Claims for Patent: 6,489,465

Summary for Patent: 6,489,465

Title:	Xylofuranosly-containing nucleoside phosphoramidites and polynucleotides
Abstract:	Novel xylo nucleoside or xylo nucleotide analogs, polynucleotides comprising xylo nucleotide substitution, processes for their synthesis and incorporation into polynucleotides.
Inventor(s):	Matulic-Adamic; Jasenka (Boulder, CO), Beigelman; Leonid (Longmont, CO)
Assignee:	Ribozyme Pharmaceuticals, Inc. (Boulder, CO)
Application Number:	09/960,192
Patent Claims:	1. A polynucleotide comprising a compound of the following formula at one or more positions: ##STR5## wherein R.sub.1 is --OH, --O--R.sub.3, --C--R.sub.3, halo, --NHR.sub.4, --ONHR.sub.5 or --ON.dbd.R.sub.6 ; R.sub.2 is independently blocking group or a phosphorus-containing group; B is independently a nucleotide base or its analog or hydrogen; X is independently a phosphorus-containing group; R.sub.3 is independently a moiety selected from a group consisting of alkyl, alkenyl, alkynyl, aryl, alkylaryl, carbocyclic aryl, heterocyclic aryl, amide and ester; R.sub.4 is independently a moiety selected from a group consisting of alkyl (C1-22), acyl (C1-22), substituted or unsubstituted aryl, or --OCH.sub.2 SCH.sub.3 (methylthiomethyl); R.sub.5 is independently a moiety selected from a group consisting of H, aminoacyl group, peptidyl group, biotinyl group, cholesteryl group, lipoic acid residue, retinoic acid residue, folic acid residue, ascorbic acid residue, nicotinic acid residue, 6-aminopenicillanic acid residue, 7-aminocephalosporanic acid residue, alkyl, alkenyl, alkynyl, aryl, alkylaryl, carbocyclic aryl, heterocyclic aryl, amide or ester; and R.sub.6 is independently pyridoxal residue, pyridoxal-5-phosphate residue, 13-cis-retinal residue, 9-cis-retinal residue, alkyl, alkenyl, alkynyl, alkylaryl, carbocyclic alkylaryl, or heterocyclic alkylaryl; the polynucleotide having one or more 2'-hydroxylamino moieties. 2. The polynucleotide of claim 1, wherein said polynucleotide is an enzymatic nucleic acid. 3. The enzymatic nucleic acid of claim 2, wherein said nucleic acid is in a hammerhead configuration. 4. The enzymatic nucleic acid of claim 2, wherein said nucleic acid is in a hairpin configuration. 5. The enzymatic nucleic acid of claim 2, wherein said nucleic acid is in a hepatitis delta virus, group I intron, VS RNA, group II intron or RNase P RNA configuration. 6. A pharmaceutical composition comprising a polynucleotide of claim 2. 7. The polynucleotide of claim 1 wherein the one or more 2'-hydroxylamino moieties reacts with an aldehyde to form an oxime. 8. The polynucleotide of claim 7, wherein said polynucleotide is an enzymatic nucleic acid. 9. The enzymatic nucleic acid of claim 8, wherein said nucleic acid is in a hammerhead configuration. 10. The enzymatic nucleic acid of claim 8, wherein said nucleic acid is in a hairpin configuration. 11. The enzymatic nucleic acid of claim 8, wherein said nucleic acid is in a hepatitis delta virus, group I intron, VS RNA, group II intron or RNase P RNA configuration. 12. A pharmaceutical composition comprising a polynucleotide of claim 8. 13. The polynucleotide of claim 1 wherein the one or more 2'-hydroxylamino moieties reacts with a carboxylic acid to form an oxyamides. 14. The polynucleotide of claim 13, wherein said polynucleotide is an enzymatic nucleic acid. 15. The enzymatic nucleic acid of claim 14, wherein said nucleic acid is in a hammerhead configuration. 