Abstract: The present disclosure relates to a novel nucleoside or nucleotide derivative, a racemate thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating viral infection-associated diseases, containing the same as an active ingredient.
Type:
Grant
Filed:
January 24, 2019
Date of Patent:
May 23, 2023
Assignee:
ST PHARM CO., LTD.
Inventors:
Kyungjin Kim, Meehyein Kim, Uk-Il Kim, Yun Young Go, Hwajung Nam, Hyung Tae Bang, Jin Soo Shin, Jihye Yoon, Yejin Jang
Abstract: Crystalline forms of the compound of Formula (I), which modulates the conversion of AMP to adenosine by 5?-nucleotidase, ecto, and compositions containing the compound and methods for preparing the crystalline forms, are described herein. The use of such crystalline form of Formula (I) and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer and immune-related disorders, that are mediated by 5?-nucleotidase, ecto is also provided.
Type:
Grant
Filed:
June 16, 2021
Date of Patent:
May 16, 2023
Assignee:
ARCUS BIOSCIENCES, INC.
Inventors:
Andrew M. K. Pennell, Eric F. Connor, Stephen Edmund Gottschling, Jim Dimetrios Colomvakos, Mohammed Asadullah Khan
Abstract: Disclosed herein is the use of a hyaluronan conjugate for treating pulmonary inflammation, including acute and chronic pulmonary inflammation. Also disclosed herein is the use of a hyaluronan conjugate for treating virus infection. The hyaluronan conjugate is a hyaluronic acid (HA)-nimesulide conjugate.
Abstract: The present invention relates to a novel therapeutic drug for a neurodegenerative disease and an application thereof. Provided is a novel compound of formula (I). The compound can effectively facilitate the proliferation of neural stem cells in both in vitro and in vivo experiments and can be used as a treatment approach for facilitating neuroregeneration to fight against cognitive decline associated with aging or a neurodegenerative disease.
Abstract: The present invention provides a novel nucleoside derivative or a salt thereof, a polynucleotide synthesis reagent, a method for producing a polynucleotide, a polynucleotide, and a method for producing a binding nucleic acid molecule. The nucleoside derivative or a salt thereof of the present invention is represented by the following chemical formula (1). In the chemical formula (1), Su is an atomic group having a sugar skeleton at a nucleoside residue or an atomic group having a sugar phosphate skeleton at a nucleotide residue, and may or may not have a protecting group, L1 and L2 are each independently a straight-chain or branched, saturated or unsaturated hydrocarbon group having 2 to 10 carbon atoms, X1 is an imino group (—NR1—), an ether group (—O—), or a thioether group (—S—), and R1 is a hydrogen atom or a straight-chain or branched, saturated or unsaturated hydrocarbon group having 2 to 10 carbon atoms.
Type:
Grant
Filed:
October 12, 2017
Date of Patent:
May 9, 2023
Assignees:
NEC SOLUTION INNOVATORS, LTD., NATIONAL UNIVERSITY CORPORATION GUNMA UNIVERSITY
Abstract: Disclosed are compounds and compositions for the activation or induction of expression of a pattern recognition receptor (e.g., STING, RIG-I, MDA5), and methods of use thereof.
Abstract: Provided herein are bifunctional compounds with a moiety (e.g., lenalidomide, thalidomide) that is a binder of an E3 ubiquitin ligase (e.g., Cereblon) and another moiety that is a binder of a target protein DOT1L to induce degradation of DOT1L. Also provided are pharmaceutical compositions comprising the bifunctional compounds, and methods of treating and/or preventing diseases (e.g., proliferative diseases, such as cancers). Provided also are methods of inducing the degradation of DOT1L by administering a bifunctional compound or composition described herein, wherein one component of the bifunctional compound is a binder of an E3 ubiquitin ligase (e.g., lenalidomide, thalidomide) and another component of the compound is a binder of the target protein DOT1L in a subject.
Abstract: The present invention relates to methods of treating disorders in which DOT1L-mediated protein methylation plays a part, such as cancer, by administering DOT1L inhibitor compounds and pharmaceutical compositions to subjects in need thereof.
Type:
Grant
Filed:
January 4, 2021
Date of Patent:
April 25, 2023
Assignee:
Epizyme, Inc.
Inventors:
Edward J. Olhava, Richard Chesworth, Kevin W. Kuntz, Victoria M. Richon, Roy M. Pollock, Scott Richard Daigle
Abstract: This invention relates to a prodrug of the monophosphate nucleotide of the well-known oncology drug gemcitabine. Specifically, it relates to gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate when present as a single phosphate diastereoisomer and, in particular, it relates to the (S)-phosphate diastereoisomer which offers a remarkable and unexpected increase in solubility relative to the (R)-diastereoisomer. The (S)-phosphate epimer is also preferentially taken up into cyclodextrin solutions over the (R)-diastereoisomer.
