Abstract: Disclosed herein, inter alia, are certain substituted thieno[3,2-b]pyrimidine compositions and methods for modulating Adenosine Receptors, for example, having the formula:
Abstract: The present disclosure relates to chemical entities useful as inhibitors of Ubiquitin Specific Protease 30 (USP30), pharmaceutical compositions comprising the chemical entities, and methods of using the chemical entities. The chemical entities as disclosed herein can be useful in the treatment of a disease, disorder, or condition involving mitochondrial dysfunction, including neurodegenerative diseases, motor neuron diseases, metabolic disorders, and cancers, among other ailments. Chemical entities disclosed herein include compounds of Formula (II): wherein A, R2, R3, R4, Ra, Rc, Rd, Re, Rf, and m are defined herein.
Type:
Grant
Filed:
October 5, 2018
Date of Patent:
February 15, 2022
Assignee:
FORMA Therapeutics, Inc.
Inventors:
Justin Caravella, Bingsong Han, Cuixian Liu, Stephanos Ioannidis, Alexandre Joseph Buckmelter, David James Richard, Matthew W. Martin, Steven Mischke, Scot Mente
Abstract: Described herein are urea compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of Olig2. Also described herein are methods of using such Olig2 inhibitors, alone and in combination with other compounds, for treating cancer and other diseases. In particular the Olig2 inhibitors may be used to treat glioblastoma.
Type:
Grant
Filed:
August 25, 2017
Date of Patent:
February 8, 2022
Assignee:
CURTANA PHARMACEUTICALS, INC.
Inventors:
Graham Beaton, Stanton F. McHardy, Ambrosio Lopez, Jr., Bismarck Campos, Hua-Yu Leo Wang
Abstract: The present invention is directed to novel protein kinase inhibitors comprising the chemical compound N-(2-chloro-6-methylphenyl)-2-[[2-methyl-6-(3-hydroxypyrrolidin-1-yl)pyrimidin-4-yl]amino]thiazole-5-carboxamide, its pharmaceutically acceptable salts, enantiomers, and enantiomeric mixtures, and methods of use to treat protein kinase-mediated diseases or conditions.
Abstract: This invention relates to xanthine derivative compounds that are inhibitors of BET bromodomains proteins, the method of preparation thereof and applications thereof.
Type:
Grant
Filed:
December 27, 2016
Date of Patent:
January 18, 2022
Assignees:
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), UNIVERSITÉ D'AIX-MARSEILLE, INSTITUT JEAN PAOLI & IRENE CALMETTES
Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g., HDAC2).
Type:
Grant
Filed:
August 31, 2020
Date of Patent:
January 18, 2022
Assignee:
Alkermes, Inc.
Inventors:
Nathan Oliver Fuller, John A. Lowe, III
Abstract: An anesthetic pharmaceutical composition, system and method is provided. The anesthetic pharmaceutical composition comprises an intraoperative local injection and one or more postoperative medications. The intraoperative local injection is long-acting and comprises at least one local anesthetic agent, such as ropivacaine; ketorolac; and at least one steroid, such as dexamethasone. The one or more postoperative medications comprise an atypical opioid agonist, such as tramadol; a non-steroidal anti-inflammatory drug, such as a cyclooxygenase-2 inhibitor; a gamma-aminobutyric acid analogue, such as pregabalin; and acetaminophen. The method comprises the steps of commencing a surgical procedure involving one or more incision sites; injecting an intraoperative local injection at the one or more incision sites; performing and completing the surgical procedure; and administering one or more postoperative medications.
Abstract: A composition containing levosimendan, one or more solubilizing and/or stabilizing agents, and one or more additional pharmaceutically acceptable additives. The one or more solubilizing and/or stabilizing agents may be a cyclodextrin or a cyclodextrin derivative. The cyclodextrin derivative may be a derivative of an alpha-cyclodextrin, or beta-cyclodextrin, or a gamma-cyclodextrin. The cyclodextrin derivative may contain a butyl ether spacer group, an alkyl ether space group, or both. The one or more additional pharmaceutically acceptable additives may be a non-citrate buffer. The composition may be used in a method of treating a health condition, such as heart failure, pulmonary hypertension, chronic kidney disease, amyotrophic lateral sclerosis, stroke, in advance of a planned cardiac surgery, or other health conditions for which a minimally invasive or repeated administration of levosimendan may be beneficial. The composition may be administered subcutaneously.
Type:
Grant
Filed:
August 19, 2019
Date of Patent:
January 4, 2022
Assignee:
TENAX THERAPEUTICS, INC.
Inventors:
Doug Randall, Douglas Hay, Nancy J. M. Hecox
Abstract: The present disclosure relates to novel compounds, and pharmaceutical compositions thereof, useful for treating for treating neurodegenerative diseases, including Alzheimer's disease and cognitive decline. Methods for inhibiting synapse number decline or membrane trafficking abnormalities associated with exposure of a neuronal cell to Abeta species are also disclosed.
Type:
Grant
Filed:
May 15, 2018
Date of Patent:
January 4, 2022
Assignee:
Cognition Therapeutics, Inc.
Inventors:
Gilbert M. Rishton, Gary C. Look, Susan M. Catalano
Abstract: The invention relates to novel heterocyclic compounds having CD73 inhibitory activity and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.
