSØE A/S
Inventors:
Amanda Birgitte Sølvhøj, Rik De Clercq, Esben Taarning
Abstract: The present disclosure provides compounds of Formula (II) wherein R1, R2, R3, R4, R5, W1, W2, W3, X, Y, and A are as described herein. The disclosed compounds modulate CD73 activity. The present disclosure also provides, pharmaceutical compositions containing these compounds, and methods of using these compounds for treating diseases associated with CD73 activity.
Type:
Grant
Filed:
June 4, 2021
Date of Patent:
February 28, 2023
Assignee:
Peloton Therapeutics Inc.
Inventors:
Bin Wang, Hanbiao Yang, Karl Bedke, Paul Wehn, James P. Rizzi
Abstract: The present invention provides a thiophene carboxamide compound of the following General Formula (I), which is a novel fluorine-substituted biphenyl carboxamide-based compound, and provides a useful compound, as an agricultural and horticultural plant disease control agent, exhibiting an excellent control effect at a low dose. wherein, R, R1, R2, R3, Xm, and Y are each as defined in the specification.
Type:
Grant
Filed:
October 7, 2019
Date of Patent:
February 14, 2023
Assignees:
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY, FARMHANNONG CO., LTD
Inventors:
Jae Wook Ryu, Hyun Suk Yeom, Myeong Su Shin, In Young Oh, Ki-Ju Park, Min-Young Song, Do-Hyoung Kim, Han-Young Lee, Kyung-Jin Jun
Abstract: Disclosed are a crystal form (I) as an inhibitor of ACC1 and ACC2, a preparation method therefor, and the use thereof in the preparation of a drug as an inhibitor of ACC1 and ACC2.
Abstract: The present disclosure relates to crystalline solid forms of a stimulator of soluble guanylate cyclase (sGC), Compound I: Also provided herein are methods for the preparation of these solid forms. The invention also relates to pharmaceutical formulations and dosage forms comprising these solid forms and their uses thereof, alone or in combination with one or more additional agents, for treating and/or preventing various diseases or disorders; these diseases or disorders are ones that may benefit from sGC stimulation or from an increase in the concentration of nitric oxide (NO) and/or cyclic guanosine monophosphate (cGMP).
Type:
Grant
Filed:
December 29, 2020
Date of Patent:
February 7, 2023
Assignee:
Cyclerion Therapeutics, Inc.
Inventors:
Vasu Sethuraman, Ahmad Hashash, Song Xue, Robert C. Livingston, Kwame Wiredu Nti-Addae
Abstract: Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds provided are racemic, non-racemic or substantially enantiomerically pure cyclic peptides of formula I: or salts or solvates thereof, where variables R, W, X1, X2, and Z and are as described in the specification and L1 is a divalent linker which contains 1-12 carbon atoms, optionally 1-4 oxygen atoms, optionally one or two carbon-carbon double bonds, and hydrogen atoms to satisfy valency. Certain dimers of the cyclic peptides are also provided. One or more cylic peptides or dimers thereof herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful in treating infections of Staphylococcus bacteria. Methods for treating such bacterial infections are also provided.
Type:
Grant
Filed:
March 24, 2020
Date of Patent:
January 24, 2023
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Helen Blackwell, Joseph Vasquez, Yiftah Tal Gan
Abstract: A polymerizable liquid crystal compound represented by the following general formula (1): (the symbols in the general formula (1) are as described in the DESCRIPTION.
Abstract: A novel non-fluorescent rhodamine dye forms a twisted intramolecular charge transfer state. A substituent that causes steric hindrance is introduced at an ortho position of a dimethylamino group on the xanthene ring of tetramethylrhodamine, which is a general rhodamine that exhibits strong fluorescence, and a certain amount of twist is imparted in a ground state. As a result, the formation of the twisted intramolecular charge transfer state is promoted in the excited state and non-fluorescence is exhibited.
Abstract: The present document is directed to co-crystals of resveratrol and/or curcumin with piperazine and their use in medicine and/or as food and feed supplements.
Type:
Grant
Filed:
April 9, 2019
Date of Patent:
January 24, 2023
Assignee:
LETAVIS AB
Inventors:
Mihaela Maria Pop, Paula Vasilichia Bulieris, Ingemar Pongratz, Victor Fruth-Oprisan, Raul-Augustin Mitran
Abstract: The present invention relates to use of an aminomethylenecyclohexane-1,3-dione compound, more particularly to use of a compound shown in the following formula (I) or a pharmaceutically acceptable salt thereof alone or in combination with other drug in preparing a drug for regulating or treating a disease related to autophagy, especially mammalian ATG8 homologous proteins.
Abstract: The present disclosure provides compounds of Formula (VIA), Formula (IIIA), Formula (IVA), and Formula (VA). The compounds are prodrugs of alpha-ketoglutarate, alpha-ketobutryrate, alpha-ketoisovalerate, and alpha-ketoisohexanoate, which are useful in treating or preventing age related diseases, disorders, or conditions.
Type:
Grant
Filed:
June 30, 2020
Date of Patent:
December 13, 2022
Assignee:
The Regents of the University of California
Inventors:
Michael E. Jung, Jing Huang, Yanpeng Xing, Brett E. Lomenick, Min Chai, Xudong Fu
Abstract: A process for the purification of organic sulfur compounds involves bringing the organic sulfur compounds, in a liquid phase, into contact with an oxide of a metal from groups VIIb or VIIIb and an oxide of a metal from groups Ia to IIIa of the periodic system, or alternatively, with a mixed-oxide thereof; for a contact period of at least 1 minute. Afterwards, the oxides and the organic sulfur compounds are separated.
Type:
Grant
Filed:
August 13, 2020
Date of Patent:
December 6, 2022
Assignee:
BASF SE
Inventors:
Indre Thiel, Thomas Maximilian Wurm, Peter Rudolf
Abstract: Disclosed are 3-methylideneoxan-4-one compounds, derivatives thereof, and methods of their synthesis and methods of their use in treating a disease or disorder in a subject in need thereof, such as diseases and disorders that are associated with telomerase activity such as cancer. The disclosed compounds may be formulated in a pharmaceutical composition for treating diseases and disorders that are associated with telomerase activity such as cancer.
Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof. Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.