Polypeptides having anti-HIV activity and compositions...

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – 15 to 23 amino acid residues in defined sequence

Reexamination Certificate

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C530S327000, C530S333000, C530S857000

Reexamination Certificate

active

07138488

ABSTRACT:
Polypeptides of A1-Arg-A2-Cys-Tyr-A3-A4-X-A5-A6-Cit Cys-A7 (I) or their salts (wherein A1 is hydrogen or a residue of arginine, lysine, ornithine, citrulline, alanine, or the like; A2 is an aromatic amino acid residue; A3, A4 and A6 are each a residue of arginine, lysine, ornithine, citrulline, or alanine; A5 is a residue of tyrosine, phenylalanine, alanine, naphthylalanine, or citrulline; A7 is a lysine or arginine residue whose carboxyl group may be converted into amido; and X is a residue of D-ornithyl-proline, prolyl-D-ornithine, D-lysylproline, or the like, with the proviso that any one of A1, A3, A4, A5, A6 and A7 is a residue of alanine or the like or that X is citrulline or the like).

REFERENCES:
patent: WO 01/64716 (2001-09-01), None
Nakashima et al. “Anti-human immunodeficiency virus activity of a novel synthetic peptide, T22 ([Tyr-5,12, Lys-7]polyphemusin II): a possible inhibitor of virus-cell fusion”, Antimicrob Agents Chemother. Jun. 1992; 36(6): 1249-1255.
2000 Development of Specific CXCR4 Inhibitors Based on an Anti-HIV Peptide, T140, and Their Structure-Activity Relationships Study Akane Omagari et al. Peptide Science vol. 2000, No. 37th 129-132.
Sep. 14, 2000 Pharmacophore Identification of a Specific CXCR4 Inhibitor, T140, Leads to Development of Effective Anti-HIV Agents with Very High Selectivity Indexes Hirokazu Tamamura et al. Bioorganic & Medical Chemistry Letters vol. 10, No. 23 2633-2637.
Mar. 2001 Increase of R5 HIV-1 Infection and CCR5 Expression in T Cells Treated With High Concentration of CXCR4 Antagonists and SDF-1 Kazuko Gotoh et al. Journal of Infection and Chemotherapy vol. 7, No. 1 28-36.
1998 HIV-cell Fusion Inhibitors Targeted to the HIV Second Receptor: T22 and Its Downsized Analogs with High Activity Hirokazu Tamamura et al. Peptide Science vol. 1998, No. 35 49-52.
Dec. 30, 1998 A Low-Molecular-Weight Inhibitor against the Chemokine Receptor CXCR4: A Strong Anti-HIV Peptide T140 Hirokazu Tamamura et al. Biochemical and Biophysical Research Communications vol. 253, No. 3 877-882.
Oct. 16, 1997 Effective Lowly Cytotoxic Analogs of an HIV-cell Fusion Inhibitor, T22([Tyr5,12, Lys7]-polyphemusin II( Hirokazu Tamamura et al. Bioorganic & Medical Chemistry vol. 6, No. 2 231-238.
Feb. 1, 1999 “T134, a Small Molecule CXCR4 Inhibitor, Has No Cross-Drug Resistance with AMD3100, a CXCR4 Antagonist with a Different Structure” Rieko Arakaki et al. Journal of Virology vol. 73, No. 2 pp. 1719-1723.

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