OXYINDOLE DERIVATIVES POSSESSING AGONIST ACTIVITY ON MOTILIN RECEPTOR Russian patent published in 2014 - IPC C07D401/14 C07D401/04 A61K31/497 A61P1/06 A61P1/04 

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to new oxyindole derivatives of formula (I) or their pharmaceutically acceptable salts, based pharmaceutical compositions and using them for treating various disorders, which are mediated through the motilin receptor (GPR38). In general formula I, R¹ means hydrogen, C₁-C₄alkyl or C₃-C₇cycloalkyl; R² means C₁-C₄alkyl or C₃-C₇cycloalkyl; or R¹ and R² together with atoms which they are bound to, form a 3-6-merous ring, which can contain oxygen; R³ and R⁴ mean hydrogen or C₁-C₄alkyl; R⁵ means hydrogen or C₁-C₄alkyl; R⁶ and R⁷ mean hydrogen, C₁-C₄alkyl or C₁-C₄alkoxy C₁-C₄alkyl; or R⁶ and R⁷ together with a nitrogen atom which they are bound to, form a 4-6-merous ring, which can contain nitrogen or oxygen; the 4-6-merous ring is optionally substituted by 1-4 substitutes specified in a group consisting of C₁-C₄alkyl, amino, C₁-C₄alkylamino and di(C₁-C₄alkyl)amino; A means or , wherein p, q and r independently have the values of 0, 1 or 2; R⁸ and R⁹ mean hydrogen or C₁-C₆alkyl; wherein alkyl is optionally substituted by hydroxy, C₁-C₄alkyl, amino, C₁-C₄alkylamino and di(C₁-C₄alkyl)amino; or R⁸ and R⁹ can be combined to form a C₃-C₇-merous ring; or R⁸ and R⁹ can be independently combined with one or both R⁸ and R⁹ groups to form alkylene bridges between terminal nitrogen and an alkyl part of R⁸ or R⁹ groups; the bridge contains 1 to 5 carbon atoms; the above bridge is optionally substituted by 1-4 C₁-C₄ alkyl groups; W means N-R¹⁰, the above R¹⁰ means hydrogen or C₁-C₄alkyl; X means C₀-C₄alkylene or C₀-C₄alkylene-K-C₀-C₄alkylene, wherein K means -O- and wherein alkylene is optionally substituted by C₁-C₄alkyl; Y means hydrogen or a 5-10-merous ring; the above ring is optionally substituted by hydroxyl, halogen, halogen C₁-C₄alkyl, C₁-C₄alkyl or C₁-C₄alkoxy; provided X means C₀, Y means other than hydrogen; Z means halogen or C₁-C₄alkyl; m has the value of 0, 1, 2, 3 or 4; n has the value of 0, 1 or 2.

EFFECT: preparing the new oxyindole derivatives.

10 cl, 15 tbl, 99 ex