Abstract: A compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy is provided. The present inventors have conducted studies on a compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy, and confirmed that a heteroaryl carboxamide compound has DGK ? (DGKzeta) inhibitory effect, leading to completion of the present invention. The heteroaryl carboxamide compound of the present invention has DGK ? inhibitory effect, and can be used as a therapeutic agent for treatment of cancer related to activation of immune cells or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy.
Abstract: Provided are novel compounds of Formulas (I) and (II), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful as dual FKBP12/FKABP inhibitors. Also provided are pharmaceutical compositions comprising the novel compounds of Formulas (I) and (II) and their use in treating Parkinson's disease.
Type:
Grant
Filed:
August 21, 2018
Date of Patent:
August 20, 2024
Assignee:
PLEX PHARMACEUTICALS, INC.
Inventors:
Surya Kanta De, Sridhar G. Prasad, Marshall C. Peterman
Abstract: Disclosed herein are compositions containing an isolated bioactive compound of Formula (X): including less than about 2 wt % of halifordin. Also disclosed are methods for obtaining and using compositions containing the isolated bioactive compound.
Type:
Grant
Filed:
August 28, 2019
Date of Patent:
August 20, 2024
Assignee:
HARDIE HEALTH LIMITED
Inventors:
Peter Thomas Northcote, Ameet Jonathan Singh
Abstract: An aqueous suspension-form pesticidal composition comprising: at least one pesticidal active ingredient selected from the group consisting of amine derivatives represented by the following general formula (1) and salts thereof; a highly-purified and partially-desulfonated lignosulfonate; and an aqueous dispersion medium
Type:
Grant
Filed:
September 27, 2019
Date of Patent:
August 20, 2024
Assignee:
MITSUI CHEMICALS CROP & LIFE SOLUTIONS, INC.
Inventors:
Kazuko Ochiai, Tomohiko Okuda, Atsushi Sato
Abstract: The present invention discloses a solution formulation for aerosol inhalation of naringenin and preparation method thereof. The formulation is prepared from 1 part by weight of naringenin, 15-30 parts by weight of hydroxypropyl ?-cyclodextrin, a buffer-salt solution and an appropriate amount of an excipient. The preparation method includes: preparing a buffer-salt solution of a pH value of 7-8.5 by using the buffer salt, adding the naringenin into the buffer-salt solution, then adding the hydroxypropyl ?-cyclodextrin, shaking in a constant-temperature air bath till complete dissolving and coating, adding an appropriate amount of the excipient, filtering, filling and sterilizing. The present invention, by firstly increasing the solubility of the free naringenin in the solvent by adjusting the pH value, and then coating the naringenin with the hydroxypropyl ?-cyclodextrin, significantly increases the overall concentration of the naringenin in the solvent.
Abstract: Disclosed are compounds of Formula (I) to (VIII): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a bicyclic heteroaryl group substituted with zero to 3 R3a; and R1, R2, R3a, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.
Type:
Grant
Filed:
December 16, 2020
Date of Patent:
August 13, 2024
Assignee:
Bristol-Myers Squibb Company
Inventors:
Xiaojun Zhang, Eldon Scott Priestley, J. Alex Bates, Oz Scott Halpern, Samuel Kaye Reznik, Jeremy M. Richter
Abstract: The invention relates to a co-crystal or salt comprising psilocybin and a co-former. The co-crystal or salt is useful in methods of treating or preventing a disease or condition selected from depression, anxiety, death anxiety, demoralization, adjustment disorders, hopelessness, suicidal ideation, desire for hastened death, cocaine-related disorders, opioid-related disorders and stimulant-related disorders in a patient. A kit comprising the co-crystal or salt is also described.
Abstract: Provided, inter alia, are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.
Abstract: According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor. A process for the preparation of the compound, pharmaceutical compositions comprising the compound, and methods of treatment comprising administration of an effective amount of the compound are also disclosed.
Type:
Grant
Filed:
April 23, 2021
Date of Patent:
August 6, 2024
Assignee:
Nxera Pharma UK Limited
Inventors:
Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
Abstract: The present disclosure relates to compounds of formula (I?) and pharmaceutically acceptable salts thereof useful as inhibitors of Ubiquitin Specific Peptidase 30 (USP30), pharmaceutical compositions thereof, and methods of use thereof. Compounds as disclosed herein can be useful in the treatment of a disease or disorder involving mitochondrial dysfunction, including neurodegenerative diseases.
Type:
Grant
Filed:
May 16, 2019
Date of Patent:
July 30, 2024
Assignee:
FORMA Therapeutics, Inc.
Inventors:
Matthew W. Martin, Alexandre Joseph Buckmelter
Abstract: Disclosed herein are methods and compositions comprising atropine and a polymer in a gel formulation for decreasing saliva production and treating sialorrhea.
