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：
PE2011002025
公开号：
PE20120345A1
申请日:
2010.05.26
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
It refers to non bicycle formula compound (I), where A1 is n or C (A2),WHERE A2 IS H, F, CN, NO2, AMONG OTHERS； B1 IS H, NHC (O) NH2, SO2NH2, AMONG OTHERS； D1 IS H, C (O) NHNOH, CN, AMONG OTHERS； E1 IS H, SO2NH2, OH, CF3, AMONG OTHERS； Y1 IS H, CN, NO2, OCF3, AMONG OTHERS； G1 ES H O C (O) O； Z1 IS R26, AMONG OTHERS； Z2 IS R28, AMONG OTHERS, WHERE R26 AND R28 ARE EACH PHENYLENE； Z1A AND Z2A ARE ABSENT OR TAKEN TOGETHER TO FORM CH2, CH2CH2, AMONG OTHERS； L1 IS C (O) NH, SO2NH, AMONG OTHERS； Z3 IS R38, AMONG OTHERS, WHERE R38 IS FENILE FUSED OR NOT WITH BENZENE, CYCLOALCAN,AMONG OTHERS. THEY ARE PREFERRED COMPOUNDS: 4- {4 - [(4'-CHLORINE-1,1'-BIPHENYL-2-IL) METHYL] PIPERAZIN-1-IL} -N - ({3-NITRO-4 - [(TETRAHYDRO- 2H-PIRAN-4-ILMETIL) AMINO] FENIL} SULFONIL) -2- (1H-PIRROLO [2,3-b] PIRIDIN-5-ILOXI) BENZAMIDE； 4- (4 - {[2- (4-CHLOROPHENYL) -4,4-DIMETILCICLOHEX-1-EN-1-IL] METHYL} PIPERAZIN-1-IL) -N - ({4 - [(4-METHYLPIPERAZIN- 1-IL) AMINO] -3-NITROFENIL} SULFONIL) -2- (1H-PIRROLO [2,3-b] PIRIDIN-5-ILOXI) BENZAMIDE； AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE INHIBITORS OF THE ACTIVITY OF 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-b]PIRIDIN-5-ILOXI)BENZAMIDA； 4
