IMIDAZOPYRIMIDINE AND IMIDAZOTRIAZINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAID DERIVATIVE Russian patent published in 2019 - IPC C07D487/04 A61K31/519 A61K31/53 A61P25/18 

Abstract RU 2710556 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of chemical formula (1) or a pharmaceutically acceptable salt thereof, in which X is CH or N; Z is O or S; R1 is phenyl, optionally substituted with one or more substitutes selected from halogen, hydroxy, C1-C5 alkyl, C1-C5 alkoxy, C1-C5 alkylthio, amino, di(C1-C5)alkylamino, cyano, formyl, halogen-C1-C5 alkyl, hydroxy-C1-C5 alkyl, C1-C5 alkoxy C1-C5 alkyl, carbamoyloxyC1-C5 alkyl, C1-C5 alkyl-C(O)O-C1-C5 alkyl, di(C1-C5)alkylamino-C1-C5 alkyl and 5-member heterocyclic1-C5 alkyl, where heterocycloalkyl has 1 heteroatom selected from N; or 9-member unsaturated heterocyclyl, having 2 heteroatoms selected from O, which is optionally substituted with one or more substitutes selected from halogen; 5–10 membered heteroaryl having 1 or 2 heteroatoms selected from N or S, which is optionally substituted with one or more substitutes selected from halogen, hydroxy, C1-C5 alkyl, C1-C5 alkoxy, halogenC1-C5 alkyl and di(C1-C5)alkylamino, and R2 is phenyl, optionally substituted with one or more substitutes selected from halogen, deuterium and hydroxy, or 6–10-member heteroaryl, having 1 or 2 heteroatoms selected from N, which is optionally substituted with one or more substitutes selected from halogen and C1-C5 alkyl. Invention also relates to a pharmaceutical composition for preventing or treating a disorder mediated by dysfunction of glutamate and a metabotropic glutamate receptor of subtype 5 (mGluR5).

EFFECT: technical result is obtaining novel compounds of formula (1), having the properties of a positive allosteric modulator of metabotropic receptor glutamate subtype 5 (mGluR5).

19 cl, 1 tbl, 199 ex

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RU 2 710 556 C2

Authors

Park, Chun Eung

Jang, Young Koo

Shin, Yong Je

Kim, Ji Yeon

Ham, Seung Mo

Kim, Yong Gil

Min, Hye Kyung

Cha, Soo Bong

Jung, Hyo Jun

Lee, Ju Young

Han, Seung Nam

Chung, Jin Yong

Choi, Eun Ju

Joung, Chan Mi

Park, Jong Sil

Lee, Ji Won

Cho, Nahm Ryune

Ryu, Eun Ju

Maeng, Cheol Young

Dates

2019-12-27Published

2016-02-25Filed