ORGANIC COMPOUNDS Russian patent published in 2022 - IPC C07D471/16 A61K31/4985 A61P25/00 

Abstract RU 2785871 C2

FIELD: medicine.

SUBSTANCE: invention relates to a pharmaceutical composition for the treatment of a disease with involvement of one of paths of serotonin 5-HT2A, dopamine D2, and/or serotonin reuptake transporter (hereinafter – SERT), including a compound of the formula I: , where: R1 is CH3 or CD3; R2 and R3, each independently, is H or D; R4 and R5, each independently, is H or D; provided that R2, R3, R4, and R5 are not all H, when R1 is CH3, and where D is deuterium in a free form or in the form of pharmaceutically acceptable salt, in a combination or association with a pharmaceutically acceptable solvent or carrier, where the composition contains therapeutically effective amount of a compound of the formula I from 1 to 100 mg. The invention also relates to a method for the treatment or prevention of a disorder of the central nervous system with involvement of 5-HT2A receptor, SERT, and/or paths including signal systems D1/D2 of dopamine receptors, including administration to a patient who needs it of therapeutically effective amount of the compound of the formula I.

EFFECT: invention provides compounds, which partially limit metabolism of ketone and/or N-methyl substitute by introduction of deuterium atoms at different positions.

9 cl, 1 tbl

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RU 2 785 871 C2

Authors

Mates, Sharon

Li, Peng

Wennogle, Lawrence P.

Davis, Robert

Dates

2022-12-14Published

2015-04-03Filed