Trifluoromethylketone derivatives, processes for preparation the

Details Trifluoromethylketone derivatives, processes for preparation the Trifluoromethylketone derivatives, processes for preparation the

1991-12-12

1994-03-22

Moezie, F. T.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Tripeptides, e.g., tripeptide thyroliberin , etc.

564153, 564 51, 548537, 544164, 544168, 562435, 562439, 562450, 560 20, 560 34, 560 41, 530332, C07K 500, C07K 506

Patent

active

052965910

ABSTRACT:
The trifluoromethylketone derivatives (I) and pharmaceutically acceptable salts thereof have a human leukocyte elastase inhibiting activity and are useful as human leukocyte elastase inhibitors for treating or preventing degenerative diseases. The trifluoromethylketone derivatives (I) have the following formula: ##STR1## wherein R.sup.1 is C.sub.1-6 alkyl which has one or two substituents selected from carboxy, esterified carboxy and di-C.sub.1-6 alkylcarbamoyl; phenyl(C.sub.1-6) alkyl, the phenyl moiety of which may have halogen or nitro or amino substituents and the alkyl moiety of which may have carboxy or esterified carboxy substituents; halo-phenyl; morpholino; or morpholino(C.sub.1-6) alkyl,

REFERENCES:
patent: 4910190 (1990-03-01), Bergeson
patent: 5221665 (1973-06-01), Skiles
Skiles et al Chemical Abstracts, 116 (11), 1992--abst. No. 106736y.
Research Communications in Chemical Pathology and Pharmacology, vol. 68, No. 3, Jun. 1990, pp. 365-374, Jerry W. Skiles, et al., "Inhibition of Human Leukocyte Elastase by N-substituted Tripeptide Trifluoromethyl Ketones".

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