BRUNCKO, MILAN,DAI, YUJIA,DING, HONG,DOHERTY, GEORGE A.,ELMORE, STEVEN W.,HASVOLD, LISA A.,HEXAMER, LAURA,KUNZER, AARON R.,MANTEI, ROBERT A.,MCCLELLAN, WILLIAM J.,PARK, CHANG H.,PARK, CHEOL-MIN,PETROS
申请号：
PE0011472011
公开号：
PE01362012A1
申请日:
2009.12.04
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Relates to Heterocyclic compounds of formula (i), where A1 is C (A2) or n, where A2 is H, NHC (NH2), so2nh2, among others B1 is H, C (o) nhnoh, C (NH) NH2, CN, among others D1 is H, so2nh2, CF3, C (o) Oh, among others E1 is H, C (NH) NH2, F, CN, among others y1 is H, NO2, CN, Z1 is ocf3, among others R26, R27, where phenylene R26 is not merged or merged with BenzeneAmong others, heteroarileno R27 is not merged or merged with Benzene, among others Z2 is R28, R29, among others, where phenylene R28 is not merged or merged with Benzene, among others heteroarileno R29 is not merged or merged with Benzene, among others Z1A panel rc-z2a and both are absent or Form An ch2ch2 together CH2, among others L1 is C (o) NH, NH so2nh, C (n), among others Z3 is R38, R39,Among others, where it is FUSED or unfused R38 phenyl benzene, among others R39 is not merged or heteroaryl FUSED benzene, among others.Preferred compounds are: 4 - ((4 - (4 - Chloro - 1,1 - biphenyl - 2 - yl) methyl) piperazin-1-yl) - 2 - (3 - ((dimethylamino) methyl) phenoxy) - N - (3 - ((4 - (nitro - tetrahydro - 2H - piran - 4 - ylmethyl) sulfonyl) amino) phenyl) benzamide 2 - (3 - (Acetylamino) phenoxy) - 4 - ((4 - (4 - Chloro - 1,1 - biphenyl - 2 - yl) methyl) piperazin-1-yl) - N - (3 - (4 - nitro - (tetrah Idro - 2H - piran - 4 - ylmethyl) sulfonyl) amino) phenyl) benzamide among others.These compounds inhibit the activity of anti apoptotic Proteins bcl-2 being useful in the treatment of bladder cancer, Lymphoblastic Leukemia, melanomaSE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (I) DONDE A1 ES C(A2) O N, EN DONDE A2 ES H, NHC(O)NH2, SO2NH2, ENTRE OTROS B1 ES H, C(O)NHNOH, C(NH)NH2, CN, ENTRE OTROS D1 ES H, SO2NH2, CF3, C(O)OH, ENTRE OTROS E1 ES H, C(NH)NH2, F, CN, ENTRE OTROS Y1 ES H, NO2, CN, OCF3, ENTRE OTROS Z1 ES R26 O R27, EN DONDE R26 ES FENILENO NO FUSIONADO O FUSIONADO CON BENCENO, ENTRE OTROS R27 ES HETEROARILENO NO FUSIONADO O FUSIONADO CON BENCENO, ENTRE OTROS Z2 ES R28, R29, ENTRE OTROS, EN D
