Abstract: The invention provides a method of inhibiting a TYK2 kinase, which method comprises bringing into contact with the TYK2 kinase an effective TYK2 kinase-inhibiting amount of a compound having the formula (0): or a salt or stereoisomer thereof. The invention also provides a novel subset of compounds within formula (0) as well as pharmaceutical compositions containing them and their use in medicine.
Abstract: This application relates generally to certain substituted pyrrolizine compounds, and pharmaceutical compositions which inhibit HBV replication, and methods of making and using them.
Type:
Grant
Filed:
May 3, 2019
Date of Patent:
December 29, 2020
Assignee:
GILEAD SCIENCES, INC.
Inventors:
Jinfa Du, Joshua A. Kaplan, Thorsten A. Kirschberg, Tetsuya Kobayashi, Scott E. Lazerwith, Rick Andrew Lee, Jonathan William Medley, Michael L. Mitchell, Philip Anthony Morganelli, Hyung-Jung Pyun, Sophia L. Shevick, Neil H. Squires, William J. Watkins
Abstract: Lonafarnib and ritonavir, or a pharmaceutically acceptable salt thereof, are used in combination to treat HDV infection. In one aspect, amorphous co-precipitates comprising lonafarnib, ritonavir, and a co-polymer are provided.
Abstract: This invention relates to the use of the phytocannabinoid cannabidivarin (CBDV) and combinations of the phytocannabinoid CBDV with tetrahydrocannabivarin (THCV) and cannabidiol (CBD) in the treatment of epilepsy. The invention further relates to the use of the phytocannabinoid CBDV in combination with standard anti-epileptic drugs (SAEDs). Preferably the SAED is one of ethosuximide, valproate or phenobarbital.
Abstract: The invention provides a compound of formula (I): or a salt thereof, wherein R1-R5 have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as RNA polymerase inhibitors and antibacterial agents.
Abstract: Topical dosages and formulations of chloroprocaine and pharmaceutically acceptable salts thereof are provided that are efficacious, chemically stable and physiologically balanced for safety and efficacy, particularly during ophthalmic procedures or in response to ophthalmic abrasions or trauma.
Type:
Grant
Filed:
September 14, 2018
Date of Patent:
October 6, 2020
Assignee:
Sintetica S.A.
Inventors:
Augusto Mitidieri, Elisabetta Donati, Clara Bianchi
Abstract: The present invention relates to compositions and methods for the treatment of amyotrophic lateral sclerosis. More specifically, the present invention relates to novel combinatorial therapies for treating amyotrophic lateral sclerosis or a related disorder.
Type:
Grant
Filed:
February 15, 2019
Date of Patent:
June 16, 2020
Assignee:
PHARNEXT
Inventors:
Daniel Cohen, Serguei Nabirochkin, Ilya Chumakov, Rodolphe Hajj
Abstract: The invention provides, inter alia, fatty acyl hydroxy fatty acid (FAHFA; a novel class of estolide-related molecules) and diagnostic and treatment methods for a variety of disorders—including diabetes-related disorders, Metabolic Syndrome, polycystic ovarian syndrome, cancer, and inflammatory disorders—using them; as well as methods of screening for additional compounds that are useful in treating these disorders and/or that modulate FAHFA levels, FAHFA-mediated signaling, and FAHFA-mediated biological effects.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
March 31, 2020
Assignees:
Beth Israel Deaconess Medical Center, Inc., President and Fellows of Harvard College
Inventors:
Barbara B. Kahn, Mark A. Herman, Alan Saghatelian, Edwin Homan
Abstract: A method of treating age-related macular degeneration. The method includes the step of administering orally or parenterally an effective amount of aurin tricarboxylic acid, aurin quadracarboxylic acid, and/or aurin hexacarboxylic acid, wherein the method excludes administration of components of aurin tricarboxylic acid complex of greater than or equal to 1 kilodalton in molecular weight.
Abstract: Water-based formulations (EW) are provided containing no VOC's or alternatively are low in VOC's for wide area space spray to control mosquitoes, flies, and other public health pests. Application via ULV, these formulations have been observed to provide significantly superior control of pests when compared to competitive adulticides. The present formulations provide exceptional preservation of both droplet density in the spray cloud and droplet size as measured by volume mean diameter (VmD). The present formulations provide superior bio-efficacy as measured by both mortality and knockdown of target organisms. The present formulations provide superior biological control, droplet density, and droplet size when applied at concentrations 20-80× less than competitive formulations.