16. The enzymatic nucleic acid of claim 14, wherein said nucleic acid is in a hairpin configuration. 17. The enzymatic nucleic acid of claim 14, wherein said nucleic acid is in a hepatitis delta virus, group I intron, VS RNA, group II intron or RNase P RNA configuration. 18. A pharmaceutical composition comprising a polynucleotide of claim 14. 19. A compound of the formula ##STR6## wherein R.sub.1 is --OH, --O--R.sub.3, --C--R.sub.3, halo, --NHR.sub.4, --ONHR.sub.5 or --ON.dbd.R.sub.6 ; R.sub.2 is independently blocking group or a phosphorus-containing group; B is independently a nucleotide base or its analog or hydrogen; X is independently a phosphorus-containing group; R.sub.3 is independently a moiety selected from a group consisting of alkyl, alkenyl, alkynyl, aryl, alkylaryl, carbocyclic aryl, heterocyclic aryl, amide and ester; R.sub.4 is independently a moiety selected from a group consisting of alkyl (C1-22), acyl (C1-22), substituted or unsubstituted aryl, or --OCH.sub.2 SCH.sub.3 (methylthiomethyl); R.sub.5 is independently a moiety selected from a group consisting of H, aminoacyl group, peptidyl group, biotinyl group, cholesteryl group, lipoic acid residue, retinoic acid residue, folic acid residue, ascorbic acid residue, nicotinic acid residue, 6-aminopenicillanic acid residue, 7-aminocephalosporanic acid residue, alkyl, alkenyl, alkynyl, aryl, alkylaryl, carbocyclic aryl, heterocyclic aryl, amide or ester; and R.sub.6 is independently pyridoxal residue, pyridoxal-5-phosphate residue, 13-cis-retinal residue, 9-cis-retinal residue, alkyl, alkenyl, alkynyl, alkylaryl, carbocyclic alkylaryl, or heterocyclic alkylaryl; wherein the compound is used as an anticancer or antitumor agent. 20. An enzymatic nucleic acid comprising a compound of the following formula at one or more positions: ##STR7## wherein R.sub.1 is --OH, --O--R.sub.3, --C--R.sub.3, halo, --NHR.sub.4, --ONHR.sub.5 or --0N.dbd.R.sub.6 ; R.sub.2 is independently blocking group or a phosphorus-containing group; B is independently a nucleotide base or its analog or hydrogen; X is independently a phosphorus-containing group; R.sub.3 is independently a moiety selected from a group consisting of alkyl, alkenyl, alkynyl, aryl, alkylaryl, carbocyclic aryl, heterocyclic aryl, amide and ester; R.sub.4 is independently a moiety selected from a group consisting of alkyl (C1-22), acyl (C1-22), substituted or unsubstituted aryl, or --OCH.sub.2 SCH.sub.3 (methylthiomethyl); R.sub.5 is independently a moiety selected from a group consisting of H, aminoacyl group, peptidyl group, biotinyl group, cholesteryl group, lipoic acid residue, retinoic acid residue, folic acid residue, ascorbic acid residue, nicotinic acid residue, 6-aminopenicillanic acid residue, 7-aminocephalosporanic acid residue, alkyl, alkenyl, alkynyl, aryl, alkylaryl, carbocyclic aryl, heterocyclic aryl, amide or ester; and R.sub.6 is independently pyridoxal residue, pyridoxal-5-phosphate residue, 13-cis-retinal residue, 9-cis-retinal residue, alkyl, alkenyl, alkynyl, alkylaryl, carbocyclic alkylaryl, or heterocyclic alkylaryl; the enzymatic nucleic acid having complimentarity with a target nucleic acid molecule.

Details for Patent 6,489,465

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Merck Sharp & Dohme Corp.	INTRON A	interferon alfa-2b	For Injection	103132	06/04/1986		2017-08-22
Merck Sharp & Dohme Corp.	INTRON A	interferon alfa-2b	For Injection	103132			2017-08-22
Merck Sharp & Dohme Corp.	INTRON A	interferon alfa-2b	Injection	103132			2017-08-22