Abstract: Divalent salts of S-allylmercapto-N-acetylcysteine and related compositions are disclosed which can be administered in order to provide protection from the formation of aldehyde-protein adducts, protein carbonylation, protein aggregation, and the resulting neuroinflammation. Various neurodegenerative diseases which are suitable for treatment using these compositions include Alzheimer's disease, senile dementia, Parkinson's disease, multiple sclerosis, Lewy body disease, peripheral neuropathy, spinal cord injury, stroke and cerebral ischemia.
Abstract: Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells.
Type:
Grant
Filed:
March 1, 2019
Date of Patent:
August 25, 2020
Assignees:
Eastern Virginia Medical School, The Regents of the University of California Santa, The United States of America Department of Health, Thomas Jefferson University
Inventors:
David J. Maloney, Diane K. Luci, Ajit Jadhav, Theodore Holman, Jerry L. Nadler, Michael Holinstat, David Taylor-Fishwick, Anton Simeonov, Adam Yasgar, Steven McKenzie
Abstract: Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}-sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
Type:
Grant
Filed:
November 8, 2017
Date of Patent:
August 4, 2020
Assignee:
AbbVie Inc.
Inventors:
Nathaniel Catron, Shuang Chen, Yuchuan Gong, Geoff G. Zhang
Abstract: The present disclosure provides compositions including a beta-lactamase inhibitor, pharmaceutical compositions including a beta-lactamase inhibitor, methods of treatment of a condition (e.g., infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.
Type:
Grant
Filed:
July 30, 2018
Date of Patent:
June 23, 2020
Assignees:
UNIVERSITY OF SOUTH FLORIDA, The Regents of the University of California
Inventors:
Yu Chen, Nicholas Joseph Torelli, Orville Antonio Pemberton, Xiujun Zhang, Adam Renslo, Kyle Defrees, Priyadarshini Jaishankar
Abstract: Methods of treating or preventing allergic or pulmonary diseases characterized by endothelial dysfunction with Alda-1 are presented. Treatment of pulmonary endothelial cells subjected to hyperoxia with Alda-1 showed an increase in ALDH2 activity and expression. Treatment with Alda-1 also illustrated a decrease in oxidative stress, a decrease in reactive oxygen species (ROS), a decrease in apoptosis, a decrease in inflammation and an enhancement of mitochondrial membrane potential.
Type:
Grant
Filed:
February 22, 2019
Date of Patent:
May 26, 2020
Assignee:
University of South Florida
Inventors:
Narasaiah Kolliputi, Richard F. Lockey, Lakshmi Galam
Abstract: Compounds and pharmaceutically acceptable salts thereof that may be used to treat a disease, for example, Duchenne muscular dystrophy, AIDS, and progeria. The compounds and pharmaceutically acceptable salts thereof may be part of a pharmaceutical composition including a pharmaceutically acceptable support.
Type:
Grant
Filed:
October 5, 2018
Date of Patent:
May 19, 2020
Assignees:
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE DE MONTPELLIER
Inventors:
Jamal Tazi, David Grierson, Florence Mahuteau-Betzer, Pierre Roux
Abstract: Compounds of Formulae I? and I are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.
Type:
Grant
Filed:
November 2, 2018
Date of Patent:
May 5, 2020
Assignee:
Cyclerion Therapeutics, Inc.
Inventors:
Takashi Nakai, Joel Moore, Nicholas Robert Perl, Rajesh R. Iyengar, Ara Mermerian, G-Yoon Jamie Im, Thomas Wai-Ho Lee, Colleen Hudson, Glen Robert Rennie, Lei Jia, Paul Allan Renhowe, Timothy Claude Barden, Xiang Y. Yu, James Edward Sheppeck, Karthik Iyer, Joon Jung, George Todd Milne, Kimberly Kafadar Long, Mark G. Currie
Abstract: The invention provides carbazole derivatives for the treatment of fibrotic diseases (pathological collagen deposition) in tissues and organs, and related symptoms, and conditions thereof.
Abstract: Current therapeutic approach to treating heart allotransplantation rejection focus on immunosuppression protocols that carry harmful side effects after chronic use, which include global immune depression to the patient. The present inventors have discovered alternative and synergistic protocols based on inhibiting NF-?B and NLRP3 inflammasome-dependent IL-1? release with nitrated NSAID derivatives.
