OXAZOLIDEN-1-ONE DERIVATIVES, AND DRUG BASED THEREON Russian patent published in 1999 - IPC

Abstract RU 2133743 C1

FIELD: pharmaceutical industry. SUBSTANCE: described are new oxazolidine-2-one derivatives of general formula I wherein R is lower alkyl; X is cycloalkenyl; bicyclo [2,2,1]-hept-2-yl optionally substituted by phenyl-2-oxo- 5-methoxymethyloxazolidinyl; bicyclo [2,2,1] hept 5-en-2- yl; adamantyl; or cycloalkyl or piperidine optionally mono-or multiple substituted by halogen, amino, lower alkyl, nitrile, oxo, hydroxyimino, ethylenedioxy or OR1 wherein R1 is -CH/C6H5/2-/CH2/nC6H5, lower alkyl, hydrogen, /CH2/nNHCOCH3-/CH2/nNH2-/CH2/nSOCH3,, -/CH/nCN, -/CH2/nSCH3,, /CH2/nSO2CH3-CO- lower alkyl, -COC6H5 optionally substituted by oxazolidinyl; or substituted =CR2R3 wherein R2 is hydrogen or lower alkyl; R3 is hydrogen, nitrile, lower alkyl, phenyl or COO-lower alkyl; or substituted -/CH2/nR4 wherein R4 is nitrile, amino, -NHCOCH3-,, -COC6H4 hal, phenyl or hydroxy group; or substituted -COR5 wherein R5 is lower alkyl, -CH=CH-C6H5,, -C6H5CF3,, -O-C/CH3/3 or -O-lower alkyl; or substituted -NR6R7, wherein R6 is hydrogen or -COCH3, R7 is -COCH3 benzyl or -/CH2/nNHCOC6H4 hal;; n is 1-3; Y1- is -CH= or -N=; Y2 is -CH=, -C(OH)=, -C/NO2/, -C/NH2/, -C(hal) or -N=, and also pharmaceutically acceptable salts of main compounds of formula I with acids. These compound are capable of inhibiting monoaminooxidase. Also described is drug based on compounds of formula I which is useful in treating states of depression, panic and hear. EFFECT: improved properties of the drug. 24 cl, 105 ex

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RU 2 133 743 C1

Authors

Janos Borgulia

Khans Bruderer

Roland Jakob-Retne

Stefan Rever

Dates

1999-07-27Published

1994-12-13Filed