Abstract: The invention relates to compounds exhibiting kallikrein inhibitory activity, and to compositions comprising at least one of these compounds for use in the treatment of diseases or disorders in which kallikrein activity is dysregulated, particularly neurodegenerative and inflammatory diseases.
Type:
Grant
Filed:
February 13, 2019
Date of Patent:
January 3, 2023
Assignees:
SARBONNE UNIVERSITE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE, ASSISTANCE PUBLIQUE—HÔPITAUX DE PARIS, INSTITUT DU CERVEAU ET DE LA MOELLE EPINIERE, UNIVERSITÉ DE MONTPELLIER, ECOLE NATIONALE SUPERIEURE DE CHIMIE DE MONTPELLIER
Inventors:
Chahrazade El Amri, Feryel Soualmia, Nicolas Masurier, Sabrina Aït Amiri, Brahim Nait Oumesmar, Cyrille Deboux
Abstract: The present invention relates to a method of preparing a composition comprising ferulic acid. An aspect of the invention is a composition comprising hydrolysed wheat bran for use in the treatment or prevention of metabolic disease.
Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Type:
Grant
Filed:
September 21, 2020
Date of Patent:
December 27, 2022
Assignee:
CELGENE QUANTICEL RESEARCH, INC
Inventors:
Amogh Boloor, Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
Abstract: The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.
Type:
Grant
Filed:
April 2, 2020
Date of Patent:
December 27, 2022
Assignee:
Massachusetts Institute of Technology
Inventors:
Mohammad Movassaghi, Chase Robert Olsson, Tony Z. Scott, Jaime Cheah, Joshua Nathaniel Payette
Abstract: The invention relates to inhibitors of dihydrofolate reductase and pharmaceutical preparations thereof. The invention further relates to methods of treatment of parasitic infections, such as T. gondii, T. cruzi, P. falciparum, T. brucei, or L. major infections, using the novel inhibitors of the invention.
Type:
Grant
Filed:
September 10, 2020
Date of Patent:
December 20, 2022
Assignee:
Vyera Pharmaceuticals, LLC
Inventors:
Stephen B. Thomas, Allen T. Hopper, Matthew Welsch
Abstract: Substituted Pyrazolo-pyridines as GluN2B receptor ligands. Such compounds may be used in GluN2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by GluN2B receptor activity.
Type:
Grant
Filed:
June 12, 2020
Date of Patent:
December 20, 2022
Assignee:
JANSSEN PHARMACEUTICA NV
Inventors:
Afton Hiscox, Brice Stenne, Christa Chrovian, Christine Gelin, Andrew Samant, Michael A. Letavic, Curt Dvorak
Abstract: The invention provides alkyne substituted quinazoline compounds, such as compounds of the formula (I), which are irreversible ErbB kinase inhibitors. The compounds are useful in the treatment of diseases and disorders where ErbB kinase activity is implicated such as a hyperproliferative disorder (e.g., cancer).
Type:
Grant
Filed:
March 27, 2020
Date of Patent:
December 13, 2022
Assignee:
Newgen Therapeutics, Inc.
Inventors:
Wang Shen, Aimin Zhang, Jack Maung, Xiaoling Zheng
Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
Type:
Grant
Filed:
September 14, 2020
Date of Patent:
December 6, 2022
Assignee:
ALKERMES PHARMA IRELAND LIMITED
Inventors:
Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
Abstract: A P2Y12 receptor antagonist containing a guanidyl, and a preparation method and the use thereof. In particular, the present disclosure provides a pyridazinone-guanidine compound that is a compound of structural formula (I), or a stereoisomer of the above-mentioned compound, a pro-drug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof. Such a compound has multiple pharmacological activities, especially has an inhibitory effect on platelet aggregation, and can be used for preparing an anti-platelet aggregation pharmaceutical composition.
Type:
Grant
Filed:
November 25, 2020
Date of Patent:
November 29, 2022
Assignee:
Anhui New Star Pharmaceutical Development Co., Ltd
Abstract: A genus of dihydropyridine chemical modulators of synaptojanin is disclosed. These modulators are selective inhibitors of synaptojanin 1 and may be used to treat cognitive impairment or traumatic brain injury, including promoting regeneration in cases of traumatic brain injury, or for treating neurodegenerative disorders.
