COHEN, FREDERICK,DESHAYES, KURT,FAIRBROTHER, WAYNE J,FENG, BAINIAN,FLYGARE, JOHN,GAZZARD, LEWIS J,TSUI, VICKIE HSIAO-WEI
申请号：
NZ58879905
公开号：
NZ588799A
申请日:
2005.07.05
申请国别(地区):
NZ
年份:
2012
代理人:
摘要：
Disclosed are heterocyclic amide derivatives of proline peptides, as represented by the general formula (I), wherein: X1, X2 and X3 are independently O or S； Y is (CHR7)n, O or S； wherein n is 1 or 2 and R7 is H, halogen, alkyl, aryl, aralkyl, amino, arylamino, alkylamino, aralkylamino, alkoxy, aryloxy or aralkyloxy； A is an optionally substituted 5-membered heterocycle； R1 is H or R1 and R2 together form a 5-8 member ring； R2 is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, a heterocycle or heterocyclylalkyl, each optionally substituted with hydroxyl, mercapto, halogen, amino, carboxyl, alkyl, haloalkyl, alkoxy or alkylthio； R3 is H or alkyl； R4 and R4' are independently H, hydroxyl, amino, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, or heteroarylalkyl wherein each alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl and heteroarylalkyl is optionally substituted； R5 and R5' are each independently H or alkyl； R6 and R6' are each independently H, alkyl, aryl or aralkyl； and salts and solvates thereof. Further disclosed is a pharmaceutical composition which comprises a compound as defined above and a carrier, diluent or excipient for the treatment of cancer and / or for inducing apoptosis in a cell.
