SPIROINDOLINONE PYRROLIDINES, USEFUL WHEN TREATING MALIGNANT GROWTHS Russian patent published in 2015 - IPC C07D487/10 A61K31/407 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, and specifically to novel spiroindolinone pyrrolidine derivatives of general formula or pharmaceutically acceptable salts and enantiomers thereof, where X is selected from a group which includes Cl and Br, Y is selected from a group which includes F, Cl and Br, R₁ is a substituted lower alkyl selected from: where R₉, R₁₀ are both a methyl; R₁₁ is (CH₂)_q-R₁₂; R₁₂ is selected from hydrogen, hydroxyl; q = 1 or 2; R₂ is selected from a group which includes phenyl, phenyl substituted with 1-3 substitutes, heteroaryl and heteroaryl substituted with 1-2 substitutes, where the heteroaryl is selected from pyrrolyl, pyrazolyl, furanyl, thiophenyl, thiazolyl, pyridinyl, pyrimidinyl, benzothiophenyl; where the substitutes for the substituted phenyl and the substituted heteroaryl are selected from a group which includes hydrogen, lower alkyl, halogen, CN, NH₂, N(H, lower alkyl), N(lower alkyl)₂, aminocarbonyl, lower dialkylaminocarbonyl, carboxy, NO₂, lower alkoxy, lower alkylsulphonyl, lower alkylcarbonyl, lower alkoxycarbonyl, lower alkylcarbonyl-NH, lower alkoxycarbonyl-lower alkoxy, lower alkylcarbonyl-oxy-lower alkoxy, carboxy-lower alkoxy, hydroxy-lower alkoxy, lower alkyl-thio-lower alkoxy, lower alkylsulphonyl-lower alkoxy, aminocarbonyl-lower alkoxy, lower alkylthionyl-lower alkoxy, halogen-lower alkoxy, dimethylmorpholine, morpholine, tetrazole, lower alkylsulphonylamino, hydroxy-lower alkylcarbonyl, morpholine-4-sulphonyl, tetrahydropyranoxy, -NH-CH₂-COOH, -NH-CH₂-COOEt, -CONH-CN, oxo-group and lower alkyl, which is substituted with one substitute selected from hydroxy, lower alkoxycarbonyl, lower alkylcarbonyl, carboxy, aminocarbonyl; R₃, R₄, R₅ are selected from H or F under the condition that at least two of R₃, R₄, R₅ are hydrogen; R₆, R₇, R₈ are selected from H or F under the condition that at least two of R₆, R₇, R₈ are hydrogen. The invention also relates to a compound of formula where the values of radicals are given in the claim, specific spiroindolinone pyrrolidinyl derivatives, a pharmaceutical composition based on spiroindolinone pyrrolidinyl derivatives, use thereof and a method of treating malignant growths.

EFFECT: obtaining novel spiroindolinone pyrrolidinyl derivatives, having useful biological properties.

21 cl, 225 ex