Abstract: The present invention provides compounds of formula (Id) that are prodrugs of catecholamine for use in treatment of neurodegenerative diseases and disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating neurodegenerative or neuropsychiatric diseases and disorders using the compounds of the invention, in particular Parkinson's disease.
Type:
Grant
Filed:
July 28, 2021
Date of Patent:
July 25, 2023
Assignee:
H. Lundbeck A/S
Inventors:
Klaus Gjervig Jensen, Lisbet Kværnø, Morten Jørgensen, Martin Juhl
Abstract: Processes for the preparation of phosphorylated heptose compounds are provided. Embodiments of the invention relate to the chemical synthesis of heptopyranose phosphate compounds. Also, embodiments of the invention relate to the use of compounds according to the invention in modulating an immune response in a subject.
Type:
Grant
Filed:
May 11, 2018
Date of Patent:
July 25, 2023
Assignees:
UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, NATIONAL RESEARCH COUNCIL OF CANADA
Inventors:
Andrew Cox, Janelle Sauvageau, Stefan Oscarson, Lorenzo Guazzelli
Abstract: The present invention relates to novel spirobicyclic analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
Type:
Grant
Filed:
June 10, 2021
Date of Patent:
July 18, 2023
Assignee:
Janssen Pharmaceutica NV
Inventors:
Jonas Verhoeven, Guido Alfons F. Verniest, Johannes Wilhelmus John F. Thuring, Tongfei Wu, Vineet Pande, Lieven Meerpoel, Dirk Brehmer, Weimei Sun, Scott E. Denmark
Abstract: The present invention provides a crystalline and an amorphous form of a Molnupiravir and methods of making the crystalline form and amorphous form of Molnupiravir.
Abstract: This invention is intended to discover a novel solvent that can be used as an alternative to toluene in the step of deprotection in the method of solid-phase nucleic acid synthesis. With the use of such novel solvent, various problems caused by the use of toluene are dissolved. This invention is also intended to provide a method of solid-phase nucleic acid synthesis in which protected nucleoside phosphoramidites in which a protective group is bonded to a hydroxyl group at the 5?position or the 3? position of a nucleoside are sequentially bound on a solid phase carrier, where a reaction of removing the protecting group from the protected nucleoside phosphoramidite is carried out in a solution comprising an acid with a pKa of 0.2 to 0.8 and acetonitrile.
Abstract: Mithramycin (MTM) short side chain ketone (SK) derivatives and MTM short side chain diketone (SDK) derivatives are provided. The MTM SK and MTM SDK derivatives are useful for treatment of cancer or neuro-diseases associated with an aberrant erythroblast transformation-specific transcription factor. Unique MTM SK and MTM SDK derivatives have increased selectively toward ETS transcription factor.
Type:
Grant
Filed:
September 20, 2019
Date of Patent:
July 4, 2023
Assignee:
University of Kentucky Research Foundation
Abstract: The present patent application relates to the use of an innovative amino acid derivative of glucosamine having the Formula 1 of the general structure which follows, or of a pharmaceutical composition which contains it as a single active ingredient or in association with one or more further active ingredients for the preparation of a medicament for the treatment or prophylaxis of diseases involved mainly with the regulation of the turnover of macromolecules that make up the ECM of connective tissue in general and more specifically of the cartilage.
Abstract: The invention relates to novel compositions and methods of using maribavir which enhance its effectiveness in medical therapy, as well as to maribavir isomers and methods of use thereof for counteracting the potentially adverse effects of maribavir isomerization in vivo in the event it occurs.
Abstract: The present disclosure relates to novel methods for preparing antibacterial aminoglycoside compounds and the compounds used in such preparations.
Type:
Grant
Filed:
August 24, 2018
Date of Patent:
June 13, 2023
Assignee:
Revagenix, Inc.
Inventors:
Andrew Calabrese, Timothy Robert Kane, Darin Hildebrandt, Michael Lopez, Nikolai Evdokimov, Frederick Cohen, Malken Bayrakdarian, Sanjia Xu, Samuel Desjardins, Olivier Soueidan
Abstract: The present invention pertains to novel uses of glycyrrhetinic acid (GA), glycyrrhizic acid (GR) and related compounds for mitigation and/or treatment of pneumonitis/pneumonia/pulmonary fibrosis induced by various chemicals/bioagents and/or pathogens, such as anti-cancer therapies and/or virus. Also embodied are therapeutic uses of prodrugs, metabolites, derivatives (e.g., acids, esters and ethers), and salts of glycyrrhetinic acid (GA) and glycyrrhizic acid (GR) in a form of drugs, health products, foods or food additives.
