COHEN, FREDERICK,DESHAYES, KURT,KOEHLER, MICHAEL F. T.,WANG, LAN,INDUBAKU, CHUDI,FLYGARE, JOHN A.,GAZZARD, LEWIS J.
申请号：
PE0018052012
公开号：
PE01502013A1
申请日:
2008.04.29
申请国别(地区):
PE
年份:
2013
代理人:
摘要：
Refers to a compound of formula M - U1 U2, where U1 and U2 have the formula (i) wherein: x1 and x2 are independently o or s R2 is alkyl C1 - 10, carbociclo, carbociclilalquilo, heterociclilalquilo heterocycle or optionally substituted with nitro, amino, Oxo,Among others R3 is H or alkyl, optionally substituted by Halogen C1 - 10 or hydroxyl R3 and R4 are three to six members Heterocycles r3\u00b4 is H r3\u00b4 form a carbociclo R3 and R4 3 to 6 members and r4\u00b4 are independently h, amino, hydroxyl, carbociclo R5 is H, among others alkyl or C1 - 10 M is a Linker Group covalently attached U1 and U2 G Is (VAT), (IVB), among others, where R1 is H,Alkyl Oh or C1 - 10 r5\u00b4 is H or alkyl of C1 - 10 and R6 are independently r6\u00b4 C1 - 10 h, alkyl, aryl or Heterocyclic aralquilo A1 is 5 members with 1 to 4 hetero optionally substituted with hydroxyl, amino, mercapto, among others l is a Link, - C (x3) -, - C or - (x3), among others X3 is or Or s and is a Link, or s, among others r9\u00b4 is Q1 and Q2, Q1 and Q2 are independently h, alkyl,Among others, this Compound is an inhibitor of Apoptosis Protein (IAP) being useful in the treatment of malignanciesSE REFIERE A UN COMPUESTO DE FORMULA U1-M-U2, DONDE U1 Y U2 TIENEN LA FORMULA (I) DONDE: X1 Y X2 SON INDEPENDIENTEMENTE O O S R2 ES ALQUILO C1-10, CARBOCICLO, CARBOCICLILALQUILO, HETEROCICLO O HETEROCICLILALQUILO, OPCIONALMENTE SUSTITUIDO CON NITRO, AMINO, OXO, ENTRE OTROS R3 ES H O ALQUILO C1-10 OPCIONALMENTE SUSTITUIDO POR HALOGENO O HIDROXILO R3 Y R4 FORMAN HETEROCICLO DE 3 A 6 MIEMBROS R3´ ES H R3 Y R3´ FORMAN UN CARBOCICLO DE 3 A 6 MIEMBROS R4 Y R4´ SON INDEPENDIENTEMENTE H, AMINO, HIDROXILO, CARBOCICLO, ENTRE OTROS R5 ES H O ALQUILO C1-10 M ES UN GRUPO ENLAZADOR QUE UNE COVALENTEMENTE U1 Y U2 G ES (IVa), (IVb), ENTRE OTROS, DONDE R1 ES H, OH O ALQUILO C1-10 R5´ ES H O ALQUILO C1-10 R6 Y R6´ SON INDEPENDIENTEMENTE H, ALQUILO C1-10, ARILO O ARALQUILO A1 ES HETEROCICLO DE 5 MIEMBROS CON 1 A 4 HETEROATOMOS OPCIONAL
