Abstract: Provided are compounds generated by conjugation of triptolide with glucose to form glucose-triptolide conjugates, provides compounds with effective anti-proliferative activity and improved tolerability as compared to naturally occurring triptolide compounds.
Type:
Grant
Filed:
February 3, 2017
Date of Patent:
June 30, 2020
Assignees:
The Johns Hopkins University, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences
Inventors:
Jun Liu, Qingli He, Martin G. Pomper, Il Minn, Biao Yu, Qiaoling Wang
Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection, with a nucleoside, a nucleotide and an analog thereof.
Type:
Grant
Filed:
February 13, 2018
Date of Patent:
June 30, 2020
Assignee:
Janssen BioPharma, Inc.
Inventors:
Natalia Dyatkina, Guangyi Wang, Leonid Beigelman, Vivek Kumar Rajwanshi
Abstract: Provided are a solid preparation comprising an alkyl cellulose which provides excellent moldability and disintegrability even in a small amount of the alkyl cellulose, and a production method therefor. Specifically, provided are a solid preparation having an alkyl cellulose having a specific surface area by BET method of 0.5 to 10.0 m2/g and a dissolution start temperature of 5 to 27° C.; and a method for producing a solid preparation having the steps of: mixing a cellulose pulp and a first alkali metal hydroxide solution with stirring to obtain alkali cellulose, reacting the alkali cellulose with an alkylating agent to obtain a first reaction mixture, mixing the first reaction mixture and a second alkali metal hydroxide solution with stirring and without further addition of any alkylating agent to obtain a second reaction mixture, and pulverizing an alkyl cellulose isolated from the second reaction mixture to obtain an alkyl cellulose.
Abstract: The present disclosure relates to processes for inverting oligonucleotide probes in an in situ synthesized array. These processes can be used to reverse the orientation of probes with respect to the substrate from 3?-bound to 5?-bound. These processes can also be used to reduce or eliminate the presence of truncated probe sequences from an in situ synthesized array.
Abstract: The invention is directed to a method for improving learning and/or memory (e.g., auditory, visual, somatosensory or motor) in adults and children of an age which is beyond the early critical period for learning, said method comprising inhibiting (i) ecto-5?-nucleotidase (Nt5e, aka CD73) or (ii) A1 adenosine receptor (A1R, aka Adora1) expression or function in the brain. The invention is also directed to a method for treating learning and memory defects and neurological diseases associated with an abnormal auditory, visual, or somatosensory perception by inhibiting Nt5e or A1R expression or function in the brain.
Type:
Grant
Filed:
February 18, 2016
Date of Patent:
June 30, 2020
Assignee:
ST. JUDE CHILDREN'S RESEARCH HOSPITAL, INC.
Inventors:
Stanislav S. Zakharenko, Jay A. Blundon
Abstract: The present disclosure provides methods of making nicotinoyl riboside compounds or derivatives of formula (I): wherein X?, Z1, Z2, n, R1, R2, R3, R4, R5, R6, R7, and R8 are described herein, reduced analogs thereof, modified derivatives thereof, phosphorylated analogs thereof, and adenylyl dinucleotide conjugates thereof, or salts, solvates, or prodrugs thereof; and novel crystalline forms thereof.
Type:
Grant
Filed:
November 10, 2017
Date of Patent:
June 23, 2020
Assignees:
The Queen's University of Belfast, ChromaDex Inc.
Inventors:
Marie Eugenie Migaud, Philip Redpath, Kerri Crossey, Richard Cunningham, Aron Erickson, Richard Nygaard, Amanda Storjohann
Abstract: A method comprises: sorbing a sample solution comprising nucleic acids to a sample receiving portion of a quartz fiber filter by contacting the sample solution with the sample receiving portion; and washing the sample receiving portion while keeping most of nucleic acids around the sample receiving portion by flowing a wash solution through the sample receiving portion under a wicking force directed away from the sample receiving portion. An associated apparatus is also provided.
Type:
Grant
Filed:
May 22, 2018
Date of Patent:
June 16, 2020
Assignee:
General Electric Company
Inventors:
Lin Chen, Bing Zhang, Klaus Hochleitner, Rong Hou, Yanju Wang
Abstract: Described are arylnaphthalene lactone derivatives. Also disclosed herein are methods of use of the arylnaphthalene lactone derivatives as anticancer agents.
Type:
Grant
Filed:
April 26, 2017
Date of Patent:
June 16, 2020
Assignee:
OHIO STATE INNOVATION FOUNDATION
Inventors:
James Fuchs, Alan Douglas Kinghorn, Andrew Huntsman
Abstract: The present disclosure provides procedures and intermediates for the preparation of Sofosbuvir, comprising the step of reacting a compound of formula 2: wherein R1 and R2 can independently be hydrogen or halogen, provided that at least one of R1 and R2 is a halogen.
