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: 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: 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: 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: 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: The presently-disclosed subject matter includes fluorescent indicators, including bright and targetable red Ca2+ indicators. The presently-disclosed subject matter also includes kits comprising the same as well as methods for using the same to detect a target substance.
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.
Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.
Abstract: This invention describes a method of conjugating a cell binding agent such as an antibody with an effector group (e.g., a cytotoxic agent) or a reporter group (e.g., a radionuclide), whereby the reporter or effector group is first reacted with a bifunctional linker and the mixture is then used without purification for the conjugation reaction with the cell binding agent. The method described in this invention is advantageous for preparation of stably-linked conjugates of cell binding agents, such as antibodies with effector or reporter groups. This conjugation method provides in high yields conjugates of high purity and homogeneity that are without inter-chain cross-linking and inactivated linker residues.
Type:
Grant
Filed:
September 24, 2020
Date of Patent:
November 15, 2022
Assignee:
IMMUNOGEN, INC.
Inventors:
Brenda A. Kellogg, Rajeeva Singh, Ravi V. Chari
Abstract: Compounds of formula (I), as defined herein, to processes for preparing them, to pesticidal, in particular insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control pests such as insect, acarine, molluse and nematode pests.
Type:
Grant
Filed:
August 9, 2018
Date of Patent:
November 8, 2022
Assignee:
SYNGENTA PARTICIPATIONS AG
Inventors:
Denis Gribkov, Myriem El Qacemi, André Stoller, André Jeanguenat, Aurelien Bigot
Abstract: The present invention relates to new pharmaceutical agents, and to their use in the treatment of proliferative diseases, such as cancer (in particular, brain cancer). In some embodiments, the present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or prodrugs thereof.
Type:
Grant
Filed:
February 1, 2019
Date of Patent:
October 18, 2022
Assignee:
THE UNIVERSITY OF SYDNEY
Inventors:
Michael Kassiou, William Jorgensen, Lenka Munoz
Abstract: Disclosed herein is a method of converting a THC-rich cannabinoid mixture that comprises at least about 20% THC into a CBN-rich cannabinoid mixture that comprises at least about 2.0% CBN. The method comprises contacting the cannabinoid mixture with a benzoquinone reagent under reaction conditions comprising: (i) a reaction temperature that is within a target reaction-temperature range; and (ii) a reaction time that is within a target reaction-time range, such that at least a portion of the of the THC in the THC-rich cannabinoid mixture is converted into CBN.
Type:
Grant
Filed:
February 22, 2022
Date of Patent:
October 18, 2022
Assignee:
Canopy Growth Corporation
Inventors:
Christopher Adair, Mahmood Azizpoor Fard, Ben Geiling, Mohammadmehdi Haghdoost Manjili
Abstract: The present disclosure relates to fungicidal active compounds, more specifically to heteroarylphenylaminoquinolines according to formula (I): and analogues thereof, processes and, intermediates for their preparation and use thereof as fungicidal active compound, particularly in the form of fungicide compositions. The present disclosure also relates to methods for the control of phytopathogenic fungi of plants using these compounds or compositions comprising thereof.
Abstract: A series of novel EHop-016 derivatives is presented herein via designing and synthesizing compounds that mimics its more favorable “U-shaped” conformation that appears to be critical for inhibitory activity against Rac. Based on modeling studies on EHop-016, compounds with a more rigid structural conformation can mimic this “U-shaped” conformation and would improve the anti-migration activity against metastatic cells. Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases, for instance compounds of formula Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.
Abstract: The present invention relates to benzimidazole and benzotriazole compounds which are of use in the field of agriculture as fungicides, wherein the compounds include benzimidazole and benzotriazole compounds having a structure according to formula 1, or an agronomically acceptable salt or N-oxide thereof:
Type:
Grant
Filed:
January 15, 2019
Date of Patent:
September 13, 2022
Assignee:
GLOBACHEM NV
Inventors:
Christopher John Urch, Victoria Elizabeth Jackson, Linda Jordan, Effi Baetzner, Oliver James Stephen McGaw