Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Peptides with at least one nonpeptide bond other than a...
Patent
1995-06-07
1998-12-15
Russel, Jeffrey E.
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
Peptides with at least one nonpeptide bond other than a...
514 17, 514 18, 514 19, 514551, 514620, 514676, 530330, 530331, 530345, 560 39, 562440, 564157, 568305, 568306, 568307, 930 23, 930 30, C07C 4900, C07C23300, C07K 500, C07K 700
Patent
active
058498664
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of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety.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: 5496927 (1996-03-01), Kolb et al.
patent: 5541290 (1996-07-01), Harbeson et al.
patent: 5597804 (1997-01-01), Webb et al.
Gelb et al., "Fluoro Ketone Inhibitors of Hydrolytic Enzymens," 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 Pancreatic 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 Difluorostatone-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.
Peet, NP. et al. J. Medicianl Chemistry, (1990) vol. 33 No. 1, pp. 394-407.
Angelastro, M.R. et al., Biooganic & Medicinal Chemistry Ltrs., vol. 2, No. 10, pp. 1235-1238, (1992).
Angelastro, M.R. et al., JK. Med. Chem., (1990) 33, 11-13.
Burkhart Joseph P.
Gerhart, deceased Fritz E.
Giroux Eugene L.
Jung Michel J.
Kolb H. Michael
Merrell Pharmaceuticals Inc.
Russel Jeffrey E.
Wille Louis J.
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