Abstract: A method of treating retinal degeneration in a subject includes administering to the subject a therapeutically effective amount of a compound of formula (I).
Type:
Grant
Filed:
September 5, 2023
Date of Patent:
March 18, 2025
Assignees:
CASE WESTERN RESERVE UNIVERSITY, UNIVERSITY OF PITTSBURGH—OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
Abstract: Disclosed herein is a specific crystalline forms of (E)-N-hydroxy-3-(1-(phenylsulfonyl) indolin-5-yl) acrylamide (ABT-301), the pharmaceutical composition and capsule comprising the same, the intermediate and the medical application thereof. Said crystalline forms of ABT-301 can exhibit unexpected stability and improved pharmacokinetic properties compared to other forms or salt thereof, thereby allowing said compound more suitable for drug development and satisfying the requirements for bioavailability and drug efficacy.
Abstract: The present invention relates to uracilpyridines of formula (I), or their agriculturally acceptable salts, wherein the variables are defined according to the description, process for preparation their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidal effective amount of at least one uracil pyridine of formula (I) to act on plants, their seed and/or their habitat.
Abstract: Disclosed herein is a method and apparatus for synthesizing co-crystals from the vapor phase without the need for liquid solvent. Also disclosed herein are co-crystals formed from the vapor phase, substrates coated with said co-crystals, pharmaceutical compositions thereof and apparatuses for producing said co-crystals.
Type:
Grant
Filed:
December 11, 2019
Date of Patent:
March 4, 2025
Assignee:
REGENTS OF THE UNIVERSITY OF MICHIGAN
Inventors:
Max Shtein, Siddharth Borsadia, Eugene Shteyn
Abstract: The present invention provides compounds used in the synthesis of chemiluminescent acridinium compounds and methods of producing these compounds. Specifically, methods are provided for the N-alkylation of acridan compounds using alkylating reagents. Typically, these alkylating reagents comprise a protected sulfonate group protected with an acid-labile protecting group.
Abstract: The invention discloses a method for synthesizing 1,7-naphthyridine derivatives, which relates to the technical field of synthesizing pharmaceutical intermediates and organic chemical intermediates, wherein the method includes: (1) 2-chloro-3-amino-pyridine being used as Compound I as a starting material, and protecting an amino group to prepare Compound II; (2) the Compound II reacting with an aldehydation reagent under alkaline conditions to obtain Compound III; (3) cyclizing the Compound III with acrylate compounds under the action of Lewis acid to prepare compound IV.
Type:
Grant
Filed:
November 17, 2020
Date of Patent:
February 25, 2025
Assignee:
ChengDa Pharmaceuticals Co., Ltd.
Inventors:
Wei Qian, Yuhua Shi, Xing Huang, Changming Dong, Junkui Dang, Zhipeng Wang, Yu Feng, Hong Xu, Zongxi Huang, Ye Chen, Huafei Shen, Jun Zhang
Abstract: The invention relates to novel crystalline solid forms of salts of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N?-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly renal cell carcinoma (RCC) and medullary thyroid cancer (MTC).
Abstract: In vitro or ex vivo methods for screening a quinoline derivative, or anyone of its pharmaceutically acceptable salt, presumed effective in treating and/or preventing an inflammatory disease, the method including: providing an eukaryotic cell, bringing into contact said cell with a quinoline derivative, measuring an expression of miR-124 in the cell, and selecting the candidate presumed effective in treating and/or preventing an inflammatory disease when the level of expression of miR-124 measured is increased relatively to a reference value.
Type:
Grant
Filed:
May 17, 2022
Date of Patent:
January 21, 2025
Assignees:
ABIVAX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE DE MONTPELLIER
Abstract: The present invention refers to oxadiazole compounds suitable as HDAC6 inhibitors. Processes for their preparation and their medical uses in treating HDAC6-related diseases or disorders are also disclosed.
Type:
Grant
Filed:
April 16, 2020
Date of Patent:
January 21, 2025
Assignees:
QUIMATRYX, S.L., FUNDACIÓN KERTOR
Inventors:
Yosu Ion Vara Salazar, Eneko Aldaba Arévalo, Tamara Bello Iglesias, Richard Spurring Roberts, Laureano Simón Buela, José Manuel Brea, Ángel Carracedo, María Isabel Loza García
Abstract: Disclosed is a 5-methylchromone and the preparation method and application thereof, the 5-methylchromone has the following structure: wherein R1 and R2 are alkyl groups. The substituted chromone has the biological activity of inhibiting tyrosinase. The preparation method uses 3,5-dihydroxytoluene as a raw material, and synthesis of chromones substituted with different groups at 2-C through acylation, esterification, rearrangement and cyclization reactions, etc. The 5-methylchromone is a completely new compound in condition that R1 is —CH2CH2CH3, and R2 is —CH2CH3, or that R1 is —C(CH3)3, and R2 is H. All the compounds have obvious inhibitory activity against tyrosinase, and can be used to prepare tyrosinase inhibitors or whitening agents.
