Abstract: The present invention aims to provide a compound acting as a specific agonist for LPA4 receptors, and a pharmaceutical composition containing the compound. The present invention relates to a novel lysophosphatidic acid derivative having an agonistic action on LPA4 receptors and useful for the prophylaxis and/or treatment of diseases associated with angiogenesis abnormalities involving LPA4 receptors, diseases associated with vascular disorders, or the symptoms associated therewith, and a pharmaceutical composition containing the derivative.
Type:
Grant
Filed:
November 3, 2021
Date of Patent:
October 31, 2023
Assignees:
MITSUBISHI TANABE PHARMA CORPORATION, OSAKA UNIVERSITY
Abstract: The present disclosure is directed toward uses of compound 1 (or its stereoisomers) and compositions and/or dosage forms containing compound 1: or a pharmaceutically acceptable salt thereof. Some uses of Compound 1 and/or its stereoisomers include treating a variety of diseases and disorders, including pain, depression, and schizophrenia. In some embodiments, Compound 1 and/or its stereoisomers may be useful in the treatment of a substance use disorder while inducing fewer withdrawal symptoms than a standard-of-care opioid addiction treatment.
Abstract: The present invention relates to the use of 7-hydroxy-cannabidol (7-OH-CBD) and/or 7-hydroxy-cannabidivarin (7-OH-CBDV) in the treatment of epilepsy. Preferably the cannabinoid metabolites are isolated from plants to produce a highly purified extract or can be reproduced synthetically.
Type:
Grant
Filed:
September 10, 2021
Date of Patent:
October 24, 2023
Assignee:
GW Research Limited
Inventors:
Colin Stott, Nick Jones, Benjamin Whalley, Gary Stephens, Claire Williams
Abstract: The present invention relates to a composition comprising, in a physiologically acceptable medium: a) at least one saccharide, b) at least one amino acid, c) DMSO or at least one C3-C5 alkanediol, d) at least one antioxidant, and e) cells for therapeutic purposes, said composition having a pH between 7.0 and 8.5, preferably between 7.0 and 8.3. It also relates to a method for the cryopreservation of at least one sample of cells for therapeutic purposes, comprising the following steps: i) mixing the sample of cells for therapeutic purposes with ingredients a) to d) above and a physiologically acceptable medium, so as to obtain a composition having a pH between 7.0 and 8.5, preferably between 7.0 and 8.3, then ii) freezing the composition obtained in step i).
Type:
Grant
Filed:
November 27, 2018
Date of Patent:
October 17, 2023
Assignee:
Laboratoire Francais du Fractionnement et des Biotechnologies
Inventors:
Joffrey De Larichaudy, Sandy Cazalon Nemorin
Abstract: The invention provides methods of chemical synthesis of the pharmacological agent 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate, also called CV-8972. The methods entail formation of a free base form of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethanol, also called CV-8814, as intermediate without producing a salt form of CV-8814.
Type:
Grant
Filed:
June 28, 2021
Date of Patent:
October 10, 2023
Assignee:
IMBRIA PHARMACEUTICALS, INC.
Inventors:
Neil Buckley, Dan Belmont, Bryan Hauser, Myoung Goo Kim, Kumar Kannan
Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.
Type:
Grant
Filed:
May 18, 2021
Date of Patent:
October 3, 2023
Assignee:
SRX CARDIO, LLC
Inventors:
Thomas E Barta, Jonathan W Bourne, Kyle D Monroe, Michael M Muehlemann
Abstract: The present invention provides dihydrooxydiazinone compounds of general formula (I) in which R1, R2, R3, and R4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.
Type:
Grant
Filed:
July 14, 2022
Date of Patent:
October 3, 2023
Assignees:
Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
Inventors:
Manuel Ellermann, Stefan Nikolaus Gradl, Charlotte Christine Kopitz, Martin Lange, Adrian Tersteegen, Philip Lienau, Christa Hegele-Hartung, Detlev Sülzle, Timothy A. Lewis, Heidi Greulich, Xiaoyun Wu, Matthew Meyerson, Alex Burgin
Abstract: Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
Type:
Grant
Filed:
June 16, 2021
Date of Patent:
October 3, 2023
Assignee:
ORGANOVO, INC.
