Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
Type:
Grant
Filed:
March 10, 2022
Date of Patent:
April 1, 2025
Assignee:
VALO HEALTH, INC.
Inventors:
Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin
Abstract: This invention relates the use of cortisol blockers (e.g., glucocorticoid receptor [GR] antagonists) for the treating or preventing viral infections, treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.
Type:
Grant
Filed:
October 31, 2022
Date of Patent:
April 1, 2025
Assignee:
Pop Test Oncology LLC
Inventors:
Randice Lisa Altshul, Neil David Thiese, Andreas J. Kesel, Myron Rapkin, Rebecca O'Brien, Anthony Arment
Abstract: Heterocyclic compounds useful as antagonists of adenosine receptors, and methods of treatment of diseases using antagonists of adenosine receptors are disclosed herein. Also disclosed herein are pharmaceutical compositions and methods of administration of heterocyclic antagonists of adenosine receptors and processes for producing heterocyclic antagonists of adenosine receptors.
Abstract: The present invention relates to compounds having a structure of general formula (I), processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in humans and warm-blooded animals.
Type:
Grant
Filed:
September 3, 2019
Date of Patent:
March 25, 2025
Assignees:
Univerza v Ljubljani, Szegedi Biológiai Kutatóközpont
Inventors:
Tihomir Tomašič, Nace Zidar, Martina Durcik, Janez Ilaš, Anamarija Zega, Cristina Durante Cruz, Päivi Tammela, Csaba Pál, Ákos József Nyerges, Danijel Kikelj, Lucija Peterlin Mašič
Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
Inventors:
Koen Vandyck, Dorothée Alice Marie-Eve Bardiot, Pierre Jean-Marie Bernard Raboisson, Leonid Beigelman, Antitsa Dimitrova Stoycheva, Sandro Boland, Arnaud Didier Marie Marchand
Abstract: The present invention provides compounds useful as inhibitors of TIR NADase activity, compositions thereof, and methods of using the same. The present invention is useful for inhibition of TIR-domain NADase activity and/or treating microbial infection and/or modulating microbial physiology.
Type:
Grant
Filed:
November 29, 2022
Date of Patent:
March 11, 2025
Assignee:
Washington University
Inventors:
Jeffrey D. Milbrandt, Aaron DiAntonio, Kow Essuman, Xianrong Mao, Yo Sasaki, Dan Summers
Abstract: Disclosed are compounds of Formula (I?), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
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: 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: 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: 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.