THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH
发明人:
LESSENE, GUILLAUME LAURENT,BAELL, JONATHAN
申请号:
CA2570213
公开号:
CA2570213C
申请日:
2005.07.01
申请国别(地区):
CA
年份:
2014
代理人:
摘要:
Compounds of formula (l):(see formula I)whereinR1 is selected from the group consisting of CO2H and a carboxylic acidor carboxylate bioisostere;R2 is selected from the group consisting of an amino acid side chainand a groupR a-(CHR')x-A-(CH2)y-; andR3 is selected from the group consisting of C1-6alkyl, C2-6alkenyl,C2-6alkynyl, cycloalkyl, cycloalkenyl, aryl, heterocyclyl, heteroaryl and agroupR d-(CH2)p-W-(CH2)q-;and wherein R4, R5, R a, R1 , A, R d, W, n, m, x, y, p and q are as definedherein;and pharmaceutically acceptable salts and prodrugs thereof; aredisclosed herein. Further disclosed are conjugates and compositions comprisingsuch compounds, and uses thereof for regulating cell death, or treatment orprophylaxis of a pro-survival Bcl-2 family member mediated disease orcondition.