Penam derivatives and salts thereof, processes for producing...

C - Chemistry – Metallurgy – 07 – D

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C07D 499/21 (2006.01) A61K 31/43 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) C07D 499/00 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2019260

A penam derivative represented by the following general formula or a salt thereof: (see fig. I) wherein R1 represents a hydrogen atom, an amino-protecting group or an acyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 represents a hydrogen atom, a lower alkoxy group, a lower alkylthio group or a formamido group; R4 represents a protected or unprotected carboxyl group or a carboxylato group; R represents a group of the formula, -NHR5 or -NR5R6 (in which R5 and R6, which may be the same or different, represent protected or unprotected hydroxyl groups, cyano groups, sulfo groups, or unsubstituted or substituted lower alkyl, aryl, acyl, carbamoyl, sulfamoyl, lower alkylsulfonyl or heterocyclic groups) or a group of the formula, -N=CR7R8 (in which R7 and R8, which may be the same or different, represent hydrogen atoms or protected or unprotected carboxyl groups, cyano groups or unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl, aryl, amino, acyl, acyloxy, carbamoyl, carbamoyloxy, sulfamoyl, lower alkylthio, ureido or heterocyclic groups, or R7 and R8 may form a cycloalkene or a heterocyclic ring with the carbon atom to which R7 and R8 are attached); and n represents 1 or 2. The above penam derivative or its salt is very effective as antibacterial agents.

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