发明名称 RAPAMYCIN HYDROXYESTERS, METHOD OF THEIR SYNTHESIS AND METHODS OF TREATMENT
摘要 FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new compounds of the formula (I) where each of R and R means independently hydrogen atom or -CO(CR<SP>3</SP>R<SP>4</SP>)<SB>b</SB>(CR<SP>5</SP>R<SP>6</SP>)<SB>d</SB>CR<SP>7</SP>R<SP>8</SP>R where each of R and R means independently hydrogen atom, alkyl with 1-6 carbon atoms; each of R and R means independently hydrogen atom, alkyl with 1-6 carbon atoms or R and R can form in common the group X or cycloalkyl ring with 3-8 carbon atoms; R means hydrogen atom, alkyl with 1-6 carbon atoms; each of R and R means independently hydrogen atom, alkyl with 1-6 carbon atoms, -(CR<SP>3</SP>R<SP>4</SP>)<SB>f</SB>OR or R and R can in common form groups X or cycloalkyl ring with 3-8 carbon atoms; R 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 R and R are not hydrogen atom simultaneously and either R or R has at least one (CR<SP>3</SP>R<SP>4</SP>)<SB>f</SB>OR , 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
申请公布号 RU2134267(C1) 申请公布日期 1999.08.10
申请号 RU19960122172 申请日期 1995.04.14
申请人 AMERIKAN KHOUM PRODAKTS KORPOREJSHN 发明人 DZHERAL'D STENLI SKOTNITSKI;KRISTINA LUIZA LEON;GAJ ALAN SHIZER
分类号 C07D487/18;A61K31/435;A61K31/436;A61P9/00;A61P9/10;A61P11/00;A61P19/02;A61P29/00;A61P31/00;A61P31/04;A61P31/10;A61P35/00;A61P37/06;C07D498/18;(IPC1-7):C07D487/18;A61K31/44;A61K31/71 主分类号 C07D487/18
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