Oligonucleotide compounds, their production and use

Details Oligonucleotide compounds, their production and use Oligonucleotide compounds, their production and use

C - Chemistry, Metallurgy

07

H

C07H 21/00 (2006.01) A61K 31/70 (2006.01) C07H 13/04 (2006.01) C07H 15/04 (2006.01) C07H 19/04 (2006.01) C12Q 1/02 (2006.01)

Patent

CA 2129565

OLIGONUCLEOTIDE COMPOUNDS, THEIR PRODUCTION AND USE Abstract of the Disclosure An oligonucleotide compound or a salt thereof, which has a nucleotide sequence represented by formula (I): (I) Image wherein W represents hydrogen or a protective group; B1, B2 and B3 each represent nucleic acid residues, wherein each B2 may be the same or different when n is 2 or more; X1, X2 and X3 each represent OH, SH, C1-5 alkyl, C1-5 alkoxy, C1-5 monoalkylamino or an aromatic ring group which may be substituted or unsubstituted, wherein each X3 may be the same or different when n is 2 or more; R1, R2 and R3 each represent hydrogen, OH, halogen, C1-5 alkoxy or C1-5 alkoxyalkyloxy, wherein each R2 may be the same or different when n is 2 or more; and n represents an integer from 1 to 98 is disclosed. The oligonucleotides (I) of the present invention or the salts thereof can (1) inhibit expression of genes associated with the development of malignant tumors in malignant tumor cells, (2) inhibit expression of viral genes derived from viruses, (3) inhibit expression of genes producing proteins which contribute to the development of inflammations, (4) control expression of drug-resistant genes which cause complications in chemotherapy of malignant tumors, and (5) inhibit production of cell growth factors related to reangiostenosis after PCTA (percutaneous transluminal coronary angioplasty) by complementation to DNAs or mRNAs of genes inducing various diseases. They can be therefore used as antitumor agents, antiviral agents, antiinflammatory agents and drugs for controlling expression of specific genes such as resistance genes. These oligonucleotides can also be used as probes. Further, these oligonucleotides can be used in novel drug screening assays.

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