Abstract: Described herein are compounds of the formula (I), as well as pharmaceutical compositions comprising such compounds, and methods for using such compounds/pharmaceutical compositions for treating neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, and multiple sclerosis (MS).
Type:
Grant
Filed:
October 24, 2022
Date of Patent:
January 28, 2025
Assignee:
University of Massachusetts
Inventors:
Jeanne A. Hardy, Penchala Narasimharao Meka
Abstract: Disclosed herein are compounds of Formula (I?). Compounds of Formula (I?) inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
Abstract: The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 and R3 are each independently hydrogen or an optionally substituted hydrocarbyl group, or R1 and R3 together with the nitrogen atom to which they are attached may form a 3- to 12-membered optionally substituted cyclic group; and R2 is a cyclic group substituted at the position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
Type:
Grant
Filed:
August 12, 2019
Date of Patent:
January 7, 2025
Assignee:
INFLAZOME LIMITED
Inventors:
Matthew Cooper, David Miller, Angus MacLeod, Jonathan Shannon, Jokin Carrillo Arregui, Jimmy Van Wiltenburg, Jochem Theodoor Van Herpt
Abstract: Described herein are compounds represented by formulas (IA) or (IB) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables R1, R3, R4, Y1, Y2, Ar, Z and n are as defined herein.
Type:
Grant
Filed:
September 18, 2019
Date of Patent:
December 31, 2024
Assignee:
BIOGEN MA INC.
Inventors:
Nathan Genung, Kevin M. Guckian, Jeffrey Vessels, Lei Zhang, Ryan Gianatassio, Edward Yin Shiang Lin, Zhili Xin
Abstract: Provided herein is a process for preparing a pyridazine amine compound of formula V, and a process for preparing dichloropyridazine amine compounds of formula IVa, IVb, and mixtures thereof. Further, provided herein are dichloropyridazine amine compounds of formula IVa, IVb, and mixtures thereof, wherein the amino group is an ethylamino group.
Type:
Grant
Filed:
May 18, 2021
Date of Patent:
December 10, 2024
Assignee:
BASF SE
Inventors:
Eric George Klauber, Michael Rack, Roland Goetz, Sebastian Soergel
Abstract: A pharmaceutical composition contains chlorogenic acid and coumaroyl quinic acid. The combined use of chlorogenic acid and coumaroyl quinic acid at a certain ratio can generate a synergistic enhancing effect to effectively inhibit the growth of human kidney cancer cell strain A479, rat kidney cell strain RuCa, and rat transplanted tumor RuCa, providing a novel choice for clinical treatment of kidney cancer and having good market application prospects.
Type:
Grant
Filed:
May 31, 2019
Date of Patent:
December 3, 2024
Assignee:
SICHUAN JIUZHANG BIOLOGICAL SCIENCE AND TECHNOLOGY CO., LTD
Inventors:
Jie Zhang, Xiaoguang Chen, Wang Huang, Ya Zhang
Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
Type:
Grant
Filed:
October 11, 2019
Date of Patent:
November 26, 2024
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Dane Clausen, Ping Chen, Xavier Fradera, Liangqin Guo, Yongxin Han, Shuwen He, Jongwon Lim, Theodore A. Martinot, Alexander Pasternak, Li Xiao, Wensheng Yu
Abstract: Provided herein are heteroaryl compounds, for example, a compound of Formula I or IA, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, ameliorating, or preventing one or more symptoms of a disorder, disease, or condition mediated by a casein kinase 1 (CK1), an interleukin-1 receptor associated kinase (IRAK1), or a cyclin-dependent kinase 9 (CDK9).
Type:
Grant
Filed:
January 25, 2023
Date of Patent:
November 12, 2024
Assignee:
Yissum Research Development Company of the Hebrew University of Jerusalem Ltd
Inventors:
Irit Snir-Alkalay, Joseph P. Vacca, Yinon Ben-Neriah
Abstract: A method for producing a halogenated zinc phthalocyanine pigment includes a step of forming a halogenated zinc phthalocyanine crude pigment into a pigment. The halogenated zinc phthalocyanine crude pigment is obtained by deposition of a halogenated zinc phthalocyanine, which is synthesized by using a compound that generates an acid by reacting with water, and the step includes a pretreatment step of heating the halogenated zinc phthalocyanine crude pigment in water to obtain a halogenated zinc phthalocyanine prepigment having a pH of 5.0 or more.
Abstract: The disclosure relates to crystalline form 1 of [2-(5-methoxy-1H-indol-3-yl)ethyl]dipropylamine (5-MeO-DPT) and to crystalline form 1 of bis([2-(5-methoxy-1H-indol-3-yl)ethyl]dipropylazanium) (2E)-but-2-enedioate (5-MeO-DPT fumarate), and to pharmaceutical compositions containing the compounds and methods of treatment using them.
Abstract: Apurinic/apuyrimidinic endonuclease 1/Redox Factor-1 (APE/Ref-1) inhibitors are provided along with methods of using the same. The inhibitor has the structure of Formula I: or a pharmaceutically acceptable salt thereof. n is an integer from 4 to 14, X and X? are each independently H or OH, and Y and Y? are each independently H or OH.
