Abstract: The present invention relates to a method of preparing triphosphate-modified oligonucleotides using a capture tag. The method allows the synthesis and purification of triphosphate-modified oligonucleotides in high yield and purity suitable for pharmaceutical applications.
Abstract: The invention relates to iRNA agents, which preferably include a monomer in which the ribose moiety has been replaced by a moiety other than ribose. The inclusion of such a monomer can allow for modulation of a property of the iRNA agent into which it is incorporated, e.g., by using the non-ribose moiety as a point to which a ligand or other entity, e.g., a lipophilic moiety. e.g., cholesterol, is directly, or indirectly, tethered. The invention also relates to methods of making and using such modified iRNA agents.
Abstract: Process for recovery and separation of sugars and oil from plants where the stems and leaves of such plants have substantial levels of both sugars and oils.
Type:
Grant
Filed:
October 14, 2014
Date of Patent:
July 19, 2016
Assignee:
The Board of Trustees of the University of Illinois
Inventors:
Stephen P Long, Vijay Singh, Haibo Huang
Abstract: The present application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.
Type:
Grant
Filed:
December 22, 2014
Date of Patent:
July 19, 2016
Assignee:
Alios BioPharma, Inc.
Inventors:
Anuj K. Kuldipkumar, Ales Medek, Lori Ann Ferris, Praveen Mudunuri, Young Chun Jung, David Richard Willcox, Michael Waldo, William Aloysius Nugent
Abstract: The present invention relates to a novel amphiphilic block copolymer and the preparation method thereof, as well as a micellar drug-loaded system formed by said copolymer and an anti-tumor drug. Said amphiphilic block copolymer comprises a hydrophilic segment and a hydrophobic segment, and the end group of said hydrophobic segment is end-capped with a hydrophobic group. Methoxypolyethylene glycol (or polyethylene glycol)-polyester block copolymer which has recognized safety is used as a fundamental material of the amphiphilic block copolymer of the present invention, and the terminal hydroxyl group of the polyester segment is modified with a hydrophobic group, whereby the compatibility between the drug molecule and the hydrophobic segments of the block copolymer is improved, and the interaction therebetween is enhanced. Moreover, a larger space for accommodating the drug molecules is provided.
Abstract: Disclosed herein are 2?-spiro-nucleosides and derivatives thereof useful for treating a subject infected by hepatitis C virus or dengue virus.
Abstract: The present invention includes a composition and method of treatment having arabinogalactan and polyphenols from larch trees for the use in prophylactic treatment of upper respiratory tract infections. The invention also includes treatment using such composition.
Abstract: Alkynyl-derivatized cap analogs, alkynyl-modified capped RNA, 1,4-disubstituted triazole-derivatized capped RNA, methods of preparation, methods of isolation, and uses thereof are provided. The “click” modification facilitates detection and isolation of capped RNAs and the 1,4-disubstituted triazole derivatives formed by the “click” reaction are useful for producing RNA transcripts and encoded protein.
Abstract: A process for making a hydrogel forming material from an unbleached cellulose pulp comprised of isolating pulp fines from the cellulose pulp by screening and/or dissolved air filtration, reacting the isolated pulp fines with alkaline hydroxide to form an alkali cellulose composition, preparing a heterogeneous mixture of the alkali cellulose composition and an etherifying agent, and optionally organic cross-linking agent, and reacting the components of the mixture to produce a hydrogel forming material. A polyvalent metal cross-linking agent can optionally be reacted with the hydrogel forming material to enhance its gel strength.
Abstract: The invention provides derivatives of decitabine with superior chemical stability and shelf life, with similar physiological activity. The derivatives are provided in a non-aqueous formulation, which further stabilizes the derivatives. Methods of treating one or more myelodysplastic syndromes, leukemia, or solid tumors using the formulations are described.
Abstract: A method and composition for the treatment, prevention and/or prophylaxis of a host, and in particular, a human, infected with Epstein-Barr virus (EBV), is provided that includes administering an effective amount of a 5-substituted uracil nucleoside or its pharmaceutically acceptable salt or prodrug, optionally in a pharmaceutically acceptable diluent or excipient.
Type:
Grant
Filed:
December 4, 2013
Date of Patent:
July 5, 2016
Assignees:
EMORY UNIVERSITY, BETH ISRAEL DEACONESS MEDICAL CENTER, INC.
