COMPOUNDS AND METHODS OF INHIBITING INTERACTION OF Bcl PROTEINS WITH BINDING PARTNERS Russian patent published in 2012 - IPC C07D261/02 C07D413/10 C07D413/12 C07D417/12 A61K31/422 A61P35/00 

FIELD: medicine.

SUBSTANCE: in claimed invention described is compound of general formula 1, or its pharmaceutically acceptable salt, where in each case independently on each other m equals 0, 1; p equals 1 or 2; R₁ is selected from group, including -OH, -OC(O)NHMe, -OC(O)NMe₂, -OC(O)NH(CH₂)₂Ph and OC(O)NH(CH₂)₂NMe₂; R₂ stands for -OH, -OC(O)Me, -OCH₂CO₂H, -OCH₂CO₂Et, -N₃, -N=C(NMe₂)₂, -NH₂, -NMe₂, -NHC(O)Me, -NHC(O)CF₃, - NHC(O)Ph, -NHC(O)NHPh, -NHC(O)CH₂CH₂CO₂H, -NHC(O)CH₂CH₂CO₂Me, - NHCH₂Ph, -NHCH₂(4-pyridyl), -NHCH₂(2-pyridyl), -NHCH₂(4-(CO₂H)Ph), - NHCH₂(3-(CO₂H)Ph), -NHEt, -NHCHMe₂, -NHCH₂CHMe₂, -N(CH₂CHMe₂)₂, - NHCH₂(cyclopropyl) or -NHC(O)CH₂CH₂NMe₂; R₃ stands for -OMe, -OEt, - OCH₂(cyclopropyl), F, -O(CH₂)₂NMe₂ or -O(CH₂)₂(4-morpholino); R₄ stands for -NMe₂, -NEt₂, -NHEt, -NHCH₂CHMe₂, -N(Me)CH₂CHMe₂, - N(Me)CH₂CH₂NHS(O)₂Me, -N(Me)CH₂CH₂NHS(O)₂CF₃, -NHCH₂CH₂OH, - N(Me)CH₂CH₂OH, -N(Me)CH₂CO₂H, -N(Me)CH₂C(O)NH₂, N(Me)CH₂C(O)NHMe, -N(Me)CH₂C(O)NMe₂, -NHC(O)Me, 1-piperidinyl, 4-morpholino, (R)-2-(hydroxymethyl)-1-pyrrolidinyl, -NH₂, -NO₂, Br, CI, F, -C(O)Me or -CH₂NH₂; R₅ stands for -OH or -N(R₁₇)(R₁₈); R₁₇ and R₁₈ independently in each case stand for H, (C₁-C₆)-alkyl, (C₅-C₇)-aryl-(C₁-C₆)-alkyl, where said aryl contains from zero to two heteroatoms, (C₁-C₆)-alkoxy or -[C(R₁₉)(R₂₀)]_P-R₂₁ R₁₉ and R₂₀ independently in each case represent H, (C₁-C₆)-alkyl, (C₁-C₆)-alkoxy, amino-(C₁-C₆)-alkyl, acylamino, sulfonylamino, (C₅-C₇)-aryl, (C₅-C₇)-aryl-(C₁-C₆)-alkyl or 3-10-membered heterocyclyl-(C₁-C₆)-alkyl, containing in ring from one to two heteroatoms; R₂₁ independently in each case represents H, 3-10-membered heterocyclyl, containing in ring one heteroatom, (C₁-C₆)-alkylsulfonyl, (C₁-C₆)-alkylsulfonamido or amido; R₂₂ stands for halogen; R₂₃ stands for methyl; R₂₄ stands for methyl and R₂₅ stands for methyl, where said aryl stands for 5-7-membered ring, containing from zero to two heteroatoms, and said aryl or said heterocyclyl can be non-substituted or substituted halogen, (C₁-C₆)-alkyl or amino. Also described is pharmaceutical composition, possessing inhibiting activity with respect to Bcl-2 and/or Bcl-XL proteins, which includes said compound, also described is method of treating disorder, mediated by Bcl-2 and/or Bcl-XL proteins, which lies in introduction of said compound to patient, who needs such treatment, in therapeutically efficient amount.

EFFECT: increased efficiency of compound application.

41 cl, 6 dwg, 125 ex