Abstract: The present invention pertains to a medicament for preventing or treating cough, including, as an active ingredient, a compound having P2X4 receptor antagonistic action, a tautomer, stereoisomer, or pharmaceutically acceptable salt of the compound, or a hydrate or solvate thereof.
Abstract: Disclosed are various synthetic methods to prepare structural analogs of largazole and derivatives thereof. One structural analog is an amide isostere of largazole. Another structural analog replaces the thiazole ring of largazole with a pyridine moiety or an oxazole moiety. Also disclosed are various intermediate compounds obtained when preparing structural analogs of largazole and derivatives thereof, including macrocycle analogs having an alcohol functionality.
Type:
Grant
Filed:
December 16, 2021
Date of Patent:
February 18, 2025
Assignees:
COLORADO STATE UNIVERSITY RESEARCH FOUNDATION, CETYA THERAPEUTICS, INC.
Inventors:
Robert M. Williams, Sivanagireddy Koti, Subhadip De, Anil M. Shelke, Ryan E. Cerbone, Nobuyoshi Yasuda
Abstract: A method for producing a halogenated zinc phthalocyanine pigment includes a step of forming a halogenated zinc phthalocyanine crude pigment into a pigment. The halogenated zinc phthalocyanine crude pigment is obtained by depositing a halogenated zinc phthalocyanine, which is synthesized by using a compound that generates an acid by reacting with water, and the aforementioned step includes a pretreatment step of dry-crushing the halogenated zinc phthalocyanine crude pigment by using an attritor and then washing the dry-crushed halogenated zinc phthalocyanine crude pigment with water.
Abstract: The present invention provides compounds of Formula I?, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer).
Inventors:
Henry Yu, Michael Clark, Guy Bemis, Michael Boyd, Kishan Chandupatla, Philip Collier, Hongbo Deng, Huijun Dong, Warren Dorsch, Russell R. Hoover, Mac Arthur Johnson, Jr., Shashank Kulkarni, Marina Penney, Steven Ronkin, Darin Takemoto, Qing Tang, Nathan D. Waal, Tiansheng Wang, David J. Lauffer, Pan Li
Abstract: The present invention provides a compound having the basic structure shown by Formula (I) in which the indole ring and the pyrazolopyridine structure is bound through a substituent, a salt thereof or a solvate of either the compound or a salt of the compound, as well as a preventative agent or a therapeutic agent for non-insulin-dependent diabetes mellitus (Type 2 diabetes) or obesity containing such compound, salt or solvate as an active ingredient.
Abstract: The present disclosure provides antibody-drug conjugate (ADC) structures, which include a camptothecine or a camptothecine derivative linked to a polypeptide (e.g., an antibody) through a linker. The disclosure also encompasses compounds and methods for production of such conjugates, as well as methods of using the conjugates.
Type:
Grant
Filed:
December 22, 2022
Date of Patent:
January 7, 2025
Assignee:
R.P. Scherer Technologies, LLC
Inventors:
Stepan Chuprakov, Ayodele O. Ogunkoya, Penelope M. Drake
Abstract: Disclosed is an advancement in provoked chemical cleavage. Thereby the invention provides the use of a diene as a chemically cleavable group attached to a Construct, and the use of a dienophile to provoke the release of the Construct by allowing the diene to react with a dienophile capable of undergoing an inverse electron demand Diels Alder reaction with the diene. The invention includes a kit for releasing a Construct CA bound to a Trigger TR, the kit having a tetrazine and a dienophile, wherein the Trigger is the tetrazine. The invention also includes the use of the formation of a pyridazine by reacting a tetrazine having a Construct CA bound thereto and a dienophile, as a chemical tool for the release, in a chemical, biological or physiological environment, of the Construct.
Type:
Grant
Filed:
September 20, 2022
Date of Patent:
January 7, 2025
Assignee:
Tagworks Pharmaceuticals B.V.
Inventors:
Marc Stefan Robillard, Wolter Ten Hoeve, Freek Johannes Maria Hoeben, Ronny Mathieu Versteegen, Henricus Marie Janssen, Arthur Henry Antoon Marie Van Onzen, Raffaella Rossin
Abstract: The present invention is directed to derivatives of aceclidine. The present invention is further directed to ophthalmological compositions comprising a therapeutically effective amount of a compound of the present invention and one or more pharmaceutically acceptable excipients. The present invention is further directed to a methods of treating presbyopia or glaucoma or reducing hyperemia comprising administering to a patient in need thereof a therapeutically effective amount of a compound of the present invention.
