| abstract |
FIELD: pharmaceutics. n SUBSTANCE: invention relates to compound of formula (IV) or its N-oxide, or pharmaceutically acceptable salt of such compounds, where A is O or CH 2 ; Q is NH 2 , NHR b , NR b R c or OH, where each R b and R c independently represent C 1 -C 6 alkyl; X is N or group CR x , where R x is H; Y is H or R d , where R d is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or C 3 -C 8 cycloalkyl, and R d is optionally substituted with one or more substitutes, selected from group consisting of halogen and C 3 -C 8 cycloalkyl; each of R 1 and R 2 is H; each of R e , R f , R g and R h independently represent group -M 2 -T 2 , where M 2 is bond or O-C 1 -C 4 alkyl linker, and T 2 is H, halogen or R S4 , where R S4 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl or oxetanyl, and each of O-C 1 -C 4 alkyl linker and R S4 is optionally substituted with one or more substitutes, selected from group consisting of halogen, hydroxyl, cyano, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl and C 1 -C 6 alkoxyl; and m equals to 0, 1 or 2. Invention relates to specific compounds. Disclosed compounds are intended for producing pharmaceutical composition with antiproliferative activity, including therapeutically effective amount of compound and pharmaceutically acceptable carrier. Besides compound is applied for treating leukemia and inhibiting DOT1L-mediated protein methylation. n EFFECT: substituted purine or 7-deazapurine compound effective in treating leukemia and inhibiting DOT1L-mediated protein methylation. n 24 cl, 1 tbl, 3 dwg, 11 ex |