Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
Type:
Grant
Filed:
December 29, 2020
Date of Patent:
February 6, 2024
Assignee:
Siga Technologies, Inc.
Inventors:
Shanthakumar R. Tyavanagimatt, Melialani A. C. L. S. Anderson, William C. Weimers, Dylan Nelson, Tove' C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
Abstract: The present disclosure provides an antimicrobial substrate including a substrate and a polythiophene polymer. The polythiophene polymer has a number of repeated monomer units from n is 5-14 or 30 to 120, a number average molecular weight (Mn) from 1,000 to 4,000 or 10,000 to 40,000; and a polydispersity index (PDI) from 1 to 1.3. The present disclosure also provides the polythiophene polymer and uses thereof.
Type:
Grant
Filed:
September 23, 2021
Date of Patent:
January 30, 2024
Assignee:
UNM Rainforest Innovations
Inventors:
David G. Whitten, Dylan Brown, Jianzhong Yang, Edward Strach, Mohammed Khalil
Abstract: The present disclosure provides certain 3H,4H,5H,6H,7H-pyrimido[4,5-b][1,4]oxazine-4,6-dione derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.
Type:
Grant
Filed:
April 13, 2022
Date of Patent:
January 30, 2024
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Martin Thomas Fleck, Florian Paul Christian Binder
Abstract: A method for reducing the appearance of hyperpigmented skin is disclosed. The method can include topically applying to hyperpigmented skin of a person a composition that includes at least one of, at least two of, or all three of (i) an effective amount of Schinus terebinthifolius seed extract, (ii) an effective amount of a mixture comprising Ptychopetalum olacoides bark/stem extract, Pfaffia paniculata root extract, and Trichilia catigua bark extract, and/or (iii) an effective amount of a mixture comprising Himanthalia elongata extract and Undaria pinnatifida extract. Topical application of the composition can reduce the appearance of the hyperpigmented skin.
Abstract: A compound 7-(4-((5-(4-chlorobenzylideneamino)-2-thioxo-1,3,4-thiadiazol-3(2H)-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-inflammation agent.
Type:
Grant
Filed:
September 25, 2023
Date of Patent:
January 16, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Hany Mohamed Abd El-Latef Ahmed, Mai Mostafa Khalaf Ali, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
Abstract: The present invention relates to compounds of formula (I) and their use for treating or preventing a bacterial infection or as an antibacterial agent and/or as a ?-lactamase inhibitor.
Type:
Grant
Filed:
July 29, 2019
Date of Patent:
January 9, 2024
Assignee:
MUTABILIS
Inventors:
Julien Barbion, Audrey Caravano, Sophie Chasset, Francis Chevreuil, Frédéric Le Strat, Christophe Simon, Julie Brias, Rémi Lebel
Abstract: Pharmaceutical carriers which provide an environment of physical and chemical stability comprising a therapeutically effective amount of an active pharmaceutical ingredient (API) compound of structure I, one or more antioxidants, one or more chelators and a vehicle base comprising water and one or more pharmaceutically acceptable non-aqueous solvents, one or more absorption enhancers, one or more gelling agents and one or more pH buffering agents are described.
Type:
Grant
Filed:
June 6, 2017
Date of Patent:
January 9, 2024
Assignee:
LIPIDIO PHARMACEUTICALS INC.
Inventors:
Nigel R. A. Beeley, J. Gordon Foulkes, Kieran George Mooney, Charles Rodney Greenaway Evans, Keith Arthur Johnson, Howard G. Welgus, Celia P. Jenkinson
Abstract: The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto.
Abstract: Novel dual 5-LO inhibitors of well validated electrophilic Michael acceptors and nitrogen-heterocycles are presented and designed to maintain specific structural features of currently known dual 5-LO inhibitors and to overcome their drawbacks. The Michael acceptor scaffold will act as a carrier and will provide a stable anchorage via covalent binding to cysteine/histidine residues within the catalytic cleft and/or the surface interface of the 5-LO; whereas, the nitrogen-heterocycles will ensure the access to the Fe(II) catalytic center. These combinations offer potential for more than one mode of iron chelation and 5-LO inhibition.
Type:
Grant
Filed:
June 27, 2023
Date of Patent:
December 19, 2023
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Saadeldin Elsayed Ibrahim Shabaan, Hany Mohamed Abd El-Lateef Ahmed
Abstract: Problem to be solved: An object of the present invention is to provide a novel fat absorption inhibiting agent. Solution to the problem: The present invention provides a fat absorption inhibiting agent comprising pulverized defatted sesame seeds or a processed product thereof. The present invention also provides a fat absorption inhibiting agent comprising defatted sesame seeds having a 50th percentile particle size of 1 to 200 ?m as determined by laser diffraction/scattering and a compressibility index of 30 to 80%. The fat absorption inhibiting agent of the present invention preferably has lipase inhibitory activity. The present invention also provides a food comprising the agent. The present invention also provides defatted sesame seeds having a 50th percentile particle size of 1 to 200 ?m as determined by laser diffraction/scattering and a compressibility index of 30 to 80%.
Type:
Grant
Filed:
February 24, 2021
Date of Patent:
December 19, 2023
Assignees:
Pharma Foods International Co .. Ltd., Mitsui DM Sugar Co., Ltd.
