Abstract: The present invention is directed to bi-functional compounds which find use as pharmaceutical agents in the treatment of disease states and/or conditions which are mediated through macrophage migration inhibitory factor (MIF) or immunoglubin G (IgG). The present invention is also directed to pharmaceutical compositions which comprise these bi-functional compounds as well as methods for treating disease states and/or conditions which are mediated through MIF/IgG or where MIF/IgG is a contributing factor to the development and perpetuation of diseases and/or conditions, especially including autoimmune diseases and cancer, among others. The purpose of the present invention is to provide a molecular strategy to lower plasma MIF/IgG level in patients with autoimmune diseases or certain types of cancers.
Abstract: The present invention provides a novel compound represented by Chemical Formula 2, or a pharmaceutically acceptable salt thereof. The novel compound according to the present invention exhibits an excellent acid secretion inhibitory effect.
Type:
Grant
Filed:
June 16, 2021
Date of Patent:
September 26, 2023
Assignee:
ILDONG PHARMACEUTICAL CO., LTD.
Inventors:
Hong Chul Yoon, Joon Tae Park, Jung Woo Lee, Kyung Mi An, Rang A Im, Woo Jin Jeon, Jae Ho Heo, Chang Hee Hong, Jung Eun Park, Te Ik Sohn, Da Hae Hong, Jung Ho Kim, Jae Eui Shin, Yeong Ran Yoo, Min Whan Chang, In Gyu Je, Su Yeon Kang, Yoon Sung Song, Joo Yun Lee
Abstract: The present disclosure relates to compositions of N-acetylcysteine for use in treating aortic stenosis. Methods of treating aortic stenosis in a subject comprising administering to said subject an effective amount of N-acetylecysteine (NAC) or other thiol-reactive compound, or agents that inhibit TGF-Beta activation and/or signaling.
Abstract: Compounds of formula I and their metabolites are potent mediators of an inflammatory response: where a, b, c, d, e, f, V, W, X, Y, Ra, Ra?, Rb, Rb?, Rc, and Rc? are defined herein. In particular, the compounds of the invention are candidate therapeutics for treating inflammatory conditions.
Type:
Grant
Filed:
October 14, 2020
Date of Patent:
August 15, 2023
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
Bruce A. Freeman, Francisco J. Schopfer
Abstract: Described herein are novel compounds that block the activity of LOX family members having good IC50 values, no cellular toxicity below 10 ?M, induce sensitization of the cells to doxorubicin, strong activity in a recombinant LOX/LOXL2 activity, and a chemical structure that is drug-like and does not have a PAINS flag, as well as, methods of treatment using the compounds with respect to cancer, organ fibrosis, neurodegenerative and cardiovascular diseases.
Abstract: Disclosed herein are compounds and compositions useful in the treatment of GLS1 mediated diseases, such as cancer, having the structure of Formula I: Methods of inhibition GLS1 activity in a human or animal subject are also provided.
Type:
Grant
Filed:
July 1, 2020
Date of Patent:
August 1, 2023
Assignee:
Board of Regents, The University of Texas System
Inventors:
Richard Thomas Lewis, Philip Jones, Alessia Petrocchi, Naphtali Reyna, Matthew Hamilton, Michael J. Soth, Timothy Heffernan, Michelle Han, Jason P. Burke
Abstract: The present invention relates to methods and compounds for regulating or enhancing erythropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.
Type:
Grant
Filed:
December 23, 2020
Date of Patent:
June 20, 2023
Assignee:
FibroGen, Inc.
Inventors:
Stephen J. Klaus, Al Y. Lin, Thomas B. Neff, Volkmar Guenzler-Pukall, Qingjian Wang, Lee A. Flippin, Michael P. Arend
Abstract: The present invention relates to methods and compounds for regulating or enhancing erthropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.
Type:
Grant
Filed:
December 23, 2020
Date of Patent:
June 20, 2023
Assignee:
FibroGen, Inc.
Inventors:
Stephen J. Klaus, Christopher J. Molineaux, Thomas B. Neff, Volkmar Guenzler-Pukall, Robert C. Stephenson, Todd W. Seeley, Ingrid Langsetmo Parobok
Abstract: Disclosed are a thiazolone derivative of N6022 and a pharmaceutical use thereof. The characteristic structure of the thiazolone derivative of N6022 is: Compared to N6022, the compound of the present disclosure has good oral bioavailability and a longer half-life period. In in-vitro experiments, administering the compound of the present disclosure can improve migration ability, tube formation ability and, the permeability of human umbilical vein endothelial cells caused by high glucose, and administering the compound of the present disclosure at an animal level can obviously promote the angiogenesis and blood flow recovery of ischemic lateral limbs of diabetic mice. Overall, it suggests that the compound of the present disclosure can be used for treating diseases related to diabetic vascular complications.
