FOOTE, KEVIN MICHAEL,NISSINK, JOHANNES WILHELMUS MARIA
申请号：
PE0012592011
公开号：
PE08942011A1
申请日:
2009.12.22
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Refers to indole compounds of pyrimidine Derivatives of formula (i) where the ring is cycloalkyl or heterocyclic (C3 and C6) 4-6 members ILO (R1 is - 4 - 3 - 4 - Sulfate, ILO, ILO dimetilmorfolin - 3.5 - 4 - or 8 - oxa - 3-azabicyclo [3,2,1] octan-3-yl - 3 - ilo R2 and R5 are H or h R3 is Methyl R4 is H, meti So, Fluorine, Chlorine, cn or methoxy R6 R is Methyl, Ethyl, propyl or ciclopropilo -.Preferred compounds are: 4 - (4 - [1 - (methylsulfonyl) cyclopropyl] - 6 - 4 - (2 - ilpirimidin - il) - 1H indole 6 - Chloro - 5 - (4 - [1 - (methylsulfonyl) cyclopropyl] - 6 - 4 - 2 (IL - ilpirimidin} - 1H indole 4 - (4 - [(3S) - 3 - 4 - sulfate il] - 6 - [1 - (methylsulfonyl) ciclopentil] pyrimidine 2 - il) - 1H indole among others. It also relates to a Pharmaceutical composition.These compounds are inhibitors of Protein related kinase ataxia telangiectasia mutated and Rad - 3 (ATR) being useful in the treatment of cancerSE REFIERE A COMPUESTOS DERIVADOS DE PIRIMIDIN INDOL DE FORMULA (I) DONDE EL ANILLO A ES CICLOALQUILO(C3-C6) O HETEROCICLICO DE 4-6 MIEMBROS R1 ES MORFOLIN-4-ILO, 3-METILMORFOLIN-4-ILO, 3,5-DIMETILMORFOLIN-4-ILO O 8-OXA-3-AZABICICLO[3,2,1]OCTAN-3-ILO R2 Y R5 SON H R3 ES H O METILO R4 ES H, METILO, FLUORO, CLORO, CN O METOXI R6 ES METILO, ETILO, i-PROPILO O CICLOPROPILO. SON COMPUESTOS PREFERIDOS: 4-{4-[1-(METILSULFONIL)CICLOPROPIL]-6-MORFOLIN-4-ILPIRIMIDIN-2-IL}-1H-INDOL 6-CLORO-4-{4-[1-(METILSULFONIL)CICLOPROPIL]-6-MORFOLIN-4-ILPIRIMIDIN-2-IL}-1H-INDOL 4-{4-[(3S)-3-METILMORFOLIN-4-IL]-6-[1-(METILSULFONIL)CICLOPENTIL]PIRIMIDIN-2-IL}-1H-INDOL ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA PROTEINA QUINASA RELACIONADA CON ATAXIA-TELANGIECTASIA MUTADA Y RAD-3 (ATR) SIENDO UTILES EN EL TRATAMIENTO DE CANCER
