SUBSTITUTED PYRAZINE PYRIMIDINONES AS TRPA1 CHANNEL BLOCKERS, PHARMACEUTICAL COMPOSITION, METHODS OF PRODUCTION AND USE THEREOF Russian patent published in 2016 - IPC C07D487/04 A61K31/519 A61P29/00 

Abstract RU 2603770 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted pyrazine pyrimidinones of general formula I or racemic mixtures, individual optical isomers and pharmaceutically acceptable salts thereof, which possess properties of TRPA1 channel blockers. In formula I, R1=H, (C1-C5) alkyl; R2=H, (C1-C5) alkyl; R3=H, (C1-C5) alkyl; R4=H, (C1-C7) alkyl, (C1-C7) alkyl, substituted with (C3-C7) cycloalkyl, (C3-C7) cycloalkyl; R5=H, (C1-C5) alkyl, heterocyclyl, where heterocyclyl denotes a saturated monocyclic system including 4 to 6 carbon atoms, in which one carbon atom is substituted by a heteroatom, such as nitrogen.

EFFECT: invention also relates to a method of producing compounds of general formula I, an active component, a pharmaceutical composition and a method of anaesthesia using said compounds.

6 cl, 3 tbl, 1 dwg, 3 ex

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RU 2 603 770 C2

Authors

Kochkarov Vladimir Iskhakovich

Nikitin Aleksandr Vladimirovich

Gureev Vladimir Vladimirovich

Korokin Mikhail Viktorovich

Gudyrev Oleg Sergeevich

Pokrovskaja Tatjana Grigorevna

Beskhmelnitsyna Evgenija Aleksandrovna

Kravchenko Dmitrij Vladimirovich

Jakushev Vladimir Ivanovich

Shabelnikova Anna Sergeevna

Ivashchenko Andrej Aleksandrovich

Shafeev Mikhail Ajratovich

Korokina Lilija Viktorovna

Pokrovskij Mikhail Vladimirovich

Dates

2016-11-27Published

2014-11-28Filed