Abstract: The present invention provides a compound that has an excellent control effect on arthropod pests, and is represented by formula (I) [wherein Q represents a group represented by Q1, or the like, n is 0, 1, or 2, R2 represents a C1-C6 alkyl group which may optionally have one or more halogen atoms, or the like, Ya represents an oxygen atom, a sulfur atom, or NR3a, G1 represents a nitrogen atom or CR5a, G2 represents a nitrogen atom or CR5b, A2 represents a nitrogen atom or CR4a, A3 represents a nitrogen atom or CR4b, A4 represents a nitrogen atom or CR4c, and R3a, R4a, R4b, R4c, R5a, and R5b represent a C1-C6 chain hydrocarbon group or the like, and T represents a C1-C10 chain hydrocarbon group which may optionally have one or more halogen atoms, or the like].
Abstract: Defined herein are immunomodulating Formula (1) compounds wherein R, R0, R1, R2, R3 and W are as defined herein, stereoisomers thereof, and pharmaceutically acceptable salts thereof; and compositions comprising said compounds. The invention also includes methods for treating an inflammatory and/or immunological disease or disorder in an animal by administering a therapeutically effective amount of a Formula (1) compound, stereoisomer thereof, and a pharmaceutically acceptable salt thereof; or use of said compound of Formula (1) to prepare a medicament for treating an inflammatory and/or immunological disease or disorder in an animal.
Type:
Grant
Filed:
March 11, 2021
Date of Patent:
October 3, 2023
Assignee:
Zoetis Services LLC
Inventors:
Mark R. Cox, Timothy L. Stuk, Todd M. Maddux, Richard Andrew Ewin, Paul D. Johnson, Tomasz Respondek, Graham M. Kyne, Rajendran Vairagoundar
Abstract: Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2): wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.
Type:
Grant
Filed:
October 6, 2021
Date of Patent:
September 12, 2023
Assignees:
OP BIO FACTORY CO., LTD., SEED RESEARCH INSTITUTE CO., LTD.
Abstract: The present disclosure relates to a new class of antimicrobial agents. In particular, this disclosure provides the identification and characterization of novel spiro-lactam compounds as anti-HIV/AIDS and anti-malarial agents. Furthermore, this disclosure also provides the preparation of spiro-?-penicillanic acids, which proved to be potent inhibitors of HIV.
Type:
Grant
Filed:
May 14, 2018
Date of Patent:
June 6, 2023
Assignees:
UNIVERSIDADE DE COIMBRA, EGAS MONIZ—COOPERATIVA DE ENSINO SUPERIOR, CRL, INSTITUTO DE MEDICINA MOLECULAR
Inventors:
Teresa Margarida Vasconcelos Dias De Pinho E Melo, Bruna C. Suzano Santos, Inês Bártolo, Rui Miguel Prudêncio Pignatelli, Nuno Eduardo Moura Dos Santos Da Costa Taveira
Abstract: The present technology provides pyrrolidine and piperidine compounds or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. In particular, said compounds may be usefully applied in the treatment and prevention of FAP-mediated diseases.
Type:
Grant
Filed:
November 5, 2020
Date of Patent:
May 23, 2023
Assignee:
YUHAN CORPORATION
Inventors:
Tae Han Dong, Yoo Hoi Park, Tae Kyun Kim, Jae Eun Joo, Eun Hye Jung, Jae Won Jeong, Hyun Seung Lee, Do Hoon Kim, Ji Eun Yang, Jun Chui Park, Sang Myoun Lim, Na Ry Ha, Da In Chung, Ji Yeong Gal
Abstract: The present invention provides use of berbamine dihydrochloride in preparation of an Ebola virus inhibitor. In the present invention, the primed glycoprotein of the Ebola virus (EBOV-GPcl) is taken as a target site, and an antiviral active compound with the capability of binding to the EBOV-GPcl, i.e., berbamine dihydrochloride, is obtained through structure-based virtual screening. Berbamine dihydrochloride can specifically inhibit the entry of an Ebola recombinant virus by binding to the target protein EBOV-GPcl, thereby achieving the effect of anti-Ebola virus infection. The half-maximum effect concentration (EC50) of berbamine dihydrochloride against EBOV is 0.49 ?M, which indicates that berbamine dihydrochloride has a strong inhibition effect on EBOV.
Type:
Grant
Filed:
June 19, 2019
Date of Patent:
May 23, 2023
Assignee:
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences
Inventors:
Shan Cen, Quanjie Li, Dongrong Yi, Yi Shi, Han Wang, Jinming Zhou
Abstract: The present invention relates to novel active compound combinations comprising at least one known compound of the formula (I) and at least one further active compound, which combinations are highly suitable for controlling animal and microbial pests such as unwanted insects and/or unwanted acarida and/or unwanted nematodes.
Type:
Grant
Filed:
October 12, 2018
Date of Patent:
May 16, 2023
Assignee:
Bayer Aktiengesellschaft
Inventors:
Silvia Cerezo-Galvez, Christian Marienhagen, Holger Weckwert, Wolfgang Thielert, Marita John
Abstract: A method of synthesizing a clopidogrel metabolite is provided. A piperidone intermediate is formed from a mandelate. An asymmetric ketone reduction of the piperidone intermediate is performed. A mercapto installation is performed on the piperidone intermediate to form a clopidogrel metabolite that includes a 4-carbon chiral center having an (R) configuration.
Type:
Grant
Filed:
September 28, 2020
Date of Patent:
May 9, 2023
Assignee:
Board of Regents, The University of Texas System
Abstract: Disclosed are small molecule PLK inhibitors that can target the polo box domain (PBD). Inhibitors can have an atomic mass of about 1000 Da or less and a general structure of For instance, the inhibitors can include an alkyl benzamido benzoic acid core structure.
