Positively charged non-natural amino acids, methods of making th

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

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436 86, 530324, 530325, 530326, 530327, 530328, 530329, 530330, 530331, 514 13, 514 14, 514 15, 514 16, 514 17, 514 18, 514 19, A61K 3800

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060432187

ABSTRACT:
This invention relates to positively charged non-natural amino acids, methods of making thereof, and utilization thereof in peptides. In one embodiment, the invention relates to non-natural amino acids that closely replicate the natural amino acids lysine and arginine.

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Lindeberg, et al, Solid Phase Synthesis And Some Hormonal Activities of 1-Deamino-4-L-Valine-8-D-Homolysine-And 1-Deamino-4-L-Valine-8-D-Homoarginine-Vasapressin, Int. J. Peptide Protein Res. 10, 240-244, 1977.
Moore, et al., Effect of the basic amino-acid side chain length and the penultimate residue on the hydrolysis of benzoyldipeptides by carboxpeptidbase B.sup.1, Can. J. Biochem, 56, 315-318, 1978.
Nestor, et al., Potent, Long-Acting Luteinizing Hormone-Releasing Hormone Antagonist Containing New Synthetic Amino Acids: N,N-Dialkyl-D-homoarginines .sup.1, J. Med. Chem, 31, 65-72, 1988.
Hilbert, et al., Design and Synthesis of Potent and Highly Selective Thrombin Inhibitors, J. Med. Chem. 37, 3889-3901, 1994.

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