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1.发明授权NEW 3-DECLADINOSYL 9a-N -CARBAMOYL AND 9a-N -THIOCARBAMOYL DERIVATIVES OF 9-DEOX-9-DIHYDRO-9a-AZA-9A-HOMOERYTHROMYCIN A 有权9-脱氧-9-二氢-9a-AZA-9A-异黄嘌呤霉素A的新的3-脱氨酰基9a-N-氨基甲酰基和9a-N-氨基甲酰氨基甲酸衍生物
公开(公告)号：EP1631575B1
公开(公告)日：2006-11-02
申请号：EP04732143.5
申请日：2004-05-11
CPC分类号： C07H17/08
摘要： The present invention relates to the new 3-decladinosyl derivatives of 9a-N-carbamoyland 9a-N-thiocarbamoyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin A of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, Wherein R1 individually stands for hydrogen or together with R2 stands for double bond, R2 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein Y individually stands for monocyclic aromatic ring, unsubstituted or substituted with groups which are selected independently from halogen, OH, OMe, NO2, NH2 or R2 together with R3 stands for ketone or together with R1 stands for double bond, R3 individually stands for hydrogen or together with R2 stands for ketone or together with R4 stands for ether, R4 individually stands for hydroxyl, a OCH3 group or together with R3 stands for ether, R5 individually stands for C1-C4 alkyl group, C2-C4 alkenyl group, -(CH2)m Ar, wherein Ar individually stands for phenyl or phenyl substituted with one or two groups which are selected independently from halogen or halogen alkyl, and m is 0-3, R6 individually stands for hydrogen or hydroxyl protected group, X stands for oxygen or sulphur, to intermediates for synthesis of other macrolide compounds with antibacterial activity, to the process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to the process for the preparation of pharmaceutical compositions, as well as the use of pharmaceutical compositions for treating bacterial infections.
摘要翻译： 本发明涉及通式（I）的9a-N-氨基甲酰基-9a-N-硫代氨基甲酰基-9-脱氧-9-二氢-9a-氮杂-9a-高红霉素A的新的3-脱氢紫核糖衍生物，它们的药学上可接受的 其中R 1独立地代表氢或与R 2一起代表双键，R 2分别代表氢，羟基或式（II）的基团，其中Y独立代表单环芳香族基团 环，未被取代或被独立选自卤素，OH，OMe，NO 2，NH 2或R 2的基团取代，连同R 3代表酮或与R 1一起代表双键，R 3单独代表氢或与R 2一起代表酮 或者与R4一起代表醚，R4分别代表羟基，OCH3基团或与R3代表醚，R5分别代表C1-C4烷基，C2-C4链烯基， - （CH2）mAr，其中Ar individ 表示苯基或被一个或两个独立地选自卤素或卤素烷基的基团取代的苯基，m为0-3，R6分别代表氢或羟基保护基团，X代表氧或硫，用于合成中间体 的具有抗菌活性的其它大环内酯化合物，其制备方法，其与无机或有机酸及其水合物的药学上可接受的加成盐，制备药物组合物的方法，以及药物组合物用于治疗 细菌感染。
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