Type:
Grant
Filed:
March 12, 2021
Date of Patent:
January 14, 2025
Assignee:
HAINAN MEDICAL UNIVERSITY
Inventors:
Youbin Li, Xuesong Wang, Yan Wang, Junyu Xu, Yu Chen, Tingting Zeng, Xue Cui, Yinfeng Tan, Jingwen Gong
Abstract: A rapid synthesis method for a biomass-based amine, including: using formamide as an amine source, formic acid as a hydrogen source, and biomass aldehyde or ketone as a raw material, conduct rapid heating promoting direct addition of formamide and aldehyde or ketone compound through microwave-assisted heating and without a solvent and catalyst, and carrying out formic acid reduction preparing and obtaining a corresponding formamide derivative; selectively converting the formamide derivative under the action of a base into a corresponding primary amine through alcoholysis.
Abstract: Described herein are polymorphic forms of a CB1 modulator, methods of making such forms, pharmaceutical compositions and medicaments comprising such forms, and methods of using such forms in the treatment of conditions, diseases, or disorders that would benefit from modulation of the CB1 receptor.
Type:
Grant
Filed:
September 20, 2023
Date of Patent:
December 31, 2024
Assignee:
Anebulo Pharmaceuticals, Inc.
Inventors:
Joseph Fenton Lawler, Daniel Pawel Schneeberger
Abstract: The present invention relates to a new intermediate, (2,2-dimethyl-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propanamide) useful in the synthesis of lasmiditan, to a method for obtaining same, to the use of said intermediate for preparing lasmiditan, to a method for preparing lasmiditan making use of said intermediate, and to a method for preparing an intermediate ((6-amino-pyridin-2-yl)-(1-methyl-piperidin-4-yl)-methanone) from (2,2-dimethyl-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propanamide).
Abstract: Disclosed herein is a tricyclic octacationic cyclophane and complexes comprising the tricyclic octacationic cyclophane and a perylene diimide dye complexed therein and methods of using and making the cyclophane and complexes.
Abstract: The present invention provides turn-ON dioxetane-based chemiluminescence probes based on the Schapp's adamantylidene-dioxetane probe, which are capable of detecting or imaging, more specifically, determining the presence, or measuring the level, of proteases, as well as compositions and uses thereof.
Abstract: The present invention relates to a method for preparing 2-alkoxy-4-amino-5-methylpyridines of the formula (I) and/or 2-alkoxy-4-alkylamino-5-methylpyridines of the formula (II) from the corresponding 2-haloaminopyridines and the appropriate alcohols in the presence of base, and to the compounds resulting therefrom.
Abstract: The present invention relates to pharmaceutical compounds of Formula (I): as further described herein, and pharmaceutical compositions containing such compounds, as well as methods of using these compounds to modulate the activity of aryl hydrocarbon receptor (AhR) and to treat conditions comprising inflammation inside the intestinal tract and certain disorders of the central nervous system affected by the gut-brain axis, including IBD, ulcerative colitis, Crohn's disease, Huntington's disease, and multiple sclerosis.
Abstract: The present invention relates to compounds of formula (I): (I) wherein Q is selected from O or S; R1 is an optionally substituted hydrocarbyl group which may optionally include one or more heteroatoms N, O or S in its carbon skeleton, provided that the hydrocarbyl group includes at least one heteroatom N, O or S in its carbon skeleton or is substituted with a substituent comprising at least one heteroatom N, O or S, and provided that the atom of R1 which is attached to the sulfur atom of the remainder of the molecule is not a ring atom of a cyclic group; R2 is an ?,??-substituted cyclic group which may optionally be further substituted; R3 and R4 are each independently hydrogen, halogen, —OH, —NH2, —CN, —R5, —OR5, —NHRs or —N(R5)2; or R3 and R4 together with the carbon atom to which they are attached may form a 3- to 7-membered saturated or unsaturated, optionally substituted cyclic group; and R5 is independently optionally substituted C1-C4 alkyl.
Type:
Grant
Filed:
March 1, 2019
Date of Patent:
December 17, 2024
Assignee:
INFLAZOME LIMITED
Inventors:
Matthew Cooper, David Miller, Jimmy Van Wiltenburg, Jonathan Shannon, Stephen St-Gallay