Abstract: The present invention provides solid forms, solvates and hydrates of 3-[2-amino-6-(1-{[6-(2-hydroxypropan-2-yl)pyridin-2-yl]methyl}-1H-1,2,3-triazol-4-yl)pyrimidin-4-yl]-2-methylbenzonitrile (Compound I), and methods of making and using the same.
Type:
Grant
Filed:
July 17, 2019
Date of Patent:
May 28, 2024
Assignee:
ARCUS BIOSCIENCES, INC.
Inventors:
Jenna Leigh Jeffrey, Manmohan Reddy Leleti, Dillon Harding Miles, Jay Patrick Powers
Abstract: Bridged compounds of Formula (I) and Formula (II), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. wherein R2, R3 R4, R5 and R6 are defined herein.
Type:
Grant
Filed:
January 27, 2023
Date of Patent:
May 28, 2024
Inventors:
Michael K. Ameriks, Gang Chen, Chaofeng Huang, Brian Ngo Laforteza, Suchitra Ravula, Wei Zhang
Abstract: The present invention relates to heterobicyclic amides and related compounds which are inhibitors of CD38 and are useful in the treatment of cancer.
Type:
Grant
Filed:
December 5, 2022
Date of Patent:
May 21, 2024
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Laurie B. Schenkel, Melissa Marie Vasbinder, Kevin Wayne Kuntz, Nicholas Robert Perl, Jennifer Downing
Abstract: Disclosed is a method for selecting a cancer therapeutic for a patient that involves assaying a tumor biopsy sample from the subject to detect PAXIP1 expression, and selecting a WEE1 inhibitor as the cancer therapeutic if PAXIP1 is detected in the tumor biopsy sample.
Type:
Grant
Filed:
August 2, 2019
Date of Patent:
May 21, 2024
Assignee:
H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
Abstract: A compound 3-(4-methoxyphenyl)-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:
December 5, 2023
Date of Patent:
May 14, 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: A compound 3-(4-methoxyphenyl)-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:
December 5, 2023
Date of Patent:
May 14, 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 provides bicyclic heterocyclyl kinase enzyme inhibitor compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors. wherein A, Y, Z, X1, X2, X3, R1, R3, ‘m’, ‘n’ and ‘p’ have the meanings given in the specification and pharmaceutically acceptable salts or stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in diseases or disorders mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical compositions comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
Abstract: Invented are compounds of Formula I and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.
Type:
Grant
Filed:
October 6, 2021
Date of Patent:
May 7, 2024
Assignee:
Merck Sharp & Dohme, LLC
Inventors:
Yeon-Hee Lim, Eric R. Ashley, Jianming Bao, Chen Cheng, James P. Roane, Emma Helen Southgate
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: 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 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: 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: 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: 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: 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: 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: The present application describes deuterium-enriched pioglitazone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.