Inventors:
Raymond F. Schinazi, Junxing Shi, Joyce D. Fingeroth, Erik Gustafson
Abstract: Provided is a method for preparing a cellulose ether having a low degree of polymerization and undergoing less yellowing and a cellulose ether prepared thereby. Specifically, provided is a method for preparing a cellulose ether having a low degree of polymerization, the method including a step of bringing pulp and an alkali metal hydroxide solution into contact with each other or mixing them to obtain a corresponding alkali cellulose, a first depolymerization step of reacting the alkali cellulose with oxygen to adjust a viscosity reduction percentage of the alkali cellulose to from 10 to 95%, a step of reacting the depolymerized alkali cellulose with an etherifying agent, a step of washing and drying the reaction product to obtain a cellulose ether, and a second depolymerization step of bringing the cellulose ether into contact with hydrochloric acid to adjust a viscosity reduction percentage of the cellulose ether from 40 to 99.9%.
Abstract: A process for producing a cellulose derivative, including reacting a reactant and a cellulose or a derivative thereof in a solid-liquid heterogeneous system to form a cellulose derivative containing a long-chain organic group having 5 or more carbon atoms introduced therein, in a swollen state, and performing solid-liquid separation to obtain the cellulose derivative containing a long-chain organic group introduced therein.
Abstract: Includes the following steps: (1) Mix organs and tissues with formamide and monovalent cation salt solution, homogenize them to obtain the dehydrated biological sample; (2) Mix the dehydrated biological sample with monovalent cation salt solution for incubation; (3) Add the monovalent cation salt solution with precipitation effect to the mixture, mix them and centrifuge, then pour the supernatant into another centrifuge tube; (4) Add isopropanol, mix it and centrifuge, and then discard the upper phase liquid, the lower phase liquid and the visible residual impurities between the upper and lower phases to get white RNA precipitate. This method proposed in the invention enables efficient isolation of protein from RNA in the biological samples.
Abstract: The subject of the invention is a new method of the synthesis of polyphosphate analogs, such as nucleosides, oligonucleotides, carbohydrates, peptides and proteins, which are of biological importance and are used in organic chemistry, molecular biology and biotechnology. Polyphosphate analogs, including in particular nucleoside 5?-triphosphates, display high biological activity and are responsible for the provision and storage of energy in live organisms. The method relates to the synthesis of organic polyphosphates of general formula (1), where n has a value of 0 to 2, while X stands for an organic radical, in particular nucleoside, oligonucleotide, peptide-carbohydrate or a protein radical.
Type:
Grant
Filed:
July 29, 2013
Date of Patent:
June 28, 2016
Assignee:
INSTYTUT CHEMII BIOORGANICZNEJ POLSKIEJ AKADEMII NAUK
Inventors:
Marcin Krzysztof Chmielewski, Joanna Romanowska
Abstract: A degree of polymerization of cellulose ether is accurately controlled, and quality and a manufacturing process of the cellulose ether are stabilized. There is provided a method for producing depolymerized alkali cellulose having a degree of polymerization controlled, comprising at least a step of depolymerizing, in the presence of an oxygen-containing gas flow, alkali cellulose obtained by bringing a pulp into contact with an alkali solution, while measuring feeding and discharging amounts of oxygen in the oxygen-containing gas flow. There is also provided a method for producing cellulose ether, comprising at least a step of adding an etherifying agent to the depolymerized alkali cellulose having a degree of polymerization controlled.
Abstract: The present invention provides a protected nucleotide for elongation, which can be purified efficiently and in a high yield by a liquid-liquid extraction operation, and can achieve an oligonucleotide production method by a phosphoramidite method. It has been found that the above-mentioned problem can be solved by a particular oligonucleotide comprising a protected base and/or particular oligonucleotide protected by a branched chain-containing aromatic group at 3?-position.
Abstract: The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z?)(Z?)O-nucleoside, —P(Z?)(Z?)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z?)(Z?)O-Linker-OP(Z??)(Z??)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z?)(Z?)-formula (I), —P(Z?)(Z?)- or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g.
Type:
Grant
Filed:
July 11, 2014
Date of Patent:
June 21, 2016
Assignee:
ALNYLAM PHARMACEUTICALS, INC.
Inventors:
Muthiah Manoharan, Kallanthottathil G. Rajeev, Jayaprakash Nair, Martin Maier
Abstract: The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z?)(Z?)O-nucleoside, —P(Z?)(Z?)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z?)(Z?)O-Linker-OP(Z??)(Z??)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z?)(Z?)-formula (I), —P(Z?)(Z?)- or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g.
Type:
Grant
Filed:
July 11, 2014
Date of Patent:
June 21, 2016
Assignee:
ALNYLAM PHARMACEUTICALS, INC.
Inventors:
Muthiah Manoharan, Kallanthottathil G. Rajeev, Jayaprakash Nair, Martin Maier
Abstract: The present invention is directed towards the synthesis of high purity deuterated sugars, deuterated phosphoramidites, deuterated nucleobases, deuterated nucleosides, deuterated oligonucleotides, and deuterated RNA's of defined sequences which can exhibit biochemically useful and biologically valuable properties, thus having potential for therapeutic uses.