L-nucleosides

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

514 47, 514 49, 514 50, 514 51, 536 2626, 536 267, 536 268, 536 276, 536 285, 536 2854, 536 2855, 424420, 424457, A61K 3170

Patent

active

055873626

ABSTRACT:
A compound, and a pharmaceutical composition comprising an effective mount to treat HBV or EBV of a compound, of the formula: ##STR1## wherein R is selected from the group consisting of 5-methyluracil, adenine and cytosine, and R' is hydrogen, acyl, or alkyl or a monophosphate, diphosphate or triphosphate ester, or its pharmaceutically acceptable salt.

REFERENCES:
patent: 3116266 (1963-12-01), Hunter
patent: 3553192 (1971-01-01), Gauri
patent: 4000137 (1976-12-01), Dvonoch et al.
patent: 4336381 (1982-06-01), Nagata et al.
patent: 4861759 (1989-08-01), Mitsuya et al.
patent: 4879277 (1989-11-01), Mitsuya et al.
patent: 4900828 (1990-02-01), Belica et al.
patent: 4916122 (1990-04-01), Chu et al.
patent: 4963533 (1990-10-01), de Clercq et al.
patent: 4968674 (1990-11-01), Taniyama et al.
patent: 5041449 (1991-08-01), Belleau et al.
patent: 5047407 (1991-09-01), Belleau et al.
patent: 5059690 (1991-10-01), Zahler et al.
patent: 5071983 (1991-12-01), Koszalka et al.
patent: 5089500 (1992-02-01), Daluge
patent: 5151426 (1992-09-01), Belleau et al.
patent: 5179104 (1993-01-01), Chu et al.
patent: 5185437 (1993-02-01), Koszalka et al.
patent: 5204466 (1993-04-01), Liotta et al.
patent: 5210085 (1993-05-01), Liotta et al.
patent: 5215971 (1993-06-01), Datema et al.
patent: 5234913 (1993-08-01), Furman, Jr. et al.
patent: 5246924 (1993-09-01), Fox et al.
patent: 5248776 (1993-09-01), Chu et al.
patent: 5270315 (1993-12-01), Belleau et al.
patent: 5276151 (1994-01-01), Liotta
patent: 5409906 (1995-04-01), Datema et al.
patent: 5432165 (1995-07-01), Adair et al.
patent: 5444063 (1995-08-01), Schinazi
patent: 5448029 (1995-08-01), Eriksson et al.
patent: 5466806 (1995-11-01), Belleau et al.
Asseline, U., et al., "Synethesis and Physiocochemical Properties of Oligonucleotides Built with Either .alpha.-L or .beta.-L Nucleotides Units and Covalently Linked to an Acridine Derivative," Nucleic Acids Research, 19(15):4067-4074 (1991).
Balzarini, J., et al., "Potent and Selective Anti-HTLV-III/LAV Activity of 2',3'-Dideoxycytidinene, . . . , " Bioch. and Bioph. Res. Comm. 140(2):735-742 (1986).
Beach, J. W., et al., "Synthesis of EnantiomericallyPure (2'R,5'S)-(-)-1-[2-(hydroxymethyl)-oathiolan-5-yl]Cytosine . . . , " J. Org. Chem. 57:2217-2219 (1992).
Belleau, B., et al., "Design and Activity of a Novel Class of Nucleoside Analogs . . . , " Intl. Conf. on AIDS, Montreal, Quebec, Canada, Jun. 4-9, 1989.
Bouffard, D. Y., et al., "Kinetic Studies on 2',2'-Difluorodeoxycytidine(Gemcitibine) with purified Human Deoxycytidine Kinase and Cytidine Deaminase," Biochem. Pharmacol. 45(9):1857-1861 (1993).
Carter, et al., "Activities of (-)-Carbovir and 3'-Azido-3'-Deoxythymidine Against Human Immunodeficiency Virus In Vitro," Antimicrobial Agents and Chemotherapy, 34(6):1297-1300 (1990).
Chang, C-N., et al., "Biochemical Pharmacology of (+) and (-)-2',3'-Dideoxy-3'Thloacytidine as Anti-Hepatitis B Virus Agents," J. Biol. Chem. 267(31):22414-22420 (1992).
Chang, Chien-Neng, et al., "Deoxycytidine Deaminase-resistant Sterolisomer is the Active Form of . . . , " J. Bio. Chem., 267(20):13938-13942 (1992).
Chang, Chungming, et al., "Production of Hepatitis B Virus in vitro by Transient Expression . . . , " The EMBO J. 6(3):675-680 (1987).
Chen, Chin-Ho, et al., "Delayed Cytotoxicity and Selective Loss of Mitochondrial DNA in Cells . . . , " J. Bio. Chem. 264(20):11934-11937 (1989).
Cheng, Y. C., et al., "Human Deoxycytidine Kinase Purification and Characterization . . . , " Biochim. Biophys. Acta 481:481-492 (1977).
Chottiner, E. G., "Cloning and Expression of Human Deocytctidine Kinase cDNA," Proc. Natl. Sci. USA, 88:1531-1535 (1991).
Chu, C. K., et al., "An Efficient Total Synthesis of 3'-Azido-3'-Deoxythiymidine (AZT) and 3'-Azido-2',3'-Dideoxyuridine (AZDDU, CS-87) . . . , " Tetrahedron Lett., 29(42):5349-5352 (1988).
Chu et al., "Comparative Activity of 2',3'-Saturated and Unsaturated Pyrimidine and Purine Nucleosides . . . , " Biochem. Pharm. 37(19):3543-3548 (1988).
Chu, et al., "Structure-Activity Relationships of Pyrimidine Nucleosides as Antiviral Agents . . . , " J. Med. Chem. 32:612-617 (1989).