Abstract: This application relates to the treatment of lysosomal storage disorders resulting from a deficiency of acid maltase and/or acid ?-glucosidase by administering active barley in comminuted form. Also disclosed are methods of replacing acid maltase and/or acid ?-glucosidase by administering active barley in comminuted form. Further disclosed are compositions for carrying out these methods.
Type:
Grant
Filed:
August 17, 2021
Date of Patent:
December 12, 2023
Assignee:
JME GROUP ASSOCIATES INC.
Inventors:
Frank Martiniuk, Elena Arvanitopoulos, John Arvanitopoulos, Angelo Kambitsis
Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain substituted 1-methyl-4-[(4-phenylphenyl)sulfonylmethyl]cyclohexanol and 1-methyl-4-[[4-(2-pyridyl)phenyl]sulfonylmethyl]cyclohexanol compounds (collectively referred to herein as CHMSA compounds) that are useful, for example, in the treatment of disorders (e.g., diseases) including, e.g., multiple myeloma, diffuse large B-cell lymphoma, acute myeloid leukemia, eosinophilic leukemia, glioblastoma, melanoma, ovarian cancer, chemotherapy resistant cancer, radiation resistant cancer, inflammatory arthritis, rheumatoid arthritis, psoriatic arthritis, psoriasis, ulcerative colitis, Crohn's disease, systemic lupus erythematosus (SLE), lupus nephritis, asthma, chronic obstructive pulmonary disease (COPD), non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), autoimmune hepatitis, hidradenitis suppurativa, etc.
Abstract: Compounds as STAT3 inhibitors are described. A pharmaceutical composition comprising the same, methods of making the same, and a method for treating or preventing conditions such as cancer, chronic inflammation, and fibrosis using the same, are described.
Type:
Grant
Filed:
April 18, 2019
Date of Patent:
November 28, 2023
Assignees:
Tvardi Therapeutics, Baylor College of Medicine
Abstract: Embodiments relate to a method for treatment of blepharitis in a patient in need thereof comprising administering to a subject in need thereof a pharmaceutical composition comprising a pharmaceutically effective amount of at least one cannabinoid, via the topical route. Optionally, the pharmaceutical composition is administered in combination with an additional agent selected from the group consisting of: an essential oil, a steroid, an antibiotic, an anti-parasitic, a disinfectant, an anesthetic, a terpene, a moisturizer and a vitamin.
Abstract: A method of attenuating, treating or preventing cognitive aging in an individual who does not have dementia includes administering to the individual a therapeutically effective amount of a composition containing an omega-3 fatty acid and choline. The method can achieve a benefit that is one or more of decreasing brain atrophy, increasing or maintaining number of synapses, increasing amyloid-? phagocytosis, or decreasing or maintaining neuroinflammation in the non-demented individual. The method can prevent dementia in an individual at risk thereof, for example an elderly human. The composition can be administered to the individual in a daily dose that provides 5.5 mg/day to 5,500 mg/day of the choline, for example 85 mg/day to 3,500 mg/day of the choline.
Type:
Grant
Filed:
September 29, 2017
Date of Patent:
November 14, 2023
Assignee:
Societe des Produits Nestle S.A.
Inventors:
Claus Rieker, Julie Hudry-Labbe, Jeroen Antonius Johannes Schmitt, Corina Boschat, Yvonne Beata Silber
Abstract: The present disclosure provides methods of treating COVID-19 by administering a pharmaceutical composition providing inhibition of severe acute respiratory syndrome-coronavirus 2 (SARS-CoV-2) main protease (MPro) in a patient. The disclosure also provides other methods as well as pharmaceutical formulations for use in treating COVID-19 patients.
Type:
Grant
Filed:
May 19, 2022
Date of Patent:
November 7, 2023
Assignee:
THE TEXAS A&M UNIVERSITY SYSTEM
Inventors:
Wenshe Liu, Kai Yang, Erol Vatansever, Shiqing Xu
Abstract: Described herein is the use of a LOXL2 inhibitor in the treatment or prevention of conditions, diseases, or disorders associated with LOXL2 activity.
Type:
Grant
Filed:
September 6, 2017
Date of Patent:
October 24, 2023
Assignee:
PHARMAKEA, INC.
Inventors:
Gretchen Bain, Jillian Frances Evans, Deidre A. Mackenna, John Howard Hutchinson
Abstract: Compounds that are inhibitors of retinoic acid inducible P450 (CYP26) enzymes. The compounds have retinoid activity, are resistant to CYP26-mediated catabolism, act as inhibitors of CYP26B1, and are used for treating diseases that are responsive to retinoids.
Type:
Grant
Filed:
December 12, 2018
Date of Patent:
October 24, 2023
Assignee:
Queen's University at Kingston
Inventors:
Donald Andrew Cameron, Martin Petkovich, Uttam Saha
Abstract: Disclosed herein are methods for increasing circulating mesenchymal stem cells by administering a compound having the general formula 1 as defined herein, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
August 9, 2018
Date of Patent:
October 17, 2023
Assignee:
University of Southern California
Inventors:
Kevin J. Gaffney, Kathleen E. Rodgers, Maira Soto, Michael Weinberg
Abstract: The present invention relates to the field of prostate cancer treatment, and in particular the field of prostate cancer treatment by Androgen Deprivation Therapy (ADT). The present treatment involves oral administration of an estetrol component in conjunction with ADT.