Beta-lactam elastase inhibitors

Details Beta-lactam elastase inhibitors Beta-lactam elastase inhibitors

1989-06-01

1992-07-21

Rizzo, Nicholas S.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514210, 540303, 540304, 540310, C07D51302, C07D49900, A61K 31385

Patent

active

051323001

ABSTRACT:
Novel beta lactam compounds having potent elastrase inhibition activity are disclosed. These compounds are characterized by the general structural formulae I, II, and III: ##STR1## These compounds are further characterized such that X and Y are each --S-- or --CH.sub.2 --, with at least one of X and Y being --S--, or alternatively, X is --SO-- or --SO.sub.2 -- and Y is --CH.sub.2 --; R.sup.1 is hydrogen, tri(lower alkyl)silyl, --COOR" or --CONHR"', wherein R" and R"' are each lower alkyl or phenyl(lower alkyl), and may be the same or different; R.sup.3 is hydrogen, lower alkyl or (lower alkyl)oxy; one of B and D is (lower alkyl)oxycarbonyl, (lower alkenyl)oxycarbonyl, allyloxycarbonyl or phenyl(lower alkyl)oxycarbonyl; and the other of B and D is hydrogen or lower alkyl.
The compounds are useful as anti-inflammatory agents, particularly in the treatment of adult respiratory distress syndrome and rheumatoid arthritis.

REFERENCES:
patent: 4797396 (1989-01-01), Finke et al.
patent: 4847247 (1989-07-01), Thompson et al.

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