Tylosin derivatives, their preparation and pharmaceutical compositions

Abstract

Tylosin compounds of the formula ##STR1## wherein R.sub.1 represents a hydroxyl group; a halogen atom; ##STR2## group (wherein R.sub.5 is a hydrogen atom or a lower alkyl group which may be substituted by a hydroxyl group and R.sub.6 is a hydrogen atom, a lower alkyl group which may be substituted by a hydroxyl group, an aryl group, an aralkyl group, a cycloalkyl group having 3-10 carbon atoms, --CO(O).sub.m --R.sub.7 group (wherein m is 0 or 1 and R.sub.7 is a lower alkyl group, an aryl group, an aralkyl group, a furanyl group, or a pyridyl group), or --CH.sub.2 --R.sub.13 group (wherein R.sub.13 is a mono-, di-, or trifluoromethyl group)); --N(CH.sub.2).sub.n group (wherein n is an integer of 2-15) which may be substituted by an oxo group, a hydroxyl group, a lower alkyl group, or a hydroxy lower alkyl group; an imidazolyl group, a morpholino group, or a piperazino group each may be substituted by a lower alkyl group; or --OOCCH.sub.2 --R.sub.8 group (wherein R.sub.8 is ##STR3## group (wherein R.sub.9 and R.sub.10, which may be the same or different, each is a hydrogen atom or a lower alkyl group; said R.sub.9 and R.sub.10 may be combined with each other to form an alkylene group having 3-7 carbon atoms) or --S--R.sub.11 group (wherein R.sub.11 is a furanyl group or a pyridyl group)); R.sub.2 represents a hydrogen atom or a lower alkanoyl group; R.sub.3 represents a methyl group or --CH.sub.2 CHO group; R.sub.4 represents a hydrogen atom or a hydroxyl group; A represents 0.dbd., ##STR4## line represents a single bond or a double bond; and line ---- represents a single bond, a double bond, or ; however, when said R.sub.1 is a hydroxyl group, said R.sub.3 is a methyl group and R.sub.4 is a hydrogen atom, or said line ---- is ; or when said R.sub.1 is a halogen atom, said R.sub.3 is a methyl group of said line ---- is . The foregoing compounds of this invention are useful as antibiotics.