Abstract: This invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof, in which R-groups R1 to R23, A, Q, U, V, W, X, Y, Z, n, p and q are as defined herein, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject.
Type:
Grant
Filed:
December 7, 2021
Date of Patent:
August 5, 2025
Assignee:
Pfizer Inc.
Inventors:
Ping Chen, Sujin Cho-Schultz, Judith Gail Deal, Gary Michael Gallego, Mehran Jalaie, Robert Steven Kania, Sajiv Krishnan Nair, Sacha Ninkovic, Suvi Tuula Marjukka Orr, Cynthia Louise Palmer
Abstract: A method of phytosanitary treatment, which includes the step of administering a nematicidal composition, is disclosed. The nematicidal composition includes cinnamic aldehyde and terpene alcohol as active ingredients as a nematicide in a phytosanitary treatment, particularly in crops of banana, plantain, table and wine grapes, fruit trees, citrus plants, strawberries, and soy. Main advantages of the invention include high efficacy against nematodes, great stability over time, and the very low toxicity of the composition, both for plants and humans.
Type:
Grant
Filed:
November 20, 2019
Date of Patent:
July 29, 2025
Assignee:
DESARROLLO AGRICOLA Y MINERO, S.A.
Inventors:
Carlos Solans Artigas, Maria De Los Angeles Lario Carraminana, Eitan Martin Oro, David Bernad Viamonte
Abstract: A new and improved method for preparing maxacalcitol and an intermediate therefor is provided. The method is an efficient and cost-effective process for preparing maxacalcitol and an intermediate therefor.
Type:
Grant
Filed:
November 26, 2020
Date of Patent:
July 8, 2025
Assignee:
YONSUNG FINE CHEMICAL CO., LTD.
Inventors:
Seung Woo Kim, Se Gyo Jung, In A Jung, Hyunik Shin
Abstract: There is disclosed a method of preparing a compound of Formula (1), or a salt thereof (1) the method comprising: a) treating a compound of Formula (2) sequentially with o-tolylmagnesium chloride, N-methylpiperazine and iodine, under conditions sufficient to obtain a compound of Formula (3) b) treating the compound of Formula (3) from step a) with 3,5-bis(trifluoromethyl)benzyl bromide and a suitable base, under conditions sufficient to obtain a compound of Formula (1).
Abstract: The present invention provides novel triazolopyrimidines derived from nucleobase thymine, and methods of producing the same, as well as various biologically active substances obtained by the methods, particularly antitumor agents. The triazolopyrimidine compounds represented by the following formulas (I) to (VIII) (wherein R represents a hydrogen atom, an alkyl group, or an aryl group) and methods of producing the same.
Abstract: Some embodiments of the invention provide compounds having the general formula I: wherein R1, R2, R3a and R3b are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.
Abstract: A compound of formula (I) or (Ia), or a tautomer or a pharmaceutically acceptable salt thereof is provided. Compounds of formula (II) to (V), or a tautomer or a pharmaceutically acceptable salt thereof are also provided. These compounds and the pharmaceutical compositions containing them are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.
Abstract: A pharmaceutically acceptable salt of an acyclic nucleotide phosphoramidate to treat HPV and related conditions including neoplasia, as well as pharmaceutical compositions, morphic forms and dosage forms thereof.
Type:
Grant
Filed:
October 31, 2023
Date of Patent:
June 17, 2025
Assignee:
Antiva Biosciences, Inc.
Inventors:
Barry Aldous, Ramakrishna Gadiraju, Ankush Argade, Zhengle Zhao, Siyi Jiang, Runyan Li, Chao Liu, Minyan Liu
Abstract: The present invention relates to compound according to Formula I: or a pharmaceutically acceptable salt thereof, or a solvate or the salt of a solvate thereof, pharmaceutical compositions comprising the same, and methods of treatment using the same, for use in the treatment of psoriatic arthritis, by administering the compound according to Formula I.
Abstract: This invention, in at least some embodiments, relates to an inventive molecule, compositions comprising same, and methods of use thereof for treatment of a neurological disorder.
Type:
Grant
Filed:
August 24, 2021
Date of Patent:
May 27, 2025
Assignee:
GLIAPHARM SA
Inventors:
Sylvain Lengacher, Charles Finsterwald, Pierre Magistretti
Abstract: The embodiment of the present disclosure provides a method for preparing a boron dipyrromethene (BODIPY) derivative and an application of the BODIPY derivative. The method comprises: 1) taking BODIPY-1, diphenylacetylene, copper acetate monohydrate, anhydrous sodium carbonate, and metal catalyst, and dispersing the BODIPY-1, the diphenylacetylene, the copper acetate monohydrate, the anhydrous sodium carbonate, and the metal catalyst in an organic solvent for carrying out a cyclization reaction to obtain a cyclization product mixture; 2) rotary evaporating the cyclization product mixture to obtain a concentrated solution of a reaction system; 3) purifying the concentrated solution of the reaction system by a column chromatography, continuing to rotary evaporate a purified product, and then drying a product after the rotary evaporating to obtain a photocatalytic material BODIPY-2.
