| 摘要 |
The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-9a-aza9a-homoerythromycin A 9a,11-cyclic carbamate of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, wherein R<SUB>1 </SUB>individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C<SUB>1</SUB>-C<SUB>6</SUB>alkyl group, C<SUB>2</SUB>-C<SUB>6</SUB>alkenyl group or X individually stands for C<SUB>1</SUB>-C<SUB>6</SUB>alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH<SUB>2</SUB>)<SUB>n</SUB>-Ar or X individually stands for (CH<SUB>2</SUB>)<SUB>n</SUB>-heterocycloalkyl, wherein (CH<SUB>2</SUB>)<SUB>n </SUB>individually stands for alkyl, wherein n is 1-10, with or without incorporated atom O, S or N, wherein Ar individually stands for 5-10-membered monocyclic or bycyclic aromatic ring with 0-3 atom O, S or N, unsubstituted or substituted with 1-3 group, which are selected independently from halogen, OH, OMe, NO<SUB>2</SUB>, NH<SUB>2</SUB>, amino-C<SUB>1</SUB>-C<SUB>3</SUB>alkyl or amino-C<SUB>1</SUB>-C<SUB>3</SUB>dialkyl, CN, SO<SUB>2</SUB>NH<SUB>2</SUB>, C<SUB>1</SUB>-C<SUB>3</SUB>alkyl, and heterocycloalkyl stands for unaromatic, partially or completely saturated 3-10-membered monocyclic or bicyclic ring system, which includes 3-8-membered monocyclic or bicyclic ring, which includes 6-membered aromatic or heteroaromatic ring connected with a unaromatic ring with or without incorporated O, S or N atom, unsubstituted or substituted with 1-4 group, which are selected independently from halogen, OH, OMe, NO<SUB>2</SUB>, NH<SUB>2</SUB>, amino-C<SUB>1</SUB>-C<SUB>3</SUB>alkyl or amino-C<SUB>1</SUB>-C<SUB>3</SUB>dialkyl, CN, SO<SUB>2</SUB>NH<SUB>2</SUB>, C<SUB>1</SUB>C<SUB>3</SUB>alkil, -C(O)-, COOH or R<SUB>1 </SUB>together with R<SUB>2 </SUB>stands for ketone, R<SUB>2 </SUB>individually stands for hydrogen or together with R<SUB>1 </SUB>stands for ketone or together with R<SUB>3 </SUB>stands for ether, R<SUB>3 </SUB>individually stands for hydroxyl, a group of the formula -OX or together with R<SUB>2 </SUB>stands for ether, R<SUB>4 </SUB>individually stands for hydrogen, C<SUB>1</SUB>-C<SUB>4</SUB>alkyl group or C<SUB>2</SUB>-C<SUB>4</SUB>alkenyl group, and R<SUB>5 </SUB>individually stands for hydrogen or hydroxyl protected group, 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 |
