Abstract: The present invention provides 11-arylcinnolino[2,3-f]phenanthridinium salt compounds and method for producing the same by highly regioselective synthesis of 11-phenylimino[2,3-f]phenanthridin-9-ium salts from 2-azobiaryls and alkenes under catalysis of palladium, through double oxidative C—H coupling of alkenes, to give the polycyclic cinnolinophenanthridinium salts in moderate yields. The reaction mechanism involves ortho C—H olefination of 2-azobiaryls by alkenes, intramolecular aza-Michael addition, ?-hydride elimination, electrophilic palladation followed by intramolecular C—H activation and reductive elimination. The prepared quaternary ammonium salts are candidate materials for solution-processable OLED and bioimaging materials.
Abstract: A 9-(2-hydroxyquinolin-3-yl)-10-(2-hydroxyethyl)-3,3,6,6-tetramethyl-3,4,6,7,9,10-hexahydroacridine1,8(2H,5H)-dione compound, its synthesis, and its use as an antimicrobial agent.
Type:
Grant
Filed:
November 16, 2023
Date of Patent:
April 30, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Hany Mohamed Abd El-Lateef Ahmed, Mai Mostafa Khalaf Ali, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
Abstract: The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
Type:
Grant
Filed:
November 8, 2022
Date of Patent:
April 30, 2024
Assignee:
Ajax Therapeutics, Inc.
Inventors:
Craig E. Masse, Jeremy R. Greenwood, Jiayi Xu, Sayan Mondal, Phani Ghanakota
Abstract: The present invention relates to novel oxazolidinones (Formula I): or a pharmaceutically acceptable salt having ring A characterized by N-containing monocyclic, bicyclic or spirocyclic substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.
Type:
Grant
Filed:
January 13, 2020
Date of Patent:
April 23, 2024
Assignee:
The Global Alliance for TB Drug Development, Inc.
Inventors:
Christopher B. Cooper, Haihong Huang, Dongfeng Zhang, Nader Fotouhi, Takushi Kaneko
Abstract: Preparation of optionally substituted dihydroisoquinolines. The present invention relates to a process for the preparation of optionally substituted dihydroi-soquinolines of the formula I.
Type:
Grant
Filed:
January 14, 2019
Date of Patent:
April 16, 2024
Assignee:
BASF SE
Inventors:
Bernd Mueller, Michael Rack, Michael Seet, Ana Escribano Cuesta, Jan Klaas Lohmann, Georg Christoph Rudolf, Markus Nett, Rainer Hoffmann
Abstract: The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.
Type:
Grant
Filed:
November 16, 2020
Date of Patent:
April 16, 2024
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Christopher F. Claiborne, Todd B. Sells, Stephen G. Stroud
Abstract: Synthetic amino acid-modified polymers and methods of making the same and using the same are disclosed. The synthetic amino acid-modified polymers possess distinct thermosensitive, improved water-erosion resistant, and enhanced mechanical properties, and are suitable of reducing or preventing formation of postoperative tissue adhesions. Additionally, the amino acid-modified polymers can also be used as a vector to deliver pharmaceutically active agents.
Abstract: A compound represented by the following formula (A) has excellent control efficacy against weeds, and shows high safety against useful plants.
Abstract: A medicament for preventive and/or therapeutic treatment of multiple sclerosis, especially a pain accompanying multiple sclerosis such as neuropathic pain, which contains a compound having a P2X4 receptor antagonist activity such as a compound represented by the general formula (IH), or a salt thereof or a hydrate or solvate thereof as an active ingredient.
Type:
Grant
Filed:
April 27, 2017
Date of Patent:
March 5, 2024
Assignees:
NIPPON CHEMIPHAR CO., LTD., KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION
Abstract: The present embodiments are directed, in part, to compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof for modulating the activity of S1P1 receptor and methods of using the same.
Type:
Grant
Filed:
June 12, 2018
Date of Patent:
February 27, 2024
Assignee:
TREVENA, INC.
Inventors:
Philip Michael Pitis, Robert Eugene Boyd, Tamara Ann Miskowski Daubert, Michael John Hawkins, Guodong Liu, Aimee Crombie Speerschneider
Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
Type:
Grant
Filed:
September 24, 2020
Date of Patent:
February 20, 2024
Assignee:
Amgen Inc.
