S-SUBSTITUTED [(HETERO)ARYL]ALKYLISOTHIOUREAS, PRODUCTION THEREOF, PHARMACEUTICAL COMPOSITION, INVESTIGATION OF GLUTAMATERGIC SYSTEM, TREATMENT METHODS (VARIANTS) Russian patent published in 2005 - IPC

Abstract RU 2252936 C2

FIELD: organic chemistry, pharmaceutical industry, medicine.

SUBSTANCE: invention relates to new derivatives of S-substituted N-1-[(hetero)aryl]alkyl-N'-1-[(hetero)aryl]alkylisothioureas of general formula I

in form of free base and salts with pharmaceutically accepted acids, as well as racemate, individual optical isomers or mixture thereof. In formula R1, R2, R3, R4, Y and Z are as described in specification. Compounds of present invention are capable to potentiate (positively modulate) AMPA/KA glutamate receptors and simultaneously to block transmembrane currents induced by activation of NMDA glutamate receptors. Also disclosed are method for production of said compounds, including optical isomers; pharmaceutical composition; method for investigation of glutamatergic system, and method for Alzheimer's disease, treatment; as well as method for extreme retentiveness of memory by administering of effective amount of claimed compounds.

EFFECT: new pharmaceutically active compounds for Alzheimer's disease treatment.

23 cl, 1 tbl, 11 ex

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RU 2 252 936 C2

Authors

Tkachenko S.E.

Proshin A.N.

Dmitriev M.Eh.

Lermontova N.N.

Grigor'Ev V.V.

Bachurin S.O.

Zefirov N.S.

Dates

2005-05-27Published

2002-12-05Filed