FIELD: chemistry.
SUBSTANCE: invention relates to substituted benzene compounds represented by formulae I, III, VI, VII. Compound of formula III:
,
or a pharmaceutically acceptable salt thereof, where R801 is C1-6 alkyl, C2-6 alkynyl, heterocycloalkyl, selected from morpholine, pyrrolidine, tetrahydrothiophene, piperidine, piperazine, oxetane, pyran, tetrahydropyran, azetidine and tetrahydrofuran, phenyl or heteroaryl, selected from pyrrole, furan, thiophene, thiazole, isothiazole, imidazole, triazole, tetrazole, pyrazole, oxazole, isoxazole, pyridine, pyrazine, pyridazine and pyrimidine, each of which contains, as a substituent, OC1-6 alkyl-Rx, where Rx is hydroxyl or OC1-3 alkyl and Rx optionally further substituted with OC1-3 alkyl; each of R802 and R803 independently is H, halogen, C1-4 alkyl or C1-6 alkoxy; each of R804 and R805 is independently C1-4 alkyl; and R806 is -Qx-Tx, where Qx is a bond or C1-4 alkyl linking group, Tx is H, tetrahydropyranyl, piperidinyl substituted with 1, 2 or 3 C1-4 alkyl groups, or cyclohexyl, containing, as a substituent, N(C1-4 alkyl)2, where one or both C1-4 alkyl optionally have as substituent C1-6 alkoxy; which have the ability to inhibit the activity of EZH2, as well as to pharmaceutical compositions containing said compounds and methods of treatment.
EFFECT: treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.
55 cl, 7 tbl, 3 ex
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Authors
Dates
2018-06-26—Published
2013-10-15—Filed