发明授权
EP1631575B1 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
- 专利标题: NEW 3-DECLADINOSYL 9a-N -CARBAMOYL AND 9a-N -THIOCARBAMOYL DERIVATIVES OF 9-DEOX-9-DIHYDRO-9a-AZA-9A-HOMOERYTHROMYCIN A
- 专利标题(中): 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
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申请号: EP04732143.5申请日: 2004-05-11
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公开(公告)号: EP1631575B1公开(公告)日: 2006-11-02
- 发明人: MARUSIC ISTUK, Zorica , KUJUNDZIC, Nedjeljko , MUTAK, Stjepan
- 申请人: GlaxoSmithKline istrazivacki centar Zagreb d.o.o.
- 申请人地址: Prilaz Baruna Filipovica 29 10000 Zagreb HR
- 专利权人: GlaxoSmithKline istrazivacki centar Zagreb d.o.o.
- 当前专利权人: GlaxoSmithKline istrazivacki centar Zagreb d.o.o.
- 当前专利权人地址: Prilaz Baruna Filipovica 29 10000 Zagreb HR
- 代理机构: von Füner, Nicolai
- 优先权: HR20030381 20030514
- 国际公布: WO2004101591 20041125
- 主分类号: C07H17/08
- IPC分类号: C07H17/08 ; A61K31/70 ; A61P31/04
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.
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