Penem derivatives, their preparation and pharmaceutical composit

Details Penem derivatives, their preparation and pharmaceutical composit Penem derivatives, their preparation and pharmaceutical composit

1995-03-17

1998-05-05

Ford, John M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

540310, 540311, 514192, 514197, C07D499861, A61K 3143

Patent

active

057474834

ABSTRACT:
Penem derivatives of general formula (I), below, and pharmaceutically acceptable salts thereof are disclosed. ##STR1## wherein: R.sub.1 is H, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.7 cycloalkyl, or an optionally protected C.sub.1 -C.sub.6 hydroxyalkyl; R.sub.2 is a free or esterified carboxyl group or a carboxylate anion; R.sub.3 is H or C.sub.1 -C.sub.6 alkyl; R.sub.4 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 mercaptoalkyl, C.sub.1 -C.sub.6 aminoalkyl, C.sub.1 -C.sub.6 alkyl substituted by a quaternary ammonium group, C.sub.1 -C.sub.6 carboxyalkyl, cycloalkyl, aryl, arylalkyl, heterocyclyl-alkyl optionally substituted, saturated or unsaturated heterocycle, or R.sub.3 and R.sub.4 are linked together to form a heterocyclic ring having 3-7 atoms; R.sub.5 and R.sub.6 independently are H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 mercaptoalkyl, C.sub. -C.sub.6 aminoalkyl, alkenyl, cycloalkyl, aryl, arylalkyl, alkylaryl, heterocyclyl-alkyl, C.sub.1 -C.sub.6 alkyl carboxyamide, or R.sub.5 and R.sub.6 are taken together to form a heterocyclic ring having 3-7 atoms, and n is an intiger from 1 to 3.

REFERENCES:
Perrone et al., Chemical Abstracts, vol. 105, entry 60470 (1986).
C.S. Marvel et al., The Structure of Urea-Formaldehyde Resins, Sep. 17, 1946, Journal of the American Chemical Society, vol. 68, No. 9. 22101 and FCE 22891), Journal of Labelled Compounds and Radiopharmaceuticals, vol. XXIV, No. 1, 1987.
A.J. Corraz, et al., Dual-Action Penems and Carbapenems, J. Med. Chem. 1992, 35, 1828-1839.

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