LYSIN-SPECIFIC DEMETHYLASE-1 INHIBITORS AND USE THEREOF Russian patent published in 2016 - IPC C07D207/14 C07D211/04 C07D241/04 A61K31/40 A61K31/495 A61P35/00 

Abstract RU 2602814 C2

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, specifically to a heterocyclic compound of general formula (I), where (A) denotes phenyl or pyridyl; each (A′), if present, is independently selected from a group consisting of phenyl, phenylC1-C10alkoxy group, phenylC1-C-10alkyl, phenyloxy group and halogen, where each (A′) contains 0, 1, 2 or 3 substitutes independently selected from a group, including halogen, halogenC1-C-10alkyl, phenyl, C1-C10alkyl and C1-C10alkoxy group; X equals 0, 1 or 2; (B) denotes cyclopropyl ring, where (A) and (Z) are covalently bonded to different carbon atoms in (B); (Z) denotes -NH-; (L) is selected from -CH2CH2-, -CH2CH2CH2- and -CH2CH2CH2CH2-; and (D) is selected from -N(-R1)-R2, -O-R3 and -S-R3, where R1 and R2 are bonded to each other, and together with a nitrogen atom to which R1 and R2 are bonded, form a 5- or 6-member heterocyclic ring, where said heterocyclic ring contains 0, 1 or 2 substitutes, independently selected from a group comprising -NH2, -NH(C1-C6-alkyl), -N(C1-C6-alkyl)(C1-C6-alkyl) and C1-C10alkyl, or R1 and R2 are independently selected from a group including -H, C1-C-10alkyl and C3-C7-cycloalkyl, where total number of substitutes in R1 and R2 is equal to 0, 1 or 2 and substitutes are independently selected from -NH2, -NH(C1-C6-alkyl) and -N(C1-C6-alkyl) (C1-C6-alkyl); and R3 denotes C1-C10alkyl; or its enantiomer, diastereomer or mixture thereof, or its pharmaceutically acceptable salt or solvate; provided that following compounds are excluded: N1,N1-dimethyl-N2-(2-phenylcyclopropyl)-1,3-propandiamine and N1,N1-dimethyl-N2-(2-phenylcyclopropyl)-1,2-ethanediamine. Invention also relates to a heterocyclic compound of formula (I'), a pharmaceutical composition based on compound of formula (I) and use of compound of formula (I).

EFFECT: technical result is obtaining novel heterocyclic compounds having activity as a LSD1 inhibitor.

29 cl, 7 dwg, 1 tbl, 40 ex

(I) (I')

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RU 2 602 814 C2

Authors

Alberto Ortega Munos

Khulio Kastro-Palomino Larija

Mattju Kolin Tor Fajf

Dates

2016-11-20Published

2010-04-19Filed