Abstract: Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed.
Type:
Grant
Filed:
February 1, 2021
Date of Patent:
August 15, 2023
Assignee:
Aldeyra Therapeutics, Inc.
Inventors:
Thomas A. Jordan, John E. Dowling, John Clifford Chabala
Abstract: The present invention discloses an improved process for extracting cholesterol in high yield and purity from fish oil waste residue. The so obtained cholesterol of pharmaceutical grade is useful as a precursor for the preparation of vitamin D3.
Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.
Type:
Grant
Filed:
February 26, 2021
Date of Patent:
August 8, 2023
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Guoqiang Wang, Yat Sun Or, Ruichao Shen, Jiang Long, Peng Dai, Xuechao Xing, Jing He
Abstract: The present invention includes a composition and method of producing aspirin in situ, the method comprising: identifying a subject in need of aspirin or aspirin-like compounds; and providing the subject with a composition comprising: a source of methyl salicylate, an acetyl donor, and L-Arginine, wherein the composition is effective to produce aspirin-triggered resolvins in the subject without the deleterious effect of the aspirin or aspirin-like compounds in the stomach.
Abstract: A method of managing non-infective nasal symptoms may include combining a steroid with a diluent, and acetylcysteine, azelastine, or theophylline. The combined ingredients may be mixed to formulate a topical composition for intranasal irrigation or nebulization. The steroid may include fluticasone, budesonide, or methylprednisolone.
Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
Type:
Grant
Filed:
December 8, 2020
Date of Patent:
May 9, 2023
Assignee:
GENENTECH, INC.
Inventors:
Andreas Stumpf, Remy Angelaud, Andrew McClory, Herbert Yajima, Chudi Ndubaku, Alan Olivero
Abstract: The present invention is directed to cell-protective, in particular, cardio- and renal-protective organic compounds, preferably to organic compounds that inhibit substrate phosphorylation by the G-protein-coupled receptor kinase 2 (GRK2, ADRBK1). Preferably, the organic compounds inhibit the GRK2-mediated phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1, ASF-1, SF2) and/or phosducin for treating hypertension, heart diseases, heart dysfunction or failure and heart disease-associated pathologies, e.g. cardiomyocyte necrosis, ischemic cardiac disease and/or ischemic heart damage or ageing. Furthermore, the present invention is directed to a method for the identification of inhibitors of the (GRK2)-mediated phosphorylation of (SRSF1) and/or phosducin.
Type:
Grant
Filed:
January 10, 2018
Date of Patent:
April 18, 2023
Assignee:
ETH ZURICH
Inventors:
Joshua Abd Alla, Stefan Wolf, Ursula Quitterer
Abstract: The present invention provides a compound of Formula I: wherein R1 is H, halogen, C1-C3 alkyl, or C1-C3 alkoxy; R2 is H or halogen; and X is O, OCH2, or CH2, or a pharmaceutically acceptable salt thereof, wherein the compound of Formula I, or pharmaceutically acceptable salt thereof is useful for treating autoimmune and inflammatory diseases, such as atopic dermatitis, rheumatoid arthritis, and lupus nephritis.
Type:
Grant
Filed:
March 22, 2022
Date of Patent:
April 4, 2023
Assignee:
Eli Lilly and Company
Inventors:
Ryan Edward Stites, Jacqueline Mary Wurst
Abstract: The present invention relates to oral extended release composition, comprising memantine or its pharmaceutically acceptable salt as an active ingredient, resin complexation ingredient, release retardant, extended release coating system and the composition further comprising diluents, viscosity increasing agents, glidants, sweeteners, stabilizing agents, preservatives and other pharmaceutically acceptable excipients, wherein the drug-resin complex and drug-resin complex matrix particulates and coated drug-resin complex particulates have the specific particle size range. The present invention also relates to a process for the preparation of memantine or its salt oral extended release composition comprising the steps of drug-resin complexation, matrix resinate/particulates preparation process followed by extended release coating.
Abstract: The present invention includes DNP derivatives that are useful for preventing or treating a metabolic disease or disorder in a subject in need thereof. In certain embodiments, the subject is further administered at least one additional therapeutic agent.
Abstract: Disclosed herein are C4 modified oleanolic acid derivatives of the formula: Formula (X) or Formula (XII), as well as analogs thereof, wherein the variables are defined herein. In addition, disclosed herein are pharmaceutical compositions of these derivatives or analogs, methods for their manufacture, and methods for their use, including for the prevention and treatment of diseases or disorders associated with overproduction of IL-17.
Type:
Grant
Filed:
September 23, 2016
Date of Patent:
February 21, 2023
Assignee:
REATA PHARMACEUTICALS, Inc.
