DERIVATIVES OF INDOLE-3-YL Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of indol-3-yl of the formula (I):

wherein each A and B represents independently of one another oxygen atom (O), NH, CONH, NHCO or a direct bond; X means (C₁-C₂)-alkylene or a direct bond; R¹ means hydrogen atom (H); R² means hydrogen atom (H); R³ means NHR⁶, -NR⁶-C(=NR⁶)-NHR⁶, -C(=NR⁶)-NHR⁶, -NR⁶-C(=NR⁹)-NHR⁶, -C(=NR⁹)-NHR⁶ or Het¹; each R⁴ and R⁵ represents independently of one another hydrogen atom (H); R⁷ means -(CH₂)_o-Ar, Het, OR⁶; R⁶ means hydrogen atom (H); R⁷ means (C₁-C₁₀)-alkyl, (C₃-C₁₀)-cycloalkyl; R⁸ means Hal, NO₂ (nitro-group), CN (cyano-group), Z, -(CH₂)_o-Ar, COOR¹, OR¹, CF₃, OCF₃, NHR¹; R⁹ means CN or NO₂; Z means (C₁-C₆)-alkyl; Ar means aryl that can represent unsubstituted, monosubstituted, or polysubstituted R⁸; Hal means F, Cl, Br, J; Het means saturated, partially or completely saturated monocyclic or bicyclic heterocyclic radical comprising from 5 to 10 ring members wherein 1 or 2 nitrogen atom (N) and/or 1 or two sulfur atom (S) present, and heterocyclic radical can be monosubstituted with phenyl; Het¹ means saturated, partially or completely unsaturated monocyclic or bicyclic heterocyclic radical comprising from 5 to 10 ring members and from 1 to 4 nitrogen atoms (N) that can be unsubstituted or monosubstituted NHX, or oxo-group; n = 0, 1 or 2; m = 0, 1, 2, 3, 4, 5 or 6; o means 0, 1 or 2; and their physiologically acceptable salts and solvates. Compounds of the formula (I) elicit intergin-inhibitory effect that allows their using as components of pharmaceutical composition. Also, invention describes intermediate compounds.

EFFECT: valuable medicinal properties of compounds.

11 cl, 4 sch, 1 tbl, 34 ex