Chu, C. K., et al., "2'-Fluoro-5-Methyl-.beta.-L-Arabinofuranosyluracil as a Novel Antiviral Agent for Hepatitis B . . . , " Antimicrob. Agents Chemother., 39(4):979-981 (1995).
Coates, J., et al., "The Separated Enaniomers of 2'-deoxy-3'-thiacytidine (BCH-189) . . . , " Antimicrob. Agents Chemother. 36(1):202-205 (1992).
Cretton, E., et al., "Catabolism of 3'-Azido-3'-Deoxythymidine in Heptaocytes and Liver Microsomes . . . , " Molecular Pharmacology, 39:258-266 (1991).
Cretton, E., et al., "Pharmokinetics of 3'-Azido-3'-Dexoythymidine . . . , " Antimicrobial Agents and Chemotherapy, 35(5):801-807 (1991).
Di Bisceglie, Adrian M., Rustgi, Vinod K. et al., "Hepatocellular Carcinoma," NIH Conference, Annals of Internal Medicine, 108:390-401 (1988).
Doong, Shin-Lian., et al., "Inhibition of the Replication of Hepatitis B Virus in vitro . . . , " Natl. Acad. Sci. USA, 88:8495-8499 (1991).
Evans, David A., et al., "New Procedure for the Direct Generation of Titanium Enolates . . . , " J. Am. Chem. Soc., 112:8215-8216 (1990).
Finlay, G. J., et al., "A Semiautomated Microculture Method for Investigating Exponentially Growing Carcinoma Cells," Anal. Biochem., 139:272-277 (1984).
Furman, et al., "The Anti-Hepatitis B Virus Activities, Cytotoxicities, and Anabolic Profiles . . . , " Antim. Agents and Chemo., 36(12):2686-2692 (1992).
Ganem, Don et al., "The Molecular Biology of the Hepatitis B Viruses," Ann. Rev. Biochem., 56:651-693 (1987).
Gosselin, G., "Enantiomeric 2',3'-Deoxycytidine Derivatives are Potent Human Immunodeficiency Virus Inhibitors in Cell Cultures," C.R. Acad. Sci. Paris Sci. Vie. 317:85-89 (1994).
Jeong, L., et al., "Asymmetric Synthesis and Biological Evaluation of .beta.-L-(2R,5S)- and a-L-(2R-5R)-1,3-Oxathiolane-Pyrimidine and -Purine Nucleosides and Potential Anti-HIV Agents," J. Med. Chem., 36(2):181-195 (1993).
Kasslanides, Chris, et al., "Inhibition of Duck Hepatitis B Virus Replication by 2',3'-Dideoxycytidine," Gastroenterology, 97(5):1275-1280 (1989).
Kim, H. O., et al., "Potent Anti-HIV and Anti-HBV Activities of (-)-L-.beta.-Dioxolane-C . . . , " Tetrahedron Lett., 33(46):6899-6902 (1992).
Kim, H. O., et al., "L-.beta.-(2S,4S)-and L-.alpha.-(2S,4R)-Dioxolanyl Nucleosides as Potential Anti-HIV Agents: . . . , " J. Med. Chem., 36(5):519-528 (1993).
Kim, H. O., et al., "1,3-Dioxolanylpurine Nucelosides (2R,4R) and (2R,4S) with Selective Anti-HIV-1 Activity . . . , " J. Med. Chem. 36(1):30-37 (1993).
Krenitsky, T. A., et al., "3'-Amino-2',3'-Dideoxyribonucleosides of Some Pyrimidines; Synthesis and Biological Activities," J. Med. Chem., 26(6)891-895 (1983).
Kukhanova, M., et al., "L- and D-Enantiomers of 2',3'-Dideoxycytidine 5'-Triphosphate Analogs as Substrates for Human DNA Polymerases," J. Bio. Chem., 270(39):23056-23059 (1995).
Lee, Bonita, et al., "In Vitro and In Vivo Comparison of the Abilities of Purine and . . . , " Antimicrobial Agents and Chemotherapy, 33(3):336-339 (1989).
Lin, T. S., et al., "Antiviral Activity of 2',3'-Dideoxy-.beta.-L-5-fluorocytidiine(.beta.-L-FddC) Against Hepatitis B Virus . . . , " 1:65-68 (1991).
Lin, et al., "Potent and Selective In Vitro Activity of 3'-Deoxythmindine-2-Ene-. . . , " Biochem. Pharm., 36(17):2716 (1987).
Mansuri, M. M., et al., "Preparation of the Geometric Isomers of DDC, DDA, D4C, and D4T . . . , " Bioorg. Med. Chem. Lett., 1:65-68 (1991).
Matthes, E., et al., "Potent Inhibition of Hepatitis B Virus Production In Vitro by Modified . . . , " Anti. Agents and Chemot., 34(10):1986-1990 (1990).
Miller, Roger H., et al., "Common Evolutionary Origin of Hepatitis B Virus and Retroviruses," Proc. Natl. Acad. Sci. USA, 83:2531-2535 (1986).
Mitsuya, H., et al., "3'-Azido-3'-Deoxythymidine (BW A 509U): An Antiviral Agent that Inhibits . . . , " Proc. Natl. Acad. Sci., USA, 82:7097-7100 (1985).
Mitsuya, H., et al., "Rapid in Vitro Systems for Assessing . . . , " AIDS: Modern Concepts and Therapeutic Challenges, S. Broder, Ed. p. 303, Marcel-Dekk

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

L-nucleosides does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with L-nucleosides, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and L-nucleosides will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-1178596

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.