Abstract: The present invention relates to methods of treating immune disorders and/or inflammation using certain modulator compounds. In one embodiment, the present invention provides a method of treating an immune and inflammatory disorders disorder by administering a composition comprising a therapeutically effective dosage of an ascaroside compound, or a mixture of ascaroside compounds, or a mixture containing at least one ascaroside.
Type:
Grant
Filed:
August 1, 2022
Date of Patent:
June 13, 2023
Assignees:
California Institute of Technology, Boyce Thompson Institute for Plant Research
Inventors:
Andrea Choe, Paul W. Sternberg, Frank C. Schroeder, Stephan H. Von Reuss
Abstract: High-purity hydrous D-allose crystals and a method of efficiently obtaining the crystals are provided. To a D-allose-containing solution having a purity of D-allose of at least 80% (g/g) in a solute, in a metastable region in a supersaturated state of 30° C. or less, D-allose seed crystals are added. Then, the temperature of the solution is lowered by 10° C. or more for cooling and crystallization to initially obtain “hydrous D-allose crystals”, and the crystallization water thereof is removed in a specified temperature zone to obtain novel “anhydrous D-allose crystals”.
Abstract: A cyclic dinucleotide compound of Formula (I): wherein X1 is H or F; X2 is H or F; at least one among X1 and X2 is a fluorine atom; Z is OH, OR1, SH or SR1, wherein: R1 is Na or NH4, or R1 is an enzyme-labile group which provides OH or SH in vivo such as pivaloyloxymethyl; B1 and B2 are bases chosen from Adenine, Hypoxanthine or Guanine, and B1 is a different base than B2 and a pharmaceutically acceptable salt thereof. Pharmaceutical compositions including the cyclic dinucleotide, as well as their use in the treatment of a bacterial infection, a viral infection or a cancer are also described.
Abstract: According to the present invention, there are provided a benzimidazole carbamate-sugar compound conjugate compound represented by the following Chemical Formula 1, a preparation method thereof, and a use thereof as an anti-cancer agent: Wherein, R1, R2, R3 and X are as defined in the specification and claims.
Abstract: The present invention relates to certain SGLT-2 inhibitors for treating, preventing, protecting against and/or delaying the progression of chronic kidney disease in patients, for example patients with prediabetes, type 1 or type 2 diabetes mellitus.
Type:
Grant
Filed:
November 10, 2020
Date of Patent:
June 6, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Uli Christian Broedl, Odd-Erik Johansen, Eric Williams Mayoux, Nima Soleymanlou, Maximilian von Eynatten, Hans-Juergen Woerle, David Z.I. Cherney, Bruce A. Perkins
Abstract: The present invention relates to a method for preparing stereodefined phosphorothioate oligonucleotides, especially locked stereodefined phosphorothioate oligonucleotides with a high yield, using pyridinium acidic salts as a coupling activator.
Abstract: Methods for preparing 3?-O-amino-2?-deoxyribonucleoside-5?-triphosphates with reduced 3?-hydroxy-2?-deoxyribonucleoside-5?-triphosphate contamination by converting 3?-(N-acetone-oxime)-2?-deoxynucleoside triphosphate to 3?-O-amine-2?-deoxynucleoside triphosphate by treatment with an aryl-oxyamine and compositions produced therefrom.
Abstract: The present invention is directed to compounds of the formula (I), wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
Type:
Grant
Filed:
October 9, 2018
Date of Patent:
May 30, 2023
Assignee:
BRISTOL-MYERS SQUIBB COMPANY
Inventors:
Brian E. Fink, Dharmpal S. Dodd, Yufen Zhao, Lan-Ying Qin, Zheming Ruan, Lalgudi S. Harikrishnan, Muthoni G. Kamau
Abstract: Provided are methods for treating 2019-nCoV virus (SARS-CoV-2) infections by administering nucleosides and prodrugs thereof, of Formula I: wherein the 1? position of the nucleoside sugar is substituted.
Type:
Grant
Filed:
January 26, 2021
Date of Patent:
May 30, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Tomas Cihlar, Anuoluwapo Osinusi, Danielle L. Porter