Abstract: The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.
Type:
Grant
Filed:
July 17, 2019
Date of Patent:
June 22, 2021
Assignee:
BENEVOLENTAI CAMBRIDGE LIMITED
Inventors:
Edward Savory, Michael Higginbottom, Kathryn Oliver, Viet-Anh Anne Horgan
Abstract: Provided herein are compounds of Formulae (RL), (I), (II), (III), (IV), and (V), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, prodrugs, and isotopically labeled derivatives thereof. Also provided are pharmaceutical compositions, kits, and methods involving the inventive compounds for the treatment of metabolic disorders (e.g., diabetes, hyperglycemia, impaired glucose tolerance, insulin resistance, obesity). The compound are useful as substrate selective inhibitors of insulin-degrading enzyme (IDE).
Type:
Grant
Filed:
April 22, 2016
Date of Patent:
June 22, 2021
Assignee:
President and Fellows of Harvard College
Abstract: Disclosed herein are inhibitors of the GGDPS enzyme, and methods for their use in treating or preventing diseases, such as multiple myeloma. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are described.
Type:
Grant
Filed:
April 25, 2018
Date of Patent:
June 15, 2021
Assignees:
BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA, UNIVERSITY OF IOWA RESEARCH FOUNDATION
Abstract: Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein.
Abstract: Provided herein are pharmaceutical compositions comprising deuterated derivatives of psilocybin. The provided compositions may be useful for treating and/or preventing various diseases and conditions, such as mood or psychiatric disorders.
Abstract: The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.
Type:
Grant
Filed:
October 24, 2019
Date of Patent:
May 4, 2021
Assignee:
Cancer Research Technology Limited
Inventors:
Alison E. McGonagle, Allan M. Jordan, Bodhan Waszkowycz, Colin P. Hutton, Ian D. Waddell, James R. Hitchin, Kate M. Smith, Niall M. Hamilton
Abstract: The present technology provides compounds according to Formula I or Formula III as well as compositions including such compounds useful for the treatment of metastatic cancer and/or glaucoma.
Type:
Grant
Filed:
October 31, 2017
Date of Patent:
April 13, 2021
Assignees:
University of Kansas, University of South Florida
Inventors:
Sanket Jaiprakash Mishra, Brian S. J. Blagg, Chad Anthony Dickey
Abstract: It is an object of the present invention to provide a novel and advantageous process for commercially preparing of 2-cyanoimidazole compounds. More particularly, it relates to an efficient method of preparation of cyazofamid synthetic precursor by simultaneous conversion of aldoxime group to the corresponding cyano-derivative and reducing of N-oxygenated-imidazole ring to imidazole under mild conditions using reducing agent selected from the group consisting of metal salts of sulfur-containing derivatives in the presence of a polar organic solvent.
Type:
Grant
Filed:
February 23, 2018
Date of Patent:
April 6, 2021
Assignee:
Adama Makhteshim Ltd.
Inventors:
Meka Bhoopal, Sura Jagadeesh, Bijukumar Gopinathan Pillai, Michael Grabarnik, Doron Mason
Abstract: The specification relates to compounds of Formula (I): and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cell proliferative disorders.
Type:
Grant
Filed:
January 28, 2020
Date of Patent:
March 30, 2021
Assignee:
AstraZeneca AB
Inventors:
Bernard Christophe Barlaam, Daniel Hillebrand O'Donovan, Samantha Jayne Hughes, Thomas Andrew Moss, Johannes Wilhelmus Maria Nissink, James Stewart Scott, Bin Yang
Abstract: Cathepsin-D and angiogenesis inhibitors and compositions thereof for treating breast cancer are provided. More particularly, the embodiments relate to the design and synthesis of inhibitors of Cathepsin D, which exhibits antiproliferative activity and also inhibits angiogenesis. Also provided are compositions thereof for treating breast cancer.
Abstract: The present invention is directed to a method for preparing 5-nitrotetrazolate using a strongly acidic ionic cation exchange resin that has improve yields over prior art methods. The methods disclosed herein can be used either in a batch process or continuous flow reactor. In one exemplary process, starting material sodium 5-aminotetrazolate in solution is added into a reaction vessel containing a strongly acidic ionic cation exchange resin to facilitate production of 5-nitrotetrazolate. Multiple reactors containing resins may be connected in series to improve 5-nitrotetrazolate yields and purity levels.
