Abstract: Multitarget-directed compounds combining the features of reactive oxygen species (ROS) modulators, poly (ADP-ribose) polymerase 1 (PARP1), and/or heat shock protein 90 (Hsp90) inhibitors in a single molecule. These single agents constitute a systemic regimen for treating the triple-negative breast cancer phenotype that overcomes drug resistance and tumor recurrence, and may be used for other indications as well, such as the treatment of various neurodegenerative disorders.
Type:
Grant
Filed:
June 30, 2023
Date of Patent:
February 6, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Saad Shaaban, Hany Mohamed Abd El-Lateef Ahmed, Bander Alshemary
Abstract: The present embodiments relate to substituted heterocyclic derivative therapeutic compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of diseases mediated by aberrant cell signalling, such as inflammatory disorders, cancer and neoplastic disease. Particular compounds described herein exhibit selective inhibitory activity against CBP compared with BRD4.
Type:
Grant
Filed:
March 15, 2021
Date of Patent:
February 6, 2024
Inventors:
Lynnie Trzoss, Juan Manuel Betancort, Toufike Kanouni, Michael Brennan Wallace, Amogh Boloor
Abstract: Provided is a compound including a moiety A and one or two moieties B fused with the moiety A at fusing sites, in which X is N, O, S or C; and when X is O or S, Ar2-L1- is absent; Y1-Y4 are each independently C or N; L1 and L2 are each independently a single bond, a substituted or unsubstituted C6-C30 arylene, a substituted or unsubstituted C10-C40 fused arylene, or a substituted or unsubstituted C4-C30 heteroarylene; Ar1 and Ar2 are each independently a substituted or unsubstituted C6-C30 aryl, a substituted or unsubstituted C10-C40 fused aryl, a substituted or unsubstituted C4-C30 heteroaryl, or a substituted or unsubstituted C6-C40 fused heteroaryl, and * represents one of the fusing sites, N or CRa, where Ra is a substituted or unsubstituted C1-C20 alkyl, a substituted or unsubstituted C6-C30 aryl, or a substituted or unsubstituted C3-C30 heteroaryl.
Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
Type:
Grant
Filed:
April 13, 2022
Date of Patent:
January 30, 2024
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 P. Fischer, Ronald Jay Hinklin, Yutong Jiang, Oren Teague McNulty, Macedonio J. Mejia, Martha E. Rodriguez, Christina Elizabeth Wong
Abstract: A 7-(4-((4-benzylidene-5-oxo-2-phenyl-4,5-dihydro-1H-imidazol-1-yl)methyl)piperazin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid compound, its synthesis, and its use as an anti-inflammatory agent.
Type:
Grant
Filed:
September 20, 2023
Date of Patent:
January 30, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Hany Mohamed Abd El-Lateef Ahmed, Mai Mostafa Khalaf Ali, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
Abstract: A series of functionalized imidazophenthridine analogue-based blue phosphorescent emitters have been designed, where bulky substituents (e.g., tetrabutyl, phenyl, mesityl, triisopropylbenzene, etc.) are introduced on an imidazophenthridine fragment of the emitters. Bulky substituents may suppress potential excimer formation, as well as improve the solubility of the complexes. This class of emitters may be utilized in luminescent labels, emitters for organic light emitting devices, and lighting applications.
Type:
Grant
Filed:
January 24, 2020
Date of Patent:
January 23, 2024
Assignee:
Arizona Board of Regents on behalf of Arizona State University
Abstract: Crystalline forms of Compound I: pharmaceutically acceptable salts thereof, and solvates and hydrates thereof are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.
Type:
Grant
Filed:
August 13, 2020
Date of Patent:
January 16, 2024
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Yi Shi, Kevin J. Gagnon, Jicong Li, Jennifer Lu, Ales Medek, Muna Shrestha, Michael Waldo, Beili Zhang, Carl L. Zwicker, Corey Don Anderson, Jeremy J. Clemens, Thomas Cleveland, Timothy Richard Coon, Bryan Frieman, Peter Grootenhuis, Sara Sabina Hadida Ruah, Jason McCartney, Mark Thomas Miller, Prasuna Paraselli, Fabrice Pierre, Sara E. Swift, Jinglan Zhou
Abstract: Nitrogen containing bicyclic compounds of Formula (I), pharmaceutical compositions comprising these compounds and their use in treating bacterial infection is disclosed.
Abstract: The invention provides a novel class of therapeutics that are safe and effective inhibitors of Janus kinase 1 and pharmaceutical composition and methods of preparation and use thereof in the treatment of various diseases and disorders (e.g., inflammatory diseases, immune-mediated diseases or cancer).