Type:
Grant
Filed:
January 24, 2019
Date of Patent:
April 28, 2020
Inventors:
Carlos Batthyány, Gloria Virginia López, Carlos Escande, Williams Arturo Porcal Quinta, Germán Adrian Galliussi López, Marcelo Hill, Mercedes Segovia
Abstract: Provided in the present invention is a pharmaceutical composition containing an imidazoline derivative. In particular, the pharmaceutical composition provided in the present invention contains (S)-4-(3-(4-(2,3-dihydroxypropoxy)phenyl)-4,4-dimethyl-5-carbonyl-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile and cellulose ether; and the composition has a good stability, dissolution rate and bioavailability.
Abstract: Epoxides and hydroperoxide compounds having antifungal activities derived from the oxidation linalyl acetate, a major component of lavender oil, are disclosed. Also, disclosed are pharmaceutical composition and methods of treating and protecting a subject from fungal infection.
Abstract: Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.
Type:
Grant
Filed:
August 9, 2018
Date of Patent:
March 3, 2020
Assignee:
THE UNIVERSITY OF HONG KONG
Inventors:
Chi Ming Che, Sin Ki Fung, Tian Feng Chen
Abstract: Two isoforms of thyroid receptor alpha (THR?1 and THR?2) have been found to be associated with the growth of cancer. Use of inhibitors of THR?1 (Formula I) and/or agonists of THR?2 (Formula II) in the treatment of such cancers is disclosed. Treatment of other disorders associated with such receptors is also contemplated, as is the use of diagnostic methods for predicting therapeutic outcomes based on the levels of expression of THR?1 and THRa?2 in a tissue sample.
Type:
Grant
Filed:
December 22, 2016
Date of Patent:
March 3, 2020
Assignee:
McMaster University
Inventors:
Sukhbinder Dhesy-Thind, Katarzyna J. Jerzak, Anita Bane, Jessica G. Cockburn, John A. Hassell
Abstract: A method of treating a pervasive development disorder in a subject includes administering to the subject an amount of an NMDAR antagonist effective to ameliorate biochemical and functional abnormalities in the subject associated with loss-of-function mutations of the gene encoding methyl-CpG binding protein 2 (MeCP2).
Abstract: The present invention provides a compound of formula I; wherein R1 is an alkyl pyrazole or an alkyl carboxamide, and R2 is a hydroxycycloalkyl; or a pharmaceutically acceptable salt thereof, and compositions containing these compounds, for use to treat a brain tumor, particularly glioblastoma. The invention provides effective treatment of a brain tumor and can be used by oral administration of a compound of Formula I as further described herein. The invention also provides a method to treat a subject having a brain tumor such as glioblastoma, wherein the method comprises administering to the subject an effective amount of a compound of Formula I. Gene signatures correlated with successful treatment using these methods are also disclosed.
Type:
Grant
Filed:
June 4, 2018
Date of Patent:
January 21, 2020
Assignees:
Novartis AG, Sloan-Kettering Institute for Cancer Research
Inventors:
Dylan Daniel, Johanna Joyce, James Sutton
Abstract: Compounds of Formulae I? and I are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.
Type:
Grant
Filed:
January 16, 2017
Date of Patent:
December 31, 2019
Assignee:
Cyclerion Therapeutics, Inc.
Inventors:
Takashi Nakai, Joel Moore, Nicholas Robert Perl, Rajesh R. Iyengar, Ara Mermerian, G-Yoon Jamie Im, Thomas Wai-Ho Lee, Colleen Hudson, Glen Robert Rennie, Paul Allan Renhowe, Timothy Claude Barden, Xiang Y. Yu, James Edward Sheppeck, Karthik Iyer, Joon Jung, George Todd Milne, Kimberly Kafadar Long, Mark G. Currie, James Jia
Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.
Type:
Grant
Filed:
July 11, 2018
Date of Patent:
December 31, 2019
Assignee:
Incyte Corporation
Inventors:
Yun-Long Li, David M. Burns, Hao Feng, Joseph Glenn, Chunhong He, Song Mei, Jun Pan, Xiaozhao Wang, Yingda Ye
Abstract: Provided herein are methods of treating or ameliorating a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a pediatric liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 25, 2016
Date of Patent:
December 24, 2019
Assignee:
LUMENA PHARMACEUTIALS LLC
Inventors:
Bronislava Gedulin, Michael Grey, Niall O'Donnell