BENNETT, MICHAEL JOHN,BETANCORT, JUAN MANUEL,VEAL, JAMES MARVIN,KALDOR, STEPHEN W.,STAFFORD, JEFFREY ALAN,BOLOOR, AMOGH
申请号：
PE0005202016
公开号：
PE10652016A1
申请日:
2014.10.17
申请国别(地区):
PE
年份:
2016
代理人:
摘要：
The present Invention relates to a compound of formula I, where R2 is CH3, CH2CH3, among others X5 is C - R5 or R6 is C - N X6 or X7 N c - or n R7 R8 x8 is C - or N R5 is H, halogen, among others R6 h, Halogen, among others R7 is H, halogen, among others R8 is H, halogen, among others ras A group of the formula (b) where it is n, among others R13 and - Where is Z and is link, CH2,Among others Z is \u2013so2r21, among others X3 is n, among others x4 is n, among others r1 is alkyl, among others. It also refers to a compound of formula II, where R2 is alkyl, cycloalkyl, among others X6 is C - H OR N R5 X5 is c or n where R5 is Hydrogen, halogen, among others R4 is Hydrogen, halogen, among others.Preferred compounds are: N - [3 - (4 - methyl - 2 - methyl - 1 - oxoisoquinolin - 4-yl) phenyl] methanesulfonamide 4 - [2 - (Cyclopropylmethoxy) - 5 - metilisoquinolin metilsulfonilfenil] - 2 - 1 - ona, among others.These compounds are involved in epigenetic Regulation mediated by inhibition of recognition of bromodomain acetyl lysine regions of Proteins such as histones, being useful for the treatment of cancerLa presente invencion se refiere a un compuesto de formula I, donde: R2 es CH3, CH2CH3, entre otros X5 es C-R5 o N X6 es C-R6 o N X7 es C-R7 o N X8 es C-R8 o N R5 es H, halogeno, entre otros R6 es H, halogeno, entre otros R7 es H, halogeno, entre otros R8 es H, halogeno, entre otros RA es un grupo de la formula (B) donde X2 es N , entre otros R13 es Y-Z donde Y es enlace, CH2, entre otros Z es –SO2R21, entre otros X3 es N, entre otros X4 es N, entre otros R21 es alquilo, entre otros. Tambien se refiere a un compuesto de formula II, donde: R2 es alquilo, cicloalquilo, entre otros X6 es C-H o N X5 es C-R5 o N en donde R5 es hidrogeno, halogeno, entre otros R6 es hidrogeno, halogeno, entre otros. Son compuestos preferidos: N-[4-metil-3-(2-metil-1-oxoisoquinolin-4-il)fenil]metanosulfonamida 4-[2-ciclopropilmetoxi)-5-metilsulfonilfenil]-2-metilisoquinolin-1-ona, entre otros.
