DERIVATIVES OF CARBAPENEM, THEIR USING FOR PREPARING PHARMACEUTICAL COMPOSITION, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD FOR TREATMENT AND/OR PROPHYLAXIS OF INFECTIOUS DISEASES Russian patent published in 2006 - IPC C07D519/06 A61K31/431 A61P31/04 

FIELD: organic chemistry, antibiotics, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of carbapenem possessing high antibiotic activity with respect to methicillin-resistant microorganism Staphylococcus aureus, penicillin-resistant microorganism Streptococcus pneumoniae, influenza virus and microorganisms producing β-lactamase, and showing stability with respect to renal dehydropeptidase. Proposed derivatives of carbapenem represent compounds of the formulae (I) and (II) or their pharmaceutically acceptable salts wherein R¹ represents hydrogen atom or methyl; each R² and R³ represents independently hydrogen, halogen atom, carbamoyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylthio-group or formyl; n = 0-4; Hy represents 4-7-membered monocyclic or 9-10-bicyclic saturated or unsaturated heterocyclic group comprising 1-4 heteroatoms chosen from the group consisting of nitrogen and sulfur atoms wherein Hy group can be optionally substituted with halogen atom; substituted or unsubstituted lower alkyl, (lower alkyl)-thio-group, (lower alkyl)-sulfonyl, carboxyl, amino-group, aryl; or 6-membered monocyclic heterocyclic group comprising one or some nitrogen atoms. Also, invention describes the methods for treatment and/or prophylaxis of infectious diseases caused by gram-positive and gram-negative microorganisms that involve administration of indicated derivative of carbapenem in therapeutically and/or prophylactically effective doses to mammals including humans.

EFFECT: improved method for treatment and prophylaxis, valuable medicinal properties of derivatives.

22 cl, 2 tbl, 73 ex