6,7,8,9-TETRAHYDRO-5H-PYRIDO[2,3-D]AZEPINE LIGANDS OF DOPAMINE RECEPTORS D3 Russian patent published in 2020 - IPC C07D471/04 A61K31/55 A61P3/00 A61P9/00 A61P15/00 A61P21/02 A61P25/16 A61P25/24 A61P25/30 

Abstract RU 2712455 C1

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to novel heterocyclic compounds of formula I or pharmaceutically acceptable salts thereof, where R1 is selected from a group consisting of hydrogen and C1-C6-alkyl; where C1-C6-alkyl is optionally substituted with one substitute independently selected from halogen, hydroxy or C1-C3-alkoxy; R2 is C1-C3-alkyl; is 0 or 1; R3 is selected from a group consisting of hydroxy, C1-C6-alkyl and C1-C6-alkoxy, where each of C1-C6-alkyl and C1-C6-alkoxy is optionally substituted with 2–3 fluorine atoms; R4 is hydrogen; A is selected from a group consisting of phenyl and 6-member heteroaryl, 1 or 2 ring atoms in 6-member heteroaryl are nitrogen and the remaining ring atoms are carbon; and where phenyl and 6-member heteroaryl are optionally substituted with 1 R6; R5 is selected from a group consisting of halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkoxy-C1-C6-alkyl, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C6-alkyl, C3-C7-cycloalkoxy, phenoxy, 4–6-member heterocycloalkyl and 5–6-member heterocycloalkoxy, where 1 ring atom in heterocycloalkyl and heterocycloalkoxy is oxygen, and the remaining ring atoms are carbon; where C1-C6-alkyl, C1-C6-alkoxy and C1-C6-alkoxy-C1-C6-alkyl is optionally substituted with one or two substitutes independently selected from halogen or hydroxy; and where C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C6-alkyl, C3-C7-cycloalkoxy, phenoxy, 4–10-member heterocycloalkyl and 4–10-member heterocycloalkoxy are optionally substituted with one to two R7; R6 is selected from a group consisting of halogen, and C1-C6-alkyl; or R5 and R6, when they are bonded to adjacent carbon atoms and taken together with adjacent carbon atoms to which they are bonded, form a condensed tetrahydropyrine or tetrahydrofuran ring which is optionally substituted with one or two R8; R7 in each case is independently selected from a group consisting of halogen, hydroxy, C1-C3-alkyl optionally substituted with three fluorine atoms or C1-C3-alkoxy, and C1-C3-alkoxy, optionally substituted with one fluorine atom; and R8 in each case is C1-C3-alkyl. Also disclosed are specific compounds of formula (I), a pharmaceutical composition based on the compound of formula (I) and use of the compound of formula (I) as a D3 receptor modulator.

I

EFFECT: technical result is obtaining novel pyrido[2,3-d]azepine derivatives useful for treating a disease mediated by D3 receptors.

29 cl, 8 tbl, 15 ex

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RU 2 712 455 C1

Authors

Chappi Tomas Allen

Khenderson Zhaklin Luiz

Yang Dzhozef Majkl

Uejdzher Trevis T.

Kormos Betani Lin

Patel Nandini Chaturbkhaj

Shchiabola Simone

Tattl Dzhejmison Brajs

Verkhust Patrik Robert

Taker Dzhozef Uolter

Dates

2020-01-29Published

2017-01-09Filed