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IP Update: Aug 27, 2009

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Title: Oligonucleotides Comprising a Modified or Non-Natural Nucleobase

Number: 7,579,451

Filed: July 21, 2005

Lead Inventor: Muthiah Manoharan, Alnylam Pharmaceuticals

The invention, the patent’s abstract states, “relates to a double-stranded oligonucleotide comprising at least one non-natural nucleobase. In certain embodiments, the non-natural nucleobase is difluorotolyl, nitroindolyl, nitropyrrolyl, or nitroimidazolyl. In a preferred embodiment, the non-natural nucleobase is difluorotolyl.

“In certain embodiments, only one of the two oligonucleotide strands comprising the double-stranded oligonucleotide contains a non-natural nucleobase,” the abstract adds. “In certain embodiments, both of the oligonucleotide strands comprising the double-stranded oligonucleotide independently contain a non-natural nucleobase … [while in other] embodiments, the oligonucleotide strands comprise at least one modified sugar moiety.”

The abstract adds that “another aspect of the … invention relates to a single-stranded oligonucleotide comprising at least one non-natural nucleobase. In a preferred embodiment, the non-natural nucleobase is difluorotolyl. In certain embodiments, the ribose sugar moiety that occurs naturally in nucleosides is replaced with a hexose sugar, polycyclic heteroalkyl ring, or cyclohexenyl group … [while in other] embodiments, at least one phosphate linkage in the oligonucleotide has been replaced with a phosphorothioate linkage.”


Title: siRNA Targeting Carbonic Anhydrase II

Number: 7,579,457

Filed: Dec. 7, 2006

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.”


Title: siRNA Targeting Synuclein, Alpha

Number: 7,579,458

Filed: July 25, 2007

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 including those directed to SNCA-1.”


Title: Method of Producing Antibodies with Improved Function

Number: 20090208500

Filed: June 5, 2006

Lead Inventor: John Joly, Genentech (Roche)

“The invention provides methods for controlling fucosylation levels and improving ADCC activity in antibodies,” the patent application’s abstract states.

The application specifically claims the use of siRNAs to “inhibit the expression of FUT8 and reduce the fucosylation level of the antibody.”


Title: Compositions of Asymmetric Interfering RNA and Uses Thereof

Number: 20090208564

Filed: Aug. 27, 2008

Lead Inventor: Chiang Jia Li, Boston Biomedical (AiRNA)

The invention “provides asymmetrical duplex RNA molecules that are capable of effecting sequence-specific gene silencing,” according to the patent application’s abstract. “The RNA molecule comprises a first strand and a second strand … [with the] first strand [being] longer than the second strand. The RNA molecule comprises a double-stranded region formed by the first strand and the second strand, and two ends independently selected from the group consisting of 5'-overhang, 3'-overhang, and blunt end.

“The RNA molecules of the … invention can be used as research tools and/or therapeutics,” the abstract adds.


Title: microRNA Fingerprints During Human Megakaryocytopoiesis

Number: 20090209450

Filed: March 19, 2007 PCT Filed: March 19, 2007

Lead Inventor: Carlo Croce, Ohio State University

The invention, the patent application’s abstract states, “provides novel methods and compositions for the diagnosis, prognosis, and treatment of cancer and myeloproliferative disorders. The invention also provides methods of identifying anti-cancer agents.”


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

Number: 20090209478

Filed: Sept. 21, 2007

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, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of the HAMP gene,” 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 HAMP gene expression, and the expression of the HAMP gene using the pharmaceutical composition.”


Title: Compositions and Methods for Decreasing microRNA Expression for the Treatment of Neoplasia

Number: 20090209621

Filed: June 2, 2006 PCT Filed: June 2, 2006

Lead Inventor: Joshua Mendell, Johns Hopkins University

“The invention generally features compositions and methods that are useful for treating or diagnosing a neoplasia,” the patent application’s abstract states. “The invention is based in part on the observation that c-Myc activated expression of a cluster of six miRNAs on human chromosome 13. Accordingly, the invention provides therapeutic compositions and methods for altering the expression of a microRNA of the invention thereby treating a neoplasia, as well as compositions and methods for diagnosing a neoplasia.”


Title: Duplex Oligonucleotide with Enhanced Functionality in Gene Regulation

Number: 20090209626

Filed: Feb. 10, 2009

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

The invention, the patent application’s abstract states, comprises “methods of enhancing functionality of duplex oligonucleotides and compositions made by the methods. The duplex oligonucleotides include siRNAs, miRNA mimics, and piRNA mimics [that] contain modified nucleotides and mismatches between the two strands of the molecule at specific nucleotide positions.”


Title: RNAi-Mediated Inhibition of Connexion 43 for Treatment of IOP-Related Conditions

Number: 20090209627

Filed: Feb. 13, 2009

Lead Inventor: Jon Chatterton, Alcon

“RNA interference is provided for inhibition of connexin 43 in intraocular pressure-related conditions, including ocular hypertension, and glaucoma, such as normal-tension glaucoma and open-angle glaucoma,” according to the patent application’s abstract.


Title: Multiple RNA-Expression Cassettes for Simultaneous Delivery of RNAi Agents Related to Heterozygotic Expression Patterns

Number: 20090209628

Filed: Feb. 13, 2009

Lead Inventor: Elisabeth Evertsz, Benitec

The invention, the patent application’s abstract states, “provides compositions and methods suitable for expressing y-x multiple-RNAi agents against an allele or alleles of interest in cells, tissues, or organs of interest in vitro and in vivo so as to treat diseases.”


Title: Nucleic Acid-Functionalized Nanoparticles for Therapeutic Applications

Number: 20090209629

Filed: June 8, 2006 PCT Filed: June 8, 2006

Lead Inventor: Chad Mirkin, Northwestern University

The patent application, its abstract states, claims “materials and methods for regulating gene expression using nanoparticles functionalized with antisense oligonucleotides.”


Title: shRNA and siRNA Expression in a Living Organism Under Control of a Codon-Optimized Repressor Gene

Number: 20090210955

Filed: June 8, 2006 PCT Filed: June 8, 2006

Lead Inventor: Jost Seibler, Artemis Pharmaceuticals

The invention “relates to a biological entity carrying a regulator construct comprising a specific repressor gene and a responder construct [made up of] at least one segment corresponding to a short hairpin RNA or corresponding to complementary short interfering RNA strands,” according to the patent application’s abstract. “At least one segment [of the responder construct is] under control of a promoter [that] contains an operator sequence corresponding to the repressor.”

“The invention further relates to a method for preparing said biological entity and its use,” the abstract adds.

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