Abstract: The present invention relates to pyrimidinium compounds of formula (I), to the stereoisomers, salts, tautomers and N-oxides thereof, their mixtures and to compositions comprising such compounds or mixtures. The invention also relates to methods and uses of these pyrimidinium compounds and of compositions thereof, for combating and controlling animal pests. Furthermore, the invention relates also to pesticidal methods of applying such substituted pyrimidinium compounds. The pyrimidinium compounds of the present invention are defined by the following general formula (I): wherein R1, R2 and Het are defined as in the description.
Abstract: The present disclosure relates to: a) solid state forms of hydrobromide salts of Compound 1; b) pharmaceutical compositions comprising one or more solid state forms of hydrobromide salts of Compound 1, and, optionally, a pharmaceutically acceptable carrier; c) methods of treating tumors or cancers by administering one or more solid state forms of hydrobromide salts of Compound 1 to a subject in need thereof; and d) methods for the preparation of solid state forms of Compound 1.
Type:
Grant
Filed:
February 19, 2021
Date of Patent:
January 31, 2023
Assignee:
Pfizer Inc.
Inventors:
Elaine Greer, Stephen Anderson, Mark Maloney, Shu Yu, Ekaterina Albert, Emily Rigsbee
Abstract: The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.
Type:
Grant
Filed:
November 9, 2020
Date of Patent:
January 10, 2023
Assignee:
BAYER CROPSCIENCE AG
Inventors:
Eike Kevin Heilmann, Joerg Greul, Axel Trautwein, Hans-Georg Schwarz, Isabelle Adelt, Roland Andree, Peter Luemmen, Maike Hink, Martin Adamczewski, Mark Drewes, Angela Becker, Arnd Voerste, Ulrich Goergens, Kerstin Ilg, Johannes-Rudolf Jansen, Daniela Portz
Abstract: The present invention relates to novel active compound combinations comprising at least one known compound of the formula (I) and at least one further active compound, which combinations are highly suitable for controlling animal and microbial pests such as unwanted insects and/or unwanted acarids and/or unwanted nematodes.
Type:
Grant
Filed:
October 12, 2018
Date of Patent:
January 3, 2023
Assignee:
BAYER AKTIENGESELLSCHAFT
Inventors:
Silvia Cerezo-Galvez, Christian Marienhagen, Holger Weckwert, Wolfgang Thielert, Marita John
Abstract: Methods described herein enable the production of numerous molecular species through decarboxylative cross-coupling via use of photoredox and transition metal catalysts. For example, methods described herein enable the production of numerous molecular species through decarboxylative cross-coupling via use of photoredox and transition metal catalysts. A method described herein, in some embodiments, comprises providing a reaction mixture including a photoredox catalyst, a transition metal catalyst, a coupling partner and a substrate having a carboxyl group. The reaction mixture is irradiated with a radiation source resulting in cross-coupling of the substrate and coupling partner via a mechanism including decarboxylation, wherein the coupling partner is selected from the group consisting of a substituted aromatic compound and a substituted aliphatic compound.
Abstract: Provided is a method for treating a symptom of vibrio infection by using an RTX toxin production inhibitor comprising N-(4-oxo-4H-thieno[3,4-c]chromen-3-yl)-3-phenylprop-2-ynamide having derivatives thereof which can repress (prevent or treat) a symptom of vibrio infection by inhibiting RTX toxin production, other than directly killing vibrio bacteria, to not allow vibrio bacteria to have pathogenicity, and thereby can be an alternative to antibiotics that aim to kill bacteria themselves and thus fundamentally retain the problem of resistance incurrence.
Type:
Grant
Filed:
January 7, 2019
Date of Patent:
November 29, 2022
Assignee:
SEOUL NATIONAL UNIVERSITY R&DB FOUNDATION
Inventors:
Sang Ho Choi, Lak Shin Jeong, Ho Jae Han, Nam Chul Ha, Byoung Sik Kim, Kyung Ku Jang, Zee-Won Lee
Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CB1 receptor mediating scaffold conjugated to (ii) a second therapeutic scaffold.
Type:
Grant
Filed:
May 8, 2020
Date of Patent:
November 1, 2022
Assignee:
The United States of America, as represented by the Secretary, Department of Health and Human Services
Inventors:
George Kunos, Malliga Iyer, Resat Cinar, Kenner C. Rice
Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
Type:
Grant
Filed:
November 1, 2017
Date of Patent:
October 4, 2022
Assignee:
ARVINAS OPERATIONS, INC.
Inventors:
Andrew P. Crew, Michael Berlin, Hanqing Dong, Alexey Ishchenko
Abstract: The invention includes 2-?-naphthyl-acetic acid derivatives, which are selective AKR1C3 inhibitors. In certain embodiments, the compounds of the invention are (R)-naproxen analogs. The invention further includes methods of treating cancer, such as prostate cancer and/or castration-resistant prostate cancer, using at least one compound of the invention.
Type:
Grant
Filed:
October 21, 2016
Date of Patent:
October 4, 2022
Assignees:
THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA, VANDERBILT UNIVERSITY
Inventors:
Trevor M. Penning, Adegoke Adeniji, Lawrence J. Marnett
Abstract: The present specification relates to a heterocyclic compound represented by Chemical Formula 1, and an organic light emitting device comprising the same.
Type:
Grant
Filed:
October 1, 2018
Date of Patent:
September 6, 2022
Assignee:
LT MATERIALS CO., LTD.
Inventors:
Gi-Back Lee, Seong-Jong Park, Ji-Young Kim, Won-Jang Jeong, Jin-Seok Choi, Dae-Hyuk Choi, Joo-Dong Lee