SPECIFIC ACTIVATOR AKT3 AND ITS USE Russian patent published in 2024 - IPC C07D401/12 A61K31/4709 A61P37/00 A61P29/00 

Abstract RU 2815372 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof, wherein rings A, B and C are independently phenyl, pyridine and quinoline; R1 represents -(C3-C12)-heterocycloalkyl, -(C6-C20)-aryl, or -(C3-C20)-heteroaryl groups, optionally substituted by one or more substituents selected from - (C1-C12)-alkyl or -NH2; X, Y and Z are independently -O, -NH, or -N-(C1-C30)-alkyl; R2 represents =O; and R3 on ring A is -(C1-C30)-alkyl, -(C3-C12)-heterocycloalkyl, -(C6-C20)-aryl, -O-(C1-C12)-alkyl, -N-[(C1-C12)-alkyl]2, -COOH, -CN, -NH2 or halogen; R3 on ring C is hydrogen, -(C1-C30)-alkyl or halogen; provided that when R1 is unsubstituted pyridine or N-substituted –(C1)-alkyl pyridine, X, Y and Z are NH, R2 is =O, A is quinoline or pyridine, B is phenyl or pyridine, C is phenyl, R3 on ring C is hydrogen, then R3 on ring A is not -N-[(C1)-alkyl]2, -COOH, -CN and –F; when the compound has the structure of formula III

Formula III

R1 is unsubstituted pyridine, N-substituted -(C1-C3)-alkyl pyridine or pyrimidine substituted –(C1)-alkyl and NH2, X, Y, Z are -NH, R2 is =O, then R4 is not a halogen, -(C1)-alkyl, -O-(C1)-alkyl, -NH2 and -N-[(C1)-alkyl]2; when R1 is unsubstituted pyridine, unsubstituted quinoline or quinoline substituted with -NH2, -NO2, or -N-[(C1)-alkyl]2, X, Y, Z are -NH, R2 is =O, A is pyridine, B is phenyl, C is phenyl, R3 on ring C is hydrogen, then R3 on ring A is not –(C1-C2)-alkyl and -NH2; and when R1 is acridine, X, Y, Z are -NH, R2 is =O, A is pyridine, B is phenyl, C is phenyl, R3 on ring C is hydrogen, then R3 on ring A is not –(C1)-alkyl. The invention also relates to pharmaceutical compositions and methods for selective activation of Akt3.

Formula I

EFFECT: new compounds that can be used in medicine for the effective treatment of inflammatory, autoimmune diseases, graft-versus-host disease, chronic infection and obesity.

30 cl, 112 dwg, 13 ex

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RU 2 815 372 C2

Authors

Khleif, Samir

Mkrtichyan, Mikayel

Dates

2024-03-13Published

2018-09-06Filed