TYLOSIN DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

Antibiotic tylosin derivatives shown by the general formula

wherein R1 represents a hydroxyl group; a halogen atom;

[wherein R5 represents a hydrogen atom or a C1 to C6 alkyl group which may be substituted by a hydroxyl group and R6 represents a hydrogen atom, a C1 to C6 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)m-R7 (wherein m represents 0 or 1 and R7 represents a C1 to C6 alkyl group, an aryl group, an aralkyl group, a furanyl group or a pyridyl group), or -CH2-R13 (wherein R13 represents a mono-, di-, or trifluoromethyl group)];

(wherein n represents an integer of 2-15) which maybe substituted by an oxo group, a hydroxyl group, a C1 to C6 alkyl group, or a hydroxy C1 to C6 alkyl group; an imidazolyl, morpholino, or piperazino group which may each be substituted by a C1 to C6 alkyl group; or -OOCCH2-R8 [wherein R8 represents

(wherein R9 and R10 may be the same or different and selected from a hydrogen atom and C1 to C6 alkyl groups or which may together form an alkylene group having 3-7 carbon atoms) or -S-R11 (wherein R11 represents a furanyl group or a pyridyl group)]; R2 represents a hydrogen atom or a C1 to C6 alkanoyl group; R3 represents a methyl or -CH2CHO group; R4 represents a hydrogen atom or a hydroxyl group; A represents O=,

line @ represents a single bond or a double bond; and and line @ represent a single bond, a double bond, or @; provided that when R1 is a hydroxyl group, R3 is a methyl group and R4 is a hydrogen atom, or said line @ is @; and that when R1 is a halogen atom, R3 is a methyl group or said line @ is @.