Abstract: Provided herein is a process for the preparation of (R)—N-(5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl)-1-methyl-1H-pyrazole-4-carboxamide, intermediates thereof, and salts of the foregoing.
Type:
Grant
Filed:
September 15, 2023
Date of Patent:
March 11, 2025
Assignee:
CYTOKINETICS, INC.
Inventors:
Denise Andersen, Matthew Pfeiffer, Norma Tom, Bradley P. Morgan
Abstract: Provided are methods useful for preventing and mitigating radiation injury, including acute radiation syndrome, comprising administering to a subject a therapeutically effective amount of a compound represented by formula I or a pharmaceutically acceptable salt thereof, wherein Z is —O— or —N(H)—.
Type:
Grant
Filed:
June 8, 2023
Date of Patent:
March 11, 2025
Assignees:
Georgetown University, The Board of Regents of the University of Oklahoma
Inventors:
Milton L. Brown, Yali Kong, Courtney Houchen, Sripathi M. Sureban, Parthasarathy Chandrakesan
Abstract: The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Abstract: The present invention provides pharmaceutically acceptable salts of compounds of Formula I that are potent EP4 receptor antagonists and can be used for treating cancer or inflammatory diseases alone or in combination with antibody therapy, radiation therapy, anti-metabolite chemotherapy to a subject in need thereof.
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
Abstract: Pyrimidine and Pyridine containing compounds are described herein that are enzyme p70S6K inhibitors useful in the treatment of S6K-dependent or S6K-mediated diseases and conditions, including but not limited to cancer, fibrotic metabolic and certain neurological disorders.
Type:
Grant
Filed:
December 6, 2023
Date of Patent:
February 25, 2025
Assignee:
EPIGEN Biosciences, Inc.
Inventors:
Graham Beaton, Fabio Tucci, Satheesh Ravula, Suk Joong Lee, Chandravadan Shah
Abstract: The disclosure provides methods of treating a patient having primary hyperoxaluria or idiopathic hyperoxaluria comprising administering a therapeutically effective amount of compound of the formula and pharmaceutically acceptable salts, solvates, and hydrates thereof to the patient. The variables, e.g. ring A, n, R, R3, R10, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful inhibiting the conversion of glyoxylate to oxalate. When administered to a patient having a disease or disorder associated with elevated oxalate levels, such as PH type 1, type 2, or type 3 or idiopathic hyperoxaluria the compounds prevent or substantially reduce the amount and buildup of oxalate the patient's kidneys, bladder, urinary tract and other parts of the patient's body.
Type:
Grant
Filed:
July 14, 2023
Date of Patent:
February 25, 2025
Assignees:
VANDERBILT UNIVERSITY, THE UAB RESEARCH FOUNDATION, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
Inventors:
Matthew Hall, Daniel J. Urban, John Knight, Ross Holmes, Kyle David Wood, Alex Waterson, Victor M. Darley-Usmar, Leonard M. Neckers
Abstract: Disclosed are bispecific compounds (degraders) that target ALK for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat diseases and disorders characterized or mediated by aberrant ALK activity.
Type:
Grant
Filed:
September 26, 2019
Date of Patent:
February 25, 2025
Assignee:
DANA-FARBER CANCER INSTITUTE, INC.
Inventors:
Nathanael S. Gray, John M. Hatcher, Chelsea E. Powell, Pasi A. Janne
Abstract: Provided are a JAK kinase inhibitor, preparation and use thereof. In particular, provided is a compound of Formula I, wherein each group is as described in the specification. The compound has an excellent JAK inhibitory activity, and therefore can be used to prepare pharmaceutical compositions for the treatment of cancer and other diseases related to JAK activity.
Abstract: The present disclosure relates to novel sulfonimidamide compounds and related compounds and their use in treating a disorder responsive to modulation of cytokines such as IL-1? and IL-18, modulation of NLRP3 or inhibition of the activation of NLRP3 or related components of the inflammatory process.
Type:
Grant
Filed:
January 15, 2021
Date of Patent:
February 25, 2025
Assignee:
Genentech, Inc.
