BRUNCKO MILAN,YUJIA DAI,DING HONG,DOHERTY GEORGE ANDREW,ELMORE STEVEN W.,HASVOLD LISA A,HEXAMER LAURA,KUNZER AARON R.,MANTEI ROBERT A,MCCLELLAN WILLIAM J.,CHANG H. PARK,PARK CHEOL-MIN,ANDREW M. PETROS
申请号：
CO11075973
公开号：
CO6382143A2
申请日:
2011.06.17
申请国别(地区):
CO
年份:
2012
代理人:
摘要：
Compounds of formula I which inhibit the activity of anti apoptotic Protein bcl-2, where A1 is n or C (A2)； B1 is H, R1, OR1, SR1, S (OR) R1 is H, among others； D1, R1, OR1, SR1, S (OR) R1, so2r1 among others； E1 is H, R1, OR1, SR1, S (OR) so2r1 R1, R1, C (OR), among others； y1 is H, CN, NO2, C (o) o F, Ci , BR, I, among others； Z1 or Z2 is R27 is R26, R28,R29, R30； Z1A panel rc-z2a and both are absent or are taken together to form ch2ch2 or CH2, z12a； z12a is C2 - C6 alquileno with one or two CH2 units replaced by NH (CH3), N, S, S (OR) or SO2； L1 is a or37 sr37 R37,,, S (or so2r37 R37), C (OR) R37, CO (OR) R37, OC (OC) or37 R37, (OR), nhr37, C (o) NH. C (or nr37 (c), or Nhor37), C (o) nhso2r37, so2nh, so2nhr37 NH (n, c), C (n) and nhr37； Z3 is R38, R39 and R40.Furthermore, this Invention includes compositions containing such compounds and Methods of treatment of diseases during the course there is expression of the anti apoptotic Protein Bcl - 2.Compuestos de Fórmula I que inhiben la actividad de proteínas anti-apoptóticas Bcl-2,en donde A1 es N o C(A2)； B1 es H, R1, OR1, SR1, S(O)R1, entre otros； D1 es H, R1, OR1, SR1, S(O)R1, SO2R1, entre otros； E1 es H, R1, OR1, SR1, S(O)R1, SO2R1, C(O)R1, entre otros； Y1 es H, CN, NO2, C(O)OH, F, CI, Br, I, entre otros； Z1 es R26 o R27； Z2 es R28, R29 o R30； Z1A y Z2A están ambos ausentes o se toman juntos para formar CH2, CH2CH2 o Z12A； Z12A es C2-C6-alquileno con una o dos unidades CH2 reemplazadas por NH, N(CH3), S, S(O) o SO2； L1 es un R37, OR37, SR37, S(O)R37, SO2R37, C(O)R37, CO(O)R37, OC(O)R37, OC(O)OR37, NHR37, C(O)NH, C(O)NR37, C(O)NHOR37, C(O)NHSO2R37, SO2NH, SO2NHR37, C(N)NH, C(N)NHR37； y Z3 es R38, R39 o R40. Además, esta invención comprende las composiciones que contienen dichos compuestos y métodos de tratamiento de enfermedades durante cuyo transcurso hay expresión de la proteína anti-apoptótica BcI-2.
