NITROGEN-CONTAINING HETEROARYL DERIVATIVES Russian patent published in 2015 - IPC C07D401/14 C07D409/14 C07D413/14 C07D417/14 A61K31/44 A61K31/506 A61P25/16 A61P25/18 A61P25/28 

Abstract RU 2559895 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel nitrogen-containing heteroaryl derivatives of formula

,

where A1 and A2 are independently selected from a group consisting of CH and N, under the condition that A1 and A2 are simultaneously N; R1 is C1-C7-alkyl, C1-C7-alkoxy, C1-C7-alkoxy-C1-C7-alkyl or cycloalkyl; R2 and R3 are independently a hydrogen atom or C1-C7-alkyl; R4 is a 6-member heteroaryl containing 2 heteroatoms selected from N; Y is a 5-member heteroaryl selected from a group consisting of:

where said heteroaryl is optionally substituted with one substitute selected from a group consisting of C1-C7-alkyl, which is optionally substituted with 1-3 substitutes selected from a group consisting of aryl, cycloalkyl, a 6-member heterocyclyl 2 heteroatoms selected from O and N, C1-C7-alkoxy, hydroxyl, halogen atom, amino group, optionally substituted with one or two C1-C7-alkyl substitutes, cyano and a 5-member heteroaryl containing 2 heteroatoms selected from N, optionally substituted with 1-3 substitutes selected from C1-C7-alkyl, COO-C1-C7-alkyl, cycloalkyl and a 6-member heterocyclyl containing 1 heteroatom, selected from O, N, optionally substituted with 1-3 substitutes selected from C1-C7-alkyl; and R5 is phenyl or a 6- or 10-member heteroaryl containing one or two nitrogen atoms, where said phenyl and said heteroaryl are optionally substituted with 1-3 substitutes selected from a group consisting of a halogen atom, C1-C7-alkoxy, or pharmaceutically acceptable salts thereof.

EFFECT: compounds inhibit PDE10A (phosphodiesterase 10A) and can be used as medicinal agents.

14 cl, 66 ex, 1 tbl

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RU 2 559 895 C2

Authors

Blajger Konrad

Flor Aleksandr

Grebke Tsbinden Katrin

Kerner Mattias

Kun Bernd

Peters Jens-Uve

Rodrigez Sarmiento Roza Marija

Viejra Ehrik

Dates

2015-08-20Published

2011-01-19Filed