Previns as specific inhibitors and therapeutic agents for...

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

Reexamination Certificate

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Details

C514S015800, C530S300000, C435S007100, C435S320100, C435S325000, C424S239100, C536S023500

Reexamination Certificate

active

11268757

ABSTRACT:
The compounds of the invention are generally described by the formula:in-line-formulae description="In-line Formulae" end="lead"?B1Z*2B3Z*4X*5Q6F7X8X9X10X11,   (1)in-line-formulae description="In-line Formulae" end="tail"?in-line-formulae description="In-line Formulae" end="lead"?B1X2X3X4X5Q6F7X8X9X10X11, or   (2)in-line-formulae description="In-line Formulae" end="tail"?in-line-formulae description="In-line Formulae" end="lead"?B1Z2B3X4Z5Q6F7Z8X9X10X11  (3)in-line-formulae description="In-line Formulae" end="tail"?and the salts, esters, amides, and acyl forms thereof. Each position represented by a letter indicates a single amino acid residue: B is a basic of polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large of hydrophobic amino acid or a modified form thereof. As described below, one or more of the peptide linkages between the amino acid residues may be replaced by a peptide linkage mimic.These compounds may be used as molecular building blocks to create compounds that are optimized for inhibiting the protease activity of Botulinum b and tetanus toxins.

REFERENCES:
patent: 6573244 (2003-06-01), Gordon et al.
patent: WO 99/37664 (1999-07-01), None
Garcia et al., Botulinum B Toxin Activity is Inhibited by Burorin I:, FASEB J., 12, A-1492 (1998).
Boksa et al., “Characterization of substance P and somatostatin receptors on adrenal chromaffin cells using structural analongs”, Brain Res., (1982), 245(2), pp. 275,283.
Park et al., “A Novel Antimicrobial Peptide from Bufo bufo gargarizans”, Biochemical and Biophysical Research Communication, 218, pp. 408-413, (1996).
Norinder et al., “A quantitative structure-activity relationship study of some substance P-related peptides”, K/ (e[tode Res. 49. pp. 155-162, (1997).
Niedzwiecki et al., “Substrate Specificity of the Human Matrix Metalloproteinase Stromelysin and the Development of Continuous Fluorometric Assays”. Biochemistry 31, pp. 12618-12623, (1992).

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