Abstract: A method of producing tetrahydrocannabinolic acid (THCA), the method includes obtaining a starting compound, the starting compound being selected from the group consisting of delta 9-THC, delta 8-THC, and delta 10-THC; placing the starting compound into a high pressure reaction chamber; treating the starting compound with a high heat, a high pressure, and carbon dioxide within the high pressure reaction chamber to create a resulting product; and treating the resulting product with sulfuric acid to yield the THCA.
Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.
Type:
Grant
Filed:
March 15, 2021
Date of Patent:
September 10, 2024
Assignee:
Novartis AG
Inventors:
Vincent Bordas, Cara Brocklehurst, Patrick Chene, Pascal Furet, Vito Guagnano, Patricia Imbach-Weese, Joerg Kallen, Mickael Le Douget, Edwige Liliane Jeanne Lorthiois, Joseph McKenna, Bahaa Salem, Tobias Schmelzle, Holger Sellner, Nicolas Soldermann, Markus Voegtle, Markus Wartmann
Abstract: This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.
Type:
Grant
Filed:
February 1, 2021
Date of Patent:
September 3, 2024
Inventors:
Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Yanke Liang, Mark E. Fitzgerald, Minsheng He, Ryan E. Michael
Abstract: The present disclosure related to compositions, methods, dosages, dosage regimens, articles of manufacture and kits for the treatment and/or prevention ectopic calcifications, and in particular cutaneous calcifications such as calciphylaxis calcifications comprising inositol phosphate, inositol phosphate analogs, inositol phosphate derivatives, or combinations thereof. In a particular aspect the disclosure provides a dosage regimen to treat calciphylaxis comprising the administration of 6 mg/kg to 9 mg/kg daily doses of myo-inositol hexaphosphate, three times a week, for at least 1 to 8 months.
Type:
Grant
Filed:
March 4, 2021
Date of Patent:
August 27, 2024
Assignee:
SANIFIT THERAPEUTICS S.A.
Inventors:
Joan Perello Bestard, Carolina Salcedo Roca, Ana-Zeralda Canals Hamann
Abstract: One aspect of the present disclosure relates to a pharmaceutical composition, containing (R)-N-[1-(3,5-difluoro-4-methanesulfonylamino-phenyl)-ethyl]-3-(2-propyl-6-trifluoromethyl-pyridin-3-yl)-acrylamide as a first ingredient and containing a vinylpyrrolidone-based polymer as a second ingredient. The composition of one aspect of the present disclosure has a formulation characteristic in which the crystal formation of a compound represented by chemical formula 1 is delayed for a long time.
Type:
Grant
Filed:
March 21, 2019
Date of Patent:
August 13, 2024
Assignee:
Amorepacific Corporation
Inventors:
Joonho Choi, Wonkyung Cho, Jong Hwa Roh, Kwanghyun Shin, Byoung Young Woo, Min Soo Kim, Miyoung Park, Youngho Park, Eunsil Park, Jaehong Park, Kiwha Lee
Abstract: The present disclosure concerns methods and formulations for delivery of hydrophobic agents (such as ubiquinone or poorly soluble drugs) for therapeutic and bioanalytical use. It further concerns use of lipopeptides (e.g. caspofungin) or surfactants to solubilize hydrophobic agents and thus increase their bioavailability. Also described are therapeutic methods for the treatment of conditions that benefit from such hydrophobic agents. The present disclosure further relates to methods of identifying drug candidates for treatment of ubiquinone deficiency.
Type:
Grant
Filed:
January 31, 2019
Date of Patent:
August 6, 2024
Assignee:
THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIVERSITY
Abstract: The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
Type:
Grant
Filed:
August 16, 2023
Date of Patent:
August 6, 2024
Assignees:
Gilead Sciences, Inc., Carna Biosciences, Inc.
Inventors:
Masaaki Sawa, Mai Arai, Ryoko Nakai, Hirokazu Matsumoto, Jonathan William Medley, Leena Patel, Qingming Zhu, Tetsuya Kobayashi
Abstract: The present invention relates to crystalline forms of the free base of the c-Met inhibitor, Compound 1. The invention also relates to crystalline forms of salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid polymorphs of the free base and salts of Compound 1. The invention further relates to methods of treating a disease, disorder, or syndrome mediated at least in part by modulating in vivo activity of a protein kinase.
Type:
Grant
Filed:
December 12, 2019
Date of Patent:
June 25, 2024
Assignee:
Exelixis, Inc.
Inventors:
Frenel DeMorin, Khalid Shah, Sagar Shakya, Peter Wong, Courtney S. Johnson, Melanie Janelle Bevill, Stephan D. Parent
Abstract: Disclosed are a novel hypoxia-inducible factor 1? (HIF-1?) inhibitor, a method of preparing the same, and a pharmaceutical composition for preventing or treating an angiogenesis-related eye disease containing the same as an active ingredient. The compound of Example provided according to an embodiment of the present invention is capable of effectively inhibiting HIF-1? and is thus useful as a pharmaceutical composition for preventing or treating an angiogenesis-related eye disease.
