1-methylcarbapenem derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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540350, A61K 3140, C07D48704

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active

059770970

ABSTRACT:
A 1-methylcarbapenem compound represented by the following formula: ##STR1## [wherein R.sup.1 represents a hydrogen atom or a lower alkyl group, R.sup.2 represents a hydrogen atom or a lower alkyl group, R.sup.3 represents a hydrogen atom, a lower alkyl group, a lower alkyl group which has a substituent, a cycloalkyl group or a group of formula --C(.dbd.NH)R.sup.4 (in which R.sup.4 represents a hydrogen atom, a lower alkyl group or an amino group)]; or a pharmacologically acceptable salt or derivative thereof. The 1-methylcarbapenem compounds of the present invention exhibit excellent antibacterial activity and are therefore effective as a preventive or remedy of infections.

REFERENCES:
patent: 5122604 (1992-06-01), Sunagawa et al.
patent: 5712267 (1998-01-01), Kawamoto et al.
Kropp et al "Metabolism of Thienamycin and Related Carbapenem Antibiotics by the Renal Dipeptidase, Dehydropeptidase-1", Antimicrobial Agents and Chemotherapy, vol. 22, No. 1, pp. 62-70 (1982).
Norrby et al "Urinary Recovery of N-Formimidoyl Thienamycin (MK0787) as Affected by Coadministration of N-Formimidoyl Thienamycin Dehydropeptidase Inhibitors", Antimicrobial Agents and Chemotherapy, vol. 23, No. 2, pp. 300-307 (1983).
Kawamoto et al "A Convenient Synthesis of Versatile Side-chain Intermediates for Carbapenem Antiobiotics", Synlett, pp. 575-577 (1995).

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