Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.
Type:
Grant
Filed:
July 11, 2023
Date of Patent:
April 1, 2025
Assignee:
Tetra Discovery Partners
Inventors:
Mark E. Gurney, Timothy J. Hagen, Xuesheng Mo, A. Samuel Vellekoop, Donna L. Romero, Robert Campbell, Joel R. Walker, Lei Zhu
Abstract: Described herein is a process for the preparation of a compound of Formula I, wherein R1 and R2 each have the meanings provided in the description. Also described is a process for the preparation of pharmaceutically-active compounds including the process for the preparation of compounds of Formula I.
Abstract: The present disclosure provides compounds which are useful for a number of catalytic transformations of organic molecules, non-limiting examples including dehydrogenation of alkanes. The present disclosure further relates to methods of preparing the compounds of the present disclosure.
Type:
Grant
Filed:
April 22, 2024
Date of Patent:
April 1, 2025
Assignee:
Rutgers, The State University of New Jersey
Abstract: The present disclosure provides CDK9 inhibitors. Also provided are methods of treating a disease or a disorder comprising administering to a subject in need of treatment one of the CDK9 inhibitors disclosed herein. In some embodiments, the disease or disorder to be treated is cancer. In some embodiments, the disease or disorder is liver cancer.
Type:
Grant
Filed:
January 17, 2023
Date of Patent:
April 1, 2025
Assignee:
Algen Biotechnologies, Inc.
Inventors:
Andrei W. Konradi, Chun-Hao Huang, Ko-Chuan Lee
Abstract: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3, R4, R6, R7, R8 and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates, tautomers or stereoisomers thereof, wherein R1, R2, R2a, R3, Ra2, Ra4, Ra5, Ra6, Ra7, X1, X1a, A1 and A2 have the meaning as indicated in the description and claims. The invention further relates to pharmaceutical compositions comprising said compounds, their use as medicament and in a method for treating and preventing of one or more diseases or disorders associated with integrated stress response.
Type:
Grant
Filed:
April 22, 2020
Date of Patent:
March 25, 2025
Assignee:
Evotec International GmbH
Inventors:
Holly Atton, Christopher John Brown, James Lindsay Carr, Serge Convers-Reignier, Michael Corr, Marissa Flower, Christopher Francis Palmer, Irena Reboule, Mohamad Sabbah, Scott Sadler, Jonathan Shine, Daryl Simon Walter
Abstract: The present invention provides stapled polypeptides of the Formulae (I) and (VI): and salts thereof; wherein the groups ; R1a, R1b, R1c, R2a, R3a, R2b, R3b, R4a, R4b, RA, RZ, L1a, L1b, L2, L3, XAA, v, w, p, m, s, n, t, and q are as defined herein. The present invention further provides methods of preparing the inventive stapled polypeptides from unstapled polypeptide precursors. The present invention further provides pharmaceutical compositions comprising a stapled polypeptide of Formula (I) or (VI), and methods of using the stapled peptides. The present invention also provides modifications of the staples post ring closing metathesis.
Type:
Grant
Filed:
November 17, 2020
Date of Patent:
March 25, 2025
Assignee:
PRESIDENT AND FELLOWS OF HARVARD COLLEGE
Abstract: Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-?.
Type:
Grant
Filed:
September 1, 2023
Date of Patent:
March 4, 2025
Assignee:
EDGEWISE THERAPEUTICS, INC.
Inventors:
Kevin Hunt, Kevin Koch, Alan Russell, Stephen Schlachter, Paul Winship, Chris Steele
Abstract: The invention discloses use of miloxacin in the preparation of medicines for treating and/or preventing diseases with T-type calcium channel as a therapeutic target. The invention discloses new use of miloxacin, which provides a new theoretical and technical support for developing medicines for treating and/or preventing diseases with T-type calcium channel as a therapeutic target, thus having a broad prospect of application in the field of clinical treatment.
Type:
Grant
Filed:
February 20, 2021
Date of Patent:
March 4, 2025
Assignee:
SOOCHOW UNIVERSITY
Inventors:
Jin Tao, Yuan Zhang, Yufang Sun, Xinghong Jiang
Abstract: The present invention discloses salts of a Compound 1: useful in the prophylaxis and/or treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving degradation and/or disruption of cartilage homeostasis, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.
