PYRROLO[2,3-b]PYRIDINE DERIVATIVES INHIBITING ACTIVITY OF ANTI-APOPTOTIC Bcl-2 PROTEINS Russian patent published in 2015 - IPC C07D471/04 A61K31/437 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to new heterocyclic compounds of general formula (IIIa) or its therapeutically acceptable salt, wherein A¹ represents C(A²); A² represents H; B¹ represents OR¹ or NHR¹, wherein R¹ represents C₁-alkyl substituted by R¹⁰; D¹ and E¹ represent H; and Y¹ represents NO₂; G¹ represents C₁-alkyl substituted by OP(O)(OH)(OH); R¹⁰ represents C₆-cycloalkyl, each of which has one CH₂ fragment either unsubstituted, or substituted by means of independently specified O; wherein the fragment representing R¹⁰ is either unsubstituted, or substituted by one, or two, or three, or four, or five substitutes independently specified in a group consisting of R⁵⁰, OR⁵⁰, F, Cl, Br, and I; and R⁵⁰ represents C₁-alkyl. The invention also refers to specific compounds, a pharmaceutical composition based on the compounds specified in claims No. 1-3, and a method of treating cancer.

EFFECT: there are produced new compounds, which inhibit the activity of anti-apoptotic Bcl-2 proteins.

6 cl, 4 tbl, 7 ex