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
individually stands for hydrogen, hydroxyl or a group of the formula
(II), wherein X individually stands for C.sub.1-C.sub.6alkyl group,
C.sub.2-C.sub.6alkenyl group or X individually stands for
C.sub.1-C.sub.6alkyl group with at least one incorporated O, S or N atom
or X individually stands for (CH.sub.2).sub.n--Ar or X individually
stands for (CH.sub.2).sub.n-heterocycloalkyl, wherein (CH.sub.2).sub.n
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, NH.sub.2,
amino-C.sub.1-C.sub.3alkyl or amino-C.sub.1-C.sub.3dialkyl, CN,
SO.sub.2NH.sub.2, C.sub.1-C.sub.3alkyl, 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, NH.sub.2,
amino-C.sub.1-C.sub.3alkyl or amino-C.sub.1-C.sub.3dialkyl, CN,
SO.sub.2NH.sub.2, C.sub.1C.sub.3alkil, --C(O)--, COOH or R.sub.1 together
with R.sub.2 stands for ketone, R.sub.2 individually stands for hydrogen
or together with R.sub.1 stands for ketone or together with R.sub.3
stands for ether, R.sub.3 individually stands for hydroxyl, a group of
the formula --OX or together with R.sub.2 stands for ether, R.sub.4
individually stands for hydrogen, C.sub.1-C.sub.4alkyl group or
C.sub.2-C.sub.4alkenyl group, and R.sub.5 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
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