Heterocyclic compounds having elastase-inhibiting activity...

Details Heterocyclic compounds having elastase-inhibiting activity... Heterocyclic compounds having elastase-inhibiting activity...

2006-06-27

2006-06-27

Campell, Bruce R. (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

Reexamination Certificate

active

07067491

ABSTRACT:
Heterocyclic compounds represented by the general formula (I) and having elastase inhibiting activity; and intermediates for the synthesis thereof: (I) wherein R1is a heterocyclic group represented by the general formula (II): (II) [wherein A represents the presence or absence of a benzene ring; X is oxygen, sulfur or NH; and Y is nitrogen or CH], and the heterocyclic group may be substituted with one to three substituents which may be the same or different and are selected from the group consisting of lower alkyl, lower alkoxy, and phenyl which may be substituted with optionally halogenated lower alkyl, lower alkoxy or halogeno; and R2and R3are each hydrogen or hydroxyl, or R2and R3may be united to form an oxo group, with the proviso that both are not hydrogen.

REFERENCES:
patent: 189305 (1986-07-01), None
patent: 1157998 (2001-11-01), None
patent: WO 03066671 (2003-08-01), None
Joseph P. Burkhart,; Preparation of alpha keto ester enol acetate as potential prodrugs of human neutrophil elastase inhibitors. Bioorganic & medicinal chemistry letters,; Jan. 6, 1998, pp. 63-64. (abstract only).
Fuminori Sato, et al.; Design and synthesis of peptide -based carboxylic acid-containing transition-state inhibitors of human neutrophil elastase, Bioorganic & medicinal., Feb. 25, 2002, pp. 551-555. (abstract only).
P.D. Edwards et al., “Discovery and Biological Activity of Orally Active Peptidyl Trifluoromethyl Ketone Inhibitors of Human Nautrophil Elastase”, J. Med. Chem., vol. 40, No. 12, 1997, pp. 1876-1885.

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