Abstract: Provided herein are alpha5-containing GABAA receptor agonists and pharmaceutical compositions and methods of treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders using them.
Type:
Grant
Filed:
August 2, 2023
Date of Patent:
December 31, 2024
Assignee:
UWM Research Foundation, Inc.
Inventors:
James M. Cook, Guanguan Li, Michael Ming-Jin Poe, Miroslav M. Savic, Etienne Sibille
Abstract: This discloses that compounds of Formula 1 have antifibrotic properties. In particular, this discloses a pharmaceutical composition including one or more compounds of Formula 1 and methods of using compounds of Formula 1 in fibrosis treatment and inhibiting type 1 collagen synthesis.
Type:
Grant
Filed:
November 22, 2022
Date of Patent:
December 31, 2024
Assignees:
Florida State University Research Foundation, Inc., The Florida International University Board of Trustees
Abstract: The present invention relates to methods of treating a human patient suffering from brain injury. These method may comprise (starting) administering to a selected patient within a time period of ?12 hours or within a time period of >12 hours after the occurrence of the brain injury a therapeutically effective amount of a biopterin compound such as 4-Amino-(6R,S)-5,6,7,8-tetrahydro-L-biopterin. The invention also relates to methods of increasing the value of the extended Glasgow Outcome Scale (eGOS) of patients suffering from brain injury, thereby improving the condition of the patient.
Abstract: The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof. The compounds, compositions, methods and kits of the invention are particularly useful for the treatment of itch and other dermal conditions.
Type:
Grant
Filed:
March 10, 2021
Date of Patent:
December 10, 2024
Assignee:
Nocion Therapeutics, Inc.
Inventors:
Bridget McCarthy Cole, James Lamond Ellis
Abstract: The present invention discloses a 1,4-sulfur-bridged polycyclic compound containing dihydrobenzofuran structure which has a structural formula (I). A preparation method is also disclosed which includes the steps of: dissolving 2-nitrobenzofuran (II) and 5H-thiazolone (III) in an organic solvent; then adding molecular sieve and chiral catalyst, stirring and allowing reaction at room temperature under argon protection until the reaction is completed; and carrying out separation and purification to obtain a 1,4-sulfur-bridged polycyclic compound (I) containing dihydrobenzofuran structure. The polycyclic compounds of the present invention have a substructure of dihydrobenzofuran and 1,4-thiopiperidinone. The application of the compound for the preparation of antitumor drugs is also disclosed, which has a good potential value in antitumor drug research. The preparation method has the advantages of novelty, simplicity, simple operation, mild reaction conditions, high yield and high stereoselectivity, and etc.
Abstract: Compounds of formula (I), wherein A, R, W, Q, n, and m have the meaning according to the claims, can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
Type:
Grant
Filed:
December 15, 2021
Date of Patent:
December 3, 2024
Assignee:
Asceneuron SA
Inventors:
Anna Quattropani, Santosh S. Kulkarni, Awadut Gajendra Giri
Abstract: The present disclosure relates generally to compounds and compositions, intermediates, processes for their preparation, and their use as kinase inhibitors.
Type:
Grant
Filed:
October 26, 2021
Date of Patent:
October 29, 2024
Assignee:
DENALI THERAPEUTICS INC.
Inventors:
Javier de Vicente Fidalgo, Anthony A. Estrada, Jianwen A. Feng, Brian Fox, Cinzia Maria Francini, Christopher R. H. Hale, Cheng Hu, Colin Philip Leslie, Maksim Osipov, Elena Serra, Zachary K. Sweeney, Arun Thottumkara
Abstract: The aim of the present invention is to provide a method capable of producing an optically active pyrimidinamide derivative on an industrial scale. Compound (I) or a salt thereof is subjected to an asymmetric reduction reaction, the obtained compound (II) or a salt thereof is subjected to a deprotection reaction, and the obtained compound (III) or a salt thereof is reacted with compound (VI) or a salt thereof to obtain compound (V) or a salt thereof. wherein each symbol is as defined in the specification.
Abstract: Methods of treating a patient having an organic acidemia or a defect in mitochondria chain oxidation are provided. The methods comprise treating the patient with an effective amount of a mitochondria-targeting reactive oxygen species scavenger.
Type:
Grant
Filed:
December 23, 2021
Date of Patent:
October 29, 2024
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
Gerard Vockley, Peter Wipf, Al-Walid A. Mohsen