Icn Pharmaceuticals, Inc.

Vitagenix, Inc.

Wilfried E Seifert

Kandasamy Ramasamy

Guangyi Wang

Zbigniew Pietrzkowski

Dusan Miljkovic

Esmir Gunic

The invention features antisense oligonucleotide molecules that specifically bind polynucleotides encoding COX-2. The present invention provides antisense oligonucleotides capable of inhibiting COX-2 expression, and methods of use thereof to reduce activity of COX-2 in tissues in order to treat diseases such as, for example, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis, chronic liver disease, ulcerative colitis, cell proliferative disorders, and inflammation associated with Alzheimer's Disease and stroke.

Compositions and methods for inhibiting cox-2 expression and treating cox-2 associated disorders by using cox-2 antisense oligonucleotides

The present invention provides various novel oligonucleotide analogs having one or more properties that make the subject compounds superior to conventional oligonucleotides for use in procedures employing oligonucleotides. The compounds of the invention are oligonucleotide analogs in which the furanose ring of a naturally occurring nucleic acid is replaced with an amino acid or a modified amino alcohol residue. Some embodiments of the novel compounds of the invention are particularly useful for the antisense control of gene expression. The compounds of the invention may also be used as nucleic acid hybridization probes or as primers. Another aspect of the invention is to provide monomeric precursors of the oligonucleotide analogs of the invention. These monomeric precursors may be used to synthesize the subject polynucleotide analogs. Another aspect of the invention is to provide formulations of the subject polynucleotide analogs that are designed for the treatment or prevention of disease conditions. Yet another aspect of the invention is to provide methods for treating or preventing diseases, particularly viral infections and cell growth disorders. The subject disease treatment methods comprise the step of administering an effective amount of the subject polynucleotide analogs for use as antisense inhibitors.

Oligonucleotide analogs with an amino acid or a modified amino alcohol

Methods and compositions are provided which increase the cellular uptake of bioactive materials by covalently bonding such compounds to carbohydrate moieties through chemical linkers using other than glycosidic bonds. Numerous carbohydrates, linkers and bioactive materials can be joined in this way to form novel compositions, which are collectively referred to herein as glinkosides. Preferred glinkosides are preferentially taken up by glucose receptor and/or other cellular receptors, and once inside the cells, the glinkosides are cleaved into a sugar, a linker or linker fragments, and a biologically active compound. Various aspects of the invention include processes for synthesizing glinkosides, glinkoside compositions, and methods of treating diseases using glinkosides.

Carbohydrate conjugated bio-active compounds

A number of modified nucleosides are disclosed composed of modified sugar moieties which contain substituents at C1 and C4 positions, or branched substituents at C3 and C5 positions of deoxyribose or ribose. Each nucleoside is converted to or properly protected and then converted to the corresponding phosphoramidites. These phosphoramidites are used to assemble oligonucleotides in which there is at least one forenoted nucleosides. These sugar modified oligonucleotides have the potential to be used as antisense therapies since they are expected to enhance nuclease resistance and cellular uptake while they maintain sequence-specificity and affinity to nucleic acid targets in vitro or in vivo.

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La Jolla, CA, United States of America

Wilfried E Seifert