Abstract: The various examples presented herein are directed to compounds of the formula A-L1-Het1-L2-Cy1 or a pharmaceutical acceptable salt, polymorph, prodrug, solvate or clathrate thereof, wherein: A is cycloalkyl, aryl, arylalkyl or heterocyclyl; Het1 is heterocyclyl containing at least two heteroatoms; Cy1 is a heterocyclyl; L1 is a bond, alkyl, alkenyl or alkynyl linker; L2 is an acyl or alkyl linker; and A and Cy1 are different. The compounds are useful in the treatment of fibrotic diseases, abnormal vascular leak and pathological angiogenesis.
Type:
Grant
Filed:
March 8, 2019
Date of Patent:
April 23, 2024
Assignees:
Cornell University, Tri-Institutional Therapeutics Discovery Institute
Inventors:
Timothy Hla, Irina Jilishitz, Peter Meinke, Andrew Stamford, Michael Foley, Ayumu Sato, Yasufimi Wada, Yoshiyuki Fukase, Asato Kina, Hiroki Takahagi, Hideyuki Igawa, William J. Polvino
Abstract: The present invention relates to a method for preparing Asenapine. In particular, the present invention relates to a method for preparing pharmaceutically acceptable Asenapine free base and new crystal form thereof, and also relates to methods for preparing the intermediate compounds used in said method.
Abstract: Benzoxazine compounds, methods of making them, polymers made therefrom and methods of polymerizing the benzoxazines. These renewable benzoxazine monomers and polymers that utilize the variety of building blocks found in renewable plant biomass, demonstrate excellent processability and large temperature windows for processing of resin systems.
Type:
Grant
Filed:
March 24, 2023
Date of Patent:
April 16, 2024
Assignees:
Drexel University, The United States of America as represented by The Secretary of the Army
Inventors:
Giuseppe R. Palmese, Santosh K. Yadav, John J. LaScala
Abstract: The pyrazolidinedione derivatives were found to possess blood glucose lowering properties. These compounds were designed as potential PPAR gamma inhibitors, an essential molecular target for clinically used antidiabetic drugs. Owing to their promising anti-hyperglycemic activity, these derivatives may find useful applications for the treatment and/or prevention of obesity, diabetes type II and I, hyperglycemia and other diseases where PPAR gamma is implicated such as cancer, atherosclerosis and hyperlipidemia.
Abstract: The present invention relates hydroxypyridoxazepine compounds, methods of making them, pharmaceutical compositions containing them and their use as Nrf2 activators. In particular, the invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, or a tautomer thereof, or a hydrate thereof.
Type:
Grant
Filed:
February 11, 2020
Date of Patent:
April 2, 2024
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Mark Elban, Michal Pawel Glogowski, Michael Clinton Koetting, Brian Griffin Lawhorn, Jay M. Matthews, Jaclyn Renee Patterson
Abstract: This disclosure is drawn to substituted pyridine compounds and compositions, and associated methods, useful for inhibition of SARM1 activity and/or for treating or preventing neurological diseases.
Type:
Grant
Filed:
September 15, 2021
Date of Patent:
April 2, 2024
Assignee:
NURA BIO, INC.
Inventors:
Sean Pomeroy Brown, Keira Garland, Shilpa Sambashivan, Christopher Michael Tegley, Liusheng Zhu
Abstract: Disclosed herein are polymorphic and amorphous forms of anhydrate, hydrate, and solvates of (R)-2-hydroxy-2-methyl-4-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dienyl)butanamide and methods of using such compositions for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging. Further disclosed are methods of making such polymorphic and amorphous forms.
Type:
Grant
Filed:
March 10, 2022
Date of Patent:
March 26, 2024
Assignee:
PTC THERAPEUTICS, INC.
Inventors:
Paul Mollard, Peter Giannousis, Shazad Suchit, Mahmoud Mirmehrabi, Christopher R. Cornell, Kieron E. Wesson
Abstract: This invention relates to the large-scale production of psilocybin for use in medicine. More particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin.
Type:
Grant
Filed:
April 17, 2023
Date of Patent:
March 26, 2024
Assignee:
Compass Pathfinder Limited
Inventors:
Derek John Londesbrough, Christopher Brown, Julian Scott Northen, Gillian Moore, Hemant Kashinath Patil, David E. Nichols
Abstract: Methods of inhibiting cyclooxygenase enzyme-2 (COX-2) using thieno[2,3-d]pyrimidine compounds. These methods can be effective for treating inflammation, pain, or any other COX-2 mediated disorder.
