DERIVATIVES OF INDOLINE USED AS PROTEIN KINASE INHIBITORS Russian patent published in 2008 - IPC C07D403/06 C07D403/14 A61K31/404 A61P35/00 

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

SUBSTANCE: invention relates to novel derivatives of indoline of the formula (I): wherein (i) R¹ means hydrogen atom (H), (C₁-C₄)-alkyl; R² means -A¹-NR⁵R⁶ wherein each substitute R⁵ and R⁶ means independently H, (C₁-C₄)-alkyl; A¹ means -(CH₂)_m, -(CH₂)_n-A²-(CH₂)_p or -(CH₂CH₂O)_qCH₂CH₂ wherein m means a whole number from 2 to 10; each n and p means a whole number from 1 to 6; A² means -CH=CH, phenylene, biphenylene, cyclohexylene or piperazinylene; q = 1, 2 or 3; (ii) R¹ and R² represent in common -A³-NR⁷-A⁴ wherein each A³ and A⁴ means independently -(CH₂)_r or -(CH₂CH₂O)_sCH₂CH₂ wherein r means a whole number from 2 to 6; s = 1, 2 or 3; R⁷ means H, (C₁-C₄)-alkyl; (iii) R¹ and R² in common with nitrogen atom to which they are bound form piperidinyl that comprises a substitute of the formula: -A⁵-R⁸ at 4 position wherein A⁵ represents (C₁-C₄)-alkylene, and R⁸ represents piperidin-4-yl; or (iv) R¹ and R² in common with nitrogen atom to which they are bound form piperidinyl, and each R³ and R⁴ means independently H, or its pharmaceutically acceptable salt. Proposed compounds inhibit tyrosine kinase receptors that allow their using as components of pharmaceutical compositions for treatment. Also, invention describes methods for synthesis of compounds of the formula (I).

EFFECT: valuable medicinal and biochemical properties of compounds and pharmaceutical compositions.

15 cl, 1 tbl, 24 ex