Abstract: The present invention presents 2-(acylamino)imidazoles with therapeutic activity, including selective activity against cancer cells, and compositions comprising them. Methods of using and preparing the 2-(acylamino)imidazoles are also presented.
Type:
Grant
Filed:
September 27, 2019
Date of Patent:
May 24, 2022
Assignees:
Curza Global, LLC, The University of Utah
Inventors:
Ryan E. Looper, Justin M. Salvant, Emily K. Kirkeby, Wenxing Guo, Katrin P. Guillen, Bryan E. Welm
Abstract: Described herein is a process for antibiotic development comprising: (a) generating a compound of formula (III): or a salt or stereoisomer or prodrug thereof; wherein R1-R3 and R5-R10 are independently selected from H, alkyl group, substituted alkyl group, halogen, OH, NH2, or SH; R4 is H, alkyl group or substituted alkyl group; X1-X2 are independently selected from ?O, ?S, ?NH, H, alkyl, halogen, OH, SH, or NH2; W is a saturated acyclic hydrocarbon chain of 1 to 15 carbon atoms; and Z is a neutral or positively charged organic group comprising a nitrogen or phosphorus atom; and; and (b) determining efficacy of the compound to inhibit growth of a bacteria. Systems of drug development of these antibiotic compounds are also described.
Type:
Grant
Filed:
July 15, 2020
Date of Patent:
May 10, 2022
Inventors:
Pavel Dibrov, Elena Dibrov, Grant Pierce
Abstract: A nitrogen-containing cyclic organoxysilane compound having a formula (1): wherein R1 is a divalent hydrocarbon group, R2 is a monovalent hydrocarbon group or an organoxy group having a formula (2): —OR4??(2) wherein R4 is a monovalent hydrocarbon group, R3 is a divalent hydrocarbon group, A is a group having a formula (3) or (4): wherein each of R5 and R6 is a monovalent hydrocarbon group, a triorganosilyl group, or the like, R7 is a monovalent hydrocarbon group or triorganosilyl group, each of R8 and R9 is a divalent carbon atom having 1 to 20 carbon atoms, and R10 is C—H or a nitrogen atom, and E is an oxygen atom, a sulfur atom, or a group having a formula (5): wherein R3 is the same as described above, each of E1 and E2 independently is an oxygen atom or a sulfur atom, and n is an integer of 1 to 10.
Abstract: Pesticidal mixtures including a pesticidally active anthranilamide compound of formula (I) and at least one further pesticidal active ingredient. The pesticidal mixtures are useful for combating and controlling insects, acarids or nematodes in and on plants, and for protecting such plants being infested with pests.
Type:
Grant
Filed:
February 9, 2017
Date of Patent:
April 12, 2022
Assignee:
BASF SE
Inventors:
Robert Reinhard, Pascal Bindschaedler, Karsten Koerber, Juergen Langewald
Abstract: The present disclosure provides methods of increasing skin pigmentation in a subject in need thereof using salt-inducible kinase (SIK) inhibitors, such as macrocyclic compounds of Formula (I), bicyclic urea compounds of Formula (II), (III), and (IV), and compounds of Formula (V), (VI), (VI-A), or (VII). Also provided are pharmaceutical compositions, methods, and uses that include or involve a compound described herein.
Type:
Grant
Filed:
February 28, 2018
Date of Patent:
March 29, 2022
Assignees:
The General Hospital Corporation, Dana-Farber Cancer Institute, Inc.
Inventors:
David E. Fisher, Nisma Mujahid, Ryo Murakami, Nathanael S. Gray, Yanke Liang, Hwan Geun Choi
Abstract: Use of the molecule with the following formula (I) for its fungicidal and/or bactericidal activity on fungi, oomycetes and/or pathogenic bacteria of plants and crop seeds.
Abstract: Compounds of the formulas which are useful as colony stimulating factor-1 receptor inhibitors (“CSF-1R inhibitors”).
