TAO, ZHI-FU,WANG, XILU,SOUERS, ANDREW J.,CATRON, NATHANIEL D.,SULLIVAN, GERARD
申请号：
PE0022192012
公开号：
PE02212013A1
申请日:
2011.05.25
申请国别(地区):
PE
年份:
2013
代理人:
摘要：
Refers to compounds of formula (i), (ii) or (iii), where A1 is n or C (A2), A2 is H, CN, NO2, Oh, among others B1 is H, C (o) h, CH (noch3), NF3, C (o) Oh among others D1 is H, C (NH) NH2, CN, NO2, C (o) NH2, among others E1 is H, C (o) h, chnoh, CH (noch3), among others y1 is C (o) Oh, ocf3, cf2cf3, NH2, C ( (o) NH2, among others G1 is r1b, or1b, r1b is R2, or nhr1bAmong other phenyl, R2 is not merged or merged with Benzene, heteroareno, cicloalcano or cycloalkyl or cicloalquenilo is heterocicloalcano R30.A Preferred Compound is: diacid phosphate (5 - (5 - (4 - [2 - (4-chlorophenyl) - 4.4 - dimetilciclohex - 1 - 1 - il] methyl} piperazin-1-yl) - {[2 - (3 - [4 - (nitro - tetrahydro - 2H Piran - 4 - methyl) amino] phenyl] sulfonyl) Carbamoyl] phenoxy) - 7h pyrrolo [2,3-b] pyridin - 7 - yl) methyl among others. Also referred to a Pharmaceutical composition. These compounds inhibit the activity of the anti apoptotic Proteins bcl-2SE REFIERE A COMPUESTOS DE FORMULAS (I), (II) O (III), DONDE: A1 ES N O C(A2), A2 ES H, CN, NO2, OH, ENTRE OTROS B1 ES H, C(O)H, CH(NOCH3), CF3, C(O)OH, ENTRE OTROS D1 ES H, C(NH)NH2, CN, NO2, C(O)NH2, ENTRE OTROS E1 ES H, C(O)H, CHNOH, CH(NOCH3), ENTRE OTROS Y1 ES C(O)OH, OCF3, CF2CF3, NH2, C(O)NH2, ENTRE OTROS G1 ES R1B, OR1B, O NHR1B R1B ES R2, ENTRE OTROS R2 ES FENILO NO FUSIONADO O FUSIONADO CON BENCENO, HETEROARENO, CICLOALCANO O HETEROCICLOALCANO R30 ES CICLOALQUILO O CICLOALQUENILO. UN COMPUESTO PREFERIDO ES: FOSFATO DIACIDO DE (5-{5-(4-{[2-(4-CLOROFENIL)-4,4-DIMETILCICLOHEX-1-EN-1-IL]METIL}PIPERAZIN-1-IL)-2-[({3-NITRO-4-[(TETRAHIDRO-2H-PIRAN-4-ILMETIL)AMINO]FENIL}SULFONIL)CARBAMOIL]FENOXI}-7H-PIRROLO[2,3-b]PIRIDIN-7-IL)METILO ENTRE OTROS. REFERIDO ADEMAS UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA ACTIVIDAD DE LAS PROTEINAS ANTI-APOPTOTICAS Bcl-2
