FIELD: antibiotics, pharmacy. SUBSTANCE: invention describes the novel derivatives of rapamycin of the formula (I) where R1 means C1-C10-alkyl, C3-C10-alkynyl, C3-C10-hydroxyalkynyl; R2 is taken among of the formula (II) where R3 is taken among of H, C1-C6-alkyl, hydroxy-C1-C6-alkyl or C1-C6-alkoxy-C1-C6- -alkyl; R4 means H or methyl and X means OH or H under condition that if X means OH then R1 means C1-C6-alkyl and R2 means residue of the formula (II) and in this case R3 is not H. Compounds of the formula (I) show immunosuppressive activity. Invention describes also pharmaceutical composition based on thereof. EFFECT: new rapamycin derivatives indicated above, valuable medicinal properties. 6 cl, 6 ex
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