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Twelve RNAi-Related Patent Applications Published by the USPTO

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Title: MicroRNAs in Plants

Number: 20050144669

Filed: July 1, 2004

Inventor: Brenda Reinhart, Whitehead Institute

The patent application, its abstract states, "generally relates to the production and expression of microRNA in plants. In some cases, production and expression of miRNA can be used to at least partially inhibit or alter gene expression in plants. For instance, in some embodiments, a nucleotide sequence, which may encode a sequence substantially complementary to a gene to be inhibited or otherwise altered, may be prepared and inserted into a plant cell," the abstract states.

"Expression of the nucleotide sequence may cause the formation of precursor miRNA, which may, in turn, be cleaved (for example, with Dicer or other nucleases, including, for example, nucleases associated with RNA interference), to produce an miRNA sequence substantially complementary to the gene," the abstract adds. "The miRNA sequence may then interact with the gene (e.g., complementary binding) to inhibit the gene. In some cases, the nucleotide sequence may be an isolated nucleotide sequence. Other embodiments of the invention are directed to the precursor miRNA and/or the final miRNA sequence, as well as methods of making, promoting, and use thereof."


Title: RNA Interference-Mediated Inhibition of Interleukin and Interleukin Receptor Gene Expression Using Short Interfering Nucleic Acid

Number: 20050143333

Filed: June 9, 2004

Lead Inventor: Ivan Richards, Sirna Therapeutics

"This invention relates to compounds, compositions, and methods useful for modulating interleukin and/or interleukin receptor gene expression using short interfering nucleic acid molecules," the patent application's abstract states. "This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of interleukin and/or interleukin receptor gene expression and/or activity by RNA interference using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid, short interfering RNA, double-stranded RNA, microRNA, and short hairpin RNA molecules and methods used to modulate the expression of interleukin and/or interleukin receptor genes such as IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-7, IL-8, IL-9, IL-10, IL-11, IL-12, IL-13, IL-14, IL-15, IL-16, IL-17, IL-18, IL-19, IL-20, IL-21, IL-22, IL-23, IL-24, IL-25, IL-26, and IL-27 genes and IL-IR, IL-2R, IL-3R, IL-4R, IL-5R, IL-6R, IL-7R, IL-8R, IL-9R, IL-10R, IL-11R, IL-12R, IL-13R, IL-14R, IL-15R, IL-16R, IL-17R, IL-18R, IL-19R, IL-20R, IL-21R, IL-22R, IL-23R, IL-24R, IL-25R, IL-26R, and IL-27R genes."


Title: Compositions and Processes Using siRNA, Amphipathic Compounds, and Polycations

Number: 20050143332

Filed: May 14, 2004

Lead Inventor: Sean Monahan, Mirus Bio

According to the patent application's abstract, the invention "is a deliverable composition with low toxicity comprising an amphipathic compound, a polycation, and a siRNA. The composition may be used in the process of delivering a siRNA to an animal cell or more particularly, a mammal cell."


Title: MicroRNAs as Ligands and Target Molecules

Number: 20050142581

Filed: Sept. 3, 2004

Lead Inventor: Richard Griffey, Isis Pharmaceuticals

"The … invention provides methods for the identification of target molecules that bind to ligands, particularly microRNA ligands and mimics thereof and/or microRNA target molecules and mimics thereof, with as little as millimolar affinity using mass spectrometry," the patent application's abstract states. "The methods may be used to determine the mode of binding interaction between two or more of these target molecules to the ligand as well as their relative affinities. Also provided are methods for designing compounds having greater affinity to a ligand by identifying two or more target molecules using mass spectrometry methods of the invention and linking the target molecules together to form a novel compound."


Title: RNA Interference-Mediated Target Discovery and Target Validation Using Short Interfering Nucleic Acid

Number: 20050142578

Filed: Aug. 19, 2004

Lead Inventor: Nassim Usman, Sirna Therapeutics

The invention, the patent application's abstract states, "concerns methods and reagents useful in target discovery. Specifically, the invention relates to small nucleic acid molecules capable of mediating RNA interference, such as short interfering nucleic acid (siNA) short interfering RNA, double-stranded RNA, microRNA, and short hairpin RNA molecules and methods of target discovery using siRNA."


Title: Gene Silencing

Number: 20050138689

Filed: Oct. 12, 2004

Lead Inventor: Milo Aukerman, Pioneer Hi-Bred International

"The invention provides methods and compositions useful in target sequence suppression and target sequence validation," the patent application's abstract states. "The invention provides polynucleotide constructs useful for gene silencing, as well as cells, plants and seeds comprising the polynucleotides. The invention also provides a method for using microRNA to silence a target sequence."


