Abstract: The present invention relates to compounds of formula (I) that are capable of modulating, e.g., inhibiting or activating, one or more kinases, especially LRRK2 and/or NUAK1 and/or TYK2 or mutants thereof. The compounds are useful for treating diseases, such as autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, Alzheimer's disease, Parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 40 to 146; examples 1 to 63; compounds 1 to 248; tables 1 to 3). Preferred compounds are e.g. 1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds. An exemplary compound is e.g. 5-(2,6-difluorophenyl)-8-methoxy-1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine (example 49).
Type:
Grant
Filed:
September 11, 2020
Date of Patent:
August 12, 2025
Assignee:
Origenis GMBH
Inventors:
Roland Koestler, Jean Tassel, Michael Thormann, Nasser Yehia, Andreas Treml, Michael Almstetter
Abstract: Disclosed herein are methods of administering relatively high doses of dexmedetomidine or a pharmaceutically acceptable salt thereof to a human subject, without also inducing significant sedation. The disclosed methods are particularly suitable for the treatment of agitation, especially when associated with neurodegenerative and/or neuropsychiatric diseases such as schizophrenia, bipolar illness such as bipolar disorder or mania, dementia, depression, or delirium.
Type:
Grant
Filed:
March 8, 2024
Date of Patent:
July 22, 2025
Assignee:
BioXcel Therapeutics, Inc.
Inventors:
Vasukumar Kakumanu, David Christian Hanley, Frank Yocca, Chetan Dalpatbhai Lathia, Lavanya Rajachandran, Robert Risinger
Abstract: Provided herein are stable amlodipine oral liquid formulations. Also provided herein are methods of using amlodipine oral liquid formulations for the treatment of certain diseases including hypertension and Coronary Artery Disease (CAD).
Abstract: A method for treating AR+ breast cancer in a subject comprising administering to the subject an AR agonist (e.g., SARMs such as RAD140), or in combination with one or more therapeutic agents selected from the group consisting of cdk4/6 inhibitors, m-TOR inhibitors, PI3k inhibitors, PARP inhibitors, BCL-2 inhibitors, and MCL-1 inhibitors.
Type:
Grant
Filed:
September 29, 2023
Date of Patent:
June 17, 2025
Assignee:
Ellipses Pharma Ltd
Inventors:
Gary Hattersley, Jamal Saeh, Ziyang Yu, Chris P. Miller, Teeru Bihani
Abstract: The present invention relates to a preparation method and application of a micelle preparation containing thymol and a derivative thereof. The micelle preparation contains thymol, a thymol derivative, a derivative (CST) formed by vitamin E and chondroitin sulfate, a derivative (TPGS) formed by vitamin E and polyethylene glycol, and water. On the one hand, the thymol is transformed into its derivative, so that the pungency degree of the thymol is effectively reduced, and the gasoline smell of the thymol is masked; on the other hand, the thymol and the derivative of the thymol are encapsulated by the vitamin E derivative to form micelles, so that the two components are effectively solubilized, and the biological adhesion of the micelle preparation is greatly enhanced. The micelle preparation can be used for oral ulcer treatment, oral care and correction of related oral cavity abnormalities.
Abstract: Disclosed is a method for improving the sensorial properties of an oil-in-water type emulsion for topical application, including, for 100% of its mass, 5% to 30% by weight of glycerol, characterised in that the oil-in-water type emulsion for topical application includes an effective quantity of a mixture of saturated cyclic or acyclic, linear or branched hydrocarbons, of which at least 95% by weight have between fifteen and nineteen carbon atoms. Also disclosed is a new oil-in-water type emulsion for topical use, including the mixture, and to the use of same in cosmetics.
Type:
Grant
Filed:
December 12, 2017
Date of Patent:
April 29, 2025
Assignees:
Societe d'Exploitation de Produits pour les Industries Chimiques SEPPIC, TotalEnergies OneTech
Inventors:
Sophie Cambos, Emmanuelle Merat, Cécile Taillebois, Benjamin Swoboda
Abstract: Disclosed is a method for improving the sensorial properties of an oil-in-water type emulsion for topical application, including, for 100% of its mass, 1% to 30% by weight of glycerol, characterised in that the oil-in-water type emulsion for topical application includes an effective quantity of a mixture of saturated cyclic or acyclic, linear or branched hydrocarbons, of which at least 95% by weight have between fifteen and nineteen carbon atoms. Also disclosed is a new oil-in-water type emulsion for topical use, including the mixture, and to the use of same in cosmetics.
