Method of inhibiting .beta.-lactamase forming pathogens

Details Method of inhibiting .beta.-lactamase forming pathogens Method of inhibiting .beta.-lactamase forming pathogens

1981-10-20

1985-04-23

Rizzo, Nicholas S.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

2602452R, 514195, C07D49900, A61K 31425

Patent

active

045129991

ABSTRACT:
There are presented .beta.-lactams of the formula ##STR1## wherein R.sup.1 is cyano or a group of the formula R.sup.4 --CO-- or R.sup.5 --A--CO--, R.sup.2 is hydrogen, lower alkyl or halogen, R.sup.3 is hydrogen or a group readily cleavable by hydrolysis, n is the number 0, 1 or 2, R.sup.4 is hydrogen, hydroxy, lower alkoxy, lower alkyl, aryl or a group of the formula ##STR2## R.sup.5 is halogen, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl or di-(loweralkoxy)phoshinyl, R.sup.6 and R.sup.7 are lower alkyl and A is lower alkylene,
and pharmaceutically acceptable salts of carboxylic acids of formula I with bases.
The compounds exhibit pronounced .beta.-lactamase-inhibiting properties.

REFERENCES:
patent: 4020077 (1977-04-01), Cook et al.
patent: 4143046 (1979-03-01), Sheehan
patent: 4207323 (1980-06-01), Beattie et al.
patent: 4236001 (1980-11-01), Gleason
patent: 4282149 (1981-08-01), Sheehan et al.

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