发明名称 N-ACYLAMINOBENZENE DERIVATIVES AS SELECTIVE MONOAMINE OXIDASE B INHIBITORS
摘要 This invention relates to N-acylamino aryl derivatives of the general formula (I), wherein R1 is halogen, halogen-(C1-C6)-alkyl, cyano, C1-C6-alkoxy or halogen-(C1-C6)-alkoxy; R21, R22, R23 and R24 independently from each other are selected from the group consisting of hydrogen, (C1-C6)-alkyl, halogen, halogen-(C1-C6)-alkyl, hydroxy, C1-C6-alkoxy or -CHO; R3 is hydrogen or C1-C3-alkyl; R4, R5 independently from each other are selected from the group consisting of hydrogen, C1-C6-alkyl, C1-C6-alkoxy or -COO(C1-C6) alkyl; or R4 and R5 form together with the C-atom to which they are attach a C3-C7-cycloalkyl ring; R6 is -CO-NR7R8; -COO(C1-C6)- alkyl, -CN, -NR2 or -NHC(O)R; R7 and R8 independently from each other are selected from the group consisting of hydrogen, C1-C6- alkyl, NH2 or hydroxy; R is hydrogen or C1-C6-alkyl; n is 0, 1, 2 or 3. X is -CHRO, -OCHR, -CH2S-, -SCH2-, -CH2CH2-, -CH=CH- or -CˆC-; and to pharmaceutically active acid addition salts thereof. It has been found that the compounds of general formula (I) are selective monoamine oxidase B inhibitors and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B inhibitors, for example for the treatment of AlzheimerâÇÖs disease or senile dementia.
申请公布号 RS101204(A) 申请公布日期 2007.02.05
申请号 YU2004P001012 申请日期 2003.05.21
申请人 F.HOFFMANN-LA ROCHE AG 发明人 JOLIDON SYNESE;RODRIGUEZ SARMIENTO R.M.;THOMAS ANDREW WILLIAM;WYLER RENE
分类号 A61P3/00;C07C233/25;A61K31/15;A61K31/167;A61K31/216;A61K31/275;A61P3/04;A61P25/00;A61P25/16;A61P25/18;A61P25/22;A61P25/24;A61P25/28;A61P25/30;A61P25/32;A61P25/34;A61P29/00;A61P43/00;C07C231/02;C07C233/15;C07C233/33;C07C233/60;C07C235/16;C07C237/04;C07C237/22;C07C243/14;C07C243/28;C07C255/19;C07C255/23;C07C255/25;C07C255/58;C07C259/06;C07C323/41 主分类号 A61P3/00
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