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IP Update: Recent Patents, Patent Applications Awarded to Opko, Devgen, Alnylam, and More

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Title: Compositions and Methods for Selective Inhibition of VEGF

Patent Number: 8,470,792

Filed: Dec. 4, 2009

Lead Inventor: Phillip Frost, Opko Health (RXi Pharmaceuticals)

The invention, the patent’s abstract states, comprises “siRNA compositions and methods useful for inhibiting expression of vascular endothelial growth factor isoforms. Such compositions and methods further involve siRNA capable of selectively targeting angiogenic VEGF isoforms while selectively sparing anti-angiogenic isoforms. Diseases which involve angiogenesis stimulated by overexpression of VEGF, such as diabetic retinopathy, age-related macular degeneration, and many types of cancer, can be treated by administering small interfering RNAs as disclosed.”


Title: Downregulation of Mortalin by siRNA

Patent Number: 8,470,793

Filed: June 29, 2010

Lead Inventor: Zvi Fishelson, Tel-Aviv University

The patent, its abstract states, claims the “use of a siRNA molecule … for treating a disease associated with a pathological cell population in a subject in need thereof. … Pharmaceutical compositions and articles of manufacture comprising the siRNAs are also disclosed.”


Title: Increasing Erythropoietin Using Nucleic Acids Hybridizable to microRNA and Precursors Thereof

Patent Number: 8,470,794

Filed: Aug. 10, 2010

Lead Inventor: Sumedha Jayasena, Amgen

The patent, its abstract states, claims “methods and compositions relating to nucleic acids targeting certain miRNA molecules. … The nucleic acids are useful, for example, in methods of increasing the expression and/or secretion of EPO and treating various disease states including anemia, hemophilia, and/or sickle cell disease.”


Title: Treatment of Cancer by Inhibition of IGFBPs and Clusterin

Patent Number: 8,470,796

Filed: April 15, 2011

Lead Inventor: Martin Gleave, University of British Columbia

“Agents that reduce the amount of IGFBP-2 and/or IGFBP-5 and that are known to be useful in the treatment of cancer result in increased expression of the protein clusterin,” the patent’s abstract states. “Since clusterin can provide protection against apoptosis, this secondary effect detracts from the efficacy of the therapeutic agent. In overcoming this, the … invention provides a combination of therapeutic agents that is useful in the treatment of cancer … [including] an agent that reduces the amount of IGFBP-2 and/or IGFBP-5 and that stimulates expression of clusterin as a secondary effect, and an oligonucleotide that is effective to reduce the amount of clusterin in cancer cells. In some embodiments of the invention, the agent that reduces IGFBP-2 and/or IGFBP-5 is a bispecific antisense species. The oligonucleotide may be an antisense oligonucleotide or an RNAi oligonucleotide.”


Title: Inducible Small RNA Expression Constructs for Targeted Gene Silencing

Patent Number: 8,470,797

Filed: April 3, 2012

Lead Inventor: Thomas Tuschl, Max Planck Institute

“The invention relates to vectors for the inducible expression of RNA molecules in eukaryotic, particularly mammalian, cells and transgenic animals,” the patent’s abstract states.


Title: Compositions and Methods for Inhibiting Expression of the HAMP Gene

Patent Number: 8,470,799

Filed: Aug. 21, 2012

Lead Inventor: Tomoko Nakayama, Alnylam Pharmaceuticals

“The invention relates to a double-stranded ribonucleic acid for inhibiting the expression of the HAMP gene, comprising an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length … and which is substantially complementary to at least a part of the HAMP gene,” according to the patent’s abstract. “The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier, [and] methods for treating diseases caused by HAMP gene expression and the expression of the HAMP gene using the pharmaceutical composition.”


Title: Single-stranded and Double-stranded Oligonucleotides Comprising 2-Arylpropyl Moiety

Patent Number: 8,470,988

Filed: Oct. 23, 2009

Lead Inventor: Muthiah Manoharan, Alnylam Pharmaceuticals

The invention, the patent’s abstract states, comprises “single-stranded and double-stranded oligonucleotides [with] at least one aralkyl ligand that improvise the pharmacokinetic properties of the oligonucleotide. The aralkyl ligands of the … invention include naproxen, ibuprofen, and derivatives thereof. The … invention also provides method for modulating gene expression using the modified oligonucleotide compounds and compositions comprising those modified oligonucleotides.”


