COHEN, FREDERICK,TSUI, VICKIE HSIAO-WEI,LY, CUONG,FLYGARE, JOHN A
申请号：
NZ58967005
公开号：
NZ589670A
申请日:
2005.12.19
申请国别(地区):
NZ
年份:
2013
代理人:
摘要：
589670 Disclosed are 2-(thiazolyl)pyrrolidine, 2-(oxazolyl)pyrrolidine and 2-(imidazolyl)pyrrolidine peptide derivatives as represented by the general formula (I), wherein: Q is alkyl, a carbocycle or a heterocycle wherein alkyl, carbocycle and heterocycle are each optionally substituted with one or more hydroxyl, alkoxy, acyl, halogen, mercapto, oxo, carboxyl, alkyl, amino, cyano, nitro, amidino, guanidino, an optionally substituted carbocycle or an optionally substituted heterocycle wherein one or more CH2 groups of the alkyl substituent on Q is optionally replaced with -O-, -S-, -S(O)-, S(O)2, -N(R8)-, -C(O)-, -C(O)-NR8-, -NR8-C(O)-, -SO2-NR8-, -NR8-SO2-, -NR8-C(O)-NR8-, -NR8-C(NH)-NR8-, -NR8-C(NH)-, -C(O)-O- or -O-C(O)- X1 and X2 are each independently O or S Y is CH2 R1 is H or R1 and R2 together form a 5-8 member ring R2 is alkyl, a carbocycle, carbocyclylalkyl, a heterocycle or heterocyclylalkyl, each optionally substituted with halogen, hydroxyl, oxo, thione, mercapto, carboxyl, alkyl, haloallcyl, alkoxy, alkylthio, sulfonyl, amino or nitro R3 is H or alkyl optionally substituted with halogen or R3 and R4 together form a 3-6 member heterocycle R3 is H or methyl, or R3 and R3 together form a 3-6 member carbocycle R4 is H and R4 is H, alkyl, aryl, aralkyl, cycloalkyl, benzyloxycarbonyl, heteroaryl, or heterocycloalkyl, wherein said alkyl is optionally substituted with imino or heteroaryl R5 is H or alkyl R6 and R6 are each independently H, alkyl, aryl or aralkyl and wherein the remaining substituents are as defined herein. Further disclosed is a pharmaceutical composition which comprises a compound as defined above and a carrier, diluent or excipient for inducing apoptosis in a cell, and for the treatment of cancer.
