ERYTHROMYCIN DERIVATIVES, PHARMACEUTICAL COMPOSITION ON THEIR BASIS, METHOD OF THEIR PREPARATION AND INTERMEDIATES Russian patent published in 1999 - IPC

FIELD: pharmaceutical chemistry. SUBSTANCE: erythromycin derivatives with general formula I: (I) are provided, in which formula R is (CH₂)_nAr₁, where n is integer from 0 to 6 and Ar₁ is (i) carbocyclic C_1-18-aryl group optionally substituted by carboxyl group (free, salt, ester, or amide), halogen, nitro group, C_1-12-alkyl, or C_1-12-alkoxy and (ii) 5- or 6-membered heterocyclic aryl group containing 1-2 endocyclic heteroatoms (N or S); or R is group XAr₂, wherein X is C_1-6-alkyl interrupted by group NH-CO- and Ar₂ is as defined above for Ar₁; Z is hydrogen or carbocyclic acid radical containing up to 18 carbon atoms. Claimed are also pharmaceutically acceptable salts of compounds I with acids. EFFECT: increased antimicrobial activity with respect to gram(+) bacteria such as staphylococci and pneumococci. 21 cl, 5 dwg, 50 ex