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：
PE2012002134
公开号：
PE20130647A1
申请日:
2011.05.05
申请国别(地区):
PE
年份:
2013
代理人:
摘要：
It refers to a formula compound (I), wherein: X and Z are respectively h, C1-C8 tar, c2-c8 alquenilo c3-c8, cycloquilo c3-c8, etc.； and are h, halo； R1 is C1-C8 tar, isopropyl tar, arilo, isopropyl tar, etc.； R2 is h, trifluorometyl, alcox, c1-lease C8 tar, halogen substitute or 1-2 groups selected from amino group and minors. R3 is h, cyanogen, trifluoroide, halogen, etc.； R6 is h, halogen, cyanogen, trifluoroenzene, amino group, arilo, etc.； R7 is h, C1-C3 tar or alcox. 1. The preferred compound is n - ((4,6-dimethyl-2-oxo-1,2-dihydropyridine-3-il) methyl) - 1-isopropyl-3-methyl-6 - (6 - (4-methylpyridine-1-il) pyridine-3-il) - 1h-indol-4-carboxamida；(R) - 6-bromo-1 - (sec-util) - N - (4,6-dimethyl-2-oxo-1,2-dihydropyridine-3-il) methyl) - 3-methyl-1h-indoli-4-anthrax amide, etc. Except for a pharmaceutical composer The compound is a hydroxybutyltransferase inhibitor for 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.
