3-amino-2-oxo-1-piperidineacetic derivatives containing an argin

Details 3-amino-2-oxo-1-piperidineacetic derivatives containing an argin 3-amino-2-oxo-1-piperidineacetic derivatives containing an argin

1995-06-07

1999-08-03

Rotman, Alan L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

540463, 540488, 540492, 540527, 544129, 544157, 544159, 544164, 544359, 544360, 546221, 546208, 548119, 548184, 548230, 5483215, 548413, 548550, A61K 31445, C07D21156

Patent

active

059327332

ABSTRACT:
The present invention discloses peptide aldehydes having a lactam group as part of the peptide backbone and having an original mimic group such as an amidinopiperidine or amidinophengyl tail. These compounds are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

REFERENCES:
patent: 4399065 (1983-08-01), Bajusz et al.
patent: 4433152 (1984-02-01), Muramatsu et al.
patent: 5371072 (1994-12-01), Webb et al.
patent: 5424334 (1995-06-01), Abood et al.
patent: 5492895 (1996-02-01), Vlasuk et al.
Skiles, J.W. et al Bioorg. Med. Chem. Lett. 1993, 3(4), 773-778.
Coughlin, P. et al Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 9417-9421.
G. Wagner et al., Pharmazie 39:5, pp. 315-317 (May 1984).
H. Vieweg et al., Pharmazie 42:4, p. 268 (Apr. 1987).
Aldrich Chemical Company, Inc. Catalog (1995) p. 283.
Bachem California Catalog (1993-1994) p. 121.
Bachem Bioscience Catalog (1995) p. 721.
Williams, et al., 2,2,1!-heptan-1 (S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperazine(L-368,889): An Orally Bioavailable, Non-Peptide Oxytocin Antagonist with Potential Utility for Managing Preterm Labor," J. Med. Chem.37:565-571 (1994).
Damewood, et al., "Nonpeptidic Inhibitors of Human Leukocyte Elastase. 2. Design, Synthesis, and in vitro Activity of a Series of 3-Amino-6-arylopyridine-2-one Trifluoromethyl Ketones," J. Med. Chem.37:3303-3312 (1994).
Skiles, et al., "Elastase Inhibitors Containing Conformationally Restricted Lactams as P.sub.3 -P.sub.2 Dipeptide Replacements," Bioorg. Med. Chem. Lett.3(4):773-779 (1993).
Freidinger, et al., "Protected Lactam-Bridged Dipeptides for Use as Conformational Constraints in Peptides," J. Org. Chem.47:104-109 (1982).

Affiliated with

Also associated with

Rating

3-amino-2-oxo-1-piperidineacetic derivatives containing an argin does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with 3-amino-2-oxo-1-piperidineacetic derivatives containing an argin, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 3-amino-2-oxo-1-piperidineacetic derivatives containing an argin will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-850657