1,3-BENZODIOXOLE DERIVATIVE Russian patent published in 2019 - IPC C07D405/12 C07D405/14 A61K31/443 A61K31/4433 A61K31/4439 A61K31/4545 A61K31/496 A61K31/5377 A61P35/00 A61P35/02 

Abstract RU 2679131 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of general formula (I) or to its pharmacologically acceptable salt, where R1 is a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 alkoxy, C3-C6 cycloalkyl group, C1-C6 alkylcarbonyl group, C2-C6 alkenyl group, C2-C6 alkynyl group, C3-C6 cycloalkenyl group, phenyl group, 5- or 6-membered aromatic heterocyclic group having 1-2 heteroatoms in the ring, independently selected from the group consisting of a nitrogen atom and a sulfur atom, or a 5- or 6-membered aliphatic heterocyclic group having an unsaturated bond in the ring portion and having 1 heteroatom in the ring, independently selected from the group consisting of a nitrogen atom and an oxygen atom, where a 5- or 6-membered aromatic heterocyclic group and 5- or 6-membered aliphatic heterocyclic group having an unsaturated bond in the part of the ring, each optionally has 1 substitute, independently selected from group A, described below, V is a single bond, C1-C6 alkylene group or oxy-C1-C6 alkylene group, R2 is C3-C6 cycloalkyl group, bicyclo-C5-C8 cycloalkyl group, a 5- or 6-membered aliphatic heterocyclic group having 1 or 2 heteroatoms in the ring, independently selected from the group consisting of a nitrogen atom and an oxygen atom, or a spiro-ring group containing two spiro-condensed rings independently selected from the group consisting of a 4–6 membered aliphatic heterocyclic ring having 1 nitrogen atom in the ring, and C3-C6 cycloalkyl ring, where C3-C6 cycloalkyl group, bicyclo-C5-C8 cycloalkyl group, a 5- or 6-membered aliphatic heterocyclic group and spiro-ring groups, each optionally having 1 substitute independently selected from group C described below, R3 is C1-C6 alkyl group, R4 is a halogen atom or C1-C6 alkyl group, R5 is C1-C6 alkyl group or C1-C6 alkoxygroup, R6 is C1-C6 alkyl group, group A consists of C1-C6 alkyl group and a 5- or 6-membered aliphatic heterocyclic group having 2 nitrogen atoms in the ring, where C1-C6 alkyl group and a 5- or 6-membered aliphatic heterocyclic group each optionally have 1 substituent independently selected from group B described below, group B consists of C1-C6 alkyl group and a 5- or 6-membered aliphatic heterocyclic group having 2 heteroatoms in the ring, independently selected from the group consisting of a nitrogen atom and an oxygen atom, and group C consists of C1-C6 alkyl group, C1-C6 alkylsulfonyl group, -NR20R21, C1-C6 alkoxy-C1-C6 alkyl group and di-C1-C6 alkylamino-C1-C6 alkyl group, where R20 and R21 each independently is a hydrogen atom, a formyl group or C1-C6 alkyl group. Also, the invention relates to a pharmaceutical composition for inhibiting EZH1 and/or EZH2 enzyme activity based on said compounds. (I).

EFFECT: obtained new compounds and pharmaceutical compositions based on them, which can be used in medicine for treatment of tumors.

18 cl, 3 tbl, 88 ex

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RU 2 679 131 C2

Authors

Kanno Osamu

Watanabe Jun

Horiuchi Takao

Nakao Akira

Suzuki Keisuke

Yamasaki Tomonori

Adachi Nobuaki

Honma Daisuke

Hamada Yoshito

Dates

2019-02-06Published

2015-03-16Filed