Peptidase inhibitors

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – 8 to 10 amino acid residues in defined sequence

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562561, 562418, 562433, 562439, 562445, 562526, 562560, 564138, 564139, 564153, 564155, 564157, 564159, 564164, 564169, 564193, 564198, 514 15, 514 16, 514 17, 514 18, 514 19, 514 20, 514538, 514541, 514542, 514551, 514563, 514564, 514565, 514617, 514626, 530329, 530330, 530331, 530338, 530343, 530345, 560 19, 560 34, 560 37, 560 40, 560155, 560169, C07K 700, C07K 102, C07K 1107, C07K 506, C07K 508, C07K 510

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active

061303151

ABSTRACT:
This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

REFERENCES:
patent: 4277395 (1981-07-01), Bey et al.
patent: 4518528 (1985-05-01), Rasnick
patent: 5066643 (1991-11-01), Abeles et al.
patent: 5496927 (1996-03-01), Kolb et al.
patent: 5541290 (1996-07-01), Harbeson et al.
patent: 5597804 (1997-01-01), Webb et al.
patent: 5849866 (1998-12-01), Kolb et al.
Imperiali et al, A Versatile Synthesis of Peptidyl Fluoromethyl Ketones, Tet. Lett. vol. 27, No. 2, pp. 135-138, Jan. 1986.
Robert et al, Basic Principles of Organic Chemistry, 2nd ed. Menlo Park: W.A. Benjamin, Inc. p. 615, 1977.
Gelb et al., "Fluoro Ketone Inhibitors of Hydrolytic Enzymes," Biochemistry 24, No. 8, 1813-1817, (1985).
Chemical Abstracts, vol. 75, 77254 (1971) abstracting Parr, et al., Tetrahedron Lett. 28, 2633-6 (1971).
Powers, J.C., et al., "Specificity of Porcine Elastase, Human Leukocyte Elastase and Cathepsin G," Biochimica et Biophysica Acta 485, 156-166 (1977).
Imperiali, B., et al., "Inhibition of Serine Proteases by Peptidyl Fluoromethyl Ketones," Biochemistry 25, Imperiali et al., 3760-7 (1986).
Chemical Abstracts vol. 92, 175119 (1980).
Hori, H., et al., "Inhibition of Human Leukocyte Elastase, Porcine Pancreatic Elastase and Cathepsin G by Peptide Ketones," Enzyme Inhibitors, Proceedings of the Ninth American Peptide Symposium pp. 819-822 (1985).
Thaisrivongs, S., et al., "Diflourostatine- and Difluorstatone-Containing Peptides as Potent and Specific Renin Inhibitors," J. of Med. Chem., vol. 28, No. 11, 1553-5 (1985).
Chemical Abstracts, vol. 96, No. 176795j, p. 315, (1982) abstracting Rich, D.H., et al., Biochem. Biophys. Res. Commun., 104(3), 1127-33 (1982).
Fieser and Fieser's Reagents for Organic Synthesis, vol. 11, p. 215 (1982).
Amino Acids, Peptides Proteins, Vo. 93, 1980 PP 989; Chemical Abstracts 93:47184y.
Peet, NP. et al. J. Medicinal Chemistry, 1990 vol. 33 No. 1, pp. 394-407.
Angelastro, M.R. et al., Bioorganic & Medicinal Chemistry Ltrs., vol. 2, No. 10, pp. 1235-1238, 1992.
Angelastro, M.R. et al., JK. Med. Chem., 1990 33, 11-13.

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