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IP Update: Recent Patents, Patent Applications Awarded to Merck, Tekmira, CalImmune, and More

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Title: Triggered RNAi

Patent Number: 8,241,854

Filed: May 22, 2009

Lead Inventor: Peng Yin, California Institute of Technology

The invention, the patent's abstract states, comprises “methods and compositions for triggering RNAi … [which is] highly versatile because the silencing targets are independent of the detection targets. In some embodiments, methods of silencing or modulating the expression of a marker gene are provided.

“The methods generally comprise providing an initiator to a cell comprising a detection target and a silencing target gene, wherein the detection target is different from the silencing target gene, wherein binding of the detection target to the initiator initiates formation of an inactivator double-stranded RNA,” it adds. “The inactivator dsRNA can silence the silencing target gene to modulate the expression of a marker gene.”


Title: siRNA of NF-kB p105 for Inhibiting Cell Proliferation and Migration and a Composition Comprising the Same

Patent Number: 8,242,094

Filed: Aug. 22, 2008

Lead Inventor: Myung-Ok Park, Biopolymed

The invention “relates to [an] siRNA [that] targets mRNA of the NF-Kappa B p105 gene to cause its degradation by RNAi induction,” according to the patent's abstract. Also claimed is a “pharmaceutical composition for the treatment of diseases associated with aberrant cell proliferation and migration, comprising the siRNA and delivery vehicle capable of intracellular delivery of the same.”


Title: siRNA Useful to Suppress Expression of EIF-5A1

Patent Number: 8,242,256

Filed: Dec. 17, 2009

Lead Inventor: John Thompson, Senesco Technologies

The invention, the patent's abstract states, “relates to apoptosis specific eukaryotic initiation factor 5A ... apoptosis factor 5A1 nucleic acids and polypeptides, and methods for inhibiting or suppressing apoptosis in cells using antisense nucleotides or siRNAs to inhibit expression of factor 5A1. The invention also relates to suppressing or inhibiting expression of pro-inflammatory cytokines by inhibiting expression of apoptosis factor 5A.”


Title: RNA Interference-Mediated Inhibition of Gene Expression Using Chemically Modified Short Interfering Nucleic Acid

Patent Number: 8,242,257

Filed: April 6, 2011

Lead Inventor: Leonid Beigelman, Merck

The invention “concerns methods and reagents useful in modulating gene expression in a variety of applications, including use in therapeutic, diagnostic, target-validation, and genomic-discovery applications,” the patent's abstract states. “Specifically, the invention relates to synthetic chemically modified small nucleic acid molecules ... capable of mediating RNA interference against target nucleic acid sequences. The small nucleic acid molecules are useful in the treatment of any disease or condition that responds to modulation of gene expression or activity in a cell, tissue, or organism.”


Title: Dual Vector for Inhibition of Human Immunodeficiency Virus

Application Number: 20120201794

Filed: May 26, 2010

Lead Inventor: Irvin Chen, CalImmune

The invention, the patent application's abstract states, “provides an expression vector for preventing or inhibiting HIV entry, fusion, or replication in mammalian cells. In particular, the invention provides a recombinant retroviral vector that encodes an inhibitor of a HIV co-receptor, such as CCR5 or CXCR4, and a protein that inhibits HIV fusion to target cells and/or HIV replication. Pharmaceutical compositions comprising such constructs and methods of use thereof to prevent or treat HIV infection in a patient are also disclosed.”


Title: Liposomes Comprising a Calcium Phosphate-Containing Precipitate

Application Number: 20120201872

Filed: Aug. 3, 2010

Lead Inventor: Leaf Huang, University of North Carolina at Chapel Hill

The invention, the patent application's abstract states, comprises “methods and compositions for the delivery of bioactive compounds to a cell, tissue, or physiological site. The compositions comprise delivery-system complexes [made of] liposomes encapsulating a biodegradable ionic precipitate [with] a bioactive compound and delivery-system complexes [made of] a biodegradable ionic precipitate ionically bound to a surrounding lipid bilayer, wherein the biodegradable ionic precipitate comprises a bioactive compound. Also provided herein are methods for the treatment of a disease or an unwanted condition in a subject … [by] administering the delivery system complexes comprising bioactive compounds that have therapeutic activity against the disease or unwanted condition.”


Title: Cell-Imaging Method for Viewing microRNA Biogenesis in the Cells

Application Number: 20120202209

Filed: Sept. 21, 2010

Lead Inventor: Jerome Cavaille, French National Center for Scientific Research

The invention comprises “a method for viewing the biogenesis of at least one microRNA, preferably a microRNA group, in a living cell … [by] transforming said cell by an encoding vector for a protein selected among the DGCR8 protein, the Drosha protein and derivatives thereof,” the patent application's abstract states. The protein is coupled with a marker and expressed, and the marker is detected, it adds.


Title: Cationic Lipids and Methods for the Delivery of Therapeutic Agents

Application Number: 20120202871

Filed: June 30, 2010

Lead Inventor: James Heyes, Protiva Biotherapeutics (Tekmira Pharmaceuticals)

The invention, the patent application's abstract states, “provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knockdown of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.”


Title: RNAi Probes Targeting Cancer-Related Proteins

Application Number: 20120202873

Filed: Feb. 24, 2012

Lead Inventor: Martin Gleave, University of British Columbia

The invention describes “RNAi sequences that are useful as therapeutics in the treatment of cancers of various types … and Alzheimer's disease,” according to the patent application's abstract. “These sequences target clusterin, IGFBP-5, IGFBP-2, both IGFBP-2 and -5 simultaneously, Mitf, and B-raf. The invention ... provides for the use of these RNAi sequences ... and a method of treating such conditions through the administration of the RNA molecules with RNAi activity to … a human.”

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