Abstract: {4-[3-(Dimethylamino)propoxy]phenyl}methyl (4S)-4-(propan-2-yl)-3H,4H,5H,6H,7H-imidazo[4,5-c]pyridine-5-carboxylate, and pharmaceutically or veterinarily acceptable salts thereof.
Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a triazole-methyl-piperidinyl-pyrolyl-propenone structure which function as modulators of shared epitope (SE)-calreticulin (CRT) binding and/or interaction, and their use as therapeutics for the treatment of immunoregulatory abnormalities (e.g., autoimmune diseases, inflammatory diseases (e.g., chronic inflammatory disease), and bone erosive diseases) by selectively inhibiting SE-CRT interactions and/or signal transduction pathways commonly overactive or dysregulated in arthritic and/or other diseases or conditions.
Type:
Grant
Filed:
November 7, 2018
Date of Patent:
July 28, 2020
Assignee:
The Regents of the University of Michigan
Abstract: The present invention relates to novel monomaleimide-functionalized platinum compounds of formula (I), including in particular novel monomaleimide-functionalized oxaliplatin and carboplatin derivatives, as well as their use as medicaments, particularly for the treatment or prevention of cancer.
Type:
Grant
Filed:
December 9, 2016
Date of Patent:
July 28, 2020
Assignees:
Medizinische Universität Wien, Universität Wien
Inventors:
Christian Kowol, Petra Heffeter, Walter Berger, Bernhard K. Keppler, Josef Mayr, Verena Pichler
Abstract: Disclosed is a process to produce a purified vapor comprising dialkyl-furan-2,5-dicarboxylate (DAFD). Furan-2,5-dicarboxylic acid (FDCA) and an alcohol in an esterification zone to generate a crude diester stream containing dialkyl furan dicarboxylate (DAFD), unreacted alcohol, 5-(alkoxycarbonyl)furan-2-carboxylic acid (ACFC), and alkyl furan-2-carboxylate (AFC). The esterification zone comprises at least one reactor that has been previously used in an DMT process.
Type:
Grant
Filed:
September 6, 2019
Date of Patent:
July 28, 2020
Assignee:
Eastman Chemical Company
Inventors:
Kevin John Fontenot, Mesfin Ejerssa Janka, Kenny Randolph Parker, Ashfaq Shahanawaz Shaikh
Abstract: Processes for producing ethylene carbonate and/or ethylene glycol, and associated reaction systems are similarly provided. Specifically, a process is provided that comprises supplying an overhead absorber stream withdrawn from an absorber to a vapor-liquid separator to yield an aqueous bottoms stream and a recycle gas stream; supplying an aqueous process stream comprising one or more impurities to a distillation apparatus to yield an overhead impurities stream and a purified aqueous process stream; supplying at least a portion of the purified aqueous process stream and an ethylene oxide product stream to the absorber; and contacting the ethylene oxide product stream with the purified aqueous process stream in the absorber in the presence of one or more carboxylation and hydrolysis catalysts to yield a fat absorbent stream comprising ethylene carbonate and/or ethylene glycol.
Abstract: The present disclosure provides methods to produce 5-(halomethyl)furfural, including 5-(chloromethyl)furfural, by acid-catalyzed conversion of C6 saccharides, including isomers thereof, polymers thereof, and certain derivatives thereof. The methods make use of acids with lower concentrations, and allows for conversion of sugars into 5-(halomethyl)furfural at higher temperatures and faster reaction or residence times.
Type:
Grant
Filed:
June 7, 2018
Date of Patent:
July 14, 2020
Assignee:
MICROMIDAS, INC.
Inventors:
Alex B. Wood, Makoto N. Masuno, Ryan L. Smith, John Bissell, Dimitri A. Hirsch-Weil, Robert Joseph Araiza, Daniel R. Henton, James H. Plonka
Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
Type:
Grant
Filed:
October 22, 2019
Date of Patent:
July 14, 2020
Assignee:
Bristol-Myers Squibb Company
Inventors:
Liqi He, Sanjeev Gangwar, Shoshana L. Posy, Yam B. Poudel, Prasanna Sivaprakasam
Abstract: This invention is benzothiophene-based selective mixed estrogen receptor downregulators and their compositions and uses to treat estrogen-related disorders.
Type:
Grant
Filed:
April 24, 2019
Date of Patent:
July 7, 2020
Assignee:
The Board of Directors of the University of Illinois
Inventors:
Gregory R. Thatcher, Rui Xiong, Yunlong Lu, Jiong Zhao, Debra A. Tonetti
Abstract: The present invention provides compounds of formula I useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
Type:
Grant
Filed:
July 27, 2017
Date of Patent:
July 7, 2020
Assignee:
Padlock Therapeutics, Inc.