Abstract: The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.
Type:
Grant
Filed:
July 28, 2021
Date of Patent:
January 2, 2024
Assignee:
JAZZ PHARMACEUTICALS IRELAND LIMITED
Inventors:
Andrew Belfield, Clifford David Jones, Jean-François Margathe, Chiara Colletto
Abstract: The invention provides a novel class of therapeutics that are safe and effective inhibitors of Janus kinase 1 and pharmaceutical composition and methods of preparation and use thereof in the treatment of various diseases and disorders (e.g., inflammatory diseases, immune-mediated diseases or cancer).
Abstract: Iridium, rhodium, and platinum complexes suitable for use as phosphorescent emitters or as delayed fluorescent and phosphorescent emitters having the following structures:
Type:
Grant
Filed:
March 25, 2021
Date of Patent:
December 26, 2023
Assignee:
Arizona Board of Regents on behalf of Arizona State University
Abstract: This invention relates to novel opioid derivatives of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R3, R4 and Z are as defined herein in the disclosure. The invention also relates to the use of such compounds for the treatment or prevention of, for example, pain.
Type:
Grant
Filed:
February 22, 2019
Date of Patent:
December 19, 2023
Assignee:
RHODES TECHNOLOGIES
Inventors:
Ping Chang, Raymond Glowaky, Michael David Rogers
Abstract: The invention provides compounds of formula (I): or pharmaceutically-acceptable salts thereof, that are inhibitors of Janus kinases and release an active metabolite in vivo. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat inflammatory skin diseases and other diseases.
Type:
Grant
Filed:
September 27, 2021
Date of Patent:
December 19, 2023
Assignee:
THERAVANCE BIOPHARMA R&D IP, LLC
Inventors:
Philip A. Gerken, Jianhua Chao, Daniel D. Long
Abstract: The present invention is directed to bicyclic pyridine N-oxide derivatives, stereoisomers, isotopologues, isotopomers and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing said compounds and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.
Type:
Grant
Filed:
March 17, 2022
Date of Patent:
December 19, 2023
Assignee:
Janssen Pharmaceutica NV
Inventors:
Guozhang Xu, Zhijie Liu, Micheal D. Gaul
Abstract: The present disclosure discloses a quinoline-2,3-fused nine-membered ring scaffold compound, and a preparation method and application thereof as an effective component in a plant fungicide. The quinoline-2,3-fused nine-membered ring scaffold compound stated in the present disclosure is prepared by the following method including steps: mixing a quinoline-derived aniline compound and a formaldehyde compound, adding a solvent and a catalyst, controlling a system temperature, and reacting with stirring to obtain a quinoline-2,3-fused nine-membered ring compound. According to the present disclosure, a 1,6-hydride transfer/cyclization strategy is triggered by aldimine condensation, the quinoline-derived aniline compound and the formaldehyde compound are prepared into the quinoline-2,3-fused nine-membered ring compound with a wide substrate scope and a potential biological activity by a “one-pot synthesis method” quickly.
Type:
Grant
Filed:
February 8, 2023
Date of Patent:
December 12, 2023
Assignee:
QINGDAO AGRICULTURAL UNIVERSITY
Inventors:
Xiao-De An, Jian Xiao, Daying Shao, Bin Qiu
Abstract: Certain embodiments of the present disclosure provide liquid pharmaceutical formulations, suitable for oral administration, that contain glycerol and an amount of apixaban in the solution phase of the formulations of from 0.5 mg/ml to 6 mg/ml.
Abstract: There is provided a therapeutic agent for Alzheimer's disease and Lewy body dementia for combined use of (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinoline-4(5H)-one represented by formula (1): or a pharmaceutically acceptable salt thereof, and donepezil represented by formula (II): or a pharmaceutically acceptable salt thereof.
Abstract: The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.
Type:
Grant
Filed:
March 22, 2022
Date of Patent:
December 5, 2023
Assignee:
NUVATION BIO INC.
Inventors:
David Hung, Jayakanth Kankanala, Christopher Paul Miller, Jeremy David Pettigrew, Son Minh Pham, Ihab S. Darwish
Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of diseases and conditions.
Type:
Grant
Filed:
May 7, 2021
Date of Patent:
November 28, 2023
Assignee:
Morphic Therapeutic, Inc.
Inventors:
Mark Brewer, Matthew G. Bursavich, Aleksey I. Gerasyuto, Kristopher N. Hahn, Bryce A. Harrison, Kyle D. Konze, Fu-Yang Lin, Blaise S. Lippa, Alexey A. Lugovskoy, Bruce N. Rogers, Mats A. Svensson, Dawn M. Troast