FIELD: medicine; chemistry.
SUBSTANCE: invention relates to an imidazoisoindole derivative of formula (I) having the properties of an indolaminopyrrole-2,3-dioxygenase (IPO) inhibitor, a method for preparing it and a pharmaceutical composition based thereon. In formula (I) M is trifluoroacetic acid; A is selected from a group consisting of 6-membered cycloalkyl or 5–6-member heterocyclyl with 1 nitrogen atom; R1 is selected from a group consisting of C1-6 alkyl, phenyl, 5–9-member heteroaryl with 1–3 heteroatoms selected from nitrogen and sulfur, -C(O)R4 and -C(O)NR5R6; R2 is selected from a group consisting of hydrogen and halogen; R3 are identical or different and each is independently selected from a group consisting of hydrogen, C1-6 alkyl, alkoxy, halogen, amino, cyano, 6-member heterocyclyl with 2 heteroatoms selected from nitrogen and oxygen, phenyl, 5–6-member heteroaryl with 1 to 2 nitrogen atoms, -OR4, -S(O)mR4, -C(O)NR5R6 and -NR5C(O)R6, where each alkyl and heteroaryl is optionally substituted with one or more groups selected from a group consisting of from C1-6 alkyl, amino, hydroxy-C1-6 alkyl, 5–6-member heterocyclyl with 1–2 heteroatoms selected from nitrogen and oxygen, -Ra, -C(O)NR7R8; Ra is selected from a group consisting of C1-6 alkyl, 6-member heterocyclyl with 1 nitrogen atom, where each alkyl and heterocyclyl are optionally substituted with one or two groups selected from a group consisting of hydroxy, alkoxy, -S(O)mR4 and -NR5C(O)R6; R4 is selected from a group consisting of C1-6 alkyl, 5–6-member heterocyclyl with 1 heteroatom selected from nitrogen and oxygen, where each heterocyclyl is optionally substituted with one -S(O)mR7 group; R5 and R6 are identical or different, and each is independently selected from a group consisting of hydrogen, C1-6 alkyl, 6-membered cycloalkyl, 6-member heterocyclyl with 1 oxygen atom and phenyl, where each cycloalkyl and phenyl are optionally substituted with one group selected from the group consisting of cyano and alkoxy; R7 and R8 are identical or different, and each is independently selected from a group consisting of hydrogen and C1-6 alkyl; p is integer 1; y is integer 0 or 1; m is integer 2; and n is integer of 0, 1 or 2.
EFFECT: invention is used for preparing a drug for treating cancer with a pathological sign of a pathogen-mediated tryptophan pathway.
15 cl, 5 tbl, 52 ex
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