Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1996-01-26
1997-08-19
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
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.
Bihovsky Ron
Chatterjee Sankar
Mallamo John P.
Tripathy Rabindranath
Cephalon Inc.
Raymond Richard L.
LandOfFree
Cysteine protease and serine protease inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Cysteine protease and serine protease inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Cysteine protease and serine protease inhibitors will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1104940