Type:
Grant
Filed:
November 20, 2018
Date of Patent:
November 29, 2022
Assignees:
Icahn School of Medicine at Mount Sinai, The United States Government as Represented by the Department of Veterans Affairs
Abstract: Compounds and compositions for modulating fibroblast activation protein (FAP) are described. The compounds and compositions may find use as therapeutic agents for the treatment of diseases, including hyperproliferative diseases.
Type:
Grant
Filed:
December 21, 2019
Date of Patent:
November 22, 2022
Assignee:
PRAXIS BIOTECH LLC
Inventors:
Brahmam Pujala, Dayanand Panpatil, Sebastian Bernales, Sebastian Belmar, Gonzalo Andrés Ureta Díaz
Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
Abstract: The present invention covers new quinoline compounds of general formula (I): in which A, R1, R2, R3, R4, R5, R6, and Q 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, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.
Type:
Grant
Filed:
October 30, 2020
Date of Patent:
November 22, 2022
Assignee:
Bayer Animal Health GmbH
Inventors:
Walter Hübsch, Johannes Köbberling, Adeline Köhler, Hans-Georg Schwarz, Daniel Kulke, Claudia Welz, Thomas Ilg, Kirsten Börngen, Wei Zhuang, Nils Griebnow, Claudia Böhm, Niels Lindner, Maike Hink, Ulrich Görgens
Abstract: Topical compositions and methods for using topical compositions comprising tapinarof to treat mild to moderate atopic dermatitis are described herein. Also described are clinical endpoints for treatment of subjects diagnosed with mild to moderate atopic dermatitis, wherein about 5% to about 35% of body surface area was affected, and Investigator Global Assessment (IGA) score was greater than or equal to 3.
Abstract: A number of crystalline forms of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-y1)phenyl)acrylamide are provided. These include a crystalline free base form, a crystalline monohydrochloride salt form, a crystalline dihydrochloride salt form, and a crystalline ethanesulfonate salt form. Methods of making and using crystalline compounds are also provided.
Type:
Grant
Filed:
December 20, 2019
Date of Patent:
November 15, 2022
Assignee:
EISAI R&D MANAGEMENT CO., LTD.
Inventors:
George Moniz, Kristen Sanders, Arani Chanda, Kenshi Yoshida, Ming-Hong Hao, Dominic Reynolds, Sudeep Prajapati, Anand Selvaraj, Takashi Satoh, John Wang
Abstract: The present invention provides methods and compositions for treating and preventing lung injuries due to or associated with coronavirus infections that cause Severe Acute Respiratory Syndrome, including COVID-19. More specifically the present invention provides methods for treating or preventing the lung injuries associated with SARS-CoV-2 infections, such as acute lung injury (ALI), lung fibrosis, and acute respiratory distress syndrome (ARDS). The methods comprise administering a therapeutically effective amount of a pharmaceutical composition comprising a protein kinase inhibitor compound having MAP3K2/MAP3K3 inhibition activity, such as pazopanib or nintedanib, or a pharmaceutically acceptable salt, solvate, or prodrug thereof, to a patient in need thereof. The present invention also provides devices for administering the compositions.
Abstract: The present invention relates to a method for treating or preventing obesity in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of certain carbamate compounds. The invention further relates to methods for reducing body weight and/or reducing food intake in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of certain carbamate compounds.
Type:
Grant
Filed:
September 22, 2020
Date of Patent:
November 15, 2022
Assignees:
Axsome Malta Ltd., SK Biopharmaceuticals Co., Ltd.
Inventors:
Moise A. Khayrallah, Gary Bream, Stephen E. Butts
Abstract: Provided herein are novel barbituric acid derivatives, their synthesis and use thereof in blocking leukocyte transmigration. The novel barbituric acid derivatives are useful for the treatment of disorders associated with leukocyte transmigration, such as for example inflammatory diseases and disorders, autoimmune diseases and disorders, and cancers.
Type:
Grant
Filed:
August 30, 2018
Date of Patent:
November 8, 2022
Assignees:
BAR-ILAN UNIVERSITY, UNIVERSITY OF GENEVA, GENEVA UNIVERSITY HOSPITALS
Inventors:
Arie Lev Gruzman, Paul Bradfield, Tamar Getter, Beat Imhof, Thomas Matthes, Hanoch Senderowitz
Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.