Type:
Grant
Filed:
May 4, 2020
Date of Patent:
April 18, 2023
Assignee:
NuCana plc
Inventors:
Hugh Griffith, Christopher McGuigan, Magdalena Slusarczyk, Michaela Serpi, Valentina Ferrari
Abstract: The disclosure relates to broad spectrum, direct acting antiviral agents. Disclosed is a group of novel nucleoside and nucleotide analogs having a 4-substituted imidazol-2-one heterocycle in place of the pyrimidine base of natural nucleic acid components and their prodrug derivatives (see Formula I).
Abstract: The present invention relates to novel phosphorous (V) (P(V)) reagents, methods for preparing thereof, and methods for preparing organophosphorous (V) compounds by using the novel reagents.
Type:
Grant
Filed:
April 12, 2019
Date of Patent:
March 28, 2023
Assignees:
Bristol-Myers Squibb Company, The Scripps Research Institute
Inventors:
Michael Anthony Schmidt, Bin Zheng, Kyle Knouse, Justine deGruyter, Martin D. Eastgate, Phil Baran, William R. Ewing, Richard E. Olson, Ivar M. McDonald
Abstract: Novel aminoglycosides, represented by Formulae Ia and Ib, as defined in the instant specification, designed to exhibit stop codon mutation readthrough activity, are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic diseases and disorders, such as diseases and disorders associated with stop codon mutations.
Abstract: The present disclosure provides compounds of formulas (1)-(3), and compositions and methods of use thereof. The present disclosure also provides methods of preparing a provided compound and composition, and methods of characterizing a provided compound and composition.
Abstract: The present disclosure discloses a method for preparation of derivatives of gram-positive bacteria surface capsular polysaccharide, and belongs to the field of carbohydrate chemistry. The present disclosure takes glucose as a glycosyl donor to obtain a target ?-glucosidic bond, then successfully synthesizes a disaccharide building block through a method of redox of a glucose C-2 site, and then takes the disaccharide building block as a repeat unit to synthesize a target oligosaccharide structure such as a derivative [?3)-?-D-Manp-(1?4)-?-D-Rhap-(1?]5-Linker of gram-positive bacteria cell wall capsular polysaccharide. A reduction end of decose is linked with a linker to be linked with a protein to make glycoconjugates for immunological studies. The method provided by the present disclosure is simple, time-saving, labor-saving and low-cost, and the resultant derivatives of the gram-positive bacteria surface capsular polysaccharide may be used for development and preparation of medicine related to autism.
Abstract: Disclosed are compounds, compositions and methods for treating of diseases, syndromes, or disorders that are affected by the modulation of STING. Such compounds are represented by Formula (I), wherein R1, R1?, X1, B1, R2, R2?, B2, X2, R3, Z-M-Y, and Y1-M1-Z1 are as defined herein.
Type:
Grant
Filed:
July 16, 2019
Date of Patent:
March 7, 2023
Assignee:
Janssen Biotech, Inc.
Inventors:
Stuart Emanuel, Mark Richter, Peter J. Connolly, James P. Edwards, Guangyi Wang, Santhosh Kumar Thatikonda, Leonid Beigelman, Gilles Bignan, Wim Bert Griet Schepens, Marcel Viellevoye, Johannes Wilhelmus J. F. Thuring
Abstract: The present invention relates to a compound of formula (II) or (IIb) Wherein X, Y, Rx, Ry, R5 and Nu are as defined in the description and in the claims. The compound of formula (II) can be used in the manufacture of oligonucleotides.
Type:
Grant
Filed:
December 21, 2018
Date of Patent:
March 7, 2023
Assignee:
ROCHE INNOVATION CENTER COPENHAGEN A/S
Inventors:
Konrad Bleicher, Joerg Duschmalé, Martina Brigitte Duschmalé, Henrik Frydenlund Hansen, Troels Koch, Meiling Li, Adrian Schaeublin, Xi Shu, Yong Wu
Abstract: A process and materials method for making a glucose tetraester may include reacting glucose with a carboxylic acid to create a glucose pentaester. The glucose pentaester was reacted with a basic reagent to create a glucose tetraester. Glucose was reacted with a carboxylic acid anhydride in the presence of 4-dimethylaminopyridine to create a glucose pentaester product. The glucose pentaester reaction product was separated. The glucose pentaester reaction product was reacted with a basic reagent, wherein the reaction steps may take place at a temperature of about 0° C. to about 60° C. and about ambient pressure, wherein the ratio of the carboxylic acid to the glucose was from about 5:1 to about 50:1, and wherein the ratio of the glucose pentaester to the basic reagent was from about 1:50 to about 1:150.
Abstract: The present invention is directed to co-therapy and methods for the treatment and prevention of glucose-related disorders such as Type 2 diabetes mellitus and Syndrome X. The present invention is further directed to pharmaceutical compositions for the co-therapy and methods described herein.
Type:
Grant
Filed:
January 24, 2017
Date of Patent:
February 14, 2023
Assignee:
Janssen Pharmaceutica NV
Inventors:
Yin Liang, John Ryan, Abraham B. Woldu, Lisa Wu