NEW DERIVATIVES OF 3-DECLADINOSIL OF 9A, 11-CYCLIC CARBAMATES OF 9-DESOXO-9-DIHIDRO-9A-AZA-9A-HOMOERITROMICINA A.

摘要

3-decladinosyl derivatives of 9a, cyclic 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin A of cyclic A of general formula (I), ** see formula ** its pharmaceutically acceptable addition salts with acids inorganic or organic and their hydrates, where R 1 individually represents hydrogen, hydroxyl or a group of formula (II), ** see formula ** X individually represents a C1-C6 alkyl group, C2-C6 alkenyl or X individually represents a C1-C6 alkyl group with at least one incorporated O, S or N atom or X individually represents (CH2) n-Ar or X individually represents (CH 2) n-heterocycloalkyl, where (CH 2) n individually represents alkylene, where n is 1-10, with or without an incorporated O, S or N atom, where Ar individually represents a 5-10 membered monocyclic or bicyclic aromatic ring with 0-3 O, S or N atoms, not substituted or substituted with 1 -3 groups, independently selected from halogen, OH, OMe, NO2, NH2, amino-alkyl C1-C3-yl or C1-C3-amino-di-alkyl, CN, SO2NH2, C1-C3 alkyl, and heterocycloalkyl represents a non-aromatic monocyclic or bicyclic ring system, partially or completely saturated, from 3 to 10 members, which includes a 3-8-membered monocyclic or bicyclic ring, which includes a 6-membered aromatic or heteroaromatic ring connected to a non-aromatic ring with or without an incorporated O, S or N atom, unsubstituted or substituted with 1-4 independently selected groups between halogen, OH, OMe, NO2, NH2, amino-C1-C3 alkyl or amino-di-C1-C3 alkyl, CN, SO2NH2, C1-C3 alkyl, -C (O) -, COOH or R1 together with R2 represents ketone, R 2 individually represents hydrogen or together with R 1 represents ketone or together with R 3 represents ether, R3 individually represents hydroxyl, a group of formula -OX or together with R2 represents ether, R 4 individually represents hydrogen, a C alkyl group 1-C 4 or a C 2 -C 4 alkenyl group, and R5 individually represents a protected hydrogen or hydroxyl group.