Abstract: The present invention provides methods for treating and/or managing pain. The invention further provides methods for reducing or inhibiting opioid tolerance, reducing risk of opioid addiction or dependence, restoring opioid efficacy, and enhancing the therapeutic effect of an opioid. The invention further provides compositions for use in the methods of the invention.
Abstract: The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
Type:
Grant
Filed:
June 21, 2022
Date of Patent:
March 12, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Julian A. Codelli, Michael Graupe, Juan A. Guerrero, Jesse M. Jacobsen, Tetsuya Kobayashi, Jonathan William Medley, Yasamin Moazami, Leena B. Patel, Jie Xu, Suet C. Yeung
Abstract: A phosphorescent emitter or delayed fluorescent and phosphorescent emitters represented by Formula I or Formula II, where M is platinum or palladium.
Type:
Grant
Filed:
November 19, 2020
Date of Patent:
March 12, 2024
Assignee:
Arizona Board of Regents on behalf of Arizona State University
Abstract: A method of treating chemical-induced lung injury in a subject in need thereof includes administering to the subject a therapeutically effective amount of ibudilast, or a pharmaceutical salt thereof.
Type:
Grant
Filed:
January 27, 2022
Date of Patent:
March 12, 2024
Assignee:
MediciNova, Inc.
Inventors:
Kazuko Matsuda, Federico Carlos Aréjola Gaeta
Abstract: The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula: wherein A, X, Y, Z, Q, R1, R2, R3, R4, R5, and n are described herein.
Type:
Grant
Filed:
December 21, 2018
Date of Patent:
March 5, 2024
Assignee:
HiberCell, Inc.
Inventors:
Johan Lindström, Lars Boukharta Persson, Madeleine Livendahl, Jenny Viklund, Tobias Ginman, Rickard Forsblom, Fredrik Rahm, Edward A. Kesicki, Kannan Karukurichi Ravi, Eugene R. Hickey, Markus K. Dahlgren, Aleksey I. Gerasyuto
Abstract: The present disclosure is directed to inhibitors of Formula (0), or a stereoisomer thereof, or pharmaceutically acceptable salt thereof, of the interaction of menin with MLL and MLL fusion proteins, pharmaceutical compositions containing the same, and their use in the treatment of cancer and other diseases mediated by the menin-MLL interaction,
Type:
Grant
Filed:
May 13, 2022
Date of Patent:
March 5, 2024
Assignees:
Syndax Pharmaceuticals, Inc., Vitae Pharmaceuticals, LLC
Inventors:
Gerard M. McGeehan, William H. Miller, Nicholas Paul Camp, Salvacion Cacatian, Santosh S. Kulkarni, Swapan Kumar Samanta, Virsinha Venkat Reddy
Abstract: Disclosed are compounds of formula (Ia) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of formula (Ia) and methods of using the same for treating cancer or a respiratory inflammatory disease and inhibiting arginase: wherein R1 is —NHR1a; R1a is —H or —C(O)CH(R1b)NHR1c; and R1b is selected from —H, —(C1-C4) alkyl and CH2OR1d and R1c is —H; or R1b and R1c, together with the atom to which they are attached, form a 5-membered heterocyclic ring; and R1d is H or —CH3.
Type:
Grant
Filed:
July 10, 2023
Date of Patent:
February 27, 2024
Assignee:
AstraZeneca AB
Inventors:
Scott Nathan Mlynarski, Tyler Grebe, Sameer Kawatkar, Maurice Raymond Verschoyle Finlay, Iain Simpson, Jianyan Wang, Steve Cook, Dedong Wu
Abstract: The invention relates to a compound which is a diazabicyclooctanone of Formula (I) or a pharmaceutically acceptable salt thereof: wherein R is as defined herein. The compounds are useful in the treatment of bacterial infection, in particular they are useful in reducing bacterial resistance to antibiotics. They are also useful in the treatment of bacteria which express serine-?-lactamase enzymes, in combination with antibiotics.
Abstract: Provided herein are compounds, salts, crystalline forms, and pharmaceutical compositions that are related to Selective Estrogen Receptor Degraders, as well as methods of preparing the same. Also provided herein are methods of using the compounds, salts, crystalline forms, and pharmaceutical compositions for the treatment of diseases or disorders, such as breast cancer.
Abstract: The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
Type:
Grant
Filed:
November 9, 2021
Date of Patent:
February 13, 2024
Assignee:
Padlock Therapeutics, Inc.
Inventors:
Rajesh Devraj, Gnanasambandam Kumaravel, Holly Atton, Edward Beaumont, Elise Gadouleau, Laura Gleave, Philip Stephen Kerry, Cristina Lecci, Mirco Meniconi, Nat Monck, Jordan Palfrey, Kostas Papadopoulos, Heather Tye, Philip A. Woods
Abstract: The present disclosure relates generally to certain 6-azabenzimidazole compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.
Type:
Grant
Filed:
November 9, 2021
Date of Patent:
February 13, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Gayatri Balan, Mark J. Bartlett, Jayaraman Chandrasekhar, Julian A. Codelli, John H. Conway, Jennifer L Cosman, Rao V. Kalla, Zachary A. Kasun, Musong Kim, Seung H. Lee, Jennifer R. Lo, Jennifer A. Loyer-Drew, Scott A. Mitchell, Thao D. Perry, Gary B. Phillips, Patrick J. Salvo, Sundaramoorthi Swaminathan, Joshua J. Van Veldhuizen, Suet C Yeung, Jeff Zablocki
Abstract: The present invention generally relates to compounds as a dual kinase-demethylase inhibitor useful for the treatment of diseases mediated by a kinase and/or a histone demethylase, such as inflammation, cancer, viral and bacterial infections, neurological and immunological disorders. Pharmaceutical compositions and methods for treating those diseases are within the scope of this invention.
Type:
Grant
Filed:
April 29, 2021
Date of Patent:
February 6, 2024
Assignee:
Purdue Research Foundation
Inventors:
Herman O. Sintim, Neetu Dayal, Clement Opoku-Temeng
Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Grant
Filed:
November 3, 2021
Date of Patent:
February 6, 2024
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Joseph Panarese, Dexter Davis, Samuel Bartlett, Katherine Chong, Nathaniel Kenton, Yat Sun Or
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