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1. 发明授权

US6077944A Secomacrolides from class of erythromycins and process for their preparation 失效
标题翻译：来自红霉素类的重庆霉素及其制备方法
公开(公告)号：US6077944A
公开(公告)日：2000-06-20
申请号：US38901
申请日：1998-03-12
申请人： Gorjana Lazarevski , Gabrijela Kobrehel , Amalija Narandja , Zrinka Banic-Tomisic
发明人： Gorjana Lazarevski , Gabrijela Kobrehel , Amalija Narandja , Zrinka Banic-Tomisic
IPC分类号： C07H17/08 , A61K31/70 , A61K31/7048 , C07H15/04 , C07H15/26 , C07H1/00 , C07H15/00
CPC分类号： C07H15/04 , C07H15/26
摘要： The invention relates to novel secomacrolides from the class of erythromycin A, potential intermediates for preparation of novel macrolide antibiotics general formula ##STR1## and its pharmaceuticaly acceptable addition salts with inorganic or organic acids, wherein R.sub.1 represents hydrogen, C.sub.1 -C.sub.4 alkanoyl group, arylcarbonyl group and together with R.sub.2 and carbon atoms to which they are bound, cyclic carbonyl or thiocarbonyl group, R.sub.2 represents hydrogen or together with R.sub.1 and carbon atoms to which they are bound, cyclic carbonyl or thiocarbonyl group, R.sub.3 represents hydrogen, C.sub.1 -C.sub.4 alkanoyl or arylcarbonyl group,Z is hydrogen or L-cladinosyl group represented by formula (i) ##STR2## wherein R.sub.4 represents hydrogen or C.sub.1 -C.sub.4 alkanoyl group, W is hydrogen or D-desosaminyl group represented by formula (ii) ##STR3## wherein R.sub.5 represents hydrogen or C.sub.1 -C.sub.4 alkanoyl or arylcarbonyl group,X and Y together represent a lactone, or X is CH.sub.2 OR.sub.6, wherein R.sub.6 represents hydrogen or C.sub.1 -C.sub.4 alkanoyl group and Y is hydroxyl group.
摘要翻译：本发明涉及来自红霉素A类的新型次氯氰菊酯，用于制备新型大环内酯类抗生素通用型的潜在中间体及其与无机或有机酸的药学上可接受的加成盐，其中R1表示氢，C1-C4烷酰基，芳基羰基和一起 R 2和它们所连接的碳原子，环状羰基或硫代羰基，R 2表示氢或与它们所连接的R 1和碳原子一起，环状羰基或硫代羰基，R 3表示氢，C 1 -C 4烷酰基或芳基羰基 Z为氢或由式（ⅰ）表示的L-克拉糖糖基，其中R 4表示氢或C 1 -C 4烷酰基，W为氢或式（ⅱ）表示的D-脱氨基甲酰基，其中R 5表示氢或C 1 -C 4烷酰基或芳基羰基，X和Y一起表示内酯，或X是CH 2 OR 6，其中R 6表示氢或C 1 -C 4烷酰基，Y是羟基。

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