Inventors:
Melean Visnick, Xin Jiang, Martha R. Hotema, Chitase Lee, Bradley William Caprathe, William H. Roark, Gary L. Bolton
Abstract: The present disclosure relates to a method for delivering a mucoadhesive composition to the oral cavity of a subject. The mucoadhesive composition comprises one or more active agents, a mucoadhesive polymer, and water. The present disclosure is further related to a method for treating a disease, disorder, or condition, such as pharyngitis, aphthous stomatitis (canker sore), bacterial infection, radiation-induced mucositis, fibromyalgia, and diabetes, comprising administering the mucoadhesive composition to the oral cavity of a subject. The present disclosure is also related a mucoadhesive composition comprising one or more active agents, a mucoadhesive polymer, and water.
Abstract: The present invention relates to a method for preparing 7?-methyl-19-aldehyde-4-androstene-3,17-dione by electrocatalytic oxidation. The method specifically includes: adopting an H-shaped electrolytic cell for reaction, in an anode chamber, using a metal oxide catalyst as a working electrode, using 7?-methyl-17,19-dihydroxy-4-androstene-3-one as a reaction substrate, and dissolving it in a mixed solvent to be used as an anolyte, and adding nitroxide radicals to be used as a medium; and in a cathode chamber, using a platinum sheet as a counter electrode, using a weakly alkaline solution as a catholyte, carrying out an electrocatalytic oxidation reaction in a constant temperature water bath, adding an organic solvent at the end of the reaction for extraction to obtain an organic extract liquor, and taking an organic layer and carrying out distilling under a reduced pressure to obtain 7?-methyl-19-aldehyde-4-androstene-3,17-dione.
Type:
Grant
Filed:
December 1, 2021
Date of Patent:
February 14, 2023
Assignee:
ZHEJIANG UNIVERSITY OF TECHNOLOGY
Inventors:
Jianguo Wang, Suiqin Li, Xing Zhong, Jiahui He
Abstract: A small molecule compound IODVA1 has been found to have cellular inhibitory activity against several transformed cell lines including Ras-driven cells. IODVA1 decreases cell-cell and cell-extra cellular matrix interactions and reduces growth of Ras-driven tumors. Applicants also synthesized compound NIRA2 and showed in vitro and in vivo efficacy and potency against models of Ph+(BCR-ABL1) B-ALL and of colon adenocarcinoma xenografts.
Type:
Grant
Filed:
May 1, 2020
Date of Patent:
January 31, 2023
Assignee:
Children's Hospital Medical Center
Inventors:
Nicolas Nassar, William Seibel, Anjelika Gasilina, Jose Cancelas
Abstract: The invention provides compositions, formulations, and methods for treatment of malignancies via activation of an inflammatory response in the subject. Such compositions, formulations, and methods for are preferably used in conjunction with other therapies for the treatment and/or management of malignancies, e.g., chemotherapy and/or radiation. The invention also provides methods of monitoring immune activation in subjects with malignancies.
Abstract: Described herein is the chemical structure of neurosteroid derivative compounds, methods of synthesizing the derivatives, and their uses in treating disorders, including those of the central nervous system. These compounds are readily synthesized and have improved pharmaceutical properties, including water solubility, compared to known neurosteroids.
Abstract: A method of treating Alcohol Use Disorder (AUD), Substance Use Disorder (SUD), tobacco use, pain, or proinflammatory disorders comprising: providing a subject with an effective amount of a modified tetracycline or derivative thereof to ameliorate or eliminate the AUD, SUD, tobacco use, pain, or proinflammatory disorder, and wherein the modified tetracycline or derivative thereof has reduced binding to a microbial ribosome and has the formula wherein R1 is acetyl, R2 is OH or acetyl, R3 is acetyl, R4 is H or acetyl, and R5 is acetyl.
Type:
Grant
Filed:
June 13, 2019
Date of Patent:
January 3, 2023
Assignee:
Texas Tech University System
Inventors:
Susan E. Bergeson, Peter Syapin, Ted W. Reid, Mayank Shashtri, Phat Tran
Abstract: Disclosed herein are novel compounds and methods for the treatment of acute organ injury, including injuries resulting from ischemic events. The compounds may be used to treat organ including the brain, heart, or kidney, which have injured as a result of events such as stroke, cardiac arrest, traumatic brain injury, hemorrhagic shock, or subarachnoid hemorrhage.
Type:
Grant
Filed:
September 26, 2019
Date of Patent:
December 27, 2022
Assignee:
University of Pittsburgh—of the Commonwealth System of Higher Education
Abstract: The invention relates to compounds of general formula (I): wherein R2a, R2b, R3a, R3b, R5, Y and R7 are as defined herein are selective agonists at the FXR receptor and are useful for the treatment or prevention of diseases and conditions including nonalcoholic steatohepatitis (NASH); primary biliary cirrhosis; primary sclerosing cholangitis; biliary atresia; cholestatic liver disease; hepatitis C infection; alcoholic liver disease; fibrosis; and liver damage arising from fibrosis.
Type:
Grant
Filed:
July 30, 2019
Date of Patent:
December 6, 2022
Assignees:
NZP UK LIMITED, THE UNIVERSITY OF SOUTHAMPTON
Inventors:
Alexander Charles Weymouth-Wilson, Gemma Packer, Bruno Jan Pol Linclau, Dannielle Kydd-Sinclair, Kimberly Ann Watson