Abstract: The present invention relates to methods of treating infectious, inflammatory and post-traumatic disorders by administering various compounds newly discovered to have TLR4 inhibitory activity. In addition to methods of treatment, the present invention further provides for pharmaceutical compositions comprising said compounds, together with a suitable pharmaceutical carrier.
Type:
Grant
Filed:
June 1, 2018
Date of Patent:
June 2, 2020
Assignees:
The John Hopkins University, University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
David Hackam, Chhinder P. Sodhi, Peter Wipf
Abstract: Pharmaceutical compositions comprising a first anti-acne compound, a second anti-acne compound, and an anti-photoaging compound are described. Methods for the treatment of acne and photoaging using the compositions are also described.
Abstract: The present invention relates to a novel compound of 4?-thionucleoside, a preparation method therefor, a pharmaceutical composition comprising the same and an application thereof. Specifically, the present invention relates to a phosphamide derivative of 4?-thionucleoside, a preparation method therefor, a pharmaceutical composition comprising the same, a use thereof in the preparation of a medicine for preventing or treating abnormal cell proliferation diseases (for example, tumors or cancers and related diseases) or virus infectious diseases, and a method of using the same for preventing or treating abnormal cell proliferation diseases (for example, tumors or cancers and related diseases) or virus infectious diseases.
Inventors:
Hong Ye, Gang Liu, Nan Yu, Hong Zeng, Mingliang Zhao, Yan Qing, Hua Deng, Wenjia Li, Donghong Li, Donghai Su, Wei Zhong, Shaohua Li, Xunwei Wu, Lichun Wang, Jingyi Wang
Abstract: The present invention relates to inorganic salts of nicotinic acid mononucleotides and compositions of Formula I, useful in the treatment of disorders and diseases associated with deficiencies in NAD+: wherein A, M1, M2, k, R1, R2, and R3 are as described herein.
Type:
Grant
Filed:
April 3, 2019
Date of Patent:
May 19, 2020
Assignees:
Jumpstart Fertility Pty Ltd, Life Biosciences, Inc.
Inventors:
Michel Wathier, Roland Dolle, Sebastian Mario Marcuccio, Rohan David Joyce, Simon Tucker
Abstract: A process for preparing an aqueous solution of a methylcellulose having anhydroglucose units joined by 1-4 linkages wherein hydroxy groups of anhydroglucose units are substituted with methyl groups such that s23/s26 is 0.36 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 3-positions of the anhydroglucose unit are substituted with methyl groups and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 6-positions of the anhydroglucose unit are substituted with methyl groups, comprises the step of mixing the methylcellulose with an aqueous liquid at a temperature of not higher than 10° C. at a shear rate of at least 1000 s?1.
Type:
Grant
Filed:
October 25, 2017
Date of Patent:
April 21, 2020
Inventors:
Puspendu Deo, Kathryn Brown, David E. Wallick, Robert L. Sammler, Yongfu Li
Abstract: The invention relates to compounds and compositions for modulation of nicotinamide adenine dinucleotide (NAD+). The invention also relates to methods of making such compounds and compositions. The invention relates to pharmaceutical compositions containing one or more NAD+ modulating compounds as a first ingredient in combination with one or more active pharmaceutical ingredients. Further, the invention relates to methods of using such compounds or compositions to promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and/or improving cell and tissue survival.
Type:
Grant
Filed:
March 22, 2019
Date of Patent:
April 14, 2020
Assignee:
Metro International Biotech, LLC
Inventors:
Bruce Szczepankiewicz, James M. McKearin
Abstract: Provided herein are methods for the synthesis of oligomeric compounds wherein removal of the 5?-terminal trityl group is performed at reduced temperature and lower pH relative to standard methods. In certain embodiments, the present methods provide detritylated oligomeric compounds having a reduced percentage of depurination relative to the same detritylated oligomeric compounds prepared using standard methods. In certain embodiments, the present methods provide detritylated oligomeric compounds with increased purity relative to the same detritylated oligomeric compounds prepared using standard methods. In certain embodiments, the present methods provide an increased rate of detritylation compared to standard methods.
Abstract: Provided herein are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, and compositions comprising such compounds that are useful for increasing the amount of NAD+ in cells. Also disclosed are methods of using the disclosed compounds and compositions for treating mitochondrial-related diseases or disorders.
Abstract: The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
Type:
Grant
Filed:
January 15, 2019
Date of Patent:
March 24, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Daniel DiRocco, Artis Klapars, Edward C. Sherer
Abstract: The present invention relates to the field of oligonucleotide conjugates and to methods of synthesis thereof. In the present method a low-water content solvent environment allows a more efficient conjugation, reducing the amount of conjugate moiety needed and increasing the conjugation reaction speed.
Type:
Grant
Filed:
September 29, 2016
Date of Patent:
March 3, 2020
Assignee:
Roche Innovation Center Copenhagen A/S
Inventors:
Dennis Jul Hansen, Christoph Rosenbohm, Michael Meldgaard