DERIVATIVES OF INDOLE, THEIR TAUTOMERS, MIXTURES OF THEIR ISOMERS OR SEPARATE ISOMERS AND PHARMACEUTICALLY ACCEPTABLE SALTS, PHARMACEUTICAL COMPOSITION SHOWING ANTITUMOR OR INHIBITING PROTEIN TYROSINE KINASE ACTIVITY AND METHOD OF INHIBITION OF PROTEIN TYROSINE KINASE-DEPENDING DISEASE OR CONTROL OF ABERRANT GROWTH OF MAMMALIAN OR HUMAN CELLS Russian patent published in 2000 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes the novel derivatives of indole of the general formula (I) and their tautomers where R₁ is hydrogen, halogen atoms, lower alkyl, hydroxyl, nitro-group, trifluoromethyl, groups OCOR and OR where R means lower alkyl being residue R₁ can replace a single group of ring with aza-atom; R₂ means groups: (CH₂)_n-COOH, (CH₂)_nCONH₂, (CH₂)_n-COOR, (CH₂)_n-CONHR, (CH₂)_n-CONRR, (CH₂)_nCONHCH₂Ph, CONHR, CONRR, CONHPh, COPhCOOH, COPhCOOR, (CH₂)_n-CONHPh or (CH₂)_n-CONHPhR where R has the above indicated value; Ph means phenyl; n = 1-4; groups COY and SO₂Y where Y means unsubstituted phenyl or phenyl substituted with lower alkyl, carboxyl or group OCOR where R has the above indicated value; R₃ is hydrogen atom, benzyl; R₄ is groups: SH, S₀X,S₀Q₁ Se₀Q′ where o = 1, 2 or 3; X is hydrogen atom, lower alkyl, benzyl; Q is 2-thio-indolyl of the general formula (I); Q′ is 2-selenoindolyl of the general formula (I) under condition that if R₄ means Se₀Q′, then R₂ means groups COOR₅ where R₅ means hydrogen atom or lower alkyl, -CONHR₆ where R₆ means lower alkyl or (CH₂)₂-lower dialkyl or group where R₂ means amino-group and Ph is phenyl but the following compounds are excluded: 2-(2-thioxo- -3-indolinyl)-acetic acid, 2-(1-methyl-2-thioxo-3-indolinyl)-acetic acid, methyl-2-(2-thioxo-3-indolinyl)acetate, ethyl- -2-(1-methyl-2-thioxo-3-indolinyl)acetate, bis-[methyl- -indolinyl-3-acetate-(2)] disulfide, bis-[indolyl-3-acetic acid-(2)] disulfide, bis-[methylindolyl-3-acetate-(2)] trisulfide, bis-[1-methylindolyl-3-acetic acid-(2)] disulfide, 2,3-dihydro-2-thioxo-1H-indole-3-acetic acid methyl ester and 2-(methylthio)-1H-indole-3-acetic acid methyl ester, mixtures of their isomers or separate isomers and pharmaceutically acceptable salts. Compounds of the formula (I) show valuable pharmacological properties, in part, they can be used as inhibitors of protein tyrosine kinase and an antitumor agent. Invention describes also pharmaceutical composition based on compounds of the formula (I), method of inhibition of protein tyrosine kinase depending disease or control of aberrant growth of mammalian or human cells. EFFECT: valuable medicinal properties of compounds. 4 cl, 3 tbl, 9 ex