Title: RNAi-mediated Inhibition of HIF1A for Treatment of Ocular Angiogenesis

Patent Number: 8,471,000

Filed: May 17, 2012

Lead Inventor: Jon Chatterton, Alcon

“RNA interference is provided for inhibition of HIF1A mRNA expression for treating patients with ocular angiogenesis, particularly for treating retinal edema, diabetic retinopathy, sequela associated with retinal ischemia, posterior segment neovascularization, and neovascular glaucoma, and for treating patients at risk of developing such conditions,” the patent’s abstract states.


Title: Lipid-formulated Single-stranded RNA

Application Number: 20130156845

Filed: April 29, 2011

Lead Inventor: Muthiah Manoharan, Alnylam Pharmaceuticals

The invention, the patent application’s abstract states, provides “compositions comprising a nucleic acid lipid particle and an oligomeric compound and uses thereof. In certain embodiments, such compositions are useful as antisense compounds. Certain such antisense compounds are useful as RNase H antisense compounds or as RNAi compounds.”


Title: miRNAs Involved in the Blood-brain Barrier Function

Application Number: 20130158096

Filed: May 27, 2011

Lead Inventor: Arie Reijerkerk, To-BBB

The invention relates to the “use of particular nucleic acids for modulating blood-brain barrier function, and for [the] use of such nucleic acids in treatment of conditions involving blood-brain barrier function, including multiple sclerosis, HIV infection, Alzheimer's disease, Parkinson's disease, epilepsy, and so on,” the patent application’s abstract states. “Also provided is an assay for identifying drugs useful in modulating blood-brain barrier function.”


Title: Compositions and Methods Directed to Treating Liver Fibrosis

Application Number: 20130158097

Filed: June 2, 2011

Lead Inventor: Greg Hinkle, Alnylam Pharmaceuticals

“The invention relates to double-stranded ribonucleic acid compositions targeting the COL1A1, TGF-beta, and SMAD2/3 genes, and methods of using such dsRNA compositions to inhibit expression of COL1A1, TGF-beta, and SMAD2/3,” the patent application’s abstract states.


Title: Compositions and Methods for Inhibiting Expression of a Gene from the JC Virus

Application Number: 20130158102

Filed: Feb. 27, 2013

Lead Inventor: Pamela Tan, Alnylam Pharmaceuticals

“The invention relates to a double-stranded ribonucleic acid for inhibiting the expression of a gene from the JC virus,” the patent application’s abstract states. “The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by JC virus expression and the expression of a gene from the JC virus using the pharmaceutical composition; and methods for inhibiting the expression of a gene from the JC virus in a cell.”


Title: Medical Devices for Delivery of siRNA

Application Number: 20130158505

Filed: Feb. 22, 2013

Inventor: Russell Ross, Kimberly-Clark

The patent application, its abstract states, claims “medical devices that incorporate siRNA. In addition to one or more siRNA constructs, devices include nanostructures fabricated on a surface to form a nanotopography. A random or non-random pattern of structures may be fabricated such as a complex pattern including structures of differing sizes and/or shapes. Microneedles may be incorporated on devices. The pattern including nanostructures may be formed on the surface of the microneedles.”


Title: Method for Downregulating Gene Expression in Fungi

Application Number: 20130160156

Filed: June 8, 2011

Lead Inventor: Simone Dorfmueller, Devgen (Syngenta)

The invention claims “methods for controlling and/or preventing fungus infestation on a cell, organism, substrate, or material via dsRNA-mediated gene silencing,” the patent application’s abstract states. “The methods of the invention are particularly used to alleviate pathogenic fungal infestation on plants, plant materials, or seeds. Suitable fungal target genes and fragments thereof, expression cassettes, dsRNA molecules, host cells expressing the dsRNA, compositions and transgenic plants, and plant cells are provided.”

The Scan

Plan Rebuffed

The Associated Press reports China has rejected the World Health Organization's proposal to include the lab-leak theory in the next phase of its investigation into the origins of SARS-CoV-2.

Opossum Change

Researchers from Riken have used CRISPR to edit marsupial genomes, as Technology Review reports.

In the Ice

Cosmos magazine reports that researchers have uncovered more than two dozen ancient viruses in a Tibetan glacier.

Nature Papers Present Method to Uncover Differential RNA Modifications, Neutrophils in Innate Immune Response

In Nature this week: computational approach to identifying differential RNA modifications, and more.