Title: RNA Interference-Mediated Treatment of Parkinson's Disease Using Short Interfering Nucleic Acid

Number: 20050137155

Filed: June 3, 2004

Lead Inventor: James McSwiggen, Sirna Therapeutics

According to the patent application's abstract, the invention "concerns methods and reagents useful in modulating Parkinson genes, for example, PARK1 (SNCA), PARK2, PARK7, and/or PARK5 gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to small nucleic acid molecules, such as short interfering nucleic acid, short interfering RNA, double-stranded RNA, microRNA, and short hairpin RNA molecules capable of mediating RNA interference against SNCA gene expression and/or activity. The small nucleic acid molecules are useful in the diagnosis and treatment of Parkinson's disease and any other disease or condition that responds to modulation of PARK1 (SNCA), PARK2, PARK7, and/or PARK5 expression or activity."


Title: RNA Interference-Mediated Inhibition of Alpha-1 Antitrypsin Gene Expression Using Short Interfering Nucleic Acid

Number: 20050137153

Filed: May 6, 2004

Lead Inventor: James McSwiggen, Sirna Therapeutics

According to the patent application's abstract, the invention "concerns compounds, compositions, and methods for the study, diagnosis, and treatment of diseases and conditions associated with alpha-1 antitrypsin allelic variants that respond to the modulation of gene expression and/or activity. The … invention also concerns compounds, compositions, and methods relating to diseases and conditions associated with alpha-1 antitrypsin allelic variants that respond to the modulation of expression and/or activity of genes involved in alpha-1 antitrypsin gene expression pathways or other cellular processes that mediate the maintenance or development of alpha-1 antitrypsin diseases and conditions such as liver disease, lung disease, and any other diseases or conditions that are related to or will respond to the levels of an alpha-1 antitrypsin variant protein in a cell or tissue, alone or in combination with other therapies," the abstract states.

"Specifically, the invention relates to small nucleic acid molecules, such as short interfering nucleic acid, short interfering RNA, double-stranded RNA, microRNA, and short hairpin RNA molecules capable of mediating RNA interference against the expression disease related genes or alleles having alpha-1 antitrypsin sequences," the abstract adds.


Title: SiRNA-Mediated Gene Silencing Technology to Inhibit Tyrosinase and Reduce Pigmentation

Number: 20050137151

Filed: Dec. 17, 2003

Lead Inventor: Ralph Binetti, Avon Products

"The … invention describes compositions and methods for treating, preventing and improving hyperpigmentation, or other unwanted pigmentation of the skin, or other unwanted skin condition, such as age spots, aged skin, skin discoloration, etc., wherein the compositions include siRNA-gene silencing oligomers specific for tyrosinase," the patent application's abstract states. "The compositions are used to treat a broad variety of pigmentation conditions, and are preferably applied to the skin, or are delivered by directed means to a site in need thereof."


Title: Nanoparticles for Delivery of Nucleic Acids and Stable Double-Stranded RNA

Number: 20050136437

Filed: Aug. 24, 2004

Lead Inventor: Steven Quay, Nastech Pharmaceuticals

According to the patent application's abstract, the invention comprises "nanoparticles of double-stranded nucleic acid complexed about a complexing agent such as the melamine derivatives of formulae I and II, preferably forming a trimeric nucleic acid complex. In alternative embodiments, polyarginine or a polymer of Gln and Asn further complexed with the double-stranded nucleic acid complex. In a preferred embodiment, the ds-nucleic acid is a double stranded RNA having 15 to 30 base pairs suitable for RNA interference. In another aspect of the invention, a dsRNA is produced in which all of the uridines are changed to 5-methyluridine. Preferably, the resultant dsRNAs have 15 to about 30 base pairs and are suitable for RNA interference," the abstract notes.


Title: RNA Interference-Mediated Inhibition of G72 and D-Amino Oxidase Gene Expression Using Short Interfering Nucleic Acid

Number: 20050136436

Filed: Aug. 19, 2004

Lead Inventor: James McSwiggen, Sirna Therapeutics

"This invention relates to compounds, compositions, and methods useful for modulating G72 and/or D-amino acid oxidase gene expression using short interfering nucleic acid molecules," the patent application's abstract states. "This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of G72 and/or D-amino acid oxidase gene expression and/or activity by RNA interference using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid, short interfering RNA, double-stranded RNA, microRNA, and short hairpin RNA molecules and methods used to modulate the expression of G72 and/or DAAO genes. The small nucleic acid molecules are useful in the treatment of schizophrenia and any other condition that responds to modulation of G72 and/or DAAO expression or activity."


Title: Inhibitor Nucleic Acids

Number: 20050136430

Filed: July 15, 2004

Inventor: Mark Davis, California Institute of Technology (Calando Pharmaceuticals)

The invention, the patent application's abstract states, "provides methods and compositions for attenuating expression of a target gene in vivo. In general, the method includes administering RNAi constructs (such as small interfering RNAs that are targeted to particular mRNA sequences, or nucleic acid material that can produce siRNAs in a cell), in an amount sufficient to attenuate expression of a target gene by an RNA interference mechanism. In particular, the RNAi constructs include one or more modifications to improve serum stability and cellular uptake and to avoid non-specific effect."

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