Cysteine protease and serine protease inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514242, 514256, 514259, 544182, 544183, 544184, 544279, 544287, 544319, A61K 31505, A61K 3153, C07D23936, C07D25304

Patent

active

056589069

ABSTRACT:
The present invention is directed to irreversible inhibitors of serine and cysteine proteases which most preferably contain a 1-oxytriazole or 1-oxyimidazole functionality. Methods for the use of the protease inhibitors are also described.

REFERENCES:
patent: 5328916 (1994-07-01), Raddatz et al.
patent: 5374623 (1994-12-01), Zimmerman et al.
patent: 5486623 (1996-01-01), Zimmerman et al.
Carpino, L.A., "1-Hydroxy-7-azabenzotriazole. An efficient Peptide Coupling Additive", J. Am. Chem Soc. 1993, 115, 4397-4398.
Deshpande et al., "Differential Distribution of Calpain in Human Lymphoid Cells", Neurochem. Res. 18:767-773 (1993).
Greene, T.W. et al., Protective Groups in Organic Synthesis, pp.15 and 48, John Wiley & Sons, New York, 1991.
Harbeson. S.L. et al., "Inhibition of Aminopeptidases by Peptides Containing Ketomethylene and Hydroxyethylene Amide Bond Replacements", J. Med. Chem. 1989, 32, 1378-.
Hayashi et al., "Activation of Intracellular Calcium-Activated Neutral Proteinase in erythrocytes and its Inhibition by Exogenously Added Inhibitors", Biochem. Biophys. Acta 1991, 1094, 249-256.
Hoffman, R.V. et al., "A New Chiral Alkylation Methodology for the Synthesis of 2-Alkyl-4-Ketoacids in High Optical Purity Using 2-Trifyloxy Esters", Tetrahedron Lett. 1993, 34(13), 2051-2054.
Konig, W. et al., "Eine neue Methode zur Synthese von Peptiden: Aktivierung der Carboxylgruppe mit Dicyclohexylcarbodiimid unter Zusatz von 1-Hydroxy-benyotriazolen", Chen. Ber. 1970, 103, 788-798.
Laemmli, U.K., "Cleavage of Structural Proteins During the Assembly of the Head of Bacteriophage T4", Nature 1970, 227, 680-685.
McGowan et al., "Inhibition of Calpain in Intact Platelets by the Thiol Protease Inhibitor E-64d", Biochem. Biophys. Res. Commun. 1989, 158, 432-435.
Mehdi et al., "Inhibition of the Proteolysis of Rat Erythrocyte Membrane Proteins by a Synthetic Inhibitor of Calpain", Biochem. Biophys. Res. Commun. 1988, 157, 1117-1123.
Remington's Pharmaceutical Sciences (Mack Pub. Co., Easton, PA, 1980.).
Roberts-Lewis et al., "Immunolocalization of Calpain I-mediated Spectrin Degradation to Vulnerable Neurons in the Ischemic Gerbil Brain", J. Neurosci. 1994, 14, 3934-3944.
Seng, F. et al., "Eine einfache Synthese von 1-Hydroxy-benzimidazol-2-carbonsaure", Synthesis 1975, p. 703-704.
Towbin et al., "Electrophoretic Transfer of Proteins from Polyacrylamide Gels to Nitrocellulose Sheets: Procedure and Some Applications", PNAS 1979, 76, 4350-4354.
Seng, F. et al., "1,3-Dihydroxy-2-N-alkylimino-benizimidazoline", Synthesis 1975, p. 703-704.

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