Patent application number | Description | Published |
20080213891 | RNAi Agents Comprising Universal Nucleobases - One aspect of the present invention relates to an oligonucleotide agent comprising at least one universal nucleobase. In certain embodiments, the universal nucleobase is difluorotolyl, nitroindolyl, nitropyrrolyl, or nitroimidazolyl. In a preferred embodiment, the universal nucleobase is difluorotolyl. In certain embodiments, the oligonucleotide is double-stranded. In certain embodiments, the oligonucleotide is single-stranded. Another aspect of the present invention relates to a method of altering the expression level of a target in the presence of target sequence polymorphism. In a preferred embodiment, the oligonucleotide agent alters the expression of different alleles of a gene. In another preferred embodiment, the oligonucleotide agent alters the expression level of two or more genes. In another embodiment, the oligonucleotide agent alters the expression level of a viral gene from different strains of the virus. In another embodiment, the oligonucleotide agent alters the expression level of genes from different species. | 09-04-2008 |
20090005549 | Processes and Reagents for Desilylation of Oligonucleotides - The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups. In a preferred embodiment, the acrylonitrile scavenger is a polymer-bound thiol. Another aspect of the present invention relates to agents used to oxidize a phosphite to a phosphate. In a preferred embodiment, the oxidizing agent is sodium chlorite, chloroamine, or pyridine-N-oxide. Another aspect of the present invention relates to methods of purifying an oligonucleotide by annealing a first single-stranded oligonucleotide and second single-stranded oligonucleotide to form a double-stranded oligonucleotide; and subjecting the double-stranded oligonucleotide to chromatographic purification. In a preferred embodiment, the chromatographic purification is high-performance liquid chromatography. | 01-01-2009 |
20090023673 | LIPID CONTAINING FORMULATIONS - Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described. | 01-22-2009 |
20090187027 | PROCESSES AND REAGENTS FOR SULFURIZATION OF OLIGONUCLEOTIDES - The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups. In a preferred embodiment, the acrylonitrile scavenger is a polymer-bound thiol. Another aspect of the present invention relates to agents used to oxidize a phosphite to a phosphate. In a preferred embodiment, the oxidizing agent is sodium chlorite, chloramine, or pyridine-N-oxide. Another aspect of the present invention relates to methods of purifying an oligonucleotide by annealing a first single-stranded oligonucleotide and second single-stranded oligonucleotide to form a double-stranded oligonucleotide; and subjecting the double-stranded oligonucleotide to chromatographic purification. In a preferred embodiment, the chromatographic purification is high-performance liquid chromatography. | 07-23-2009 |
20090239814 | Carbohydrate Conjugates as Delivery Agents for Oligonucleotides - The present invention provides iRNA agents comprising at least one subunit of the formula (I): | 09-24-2009 |
20090247608 | Targeting Lipids - The present invention provides targeting lipids of structure | 10-01-2009 |
20090247614 | Folate Conjugates - The present invention provides iRNA agent including at least one monomer having the structure shown in formula (I′) | 10-01-2009 |
20100222413 | Chemically Modified Oligonucleotides for Use in Modulating Micro RNA and Uses Thereof - This invention relates generally to chemically modified oligonuceotides useful for modulating expression of microRNAs and pre-microRNAs. More particularly, the invention relates to single stranded chemically modified oligonuceotides for inhibiting microRNA and pre-microRNA expression and to methods of making and using the modified oligonucleotides. Also included in the invention are compositions and methods for silencing microRNAs in the central nervous system. | 09-02-2010 |
20110224282 | iRNA Agents Targeting VEGF - The features of the present invention relate to compounds, compositions and methods useful for modulating the expression of vascular endothelial growth factor (VEGF), such as by the mechanism of RNA interference (RNAi). The compounds and compositions include iRNA agents that can be unmodified or chemically-modified. | 09-15-2011 |
20110250138 | SINGLE-STRANDED AND DOUBLE-STRANDED OLIGONUCLEOTIDES COMPRISING A METAL-CHELATING LIGAND - The invention provides modified oligonucleotides of formula (I), comprising at least one metal chelator which provides a powerful tool for study of the pharmacokinetics of siRNA and its correlation with in vivo activity. The chelated metals provide luminescent properties enable detection of the oligonucleotides through the use of time-resolved fluorescent quenching based on energy transfer from the metal ion to a nonfluorescent quencher which can be used as non-isotopic labels of oligonucleotides for diagnostics and evaluation of cellular uptake. | 10-13-2011 |
20110313144 | iRNA Agents Targeting CCR5 Expressing Cells And Uses Thereof - The invention relates to iRNA agents that preferably include a modification that targets CC chemokine receptor 5 (CCR5). The invention also relates to methods of making and using such modified iRNA agents. | 12-22-2011 |
20120046478 | LIPID CONTAINING FORMULATIONS - Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described. | 02-23-2012 |
20130018085 | iRNA Agents Targeting VEGF - The features of the present invention relate to compounds, compositions and methods useful for modulating the expression of vascular endothelial growth factor (VEGF), such as by the mechanism of RNA interference (RNAi). The compounds and compositions include iRNA agents that can be unmodified or chemically-modified. | 01-17-2013 |
20130109850 | MODIFIED 5' DIPHOSPHATE NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM | 05-02-2013 |
20130323836 | 5'-END DERIVATIVES - The present invention provides compounds of formula (1). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene. | 12-05-2013 |
20140073684 | CHEMICALLY MODIFIED OLIGONUCLEOTIDES FOR USE IN MODULATING MICRO RNA AND USES THEREOF - This invention relates generally to chemically modified oligonucleotides useful for modulating expression of microRNAs and pre-microRNAs. More particularly, the invention relates to single stranded chemically modified oligonucleotides for inhibiting microRNA and pre-microRNA expression and to methods of making and using the modified oligonucleotides. Also included in the invention are compositions and methods for silencing microRNAs in the central nervous system. | 03-13-2014 |