Type:
Grant
Filed:
November 14, 2022
Date of Patent:
May 13, 2025
Assignee:
SHAANXI UNIVERSITY OF SCIENCE & TECHNOLOGY
Abstract: The present invention provides methods for treating a cancer in a subject and for inhibiting tumor growth, metastasis or a dihydrorotate oxygenase enzyme activity of a tumor or cancer cell. At least one trisubstituted benzotriazole derivative with the formula (I) is administered to the subject or is contacted with the cancer cell. Compounds of formula (I) have substituents R1, R2 and R3 which have the meanings given in the specification, and pharmaceutically acceptable salts thereof.
Abstract: Described herein are compounds having Formula I or Formula II: wherein each dashed line independently represents a saturated or unsaturated bond; R1 and R?1 are aryl or heteroaryl as defined herein; and R2 and R?2 are as defined herein. Further described is a method of inhibiting nuclear translocation of ERK1/2 in a cell, by contacting the cell with a compound having Formula I or Formula II. The compounds may also be for use in treating a disease or disorder associated with nuclear translocation of ERK1/2.
Type:
Grant
Filed:
June 3, 2021
Date of Patent:
April 29, 2025
Assignees:
Yeda Research and Development Co. Ltd., Universitat de Barcelona, Institució Catalana de Recerca I Estudis Avançats
Abstract: The present disclosure provides compositions and methods for treating endometrial growth disorders in a patient, such as a human patient, and particularly pre-menopausal female human patients. Exemplary disorders that may be treated using the compounds and therapeutic regimens described herein include adenomyosis and rectovaginal endometriosis. The compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others.
Abstract: This invention, in at least some embodiments, relates to an inventive molecule, compositions comprising same, and methods of use thereof for treatment of a neurological disorder.
Type:
Grant
Filed:
August 24, 2021
Date of Patent:
April 15, 2025
Assignee:
GLIAPHARM SA
Inventors:
Sylvain Lengacher, Charles Finsterwald, Pierre Magistretti
Abstract: Disclosed herein are compositions and methods for topical delivery of mTOR inhibitors. In one embodiment, an anhydrous composition includes one or more mTOR inhibitors, one or more solvents, one or more gelling agents, and one or more antioxidants. Also disclosed herein are methods to treat skin disorders using such compositions.
Type:
Grant
Filed:
August 31, 2021
Date of Patent:
April 8, 2025
Assignee:
PALVELLA THERAPEUTICS, INC.
Inventors:
Wesley Harton Kaupinen, Braham Shroot, Simon David Betson, Charles Rodney Greenaway Evans, Marc Barry Brown
Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
Type:
Grant
Filed:
October 22, 2021
Date of Patent:
April 1, 2025
Assignee:
CYTOKINETICS, INCORPORATED
Inventors:
Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Todd Tochimoto, David J. Morgans, Jr., Erica Anne Kraynack
Abstract: The present disclosure provides a class of compounds including a ligand moiety that specifically binds to a cell surface asialoglycoprotein receptor (ASGPR). The cell surface ASGPR binding compounds can trigger the receptor to internalize into the cell a bound compound. The ligand moieties of this disclosure can be linked to a variety of moieties of interest without impacting the specific binding to, and function of, the cell surface receptor ASGPR. Also provided are compounds that are conjugates of the ligand moieties linked to a biomolecule, such as an antibody, which conjugates can harness cellular pathways to remove specific proteins of interest from the cell surface or from the extracellular milieu. Also provided herein methods of using the conjugates to target a polypeptide of interest for sequestration and/or lysosomal degradation.
Type:
Grant
Filed:
April 14, 2023
Date of Patent:
March 25, 2025
Assignee:
Lycia Therapeutics, Inc.
Inventors:
Brett Bradley Busch, Justin Thomas Ernst, Garrick K. Packard, Jason G. Lewis, Eric D. Turtle
Abstract: The present invention relates to 1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives and related compounds of Formula (I): wherein A, B, G, R1, R1b, RiC, R2 and X are as defined herein. The present compounds are vasopressin receptor antagonists (in particular of the Via receptor) for the treatment of neuro-psychological disorders, such as e.g. autism, anxiety, stress-related disorders, depression, schizophrenia or bipolar disorder. The present description discloses the synthesis of exemplary compounds, as well as pharmacological data thereof (e.g. pages 71 to 246; examples 1 to 49; tables 1 to 5). An exemplary compound is e.g. 8-chloro-1-(2-(5-fluoropyridin-2-yl)-2,6-diazaspiro[3.3]heptan-6-yl)-5-methyl-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine (example 1, compound no. 1).
Abstract: The present disclosure pertains to a pharmaceutical composition comprising fursultiamine or a salt thereof for prevention or treatment of macular degeneration. Fursultiamine decreases the upregulated expression of HIF-1? in retinal pigment epithelial cells and suppresses the growth of choroidal vascular endothelial cells. The pharmaceutical composition comprising fursultiamine or salts thereof according to the present disclosure can be used as a therapeutic agent for various neovascular ocular diseases.
Type:
Grant
Filed:
October 30, 2019
Date of Patent:
March 4, 2025
Assignee:
KYUNGPOOK NATIONAL UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION