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发明公开
CN101899076A 阿奇霉素衍生物、制备方法及中间体 失效 - 权利终止

阿奇霉素衍生物、制备方法及中间体
摘要：
本发明公开了一种式(Ⅰ)表示的阿奇霉素衍生物或其药学上可接受的盐：其中，R1代表氢、乙酰基或苯甲酰基；R2代表氢、脂肪烃基、取代芳香烃基、取代芳杂环烃基、卤素、硝基、烷氧基或-AR7；R3代表OR5，R4代表羟基；或者：R3和R4形成具有如下结构的环：X代表氧、氮；R5代表氢或CONHR6；R6代表脂肪烃基、取代芳香烃基或取代芳杂环烃基；R7代表脂肪烃基、取代芳香烃基或取代芳杂环烃基；n为1～6；A为-O-，-CO-，-CONR8-，-NHCO-，-S-中的任一种。本发明还涉及其制备的中间产物及方法、涉及其与无机或有机酸形成的可接受的加成盐、涉及药物组合物及其用于治疗细菌感染的用途。
摘要（英）：

The invention discloses an azithromycin derivative shown in the formula (I) and a pharmaceutically acceptable salt thereof, wherein R1 represents hydrogen, acetyl or benzoyl, R2 represents hydrogen, aliphatic hydrocarbon, substituted aromatic alkyl, substituted aromatic heterocyclic alkyl, halogen, nitryl, alkoxy or-AR7, R3 represents OR5, R4 represents hydroxyl; or, R3 and R4 can form a ring with a structure that X represents oxygen and nitrogen; R5 represents nitrogen or CONHR6, R6 represents aliphatic hydrocarbon, substituted aromatic alkyl or substituted aromatic heterocyclic alkyl, and R7 represents aliphatic hydrocarbon, substituted aromatic alkyl or substituted aromatic heterocyclic alkyl; n is from 1 to 6, A is one of -O-,-CO-,-CONR8-,-NHCO- and -S-. The invention further relates to a prepared intermediate and a method thereof, an acceptable salt thereof forming with inorganic or organic acid, a drug composite and application thereof in the treatment of bacterial infection.

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