Peptides and their use for the treatment of HIV infections

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

Reexamination Certificate

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Details

C530S324000, C530S326000, C424S001690, C435S005000

Reexamination Certificate

active

07655629

ABSTRACT:
The invention relates to peptides with biological activity against infection having the amino acid sequence Z1-LE-X1-IP-X2-X3-X4-P-X5-X6-X7-X8-X9-X10-K-X11-X12-X13-X14-X15-Z2, wherein X1is a lysine, alanine, or aspartic acid; X2is a cysteine, methionine or isoleucine; X3is a serine, cysteine, lysine or glycine; X4is an isoleucine, alanine, phenylalanine or cysteine; X5is a proline, D-proline or a substituted L- or D-proline; X6is a cysteine or glutamic acid; X7is an amino acid with a hydrophobic or an aromatic side chain or cysteine; X8is an amino acid with a hydrophobic or an aromatic side chain or cysteine; X9is an amino acid with an aromatic side chain; X10is a glycine, alanine or asparagine; X11is a proline, aspartic acid, octahydroindolyl-2-carboxylic acid or D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; X12is a phenylalanine, alanine, glycine, glutamic acid or D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; X13is an amino acid with a hydrophobic or an aromatic side chain; X14is an amino acid with a hydrophobic or an aromatic side chain; X15is a phenylalanine or deletion; Z1is NH2or a sequence of 1 to 10 amino acid residues; Z2is COOH or a sequence of 1 to 10 amino acid residues; and peptides which are fragments and/or covalently linked oligomers and/or derivatives, especially amidated, alkylated, acylated, sulfated, pegylated, phosphorylated and/or glycosylated derivatives, and mutants thereof, and with the provisio that (a) if X12is alanine, glycine, glutamic acid, or D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid than X13, X14and X15are phenylalanine, valine and phenylalanine respectively; and/or (b) if X12is phenylalanine, than X13, X14and X15are valine, phenylalanine and a deletion, respectively; and (c) that there are at maximum two cysteine residues in a peptide.

REFERENCES:
patent: 6200801 (2001-03-01), Ferkol et al.
patent: WO 92/18141 (1992-10-01), None
patent: WO 01/08708 (2001-02-01), None
patent: WO 01/34640 (2001-05-01), None
Shapiro, et al., “Alpha-1-antitrypsin inhibits human immunodeficiency virus type 1,” FASEB Journal, Fed. Of American Soc. For Experimental Biology, vol. 15, No. 1, Jan. 2001, p. 115-122, [XP002164955].
Detheux, et al., Journal of Experimental Medicine, s. example 3), 2000.
J. Gante, Peptidomimetics-tailored enzyme inhibitors, Angewandte Chemie International Edition 33, 1994, 1699-1720.
F. Tratar, Arkivoc 2001, 7-20, free access via internet under http://www.arkat-usa.org/ark/journal/2001/I05—Tisler/187/0109—index.asp, 2001.
H.D. Jakubke, Peptide, Spektrum Akademischer Verlag, 1996, 00. 286-296.
G.B. Wisdom (editor), Peptide Antigens—A Practical Approach, 1994, Oxford University Press, New York, pp. 117-179.

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