| abstract |
FIELD: organic chemistry, biochemistry. n 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 R 3 means residue of the formula (II): wherein D means -C(O)-; R 7 means hydrogen atom (H) or -(C 1 -C 4 )-alkyl; R 8 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) -(C 1 -C 4 )-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 -R 10 wherein x = 0, 1 or 2, or (b) 3) mono- or bi-substituted independently of one another -N(R 10 ) 2 wherein R 10 means (a) hydrogen atom (H); (b) means -(C 1 -C 6 )-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 (R 10 ) 2 residues R 10 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 -NH 2 =, =O, alkoxycarbonyl or aminocarbonyl from 1 to 3 times, or (b) means -C(O)-R 11 wherein R 11 means 1. -O-R 10 or 2. -N(R 10 ) 2 ; R 9 means (a) hydrogen atom (H); (b) means (C 1 -C 6 )-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; R 1 , R 2 and R 4 mean hydrogen atom (H); R 5 means hydrogen atom (H); R 6 means (a) phenyl wherein phenyl is unsubstituted or substituted with -NH 2 ; (b) pyridine, or (c) pyrimidine being pyridine or pyrimidine is unsubstituted or substituted with groups -NH 2 , -NH-CH 3 . Compounds of the formula (I) are specific inhibitors of IkB kinase. n EFFECT: valuable biochemical properties of compounds. n 3 cl, 3 tbl, 29 ex |