Type:
Grant
Filed:
August 2, 2016
Date of Patent:
March 17, 2020
Inventors:
Robert Britt Baker, Kurt P. Vandock, Gary Gore, Byron Reid
Abstract: The instant invention provides for novel catiome lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.
Type:
Grant
Filed:
May 10, 2017
Date of Patent:
March 3, 2020
Assignee:
SIRNA THEREAPEUTICS, INC.
Inventors:
Matthew G. Stanton, Brian W. Budzik, Gregory L. Beutner, Hongbiao Liao
Abstract: A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; X=C, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.
Type:
Grant
Filed:
November 30, 2016
Date of Patent:
February 25, 2020
Assignees:
RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY, LEHIGH UNIVERSITY
Inventors:
Jeffrey D. Laskin, Diane E. Heck, Mou-Tuan Huang, Karine Fabio, Carl J. Lacey, Sherri C. Young, Pramod Mohanta, Christophe Guillon, Ned D. Heindel
Abstract: The present invention provides novel compositions and methods for using the insect neuromodulator tyramine and/or one or more derivatives thereof delivered to insect populations to control certain aspects of such populations. The amount of tyramine and/or one or more derivatives thereof delivered on a per insect basis is significantly greater than a naturally-occurring amount of tyramine normally found in insects and causes deleterious effects including mortality of certain insect life forms and disruption of the reproductive capacity of others in the population.
Type:
Grant
Filed:
February 28, 2018
Date of Patent:
February 25, 2020
Assignees:
The United States of America, as represented by the Secretary of Agriculture, Foresight Science & Technology Inc.
Abstract: Invasive fungal infections present a formidable global public health challenge due to the limited number of approved antifungal agents and the emergence of resistance to the frontline treatment options, such as fluconazole. Three fungal pathogens of significant concern are Candida, Cryptococcus, and Aspergillus given their propensity to cause opportunistic infections in immunocompromised individuals. This disclosure provides a set of aryl isonitrile compounds that possess broad-spectrum antifungal activity primarily against species of Candida and Cryptococcus. The most potent derivatives are capable of inhibiting growth of these key pathogens at concentrations as low as 0.5 ?M. Remarkably, the most active compounds exhibit an excellent safety profile and are non-toxic to mammalian cells even at concentrations up to 256 ?M.
Type:
Grant
Filed:
March 13, 2017
Date of Patent:
October 22, 2019
Assignee:
Purdue Research Foundation
Inventors:
Kwaku Kyei-Baffour, Mohamed Seleem, Mingji Dai, Haroon Taj Mohammad
Abstract: Disclosed herein are methods of treating subjects suffering from estrogen receptor positive cancer of the brain by administering a selective estrogen receptor degrader (SERM). Also disclosed are methods of treating a cancer that is resistant to an estrogen receptor modulator by administering a SERM.
Type:
Grant
Filed:
March 28, 2015
Date of Patent:
September 24, 2019
Assignee:
Duke University
Inventors:
Suzanne E. Wardell, Erik R. Nelson, Donald P. McDonnell
Abstract: A new compound composition that is free of a side effect to a liver and used for alleviating the toxicity of an acetaminophen (APAP) medicament to the liver. The compound composition comprises (a) a pharmaceutically effective amount of acetaminophen and (b) a frequently-used safe and pharmaceutically acceptable excipient that can be combined with one or more than two medicaments that can reduce the toxicity of a drug via liver enzyme CYP2E1 metabolism to the liver.
Type:
Grant
Filed:
November 13, 2013
Date of Patent:
September 24, 2019
Assignee:
NATIONAL DEFENSE EDUCATION AND RESEARCH FOUNDATION
Abstract: A pharmaceutic composition for treating an allergic skin disorder. It has an active component and a carrier. The active component has a major active ingredient osthol and a group of minor active ingredients: xanthotoxol, xanthotoxin, isopimpinellin, bergapten, and imperatorine. The major active ingredient osthol accounts for at least 90% by weight of the active component, which accounts for 5-35% by weight of the overall pharmaceutic composition.
Abstract: The present invention provides aryl isonitrile compounds that have antibacterial properties. More specifically, the aryl isonitrile compounds of the present invention are potent inhibitors of drug resistant strains of Staphylococcus aureus.
Type:
Grant
Filed:
April 4, 2016
Date of Patent:
July 30, 2019
Assignee:
Purdue Research Foundation
Inventors:
Mohamed Seleem, Mingji Dai, Dexter Cameron Davis, Haroon Taj Mohammad