Type:
Grant
Filed:
October 17, 2019
Date of Patent:
March 16, 2021
Assignee:
U.S. Government as Represented by the Secretary of the Army
Inventors:
R. Hunter Muir, Andrew G. Pearsall, Jerry S. Salan, Matthew L. Jorgensen, Jon G. Bragg, Neha Mehta, John W. Fronabarger, Jason B. Pattison, Lily F. W. Walsh
Abstract: This invention is directed to a process for the preparation of glycopyrrolate tosylate comprising the step of reacting a halogen salt of glycopyrrolate with tosylic acid or a salt thereof in the presence of hydrogen peroxide and at least one unsaturated organic agent.
Abstract: The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.
Type:
Grant
Filed:
May 21, 2020
Date of Patent:
March 9, 2021
Assignee:
Ogeda SA
Inventors:
Hamid R. Hoveyda, Guillaume Dutheuil, Graeme Lovat Fraser, Marie-Odile Roy, Mohamed El Bousmaqui, Frederic Batt
Abstract: The invention relates to salts of Compound 1, crystalline forms thereof, methods of their preparation, pharmaceutical compositions thereof and methods of their use.
Type:
Grant
Filed:
November 27, 2019
Date of Patent:
February 23, 2021
Assignee:
PRAXIS PRECISION MEDICINES, INC.
Inventors:
Nelson B. Olivier, Kiran Reddy, Gabriel Martinez Botella, Magnus Ronn, Paul A. Laskar
Abstract: The present invention provides compounds that modulate protein function, to restore protein homeostasis and/or cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions of these compounds are also provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions are also provided.
Type:
Grant
Filed:
December 18, 2019
Date of Patent:
February 23, 2021
Assignee:
BioTheryX, Inc.
Inventors:
Kyle W. H. Chan, Frank Mercurio, Aparajita Hoskote Chourasia, Leah Fung, Robert Sullivan
Abstract: Disclosed are small molecule therapeutic compounds that are potent inhibitors of arginase 1 and arginase 2 activity. Also disclosed are pharmaceutical compositions comprising the compounds, and methods for using the compounds for treating or preventing a disease or condition associated with arginase activity.
Type:
Grant
Filed:
August 14, 2019
Date of Patent:
February 9, 2021
Assignee:
OncoArendi Therapeutics S.A.
Inventors:
Roman Blaszczyk, Joanna Brzezinska, Anna Gzik, Adam A. Golebiowski, Julita Nowicka, Bartlomiej Borek, Marek Dziegielewski, Karol Jedrzejczak, Krzysztof Matyszewski, Jacek Olczak
Abstract: The present invention relates to a five-membered heteroaryl ring bridged ring derivative, a preparation method therefor and the medical use thereof. In particular, the present invention relates to a new five-membered heteroaryl ring bridged ring derivative as shown in formula (I), a preparation method therefor and a pharmaceutical composition comprising the derivative, and the use thereof as a therapeutic agent, in particular as a TGF-? inhibitor, and the use in the preparation of a drug for treating, preventing or reducing cancers mediated by the over-expression of TGF-?, wherein the definition of each substituent in the general formula (I) is the same as defined in the description.
Abstract: Disclosed herein are novel C17-heteroaryl derivatives of oleanolic acid, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.
Type:
Grant
Filed:
July 31, 2019
Date of Patent:
January 26, 2021
Assignee:
REATA PHARMACEUTICALS, INC.
Inventors:
Xin Jiang, Christopher F. Bender, Melean Visnick
Abstract: The present invention is directed to methods of inhibiting or modulating p97 and compounds and compositions useful in such methods. Diseases and conditions that can be treated with the compounds and compositions of the invention include, but are not limited to, cancer and neurodegenerative disorders susceptible to treatment by modulation or inhibition of p97.
Type:
Grant
Filed:
May 11, 2017
Date of Patent:
January 19, 2021
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
Donna M. Huryn, Peter Wipf, Matthew G. LaPorte