Type:
Grant
Filed:
October 31, 2022
Date of Patent:
July 30, 2024
Assignee:
UNIVERSITY OF UTAH RESEARCH FOUNDATION
Inventors:
Venkata K. Yellepeddi, Nancy Alice Murphy, Hamidreza S. Ghandehari, Harlan R. Muntz, Bhuvanesh Kumar Yathavan, Kevin Watt
Abstract: The inactivation of BK virus in patients diagnosed with BK virus, those receiving a kidney that is infected or suspected of being infected by BK virus, or in the transplanted kidney before, during, and/or after transplant surgery is described.
Type:
Grant
Filed:
July 8, 2022
Date of Patent:
July 23, 2024
Assignee:
Renibus Therapeutics, Inc.
Inventors:
Donald Jeffrey Keyser, Alvaro F. Guillem, Bhupinder Singh, Stacey Ruiz
Abstract: There are provided compounds containing benzo[d][1,3]oxathiole, benzo[d][1,3]oxathiole 3-oxide, and benzo[d][1,3]oxathiole 3,3-dioxide, as well as uses/methods related thereto, including treatment of diseases and condition associated with GPR119 dysregulation, Type 2 diabetes mellitus, and related metabolic disorders.
Abstract: Compounds of general formula (I) wherein R1, R2, R3, R4 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.
Type:
Grant
Filed:
May 17, 2019
Date of Patent:
July 16, 2024
Assignee:
Enterprise Therapeutics Limited
Inventors:
Clive McCarthy, Duncan Alexander Hay, Thomas Beauregard Schofield
Abstract: A composition for an organic optoelectronic device, an organic optoelectronic device, and a display device, the composition including a first compound; a second compound; and a third compound, the first compound, the second compound, and the third compound are different from each other, the first compound is represented by Chemical Formula I, the second compound is represented by Chemical Formula II or Chemical Formula III, and the third compound is represented by Chemical Formula II or Chemical Formula III,
Type:
Grant
Filed:
February 14, 2020
Date of Patent:
July 2, 2024
Assignee:
SAMSUNG SDI CO., LTD.
Inventors:
Yongtak Yang, Dong Min Kang, Hyung Sun Kim, Jinhyun Lui, Seungin Park, Jaejin Oh, Sung-Hyun Jung, Ho Kuk Jung, Youngkyoung Jo, Pyeongseok Cho, Dalho Huh
Abstract: Disclosed in the present invention are an edaravone pharmaceutical composition and an application thereof as a sublingual preparation, the pharmaceutical composition containing edaravone or a salt thereof and mannitol. A sublingual administration preparation can avoid the first-pass effect of the liver, and samples feature good stability, convenience of transport and of use, among other advantages.
Type:
Grant
Filed:
December 27, 2018
Date of Patent:
June 25, 2024
Assignees:
BEIJING TIANTAN HOSPITAL, CAPITAL MEDICAL UNIVERSITY, NANJING BAIXINYU PHARMACEUTICAL CO. LTD.
Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.
Type:
Grant
Filed:
July 29, 2023
Date of Patent:
June 11, 2024
Assignee:
Biohaven Therapeutics Ltd.
Inventors:
Jay Edward Wrobel, Allen B. Reitz, Jeffery Claude Pelletier, Garry Robert Smith, Haiyan Bian
Abstract: The present invention relates to compounds of formula (I) for use in preventing and/or treating cancer.
Type:
Grant
Filed:
July 1, 2019
Date of Patent:
June 11, 2024
Assignees:
FUNDACIÓ HOSPITAL UNIVERSITARI VALL D'HEBRONINSTITUT DE RECERCA, INSTITUT UNIV. DE CIÈNCIA I TECNOLOGIA, S. A.
Inventors:
Josep Roma Castanyer, Marta Pascual Gilabert, José Sánchez De Toledo Codina, Soledad Gallego Melcón, Patricia Zarzosa Martínez, Javier Alonso Fernández, Sergio Pérez Ozcáriz, Cristina López Gómez, Josep Castells Boliart
Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.
Type:
Grant
Filed:
February 1, 2021
Date of Patent:
June 11, 2024
Assignee:
Biohaven Therapeutics Ltd.
Inventors:
Jay Edward Wrobel, Allen B. Reitz, Jeffrey Claude Pelletier, Garry Robert Smith, Haiyan Bian
Abstract: A 4,5-bis(4-chlorophenyl)-2-phenyl-1H-imidazole compound, its synthesis, and its use as an anticancer, anti-inflammatory, and/or antimicrobial agent.
Type:
Grant
Filed:
October 23, 2023
Date of Patent:
June 4, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Hany Mohamed Abd El-Lateef Ahmed, Mai Mostafa Khalaf Ali, Amer A. Amer, Antar Ahmed Abdelhamid Ahmed