发明名称 N-Acylamino Benzyl Ether Derivatives
摘要 This invention relates to N-acylamino aryl derivatives of the general formula (I), wherein R<1> is halogen, halogen-(C1-C6)-alkyl, cyano, C1-C6-alkoxy or halogen-(C1-C6)-alkoxy; R<21>, R<22>, R<23> and R<24> 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; R<3> is hydrogen or C1-C3-alkyl; R<4>, R<5> independently from each other are selected from the group consisting of hydrogen, C1-C6-alkyl, C1-C6-alkoxy or -COO(C1-C6)alkyl; or R<4> and R<5> form together with the C-atom to which they are attach a C3-C7-cycloalkyl ring; R<6> is -CO-NR<7>R<8>; -COO(C1-C6)-alkyl, -CN, -NR2 or -NHC(O)R; R<7> and R<8> 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 -C=C-; 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 Alzheimer's disease or senile dementia.
申请公布号 JO2541(B) 申请公布日期 2010.09.05
申请号 JO20030000058 申请日期 2003.05.28
申请人 F. HOFFMANN-LA ROCHE AG 发明人 SYNESE JOLIDON;ROSA MARIA RODRIGUEZ SARMIENTO;ANDREW WILLIAM THOMAS;RENE WYLER
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