Abstract: Disclosed in the present invention are a fused pyridone compound, and a preparation method therefor and a use thereof. Specifically, the present invention discloses a compound of formula (I-B), an optical isomer thereof and a pharmaceutically acceptable salt thereof, and the use of the compound as a KRAS inhibitor.
Abstract: A sterile, ready-to-use pharmaceutical composition having hydralazine and/or a salt thereof at a concentration of less than about 20 mg/mL and a solvent comprising an organic co-solvent, wherein the hydralazine and/or salt thereof and the organic co-solvent are provided at a first weight ratio sufficient for the hydralazine and/or salt thereof to have a change in concentration of no more than about 10% after 2 months of storage at 60° C. Also described are methods of making and using the composition.
Type:
Grant
Filed:
December 27, 2022
Date of Patent:
October 8, 2024
Assignee:
ENDO OPERATIONS LIMITED
Inventors:
Kumaresh Soppimath, Tushar Hingorani, Hari A. Attluri, Harshil H. Jain
Abstract: The present technology provides triazolones, tetrazolones, and imidazolones, or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The triazolones, tetrazolones, and imidazolones or their pharmaceutically acceptable salts exhibit inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
Type:
Grant
Filed:
April 21, 2022
Date of Patent:
October 8, 2024
Assignee:
Yuhan Corporation
Inventors:
Hee Jae Tak, Eun Kyung Kim, Hyok Jun Cho, Cheol Hee Lim
Abstract: The invention relates to crystalline tranilast salts. The crystalline tranilast salts, their preparation and their characterization are described and shown in the figures. The invention relates to pharmaceutical compositions containing a crystalline tranilast salt of the invention and a pharmaceutically acceptable carrier. The invention also relates to methods of treatment and the use of a therapeutically effective amount of a crystalline tranilast salt of the invention for treatment. The invention also relates to a method of preparing a liquid pharmaceutical composition comprising the step of dissolving a crystalline tranilast salt of the invention in a pharmaceutically acceptable solvent and to liquid pharmaceutical compositions prepared according to that method.
Abstract: The present disclosure concerns methods of detecting injury to a tissue and/or organ in a subject. In some aspects, the subject is the recipient of a transplant, such as a liver transplant. In some aspects, the subject is undergoing treatment with an immunosuppressant. In some aspects, the present disclosure concerns the identification of aberrant mitochondria in the subject to identify injury to the tissue and/or organ of the subject. Detecting aberrant mitochondria allows for remedial and/or corrective action to prevent or avoid significant injury.
Abstract: This disclosure relates to low molecular weight substituted imidazoles that inhibit the TGF-b signaling pathway. More specifically, this disclosure relates to methods of using said imidazoles for the treatment of diseases related to the TGF-b signaling pathways including, but not limited to, atherosclerosis, Marfan syndrome, Loeys-Dietz syndrome, obesity, diabetes, multiple sclerosis, keratoconus, idiopathic pulmonary fibrosis, Alzheimer's Disease, chronic kidney disease, and scleroderma.
Abstract: Disclosed is a method of treating in a subject hair loss disorders that are beneficially treated by administering a JAK1 and/or JAK2 inhibitor. The method comprises administering to the subject an amount in the range of about 4 mg to about 50 mg of Compound (I): or a pharmaceutically acceptable salt thereof. This invention also provides compositions comprising Compound (I) and the use of such compositions in the described methods.
Type:
Grant
Filed:
December 5, 2019
Date of Patent:
September 3, 2024
Assignee:
Sun Pharmaceuticals Industries, Inc.
Inventors:
Amanda T. Wagner, James V. Cassella, Philip B. Graham, Virginia Braman, Vinita Uttamsingh, Jana Von Hehn, Colleen E. Hamilton
Abstract: The present invention provides methods and compositions for modulating molecular markers, and hence treating or preventing breast cancer (e.g., triple-negative breast cancer) and melanoma with a pharmaceutically effective amount of S-equol or a pharmaceutical composition comprising S-equol. The S-equol may be administered alone or in combination with one or more cytotoxic or immunotherapeutic compound or molecule.
Type:
Grant
Filed:
November 24, 2021
Date of Patent:
August 27, 2024
Assignee:
Board of Regents, The University of Texas System
Abstract: A method for catalytically synthesizing furaneol, which uses a specific peptide to function as a catalyst, uses rhamnose to function as a raw material, and uses an organic solvent and a phosphate buffer to function as a reaction solvent to be co-heated to prepare furaneol.
Type:
Grant
Filed:
September 20, 2021
Date of Patent:
August 27, 2024
Assignee:
Xiamen Oamic Biotech Co., Ltd.
Inventors:
Chupei Xu, Zhou Zhu, Shunchuan Ke, Yibin Zhang, Gang Liu
Abstract: The present disclosure is related to processes for preparing baricitinib, salts thereof, and related synthetic intermediate compounds and salts thereof.
