BRUNCKO, MILAN,DING, HONG,DOHERTY, GEORGE A.,ELMORE, STEVEN W.,HASVOLD, LISA,HEXAMER, LAURA,KUNZER, AARON R.,MANTEI, ROBERT A.,MCCLELLAN, WILLIAM J.,PARK, CHANG H.,PARK, CHEOL-MIN,PETROS, ANDREW M.,SO
申请号:
PE0013652014
公开号:
PE23162014A1
申请日:
2009.12.04
申请国别(地区):
PE
年份:
2015
代理人:
摘要:
Refers to a compound of formula (i), where: A2, B1, D1 and E1 are h, F, CL, BR, among others y1 is H, CN, NO2, among others Z1 is R26, R27, among others phenyl R26 is not merged or merged with sandy or heteroareno heteroareno R27 is not merged or merged with Sandy, among others. You.Preferred compounds are: 4 - ((4 - (4 - Chloro - 1,1 - biphenyl - 2 - yl) methyl) piperazin-1-yl) - 2 - phenoxy - (N - (4 - ((Tetrahydro - 2H - piran - 4 - methyl) amino) phenyl) sulfonyl) - 2 - fenoxibenzamida, 4 - (4 - ((4 - Chloro - 1,1 - biphenyl - 2 - yl) methyl) piperazin-1-yl) - N - ((3 - (4 - (nitro - tetrahydro - 2H - piran - 4 - methyl) amino) phenyl] sulfonyl) Benza Measure, among others. It also relates to a Pharmaceutical composition.These compounds are inhibitors of the activity of the anti apoptotic Proteins bcl-2 or BCL XL and are useful in the treatment of bladder cancer, includingREFERIDA A UN COMPUESTO DE FORMULA (I), DONDE: A2, B1, D1, E1 SON H, F, Cl, Br, ENTRE OTROS Y1 ES H, CN, NO2, ENTRE OTROS Z1 ES R26, R27, ENTRE OTROS R26 ES FENILO QUE NO ESTA FUSIONADO O FUSIONADO CON ARENO O HETEROARENO R27 ES HETEROARENO QUE NO ESTA FUSIONADO O FUSIONADO CON ARENO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 4-(4-((4-CLORO-1,1-BIFENIL-2-IL)METIL)PIPERAZIN-1-IL)-2-FENOXI-N-((4-((TETRAHIDRO-2H-PIRAN-4-ILMETIL)AMINO)FENIL)SULFONIL)-2-FENOXIBENZAMIDA, 4-(4-((4-CLORO-1,1-BIFENIL-2-IL)METIL)PIPERAZIN-1-IL)-N-((3-NITRO-4-((TETRAHIDRO-2H-PIRAN-4-ILMETIL)AMINO)FENIL)SULFONIL)BENZAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD DE LAS PROTEINAS ANTI-APOPTOTICAS BCL-2 O BCL-XL Y SON UTILES EN EL TRATAMIENTO DEL CANCER DE VEJIGA, ENTRE OTRAS