Inventors:
Edward Jean Beaumont, Rajesh Devraj, Philip Stephen Kerry, Gnanasambandam Kumaravel, Pui Leng Loke, Mirco Meniconi, Jordan John Palfrey, Carl North, Cristina Lecci, Heather Tye
Abstract: Provided herein are small molecule inhibitors of pendrin. More specifically, the small molecules disclosed herein may be used to inhibit pendrin-mediated anion exchange. These small molecules may be used for treatment of diseases and disorders that are treatable by inhibiting pendrin, such as cystic fibrosis, rhinitis, chronic rhinosinusitis, exposure to an industrial toxin, certain viral infections, certain bacterial infections, and chronic obstructive pulmonary disease. The small molecules may further be used to potentiate a diuretic effect of a diuretic compound. The small molecules may additionally be used to treat hypertension or thyroid conditions.
Type:
Grant
Filed:
February 24, 2017
Date of Patent:
July 7, 2020
Assignee:
The Regents of the University of California
Inventors:
Alan S. Verkman, Peter M. Haggie, Onur Cil
Abstract: The present invention provides compounds that modulate the interaction of TCR with Nck, compositions thereof, and methods of treatment using the same.
Type:
Grant
Filed:
February 27, 2019
Date of Patent:
June 30, 2020
Assignee:
Artax Biopharma Inc.
Inventors:
Julio Castro, Andrés Gagete Mateos, Peter J. Machin, Christopher Loren VanDeusen
Abstract: Provided are: eushearilides; a method for producing eushearilides; a production intermediate; and a pharmaceutical composition containing eushearilides. By having the Wittig reaction process, Mukaiyama Aldol reaction process and Macrolactonizaion process serve as key processes, eushearilides represented by formula (I) are efficiently produced.
Abstract: The present invention provides compositions useful in reducing or preventing pain in a subject in need thereof. In one embodiment, the compositions comprise a halogenated volatile compound. The present invention further includes a method of reducing or preventing pain in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a composition of the invention. Dosing regimens contemplated within the invention include one-time administration, continuous administration or periodic administration.
Type:
Grant
Filed:
September 9, 2019
Date of Patent:
June 23, 2020
Assignee:
Vapogenix, Inc.
Inventors:
Danguole Spakevicius, Heather Giles, Terry Farmer
Abstract: Disclosed are an organic compound selected from a compound represented by Chemical Formula 1A, a compound represented by Chemical Formula 1B, and a combination thereof, an organic thin film including the organic compound, an organic thin film transistor, and an electronic device. The organic compound has liquid crystal properties and exhibits an ordered liquid crystal phase when being heated in a liquid crystal period due to asymmetric substituents and thereby charge mobility may be further improved.
Type:
Grant
Filed:
July 27, 2018
Date of Patent:
June 16, 2020
Assignee:
Samsung Electronics Co., Ltd.
Inventors:
Eun Kyung Lee, Jeong Il Park, Don-Wook Lee
Abstract: Provided is a novel therapeutic agent for glaucoma, which has sGC-activating action. A therapeutic agent for glaucoma or an ocular hypotensive agent, which contains, as an effective component, a compound represented by Formula (I-a) or Formula (I-b) and having a Log D value of more than 1.5 and less than 2.5, or a pharmaceutically acceptable salt thereof. [In formulae (I-a) and (I-b), each symbol is as defined in the description.
Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
Abstract: A process to decarboxylate THCA in cannabis material while minimizing the thermal decomposition of THC and the loss of volatile components such as terpenoids consists of four steps. Prepared cannabis material is first heated to about 105° C. for 20 min. to complete the dehydration of the material. The processing temperature is then increased to about 110° C. for about 30 min. to start the decarboxylation process. Thereafter, the temperature is increased to about 115° C. for about 35 min. Finally, the temperature is increased by about 2.5° C. (but not exceeding 118° C.) for about an additional 15 min. to complete the decarboxylation.
Abstract: The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of RIP2 and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of RIP2-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.
Type:
Grant
Filed:
September 17, 2015
Date of Patent:
June 9, 2020
Assignee:
ONCODESIGN S.A.
Inventors:
Jan Hoflack, Petra Blom, Pascal Benderitter
Abstract: The present invention relates to novel sulfoperoxycarboxylic acid compounds, and methods for making and using them. The sulfoperoxycarboxylic compounds of the invention are storage stable, water soluble and have low to no odor. Further, the compounds of the present invention can be formed from non-petroleum based renewable materials. The compounds of the present invention can be used as antimicrobials, and bleaching agents. The compounds of the present invention are also suitable for use as coupling agents.
Type:
Grant
Filed:
March 29, 2019
Date of Patent:
June 2, 2020
Assignee:
Ecolab USA Inc.
Inventors:
Junzhong Li, Richard K. Staub, David D. McSherry, Keith G. LaScotte, Steven J. Lange, Frank Everts