FIELD: chemistry.
SUBSTANCE: invention relates to a compound of formula:
,
where one of X1 and X2 is -C(-Rx)(-Rx '')-, -C(-Rx ')(-Rx' ')-, -N(Rx)- or -N(-Rx')-, and the other is -C(-Rx'')(-Rx'')-, -N(-Rx'') -, -C(=O)- or -O-; Rx is 
; Xs is = O; Rs is methyl; Rx 'is halogen C1-6alkyl, cyano, nitro, amino, azido or 5-member heterocyclyl containing one-three N, and unsubstituted or substituted oxo; Rx" each independently represent hydrogen, halogen, C1-6alkyl or C1-4alkoxycarbonyl; one of Y and Z is -S-, and the other is -CH=; Lx is a saturated or unsaturated C1-4 hydrocarbon chain not containing or containing one O or N atom and not unsubstituted or substituted with halogen; A and B each independently represent benzene or 5–7 membered heterocycle containing one to three N, O or S atoms; Rc is =O; RN is hydrogen or C1-6alkyl; LB is -[C(-RL)(-RL')]m-, -O-, where m is integer of 1 or 2, RL and RL', each independently represents hydrogen, hydroxyl, halogen or C1-6alkyl or RL and RL' are joined together to form C1-6alkylene; RA is hydrogen, halogen, C1-6alkyl, halogen C1-6alkyl, cyano C1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy, halogen C1-6alkoxy, cyanoC1-6alkoxy, C1-6alkylamino, diC1-6alkylamino, C1-6alkylthio, C1-6alkylaminocarbonyl, diC1-6alkylaminocarbonyl, C2-8alkynyl, C1-6alkoxycarbonylamino-C1-6alkoxy, aminoC1-6alkoxy or 3–6-member heterocyclyl; RB is hydrogen, halogen, C1-6alkyl, halogen C1-6alkyl, C1-6alkoxy or halogen C1-6alkoxy; p is integer from 0 to 4, and when p is 2 or higher, RA fragments are identical or different from each other; q is integer from 0 to 4, and when q is 2 or higher, RB fragments are identical or different from each other; and each of said heterocycle and heterocyclyl moieties independently contains at least one hetero group selected from a group consisting of -O-, -NH-, -N=, -S-, -S(=O) - and -S(=O)2-, or its pharmaceutically acceptable salts.
EFFECT: compounds have an inhibitory effect on activation of STAT3 protein and are applicable for preventing or treating diseases associated with STAT3 protein activation.
16 cl, 8 tbl, 56 ex
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