SUBSTITUTED INDOLES Russian patent published in 2005 - IPC

FIELD: organic chemistry, biochemistry.

SUBSTANCE: invention relates to new substituted indoles of the formula (I): and/or stereoisometic form of compound of the formula (I) and/or physiologically acceptable salt of compound of the formula (I) wherein R³ means residue of the formula (II): wherein D means -C(O)-; R⁷ means hydrogen atom (H) or -(C₁-C₄)-alkyl; R⁸ means (a) typical residue of amino acid among the group: phenylalanine or homophenylalanine wherein phenyl residue is unsubstituted or substituted with halogen atom; or (b) -(C₁-C₄)-alkyl wherein alkyl is a linear or branched and (b) 1) mono- or multi-substituted independently of one another with pyrrole residue wherein this residue is unsubstituted or substituted with halogen atom; (b) 2) mono- or bi-substituted independently with residue -S(O)_x-R¹⁰ wherein x = 0, 1 or 2, or (b) 3) mono- or bi-substituted independently of one another -N(R¹⁰)₂ wherein R¹⁰ means (a) hydrogen atom (H); (b) means -(C₁-C₆)-alkyl wherein alkyl is unsubstituted or substituted with halogen atom from 1 to 3 times; (c) phenyl wherein phenyl is substituted or substituted with halogen atom from 1 to 3 times; in the case (R¹⁰)₂ residues R¹⁰ have values independently of one another (a), (b), (c); Z means (a) residue of heterocycles group comprising benzothiadizine, pyrrole, pyridine, pyrimidine, pyrazine, imidazole, pyrazole, oxazole, isoxazole, thiazole, isothiazole, tetrazole, oxadiazolone, triazole being heterocycles are unsubstituted or substituted with -NH₂=, =O, alkoxycarbonyl or aminocarbonyl from 1 to 3 times, or (b) means -C(O)-R¹¹ wherein R¹¹ means 1. -O-R¹⁰ or 2. -N(R¹⁰)₂; R⁹ means (a) hydrogen atom (H); (b) means (C₁-C₆)-alkyl wherein alkyl is unbranched or branched and substituted with phenyl or =O independently of one another from 1 to 3 times; (c) phenyl wherein phenyl is unsubstituted or substituted with halogen atom; R¹, R² and R⁴ mean hydrogen atom (H); R⁵ means hydrogen atom (H); R⁶ means (a) phenyl wherein phenyl is unsubstituted or substituted with -NH₂; (b) pyridine, or (c) pyrimidine being pyridine or pyrimidine is unsubstituted or substituted with groups -NH₂, -NH-CH₃. Compounds of the formula (I) are specific inhibitors of IkB kinase.

EFFECT: valuable biochemical properties of compounds.

3 cl, 3 tbl, 29 ex