Cysteine protease and serine protease inhibitors

Details Cysteine protease and serine protease inhibitors Cysteine protease and serine protease inhibitors

1994-11-04

1996-03-12

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514242, 514243, 514256, 514259, 514303, 514359, 514395, 514398, 544182, 544183, 544184, 544279, 544287, 544319, 546117, 546118, 548255, 548256, 548259, 5483051, 5483097, 5483101, 5483114, 5483361, 5483411, 5483415, 5483421, A61K 3141, A61K 31415, A61K 3144, C07D24904

Patent

active

054986168

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:
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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-Hydroxybenyotriazolen", Chem. Ber. 1970, 103, 788-798.
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McGowan et al., "Inhibition of Calpain in Intact Platelets by the Thiol Protease Inhibitor E-64d", Biochem. Biophys. Res. Commun. 1989, 158, 432-435.
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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-Hydroxybenzimidazol-2-carbonsaure", Synthesis 1975, pp. 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-alkyliminobenizimidazoline", Synthesis 1975, pp. 703-704.

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