Beta-lactam elastase inhibitors

Details Beta-lactam elastase inhibitors Beta-lactam elastase inhibitors

C - Chemistry, Metallurgy

07

D

260/111, 167/188

C07D 499/86 (2006.01) A61K 31/425 (2006.01) C07D 499/88 (2006.01) C07D 513/04 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2017920

Novel beta lactam compounds having potent elastase inhibition activity are disclosed. These compounds are characterized by the general structural formulae I, II, and III: Image Image Image These compounds are further characterized such that X and Y are each -S- or -CH2-, with at least one of X and Y being -S-, or alternatively, X is -SO- or -SO2- and Y is -CH2-; R1 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; R3 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.

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