Type:
Grant
Filed:
July 19, 2016
Date of Patent:
March 15, 2022
Assignee:
GENZYME CORPORATION
Inventors:
John L. Kane, Jr., Claude Barberis, Mark Czekaj, Paul Erdman, Barret Giese, Michael Kothe, Tieu-Binh Le, Jinyu Liu, Liang Ma, Markus Metz, Vinod Patel, Andrew Scholte, Patrick Wai-Kwok Shum, Linli Wei
Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.
Type:
Grant
Filed:
September 11, 2018
Date of Patent:
March 8, 2022
Assignee:
SYNGENTA PARTICIPATIONS AG
Inventors:
Farhan Bou Hamdan, Laura Quaranta, Matthias Weiss
Abstract: Compounds, compositions, and methods of use of such compounds and compositions are provided for reducing human dependency to nicotine. In one example, a method of treating an individual with an addiction to nicotine comprises administering to the individual a compound that is a structural analog of trans-cinnamaldehyde ((2E)-3-Phenylprop-2-enal): Based on the administration, a rate at which nicotine is metabolized may be reduced, which in turn may reduce a desire for the individual to consume nicotine-containing products.
Abstract: A positron emission tomography (PET) radiotracer for imaging lactate uptake, wherein the tracer is [18F]-3-fluoro-2-hydroxypropionic acid, or a pharmaceutical acceptable salt and/or solvate thereof. Also, a process for the radiosynthesis of [18F]-3-fluoro-2-hydroxypropionic acid, or a pharmaceutical acceptable salt and/or solvate thereof. Further, the use of [18F]-3-fluoro-2-hydroxypropionic acid, or a pharmaceutical acceptable salt and/or solvate thereof, for imaging lactate uptake in living cells, especially in humans.
Type:
Grant
Filed:
September 9, 2020
Date of Patent:
March 1, 2022
Assignee:
GRANDIS
Inventors:
Pierre Sonveaux, Daniel Labar, Vincent Van Hée, Gwenaël Dehon, Raphaël Frédérick
Abstract: A process for preparing glycerol carbonate methacrylate, wherein glycidyl methacrylate is reacted with carbon dioxide in the presence of a catalyst and a solvent, wherein the catalyst is potassium iodide, the solvent is acetonitrile, one or more monoalcohols, or any desired mixture of acetonitrile and one or more monoalcohols, and the reaction of glycidyl methacrylate with carbon dioxide is carried out at a pressure from 0.5 to 5 bar.
Type:
Grant
Filed:
December 7, 2018
Date of Patent:
February 22, 2022
Assignee:
BASF SE
Inventors:
Andrea Misske, Christoph Fleckenstein, Matthias Klueglein
Abstract: The present disclosure relates to a method for preparing tolimidone on large scale with maintaining high purity and uniform particle size distribution, and more specifically, a method suitable for preparing tolimidone on industrially large scale by using tetrabutyl ammonium bromide catalyst and recrystallization in ethanol, which can prepare highly pure tolimidone in a time shorter than prior arts while maintaining water content and particle size distribution constantly.
Type:
Grant
Filed:
January 11, 2018
Date of Patent:
February 22, 2022
Assignee:
BUKWANG PHARMACEUTICAL CO., LTD.
Inventors:
Kwang Ok Lee, Kyung Hwa Lee, Eun Ju Jeong
Abstract: In crop production in the fields of agriculture, horticulture and the like, the damage caused by insect pests etc. is still immense, and insect pests resistant to existing insecticides have emerged. The present invention has been made in view of such circumstances, and an object of the present invention is to develop and provide a novel agricultural and horticultural insecticide. The present invention provides a benzimidazole compound represented by the general formula (1): {wherein R1 represents a hydrogen atom or a cyano group, R2 and R3 each represent a hydrogen atom, R4 represents a hydrogen atom or a haloalkoxy group, R5 represents a haloalkoxy group, a haloalkylthio group, a haloalkylsulfinyl group, or a haloalkylsulfonyl group, and m represents 0 or 2}, or a salt thereof; an agricultural and horticultural insecticide comprising the compound or the salt as an active ingredient; and a method for using the insecticide.