Type:
Grant
Filed:
August 12, 2019
Date of Patent:
June 11, 2024
Assignee:
SEOUL NATIONAL UNIVERSITY R&DB FOUNDATION
Inventors:
Youngger Suh, Seungbeom Lee, Jeonghun Kim
Abstract: A chemical entity of Formula (I): wherein V, W, Y, and Z, have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by PDE2 activity; treating neurological disorders, CNS disorders, dementia, cognitive disorders, neurodegenerative diseases, and trauma-dependent losses of function; enhancing the efficiency of cognitive and motor training, including in stroke or TBI rehabilitation; and treating peripheral disorders, including hematological, cardiovascular, gastroenterological, dermatological, inflammatory, and pain disorders.
Type:
Grant
Filed:
April 15, 2021
Date of Patent:
June 4, 2024
Assignee:
Dart NeuroScience, LLC
Inventors:
Laurent Gomez, William Francois Vernier
Abstract: Benzylamino-oxoethyl benzamide compounds for use in treating diseases and conditions associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic ?-cell dysfunction and death, for example in the treatment of Type 1 and Type 2 diabetes. The compounds can also be used in treatments for chronic heart disease, neurodegenerative diseases, retinal degeneration, and other metabolic disorders associated with ER stress.
Type:
Grant
Filed:
February 8, 2022
Date of Patent:
June 4, 2024
Assignee:
The Board of Regents of the University of Oklahoma
Abstract: Provided herein are methods of treating cancer in a subject with a ZIP9 inhibitor. In certain embodiments, the cancerous tissues do not express the nuclear androgen receptor (AR). These methods, alone or in combination with other cancer therapies, can improve treatment outcomes in patients suffering from cancer, particularly male patients.
Type:
Grant
Filed:
February 19, 2021
Date of Patent:
May 28, 2024
Assignee:
THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
Inventors:
Todd Ridky, Christopher Natale, Cristina Aguirre Portoles
Abstract: The present invention relates to a composition which comprises an electron-transporting host and a hole-transporting host, to the use thereof in electronic devices and to electronic devices containing this composition. The electron-transporting host is particularly preferably selected from the class of the lactams. The hole-transporting host is preferably selected from the class of the biscarbazoles.
Type:
Grant
Filed:
July 2, 2018
Date of Patent:
May 28, 2024
Assignee:
Merck Patent GmbH
Inventors:
Amir Parham, Jonas Kroeber, Tobias Grossmann, Anja Jatsch, Christian Eickhoff, Christian Ehrenreich
Abstract: This invention relates to compounds for treating acute myeloid leukemia or inhibiting recurrence of acute myeloid leukemia and for inhibiting growth of and/or killing leukemic stem cells.
Type:
Grant
Filed:
March 15, 2021
Date of Patent:
April 23, 2024
Assignee:
Flash Therapeutics, LLC
Inventors:
Michael Serrano-Wu, Zhixiong Ye, Kejia Ding
Abstract: Methods of identification of inhibitors of calcium release-activated calcium (CRAC) channel and small molecule inhibitors of CRAC channel, including methods of their synthesis and pharmaceutical use, are disclosed.
Abstract: The present invention relates to the novel key intermediate, 4-{4-[(SS)-(Aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]-phenyl}-morpholin-3-one perchlorate, m the synthesis of rivaroxaban. The invention further relates to the crystalline form of novel intermediate, the process to prepare the novel intermediate and method of preparing rivaroxaban using this novel intermediate. The invention provides an improved and efficient process for preparation of Rivaroxaban.
Type:
Grant
Filed:
May 3, 2021
Date of Patent:
February 6, 2024
Assignee:
Unichem Laboratories Ltd
Inventors:
Dhananjay G. Sathe, Arijit Das, Sanjay Raikar, Yashwant S. Surve, Bhushan S. Pandit
Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R1-R10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R3 or R8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.
Type:
Grant
Filed:
November 19, 2020
Date of Patent:
January 2, 2024
Assignees:
University of Pittsburgh—Of the Commonwealth System of Higher Education, The United States Government as Represented By the Department of Veterans Affairs
Abstract: The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
Type:
Grant
Filed:
December 18, 2020
Date of Patent:
December 19, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Masaaki Sawa, Mai Arai, Ryoko Nakai, Hirokazu Matsumoto, Catherine Pugh, Eric Hu, Juan Guerrero, Jesse Jacobsen, Jonathan William Medley, Jie Xu, Latesh Lad, Leena Patel, Michael Graupe, Qingming Zhu, Stephen Holmbo, Tetsuya Kobayashi, Will Watkins, Yasamin Moazami, Suet C. Yeung, Julian A. Codelli, Heath A. Weaver