Type:
Grant
Filed:
October 6, 2023
Date of Patent:
March 19, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Katharigatta N. Venugopala, Pran Kishore Deb, Raghu Prasad Mailavaram, Nizar A. Al-Shar'i, Swastika Ganguly, Bapi Gorain, Lim Tse Mun, Jamie Kow Kean Hing
Abstract: This disclosure relates to crystalline bis(4-hydroxy-N,N-d-n-propyltryptammonium)fumarate tetrahydrate (4-HO-DPT fumarate-4H2O) and to Crystalline 4-hydroxy-N,N-di-n-propyl-tryptammonium chloride (4-HO-DPT chloride). Compositions containing crystalline 4-HO-DPT fumarate-4H2O or crystalline 4-HO-DPT chloride, and methods of use are disclosed.
Abstract: The present application describes deuterium-enriched pioglitazone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
Abstract: A process for producing a cyclic alkylene urea product of Formula I: in which a compound of Formula II and/or Formula III is contacted in a reaction zone with a compound of Formula IV and/or Formula V and in the presence of one or more carbonyl delivering compounds; wherein the compound of Formula II and/or the compound of Formula III are added to a reaction zone comprising compound of Formula IV and/or compound of Formula (V) continuously or semi-continuously over a period of time, or in two or more batches.
Type:
Grant
Filed:
August 7, 2018
Date of Patent:
March 5, 2024
Assignee:
NOURYON CHEMICALS INTERNATIONAL B.V.
Inventors:
Antoon Jacob Berend Ten Kate, Karl Fredrik Lake, Michiel Jozef Thomas Raaijmakers, Rolf Krister Edvinsson, Jenny Valborg Therese Adrian Meredith, Rens Veneman, Hendrik Van Dam, Eike Nicolas Kantzer, Ina Ehlers, Slavisa Jovic
Abstract: Compounds for treating tuberculosis and, particularly, anti-tubercular compounds that are (6-methyl-4-substitutedphenyl-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)(piperidin-1-yl)methanones and their use as anti-tubercular agents are provided.
Type:
Grant
Filed:
September 13, 2023
Date of Patent:
February 27, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Katharigatta N. Venugopala, Keshab M. Bairagi, Pran Kishore Deb, Melendran Pillay, Mohamed A. Morsy, Susanta K. Nayak, Sandeep Chandrashekharappa, Osama I. Alwassil
Abstract: This application provides a biphenyl diaryl pyrimidine derivative with an aromatic heterocyclic structure, a pharmaceutically-acceptable salt, a stereoisomer, a hydrate and a solvate thereof, where the biphenyl diaryl pyrimidine derivative is shown in formula (I). This application also provides a pharmaceutical composition containing the biphenyl diaryl pyrimidine derivative, or a pharmaceutically-acceptable salt, a stereoisomer, a hydrate and a solvate thereof, and a pharmaceutically-acceptable carrier. This application further provides a method of treating AIDS by administering a therapeutically effective amount of the pharmaceutical composition to a patient in need.
Abstract: In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease, diabetes, bone loss, and cancer, using a compound of Formula I.
Type:
Grant
Filed:
August 13, 2019
Date of Patent:
February 20, 2024
Assignee:
OSSIFI THERAPEUTICS LLC
Inventors:
Debra Ellies, F. Scott Kimball, Robert N. Young
Abstract: A compound 3-(4-chlorophenyl)-5-{[5-methyl-2-(propan-2-yl)phenoxy]methyl}-1,2,4-oxadiazole, its synthesis, and its use as an anticancer and/or antimicrobial agent.
Type:
Grant
Filed:
August 28, 2023
Date of Patent:
February 20, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Hany Mohamed Abd El-Lateef Ahmed, Mai Mostafa Khalaf Ali, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer, Sahar M. Mohamed, Mohammad Mahboob Alam
Abstract: The present invention is related to processes for preparing itacitinib, or a salt thereof, and related synthetic intermediates related thereto.
Type:
Grant
Filed:
August 17, 2021
Date of Patent:
February 13, 2024
Assignee:
Incyte Corporation
Inventors:
Jiacheng Zhou, Shili Chen, Pingli Liu, David J. Meloni, Yongchun Pan, Naijing Su, Michael Xia
Abstract: This invention relates to a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of abnormal cell growth in mammals, especially humans.
Type:
Grant
Filed:
October 6, 2021
Date of Patent:
February 6, 2024
Assignee:
Pfizer Inc.
Inventors:
Eric Christian Hansen, Christopher Scott Seadeek, Anil Mahadeo Rane
Abstract: Disclosed are novel prenylated psilocybin derivative compounds and pharmaceutical and recreational drug formulations containing the same. The compounds may be produced in vitro or in vivo using a biosynthetic system which comprises cells comprising a prenyl transferase, and, optionally, additional enzymes, including a decarboxylase, and an N-acetyl transferase.
Type:
Grant
Filed:
September 29, 2022
Date of Patent:
February 6, 2024
Assignee:
ENVERIC BIOSCIENCES CANADA INC.
Inventors:
Jillian M. Hagel, Peter J. Facchini, Xue Chen
Abstract: This invention relates to a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of abnormal cell growth in mammals, especially humans.