Type:
Grant
Filed:
April 25, 2021
Date of Patent:
June 6, 2023
Assignee:
NANJING MEDICAL UNIVERSITY
Inventors:
Yong Ji, Liping Xie, Shuang Zhao, Tianyu Song, Yi Han
Abstract: The present disclosure is directed to tetrahydroquinazoline derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naïve cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).
Type:
Grant
Filed:
August 25, 2021
Date of Patent:
May 16, 2023
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Antonella Converso, Abdellatif El Marrouni, Anthony W. Shaw, David N. Hunter, Ashley Forster, Cheng Wang, Yunlong Zhang
Abstract: Compounds, pharmaceutically acceptable salts, esters, prodrugs, and pharmaceutical compositions thereof are disclosed that are useful for inhibition of the biological activity of CCL5 on mammalian cells, as well as methods of treatment for diseases involving the increased biological activity of CCL5.
Abstract: The present invention provides compounds and intermediates. The present invention also provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation. The present invention also provides compounds that may be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.
Type:
Grant
Filed:
November 24, 2020
Date of Patent:
April 11, 2023
Assignee:
C4 Therapeutics, Inc.
Inventors:
Christopher G. Nasveschuk, Fabian Dey, Annick Goergler, Roger Norcross, Philipp Schmid
Abstract: A method for manufacturing an insecticidal compound and insecticidal compositions comprising the insecticidal compound and methods of use are presented herein. The manufacturing method presented herein allows for a high purity grade of thiocyclam hydrochloride to be synthesized. The insecticidal compositions comprising the thiocyclam hydrochloride can be used for prevention of crop destruction by insects. The use of thiocyclam hydrochloride in insecticidal compositions as described herein can achieve greater efficacy than previously known insecticides, by eliminating the insect pests more reliably and efficiently.
Type:
Grant
Filed:
March 4, 2020
Date of Patent:
February 28, 2023
Assignee:
ARYSTA LIFESCIENCE NORTH AMERICA, LLC
Inventors:
Cameron S. Gibb, Christopher L. Larson, Mark T. Singleton, Kamal L. Kataria, Samantha Besse, Joseph A. Moore, III, Thomas C. Lovelace, Chandra S. Kanugala, Srinivas Vollala, Balraju Vadla
Abstract: Novel NTRK1 fusion molecules, detection reagents, and uses and kits for evaluating, identifying, assessing and/or treating a subject having a cancer are disclosed.
Type:
Grant
Filed:
November 14, 2019
Date of Patent:
February 14, 2023
Assignee:
Foundation Medicine, Inc.
Inventors:
Matthew J. Hawryluk, Doron Lipson, Vincent A. Miller, Philip James Stephens
Abstract: The invention relates to the therapy of diseases associated with the activity of histamine receptors, in particular for the treatment of allergic diseases, preferably the therapy of perennial and persistent allergic rhinitis, itch, as well as a number of other diseases associated with the activity of histamine receptor type 3 and/or 4, using compound N,N?-bis(2-(1H-imidazol-5-yl)ethyl)malonamide. This compound, as well as pharmaceutically acceptable salts, hydrates, or solvates thereof, is an antagonist of histamine receptor type 3 and/or 4. The invention also relates to pharmaceutical compositions containing a therapeutically effective amount of Compound I.
Abstract: The present invention provides new methods and kits for treating IBS; treating IBS in females; treating IBS in older subjects; and treating IBS in non-white subjects.
Abstract: Disclosed are methods for inhibiting the progression of neurodegenerative disease. The methods include administering to a patient suffering from such a disease a composition comprising either deuterated arachidonic acid or an ester thereof.
Type:
Grant
Filed:
August 20, 2021
Date of Patent:
November 29, 2022
Assignee:
Retrotope, Inc.
Inventors:
Peter Milner, Mikhail Sergeevich Shchepinov
Abstract: Some aspects of the invention provide for essential fatty acids which are substituted in specific positions to slow down oxidative damage by Reactive Oxygen Species (ROS), and to suppress the rate of consequent formation of reactive products, for the purpose of preventing or reducing the damage associated with oxidative stress associated diseases such as neurological diseases and age-related macular degeneration (AMD).
Abstract: Compounds, pharmaceutically acceptable salts, esters, prodrugs, and pharmaceutical compositions thereof are disclosed that are useful for inhibition of the biological activity of CCL5 on mammalian cells, as well as methods of treatment for diseases involving the increased biological activity of CCL5.
Abstract: Provided are methods for treating Paramyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Human parainfluenza and Human respiratory syncytial virus infections.
Type:
Grant
Filed:
May 20, 2020
Date of Patent:
November 8, 2022
Assignee:
Gilead Sciences, Inc.
Inventors:
Richard L. Mackman, Jay P. Parrish, Adrian S. Ray, Dorothy Agnes Theodore