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公开(公告)号:CA2135861A1
公开(公告)日:1995-06-14
申请号:CA2135861
申请日:1994-11-15
Applicant: HOFFMANN LA ROCHE
Inventor: BORGULYA JANOS , BRUDERER HANS , JAKOB-ROETNE ROLAND , ROEVER STEPHEN
IPC: 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
Abstract: The invention is concerned with oxazolidin-2-one derivatives of the general formula I wherein R signifies hydrogen or lower alkyl; X signifies cycloalkenyl; bicyclo¢2.2.1!hept-2-yl, optionally substituted by phenyl-2-oxo-5-methoxymethyl-oxazolidinyl; bicyclo¢2.2.1!-hept-5-en-2-yl; adamantyl; or cycloalkyl or piperidinyl, optionally mono- or multiply-substituted by halogen, amino, lower alkyl, nitrilo, an oxo group, hydroxyimino, ethylenedioxy or by -OR1, in which R1 signifies -CH(C6H5)2, -(CH2)nC6H5, lower alkyl, hydrogen, -(CH2)nNHCOCH3, -(CH2)nNH2, -(CH2)nCN,- (CH2)nSCH3, -(CH2)nSO2CH3, -CO-lower-alkyl, -COC6H5, optionally substituted by an oxazolidinyl group; or by =CR2R3, in which R2 signifies hydrogen or lower alkyl; R3 signifies hydrogen, nitrilo, lower alkyl, phenyl or COO-lower-alkyl; or by -(CH2)nR4, in which R4 signifies nitrilo, amino, -NHCOCH3,-COC6H5Hal, phenyl or hydroxy; or by -COR5, in which R5 signifies lower alkyl, -CH=CH-C6H5,-C6H5CF3, -O-C(CH3)3 or -O-lower-alkyl; or by -NR6R7, in which R6 signifies hydrogen or-COCH3; R7 signifies -COCH3, benzyl or-(CH2)nNHCOC6H4Hal; n signifies 1-3; y1 signifies -CH= or -N=; and y2 signifies-CH=, -C(OH)=, -C(NO2)=, -C(NH2)=, -C(Hal)= or -N=, as well as pharmaceutically acceptable salts of basic compounds of formula I with acids. These novel compounds and their pharmaceutically acceptable salts can be used for the prevention or control of depressive states, panic and anxiety states, cognitive disorders and neurodegenerative diseases such as Parkinson's disease and Alzheimer's disease.
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公开(公告)号:HK1257166A1
公开(公告)日:2019-10-18
申请号:HK18116047
申请日:2018-12-13
Applicant: HOFFMANN LA ROCHE
Inventor: GAVELLE OLIVIER , GRETHER UWE , NETTEKOVEN MATTHIAS , ROEVER STEPHEN , ROGERS-EVANS MARK , ROMBACH DIDIER
IPC: A61K20060101 , C07D20060101 , A61P20060101 , C07C20060101
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