JAHNKE, Wolfgang,SCHOEPFER, Joseph,SALEM, Bahaa,PELLE, Xavier Francois Andre,DODD, Stephanie Kay,MANLEY, Paul,JONES, Darryl Brynley,GROTZFELD, Robert Martin,FURET, Pasca,MARZINZIK, Andreas
申请号：
PE0010142016
公开号：
PE14162016A1
申请日:
2013.05.09
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
The present Invention relates to Derivatives of benzamide compounds of formula (i), or pharmaceutically acceptable salts of thereof, wherein: R1 is pirazolilo optionally substituted with 1 to 2 groups R6, R7 R2 is replaced with pirrolidinilo R3 is H or Halogen R4 is sedan - CF2 - or - y2 y3 R6 h, Among others R7 is hydroxyl, hydroxyl, Methyl, among others and Y1 and Y2 are CF2 is n or CH,- or or - S (o) 0 - 2 Y3 h, Chlorine, among others. It is a Preferred compound: (R) - N - (4 - (chloro difluoro methoxy) - phenyl) - 6 - (2 - hydroxy - pyrrolidin-1-yl) - 5 - (1h pyrazole - 5 - il) - Nicotinamide, among others. It also relates to a Pharmaceutical composition.These compounds inhibit the Enzymatic activity of the Protein Tyrosine Kinase Abelson, ABL1, ABL2 and chimeric protein BCR - ABL1, being useful in the treatment of cancerLa presente invencion se refiere a compuestos derivados de benzamida de formula (I) o sales farmaceuticamente aceptables de los mismos, donde: R1 es pirazolilo opcionalmente sustituido con 1 a 2 grupos R6 R2 es pirrolidinilo sustituido con R7 R3 es H o halogeno R4 es -SF5 o -Y2-CF2-Y3 R6 es H, hidroxilo, entre otros R7 es hidroxilo, metilo, entre otros Y e Y1 son CH o N Y2 es CF2, -O- o S(O)0-2 Y3 es H, cloro, entre otros. Es un compuesto preferido: (R)-N-(4-(cloro-difluoro-metoxi)-fenil)-6-(3-hidroxi-pirrolidin-1-il)-5-(1H-pirazol-5-il)-nicotinamida, entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos inhiben la actividad enzimatica de cinasa de tirosina de la proteina de Abelson: ABL1, ABL2 y la proteina quimerica BCR-ABL1, siendo utiles en el tratamiento del cancer
