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New 15-spinal ketoasalides, method of manufacture and pharmaceutical composition containing these for bacterial infections

机译:新的15-螺旋酮基内酰胺类药物,其制备方法和包含它们的药物组合物,用于细菌感染

摘要

The present invention relates to the new 15-membered ketoazalides from the class of 6-O-methyl-8a-aza-8a-homo-and 6-O-methyl-9a-aza-9a-homoerythromycin A with the general formula (I) wherein A represents NH group and B at the same time represents C=O group, or A represents C=O group and B at the same time represents NH group, R1 represents OH group, L-cladinosyl group of the formula (II) or together with R2 represents ketone, R2 represents hydrogen or together with R1 represents ketone, R3 represents hydrogen or C1-C4alkanoyl group, to intermediates and a process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to the process for the preparation of pharmaceutical compositions, as well as to the use of pharmaceutical compositions for treating bacterial infections.
机译:本发明涉及具有通式(I)的6-O-甲基-8a-氮杂-8a-同型和6-O-甲基-9a-氮杂-9a-同型红霉素A的新的15元酮氮杂化物)其中A代表NH基团,B同时代表C = O基团,或A代表C = O基团,B同时代表NH基团,R1代表OH基团,式(II)的L-cladinosyl基团或与R2一起代表酮,R2代表氢或与R1代表酮,R3代表氢或C1-C4烷酰基,作为中间体及其制备方法,以其与无机或有机酸的药学上可接受的加成盐,用于制备药物组合物,以及用于治疗细菌感染的药物组合物的用途。

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