Clavulanic acid derivatives their preparation and use

Details Clavulanic acid derivatives their preparation and use Clavulanic acid derivatives their preparation and use

1980-04-11

1984-01-17

Goldberg, Jerome D.

Drug, bio-affecting and body treating compositions

Plural fermentates of different origin

A61K 3500

Patent

active

044263775

ABSTRACT:
This invention provides the compounds of the formula (II): ##STR1## and salts and esters thereof, wherein R.sub.1 is H and R.sub.3 is H or an aryl, aralkyl, lower alkyl or substituted lower alkyl group or R.sub.1 and R.sub.3 are joined so that the CHR.sub.1.NH.CO.R.sub.3 moiety forms a group of the sub-formula (a): ##STR2## wherein R.sub.4 is a hydrogen atom or a NH.CO.R.sub.5 group wherein R.sub.5 is a lower alkyl, lower alkoxy lower alkyl, aryl, aralkyl, aryloxyalkyl, lower alkoxy or aryloxy group.
The compounds have .beta.-lactamase inhibitory and anti-bacterial properties.
The invention also provides a process for their preparation, and pharmaceutical compositions containing them.

REFERENCES:
patent: 4215128 (1980-07-01), Howarth
Pro-drugs as Novel Drug Delivery Systems by T. Higuchi and V. Stella, Amer. Chem. Soc., 1975.

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