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: 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: 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: 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: 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.
Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
Type:
Grant
Filed:
November 7, 2019
Date of Patent:
January 9, 2024
Assignee:
VIVACE THERAPEUTICS, INC.
Inventors:
Andrei W. Konradi, Tracy Tzu-Ling Tang Lin
Abstract: The present invention relates to: a novel method for preparing a heterocyclic derivative compound of chemical formula I below; a novel intermediate compound used in the preparation method; a composition for treatment or prevention of hyperuricacidemia, gout, nephritis, chronic renal insufficiency, nephrolith, uremia, urolithiasis, or a uric acid-related disease, the composition containing the compound of chemical formula I at a dose of more than 2 mg and equal to or less than 10 mg and being orally administered once a day; and a hydrochloride 1.5 hydrate of the novel compound of chemical formula I.
Abstract: Novel tetracyclic aza-podophyllotoxin analogue compounds, a method of synthesizing such compounds, a pharmaceutical composition comprising such compounds and a suitable carrier, and a method of using the compounds. The tetracyclic aza-podophyllotoxin analogue compounds are useful as antitumor agents.
Abstract: Provided herein are compounds that inhibit IDO1 and methods of use thereof. Also provided are pharmaceutical compositions and medicaments that include the compounds described herein as well as methods of treating sarcopenia or age-related muscle loss.
Type:
Grant
Filed:
January 19, 2022
Date of Patent:
January 2, 2024
Assignee:
Augusta University Research Institute, Inc.
Inventors:
Mark Hamrick, Carlos Isales, Iryna Lebedyeva
Abstract: The present invention relates to the field of optical imaging. More particularly, it relates to compounds of the cyanine family with near-infrared emission characterized by improved physico-chemical and biological properties and to conjugates with biological ligands thereof. The invention also relates to the use of these compounds as optical diagnostic agents in imaging or therapy of solid tumors, to the methods for their preparation and to the compositions comprising them.
Type:
Grant
Filed:
June 22, 2021
Date of Patent:
December 26, 2023
Assignee:
BRACCO IMAGING S.P.A.
Inventors:
Francesco Blasi, Federica Buonsanti, Federico Crivellin, Andrea Ferraris, Laura Orio, Lorena Pizzuto, Roberta Napolitano, Giovanni Valbusa
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:
November 21, 2022
Date of Patent:
December 26, 2023
Assignee:
COMPASS PATHFINDER LIMITED
Inventors:
Derek John Londesbrough, Christopher Brown, Julian Scott Northen, Gillian Moore, Hemant Kashinath Patil, David E. Nichols
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: A crystal of ethane disulfonate of (S)-1-(4-(dimethylamino)piperidin-1-yl)-3-hydroxy-3-(1-methyl-1H-imidazol-2-yl)propan-1-one, having peaks at diffraction angles 2?)(° of 12.6±0.2, 16.0±0.2, 17.7±0.2, 18.5±0.2, and 21.3±0.2 in powder X-ray diffraction; and the crystal of ethane disulfonate of (S)-1-(4-(dimethylamino)piperi din-1-yl)-3-hydroxy-3-(1-methyl-1H-imidazol-2-yl)propan-1-one, having an endothermic peak at 173° C. to 177° C. in simultaneous thermogravimetric-differential thermal analysis.
Abstract: Described herein are HSD17B13 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of liver disease, metabolic disease, or cardiovascular disease, such as NAFLD or NASH, or drug induced liver injury (DILI).
Type:
Grant
Filed:
May 10, 2023
Date of Patent:
November 28, 2023
Assignee:
INIPHARM, INC.
Inventors:
Sampath Kumar Anandan, Joshua Odingo, Heather Kay Webb Hsu, Vincent Florio, Subramanyam Janardhan Tantry, Athisayamani Jeyaraj Duraiswamy