LYSIN-SPECIFIC DEMETHYLASE-1 INHIBITORS AND USE THEREOF Russian patent published in 2016 - IPC C07C211/35 C07C211/42 C07C217/52 C07C237/24 A61K31/135 A61K31/16 A61P35/04 A61P31/16 

FIELD: chemistry.

SUBSTANCE: present invention relates to novel compounds of formula (1) or pharmaceutically acceptable salts thereof having inhibitory effect on LSD1 (lysin-specific demethylase-1 inhibitors). Said activity enables their use for treating or preventing some diseases such as cancer. Above cancer is selected from the group including breast cancer, colorectal cancer, lung cancer, prostate cancer, testicular cancer, cerebral cancer, skin cancer and blood cancer. In compounds of formula 1

,

(A) denotes a pyridyl or phenyl; each (A′), if conained, is independently selected from a group consisting of phenyl, phenyl-C₁-C₄-alkoxy group, phenyl-C₁-C₄-alkyl, halogen, C₁-C₄-alkoxy group and halogen-C₁-C₄-alkyl, where each (A′) contains 0, 1, 2 or 3 substitutes independently selected from a group comprising halogen, halogen-C₁-C₄-alkyl, phenyl, C₁-C₄-alkyl and C₁-C₄-alkoxy group; X equals to 0, 1 or 2; (B) denotes cyclopropyl ring, where (A) and (Z) covalently connected with different carbon atoms in (B); (Z) denotes -NH-; (L) is selected from rhe group including a single link, -CH₂-, -CH₂CH₂-, -CH₂CH₂CH₂- and -CH₂CH₂CH₂CH₂-; and (D) denotes C₃-C₇-cycloalkyl or benzo-C₅-C₇-cycloalkyl, where said C₃-C₇-cycloalkyl or said petrol-C₅-C₇-cycloalkyl, contains 0, 1, 2 or 3 substitutes independently selected from the group, including -NH₂, halogen, amido group, C₁-C₄-alkoxy group and halogen-C₁-C₄-alkyl; or its pharmaceutically acceptable salt. Compound, which is substituted with heteroarylcyclopropylamine or substituted arylcyclopropylamine and correponds to formula 2

,

where (R3) is present or is not, if (R3) is present, it is selected from the group consisting of phenyl-C₁-C₄-alkyl and phenyl-C₁-C₄-alkoxy group, where the said group (R3) contains 0, 1, 2 or 3 substitutes independently selected from the group including halogen, C₁-C₄-alkyl, C₁-C₄-alkoxy group, halogen-C₁-C₄-alkyl and phenyl; (W) denotes phenyl or pyridyl group, where the said (W) contains 0, 1 or 2 substitutes selected from the group including halogen, C₁-C₄-alkoxy group, halogen-C₁-C₄-alkyl and phenyl; (L′) denotes a bridge of formula -(CH₂)_n-, where n equals 0, 1, 2, 3 or 4; and R4 is C₃-C₇-cycloalkyl or benzo-C₅-C₇-cycloalkyl, wherein the above C₃-C₇-cycloalkyl or said benzo-C₅-C₇-cycloalkyl contains 0, 1, 2 or 3 substitutes, selected from the group including halogen, C₁-C₄-alkoxy group, halogen-C₁-C₄-alkyl, amine group and C-amido group; may be used as LSD1 selective inhibitor for identification method within the group of formula 2 compounds, which inhibits LSD1 in greater degree than MAO-A and/or MAO-B.

EFFECT: said compounds may be used for production of medicinal agent having LSD1 inhibiting activity for in treatment or preventing diseases or pathological condition.

51 cl, 1 tbl, 21 ex

циклопропил - cyclopropyl