BRACKLEY, JAMES,BURGESS, JOELLE LORRAINE,GRANT, SETH,JOHNSON, NEIL,KNIGHT, STEVEN D.,LAFRANCE, LOUIS,MILLER, WILLIAM H.,NEWLANDER, KENNETH,ROMERIL, STUART,ROUSE, MEAGAN B.,TIAN, XINRONG,VERMA, SHARAD
申请号：
PE0021342012
公开号：
PE06472013A1
申请日:
2011.05.05
申请国别(地区):
PE
年份:
2013
代理人:
摘要：
Refers to a compound of formula (i) wherein: X and Z are each h, alkyl C8 alquenilo C1, C2 - C3 - C8 C8, cycloalkyl, among others and it is Halo r1 is H, alkyl C8 heterocicloalquilo, C1 -, aryl, heteroaryl, R2 is H, among others trifluoromethyl alkyl, alkoxy, C1, C8, Halo substituted with 1 - or not 2 selected between amino groups and alquilamino R3 is H, cyano, trifluoromethyl, haloAmong others, R6 h, Halo, cyano, trifluoromethyl, aryl, amino, among others R7 is H, alkyl or alkoxy C1 - C3.Preferred compounds are: N - (4,6 - dimethyl - 2 - oxo - 1.2 - dihidropiridin - 3 - yl) methyl) - 1 - isopropyl - 3 - methyl - 4 - (6 - (4 - metilpiperazin - 1 - il) pyridin-3-yl) - 1H indole - 3 - carboxamide 6 - bromo - (R) - 1 - (SEC Butyl) - N - (4,6 - dimethyl - 2 - oxo - 1.2 - dihidropiridin - 3 - yl) methyl) - 1H indole - 3 - methyl - 4 - carboxamide among others. In addition to such a Pharmaceutical composition.This Compound is an inhibitor of Histone lysine METHYLTRANSFERASe useful in cancer treatment.SE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE: X y Z SON CADA UNO H, ALQUILO C1-C8, ALQUENILO C2-C8, CICLOALQUILO C3-C8, ENTRE OTROS Y ES H, HALO R1 ES ALQUILO C1-C8, HETEROCICLOALQUILO, ARILO, HETEROARILO, ENTRE OTROS R2 ES H, TRIFLUOROMETILO, ALCOXI, ALQUILO C1-C8, halo SUSTITUIDO o no CON 1-2 GRUPOS SELECCIONADOS ENTRE AMINO Y ALQUILAMINO R3 ES H, CIANO, TRIFLUOROMETILO, HALO, entre otros R6 ES H, HALO, CIANO, TRIFLUOROMETILO, AMINO, ARILO, ENTRE OTROS R7 ES H, ALQUILO C1-C3 O ALCOXI. SON COMPUESTOS PREFERIDOS: N-((4,6-DIMETIL-2-OXO-1,2-DIHIDROPIRIDIN-3-IL)METIL)-1-ISOPROPIL-3-METIL-6-(6-(4-METILPIPERAZIN-1-IL)PIRIDIN-3-IL)-1H-INDOL-4-CARBOXAMIDA (R)-6-BROMO-1-(SEC-BUTIL)-N-((4,6-DIMETIL-2-OXO-1,2-DIHIDROPIRIDIN-3-IL)METIL)-3-METIL-1H-INDOL-4-CARBOXAMIDA ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN INHIBIDOR DE HISTONA-LISINA METILTRANSFERASA UTIL EN EL TRATAMIENTO CONTRA EL CANCER.
