ANTIBACTERIAL AGENT

摘要

1340615 Kasugamycin derivatives BRISTOLMYERS CO 3 May 1971 [1 May 1970] 12811/71 Heading C2A Novel kasugamycin derivatives having the Formula (XI) wherein R7 is hydrogen or -OH; R is 2-, 3- or 4-pyridyl or 2,- 3- or 4-piperidyl, and Y is hydrogen or a ketonic residue of the formula in which R3 and R4 are alike or different and each is hydrogen or C 1 -C 8 alkyl, and salts thereof, are prepared by either (a) reacting a compound having the Formula (III) wherein Z is one of the aforesaid ketonic residues, with an imidate of formula in which R is as defined above and R1 is C 1 -C 8 alkyl, or an acid-addition salt thereof, to produce a compound (IV) having the aforesaid Formula XI wherein R7 is hydrogen, R is as defined above and Y is one of the said ketonic residues, and then if desired subjecting the compound (IV) to treatment with bromine water to replace the ketonic residue by hydrogen, and/or to hydrogenation to convert pyridyl to piperidyl; or (b) reacting a compound (III) as defined above, with an aldoxime halide of formula in which R is as defined above and X is Cl, Br or I, to give a compound (VII), having the aforesaid Formula XI wherein R is as before, R7 is -OH and Y is one of the said ketonic residues, and then if desired treating this compound with bromine water and/or by hydrogenation to replace the ketonic residue by hydrogen, and to convert pyridyl to piperidyl and the oxime group to an amine group (i.e. the compound where R7 is -OH to the compound where R7 is hydrogen). Pharmaceutical compositions having antibacterial activity comprise a kasugamycin antibiotic of Formula XI above or a non-toxic acid-addition salt thereof together with a pharmaceutically acceptable carrier. Reference has been directed by the Comptroller to Specifications 1,094,566 and 1,244,026.