COMPUESTO DE (6S,9AS)-N-BENCIL-6-[(4-HIDROXIFENIL)METIL]-4,7-DIOXO-8-({6-[3-(PIPERAZIN-1-IL)AZETIDIN-1-IL]PIRIDIN-2-IL}METIL)-2-(PROP-2-EN-1-IL)-OCTAHIDRO-1H-PIRAZINO[2,1-C][1,2,4]TRIAZINA-1-CARBOXAMIDA

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专利权人:

EISAI RandD MANAGEMENT CO.; LTD.

发明人:

INOUE, SATOSHI,YAMAMOTO, YUJI,ISO, KENTARO

申请号：

PE0007112016

公开号：

PE09322016A1

申请日:

2014.12.22

申请国别(地区):

PE

年份:

2016

代理人:

摘要：

The present Invention relates to compounds of formula (i) which has activity Modulation of the Wnt pathway for Cancer Treatment. Where is alquiloc1 - 6: R1, R2 and R3 are H or alkyl of C1 - 6 x2, X3 and X4 and X5 is Halogen are H or H or P (= o) (OH) 2.Preferred compounds are (6S, \u2013n 9aS) - Benzyl - 8 - ((4 - (3 - (4 - Ethyl piperazin-1-yl) azetidin - 1 - il) pyridin-2-yl) methyl) - 6 - ((2-fluoro-4 - hidroxfenil) methyl) - 4.7 - [2 - (prop - 2 - in - 1 - il) - octahidro - 1H - 2.1 - pirazino [c] [1,2,4] triazine - 1 - carboxamide (6S, 9aS) - N - Benzyl - 8 - 6 - ((3 - (4 - (ethyl - piperazin - 1 - I L) azetidin - 1 - il) pyridin-2-yl) methyl) - 6 - ((4 - hydroxyphenyl) methyl) - 47 - [2 - (prop - 2 - in - 1 - il) - octahidro - 1H - 2.1 - pirazino [c] [1,2,4] triazine - 1 - carboxamide among othersLa presente invencion se refiere a compuestos de formula (I) que tiene actividad de modulacion de la via Wnt para tratamiento de cancer. Donde: R1 es alquiloC1-6 R2 y R3 son H o alquilo C1-6 X2, X3 y X4 son H o halogeno y X5 es H o P(=O)(OH)2. Son compuestos preferidos: (6S, 9aS) –N- bencil -8-((6-(3-(4-etil-piperazin-1-il) azetidin-1-il)piridin-2-il)metil)-6-((2-fluoro-4-hidroxfenil)metil)-4,7-dioxo-2- (prop-2-en-1-il) - octahidro -1H- pirazino[2,1-c][1,2,4] triazina-1-carboxamida (6S,9aS) -N- bencil-8 -((6- (3- (4-etil-piperazin-1-il)azetidin-1-il)piridin-2-il)metil)-6 -((4- hidroxifenil)metil)-4,7-dioxo-2-(prop-2-en-1-il) - octahidro -1H-pirazino[2,1-c][1,2,4] triazina-1-carboxamida entre otros

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