BRUNCKO, MILAN,DING, HONG,DOHERTY, GEORGE,ELMORE, STEVEN,HASVOLD, LISA,HEXAMER, LAURA,KUNZER, AARON R.,SONG, XIAOHONG,SOUERS, ANDREW J.,SULLIVAN, GERARD,TAO, ZHI-FU,WANG, GARY T.,WANG, LE,WANG, XILU,W
申请号：
PE0020252011
公开号：
PE03452012A1
申请日:
2010.05.26
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 n or C (A2), where A2 is H, F, CN, NO2, among others B1 is H, NHC (NH2), so2nh2, among others D1 is H, C (o) nhnoh, CN, among others so2nh2 E1 is H, Oh, CF3, among others y1 is H, CN, NO2, ocf3, among others G1 is H or C (o) or R2 Z1 is 6, among others Z2 is R28, among others.Where R26, R28 are each sulfide Z1A panel rc-z2a and are absent or are taken together to form ch2ch2 CH2, among others L1 is C (o) NH, so2nh, among others Z3 is R38, among others, where R38 is phenyl or not cicloalcano merged with Benzene, among others.Preferred compounds are: 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) - 2 - (1h pyrrolo [2,3-b] pyridin - 5 - iloxi) benzamide 4 - (4 - [2 - (4-chlorophenyl) - 4.4 - dimetilciclohex - 1 - 1 - il] methyl} piperazin-1-yl) - N - (4 - [4 - ({metilpiperazin - 1 - il) amino] - 3-nitrophenyl] sulfonyl) - 2 - (1h pyrrolo [2,3-b] pyridin - 5 - iloxi) benzamide among others.It also relates to a Pharmaceutical composition. These compounds are inhibitors of the activity of the anti apoptotic Proteins bcl-2 being useful in the treatment of cancerSE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (I) DONDE A1 ES N O C(A2), EN DONDE A2 ES H, F, CN, NO2, ENTRE OTROS B1 ES H, NHC(O)NH2, SO2NH2, ENTRE OTROS D1 ES H, C(O)NHNOH, CN, ENTRE OTROS E1 ES H, SO2NH2, OH, CF3, ENTRE OTROS Y1 ES H, CN, NO2, OCF3, ENTRE OTROS G1 ES H O C(O)O Z1 ES R26, ENTRE OTROS Z2 ES R28, ENTRE OTROS, EN DONDE R26 Y R28 SON CADA UNO FENILENO Z1A Y Z2A ESTAN AUSENTES O SE TOMAN JUNTOS PARA FORMAR CH2, CH2CH2, ENTRE OTROS L1 ES C(O)NH, SO2NH, ENTRE OTROS Z3 ES R38, ENTRE OTROS, EN DONDE R38 ES FENILO FUSIONADO O NO CON BENCENO, CICLOALCANO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 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)-2-(1H-PIRROLO[2,3
