Penicillanic and cephalosporanic derivatives, preparation thereo

Details Penicillanic and cephalosporanic derivatives, preparation thereo Penicillanic and cephalosporanic derivatives, preparation thereo

1981-12-03

1982-12-07

Hazel, Blondel

Drug, bio-affecting and body treating compositions

Conjugate or complex of monoclonal or polyclonal antibody,...

Conjugated via claimed linking group, bond, chelating agent,...

536 53, 536 173, A61K 3170, C07H 1526

Patent

active

043627218

ABSTRACT:
There are disclosed penicillanic and cephalosporanic derivatives of the formula: ##STR1## wherein R is H or --OH; R.sub.1 is a carbohydrate hexose radical of 3-O-glucose, 6-O-galactose, 3-O-glucose acetals, 3-O-glucose ketals, 6-O-galactose acetals, and 6-O-galactose ketals, and R.sub.2 is: ##STR2## where R.sub.3 is H or an alkali or alkaline-earth metal. The preparation of the derivatives and pharmaceutical compositions containing same are also disclosed.
A process according to the invention comprises reacting a compound of the formula ##STR3## with a hexose carbohydrate, in --OH protected form, in an aqueous medium, in the presence of a water-miscible organic solvent, in the presence of a base, the reaction product being optionally transformed into the derivative wherein R.sub.1 is a carbohydrate in the unprotected form by treatment with Lewis' acid or a hydrogen halide acid.
The compounds according to the invention are used in pharmaceutical compositions useful for treatment of infections by gram-positive and gram-negative pathogenous bacteria.

REFERENCES:
patent: 4025622 (1977-05-01), Ogura et al.
patent: 4041161 (1977-09-01), Kocsis et al.
patent: 4285940 (1981-09-01), Machida et al.
patent: 4285941 (1981-09-01), Machida et al.

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