Abstract: A method for producing an amidate compound represented by Formula (4), comprising reacting an iminium salt represented by Formula (1) and an organic compound represented by Formula (3), wherein Formulas (1), (3), and (4) are as defined in the description.
Abstract: The invention relates to specified benzamide compounds of formula (1), and pharmaceutical compositions containing the compounds. The compounds may be inducers of ?1-antitrypsin (A1AT), and may be used in the treatment of a disease or disorder such as ?1-antitrypsin deficiency (A1AD or AATD).
Type:
Grant
Filed:
June 13, 2022
Date of Patent:
May 6, 2025
Assignee:
CENTESSA PHARMACEUTICALS (UK) LIMITED
Inventors:
Nigel Ramsden, David John Fox, James Andrew Huntington, James Michael Tomlinson
Abstract: The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
Type:
Grant
Filed:
December 27, 2023
Date of Patent:
April 22, 2025
Assignee:
ARDELYX, INC.
Inventors:
Dean Dragoli, Irina Dotsenko, Jason Lewis
Abstract: Disubstituted fluoroaryloxybenzoheterodiazole compound having general formula (I): Said disubstituted fluoroaryloxybenzoheterodiazole compound having general formula (I) may be advantageously used as a spectrum converter in luminescent solar concentrators (LSCs) capable, in turn, of improving the performance of photovoltaic devices (or solar devices) selected, for example, from photovoltaic cells (or solar cells), photovoltaic modules (or solar modules), either on a rigid support, or on a flexible support.
Type:
Grant
Filed:
March 19, 2020
Date of Patent:
April 15, 2025
Assignee:
ENI S.P.A.
Inventors:
Luigi Abbondanza, Antonio Alfonso Proto, Giuliana Schimperna
Abstract: The present invention discloses a phosphine nitrogen ligand with multiple chiral centers and its synthesis method and application. The ligand has the axial chirality of a biaryl skeleton and the central chirality of a chiral amine. The chiral ligand is synthesized from commercially available raw materials through a simple five-step reaction, and the resulting diastereomer can be separated by simple column chromatography or recrystallization. The chiral phosphine nitrogen ligand synthesized by the present invention can catalyze the asymmetric three-component coupling reaction of terminal alkynes, aldehydes and amines, and realize the efficient preparation of chiral propargyl amines with high optical activity.
Type:
Grant
Filed:
May 13, 2020
Date of Patent:
April 15, 2025
Assignee:
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES
Abstract: The present invention relates to a process for the preparation of a compound (I) or pharmaceutically acceptable salt thereof, which is useful as the key intermediate for the synthesis of compounds for prophylaxis and treatment of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
Abstract: Provided are methods of producing Active Pharmaceutical Ingredient (API) grade migalastat hydrochloride, and for purifying intermediate grade migalastat hydrochloride. Further provided are methods of producing [(2R,3S,4R,5S)-1-butyl-2-(hydroxymethyl)piperidine-3,4,5-triol hydrochloride (lucerastat hydrochloride) and other 1-deoxygalactonojirimycin compounds, as well as methods of purifying intermediate grade lucerastat hydrochloride and other 1-deoxygalactonojirimycin compounds.
Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, U, W1, W2, W3, R1-R6, and R9 are described herein.
Type:
Grant
Filed:
November 9, 2023
Date of Patent:
April 15, 2025
Assignee:
FORMA Therapeutics, Inc.
Inventors:
Jian Lin, Anna Ericsson, Ann-Marie Campbell, Gary Gustafson, Zhongguo Wang, R. Bruce Diebold, Susan Ashwell, David R. Lancia, Jr., Justin Andrew Caravella, Wei Lu
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: 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: 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 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 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 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: 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: 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: 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