PENEM DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

Described are penems derivatives of general formula (I) wherein R1 is chosen in the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, C3-C7 cycloalkyl, optionally protected C1-C6 hydroxyalkyle; R2 is chosen in the group consisting of carboxyl group free or esterified with a group easily activated 'in vivo', carboxylate anion; R3 is chosen in the group consisting of H, C1-C4 alkyl optionally substituted; R4 is chosen in the group consisting of: H, C1-C6 alkyl optionally substituted, C1-C6 hydroxyalkyl optionally substituted, C1-C6 mercaptoalkyl optionally substituted, C1-C6 aminoalkyl optionally substituted, C1-C6 alkyl substituted by a quaternary ammonium group, C1-C6 carboxyalkyl optionally substituted, cycloalkyl, aryl, arylalkyl, heterocyclyl-alkyl optionally substituted, saturated or unsaturated heterocycle wherein the heteroatoms in the heterocyclic ring can be N, O, S, or R3 and R4 linked together form a heterocyclic ring having 3-7 atoms, optionally substituted, saturated or unsaturated which can contain other heteroatoms as O, N, S. R5 and R6 independently from one another are chosen in the group consisting of: H, C1-C6 alkyl, C1-C6 hydroxyalkyl, C1-C6 mercaptoalkyl, C1-C6 aminoalkyl, alkenyl, cycloalkyl, aryl, arylalkyl, alkylaryl, heterocyclyl-alkyl, C1-C6 alkyl carboxyamide wherein the alkyl group can be linear or branched (all these groups optionally substituted), or R5 and R6 taken together form an heterocyclic ring having 3-7 atoms optionally substituted, n is chosen in the group consisting of: 1, 2, 3; and their pharmaceutically acceptable salts.