发明名称 OXAZOLIDEN-1-ONE DERIVATIVES, AND DRUG BASED THEREON
摘要 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 OR wherein R is -CH/C<SB>6</SB>H<SB>5</SB>/<SB>2</SB>-/CH<SB>2</SB>/<SB>n</SB>C<SB>6</SB>H<SB>5</SB>, lower alkyl, hydrogen, /CH<SB>2</SB>/<SB>n</SB>NHCOCH<SB>3</SB>-/CH<SB>2</SB>/<SB>n</SB>NH<SB>2</SB>-/CH<SB>2</SB>/<SB>n</SB>SOCH<SB>3</SB>,, -/CH/<SB>n</SB>CN, -/CH<SB>2</SB>/<SB>n</SB>SCH<SB>3</SB>,, /CH<SB>2</SB>/<SB>n</SB>SO<SB>2</SB>CH<SB>3</SB>-CO- lower alkyl, -COC<SB>6</SB>H<SB>5</SB> optionally substituted by oxazolidinyl; or substituted =CR<SP>2</SP>R wherein R is hydrogen or lower alkyl; R is hydrogen, nitrile, lower alkyl, phenyl or COO-lower alkyl; or substituted -/CH<SB>2</SB>/<SB>n</SB>R wherein R is nitrile, amino, -NHCOCH<SB>3</SB>-,, -COC<SB>6</SB>H<SB>4</SB> hal, phenyl or hydroxy group; or substituted -COR wherein R is lower alkyl, -CH=CH-C<SB>6</SB>H<SB>5</SB>,, -C<SB>6</SB>H<SB>5</SB>CF<SB>3</SB>,, -O-C/CH<SB>3</SB>/<SB>3</SB> or -O-lower alkyl; or substituted -NR<SP>6</SP>R<SP>7</SP>, wherein R is hydrogen or -COCH<SB>3</SB>, R is -COCH<SB>3</SB> benzyl or -/CH<SB>2</SB>/<SB>n</SB>NHCOC<SB>6</SB>H<SB>4</SB> hal;; n is 1-3; Y<SP>1</SP>- is -CH= or -N=; Y is -CH=, -C(OH)=, -C/NO<SB>2</SB>/, -C/NH<SB>2</SB>/, -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
申请公布号 RU2133743(C1) 申请公布日期 1999.07.27
申请号 RU19940043806 申请日期 1994.12.13
申请人 F.KHOFFMANN-LJA ROSH AG 发明人 JANOS BORGULIA;KHANS BRUDERER;ROLAND JAKOB-RETNE;STEFAN REVER
分类号 A61K31/42;A61K31/421;A61K31/422;A61K31/425;A61K31/44;A61K31/445;A61P25/00;A61P25/20;A61P25/22;A61P25/24;A61P25/26;A61P25/28;C07D263/24;C07D413/04;C07D413/10;C07D413/14;(IPC1-7):C07D263/24 主分类号 A61K31/42
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