Abstract: Disclosed is a combination of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate (chemical name: 2?-Deoxy-2?,2?-difluoro-D-cytidine-5?-O-[phenyl (benzoxy-L-alaninyl)]phosphate) (NUC-1031) and a platinum-based anticancer agent selected from carboplatin, dicycloplatin, oxaliplatin, satraplatin and nedaplatin. The combinations are useful in the treatment of cancer and particularly ovarian cancer.
Abstract: Embodiments of the present invention relate to 6-6 bicyclic aromatic ring substituted nucleoside analogues, including, for example, the following compound: Embodiments of the present invention also relate to uses of the disclosed compounds for the inhibition of protein arginine methyltransferase 5 (PRMT5).
Type:
Grant
Filed:
August 25, 2016
Date of Patent:
May 19, 2020
Assignee:
Janssen Pharmaceutica NV
Inventors:
Tongfei Wu, Dirk Brehmer, Lijs Beke, An Boeckx, Gaston Stanislas Marcella Diels, Ronaldus Arnodus Hendrika Joseph Gilissen, Edward Charles Lawson, Vineet Pande, Marcus Cornelis Bernardus Catharina Paradé, Wim Bert Griet Schepens, Johannes Wilhelmus John F. Thuring, Marcel Viellevoye, Weimei Sun, Lieven Meerpoel
Abstract: The present invention provides highly active cyclic-di-nucleotide (CDN) immune stimulators that activate DCs via a recently discovered cytoplasmic receptor known as STING (Stimulator of Interferon Genes). In particular, the CDNs of the present invention are provided in the form of a composition comprising one or more cyclic purine dinucleotides induce STING-dependent type I interferon production, wherein the cyclic purine dinucleotides present in the composition are substantially pure 2?,5?,2?,5? and 2?,5?,3?,5? CDNs, and preferably Rp,Rp stereoisomers thereof.
Type:
Grant
Filed:
July 31, 2017
Date of Patent:
May 19, 2020
Assignees:
ADURO BIOTECH, INC., THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Inventors:
Thomas W. Dubensky, Jr., David B. Kanne, Meredith Lai Ling Leong, Edward Emile Lemmens, Laura H. Glickman, Russell E. Vance
Abstract: Provided are methods and compositions for treating hematological malignancies in patients carrying an IDH1 mutation using a combination of an inhibitor of mutant IDH1 enzyme, (S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide, or a pharmaceutically acceptable salt thereof (COMPOUND 2) and a DNA demethylating agent.
Inventors:
Samuel V. Agresta, Krishnan Viswanadhan, Jorge DiMartino, Vivek Saroj Kumar Chopra, Kyle J. MacBeth, Robert Douglas Knight, Laurie Kenvin, Qiang Xu
Abstract: The present invention provides a nicotinamide mononucleotide derivative, or salt thereof, which is a compound represented by general formula (1), wherein R1 and R2 respectively and independently represent a hydrogen atom or acyl group having 3 to 30 carbon atoms, the hydrocarbon group bound to the carbonyl carbon of the acyl group is a linear or branched, saturated or unsaturated hydrocarbon group, and at least one of R1 and R2 is the acyl group.
Abstract: Provided are novel purine nucleoside/nucleotide analogues compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are inhibitors of CD73 and are useful in the treatment of cancer.
Type:
Grant
Filed:
April 23, 2015
Date of Patent:
May 19, 2020
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Salvacion Cacatian, David A. Claremon, Lanqi Jia, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Yajun Zheng
Abstract: The present disclosure provides pharmaceutical compositions comprising cytidine analogs for oral administration, wherein the compositions release the cytidine analog substantially in the stomach. Also provided are methods of treating diseases and disorders using the oral formulations provided herein.
Type:
Grant
Filed:
September 25, 2019
Date of Patent:
May 12, 2020
Assignee:
Celgene Corporation
Inventors:
John F. Traverse, William W. Leong, Jeffrey B. Etter, Mei Lai, Jay Thomas Backstrom
Abstract: Methods for processing polynucleotide-containing biological samples, and materials for capturing polynucleotide molecules such as RNA and/or DNA from such samples are provided. The RNA and/or DNA is captured by polyamindoamine (PAMAM (Generation 0)) bound to a surface, such as the surface of magnetic particles. The methods and materials have high efficiency of binding RNA and of DNA, and of release, and thereby permit quantitative determinations. The binding particles can be coated with PAMAM (Generation 0) dendrimer which is amide-bonded to the binding particles, wherein at least a portion of the nucleic acids in the biological sample become reversibly bonded to the binding particles.
Type:
Grant
Filed:
October 12, 2018
Date of Patent:
March 17, 2020
Assignee:
HANDYLAB, INC.
Inventors:
Sundaresh N. Brahmasandra, Elizabeth Craig
Abstract: The invention provides a process for the preparation of nicotinamide mononucleotide having formula (I): The method involves the protection of nicotinamide riboside by ketalization, followed by phosphorylation and then deprotection to provide nicotinamide mononucleotide.
