COMPOUNDS AND METHODS OF INHIBITING INTERACTION OF Bcl PROTEINS WITH BINDING PARTNERS
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; Ris selected from group, including -OH, -OC(O)NHMe, -OC(O)NMe, -OC(O)NH(CH)Ph and OC(O)N...
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Zusammenfassung: | 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; Ris selected from group, including -OH, -OC(O)NHMe, -OC(O)NMe, -OC(O)NH(CH)Ph and OC(O)NH(CH)NMe; Rstands for -OH, -OC(O)Me, -OCHCOH, -OCHCOEt, -N, -N=C(NMe), -NH, -NMe, -NHC(O)Me, -NHC(O)CF, - NHC(O)Ph, -NHC(O)NHPh, -NHC(O)CHCHCOH, -NHC(O)CHCHCOMe, - NHCHPh, -NHCH(4-pyridyl), -NHCH(2-pyridyl), -NHCH(4-(COH)Ph), - NHCH(3-(COH)Ph), -NHEt, -NHCHMe, -NHCHCHMe, -N(CHCHMe), - NHCH(cyclopropyl) or -NHC(O)CHCHNMe; Rstands for -OMe, -OEt, - OCH(cyclopropyl), F, -O(CH)NMeor -O(CH)(4-morpholino); Rstands for -NMe, -NEt, -NHEt, -NHCHCHMe, -N(Me)CHCHMe, - N(Me)CHCHNHS(O)Me, -N(Me)CHCHNHS(O)CF, -NHCHCHOH, - N(Me)CHCHOH, -N(Me)CHCOH, -N(Me)CHC(O)NH, N(Me)CHC(O)NHMe, -N(Me)CHC(O)NMe, -NHC(O)Me, 1-piperidinyl, 4-morpholino, (R)-2-(hydroxymethyl)-1-pyrrolidinyl, -NH, -NO, Br, CI, F, -C(O)Me or -CHNH; Rstands for -OH or -N(R)(R); Rand Rindependently in each case stand for H, (C-C)-alkyl, (C-C)-aryl-(C-C)-alkyl, where said aryl contains from zero to two heteroatoms, (C-C)-alkoxy or -[C(R)(R)]-RRand Rindependently in each case represent H, (C-C)-alkyl, (C-C)-alkoxy, amino-(C-C)-alkyl, acylamino, sulfonylamino, (C-C)-aryl, (C-C)-aryl-(C-C)-alkyl or 3-10-membered heterocyclyl-(C-C)-alkyl, containing in ring from one to two heteroatoms; Rindependently in each case represents H, 3-10-membered heterocyclyl, containing in ring one heteroatom, (C-C)-alkylsulfonyl, (C-C)-alkylsulfonamido or amido; Rstands for halogen; Rstands for methyl; Rstands for methyl and Rstands 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, (C-C)-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
В настоящем изобретении описано соединение общей формулы 1, указанной в тексте описания, или его фармацевтически приемлемая соль, где в каждом случае независимо друг от друга m равно 0, |
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