Type:
Grant
Filed:
September 20, 2018
Date of Patent:
February 22, 2022
Assignee:
NIHON NOHYAKU CO., LTD.
Inventors:
Ikki Yonemura, Shunpei Fujie, Ryosuke Tanaka
Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of Cezanne 1. The invention further relates to the use of DUB inhibitors in the treatment of cancer.
Type:
Grant
Filed:
April 8, 2020
Date of Patent:
February 1, 2022
Assignee:
MISSION THERAPEUTICS LIMITED
Inventors:
Mark Ian Kemp, Martin Lee Stockley, Michael David Woodrow, Alison Jones
Abstract: Provided are a nobiletin composition having excellent solubility in water and a method for simply producing the same. A method for producing a solid dispersion containing nobiletin, the method involving a step of dissolving nobiletin or a nobiletin-containing substance and a water-soluble hesperidin derivative selected from the group consisting of glucosyl hesperidin and methyl hesperidin in an ethanol aqueous solution having an ethanol concentration of from 20 to 90 vol % and a step of drying the solution.
Abstract: Disclosed are compounds, pharmaceutical compositions, and methods of treatment. The disclosed compounds are based on fused 1,4-diazepine and pyrrolidinedione scaffolds.
Abstract: The present disclosure relates to modified nucleoside reverse transcriptase inhibitors (NRTIs), such as and compositions thereof, as well as methods useful for treating retinal damage and/or retinal degradation/retinal degeneration, for inhibiting inflammasome activation by Alu RNA associated with a cell, for reducing ATP-induced permeability of a cell, for reducing an amount of mitochondrial reactive oxygen species in a cell, and for reducing an amount of mitochondrial reactive oxygen species in a cell.
Type:
Grant
Filed:
March 22, 2019
Date of Patent:
January 11, 2022
Assignee:
University of Kentucky Research Foundation
Inventors:
Jayakrishna Ambati, Benjamin Fowler, Kameshwari Ambati
Abstract: The present invention relates to a novel process for preparing and isolating 3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide (Isotianil), which can be used as an active compound with microbicidal properties, wherein the amount of waste materials—e.g. solvents and diluents—is significantly reduced and the process meets the requirements of industrial scale production, in particular that it provides the product in high yield, high purity, i.e. minimum amount of by-products and impurities, and can be carried out with tolerable corrosivity in industrial scale metal, in particular stainless steel, vessels or Cr—Ni—Mo alloy pressure filters or centrifuges.
Type:
Grant
Filed:
June 11, 2018
Date of Patent:
January 11, 2022
Assignee:
BAYER AKTIENGESELLSCHAFT
Inventors:
Taraneh Farida, Martin Littmann, Daniel Hartmann, Kyra Larissa Pabst, Ali Sanli
Abstract: The present invention relates to compounds of formula (I): wherein the variables have the meaning defined in the Specification. The compounds according to the present invention are useful for therapy and/or prophylaxis in a mammal, and in particular to spiro bicyclic compounds, pharmaceutical composition comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, myelodysplastic syndrome (MDS) and diabetes.
Type:
Grant
Filed:
September 13, 2017
Date of Patent:
January 11, 2022
Assignee:
Janssen Pharmaceutica NV
Inventors:
Patrick Rene Angibaud, Vineet Pande, Barbara Herkert, Daniel Jason Krosky, Olivier Alexis Georges Querolle, Aaron Nathaniel Patrick, Isabelle Noelle Constance Pilatte
Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to salts of (Z)-5-((Z)-3-chloro-4-((R)-2,3-dihydroxypropoxy)benzylidene)-2-(propylimino)-3-(o-tolyl)thiazolidin-4-one.