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
Abstract: The invention is directed to a method of treatment for inflammation in mammals including inflammation caused by bacterial or viral infection, the method comprising administering to a mammal, including a human, in need of such treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
August 19, 2020
Date of Patent:
August 30, 2022
Assignee:
MediSynergics, LLC
Inventors:
Dennis Michael Godek, Harry Ralph Howard, Andrew Morgan Stewart
Abstract: The present invention provides tools and methods for the systematic analysis of genetic interactions between cells. The present invention provides tools and methods for modulating cell phenotypes and compositions, combinatorial probing of cellular circuits, for dissecting cellular circuitry, for delineating molecular pathways, and/or for identifying relevant targets for therapeutics development.
Type:
Grant
Filed:
March 17, 2017
Date of Patent:
August 30, 2022
Assignee:
Massachusetts Institute of Technology
Inventors:
Alexander K. Shalek, Alexander S. Genshaft, Carly G. K. Ziegler, Jeffrey F. Van Humbeck
Abstract: The present invention relates to novel fused bicyclic heterocycle derivatives of formula (I) in which B1, B2, B3, B4, R1, R4, R5, R6 and n have the meanings mentioned above, to agrochemical formulations comprising the compounds of formula (I) and to their use as acaricides and/or insecticides for controlling animal pests, especially arthropods and in particular insects and arachnids.
Abstract: Disclosed are compounds, for example, compounds of formula I, wherein R, R0, R1-R8, n, X, Y, Y?, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.
Type:
Grant
Filed:
March 30, 2020
Date of Patent:
August 9, 2022
Assignee:
ADT PHARMACEUTICALS, LLC
Inventors:
Gary A. Piazza, Xi Chen, Adam B. Keeton, Michael R. Boyd
Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicycloheteroaryl-heteroaryl-benzoic acid compounds of the following formula (for convenience, collectively referred to herein as “BHBA compounds”), which, inter alia, are (selective) retinoic acid receptor beta (RAR?) (e.g., RAR?2) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RAR? (e.g., RAR?2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RAR? (e.g., RAR?2), that are ameliorated by the activation of RAR? (e.g., RAR?2), etc., including, e.g., neurological injuries such as spinal cord injuries.
Type:
Grant
Filed:
August 19, 2020
Date of Patent:
August 2, 2022
Inventors:
Alan David Borthwick, Mark Trevor Mills, Jane Theresa Brown, Jonathan Patrick Thomas Corcoran, Maria Beatriz De Castro Vasconcelos Goncalves, Sarkis Barret Kalindjian
Abstract: A method of preventing and/or treating disease in which reactive oxygen species (or ROSs) of mitochondrial origin are involved. The method involves use of an inhibitor of mitochondrial ROS production, in particular, of anethole trithione, for the prevention and/or treatment of benign prostatic hyperplasia.
Abstract: Disclosed are inhibitors of mevalonate pathway as an efficient vaccine adjuvant and use thereof. In particular, the inhibitor is an acetoacetyl-CoA transferase inhibitor, a HMG-CoA synthase inhibitor, a HMG-CoA reductase inhibitor, a mevalonate kinase inhibitor, a phosphomevalonate kinase inhibitor, a mevalonate-5-pyrophosphate decarboxylase inhibitor, an isopentenyl pyrophosphate isomerase inhibitor, a farnesyl pyrophosphate synthase inhibitor, a geranylgeranyl pyrophosphate synthase inhibitor or a geranylgeranyl transferase (I, II) inhibitor. Also disclosed is an immunogenic composition comprising inhibitors of mevalonate pathway as an adjuvant.
Abstract: The present invention relates to spirobifluorene compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices, and to electronic devices which comprise these compounds.
Type:
Grant
Filed:
April 7, 2020
Date of Patent:
July 12, 2022
Assignee:
MERCK PATENT GMBH
Inventors:
Elvira Montenegro, Amir Hossain Parham, Philipp Stoessel, Teresa Mujica-Fernaud, Frank Voges, Arne Buesing
Abstract: This invention relates to a process for preparing (±)-2-exo-(2-Methylbenzyloxy)-1-methyl-4-iso-propyl-7-oxabicyclo[2.2.1]heptane of the formula (I) any of its individual enantiomers or any non-racemic mixture thereof, comprising the step of reacting (±)-2-exo-hydroxy-1-methyl-4-isopropyl-7-oxabicyclo[2.2.1]heptane of the formula (II) any of its individual enantiomers or any non-racemic mixture thereof with a 2-Methylbenzyl compound of the formula (III) wherein X is a leaving group, in the presence of at least one base, at least one catalyst selected from rubidium salts, cesium salts and any combination thereof and at least one inert organic solvent S1.
Type:
Grant
Filed:
March 23, 2018
Date of Patent:
July 12, 2022
Assignee:
BASF AGRO B.V.
Inventors:
Stefan Benson, Michael Rack, Christiane Alznauer, Roland Goetz, Bernd Wolf