Type:
Grant
Filed:
March 24, 2016
Date of Patent:
March 17, 2020
Assignee:
CORNELL UNIVERSITY
Inventors:
Anthony Sauve, Farheen Sultana Mohammad
Abstract: A non-enzymatic method is provided for binding a first nucleic acid chain to a second nucleic acid chain without introducing a sulfur atom into the combined nucleic acid chain, the method comprising reacting a first nucleic acid chain having a phosphorothioate group at the 3? or 5? terminus with a second nucleic acid chain having a hydroxyl group or an amino group at the 3? or 5? terminus in the presence of an electrophile that has a leaving group and is configured to leave the leaving group and bind to a sulfur atom of the phosphorothioate group of the first nucleic acid chain at the site to which the leaving group had been bound, and remove the sulfur atom from the phosphorothioate group of the first nucleic acid chain and a hydrogen atom from the hydroxyl group or from the amino group of the second nucleic acid chain via a nucleophilic substitution with an oxygen atom of the hydroxyl group or a nitrogen atom of the amino group of the second nucleic acid chain, and thereby form a bond between a phosphorus a
Abstract: Broth compositions prepared from poultry materials are disclosed. Selected poultry raw materials are processed to obtain a broth having high protein content and high chondroitin sulfate. Certain specific amino acids are present at higher concentration as compared to home-made broth and other commercial products. The disclosed broth compositions are effective in preventing and/or treating joint diseases and may also provide other nutritional and health benefits.
Type:
Grant
Filed:
July 8, 2014
Date of Patent:
February 11, 2020
Assignee:
INTERNATIONAL DEHYDRATED FOODS, INC.
Inventors:
Roger L. Dake, Stephanie Lynch, Paul L. Durham, Ryan J. Cady, Jordan L. Hawkins
Abstract: Disclosed herein are methods of preparing a nucleoside analog, Compound (I): or a pharmaceutically acceptable salt thereof, which is useful in treating diseases and/or conditions such as viral infections, and intermediates thereof.
Type:
Grant
Filed:
February 26, 2018
Date of Patent:
December 31, 2019
Assignee:
ALIOS BIOPHARMA, INC.
Inventors:
Vladimir Serebryany, Jyanwei Liu, Leonid Beigelman
Abstract: A method of obtaining a polyalkoxylated nucleic acid, which can be used to make a modified drug, from a liquid mixture of polyalkoxylated and non-polyalkoxylated nucleic acids is described. The method involves use of a solvent or a mixture of solvents that allow the polyalkoxylated nucleic acids to precipitate out of the solution.
Abstract: This invention relates to antisense oligonucleotides comprising at least one N3??P5? phosphorodiamidate linkage (NPN) in the backbone, useful for modulating gene expression involved in the pathogenesis of a disease. Compounds useful as building blocks of said antisense oligonucleotides and methods of preparing building block compounds including NPN linkages are provided.
Abstract: Methods for treating a telomerase-expressing cell characterized by an over-activation of telomerase in a subject in need thereof comprising administering a pharmaceutical composition comprising a first amount of a 6-mercaptopurine analog, and a second amount of a telomerase inhibitor, wherein the first amount and the second amount together comprises an amount effective to reduce stability of telomere length and to induce cell death in the telomerase-expressing cell are provided. The methods can be used to treat patients with lung cancer, colon cancer, or cervical cancer.
Type:
Grant
Filed:
April 8, 2014
Date of Patent:
November 5, 2019
Assignee:
The Board of Regents of the University of Texas System
Abstract: The present disclosure provides pharmaceutical compositions comprising cytidine analogs for oral administration, wherein the compositions release the cytidine analog substantially in the stomach. Also provided are methods of treating diseases and disorders using the oral formulations provided herein.
Type:
Grant
Filed:
January 9, 2019
Date of Patent:
November 5, 2019
Assignee:
Celgene Corporation
Inventors:
John F. Traverse, William W. Leong, Jeffrey B. Etter, Mei Lai, Jay Thomas Backstrom
Abstract: Disclosed is a process for purifying nucleic acids, especially plasmid DNA, from a nucleic acid-containing, biologic sample, consisting of (a) preparation of a fluid sample containing nucleic acid and endotoxin each in dissolved form; (b) precipitation at least of nucleic acid and endotoxin from the fluid sample; (c) washing of the components of the fluid sample precipitated out in step b) in order to at least partially remove the endotoxin with at least one washing solution, which contains at least one amine compound with at least two carbon atoms and with a molar mass of ?500 g/mol and; at least one organic solvent different from the aforementioned amine compound and has a pH-value (20° C.) in the range from pH 3.0 to pH 8.5, and; (d) dissolution of the remaining nucleic acid from the washed, precipitated constituents from step c) using a dissolving buffer and collection of the dissolved nucleic acids in a separate receptacle. The process is suitable for the effective and economical removal of endotoxins.
Abstract: Provided herein are methods and compositions that relate to, inter alia, CBL0137, a carbazole compound 1,1?-[9-[2-[(1-methylethyl)amino]ethyl]-9H-carbazole-3,6-diyl]bis-ethanone, useful for the treatment of various cancers, optionally in combination with various agents.
Abstract: The disclosed and claimed compounds are chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity. The disclosed and claimed compounds include those represented by the following formula (I) or formula (XI) for introducing the chiral auxiliaries.
Abstract: The current disclosure relates to methods for treating pancreatic cancer or chronic pancreatitis in a subject comprising administering an antagonist of a dopamine receptor to the subject wherein the dopamine receptor is, in some specific cases dopamine receptor D2 (DRD2). The antagonist in some specific cases is an RNAi construct, an antibody, or a small molecule and in more specific cases pimozide or L-741,626. The disclosure also relates to diagnostic methods comprising the detection of the expression of DRD2 in pancreatic tissue and kits for doing the same.
Type:
Grant
Filed:
April 17, 2015
Date of Patent:
September 24, 2019
Assignees:
Deutsches Krebsforschungszentrum Stiftung des Öffentlichenrechts, The Royal Institution for the Advancement of Learning/McGill University