2'-N-Acylated and 2'-N-alkylated derivatives of 4-O-substituted-2-deoxystreptamine aminoglycosides

Claim 1

A 2'-N-acylated or 2'-N-alkylated derivative of a 4-0-substituted-2-deoxystreptamine aminoglycoside selected from the group consisting of: apramycin, α or β-(C 1 to C 6 alkyl)aprosaminide, α or β-(C 2 to C 6 hydroxyalkyl)aprosaminide, α or β-(C 2 to C 6 aminoalkyl)aprosaminide, α or β-(C 2 to C 6 protected aminoalkyl)aprosaminide, α or β-(C 3 to C 6 aminohydroxyalkyl)aprosaminide, α or β-(C 3 to C 6 (protected amino)hydroxyalkyl)aprosaminide, and the pharmaceutically acceptable acid addition salts thereof; wherein the acyl or alkyl substituent group is selected from the group consisting of γ-amino-α-hydroxybutyryl, γ-protected amino-α-hydroxybutyryl, β-amino-α-hydroxypropionyl, β-protected amino-α-hydroxypropionyl, glycyl, N-protected glycyl, 3-hydroxypyrrolidine-3-carbonyl, N-protected 3-hydroxypyrrolidine-3-carbonyl, 3-hydroxyazetidine-3-carbonyl, N-protected 3-hydroxyazetidine-3-carbonyl, 2-hydroxy-2-(azetidin-3-yl)acetyl, N-protected 2-hydroxy-2-(azetidin-3-yl)acetyl, 4-amino-2-hydroxybutyl, 3-amino-2-hydroxypropyl, 2-aminoethyl, 3-hydroxypyrrolidine-3-methylene, 3-hydroxyazetidine-3-methylene, 2-hydroxy-2-(azetidin-3-yl)ethyl, C 2 to C 4 alkyl, C 3 to C 5 allyl, benzyl and substituted benzyl.