发明名称 ANALOGS OF VITAMIN <EMI ID=0.688 HE=60 WI=63 TI=CHI>, METHODS OF THEIR SYNTHESIS, A PHARMACEUTICAL COMPOSITION AND A METHOD OF TREATMENT
摘要 FIELD: vitamins. SUBSTANCE: invention relates to the unknown class of compounds showing antiinflammatory and immunomodulating effects, drugs containing these compounds, method of patients treatment and a method of synthesis of the above indicated compounds. Invention proposes compounds of the formula (I) where V is a group -(CH&lt;SB&gt;2&lt;/SB&gt;)&lt;SB&gt;n&lt;/SB&gt;-Y-(CH&lt;SB&gt;2&lt;/SB&gt;)&lt;SB&gt;m&lt;/SB&gt;; n = 0, 1 or 2; m = 1 or 2; Y is oxygen or sulfur atom. 22-Methylene- or 23-methylene-group can be replaced for oxygen atom or 22- or 23-methylene-group can be replaced for a group -CH= CH-; &lt;EMI ID=0.689 HE=3 WI=3 TI=CHI&gt; is methyl- or ethyl-group and carbon atom directly bound with C-25 atom can be substituted with one or some fluorine atoms; hydroxy-groups can be substituted by groups that can be split at in vivo conditions. Method of synthesis of compounds of the formula (I) where hydroxy-group is modified involves interaction with tert.-butylbromoacetate in the presence of a base and catalyst in a solvent followed by interaction of synthesized ester with methyl- or ethylmagnesium halide. Obtained compound is subjected for isomerization at any sequence by effect of UV-light in the presence of triplet activator and removal of silyl-groups by treatment with tetra-n-butylammonium fluoride of hydrogen fluoride and producing a compound of the formula (I) where Y and V - oxygen atom. Method of prophylaxis and treatment of patients with pathological states using D&lt;SB&gt;º&lt;/SB&gt;- -vitaminotherapy involves administration of a pharmaceutical composition containing an effective dose of compound of the formula (I). EFFECT: improved method of synthesis, enhanced effectiveness of compounds synthesized. 8 cl, 2 tbl, 10 ex
申请公布号 RU2128168(C1) 申请公布日期 1999.03.27
申请号 RU19950113157 申请日期 1993.11.01
申请人 LEO FARMAS'JUTIKAL PRODAKTS LTD, A/S 发明人 MARTIN DZHON KEHLVERLI;KHENRIK PEDERSEN
分类号 A61K31/59;A61K31/593;A61P5/12;A61P9/12;A61P11/00;A61P17/00;A61P29/00;A61P37/00;A61P43/00;C07C401/00;(IPC1-7):C07C401/00 主分类号 A61K31/59
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