Type:
Grant
Filed:
April 25, 2023
Date of Patent:
February 25, 2025
Assignee:
ALFASIGMA S.P.A.
Inventors:
Nicolas Luc Sabourault, Carla De Faveri, Ahmad Sheikh, Piet Wigerinck
Abstract: The post-translational modification (PTM) and signaling molecule poly(ADP-ribose) (PAR) has an impact on diverse biological processes. PTM is regulated by a series of ADP-ribosyl glycohydrolases (PARG enzymes) that cleave polymers and/or liberate monomers from their protein targets. Disclosed herein is a substrate for monitoring PARG activity, TFMU-ADPr, which directly reports on total PAR hydrolase activity via release of a fluorophore; this substrate has excellent reactivity, generality, stability, and usability. A second substrate, TFMU-IDPr, selectively reports on PARG activity only from the enzyme ARH3. Use of these probes in whole-cell lysate experiments has revealed a mechanism by which ARH3 is inhibited by cholera toxin. TFMU-ADPr and TFMU-IDPr are versatile tools for assessing small-molecule inhibitors in vitro and probing the regulation of ADP-ribosyl catabolic enzymes.
Type:
Grant
Filed:
September 9, 2019
Date of Patent:
February 25, 2025
Assignee:
The Board of Trustees of the University of Illinois
Abstract: Disclosed are fused imidazole derivatives, preparation methods therefor and medical uses thereof. Specifically, the present disclosure relates to a fused imidazole derivative as shown in general formula (IM), a preparation method therefor, a pharmaceutical composition containing the derivative, and the use of same as a therapeutic agent, in particular the use thereof as a GLP-1 receptor agonist, and the use thereof in the preparation of drugs for the treatment and/or prevention of diabetes.
Abstract: The present invention relates to substituted pyrrolopyridinones and substituted pyrazolopyridinones which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
Abstract: Disclosed herein are pharmaceutical compositions to treat or prevent obesity, excess or overweight conditions, and metabolic syndrome comprising an effective amount of one or more mTOR inhibitors and optionally an effective amount of one or more thyroid hormones and/or an effective amount of one or more cholesterol-lowering agents. Further disclosed herein are methods of treating or preventing obesity, excess or overweight conditions, and metabolic syndrome comprising administering an effective amount of a pharmaceutical composition comprising one or more mTOR inhibitors and optionally an effective amount of one or more thyroid hormones and/or an effective amount of one or more cholesterol-lowering agents.
Abstract: The present invention is directed to pro drugs of 2-methyl-N-((5-methyl-1,3,4-thiadiazol-2-yl)methyl)-6-(((1S,2S)-2-(5-methylpyridin-2-yl)cyclopropyl)methoxy)pyrimidin-4-amine which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
Type:
Grant
Filed:
December 13, 2023
Date of Patent:
February 4, 2025
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Sachin Mittal, Jason W. Skudlarek, Izzat T. Raheem
Abstract: Disclosed are fused imidazole derivatives, preparation methods therefor and medical uses thereof. Specifically, the present disclosure relates to a fused imidazole derivative as shown in general formula (IM), a preparation method therefor, a pharmaceutical composition containing the derivative, and the use of same as a therapeutic agent, in particular the use thereof as a GLP-1 receptor agonist, and the use thereof in the preparation of drugs for the treatment and/or prevention of diabetes.
Abstract: The invention relates to compounds that are useful for the prevention or treatment of TRPM3 mediated disorders, more in particular disorders selected from pain and inflammatory hypersensitivity. The invention also relates to a method for the prevention or treatment of said TRPM3 mediated disorders.
Type:
Grant
Filed:
May 12, 2024
Date of Patent:
January 28, 2025
Assignee:
Katholieke Universiteit Leuven
Inventors:
Patrick Chaltin, Arnaud Marchand, Jean-Christophe Vanherck, Thomas Voets, Joris Vriens, Melanie Reich, André Welbers
Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.
Abstract: The subject matter described herein is directed to ferroportin inhibitor compounds of Formula I or I? and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries.
Type:
Grant
Filed:
June 15, 2023
Date of Patent:
January 21, 2025
Assignee:
Global Blood Therapeutics, Inc.
Inventors:
Qing Xu, Carsten Alt, Zhe Li, Shahul Nilar, Peter Michael Rademacher, Calvin Wesley Yee