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DERIVADOS DE ISOINDOL COMO INHIBIDORES DE BACE
专利权人:
ASTRAZENECA AB
发明人:
HOLENZ, JORG,KARLSTROM, SOFIA,KOLMODIN, KARIN,LINDSTROM, JOHAN,RAKOS, LASZLO,ROTTICCI, DIDIER,SODERMAN, PETER,SWAHN, BRITT-MARIE,VON BERG, STEFAN
申请号:
PE0010342011
公开号:
PE08752011A1
申请日:
2009.11.13
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Refers to compounds derived from 4 - fluoro - 1H - isoindol - 3 - Amine of formula (i) wherein R1 is CN, halogen, alkyl (C1 - C6), alquenilo (C2 - C6), among others a is aryl or heteroaryl optionally replaced with R5, wherein R5 is Halogen, NS, cycloalkyl (C3 and C6), among others b is aryl or heteroaryl Optionally replaced with R6, wherein R6 is Halogen, Hydroxy or CN c is H, halogen,Cycloalkyl (C3 and C6), heterociclilo, among others M is 0 to 2. Preferred compounds are: 5 - (3 - (3 - amino - 4 - fluoro - 1 - (2 - metilpiridin - 4-yl) - 1H - isoindol - 1 - il) - 4-fluorophenyl) nicotinonitrilo 4 - fluoro - 1 - (2-fluoro-5 - (5 - fluoropiridin - 3 - il) phenyl) - 1 - (2 - metilpiridin - 4-yl) - 1H - isoindol - 3 - 4 - fluoro - Amine 1 - (2-fluoro-5 - (pyrimidin-5-yl) phenyl) - 1 - (2 - (trifluoromethyl) pyridin-4-yl Isoindol) - 1H - 3 - Amine among others.It also relates to a Pharmaceutical composition. These compounds are inhibitors of the B - secretase (BACE) being useful in the treatment of Down Syndrome, Alzheimers disease, senile dementia, cerebral Amyloid angiopathy,SE REFIERE A COMPUESTOS DERIVADOS DE 4-FLUORO-1H-ISOINDOL-3-AMINA DE FORMULA (I) DONDE R1 ES HALOGENO, CN, ALQUILO(C1-C6), ALQUENILO(C2-C6), ENTRE OTROS A ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON R5, EN DONDE R5 ES HALOGENO, CN, CICLOALQUILO(C3-C6), ENTRE OTROS B ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON R6, EN DONDE R6 ES HALOGENO, HIDROXI O CN C ES H, HALOGENO, CICLOALQUILO(C3-C6), HETEROCICLILO, ENTRE OTROS m ES DE 0 A 2. SON COMPUESTOS PREFERIDOS: 5-(3-(3-AMINO-4-FLUORO-1-(2-METILPIRIDIN-4-IL)-1H-ISOINDOL-1-IL)-4-FLUOROFENIL)NICOTINONITRILO 4-FLUORO-1-(2-FLUORO-5-(5-FLUOROPIRIDIN-3-IL)FENIL)-1-(2-METILPIRIDIN-4-IL)-1H-ISOINDOL-3-AMINA 4-FLUORO-1-(2-FLUORO-5-(PIRIMIDIN-5-IL)FENIL)-1-(2-(TRIFLUOROMETIL)PIRIDIN-4-IL)-1H-ISOINDOL-3-AMINA ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA B-SECRETASA (BACE) SIENDO UTILES EN E
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