Quinoline derivatives as caspase-3 inhibitor, preparation for producing the same and pharmaceutical composition comprising the same
申请人:——
公开号:US20040260094A1
公开(公告)日:2004-12-23
The present invention relates to new quinoline derivatives of formula (1) or their pharmaceutically acceptable salts with caspase-3 inhibitory activity and their preparation methods, wherein R
2
is H; halogen; C
1-6
alkyl; C
1-6
alkoxy; C
1-6
alkoxyalkyl; or C
3-6
cycloalkyl; R
1
is formula (a); —CN; or formula (b); R is H; C
6-14
aryl unsubstituted or substituted by halogen, C
1-6
alkyl, C
1-6
alkoxy or amino; 5-15 membered heterocyclic group unsubstituted or substituted by halogen, C
1-6
alkyl, C
1-6
alkoxy or amino; or —(CH
2
)
n
—CHR
4
R
5
. The present invention relates to a pharmaceutical composition for treating caspase-associated diseases by inhibiting the activity of caspase-3 which comprises the compound of formula (1) or its pharmaceutically acceptable salt.
1
本发明涉及式(1)的新喹啉衍生物或其药学上可接受的盐,具有caspase-3抑制活性及其制备方法,其中R2为H; 卤素; C1-6烷基; C1-6烷氧基; C1-6烷氧基烷基; 或C3-6环烷基; R1为式(a); —CN; 或式(b); R为H; C6-14芳基未取代或取代卤素,C1-6烷基,C1-6烷氧基或氨基; 5-15成员的杂环基未取代或取代卤素,C1-6烷基,C1-6烷氧基或氨基; 或—(CH2)n—CHR4R5。本发明涉及一种用于通过抑制caspase-3活性治疗caspase相关疾病的制剂,包括式(1)的化合物或其药学上可接受的盐。