Type:
Grant
Filed:
November 18, 2022
Date of Patent:
October 29, 2024
Assignees:
Chapman University, The Regents of the University of California
Inventors:
Sun Yang, Keykavous Parang, Richard Chamberlin, Frank L Meyskens, Jr.
Abstract: The present application relates to a compound of formula I as a toll-Like receptor 7 (TLR7) agonist or a pharmaceutically acceptable salt thereof for treating lung cancer, a pharmaceutical combination of the TLR7 agonist and a tyrosine kinase inhibitor for treating lung cancer, and the use of the compound of formula I or the pharmaceutically acceptable salt thereof and the pharmaceutical combination for treating lung cancer.
Type:
Grant
Filed:
May 24, 2019
Date of Patent:
October 29, 2024
Assignee:
CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
Abstract: Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
Type:
Grant
Filed:
March 29, 2022
Date of Patent:
October 29, 2024
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Brydon L. Bennett, Mercedes Delgado, Jan Elsner, Paul Erdman, Robert Hilgraf, Laurie Ann LeBrun, Meg McCarrick, Mehran F. Moghaddam, Mark A. Nagy, Stephen Norris, David A. Paisner, William J. Romanow, Yoshitaka Satoh, Marianne Sloss, Jayashree Tikhe, Won Hyung Yoon
Abstract: The present invention relates to a pharmaceutical composition containing alkynyl compound, a preparation method thereof and its application. The present invention discloses a pharmaceutical composition comprising an active pharmaceutical ingredient and an available pharmaceutical excipient; The active pharmaceutical ingredient is 3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-benzamide, or its pharmaceutical acceptable salt; The available pharmaceutical excipients includes diluents and lubricants. The pharmaceutical composition can effectively improve the bioavailability of the alkynyl compound, has good dissolution and stability, and improve the drug safety.
Abstract: Disclosed are phenyltetrazole derivatives of formula (I), wherein A, R1, R2, X, R?, R?, and n are as defined herein, and pharmaceutically acceptable salts thereof. Also disclosed are methods of using the phenyltetrazole derivatives for the treatment of diseases which can be influenced by inhibition of plasma kallikrein.
Type:
Grant
Filed:
October 7, 2019
Date of Patent:
September 17, 2024
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Dieter Wiedenmayer, Andreas Gollner, Iain Lingard, Holger Wagner
Abstract: Synergistic drug combinations with the small molecule PAC-1 against uveal or cutaneous melanoma. There are no current targeted drug treatments for the mutations associated with uveal melanoma. Despite primary radiation or surgical therapy, up to 50% of patients eventually develop metastatic disease, for which there is no standard therapy nor treatment shown to improve overall survival. Drug combinations with PAC-1 allow the use of lower dosages of this compound that result in cancer cell death in uveal melanoma. Drug combinations of PAC-1 with the kinase inhibitor entrectinib have shown a synergistic effect against uveal melanoma cell lines. Specifically, PAC-1 and entrectinib are synergistic against wild-type and mutant uveal melanoma cell lines (e.g., GNAQ and GNA11).
Type:
Grant
Filed:
October 3, 2019
Date of Patent:
September 17, 2024
Assignee:
The Board of Trustees of the University of Illinois
Inventors:
Paul J. Hergenrother, Matthew Wesley Boudreau
Abstract: The present disclosure provides bifunctional compounds as HPK1 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by HPK1.
Type:
Grant
Filed:
November 9, 2022
Date of Patent:
September 17, 2024
Assignees:
Nurix Therapeutics, Inc., Gilead Sciences, Inc.
Inventors:
John Buell, Frederick Cohen, Ryan Pemberton, Hunter P. Shunatona, Lan Wang, Mark Edward Zak
Abstract: The present application provides tricyclic urea compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.
Type:
Grant
Filed:
March 16, 2023
Date of Patent:
September 10, 2024
Assignee:
Incyte Corporation
Inventors:
Cooper Taylor, Yanran Ai, Chunhong He, Ke Zhang, Eddy W. Yue
Abstract: The present invention provides novel peripherally-restricted benzodiazepines with reduced blood brain barrier permeability and methods of use thereof for reducing tactile dysfunction, social impairment, and anxiety in a subject diagnosed with Autism Spectrum Disorder, Rett syndrome, Phelan McDermid syndrome, or Fragile X syndrome.
Type:
Grant
Filed:
March 25, 2020
Date of Patent:
September 3, 2024
Assignee:
President and Fellows of Harvard College
Inventors:
David D. Ginty, Lauren L. Orefice, Jinbo Lee
Abstract: The invention provides compounds of Formula (I): as further described herein, as well as pharmaceutical compositions comprising such compounds, and methods to use the compounds and pharmaceutical compositions for treatment of certain viral disorders, including influenza.
Type:
Grant
Filed:
February 27, 2023
Date of Patent:
August 27, 2024
Assignee:
Novartis AG
Inventors:
Maxime Dauphinais, Rama Jain, Dennis Christofer Koester, James R. Manning, Vanessa Marx, Daniel Poon, Lifeng Wan, Xiaojing Michael Wang, Aregahegn Yifru, Qian Zhao