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Substituted dibenzoazepine and benzodiazepine derivatives useful as gamma-secretase inhibitors
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
FLOHR, ALEXANDER,GALLEY, GUIDO,JAKOB-ROETNE, ROLAND,KITAS, ERIC ARGIRIOS,PETERS, JENS-UWE,WOSTL, WOLFGANG
申请号:
ES04787028
公开号:
ES2548720T3
申请日:
2004.09.27
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
Compounds of general formula I ** Formula ** wherein R 1 is - (CHR ') q-aryl or - (CHR') q-heteroaryl, which are unsubstituted or mono, di- or tri-substituted by lower alkyl, alkoxy lower, CF3 or halogen, or is lower alkyl, lower alkenyl, - (CH2) n-Si (CH3) 3, - (CH2) nO-lower alkyl, - (CH2) nS-lower alkyl, - (CH2) q- cycloalkyl, - (CH2) n- [CH (OH)] m- (CF2) p-CHqF (3-q), or is - (CH2) n-CR2-CF3, where the two radicals R form together with the carbon atom a cycloalkyl ring; R 'is hydrogen or lower alkyl; n is 1, 2 or 3; m is 0 or 1; p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2 or 3; R2 is hydrogen or lower alkyl; R3 is hydrogen, lower alkyl, -CH2CF2CF3, CH2CF3, (CH2) 2CF3, CF3, CHF2, CH2F or is aryl, optionally mono, di or tri-substituted by halogen, or is - (CH2) nNR5R6, where R5 and R6 they are independently of each other hydrogen or lower alkyl; R4 is one of the following groups 20 a) or b) wherein R7 is hydrogen, lower alkyl, - (CH2) n-CF3 or - (CH2) n-cycloalkyl; R8 is hydrogen, lower alkyl, -C (O) -phenyl, -C (O) -alkyl, -C (O) O- (CH2) n-cycloalkyl, -C (O) O- (CH2) n- lower alkyl, -C (O) NH- (CH2) n-lower alkyl or -C (O) NH- (CH2) n-cycloalkyl; R9 is hydrogen, lower alkyl, - (CH2) n-cycloalkyl or - (CH2) n-CF3; wherein the term "lower" in "lower alkyl" or "lower alkoxy" means that the group contains 1 to 10 carbon atoms and the term "lower" in lower alkenyl "means that the group contains 2 to 10 atoms of carbon; and pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof.Compuestos de fórmula general I**Fórmula** en donde R1 es -(CHR')q-arilo o -(CHR')q-heteroarilo, que están sin sustituir o mono, di- o tri-sustituidos por alquilo inferior, alcoxilo inferior, CF3 o halógeno, o es alquilo inferior, alquenilo inferior, -(CH2)n-Si(CH3)3, -(CH2)n-O-alquilo inferior, -(CH2)n-S-alquilo inferior, -(CH2)q-cicloalquilo, -(CH2)n-[CH(OH)]m-(CF2)p-CHqF(3-q), o es -(CH2)n-CR2- CF3, en donde los dos radicales R
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