申请人:——
公开号:US20020058630A1
公开(公告)日:2002-05-16
Described herein are compounds that are useful as caspase inhibitors having the formula:
1
wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R
1
is hydrogen, CN, CHN
2
, R, or CH
2
Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, or an aralkyl group; Y is an electronegative leaving group; R
2
is CO
2
H, CH
2
CO
2
H, or esters, amides or isosteres thereof; and R
3
is hydrogen, an optionally substituted aryl group, an optionally substituted aralkyl group, or an optionally substituted C
1-6
aliphatic group, R
4
is an optionally substituted group selected from an aryl group or a heterocyclyl group, or R
3
and R
4
taken together with the nitrogen to which they are attached optionally form a substituted or unsubstituted monocyclic, bicyclic or tricyclic ring.
本文描述了作为caspase抑制剂有用的化合物,其化学式如下:其中环A是一个可选择取代的哌啶、四氢喹啉或四氢异喹啉环;R1是氢、CN、CHN2、R或CH2Y;R是从脂肪族群、芳香族群或芳基烷基群中选择的可选择取代的群;Y是电负离去基团;R2是CO2H、CH2CO2H或其酯、酰胺或同分异构体;R3是氢、一个可选择取代的芳基群、一个可选择取代的芳基烷基群或一个可选择取代的C1-6脂肪族群,R4是从芳基群或杂环基团中选择的可选择取代的群,或R3和R4连同它们附着的氮可选择形成一个取代或未取代的单环、双环或三环。