Type:
Grant
Filed:
December 1, 2023
Date of Patent:
April 29, 2025
Assignees:
Societe d'Exploitation de Produits pour les Industries Chimiques SEPPIC, TotalEnergies OneTech
Inventors:
Sophie Cambos, Emmanuelle Merat, Cécile Taillebois, Benjamin Swoboda
Abstract: This document relates to materials and methods for treating fibrosis (e.g., pulmonary fibrosis). For example, this document provides methods for using one or more fatty acid synthase (FASN) inhibitors to treat a mammal having fibrosis (e.g., pulmonary fibrosis), and/or a complication associated with fibrosis (e.g., hypoxia caused by pulmonary fibrosis).
Type:
Grant
Filed:
February 16, 2022
Date of Patent:
April 22, 2025
Assignee:
Mayo Foundation for Medical Education and Research
Inventors:
Edward B. Leof, Ruth Lupu, Jeong-Han Kang, Mi-Yeon Jung
Abstract: Disclosed are a nitrogen-containing fused heterocyclic SHP2 inhibitor compound, a preparation method, and use. The nitrogen-containing fused heterocyclic SHP2 inhibitor compound is represented by formula I below. The compound has high inhibitory activity for an SHP2 enzyme and tumor cell proliferation, and has good druggability.
Type:
Grant
Filed:
November 7, 2019
Date of Patent:
April 22, 2025
Assignee:
SHANGHAI RINGENE BIOPHARMA CO., LTD.
Inventors:
Huixin Wan, Jianfeng Pan, Jingui Ma, Chuantao Cha
Abstract: The present disclosure relates to compositions including a phenylbutyrate compound and a bile acid, and methods of processing such compositions.
Type:
Grant
Filed:
December 8, 2022
Date of Patent:
March 11, 2025
Assignee:
Amylyx Pharmaceuticals, Inc.
Inventors:
Joshua Cohen, Justin Klee, David Wai Fung Ma
Abstract: This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.
Abstract: The present invention provides methods of treating Restless Legs Syndrome (RLS) including administering to a subject an effective amount of a dopamine D1 receptor antagonist. Compositions and kits useful for treating RLS are also provided.
Abstract: The present disclosure provides compounds represented by Formula I: wherein R1, R2, R3, and R4 are as defined in the specification, and the salts and solvates thereof. Compounds of Formula I are EED inhibitors. EED inhibitors are useful for the treatment of cancer and other diseases.
Abstract: Disclosed herein are methods of administering relatively high doses of dexmedetomidine or a pharmaceutically acceptable salt thereof to a human subject, without also inducing significant sedation. The disclosed methods are particularly suitable for the treatment of agitation, especially when associated with neurodegenerative and/or neuropsychiatric diseases such as schizophrenia, bipolar illness such as bipolar disorder or mania, dementia, depression, or delirium.
Type:
Grant
Filed:
March 8, 2024
Date of Patent:
November 12, 2024
Assignee:
BioXcel Therapeutics, Inc.
Inventors:
Vasukumar Kakumanu, David Christian Hanley, Frank Yocca, Chetan Dalpatbhai Lathia, Lavanya Rajachandran, Robert Risinger
Abstract: The present invention provides methods and compositions for treating epithelioid cell tumors (such as a PEComa) by administering a composition comprising nanoparticles comprising an mTOR inhibitor and an albumin.
Abstract: The present invention relates to injectable pharmaceutical compositions comprising therapeutically effective amount of succinylcholine chloride, one or more pharmaceutically acceptable aqueous solvents, and one or more stabilizing agents selected from aliphatic polyols; lower alkyl alcohols; amino acids having at least one additional amino, carboxyl or hydroxyl group; amino alcohols; and aliphatic dicarboxylic acids having at least one hydroxyl or amino group, or ?-? unsaturation. The compositions are stable at room temperature for at least 30 days. Methods of manufacturing the injectable pharmaceutical compositions are also provided. The composition may be provided in a sealed container, e.g., an ampoule, vial and pre-filled syringe, and are suitable for subcutaneous, intravenous or intramuscular administration as an adjunct to general anesthesia, to facilitate tracheal intubation, and/or to provide skeletal muscle relaxation during surgery or mechanical ventilation.
Abstract: Aspects of the disclosure relate to compositions, kits, and methods for the treatment of cancer that utilize a selective histone deacetylase 3 (HDAC3) inhibitor. In some aspects, the compositions, kits, and methods relate to use of a selective HDAC3 inhibitor in combination with an immunotherapy agent (e.g., an immune checkpoint inhibitor).
Abstract: The present invention relates to a pharmaceutical composition containing ?-lapachone as an active ingredient for prevention or treatment of cholestatic liver disease, and can provide agents for effectively preventing and treating cholestatic liver disease.
Type:
Grant
Filed:
September 12, 2022
Date of Patent:
October 29, 2024
Assignee:
CUROME BIOSCIENCES CO., LTD.
Inventors:
Joo Seog Yoon, Kang Sik Seo, Jeong Su Han, Sung Je Moon, Jung Hoon Lee, Soo Bin Yoon