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
Abstract: Compounds are provided having one of the following structures (I) or (II): or (I) (II) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R3a, R3b, L1, L2, G1a, G1b, G2a, G2b and G3 are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.
Abstract: A method for destroying cells and/or microorganisms in an organism includes the following steps: (a) administering to the organism a composition including a sonosensitizing compound containing at least one transition metal with three bidentate ligands; and (b) exposing the sonosensitizing compound in the organism to ultrasound, wherein the ultrasound is effective to activate the sonosensitizing compound to destroy at least one of the cells and the microorganisms in the organism. The ultrasound is preferably used in conjunction with electromagnetic therapies comprising photodynamic therapy, low-level laser therapy, and radiation therapy. The ultrasound is preferably administered at a duty cycle in the range from 5% to 95% at a power density of 10 W/cm2 and a frequency in the range from 10 Hz to 10 MHz.
Abstract: Defined herein are immunomodulating Formula (1) compounds wherein R, R0, R1, R2, R3 and W are as defined herein, stereoisomers thereof, and pharmaceutically acceptable salts thereof; and compositions comprising said compounds. The invention also includes methods for treating an inflammatory and/or immunological disease or disorder in an animal by administering a therapeutically effective amount of a Formula (1) compound, stereoisomer thereof, and a pharmaceutically acceptable salt thereof; or use of said compound of Formula (1) to prepare a medicament for treating an inflammatory and/or immunological disease or disorder in an animal.
Type:
Grant
Filed:
March 11, 2021
Date of Patent:
October 3, 2023
Assignee:
Zoetis Services LLC
Inventors:
Mark R. Cox, Timothy L. Stuk, Todd M. Maddux, Richard Andrew Ewin, Paul D. Johnson, Tomasz Respondek, Graham M. Kyne, Rajendran Vairagoundar
Abstract: Provided herein are compounds, compositions, and methods useful for the treatment of breast cancer, particularly triple negative breast cancers. In certain aspects, provided herein are compounds of formula (I): or a pharmaceutically acceptable salt or solvate thereof. In certain aspects, provided herein are compositions comprising any of the compounds provided herein. In certain aspects, provided herein are methods for the treatment of cancer in a subject in need thereof comprising administering to the subject an effective amount of any of the compounds or compositions provided herein.
Type:
Grant
Filed:
June 13, 2019
Date of Patent:
September 5, 2023
Assignee:
QATAR UNIVERSITY
Inventors:
Ashraf Khalil, Ala-Eddin Al Moustafa, Dana H. Elkhalifa, Feras Alali
Abstract: The invention provides novel polymer-protein conjugates and molecular assemblies for controlled intracellular delivery of proteins, and compositions and methods of preparation and use thereof.
Abstract: Disclosed is a compound of formula (I) in which R1, R2, and R3 are as described herein. Also provided are pharmaceutical compositions comprising the compound of formula (I) and methods of using the compound of formula (I), including a method of treating a disease or disorder and a method for effectuating a G-protein coupled receptor (GPCR)-mediated response in a subject.
Type:
Grant
Filed:
February 6, 2019
Date of Patent:
August 29, 2023
Assignees:
The United States of America, as represented by the Secretary, Department of Health and Human Services, The Johns Hopkins University
Inventors:
Jordi Bonaventura, Juan Luis Gomez, Andrew Horti, Feng Hu, Michael Michaelides, Martin Pomper, Marta Sanchez-Soto