Type:
Grant
Filed:
September 27, 2019
Date of Patent:
December 28, 2021
Assignee:
CALITHERA BIOSCIENCES, INC.
Inventors:
Lijing Chen, Jim Li, Eric B. Sjogren, Roland J. Billedeau
Abstract: A new method for producing a crystalline form of 5-amino-2,3-dihydro-1,4-phthalazinedione (luminol) is provided. Advantageous uses for this crystalline form as a detecting agent or as an agent for forensic purposes are disclosed, as well a pharmaceutical composition containing said crystalline form.
Type:
Grant
Filed:
February 15, 2017
Date of Patent:
December 21, 2021
Assignee:
MetrioPharm AG
Inventors:
Thomas Martin, Josef Breu, Juliane Fleissner, Wolfgang Brysch, Jörg Von Wegerer
Abstract: The present disclosure provides processes for the purification of 2,5-furandicarboxylic acid (FDCA). The present disclosure further provides crystalline preparations of purified FDCA, as well as processes for making the same. In addition, the present disclosure provides mixtures used in processes for the purification of FDCA.
Type:
Grant
Filed:
July 11, 2018
Date of Patent:
December 7, 2021
Assignee:
Stora Enso Oyj
Inventors:
Henricus Johannes Cornelis Den Ouden, Valery Sokolovskii, Thomas R. Boussie, Gary M. Diamond, Eric L. Dias, Guang Zhu, Staffan Torssell, Vincent J. Murphy
Abstract: The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) and/or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP) might be desirable. Various compounds are disclosed, including those of Formula (I).
Type:
Grant
Filed:
November 7, 2017
Date of Patent:
November 23, 2021
Assignee:
Cyclerion Therapeutics, Inc.
Inventors:
Glen Robert Rennie, Timothy Claude Barden, Thomas Wai-Ho Lee, Rajesh R. Iyengar, Takashi Nakai, Ara Mermerian, Lei Jia, Karthik Iyer, G-Yoon Jamie Im, Paul Allan Renhowe, Joon Jung, Peter Germano, Kim Tang
Abstract: The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating cancers.
Type:
Grant
Filed:
October 2, 2019
Date of Patent:
November 23, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Gregory Chin, Michael O' Neil Hanrahan Clarke, Xiaochun Han, Tim Hansen, Yunfeng Eric Hu, Dmitry Koltun, Ryan McFadden, Michael R. Mish, Eric Q. Parkhill, David Sperandio, Lianhong Xu, Hai Yang
Abstract: The invention relates to novel heterocyclic compounds having CD73 inhibitory activity and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.
Type:
Grant
Filed:
September 27, 2019
Date of Patent:
November 16, 2021
Assignee:
CALITHERA BIOSCIENCES, INC.
Inventors:
Lijing Chen, Jim Li, Eric B. Sjogren, Roland J. Billedeau
Abstract: The present disclosure relates to bicyclic heterocycles of Formula (I?), and pharmaceutical compositions of the same, that are inhibitors of the FGFR3 and/or FGFR4 enzyme and are useful in the treatment of FGFR-associated diseases.
Type:
Grant
Filed:
March 12, 2020
Date of Patent:
November 16, 2021
Assignee:
Incyte Corporation
Inventors:
Alexander Sokolsky, Liangxing Wu, Wenqing Yao
Abstract: Compounds of Formula (IA), or a pharmaceutically acceptable salt thereof, and methods of use as Janus kinase inhibitors are described herein.
Type:
Grant
Filed:
June 25, 2019
Date of Patent:
October 26, 2021
Assignee:
Genentech, Inc.
Inventors:
F. Anthony Romero, Mark Zak, Guiling Zhao, Paul Gibbons, Wei Li, Yun-Xing Cheng, Po-Wai Yuen, Limin Cheng
Abstract: This invention relates to the compound (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide, and in particular to novel physical forms of the compound, a process for preparing the compound and synthetic intermediates for use in the process, and novel formulations containing the compound, as well as therapeutic uses of the compound.
Type:
Grant
Filed:
April 20, 2018
Date of Patent:
October 12, 2021
Assignee:
OTSUKA PHARMACEUTICAL CO., LTD.
Inventors:
Michael Reader, Nicola Elizabeth Wilsher, Mark Henry Saunders, Paul Anthony Baguley, Colin Thomas Lindley, Robert Craig Melling, Bozena Ewa Adamczyk, Mirka Scarati
Abstract: Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
Type:
Grant
Filed:
April 10, 2020
Date of Patent:
September 28, 2021
Assignee:
Eisai R&D Management Co., Ltd.
Inventors:
Roch Boivin, Eric Carlson, Atsushi Endo, Hans Hansen, Lynn D. Hawkins, Sally Ishizaka, Matthew Mackey, Sridhar Narayan, Takashi Satoh, Shawn Schiller
Abstract: Provided herein are deuterated compounds and compositions useful in increasing PPAR? activity. The compounds have a formula where L5 comprises at least one deuterium. Exemplary species include The compounds and compositions provided herein are useful for the treatment of PPAR? related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
Type:
Grant
Filed:
December 17, 2019
Date of Patent:
September 28, 2021
Assignee:
The Salk Institute for Biological Studies