Inventors:
Christopher McBride, Lynnie Lin Trzoss, Amogh Boloor, Nadezda V. Sokolova, Richard M. Pastor, Steven Thomas Staben, Craig Stivala, Matthew Volgraf, Sarah M. Bronner
Abstract: Salts and crystalline forms of (R)-4-((2-(1-(2-fluoro-6-(trifluoromethyl)benzyl)-2,4-dioxo-1?-((5-(trifluoromethyl)furan-2-yl)methyl)-1H-spiro[furo[3,4-d]pyrimidine-5,4?-piperidine]-3(2H,4H,7H)-yl)-1-phenylethyl)amino)butanoic acid (formula (1)) show excellent physicochemical properties including, for example, hygroscopicity, related substances, chemical stability. The salts and crystalline forms are useful and suitable for pharmaceutical uses such as the preparation of a pharmaceutical composition containing the same as an active ingredient.
Abstract: The present disclosure relates to 3-substituted 1,2,4-oxadiazole compounds and their derivatives, which are useful as T-cell immunoglobulin and mucin-domain containing-3 (TIM-3) inhibitors or as dual inhibitors of TIM-3 and the programmed cell death 1 (PD-1) signaling pathway. The disclosure also relates to treatment of disorders by inhibiting an immunosuppressive signal induced by TIM-3, PD-1, PD-L1, and/or PD-L2.
Abstract: This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.
Abstract: An organic electroluminescence device includes a first electrode, a second electrode, and an emission layer disposed between the first electrode and the second electrode, wherein the emission layer includes a polycyclic compound represented by Formula 1, thereby showing improved emission efficiency.
Abstract: The present disclosure generally relates to compositions comprising unique combinations of cannabinoids, antioxidants, and cofactors. The present disclosure also provides methods of making the compositions and methods for using the compositions for the treatment of mitochondrial ATP deficit disorders.
Type:
Grant
Filed:
December 20, 2023
Date of Patent:
January 14, 2025
Assignee:
Ilera Derm LLC
Inventors:
Brian Warrington, Karyn Grossman, Oludare Odumosu, Zoltan Kerekes
Abstract: Provided are compounds, or pharmaceutically acceptable salts thereof, which are useful for inhibiting FOXM1, inhibiting cancer growth, and/or treating cancer. In particular, these compounds and their corresponding quaternary ammonium salts may be used to treat various forms of breast cancer.
Type:
Grant
Filed:
April 9, 2019
Date of Patent:
January 7, 2025
Assignee:
The Board of Trustees of the University of Illinois
Inventors:
John A. Katzenellenbogen, Benita Katzenellenbogen, Sung Hoon Kim, Noah Bindman
Abstract: Provided herein is a method for treating a monocarboxylate transporter MCT4-mediated disorder in a subject in need thereof. The method comprises the step of administering to the subject a compound of structural Formula I and/or a salt thereof. The treatment of the monocarboxylate transporter MCT4-mediated disorder may inhibit activity of MCT4, or a mutant thereof, sometimes with at least a 100-fold selectivity for MCT4 over MCT1.
Abstract: Compounds of Formula Ia or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases.
Type:
Grant
Filed:
October 17, 2019
Date of Patent:
January 7, 2025
Assignee:
Array BioPharma Inc.
Inventors:
James Francis Blake, Mark Laurence Boys, Mark Joseph Chicarelli, Adam Wade Cook, Mohamed S. A. Elsayed, Jay Bradford Fell, John Peter Fischer, Ronald Jay Hinklin, Oren Teague Mcnulty, Macedonio J. Mejia, Martha E. Rodriguez, Christina Elizabeth Wong
Abstract: The present invention relates to an amorphous solid dispersion comprises 6-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)nicotinamide (Compound I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable polymer. The present invention also relates to pharmaceutical compositions comprising the amorphous solid dispersion. The amorphous solid dispersion of the present invention is stable upon storage and provides a better dissolution rate and bioavailability when comparing with a crystalline form.