N.sup.6 - substituted nucleotide analagues and their use

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

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514 81, 530345, 530352, 530409, 544244, 546 23, A61K 31675, A61K 3802, C07F 938, C07K 200

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active

059770619

ABSTRACT:
Novel PMP, PME and HPMP and related compounds containing N-6 substituted 2,6-diaminopurine and adenine bases are provided. These compounds are useful in a variety of utilities, including as intermediates in the preparation of flame retardants, diagnostic reagents and therapeutics, including antivirals. Of particular note are compounds otherwise not known to possess anti-DNA viral activity that become potent inhibitors of DNA viruses upon substitution of the N-6 site, thereby providing a novel and unexpected and surprising use for such compounds.

REFERENCES:
patent: 4659825 (1987-04-01), Holy et al.
patent: 4724233 (1988-02-01), De Clercq et al.
patent: 4808716 (1989-02-01), Holy et al.
patent: 5142051 (1992-08-01), Holy et al.
patent: 5208221 (1993-05-01), Kim et al.
patent: 5302585 (1994-04-01), Yu et al.
patent: 5352786 (1994-10-01), Jindrich et al.
patent: 5356866 (1994-10-01), Arai et al.
patent: 5356886 (1994-10-01), Harnden
patent: 5514798 (1996-05-01), Bischofberger et al.
patent: 5591851 (1997-01-01), Alexander
Ching et al., "Nonclinical toxicology and in vitro Toxicity Studies with the Novel Anti-HIV Agent (1S,4R)-4-[2-Amino-6-(Cyclopropylamino)-9H-Purin-9-YL]-2-Cyclopentene-1-Me thanol (1592U89) Succinate," Presentations @ the 34th Interscience Conf. on Antimicrobial Agents & Chemotherapy, Orlando, Florida Abstract # 188 (Oct. 4-7, 1994).
Cihlar et al., "Transport of 9-(2-Phosphonomethoxyethyl)Adenine across Plasma Membrane of HeLa S3 Cells Is Protein Mediated," Antimicro AG & Chemo 39(1):117-124 (1995).
Colla, et al., "Synthesis of aliphatic nucleoside analogues with potential antiviral activity," Eur J Med Chem 17:569-576 (1982).
Daluge et al., "1592U89 Succinate--A Novel Carbocylic Nucleoside Analog With Potent, Selective Anti-HIV Activity," Presentations @ the 34th Interscience Conf. on Antimicrobial Agents & Chemotherapy, Orlando, Florida Abstract # 16 (Oct. 4-7, 1994).
De Clercq et al., "Antiviral activity of phosphonylmethoxyalkyl derivatives of purine and pyrimidines," Antiviral Res 8:261-272 (1987).
Faletto et al., "Unique Intracellular Activation of a New Anti-HIV Agent (1S,4R)-4-[2-Amino-6-(Cyclopropylamino)-9H-Purin-9-YL]-2-Cyclopentene-1-Me thanol (1592U89) in the Human T-Lymphoblastoid Cell Line CEM-T4," Presentations @ the 34th Interscience Conf. on Antimicrobial Agents & Chemotherapy, Orlando, Florida Abstract # 184 (Oct. 4-7, 1994).
Good et al., "Disposition in Monkeys and Mice of (1S,R4)-4-[2-Amino-6-(Cyclopropylamino)-9H-Purin-9-YL)-2-Cyclopentene-1-Me thanol (1592U89) Succinate, A Potent Inhibitor of HIV," Presentations @ the 34th Interscience Conf. on Antimicrobial Agents & Chemotherapy, Orlando, Florida Abstract # 186 (Oct. 4-7, 1994).
Holy et al., "Antiviral Acyclic Nucleotide Analogues," Antibiotics and Antiviral Compounds 455-462 (1993).
Schaeffer, et al, "Enzyme Inhibitors. VIII. Studies on the Mode of Binding of Some 6-Substituted 9-(Hydroxyalkyl)purines to Adenosine Deaminase," J Med Chem 8(4):502-506 (1965).
Tisdale et al., "Anti-HIV Activity of (1S,4R)-4-[2-Amino-6-(Cyclopropylamino)-9H-Purin-9-YL]-2Cyclopentene-1-Met hanol (1592U89)," Presentations @ the 34th Interscience Conf. on Antimicrobial Agents & Chemotherapy, Orlando, Florida Abstract # 182 (Oct. 4-7, 1994).
Balzarini et al., "Differential Antiherpesvirus and Antiretrovirus Effects of the (S) and (R) Enantiomers of Acyclic Nucleoside Phosphonates: Potent and Selective In Vitro and In Vivo Antiretrovirus Activities of (R)-9-(2-Phosphonomethoxypropyl)-2,6-Diaminopurine," Antimicrobial Agents and Chemotherapy, 37(2):332-338 (1993).
Dvorakova et al., "Synthesis and Antiviral Activity of Acyclic Nucleoside and Nucleotide Derivatives of 8-Azaadenine," Collect. Czech. Chem. Commun., 58:253-255 (1993).
Dvorakova et al., "Synthesis and Biological Effects of 9-(3-Hydroxy-2-Phosphonomethoxypropyl)Derivatives of Deazapurine Bases," Collect. Czech. Chem. Commun., 58:1403-1418 (1993).
Holy et al., "Phosphonylmethyl Ethers of Nucleosides and Their Acyclic Analogues," Am. Chem. Soc., Nucleotide Analogues, Chpt. 4, pp. 51-71 (1989).
Naesens et al., "HPMPC (Cidofovir), PMEA (adefovir) and Related Acyclic Nucleoside Phosphonate Analogues: A Review of their Pharmacology and Clinical Potential in the Treatment of Viral Infections," Antiviral Chem. & Chemotherapy, 8(1):1-23 (1997).

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