STEPHANIE KAY DODD,PASCAL FURET,ROBERT MARTIN GROTZFELD,DARRYL BRYNLEY JONES,PAUL MANLEY,ANDREAS MARZINZIK,XAVIER FRANCOIS ANDRE PELLE,BAHAA SALEM,JOSEPH SCHOEPFER
申请号：
ARP130101692
公开号：
AR091063A1
申请日:
2013.05.15
申请国别(地区):
AR
年份:
2014
代理人:
摘要：
Compounds capable of inhibiting the activity of BCR - ABL1 and Mutants thereof. Also provided is a process for the preparation of the compounds, Pharmaceutical preparations comprising such compounds and Methods of using such compounds in the treatment of cancers. Abl protein tyrosine kinase Abelson.Claim 1: The Compound of claim 1 of the formula (1) in which r u00b9 is pirazolilo； wherein Said pirazolilo is replaced or not replaced with 1 to 2 groups r u2076； R u00b2 is pirrolidinilo； wherein Said pirrolidinilo is replaced by a Group r u2077； r u00b3 is selected from H Idr u00f3geno and Halo； r u2074 is selected from - - - - sf u2085 and y u00b2 cf u2082 or r u2076 is independently at each occurrence； SEleccionado from Hydrogen, hydroxyl, Methyl, methoxyl, cyano, trifluoromethyl Methyl, Hydroxy, amino, Halo, fluoro -, Ethyl Ethyl and ciclopropilo； r u2077 is selected from hydroxyl, Methyl, methoxyl, Halo - methyl, hydroxyl, amino, methyl - amino amino -, methyl -, trifluoromethyl, 2 Hydrox Ipropan thiocyanatoacetate, metilocarbonil - Dimethyl amino, amino, 2-amino-3 - oxilo, carboxyl, metilbutanoil)Carbonyl methoxyl, fosfonooxilo, cyano and amino carbonyl； and selected from Ch and N； y u00b9 is selected from Ch and N； y u00b2 is selected from cf u2082 or s, and (OR) and u2080 u208b u2082； or is selected from Hydrogen, Methyl, Chlorine, Fluorine, difluorometilo and trifluoromethyl or s； Ales pharmaceutically acceptable to them.Compuestos capaces de inhibir la actividad de BCR-ABL1 y mutantes de los mismos. Además se proporciona un proceso para la preparación de compuestos de la presente, preparaciones farmacéuticas que comprenden tales compuestos y métodos de utilizar tales compuestos en el tratamiento de cánceres. ABL Tirosina quinasa de la proteína de Abelson. Reivindicación 1: El compuesto de la reivindicación 1 de la fórmula (1) en el cual R¹ es pirazolilo； en donde dicho pirazolilo es sustituido o no sustituido con 1 a 2 grupos R⁶； R² es pirrolidinilo； en donde
