| 摘要 |
FIELD: chemistry.SUBSTANCE: invention relates to compounds of general formula IIIand their pharmaceutically acceptable salts, A represents (C-C)alkyl-O-, phenyl-(C-C)alkyl-O-; aryl, selected from phenyl, naphthyl,andwhich is possibly substituted by 1-3 substituents, given in the invention formula; or heteroaryl, which has four or five carbon atoms and one heteroatom, selected from oxygen, nitrogen and sulphur, which is possibly substituted by 1-3 substituents, given in the invention formula; B represents phenyl, possibly substituted by 1-3 substituents, where substituents are selected from (C-C)alkyl, (C-C)cycloalkyl, (C-C)alkyl-O-, hydroxy, amino and halogeno; and Rand Rindependently represent (C-C)alkyl, phenyl-(C-C)alkyl-, hydroxy-(C-C)alkyl, (C-C)cycloalkyl, (C-C)alkenyl or (C-C)alkynyl; on condition that Ris different from R; where absolute configuration of asymmetric Rand R-carrying carbon atom is mainly R-configuration. Invention also relates to pharmaceutical composition, possessing ability to modulate gene expression, methods of modulation of gene expression in host cell, method of regulating expression of endogenous or heterologous gene in transgenic subject, method of regulating transgenic expression in transgenic subject, method of polypeptide production and to method of obtaining formula IVcompound. Method includes stages: a) interaction of formula V compound with formula IV compound with obtaining formula VII compound; b) reduction of formula VII compound with obtaining formula VIII compound, b) interaction of formula VIII compound with formula B-CO-LG compound, where B has values, given above, and LG is leaving group representing -F, -Cl or -Br, with formation of formula IX compound, d) removal of group RCO- from formula IX compound with obtaining formula X compound, e) interaction of formula X compound with formula A-CO-LG compound, where A has values, given above, and LG is leaving group, representing -F, -Cl or -Br, with obtaining formula IV compound ( compounds of formulas V, VI, VII, VIII, IX, X are given in the invention formula).EFFECT: obtaining formula III compounds, possessing ability to modulate gene expression.19 cl, 4 ex, 2 tbl, 78 ex |
