Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, Y1, Y2, or L are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Grant
Filed:
July 11, 2014
Date of Patent:
August 23, 2016
Assignee:
Gilead Sciences, Inc.
Inventors:
Mingzhe Ji, Scott E. Lazerwith, Hyung-Jung Pyun
Abstract: Compounds represented by Formula I are provided that include synthetic transtaganolide and basiliolide products. Derivatives of these compounds and methods of synthesis are also provided.
Type:
Grant
Filed:
October 31, 2014
Date of Patent:
August 23, 2016
Assignee:
California Institute of Technology
Inventors:
Hosea Nelson, Kei Murakami, Scott C. Virgil, Brian M. Stoltz, Jonathan R. Gordon
Abstract: The invention provides 5-deuterium-enriched 2,4-thiazolidinediones (e.g., 5-[4-[2-(5-ethyl-2-pyridyl)-2-oxoethoxy]benzyl]-5-deutero-thiazolidine-2,4-dione), deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
Abstract: The present invention relates to new substituted pyrano and furanoquinolines having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
Abstract: The present invention relates to compounds acting as selective inhibitors of CD40-TRAF6 interaction, their use as medicaments and their use in the treatment of (chronic) inflammatory diseases. The present invention also relates to pharmaceutical compositions comprising these compounds.
Abstract: The present invention is directed to a method for producing artemisinin having the formula from dihydroartemisinic acid in a continuous flow reactor using singlet oxygen as well as to the continuous flow reactor for producing artemisinin.
Type:
Grant
Filed:
July 28, 2015
Date of Patent:
August 9, 2016
Assignee:
Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.
Inventors:
Peter H. Seeberger, Daniel Kopetzki, Francois Lévesque
Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
Type:
Grant
Filed:
June 9, 2015
Date of Patent:
August 2, 2016
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
Abstract: The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
Type:
Grant
Filed:
December 30, 2014
Date of Patent:
August 2, 2016
Assignee:
Controlled Chemicals, Inc.
Inventors:
Jules A. Shafer, Vladislav V. Telyatnikov, Hao Wang
Abstract: Described herein are compounds, methods, and kits for long-term tracking of cell proliferation, differentiation, and/or function. The compounds of the present invention are novel cell-tracking reagents, efficiently excitable with a 405-nm violet laser, that provide bright fluorescence intensity, uniform cell staining, and good retention within cells as well as low toxicity toward cells.
Abstract: This invention provides a family of compounds that inhibit Class II fructose 1,6-bisphosphate aldolase (FBA), which is implicated in the pathogenic activity of a broad range of bacterial and parasitic agents. The compounds were identified by empirical testing, and provide a basis for further derivatization and optimization of 8-hydroxyquinoline-2-carboxylic acid and related compounds. Crystal structure shows that the compounds don't bind directly to the catalytic site of the enzyme, and so are not defined simply as substrate analogs. Instead, they create a pocket by induced fit, resulting a powerful and specific inhibitory effect on FBA activity.
Type:
Grant
Filed:
May 8, 2014
Date of Patent:
July 19, 2016
Assignee:
The University of Denver and Regis University
Inventors:
Scott Dusan Pegan, Kateri Ahrendt, Glenn C. Capodagli, Bryan Cowen
Abstract: The present invention features tryptoline derivatives and related compounds having kinase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions, such as cancers, inflammatory disorders, or autoimmune disorders.
Type:
Grant
Filed:
January 9, 2013
Date of Patent:
July 19, 2016
Assignee:
X-Chem, Inc.
Inventors:
Anthony D. Keefe, Richard W. Wagner, Matthew Clark, Ying Zhang, Diana Gikunju, John Cuozzo, Heather Thomson
Abstract: Methods for recovering organic heteroatom compounds from a hydrocarbon feedstock include feeding into a contactor a hydrocarbon feedstock and an aqueous solvent to form an extraction mixture of the aqueous solvent with the hydrocarbon feedstock. The hydrocarbon feedstock includes a hydrocarbon and an organic heteroatom compound. The aqueous solvent includes an ionic liquid formed from pressurized carbon dioxide and water. A pressure and temperature of the extraction mixture may be established that together tune the aqueous solvent to selectively form a solvent complex with the at least one organic heteroatom compound. Then, the solvent complex is extracted to a recovery vessel from the extraction mixture in the contactor. By adjustment of a recovery temperature of the recovery vessel, a recovery pressure of the recovery vessel, or both, the solvent complex decomposes into carbon dioxide and the organic heteroatom compound. The organic heteroatom compound is then recovered from the recovery vessel.
Type:
Grant
Filed:
February 9, 2015
Date of Patent:
July 19, 2016
Assignee:
Saudi Arabian Oil Company
Inventors:
Zaki Yusuf, Ahmad D. Hammad, Stamatios Souentie, Bandar Fadhel, Nayif Rasheedi
Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
Abstract: Disclosed is use of andrographolide derivative as shown by general formula 1 in manufacture of medicaments for anti-hepatitis C virus, and preventing and treating immunological liver damage caused by virus infection and different chemical liver damage.
Type:
Grant
Filed:
February 5, 2013
Date of Patent:
July 12, 2016
Assignee:
Zhengzho University
Inventors:
Guifu Dai, Songlin Zhu, Yanan Wang, Jian Wu, Dan Zhao, Di Wu, Huanfei Liu, Haiwei Xu, Mengjiao Liu, Jing Zhao, Wei Han, Zhenwei Wu, Hang Wang, Hongmin Liu
Abstract: Novel substituted chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described.
Abstract: The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; for use in the treatment of pain.
Abstract: This invention disclose (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone in a single configuration and preparation method and use thereof. The (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone, or a pharmaceutically acceptable salt, an ester, a prodrug or a solvate thereof according to the invention are important intermediates of a variety of anti-viral and anti-tumor active ingredients. A compound obtained from (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone via an acylation reaction can be directly used for preparing various anti-viral and anti-tumor drugs. The Chiral synthesis method and the spontaneous resolution method of the compound of (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone according to the invention have the following advantages: the reaction routes are short and simple with high yield and low cost, which are suitable for industrial application.
Type:
Grant
Filed:
October 10, 2013
Date of Patent:
June 28, 2016
Assignees:
TOPHARMAN SHANGHAI CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, TOPHARMAN SHANDONG CO., LTD.