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IP Update: Recent RNAi- and microRNA-Related Patents and Patent Applications: Sep 22, 2011

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Title: siRNA Targeting Histamine Receptor H1

Patent Number: 8,022,198

Filed: Aug. 10, 2009

Lead Inventor: Anastasia Khvorova, Dharmacon (Thermo Fisher Scientific)

“Efficient sequence-specific gene silencing is possible through the use of siRNA technology,” the patent's abstract states. “By selecting particular siRNAs by rational design, one can maximize the generation of an effective gene-silencing reagent, as well as methods for silencing genes. Methods, compositions, and kits generated through rational design of siRNAs are disclosed.”


Title: siRNA Targeting Myeloid Differentiation Primary Response Gene

Patent Number: 8,022,199

Filed: Dec. 8 2009

Lead Inventor: Anastasia Khvorova, Dharmacon (Thermo Fisher Scientific)

“Efficient sequence-specific gene silencing is possible through the use of siRNA technology,” according to the patent's abstract. “By selecting particular siRNAs by rational design, one can maximize the generation of an effective gene-silencing reagent, as well as methods for silencing genes. Methods, compositions, and kits generated through rational design of siRNAs are disclosed including those directed to nucleotide sequences for MYD88.”


Title: Releasable Fusogenic Lipids for Nucleic Acids Delivery Systems

Application Number: 20110223257

Filed: Nov. 17, 2009

Lead Inventor: Hong Zhao, Enzon Pharmaceuticals

The invention, the patent application's abstract states, “relates to releasable fusogenic lipids and nanoparticle compositions … for the delivery of oligonucleotides and methods of modulating gene expression. … In particular, this invention relates to releasable fusogenic lipids containing an imine linker and a zwitterionic moiety.”


Title: microRNAs and Uses Thereof

Application Number: 20110223656

Filed: Sept. 23, 2009

Lead Inventor: Isaac Bentwich, Rosetta Genomics

The invention, the patent application's abstract states, comprises “novel polynucleotides associated with prostate and lung cancer. The polynucleotides are miRNAs and miRNA precursors. Related methods and compositions that can be used for diagnosis, prognosis, and treatment of those medical conditions are disclosed. Also described herein are methods that can be used to identify modulators of prostate and lung cancer.”


Title: Enhancement of siRNA Silencing Activity Using Universal Bases or Mismatches in the Sense Strand

Application Number: 20110223665

Filed: July 24, 2009

Lead Inventor: Martin Maier, Alnylam Pharmaceuticals

The invention relates to a “double-stranded nucleic acid useful as an siRNA, that has a sense strand and an antisense strand relative to a target nucleic acid, where the sense strand contains one or more modified nucleobases, or one or more mismatch base pairings with the antisense strand,” according to the patent application's abstract.

“Another aspect of the ... invention relates to a single-stranded oligonucleotide [made up of] at least one nucleoside comprising a non-natural nucleobase. Another aspect of the invention relates to a method of gene silencing [by] administering to a mammal in need thereof a therapeutically effective amount of a double-stranded oligonucleotide containing a sense strand and an antisense strand, where the sense strand contains one or more modified nucleobases, or one or more mismatch base pairings with the antisense strand,” the abstract adds.


Title: Oligomeric Compounds and Compositions for Use in Modulation of Small Non-Coding RNAs

Application Number: 20110224277

Filed: Dec. 31, 2008

Lead Inventor: Christine Esau, Regulus Therapeutics

The invention, the patent application's abstract states, comprises “compounds, compositions, and methods … for modulating the expression and function of small non-coding RNAs. The compositions comprise oligomeric compounds targeted to small non-coding RNAs. Methods of using these compounds for modulation of small non-coding RNAs, as well as downstream targets of these RNAs, and for diagnosis and treatment of disease associated with small non-coding RNAs, are also provided.”


Title: iRNA Agents Targeting VEGF

Application Number: 20110224282

Filed: March 8, 2011

Lead Inventor: Antonin De Fougerolles, Alnylam Pharmaceuticals

“The features of the ... invention relate to compounds, compositions, and methods useful for modulating the expression of vascular endothelial growth factor, such as by the mechanism of RNA interference,” the patent application's abstract states. “The compounds and compositions include iRNA agents that can be unmodified or chemically modified.”


Title: Putative Tumor Suppressor microRNA-101 Modulates the Cancer Epigenome by Repressing the Polycomb Group Protein EZH2

Application Number: 20110224284

Filed: Sept. 22, 2009

Lead Inventor: Jeffrey Friedman, University of Southern California

The invention relates, in general, to “microRNA profiling in disease,” the patent application's abstract states. “More specifically, the invention provides for methods and compositions of microRNA to inhibit the growth and formation of tumors.”


Title: Modified siRNA Molecules and Uses Thereof

Application Number: 20110224418

Filed: Feb. 14, 2011

Lead Inventor: Ian MacLachlan, Protiva Biotherapeutics (Tekmira Pharmaceuticals)

The invention provides “chemically modified siRNA molecules and methods of using such siRNA molecules to silence target gene expression,” the patent application's abstract states. “Advantageously, the modified siRNA of the ... invention is less immunostimulatory than its corresponding unmodified siRNA sequence and retains full RNAi activity against the target sequence.”

The invention, the abstract adds, also provides “nucleic acid-lipid particles comprising a modified siRNA, a cationic lipid, and a non-cationic lipid, which can further comprise a conjugated lipid that inhibits aggregation of particles. Methods for identifying and/or modifying an siRNA having immunostimulatory properties are also provided.”

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