Type:
Grant
Filed:
July 11, 2022
Date of Patent:
August 27, 2024
Assignee:
Incyte Corporation
Inventors:
Jiacheng Zhou, Shili Chen, Zhongjiang Jia, Pingli Liu, David Meloni, Yongchun Pan, Naijing Su, Michael Xia
Abstract: The present disclosure provides compounds according to Formula I or a pharmaceutically acceptable salt thereof: wherein each variable is as defined and described herein, compositions thereof, and methods of using the same for the inhibition of CDK2, and the treatment of CDK2 related diseases and disorders.
Type:
Grant
Filed:
January 28, 2022
Date of Patent:
August 20, 2024
Assignee:
Cedilla Therapeutics, Inc.
Inventors:
Louise Clare Kirman, Carl Eric Schwartz, Wojtek Michowski, Dale A. Porter, Jr., Justin Ripper, John Feutrill, John Paul Sherrill, Thomas P. Blaisdell
Abstract: A composition containing a compound of formula I or a pharmaceutically acceptable salt, dimer or trimer thereof, and a tyrosine kinase activity inhibitor is provided. A method of preventing and/or treating cancer by administering a subject in need thereof the composition is provided. The combination of Sotagliflozin and a tyrosine kinase activity inhibitor may exhibit a synergistic inhibitory effect on tumors, and the efficacy of the combination is significantly better than that of a single drug.
Type:
Grant
Filed:
August 19, 2020
Date of Patent:
July 30, 2024
Assignee:
NEWISH TECHNOLOGY (BEIJING) CO., LTD.
Inventors:
Hailong Qi, Xiaofang Wang, Zhongjie Sun
Abstract: Provided herein are novel conjugates of TGF-beta inhibitors and bisphosphonates, pharmaceutical compositions comprising the conjugates, methods of preparing the conjugates, and methods of using the conjugates, for example, for the treatment of a bone disease or disorder, such as osteoarthritis.
Abstract: The present disclosure provides processes for the purification of 2,5-furandicarboxylic acid (FDCA). The present disclosure further provides crystalline preparations of purified FDCA, as well as processes for making the same. In addition, the present disclosure provides mixtures used in processes for the purification of FDCA.
Type:
Grant
Filed:
November 30, 2021
Date of Patent:
July 30, 2024
Assignee:
Stora Enso Oyj
Inventors:
Henricus Johannes Cornelis Den Ouden, Valery Sokolovskii, Thomas R. Boussie, Gary M. Diamond, Eric L. Dias, Guang Zhu, Staffan Torssell, Vincent J. Murphy
Abstract: Described herein is a process for preparing a compound of formula (I) starting from a compound of formula (II) where the process is catalyzed by a metal complex.
Abstract: The present disclosure provides compounds of Formula I, methods of preparing the compounds, compositions, kits, and methods of using the compounds for treating or preventing microbial infections.
Type:
Grant
Filed:
December 23, 2021
Date of Patent:
July 9, 2024
Assignee:
Massachusetts Institute of Technology
Inventors:
Mohammad Movassaghi, Bradley L. Pentelute, Carly Schissel, Kyan Anthony D'Angelo
Abstract: This invention relates to the compound (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide, and in particular to novel physical forms of the compound, a process for preparing the compound and synthetic intermediates for use in the process, and novel formulations containing the compound, as well as therapeutic uses of the compound.
Type:
Grant
Filed:
September 1, 2021
Date of Patent:
July 9, 2024
Assignee:
OTSUKA PHARMACEUTICAL CO., LTD.
Inventors:
Paul Anthony Baguley, Colin Thomas Lindley, Robert Craig Melling
Abstract: The present invention relates to a manufacturing process and intermediates for preparing a crystalline or non-crystalline form of N-((1S,3S)-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclobutyl)propane-1-sulfonamide. The present invention also relates to salt forms and pharmaceutical compositions comprising the crystalline form, and to methods for use of the compound prepared from a crystalline form in the treatment of various diseases.
Type:
Grant
Filed:
January 10, 2022
Date of Patent:
June 25, 2024
Assignee:
Pfizer Inc.
Inventors:
Kapildev Kashmirilal Arora, Jacob Cole DeForest, Andrew Kevern Hills, Brian Patrick Jones, Kris Nicole Jones, Chad Arthur Lewis, Anil Mahadeo Rane
Abstract: The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where m, n, X1, X2, R1-R5, R5? and R6 are described herein.
Type:
Grant
Filed:
February 26, 2021
Date of Patent:
June 25, 2024
Assignee:
VALO HEALTH, INC.
Inventors:
Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, Darby Rye Schmidt, David Joseph Guerin, Justin Andrew Caravella, R. Bruce Diebold, Anna Ericsson, David R. Lancia, Jr.
Abstract: The invention relates to a crystalline methanol solvate or hydrate form of ABC, and an anhydrous form of ABC, that reversibly forms a hydrate of ABC. The invention is also directed to the preparation of the aforesaid solvate, hydrate, and anhydrous solid-state forms of ABC. Furthermore, the invention relates to pharmaceutical compositions comprising at least one of the aforesaid crystalline forms of ABC according to the invention, and the pharmaceutical use of at least one of the aforesaid crystalline forms of ABC according to the invention for treatment of a patient in need thereof.