N-aryl-azetidinones, their preparation process and their use as

Details N-aryl-azetidinones, their preparation process and their use as N-aryl-azetidinones, their preparation process and their use as

1989-12-19

1991-07-09

Berch, Mark L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514825, 514824, A61K 31395, C07D20508, C07F 9568, C07F 718

Patent

active

050306286

ABSTRACT:
The invention relates to N-aryl-azetidinones, their preparation process and their use as active serine elastase inhibitors.
The N-aryl-azetidinones are in accordance with formula: ##STR1## in which R.sup.1 and R.sup.2 can be a halogen atom or an organic radical, R.sup.3 represents a halogen atom or another good starting group and R.sup.4 represents H or an organic radical.
The compounds with R.sup.3 .dbd.Cl or OSO.sub.2 CH.sub.3, R.sup.4 .dbd.H and R.sup.1 .dbd.R.sup.2 .dbd.F or R.sup.1 .dbd.F and R.sup.2 .dbd.Br are irreversible and selective elastase inhibitors.

REFERENCES:
patent: 4680391 (1987-07-01), Firestone
patent: 4803266 (1989-02-01), Kawash
Stirling, Ed, "The Chemistry of the Sulphonium Group", pp. 269, 267 (1981).
Zrihen, European Journal of Medicinal Chemistry, vol. 18, No. 4, 1983, pp. 307-314.
Ongania, Zeitschrift Fur Naturforschung, vol. 49b, No. 1, part B, Jan. 1985, pp. 115-116.

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