Inventors:
Brian Alan Lanman, Jian Chen, Anthony B. Reed, Victor J. Cee, Longbin Liu, David John Kopecky, Patricia Lopez, Ryan Paul Wurz, Thomas T. Nguyen, Shon Booker, Nobuko Nishimura, Youngsook Shin, Nuria A. Tamayo, John Gordon Allen, Jennifer Rebecca Allen
Abstract: A N?-(2-(5-(4-chlorophenyl)-1,3,4-oxadiazol-2-ylthio)acetoxy)-4-methoxybenzimidamide compound, its synthesis, and its use as an antimicrobial agent.
Type:
Grant
Filed:
October 11, 2023
Date of Patent:
February 13, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
Abstract: Certain embodiments of the present invention relate to methods of forming and manipulating bioconjugates. Particularly, but not exclusively certain embodiments relate to methods of reversible carbon-carbon bond bioconjugation using aldol based chemical reactions at physiological conditions.
Type:
Grant
Filed:
September 27, 2017
Date of Patent:
February 13, 2024
Assignee:
The University of York
Inventors:
Martin A. Fascione, Richard J. Spears, Robin Brabham, Darshita Budhadev, Tessa Keenan
Abstract: The present invention relates to combination therapies for treating KRas G12C cancers. In particular, the present invention relates to methods of treating cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a combination of a an agent that blocks Programmed Death-1 receptor (PD-1) and Programmed Death Ligand-1 (PD-L1) signaling and a KRAS G12C inhibitor of Formula (I), Formula I-A or Formula I-B, kits comprising the compositions and methods of use therefor.
Type:
Grant
Filed:
September 23, 2020
Date of Patent:
February 6, 2024
Assignee:
Mirati Therapeutics, Inc.
Inventors:
David Briere, James Gail Christensen, Peter Olson
Abstract: Provided are novel crystalline forms of a spiro-compound which acts as a muscarinic acetylcholine receptor agonist. In particular, isolated crystalline polymorphs of (S)-2-ethyl-8-methyl-1-thia-4,8-diazaspiro[4.5]decane-3-one are described which have favorable properties in pharmaceutical manufacture. Also provided are methods to prepare said crystalline polymorphs, and to convert them into each other as well as methods for preparing medicaments containing the same which are suitable for use in the treatment of diseases and disorders that respond to modulation of the muscarinic acetylcholine receptor.
Type:
Grant
Filed:
December 22, 2020
Date of Patent:
January 9, 2024
Assignee:
NSC Therapeutics GmbH
Inventors:
Abraham Fisher, Nira Bar-Ner, Manfred Windisch
Abstract: A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.
Abstract: Compounds useful as contrast agents in image-guided surgery are provided. The compounds comprise a latent cationic lysosomotropic fragment that is detectable upon cleavage by lysosomal proteases within treated tissues, particularly within tumors and other diseased tissues. Also provided are compositions comprising the compounds and methods for using the compounds, for example in dynamically monitoring protease activity in vivo during image-guided tumor resection surgery.
Type:
Grant
Filed:
March 30, 2018
Date of Patent:
November 28, 2023
Inventors:
Matthew S. Bogyo, Martijn Verdoes, Leslie Ofori, Nimali P. Withana
Abstract: The present invention relates to amino pyrazine purine compounds that are useful as kinase inhibitors. More particularly, the present invention relates to 5-(2-(8-Oxa-3-azabicyclo[octan-3-yl)-9-(pentan-3-yl)-9H-purine-6-yl)pyrazin-2-amine compounds, including pharmaceutically acceptable salts thereof, method of preparations, pharmaceutical compositions containing these compounds and uses of these compounds in modulating phosphoinositide 3-kinase (PI3K-AKT), mammalian target of rapamycin (mTOR), DNA-PK and ATM kinase, and may be used as therapeutic agents or diagnostic probes and for the treatment of a number of proliferative conditions or disorders including tumors, cancers, hematological and lymphatic and B-malignancies, immunological and gene alterations disorders, inflammation, certain metabolic diseases, cardiovascular diseases, obesity, type 2 diabetes, anti-aging and neurological disorders.