RAPAMYCIN HYDROXYESTERS, METHOD OF THEIR SYNTHESIS AND METHODS OF TREATMENT Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new compounds of the formula (I) where each of R¹ and R² means independently hydrogen atom or -CO(CR³R⁴)_b(CR⁵R⁶)_dCR⁷R⁸R⁹ where each of R³ and R⁴ means independently hydrogen atom, alkyl with 1-6 carbon atoms; each of R⁵ and R⁶ means independently hydrogen atom, alkyl with 1-6 carbon atoms or R⁵ and R⁶ can form in common the group X or cycloalkyl ring with 3-8 carbon atoms; R⁷ means hydrogen atom, alkyl with 1-6 carbon atoms; each of R⁸ and R⁹ means independently hydrogen atom, alkyl with 1-6 carbon atoms, -(CR³R⁴)_fOR¹⁰ or R⁸ and R⁹ can in common form groups X or cycloalkyl ring with 3-8 carbon atoms; R¹⁰ means hydrogen atom, alkyl with 1-6 carbon atoms, tri (alkyl) with 1-6 carbon atoms silyl, tri (alkyl) with 1-6 carbon atoms silylethyl or tetrahydropyranyl; X means 5-[(2,2-di(alkyl] c 1-6 carbon atoms (1,3)-dioxanyl, 5-(2-spirocycloalkyl) with 3-8 carbon atoms (1,3)-dioxanyl, 4-[2,2-di(alkyl)] with 1-6 carbon atoms (1,3)-dioxanyl, 4-[2-spiro(cycloalkyl)] with 3-8 carbon atoms (1,3)-dioxanyl; b = 0-6; d = 0-6; f = 0-6 at condition that R¹ and R² are not hydrogen atom simultaneously and either R¹ or R² has at least one (CR³R⁴)_fOR¹⁰, X or cycloalkyl with 3-8 carbon atoms. Pharmaceutically acceptable salt of this compound is used as an immunosuppressive, anti-inflammatory, antifungal, antiproliferative and antitumor agent. Invention describes also a method of synthesis of compounds of the formula (I) showing immunosuppressive activity and a method of treatment of patients using compounds of the formula (I). EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 22 cl, 14 ex