Inventors:
Nicholas D. Smith, Steven P. Govek, Karensa L. Douglas, Andiliy G. Lai
Abstract: The present disclosure provides 1) an enantiomerically purified compound SRR G-1, or a derivative thereof, including specific crystal forms, salts and co-crystals that modulates G protein-coupled estrogen receptor activity, 2) pharmaceutical and cosmetic compositions comprising an enantiomerically purified SRR G-1, or a derivative thereof, and 3) methods of treating or preventing disease states and conditions and cosmetic conditions mediated through these receptors and related methods thereof in humans and animals.
Type:
Grant
Filed:
February 25, 2021
Date of Patent:
September 19, 2023
Assignee:
Linnaeus Therapeutics, Inc.
Inventors:
Christopher Natale, Patrick T. Mooney, Tina Garyantes, Wayne Luke
Abstract: The present invention features pharmaceutical compositions including sepiapterin, or a pharmaceutically acceptable salt and/or co-crystal thereof, and methods for the treatment of tetrahydrobiopterin-related disorders (e.g., tetrahydrobiopterin deficiency or phenylketonuria) with such compositions.
Abstract: Disclosed are methods and compositions which may be used in human cytochrome P450 (CYP450) enzyme phenotyping. The methods and compositions typically utilize substrate for CYP3A5 comprising eplerenone which may be administered orally to a subject. Subsequently, metabolites of eplereone may be detected in the subject's saliva as well as any non- metabolized eplerenone to calculate a metabolic ratio for CYP3A5 enzyme in order to generate a phenytopic CYP3A5 enzyme profile for the subject.
Abstract: The present invention relates to compounds of formula (I) or (II) pharmaceutically acceptable salts, solvates, tautomers, stereoisomers thereof, including enantiomers, diastereomers, racemic mixtures, mixtures of enantiomers, or combinations thereof, and pharmaceutical uses of the compounds.
Type:
Grant
Filed:
April 18, 2019
Date of Patent:
September 5, 2023
Assignees:
EÖTVÖS LORÁND TUDOMÁNYEGYETEM, PRINTNET KERESKEDELMI ÉS SZOLGÁLTATÓ KFT.
Inventors:
András Málnási-Csizmadia, Maté Gyimesi, András Szabó, Péter Hári, Suthar Sharad Kumar, Mihály Kovács, Ádám István Horváth, Máté Pénzes, István Lörincz, László Végner, Zoltán Simon, Sándor Bátori, Zoltán Szönyegi, Vajk Horváth, József Répási
Abstract: Hydantoin based compounds useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Also described are related compositions and methods of using the compounds to inhibit MMP-12 and treat diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis.
Abstract: The stable liquid formulations for parenteral administration include fentanyl or a pharmaceutically acceptable salt thereof. The formulations include a diluent and buffer, either containing sodium, in an aqueous solution that has a pH of about 3 to about 4.5. The parenteral liquid formulations are stable formulations that are supplied as a ready-to-administer product in an infusion container or bag. The stable formulations are terminally sterilized in the infusion container. The stable formulations are suitable for administration to a patient in need of therapy with fentanyl or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
November 17, 2021
Date of Patent:
August 29, 2023
Assignee:
HIKMA PHARMACEUTICALS INTERNATIONAL LIMITED
Inventors:
Andrew Conrad, Ragheb Al-Shakhshir, Ragheb AbuRmaileh
Abstract: A novel abyssomicin analogue compound and method of synthesizing the novel abyssomicin analogue compound are provided. The synthesis method includes the novel abyssomicin analogue compound being simply produced from a mixture of water and a co-solvent with linear precursors. The water molecules in the synthesis method can have dual roles, which are cyclisation followed by hydration via a unique mechanism. Abyssomicins are a family of spirotetronate natural products exhibiting promising bioactivities.
Abstract: The invention relates to particular substituted deuterated heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.
Abstract: An organic molecule, is disclosed having: one first chemical moiety with a structure of formula I: and one second chemical moiety with a structure of formula II: wherein the first chemical moiety is linked to the second chemical moiety via a single bond; and one third chemical moiety with a structure of Formula III: wherein the first chemical moiety is linked to the third chemical moiety via a single bond.