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: 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: 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: 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
Abstract: The invention relates to tungsten oxo alkylidene complexes ligated with a tetraphenylphenoxy ligand and a neutral ligand such as a phosphine or a pyridine, and method of making the complexes. The complexes are useful as catalysts for performing a ring-opening metathesis polymerization of dicyclopentadiene to poly(dicyclopentadiene).
Abstract: The present invention relates in certain aspects to the discovery of novel 2-naphthimidamide compounds that are capable of binding Type II Transmembrane Serine Proteases (TTSPs). In certain embodiments, the compounds of the invention can be used to treat or prevent Influenza A viral infection in a mammal.
Type:
Grant
Filed:
June 11, 2019
Date of Patent:
June 20, 2023
Assignee:
The Regents of the University of Colorado, a body corporate
Abstract: A tetracarboxylic dianhydride includes: at least one acid dianhydride (A) selected from the group consisting of compounds each having an endo/exo type three-dimensional structure represented by a particular general formula and their enantiomeric compounds each having an exo/endo type three-dimensional structure; and/or an acid dianhydride (B) having an endo/endo type three-dimensional structure represented by a particular general formula, wherein a content of the acid dianhydride (B) in a total amount of the acid dianhydrides (A) and (B) is 30 to 100% by mole in a mole ratio.
Abstract: The present invention relates to IL-8 inhibitor compounds, preferably dual CXCR1/CXCR2 receptor inhibitors, useful in the treatment and/or prevention of some sarcomas, preferably in the treatment and/or prevention of osteosarcoma, Ewing sarcoma, rhabdomyosarcoma or lung metastasis associated thereof.
Type:
Grant
Filed:
October 23, 2018
Date of Patent:
May 30, 2023
Assignees:
Dompe' Farmaceutici S.P.A., Research Institute at Nationwide Children's Hospital
Abstract: The present disclosure describes the use of 2,4-disulfonyl phenyl tert-butyl nitron (2,4-ds-PBN) in the treatment of temozolomide drug resistant gliomas. The 2,4-ds-PBN may be used combined with other chemo- and radiotherapies and surgery, including temozolomide, to reduce glioma occurrence, recurrence, spread, growth, metastasis, and vascularization, and to inhibit development of temozolomide resistance.
Abstract: A process for synthesizing an azo compound by oxidation of a hydrogen compound in the presence of a catalyst and a compound of formula (I) is described in which R1, R2 and R3 (R1)(R2)C(PO3(R3)2)2??(I) are as defined. The use of a compound of formula (I) as complexing agent for a catalyst is also described.