Claims for Patent: 6,316,612

Summary for Patent: 6,316,612

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:	09/135,964
Patent Claims:	1. A compound having the formula I: ##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, wherein 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, alky, 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; B is independently a nucleotide base or hydrogen; X is independently a phosphorus-containing group; and R.sub.2 is independently a blocking group or a phosphorus-containing group. 2. The compound of claim 1, wherein said compound is a nucleotide. 3. The compound of claim 1, wherein said compound is a nucleotide-triphosphate. 4. A polynucleotide comprising the compound of claim 1 at one or more positions. 5. The polynucleotide of claim 4, wherein said polynucleotide is an enzymatic nucleic acid. 6. The enzymatic nucleic acid of claim 5, wherein said nucleic acid is in a hammerhead configuration. 7. The enzymatic nucleic acid of claim 6, where in said nucleic acid is in a hairpin configuration. 8. The enzymatic nucleic acid of claim 6, wherein said nucleic acid is in a hepatitis delta virus, group I intron, VS RNA, group II intron or RNase P RNA configuration. 9. The compound of claim 1, wherein said compound is xylo riboadenosine. 10. The compound of claim 1, wherein said compound is xylo riboguanosine. 11. The compound of claim 1, wherein said compound is xylo ribonucleoside phosphoramidite. 12. The compound of claim 11, wherein said compound is xylo riboguanosine phosphoramidite. 13. The compound of claim 11, wherein said compound is xylo riboadenosine phosphoramidite. 14. A mammnalian cell comprising the compound of claim 1. 15. The mammalian cell of claim 14, wherein said cell is a human cell. 16. A mammalian cell comprising the compound of claim 5. 17. The mammalian cell of claim 16, wherein said cell is a human cell. 18. A method of making a polynucleotide of claim 4. 19. A method of modulating gene expression using a polynucleotide of claim 4. 20. A pharmaceutical composition comprising a compound of claim 1. 21. A pharmaceutical composition comprising a polynucleotide of claim 5. 22. The compound of claim 1, wherein said compound is used as an antiviral agent. 23. A process for the synthesis of a xylo ribonucleoside phosphoramidite comprising the steps of: a) oxidation of a 2' and 5'-protected ribonucleoside using an oxidant followed by reduction using a reducing agent under conditions suitable for the formation of 2' and 5'-protected xylofuranosyl nucleoside; and b) phosphitylation under conditions suitable for the formation of xylofuranosyl nucleoside phosphoramidite. 24. The process of claim 23, wherein said oxidation is carried out in the presence of chromium oxide, pyridine, and aceticanhydride. 25. The process of claim 23, wherein said oxidation is carried out in the presence of dimethylsulfoxide and aceticanhydride. 26. The process of claim 23, wherein said oxidation is carried out in the presence of Dess-Martin reagent (periodinane). 27. The process of claim 23, wherein said reduction is carried out in the presence of triacetoxy sodium borohydride. 28. The process of claim 23, wherein said reduction is carried out in the presence of sodium borohydride. 29. The process of claim 23, wherein said reduction is carried out in the presence of lithium borohydride.

Details for Patent 6,316,612

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