Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-05-07
1998-10-27
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549388, A01N 4316, C07D31182
Patent
active
058278770
ABSTRACT:
The present invention is directed to novel ketomethylene group-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.
REFERENCES:
patent: 4518528 (1985-05-01), Rasnick
patent: 5081284 (1992-01-01), Higuchi et al.
patent: 5328916 (1994-07-01), Raddatz et al.
patent: 5444042 (1995-08-01), Bartus et al.
patent: 5498616 (1996-03-01), Mallamo et al.
patent: 5498728 (1996-03-01), Sohda et al.
patent: 5545640 (1996-08-01), Beaulieu et al.
Chatterjee et al., Xanthene Derived Potent Nonpeptidic Inhibitors of Recombinant Human Calpain I., Biorganic & Medicinal Chem. Letters, vol. 6, No. 13, 1996, pp. 1619-1622.
Sebastian et al., Effect of Enzyme-Substrate Interactions Away From the Reaction Site On Carboxy Peptidase A Catalysis, Biorganic Chem., vol. 24, No. 3, 1996, pp. 290-303.
Angliker, H. et al., "Inactivation of Calpain by Peptidyl Fluoromethyl Ketones", J. Med. Chem. 1992, 35, 216-220.
Greene and Wuts, "Protective Groups in Organic Synthesis", 2nd Edition, Wiley & sons, 1991.
Hamada, Y. et al., "Efficient Total Synthesis of Didemnins A and .sup..dagger.,1 ", J. Am. Chem. Soc. 1989, 111, 669-673.
Harbeson, S. et al., "Stereospecific Synthesis of Peptidyl .alpha.-Keto Amides as Inhibitors of Calpain", J. Med. Chem. 1994, 37, 2918-2929.
Harris, B. et al., "Synthetic Studies of Didemnins. II. Approaches to Statine Diastereomers", Tetrahedron Letters 1987, 28(25), 2837-2840.
Hoffman, R. V. et al., "A New Chiral Alkylation Methodology for the Synthesis of 2-Alky-4Ketoacids in High Optical Purity Using 2-Triflyloxy Esters", Tetrahedron Letters 1993, 34(13), 2051.
Hoffman, R.V. and Kim, "The Stereoselective Synthesis of 2-Alkyl .gamma.-Keto Acid and Heterocyclic Ketomethylene Peptide Isostere Core Units using Chiral Alkylation by 2-Triflyloxy Esters", J. Org. Chem. 1995, 60, 5107-5113.
Imperiali, B. and Abeles, "A Versatile Synthesis of Peptidyl Fluoromethyl Ketones", Tetrahedron Letters 1986, 27(2), 135-138.
Lee, W.J. et al., "Factors Influencing the Binding of Calpain I to Human Erythrocyte Inside-Out Vesicles", Biochemistry International 1990, 22(1), 163-171.
Lehninger, "Biochemistry", 2nd Edition, Worth Publishers, 1975, pp. 73-75.
Luly, J.R. et al., "A Synthesis of Protected Aminoalkyl Epoxides from .gamma.-Amino Acids", J. Org. Chem. 1987, 52, 1487-1492.
Patel, D. et al., "Activated Ketone Based Inhibitors of Human Renin", J. of Medicinal Chem. Aug. 20, 1993, 36(17), 2431-2447.
"Remington's Pharmaceutical Sciences", Mack Publishing Co., Easton, PA, 1980.
Revesz, L. et al., "Synthesis of P1 Aspartate-Based Peptide Acyloxymethyl and Fluoromethyl Ketones as Inhibitors of Interleukin-1.beta.-Converting Enzyme", Tetrahedron Letters 1994, 35(52), 9693-9696.
Tung, R. and Rich, "Bis(2-oxo-3-oxazolidinyl) phosphinic Chloride (1) as a Coupling Reagent for N-Alkyl Amino Acids", J. Am. Chem. Soc. 1985, 107, 4342-4343.
Cephalon Inc.
Ngo Tamthom T.
Shah Mukund J.
LandOfFree
Ketomethylene group-containing cysteine and serine protease inhi does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Ketomethylene group-containing cysteine and serine protease inhi, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Ketomethylene group-containing cysteine and serine protease inhi will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1614188